INN: Gestodene, Ethinylestradiol
Manufacturer: Gedeon Richter JSC
Anatomical-therapeutic-chemical classification: Gestodene and estrogen
Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 014071
Registration period: 03.06.2014 - 03.06.2019
Instruction
Tradename
Lindinet 30
International non-proprietary name
Dosage form
Coated tablets
Compound
One tablet contains
active substances: ethinylestradiol 0.03 mg,
gestodene 0.075 mg,
Excipients: sodium calcium edetate, magnesium stearate, colloidal anhydrous silica, povidone, corn starch, lactose monohydrate,
shell composition: quinoline yellow (E 104), povidone, titanium dioxide (E 171), macrogol 6000, talc, calcium carbonate, sucrose
Description
Tablets, round, biconvex, film-coated yellow color(for Lindinet 30).
Pharmacotherapeutic group
Sex hormones and modulators of the reproductive system. Hormonal contraceptives for systemic use. Progestogens and estrogens (fixed combinations). Gestodene and estrogen
ATX code G03AA10
Pharmacological properties
Pharmacokinetics
Gestodene
Suction
After oral administration, gestodene is rapidly and completely absorbed. Peak plasma concentration after a single dose is reached after approximately 1 hour and is approximately 2-4 ng / ml. Bioavailability is about 99%.
Distribution
Gestodene binds to serum albumin and sex hormone-binding globulin (SHBG). Only 1-2% of the total concentration of the substance in the blood serum is in the form of a free steroid, and 50-75% is specifically associated with SHBG. The ethinylestradiol-induced increase in SHBG levels affects the amount of gestodene associated with serum protein, which causes an increase in the fraction of gestodene associated with SHBG and a decrease in the fraction associated with albumin. The apparent volume of distribution of gestodene is 0.7-1.4 l/kg.
Metabolism
Gestodene is completely metabolized through known pathways of steroid hormone metabolism.
The average rate of metabolic clearance from blood plasma is 0.8-1.0 ml / min / kg.
breeding
Serum gestodene levels undergo a biphasic decrease. The half-life in the terminal phase is 12-20 hours. Gestodene is excreted in the urine and bile only in the form of metabolites in a ratio of 6:4. The half-life of metabolites is approximately 1 day.
Equilibrium concentration
The pharmacokinetics of gestodene is affected by the level of SHBG, which increases approximately three times while taking ethinyl estradiol. After daily administration, the level of gestodene in the blood serum increases approximately three to four times, reaching an equilibrium concentration in the second half of the course of taking the drug.
Ethinylestradiol
Suction
After oral administration, ethinylestradiol is rapidly and completely absorbed. Peak plasma concentration is reached after approximately 1-2 hours and is approximately 30-80 pg/ml. Absolute bioavailability as a result of presystemic conjugation and the effect of "first pass" through the liver is approximately 60%.
Distribution
Ethinylestradiol binds strongly but non-specifically to serum albumin (approximately 98.5%) resulting in increase in serum SHBG concentration. The apparent volume of distribution of gestodene is 5-18 l/kg.
Metabolism
Ethinylestradiol is metabolized mainly by aromatic hydroxylation, however, this forms a large number of hydroxylated and methylated metabolites, including both free metabolites and conjugates with glucuronides and sulfates. The metabolic clearance rate is approximately 5-13 ml/min/kg.
breeding
Serum ethinyl estradiol levels undergo a biphasic decline, with a terminal half-life of approximately 16-24 hours. It is excreted only in the form of metabolites, the ratio between urine and bile is 2:3. The half-life of metabolites is approximately 1 day.
Equilibrium concentration
The equilibrium concentration is reached after 3-4 days, during which time the level of ethinylestradiol in serum increases by 20% compared with the level after taking a single dose.
Pharmacodynamics
The action of combined oral contraceptives (COCs) is due to the suppression of the production of gonadotropic hormones. Although the main mechanism of action is the suppression of ovulation, other mechanisms of action, including changes in the condition of the cervical mucus (which makes it difficult for sperm to enter the uterus) and the endometrium (which reduces the likelihood of implantation), also have a contraceptive effect.
In addition to the contraceptive effect, they have a number of other positive effects.
Effect on the menstrual cycle:
Regulate the menstrual cycle, reduce the loss of blood and iron during menstruation, reduce the incidence of dysmenorrhea.
Actions, associated with inhibition of ovulation:
Reduce the incidence of functional ovarian cysts and ectopic pregnancy.
Other actions
They reduce the frequency of development of fibroadenomas and fibrous cysts of the mammary glands, infections of the pelvic organs, endometrial cancer, and improve the condition of the skin with acne.
Indications for use
oral contraception
Dosage and administration
One tablet should be taken daily (preferably at the same time of day) for 21 days. Taking the tablets from the next pack should be started after a 7-day break, during which withdrawal bleeding should begin. Bleeding usually starts on the 2nd or 3rd day after the last pill and may not end before the next pack starts.
Taking Lindinet 30 for the first time
The first tablet of Lindinet 30 should be taken on the first day of the menstrual cycle.
You can also start taking the pills from days 2 to 5 of your period, but in this case you need to use additional non-hormonal contraceptive measures during the first seven days of taking the pills during the first cycle.
Switching from another combined oral contraceptive
The first tablet of Lindinet 30 should be taken the next day after taking the last active (hormonal) tablet from the previous pack of oral contraceptives, but no later than the next day after taking regular pills (or taking placebo pills) from the previous pack of oral contraceptives.
Switching from progestogen-containing drugs (“mini-pill”, injections, implant, IUD)
The transition from taking the "mini-pill" to taking Lindinet 30 can be made on any day of the menstrual cycle (from the implant and intrauterine device - on the day of their removal, from injections - on the day when the next injection is to be made). In these cases, additional contraceptive measures must be used during the first 7 days of taking the tablets.
After an abortion in the 1st trimester
Oral contraceptives can be started immediately after a first trimester abortion. Additional measures contraception is not required.
After childbirth or abortion in the 2nd trimester
Women who are not breastfeeding may start taking oral contraceptives 21-28 days after vaginal delivery or after a 2nd trimester abortion. With a later start of taking oral contraceptives during the first 7 days, barrier methods of contraception should be used as additional measures.
If sexual intercourse has already taken place, the presence of pregnancy should be excluded before taking the tablets, or the drug should be postponed until the start of the first menstrual bleeding.
Missed pills
If the tablet was not taken on time, it should be taken as soon as possible. If the missed tablet was taken within 12 hours after the usual time of taking it, the contraceptive effect of the drug does not decrease, and additional contraceptive measures are not required. Subsequent tablets should be taken at the usual time.
If the delay in taking the pill exceeds 12 hours, the contraceptive effect may be reduced. The woman should take the missed tablet as soon as she remembers, even if she has to take 2 tablets at the same time. From now on, the woman should take the tablets at the usual time. Additional contraceptive measures are required for the next 7 days of taking the tablets. If there are less than 7 tablets left in the current pack, the woman should start taking the pills from the next pack immediately after taking the last pill from the current pack: this means that there will be no break between taking the pills from two packs. In this case, withdrawal bleeding should not be expected until the pills from the second pack are finished, but spotting or breakthrough bleeding may develop.
If after the end of taking the pills from the second pack, withdrawal bleeding does not develop, then pregnancy must be excluded before taking the pills from the next pack.
Measures to be taken in case of vomiting
If vomiting occurs within 3-4 hours after taking the tablet, absorption of the tablet may not be complete. In such cases, the precautions described above for missed tablets should be taken. If a woman does not want to change her usual pill regimen, she should take the necessary additional pills from another package.
Accelerating the onset of menstruation or delaying menstruation
In order for menstrual bleeding to start earlier than usual when taking the pills, it is recommended to shorten the interval between taking the pills by the desired number of days. The shorter the break, the higher the risk of breakthrough bleeding or spotting when taking pills from the second pack (as in the case of delayed menstrual bleeding).
To delay the onset of menstrual bleeding, start taking the pills new packaging immediately after the tablets from the current package run out, without leaving a break between them. Menstruation can be delayed as long as required until all the pills from the second package run out. When taking the tablets from the second pack, breakthrough bleeding or spotting may occur. Regular intake of Lindinet 30 can be resumed after the usual 7-day break.
Side effects
Very common (≥/10)
Breakthrough bleeding, spotting between periods
Often (≥1/100 to<1/10)
Headache, dizziness, migraine
Mood changes, depression, nervousness, irritability, decreased or increased libido
Fluid retention
Vulvaginal candidiasis
Nausea, vomiting, abdominal pain
Soreness and engorgement of the mammary glands
Weight loss/increase
Uncommon (≥1/1000 to<1/100)
Decreased/increased appetite
Mammary cancer
Arterial hypertension
Chloasma, melasma
Rare (≥1/10000 to<1/1000)
Anaphylactic reactions
Impaired glucose tolerance, hyperlipidemia, hypertriglyceridemia
contact lens intolerance
Otosclerosis
thrombosis, embolism
Very pcaustically<1/1000 0 )
Gallbladder disease, cholelithiasis, pancreatitis, hepatocellular carcinoma, liver adenoma
Exacerbations of systemic lupus erythematosus
Exacerbation of chorea, optic neuritis
Stroke, myocardial infarction
Thrombosis of the retinal artery
Hemolytic uremic syndrome
The use of oral contraceptives is associated with an increased risk of developing the following conditions:
Arterial and venous thrombotic and thromboembolic complications, including myocardial infarction, stroke, venous thrombosis and pulmonary embolism.
Cervical intraepithelial neoplasia and cervical cancer
Mammary cancer
Optic neuritis can lead to partial or complete loss of vision. The use of COCs can exacerbate existing gallbladder disease and accelerate disease progression in previously asymptomatic women.
Contraindications
- hypersensitivity to the components of the drug
Pregnancy or suspicion of it
Vaginal bleeding of unknown etiology
Current or history of arterial or venous thrombosis
Serious risk factors for thrombosis or embolism (blood clotting disorders, valvular heart disease, and atrial fibrillation)
History of prodromal symptoms of thrombosis (eg, transient cerebral ischemic attack, angina pectoris)
Cardiovascular disorders (pathology of the valve (s) of the heart, arrhythmias)
Severe arterial hypertension
History of liver tumors (benign or malignant)
Serious liver disease, before normalization of parameters of liver function tests
Diagnosed or suspected breast cancer
Diagnosed or suspected endometrial malignancies or other estrogen-dependent neoplasms
Vascular ophthalmopathy
History of herpes in pregnancy
sickle cell anemia
Hyperlipidemia
Diabetes complicated by angiopathy
Migraine with focal neurological symptoms
Children and adolescents up to 18 years of age
Hereditary fructose intolerance, Lapp-lactase deficiency, glucose-galactose malabsorption
Drug Interactions
Interaction between ethinylestradiol and concomitantly used drugs can lead to an increase or decrease in plasma levels of ethinylestradiol.
A decrease in the level of ethinylestradiol in plasma can lead to an increase in the number of breakthrough bleeding and menstrual irregularities, sometimes there is also a decrease in the contraceptive effect of Lindinet 30. Therefore, in the case of simultaneous use of ethinylestradiol and drugs that reduce the level of ethinylestradiol in plasma, in addition to taking Lindinet 30, it is recommended to use non-hormonal methods of contraception (eg, condoms, spermicides). In the event that long-term use of preparations containing such active substances is necessary, it is necessary to consider the possibility of abandoning the use of hormonal contraceptives as the main method of contraception.
After stopping the use of drugs that reduce the concentration of ethinylestradiol in the blood, it is recommended to use additional non-hormonal methods of contraception for at least 7 days. After stopping the use of drugs that can cause the induction of microsomal liver enzymes and lead to a decrease in the concentration of ethinylestradiol in the blood serum, it is recommended to use additional non-hormonal methods of contraception for a longer period. Sometimes, depending on the dose, duration of treatment, and the rate of elimination of the enzyme-inducing drug, it may take weeks before the induction of liver enzymes stops completely.
Active substances that can reduce the concentration of ethinylestradiol in the blood serum:
Any active substance that reduces transit time through the gastrointestinal tract, and therefore reduces absorption;
Substances that induce liver microsomal enzymes, such as rifampicin, rifabutin, barbiturates, primidone, phenylbutazone, phenytoin, dexamethasone, griseofulvin, topiramate, certain protease inhibitors, and modafinil;
Hypericum perforatum (St. John's wort) and ritonavir (due to its ability to induce microsomal liver enzymes);
Some antibiotics (eg, ampicillin and other penicillins, tetracyclines) because they reduce hepatic estrogen recirculation.
Active substances that can increase the concentration of ethinylestradiol in the blood serum:
Atorvastatin;
Drugs that also undergo sulfation in the gastrointestinal wall, such as ascorbic acid (vitamin C) and paracetamol;
Substances that inhibit cytochrome P 450 3A4 isoenzymes, for example, indinavir, fluconazole, troleandomycin.
Troleandomycin, when used together with oral contraceptives, may increase the risk of intrahepatic cholestasis.
Ethinylestradiol may interfere with the metabolism of other drugs by inhibiting hepatic microsomal enzymes or by causing hepatic drug conjugation, in particular glucuronidation. Thus, plasma and tissue concentrations of other drugs may increase (eg, ciclosporin, theophylline, corticosteroids) or decrease. When prescribing any drugs, information on their combined use should be taken into account in order to establish possible interaction reactions.
Changes in laboratory results
The use of oral contraceptives may affect the results of some laboratory tests, including tests of liver, thyroid, adrenal, kidney function, levels of lipoproteins and carrier proteins, as well as parameters of carbohydrate metabolism, coagulation and fibrinolysis.
Usually, the changes do not go beyond the reference values and remain within the normal range.
special instructions
Circulatory disorders
The use of contraceptives is associated with an increased risk of myocardial infarction. The risk is higher in women who smoke and have additional risk factors for coronary artery disease, such as hypertension, high cholesterol, morbid obesity, and diabetes.
Smoking increases the risk of serious cardiovascular complications associated with oral contraceptives. The risk increases with age, and in the case of smoking a large number of cigarettes, this risk is quite significant in women over 35 years of age. Women taking oral contraceptives should be advised to stop smoking.
Women with risk factors for the development of cardiovascular disease should be given oral contraceptives with caution.
It has been proven that taking oral contraceptives increases the risk of developing cerebrovascular diseases (ischemic and hemorrhagic stroke).
An increase in blood pressure (BP) has also been reported in women taking oral contraceptives. An increase in blood pressure is usually observed in older women and in those who take oral contraceptives for a long time.
The data obtained show that the incidence of arterial hypertension increases depending on the amount of estrogens.
Women who have previously suffered from hypertension or diseases associated with hypertension or impaired renal function should be advised to use another method of contraception. These women should be closely monitored if they choose to take oral contraceptives. In the event of a significant increase in blood pressure, oral contraceptives should be discontinued.
In most women, elevated blood pressure normalizes after discontinuation of oral contraceptives, there are no differences in the incidence of arterial hypertension between women who have previously used and have not used oral contraceptives.
Venous and arterial thrombosis and thromboembolism
The use of combined oral contraceptives is associated with an increased risk of venous and arterial thrombotic and thromboembolic complications. For any given estrogen/progestogen combination, a dosing regimen should be prescribed that contains the minimum amount of estrogen and progestogen, and at the same time provides a low failure rate and meets the needs of the patient.
Venous thrombosis and thromboembolism
The use of any combined oral contraceptives entails an increased risk of venous thromboembolism (VTE) compared to that without the use of COCs. The additional risk of venous thromboembolism is highest during the very first year of combined oral contraceptive use. This risk is less than the risk of pregnancy-related VTE, which is 60 per 100,000 pregnancies; VTE is fatal in 1-2% of cases.
The incidence of VTE for combined oral contraceptives containing levonorgestrel and less than 50 micrograms of ethinyl estradiol is approximately 20 cases per 100,000 women per year of use. The incidence of VTE for combined oral contraceptives containing gestodene is approximately 30-40 cases per 100,000 women per year of use. The effect of relative risk on the number of additional cases is higher in women during the very first year of using combined oral contraceptives.
Epidemiological studies have not confirmed that women taking combined oral contraceptives containing desogestrel or gestodene and 0.02 mg ethinylestradiol have a lower risk of developing VTE than women taking combined oral contraceptives containing desogestrel or gestodene and 0.03 mg ethinylestradiol.
Risk factors for arterial and/or venous thromboembolism
Age
Smoking (in heavy smokers, the risk increases with age, especially in women over 35)
Hereditary predisposition (for example, arterial or venous thromboembolism in siblings or parents at a relatively young age). If there is a hereditary predisposition, before making a decision on taking oral contraceptives, a woman should be referred to a specialist
Obesity (body mass index over 30 kg/m2)
Dyslipoproteinemia
Arterial hypertension
Heart valve disease
Atrial fibrillation
Prolonged immobilization (since the risk of thromboembolism is increased in the postoperative period, it is recommended to stop taking oral contraceptives at least four weeks before a planned operation and return to taking them no earlier than two weeks after returning to normal physical activity).
Since the period immediately after childbirth is associated with an increased risk of thromboembolism, Lindinet 30 should be started no earlier than 28 days after childbirth or abortion in the second trimester of pregnancy.
Arterial thrombosis and thromboembolism
Lindinet 30 increases the risk of developing arterial thrombotic and thromboembolic complications. The described complications include myocardial infarction and cerebrovascular disorders (ischemic and hemorrhagic stroke, transient ischemic attack). The risk of developing arterial thrombotic and thromboembolic complications is higher in women with additional risk factors.
Lindinet 30 should be used with caution in women with risk factors for thrombotic and thromboembolic complications.
Examples of risk factors contributing to the development of thrombotic and thromboembolic complications:
Smoking
Certain hereditary and acquired thrombophilias
Arterial hypertension
Hyperlipidemia
Obesity
Age
Women who suffer from migraine and take COCs have an increased risk of stroke.
The drug should be stopped immediately if symptoms appear that indicate the development of thrombosis: severe chest pain, which may radiate to the left arm, unusual pain in the leg, swelling of the leg, acute pain during breathing or coughing, sputum with blood.
Biochemical parameters that indicate a hereditary or acquired predisposition to venous or arterial thrombosis include the following: resistance to activated protein C (APC), hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant).
Tumors
Some studies have reported an increased risk of cervical cancer in women taking combined oral contraceptives for a long time, but this information is controversial. Sexual behavior and other risk factors, such as the human papillomavirus (HPV), may also influence the development of cervical cancer.
A meta-analysis of 54 pharmacoepidemiological studies showed that the relative risk of developing breast cancer is slightly higher in women taking combined oral contraceptives (RR = 1.24). This increased risk gradually decreases over 10 years after discontinuation of combined oral contraceptives. However, these studies did not confirm the presence of a causal relationship between the disease and the drug.
In women taking oral contraceptives, breast cancer is diagnosed at an earlier stage than in those who do not use them.
An association has been established between the formation of benign liver tumors and the use of oral contraceptives, although such benign tumors are rare. When these tumors rupture, intraperitoneal bleeding occurs, which can be fatal.
In rare cases, the development of malignant liver tumors has been reported in women who have been taking oral contraceptives for a long time.
In patients with a history of cholestatic jaundice or itching during pregnancy, as well as in patients who have previously taken combined oral contraceptives, the risk of developing the diseases described above is higher. If such patients take Lindinet 30, careful monitoring of their condition is necessary, and if the pathological condition returns, the drug should be discontinued.
Other states
In rare cases, retinal thrombosis has been reported with oral contraceptives. In the event of unexplained partial or complete loss of vision, exophthalmos or diplopia, edema of the optic disc, or damage to the retinal vessels, it is necessary to stop taking oral contraceptives and undergo an additional medical examination.
Previous studies have shown an increased lifetime relative risk of gallbladder disease in women taking oral contraceptives and estrogen-containing products. However, recent studies have shown that the relative risk of developing gallbladder disease may be minimal in women taking low-dose oral contraceptives.
The onset of a migraine, or an increase in migraine attacks, as well as the appearance of a new type of headache, recurring, persistent or very severe, requires discontinuation of oral contraceptives.
You should immediately stop taking Lindinet 30 in case of itching all over the body or epileptic seizures.
Effects on carbohydrate and lipid metabolism
There are reports of impaired glucose tolerance in women taking oral contraceptives. Therefore, you should carefully monitor the condition of women with diabetes and using oral contraceptives.
A small number of women experience persistent hypertriglyceridemia while taking oral contraceptives. With the use of certain progestogen-containing drugs, a decrease in the level of high-density lipoprotein (HDL) has been reported. Since estrogen increases HDL cholesterol levels, the cumulative effect of oral contraceptives on lipid metabolism depends on the ratio between doses of estrogen and progestogen, the type of progestogen, and the absolute amount of progestogen used in the oral contraceptive.
Women suffering from hyperlipidemia should be carefully monitored if they decide to take oral contraceptives.
There are reports that in women with hereditary hyperlipidemia and taking oral contraceptives containing estrogen, there is a significant increase in plasma triglycerides, which can lead to pancreatitis.
Menstrual irregularities
When taking the tablets, especially during the first three months, irregular periods (spotting or breakthrough bleeding) may occur.
If irregular periods persist for a long time or develop after a regular cycle has been established, it should be taken into account that this phenomenon may have a non-hormonal cause. In this case, in order to exclude the possibility of developing a malignant neoplasm or pregnancy, it is necessary to conduct a gynecological examination. If a pathological condition is excluded, the use of other types of oral contraceptives can be recommended.
In some cases, a 7-day break in contraception is not accompanied by bleeding. In cases where the contraceptive was not taken as prescribed, or when there is no bleeding at the end of taking all the pills from the current package, pregnancy should be excluded before continuing to take the contraceptive from the next package.
Precautionary measures
Medical examination and follow-up
Before starting the use of oral contraceptives, you should collect the patient's family and personal history, conduct a general medical and gynecological examination, including blood pressure measurement, laboratory tests, examination of the mammary glands and pelvic organs, and also take a smear from the vagina for cytology; in the future, these procedures should be repeated periodically.
Patients should be advised that this drug does not protect against HIV infection (AIDS) and other sexually transmitted diseases.
liver function
In case of acute or chronic liver dysfunction, it is necessary to stop taking the drug until the liver function tests are normal. In patients with impaired liver function, the metabolism of steroid hormones may be insufficient.
affective disorders
Women who develop severe depression while using oral contraceptives should stop taking the pill. Such women should be advised to use an alternative method of contraception, and an attempt should be made to determine whether these symptoms result from the use of oral contraceptive drugs. You should carefully monitor the condition of women who have suffered from depression before; in the event that attacks of depression resume, you should stop taking the drug for oral contraception.
Folate levels
Serum folate levels may decrease due to the use of oral contraceptives. This may be of clinical importance if a woman becomes pregnant shortly after stopping oral contraceptives.
Chloasma
The appearance of chloasma is especially often observed in women with a history of chloasma during pregnancy. Women who are prone to chloasma should avoid sun exposure and ultraviolet radiation while taking COCs.
Other
In addition to the conditions listed above, increased precautions should be taken in case of otosclerosis, multiple sclerosis, epilepsy, chorea, intermittent porphyria, seizures, renal dysfunction, obesity, systemic lupus erythematosus and uterine fibroids.
Patients with rare hereditary problems such as fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase deficiency should not use this medicine.
Pregnancy and lactation
Before you start taking Lindinet 30, pregnancy should be excluded. If pregnancy occurs during the period of use of the drug, you must immediately stop taking oral contraceptives.
Extensive epidemiological studies have found neither an increased risk of congenital malformations in newborns born to women who took oral contraceptives before pregnancy, nor teratogenic effects (in particular, heart defects and limb abnormalities) in cases where oral contraceptives were inadvertently taken early in pregnancy. pregnancy.
A small amount of the active substance is excreted in breast milk, which can cause side effects in newborns such as jaundice and breast enlargement. During breastfeeding, it is not recommended to take oral contraceptives, as this can lead to a reduction in the amount of breast milk and to a change in its composition.
Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
Given the possibility of developing such side effects as dizziness, visual impairment, care must be taken when driving a vehicle and working with driving mechanisms.
Overdose
Symptoms: nausea, vomiting, slight vaginal bleeding in young girls.
Description of the dosage form
Release form, composition and packaging
Coated tablets light yellow, round, biconvex, both sides without inscriptions; on a break of white or almost white color with a light yellow edging.
Excipients: sodium calcium edetate, magnesium stearate, colloidal silicon dioxide, povidone, corn starch, lactose monohydrate.
Shell composition: quinoline yellow dye (D+S yellow No. 10) (E104), povidone, titanium dioxide, macrogol 6000, talc, calcium carbonate, sucrose.
21 pcs. - blisters (1) - packs of cardboard.
21 pcs. - blisters (3) - packs of cardboard.
Clinical and pharmacological group
Monophasic oral contraceptivepharmachologic effect
Monophasic oral contraceptive. It inhibits the secretion of gonadotropic hormones from the pituitary gland. The contraceptive effect of the drug is associated with several mechanisms. The estrogenic component of the drug is ethinylestradiol, a synthetic analogue of the follicular hormone estradiol, which, together with the corpus luteum hormone, participates in the regulation of the menstrual cycle. The progestogen component is gestodene, a derivative of 19-nortestosterone, which is superior in strength and selectivity of action not only to the natural hormone of the corpus luteum progesterone, but also to other synthetic progestogens (for example, levonorgestrel). Due to its high activity, gestodene is used in low dosages, in which it does not exhibit androgenic properties and has practically no effect on lipid and carbohydrate metabolism.
Along with the indicated central and peripheral mechanisms that prevent the maturation of an egg capable of fertilization, the contraceptive effect is due to a decrease in the susceptibility of the endometrium to the blastocyst, as well as an increase in the viscosity of the mucus in the cervix, which makes it relatively impassable for spermatozoa. In addition to the contraceptive effect, the drug, when taken regularly, also has a therapeutic effect, normalizing the menstrual cycle and helping to prevent the development of a number of gynecological diseases, incl. tumor nature.
Pharmacokinetics
Gestodene
Suction
After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract. After a single dose, Cmax is noted after 1 hour and is 2-4 ng / ml. Bioavailability - about 99%.
Distribution
Gestodene binds to albumin and sex hormone-binding globulin (SHBG). 1-2% is in plasma in free form, 50-75% specifically binds to SHBG. An increase in the level of SHBG in the blood caused by ethinyl estradiol affects the level of gestodene: the fraction associated with SHBG increases and the fraction associated with albumin decreases. Average V d - 0.7-1.4 l / kg. The pharmacokinetics of gestodene depends on the level of SHBG. The concentration of SHBG in the blood plasma under the influence of estradiol increases by 3 times. With daily intake, the concentration of gestodene in the blood plasma increases by 3-4 times and in the second half of the cycle reaches a state of saturation.
Metabolism and excretion
Gestodene is biotransformed in the liver. The average plasma clearance is 0.8-1 ml / min / kg. The level of gestodene in the blood serum decreases biphasically. T 1/2 in the β-phase - 12-20 hours. Gestodene is excreted only in the form of metabolites, 60% in the urine, 40% in the feces. T 1/2 metabolites - about 1 day.
Ethinylestradiol
Suction
After oral administration, ethinylestradiol is absorbed rapidly and almost completely. Average Cmax in blood serum is achieved 1-2 hours after ingestion and is 30-80 pg / ml. Absolute bioavailability due to presystemic conjugation and primary metabolism is about 60%.
Distribution
Completely (about 98.5%), but non-specifically binds to albumin and induces an increase in the level of SHBG in the blood serum. Average V d - 5-18 l / kg.
C ss is set to 3-4 days of taking the drug, and it is 20% higher than after a single dose.
Metabolism
It undergoes aromatic hydroxylation with the formation of hydroxylated and methylated metabolites, which are present in the form of free metabolites or in the form of conjugates (glucuronides and sulfates). Metabolic clearance from blood plasma is about 5-13 ml.
breeding
Serum concentration decreases biphasically. T 1/2 in the β-phase is about 16-24 hours. Ethinylestradiol is excreted only in the form of metabolites, in a ratio of 2:3 with urine and bile. T 1/2 metabolites - about 1 day.
Indications for the use of the drug
- contraception.
Dosing regimen
Assign 1 tablet / day for 21 days, if possible at the same time of day. After taking the last tablet from the package, a 7-day break is taken, during which withdrawal bleeding occurs. The next day after a 7-day break (i.e. 4 weeks after taking the first tablet, on the same day of the week), the drug is resumed.
The first tablet of Lindinet 20 should be taken from the 1st to the 5th day of the menstrual cycle.
At switching to Lindinet 20 from another combined oral contraceptive The first tablet of Lindinet 20 should be taken after taking the last tablet from the package of another oral hormonal contraceptive, on the first day of withdrawal bleeding.
At switching to Lindinet 20 from progestogen-only preparations ("mini-pili", injections, implant), when taking "mini-drank" you can start taking Lindinet 20 on any day of the cycle, you can switch from using the implant to taking Lindinet 20 the next day after the removal of the implant, when using injections - on the eve of the last injection. In these cases, additional methods of contraception should be used in the first 7 days.
After an abortion in the first trimester of pregnancy you can start taking Lindinet 20 immediately after surgery. In this case, there is no need to use additional methods of contraception.
After childbirth or after an abortion in the second trimester of pregnancy taking the drug can be started on the 21-28th day. In these cases, additional methods of contraception must be used in the first 7 days. With a later start of taking the drug in the first 7 days, an additional, barrier method of contraception should be used. In the case when sexual contact took place before the start of contraception, before starting the drug, pregnancy should be excluded or the start of the drug should be postponed until the first menstruation.
At pass taking the pill, the missed pill should be taken as soon as possible. If the interval in taking the tablets was less than 12 hours then the contraceptive effect of the drug is not reduced, and in this case there is no need to use an additional method of contraception. The remaining tablets should be taken at the usual time. If the interval is more than 12 hours then the contraceptive effect of the drug may decrease. In such cases, you should not make up for the missed dose, continue taking the drug as usual, but in the next 7 days, you need to use an additional method of contraception. If at the same time there are less than 7 tablets left in the package, the drug from the next package should be started without interruption. In this case, withdrawal bleeding does not occur until the completion of the second pack, but spotting or breakthrough bleeding may occur.
If withdrawal bleeding does not occur after the end of taking the drug from the second package, then pregnancy should be excluded before continuing to take the drug.
If within 3-4 hours after taking the drug begins vomiting and/or diarrhea may reduce the contraceptive effect. In such cases, you should proceed in accordance with the instructions for skipping pills. If the patient does not want to deviate from the usual contraceptive regimen, the missed pills should be taken from another package.
For acceleration of the onset of menstruation you should reduce the break in taking the drug. The shorter the break, the more likely the occurrence of breakthrough or spotting bleeding while taking the pills from the next pack (similar to cases with delayed menstruation).
For delayed start of menstruation the drug should be continued from a new package without a 7-day break. Menstruation can be delayed as long as necessary until the end of the last pill from the second package. With a delay in menstruation, breakthrough or spotting bleeding may occur. Regular intake of Lindinet 20 can be restored after the usual 7-day break.
Side effect
Side effects requiring discontinuation of the drug
From the side of the cardiovascular system: arterial hypertension; rarely - arterial and venous thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary embolism); very rarely - arterial or venous thromboembolism of the hepatic, mesenteric, renal, retinal arteries and veins.
From the sense organs: hearing loss due to otosclerosis.
Others: hemolytic-uremic syndrome, porphyria; rarely - exacerbation of reactive systemic lupus erythematosus; very rarely - Sydenham's chorea (passing after discontinuation of the drug).
Other side effects are more common but less severe. The expediency of continuing the use of the drug is decided individually after consultation with a doctor, based on the benefit / risk ratio.
From the reproductive system: acyclic bleeding / spotting from the vagina, amenorrhea after discontinuation of the drug, changes in the state of vaginal mucus, the development of inflammatory processes in the vagina, candidiasis, tension, pain, enlargement of the mammary glands, galactorrhea.
From the digestive system: epigastric pain, nausea, vomiting, Crohn's disease, ulcerative colitis, occurrence or exacerbation of jaundice and / or itching associated with cholestasis, cholelithiasis, hepatitis, liver adenoma.
Dermatological reactions: erythema nodosum, erythema exudative, rash, chloasma, increased hair loss.
From the side of the central nervous system: headache, migraine, mood lability, depression.
From the sense organs: hearing loss, increased sensitivity of the cornea (when wearing contact lenses).
From the side of metabolism: fluid retention in the body, a change (increase) in body weight, a decrease in carbohydrate tolerance, hyperglycemia, an increase in TG levels.
Others: allergic reactions.
Contraindications to the use of the drug
- the presence of severe and / or multiple risk factors for venous or arterial thrombosis (including complicated lesions of the valvular apparatus of the heart, atrial fibrillation, diseases of the cerebral vessels or coronary arteries, severe or moderate arterial hypertension with blood pressure ≥ 160/100 mm rt.st.);
- the presence or indication in the anamnesis of the precursors of thrombosis (including transient ischemic attack, angina pectoris);
- migraine with focal neurological symptoms, incl. in history;
- venous or arterial thrombosis / thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower leg, pulmonary embolism) at present or in history;
- the presence of venous thromboembolism in history;
- surgical intervention with prolonged immobilization;
- diabetes mellitus (with angiopathy);
- pancreatitis (including history), accompanied by severe hypertriglyceridemia;
- dyslipidemia;
- severe liver disease, cholestatic jaundice (including during pregnancy), hepatitis, incl. in history (before the normalization of functional and laboratory parameters and within 3 months after their normalization);
- jaundice when taking GCS;
- cholelithiasis at present or in history;
- Gilbert's syndrome, Dubin-Johnson syndrome, Rotor's syndrome;
- liver tumors (including history);
- severe itching, otosclerosis or its progression during a previous pregnancy or taking corticosteroids;
- hormone-dependent malignant neoplasms of the genital organs and mammary glands (including if they are suspected);
- vaginal bleeding of unknown etiology;
- smoking over the age of 35 (more than 15 cigarettes per day);
- pregnancy or suspicion of it;
- lactation period;
- Hypersensitivity to the components of the drug.
WITH caution the drug should be prescribed for conditions that increase the risk of developing venous or arterial thrombosis / thromboembolism: age over 35 years, smoking, hereditary predisposition to thrombosis (thrombosis, myocardial infarction or cerebrovascular accident at a young age in any of the immediate relatives), hemolytic- uremic syndrome, hereditary angioedema, liver diseases, diseases that first arose or worsened during pregnancy or against the background of previous use of sex hormones (including porphyria, herpes in pregnancy, chorea / Sydenham's disease /, Sydenham's chorea, chloasma), obesity (body mass index over 30 kg/m2), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valvular heart disease, atrial fibrillation, prolonged immobilization, major surgery, lower limb surgery, severe trauma, varicose veins and superficial thrombophlebitis , postpartum period (non-lactating women /21 days after childbirth/; lactating women after the end of the lactation period), the presence of severe depression, (including history), changes in biochemical parameters (activated protein C resistance, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, incl. . antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.
The use of the drug during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
In small quantities, the components of the drug are excreted in breast milk.
When used during lactation, milk production may decrease.
Application for violations of liver function
Contraindicated in violations of liver function.
Application for violations of kidney function
special instructions
Before starting the use of the drug, it is necessary to conduct a general medical (detailed family and personal history, measurement of blood pressure, laboratory tests) and gynecological examination (including examination of the mammary glands, pelvic organs, cytological analysis of a cervical smear). A similar examination during the period of taking the drug is carried out regularly, every 6 months.
The drug is a reliable contraceptive: the Pearl index (an indicator of the number of pregnancies that occurred during the use of a contraceptive method in 100 women for 1 year), when used correctly, is about 0.05. Due to the fact that the contraceptive effect of the drug from the start of administration is fully manifested by the 14th day, in the first 2 weeks of taking the drug, it is recommended to additionally use non-hormonal methods of contraception.
In each case, before prescribing hormonal contraceptives, the benefits or possible negative effects of their use are individually assessed. This issue must be discussed with the patient, who, after receiving the necessary information, will make the final decision on the preference for hormonal or any other method of contraception.
The state of health of women must be carefully monitored. If any of the following conditions / diseases appear or worsen while taking the drug, you must stop taking the drug and switch to another, non-hormonal method of contraception:
- diseases of the hemostasis system;
- conditions / diseases predisposing to the development of cardiovascular, renal failure;
- epilepsy;
- migraine;
- the risk of developing an estrogen-dependent tumor or estrogen-dependent gynecological diseases;
- diabetes mellitus, not complicated by vascular disorders;
- severe depression (if depression is associated with impaired tryptophan metabolism, then vitamin B 6 can be used to correct it);
- sickle cell anemia, tk. in some cases (for example, infections, hypoxia), estrogen-containing drugs in this pathology can provoke thromboembolism;
- the appearance of deviations in laboratory tests for assessing liver function.
Thromboembolic diseases
Epidemiological studies have shown that there is a connection between taking oral hormonal contraceptives and an increased risk of developing arterial and venous thromboembolic diseases (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary embolism). An increased risk of venous thromboembolic disease has been proven, but it is significantly less than during pregnancy (60 cases per 100,000 pregnancies). When using oral contraceptives, arterial or venous thromboembolism of the hepatic, mesenteric, renal or retinal vessels is very rarely observed.
The risk of developing arterial or venous thromboembolic diseases increases:
- with age;
- when smoking (heavy smoking and age over 35 are risk factors);
- if there is a family history of thromboembolic diseases (for example, in parents, a brother or sister). If a genetic predisposition is suspected, it is necessary to consult a specialist before using the drug;
- with obesity (body mass index more than 30 kg / m 2);
- with dyslipoproteinemia;
- with arterial hypertension;
- in diseases of the heart valves, complicated by hemodynamic disorders;
- with atrial fibrillation;
- with diabetes mellitus complicated by vascular lesions;
- with prolonged immobilization, after major surgery, after surgery on the lower extremities, after a severe injury.
In these cases, a temporary discontinuation of the drug is expected (no later than 4 weeks before surgery, and resumed no earlier than 2 weeks after remobilization).
Women after childbirth have an increased risk of venous thromboembolic disease.
It should be borne in mind that diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia, increase the risk of developing venous thromboembolic diseases.
It should be borne in mind that resistance to activated protein C, hyperhomocysteinemia, deficiency of proteins C and S, deficiency of antithrombin III, the presence of antiphospholipid antibodies increase the risk of developing arterial or venous thromboembolic diseases.
When assessing the benefit / risk ratio of taking the drug, it should be taken into account that targeted treatment of this condition reduces the risk of thromboembolism. The symptoms of thromboembolism are:
- sudden chest pain that radiates to the left arm;
- sudden shortness of breath;
- any unusually severe headache that lasts a long time or appears for the first time, especially when combined with sudden complete or partial loss of vision or diplopia, aphasia, dizziness, collapse, focal epilepsy, weakness or severe numbness of one half of the body, movement disorders, severe unilateral pain in calf muscle, acute abdomen.
Tumor diseases
Some studies have reported an increase in the incidence of cervical cancer in women who have taken hormonal contraceptives for a long time, but the results of the studies are conflicting. Sexual behavior, human papillomavirus infection and other factors play a significant role in the development of cervical cancer.
A meta-analysis of 54 epidemiological studies showed that there is a relative increase in the risk of breast cancer among women taking oral hormonal contraceptives, but the higher detection of breast cancer could be associated with more regular medical examinations. Breast cancer is rare among women under 40, whether they are taking hormonal birth control or not, and increases with age. Taking pills can be regarded as one of many risk factors. However, women should be advised of the potential risk of developing breast cancer based on a benefit-risk assessment (protection against ovarian and endometrial cancer).
There are few reports of the development of benign or malignant liver tumors in women who take hormonal contraceptives for a long time. This should be kept in mind in the differential diagnostic evaluation of abdominal pain, which may be associated with an increase in the size of the liver or intraperitoneal bleeding.
Chloasma
Chloasma can develop in women who have a history of this disease during pregnancy. Those women who are at risk of developing chloasma should avoid contact with sunlight or ultraviolet radiation while taking Lindinet 20.
Efficiency
The effectiveness of the drug may decrease in the following cases: missed pills, vomiting and diarrhea, simultaneous use of other drugs that reduce the effectiveness of birth control pills.
If the patient is simultaneously taking another drug that can reduce the effectiveness of birth control pills, additional methods of contraception should be used.
The effectiveness of the drug may decrease if, after several months of their use, irregular, spotting or breakthrough bleeding appears, in such cases it is advisable to continue taking the tablets until they are finished in the next package. If at the end of the second cycle, menstrual bleeding does not begin or acyclic spotting does not stop, stop taking the tablets and resume it only after pregnancy has been ruled out.
Changes in laboratory parameters
Under the influence of oral contraceptive pills - due to the estrogen component - the level of some laboratory parameters (functional parameters of the liver, kidneys, adrenal glands, thyroid gland, hemostasis indicators, levels of lipoproteins and transport proteins) may change.
Additional Information
After suffering acute viral hepatitis, the drug should be taken after normalization of liver function (not earlier than after 6 months).
With diarrhea or intestinal disorders, vomiting, the contraceptive effect may decrease. Without stopping taking the drug, it is necessary to use additional non-hormonal methods of contraception.
Women who smoke have an increased risk of developing vascular diseases with serious consequences (myocardial infarction, stroke). The risk depends on age (especially in women over 35) and on the number of cigarettes smoked.
A woman should be warned that the drug does not protect against HIV infection (AIDS) and other sexually transmitted diseases.
Influence on the ability to drive vehicles and control mechanisms
Studies on the effect of the drug Lindinet 20 on the ability to drive a car and work machinery have not been conducted.
Overdose
No severe symptoms have been described after taking the drug in high doses.
Symptoms: nausea, vomiting, in girls - bloody discharge from the vagina.
Treatment: symptomatic therapy is prescribed, there is no specific antidote.
drug interaction
The contraceptive activity of Lindinet 20 is reduced when taken simultaneously with ampicillin, tetracycline, rifampicin, barbiturates, primidone, carbamazepine, phenylbutazone, phenytoin, griseofulvin, topiramate, felbamate, oxcarbazepine. The contraceptive effect of oral contraceptives is reduced with the use of these combinations, breakthrough bleeding and menstrual disorders become more frequent. While taking Lindinet 20 with the above drugs, as well as within 7 days after completing the course of taking them, it is necessary to use additional non-hormonal (condom, spermicidal gels) methods of contraception. When using rifampicin, additional methods of contraception should be used within 4 weeks after completion of the course of its administration.
When used simultaneously with Lindinet 20, any drugs that increase gastrointestinal motility reduce the absorption of active substances and their level in blood plasma.
Sulfation of ethinyl estradiol occurs in the intestinal wall. Drugs that also undergo sulfation in the intestinal wall (including ascorbic acid) competitively inhibit the sulfation of ethinylestradiol and thereby increase the bioavailability of ethinylestradiol.
Inducers of microsomal liver enzymes reduce the level of ethinylestradiol in plasma (rifampicin, barbiturates, phenylbutazone, phenytoin, griseofulvin, topiramate, hydantoin, felbamate, rifabutin, oscarbazepine).
Liver enzyme inhibitors (itraconazole, fluconazole) increase plasma levels of ethinylestradiol.
Some antibiotics (ampicillin, tetracycline), preventing the intrahepatic circulation of estrogens, reduce the level of ethinylestradiol in plasma.
Ethinylestradiol, by inhibiting liver enzymes or accelerating conjugation (primarily glucuronidation), can affect the metabolism of other drugs (including cyclosporine, theophylline); the concentration of these drugs in the blood plasma may increase or decrease.
With the simultaneous use of Lindinet 20 with St. John's wort (including infusion), the concentration of active substances in the blood decreases, which can lead to breakthrough bleeding, pregnancy. The reason for this is the inducing effect of St. John's wort on liver enzymes, which continues for another 2 weeks after the completion of the course of taking St. John's wort. This combination of drugs is not recommended.
Ritonavir reduces the AUC of ethinylestradiol by 41%. In this regard, during the use of ritonavir, a hormonal contraceptive with a higher content of ethinyl estradiol should be used or additional non-hormonal methods of contraception should be used.
It may be necessary to correct the dosing regimen when using hypoglycemic agents, tk. oral contraceptives may reduce carbohydrate tolerance, increase the need for insulin or oral antidiabetic agents.
Terms of dispensing from pharmacies
The drug is dispensed by prescription.
Terms and conditions of storage
The drug should be stored out of the reach of children at a temperature not exceeding 30 ° C. Shelf life - 3 years.
"Compound Lindinet 20(1 tablet):
- - 0.02 mg;
- - 0.075 mg;
- magnesium stearate - 0.2 mg;
- povidone - 1.7 mg;
- corn starch - 15.5 mg;
Compound Lindinet 30(1 tablet):
- ethinylestradiol - 0.03 mg;
- gestodene - 0.075 mg;
- sodium calcium edetate - 0.065 mg;
- magnesium stearate - 0.2 mg;
- colloidal silicon dioxide - 0.275 mg;
- povidone - 1.7 mg;
- corn starch - 15.5 mg;
- lactose monohydrate - 37.165 mg.
Both pharmaceutical forms are supplied in the form of tablets, the shell of which has the following components:
- sucrose - 19.66 mg;
- - 8.231 mg;
- macrogol 6000 - 2.23 mg;
- titanium dioxide - 0.46465 mg;
- povidone - 0.171 mg;
- yellow quinoline dye (D + C yellow No. 10 - E 104) - 0.00135 mg.
Release form
In pharmacy kiosks, the drug is presented in the form of round, biconvex tablets, which are coated with a light yellow shell on both sides. There are no inscriptions or symbols. On a break, the tablet is white or close to white in color with a light yellow edging of the shell.
pharmachologic effect
Lindinet belongs to the group of monophasic combined oral medications based on sex hormones , respectively, is used mainly for the purpose of contraception. The main therapeutic effect of the drug is associated with several mechanisms of action, including a decrease in the secretion of gonadotropic hormones. , active obstruction of ovulatory processes and inhibition of the maturation of follicles in the ovaries.
First of all, it should be noted that ethinylestradiol , one of the biologically active constituents, is a synthetic analogue of the follicular hormone , which, together with the hormones of the corpus luteum, is involved in the regulation of the woman's menstrual cycle, largely inhibiting it at certain stages.
Another active ingredient is gestodene is a gestagenic 19-nortestosterone derivative and is a stronger and more selective version of natural secreted by the corpus luteum. This component is used in ultra low amounts, due to which it does not realize its androgenic capabilities (the chemical basis for gestodene is a variation of the male sex hormone) and has the weakest effect on the carbohydrate and lipid metabolism of the body.
In addition to the central mechanisms of action directly on sex hormones, the drug implements contraceptive properties indirectly through peripheral components. Under the influence of a pharmaceutical drug, susceptibility decreases to the blastocyst, which makes the process of implantation of the initial forms of the fetus almost impossible. The density and viscosity of the mucus localized in the cervix also increases, which becomes largely impassable for spermatozoa that make active movements towards the female egg.
Lindinet has not only contraceptive effects, the pharmaceutical drug contributes active prevention some gynecological diseases and not only. In particular, the possibility of the appearance of functional ovarian cysts And . Reduces the risk of in the mammary glands, congestive inflammatory processes practically disappear. The beneficial properties of the drug extend to skin , as their general condition improves and the degree of manifestation decreases (with regular use, dermatological defects disappear completely).
Pharmacodynamics and pharmacokinetics
Pharmacokinetic abilities of gestodene
After oral administration, the active component is absorbed from the gastrointestinal tract quite quickly and almost completely, because its bioavailability is about 99%, and the maximum concentration of 2-4 ng / ml is noted after 1 hour.
In the bloodstream gestodene contacts And specific globulin SHBG , only 1-2% of the amount of the active ingredient remains in free form. The pharmacokinetics of gestodene largely depends on the level of SHBG and the concentration of estradiol, because the amount of the selective carrier increases by 3 times under the influence of the sex hormone. The constant intake of oral contraceptives also contributes to the active saturation of gestodene, with its daily use, the concentration increases by 3-4 times.
The active component undergoes the main stages of biochemical transformation in the liver, after which it is excreted in the urine (60%) and feces (40%) only in the form of metabolites. The half-life of the active ingredient is biphasic and takes about 1 day, since the average plasma clearance is from 0.8 to 1 ml / million / kg.
Pharmacokinetic abilities of ethinylestradiol
The second active component has slightly lower absorption rates - due to presystemic conjugation and primary metabolism, the absolute bioavailability of the pharmacological component from the digestive tube is only 60%, and the maximum concentration of 30-80 pg / ml is reached after 1-2 hours.
On the distribution side, ethinylestradiol, on the contrary, outperforms gestodene, because 98.5% of the active substance binds to nonspecific albumins. Also, the active component induces an increase in the level of SHBG, which favorably affects the overall effectiveness of the oral contraceptive. A constant average level of ethinylestradiol is established by 3-4 days after the start of the therapeutic course, and it is 20% higher than after a single dose of the Lindinet tablet.
The biotransformation of the active substance occurs in the liver and is aromatic hydroxylation with the formation of methylated and hydroxylated metabolic products in free form or in the form of conjugates with sulfates or glucuronides. Metabolic clearance from blood plasma ranges from 5-13 ml.
Ethinylestradiol is excreted only in the form of metabolic products with urine and bile in a ratio of 2:3. The half-life, like that of gestodene, is biphasic and is about 1 day.
Indications for use
- contraception;
- functional disorders of the menstrual cycle.
Contraindications
- individual hypersensitivity to a pharmaceutical preparation or its constituent components;
- risk factors for arterial or venous thrombosis;
- moderate and severe;
- or as precursors of thrombosis;
- surgery with prolonged immobilization;
- with a pronounced increase in blood triglycerides;
- dyslipidemia ;
- severe liver disease ( hepatitis , cholestatic jaundice and etc);
- , Dubin-Johnson, Rotor;
- neoplasm localized in the liver;
- otosclerosis or the presence of it in the anamnesis of a previous pregnancy or after taking glucocorticosteroids;
- smoking over the age of 35;
- hormone-dependent malignant tumors genital organs and mammary glands;
- vaginal bleeding of unknown origin;
- period of lactation and childbearing.
Side effects
Adverse effects of treatment requiring immediate cancellation pharmaceutical therapy:
- From the side of cardio-vascular system: arterial hypertension, , , deep vein thrombosis of the lower extremities, venous or arterial thromboembolism hepatic, mesenteric, retinal or renal vessels.
- From the side sense organs: hearing loss due to otosclerosis .
- Others: porphyria , hemolytic-uremic syndrome, exacerbations of reactive , chorea of Sydenham .
Side effects, after the appearance of which the expediency of further use of the drug is decided in individual order:
- From the side reproductive system: acyclic bleeding from the vagina of unknown etiology, , colpocytological changes in vaginal mucus, inflammatory diseases, pain, breast enlargement, galactorrhea .
- From the side central nervous system: hearing loss, , , mood lability.
- Dermatological reactions: or exudative erythema , incomprehensible rash, chloasma, increased .
- From the side digestive system: epigastric pain, nausea and vomiting, Crohn's disease , nonspecific ulcerative , jaundice and itching, which is due to it, cholelithiasis , liver adenoma, hepatitis.
- From the side metabolic processes: fluid retention in the body, decreased tolerance to carbohydrates, increased levels of triglycerides or blood glucose, weight gain.
- Other allergic reactions.
Application instruction of Lindinet (Way and dosage)
Lindinet 20, instructions for use
Contraceptive pills are used orally orally once a day, without chewing and drinking plenty of water, regardless of the meal. If possible, you should take the pills at the same time of day for 21 days, then you need to take a break for 7 days, and then resume the use of contraceptives. That is, the next tablet should be used 4 weeks after the start of the course on the same day of the week. During the break, uterine bleeding will be observed, which corresponds to menstruation in a normal cycle.
A course of conservative contraception should be started from the 1st to the 5th day of the menstrual cycle, if other oral contraceptives have not been used before. Otherwise, the 1st tablet must be taken after the last dose of the previous hormone-containing pharmaceutical preparation, on the 1st day of bleeding after withdrawal.
Transition from progestogen-containing agents on Lindinet requires the use of an additional method of contraception in the first week. The date of the first intake of a new contraceptive must be consistent with the pharmaceutical form of the previous drug:
- in the form of mini-tablets - on any day of the menstrual cycle;
- in the case of injections - on the eve of the last injection;
- implant - the next day after its removal.
Lindinet 30, instructions for use
Since this pharmaceutical form is an enhanced version of Lindinet 20 with a higher concentration of ethinylestradiol, it is recommended to prescribe it after abortion so that the restoration of the physiological hormonal background takes place much faster and less painfully.
If the abortion was performed in 1st trimester of pregnancy , then there is nothing to worry about. Oral contraceptives can be started immediately after gynecological manipulation and there is no need to use additional methods of contraception.
If the abortion or childbirth occurred during 2nd trimester of pregnancy , then taking the pharmaceutical preparation can be started only on the 21-28th day after the obstetric operation. With a later start of the course of conservative protection in the first week, a barrier method of contraception should be used. If a full-fledged sexual intercourse took place before the start of taking the drug, then before taking contraceptives, you must make sure that there is no new pregnancy.
Missing an oral contraceptive pill
If the next pill was missed, then the missing amount of the pharmaceutical drug in the bloodstream must be replenished as quickly as possible. With a delay that duration does not exceed 12 hours , the clinical effects of the contraceptive are not reduced and the need for additional protection by other methods of contraception itself disappears. Subsequent tablets are taken according to the usual regimen.
If a woman misses a pill and did not make up for her loss within 12 hours , then the pharmacological efficacy of the drug is reduced, which requires special measures and precautions. First of all, as soon as possible, you should resume taking the drug and continue to carry it out as usual. It is recommended to use any other methods of contraception for a week after the pass.
This situation may become more difficult if less than 7 tablets left in the package . How to take in this case - start the next pack without observing the necessary weekly break, which is carried out only at the end of the 2nd pack of contraceptives. It should be noted that during the use of the 2nd pack, spotting or even breakthrough bleeding may be observed, which can indirectly indicate the presence of pregnancy. If hemorrhages have not stopped at the end of the 2nd package, then before continuing to take contraceptives, you should consult a doctor and exclude the presence of a developing fetus in the womb.
Overdose
Taking an excessive amount of contraceptive is accompanied by the following symptoms:
- nausea;
- vomit;
- vaginal bleeding in small amounts.
There is no specific pharmaceutical antidote for the drug, therefore, symptomatic therapy of individual clinical manifestations of intoxication is used.
Interaction
The contraceptive properties of a pharmaceutical product are reduced when it is used with drugs such as , , , barbiturates, primidon , , Phenylbutazone , Phenytoin , , Oxcarbazepine .
Therefore, if it is necessary to share these drugs with Lindinet, it is necessary to use additional non-hormonal contraceptives for 7 days (it is recommended to visit an additional consultation with your doctor and clarify the period for certain). It is also possible the appearance of spotting or breakthrough bleeding, menstrual irregularities, or some other side effects.
In conditions increased peristalsis or diarrhea the residence time of the contraceptive in the lumen of the gastrointestinal tract is reduced, which significantly reduces the absorption properties of the hormonal contraceptive. Any drug that shortens the presence of Lindinet in the digestive tube leads to a decrease in the concentration of active constituents in the blood, and, accordingly, to a decrease in their beneficial effect.
Drug Interactions at the stage of absorption are modeled on the combined use of a contraceptive with, since biologically active substances are equally exposed to sulfation in the intestinal wall, which inhibits metabolic chains and increases the bioavailability of ethinyl estradiol.
Terms of sale
The acquisition of the medicinal product is allowed only on the basis of the prescription form.
Storage conditions
It is necessary to save the pharmaceutical product in a dry place, protected from direct sunlight, inaccessible to young children at a temperature not exceeding 25 degrees Celsius.
Best before date
special instructions
Pregnancy after using hormonal contraceptives
Oral hormonal contraceptives are a group of pharmaceutical preparations based on synthetic analogues of female sex hormones (estrogen and progesterone) that prevent ovulation from occurring, preventing the very possibility of fertilization. Of course, a large audience of women is convinced that it is harmful to use them for contraceptive purposes, since a normal, physiological pregnancy after a drug change in hormonal levels most likely will not occur. However, this is one of the myths about this group of drugs.
After stopping the use of hormonal contraceptives and at the end of the course of conservative contraception, the effects of the drugs gradually disappear. The only peculiarity is that pregnancy planning you should find out the exact timing of the optimal moment for fertilization in the antenatal clinic or from your personal gynecologist. After all, every time a woman takes a pill for a headache, she does not worry about the health of an unconceived child, in this case the situation is almost identical.
When you can not be protected by barrier methods of contraception
Lindinet is a reliable hormonal contraceptive, which can be found in a special indicator of the number of pregnancies that occurred during the course of oral contraception in 100 women for 1 year. For this pharmaceutical, it is only 0.05 if the contraceptive is used correctly and only according to the scheme of application. However, the pharmacological effects of Lindinet do not develop fully immediately, but only by the 14th day from the start of taking the tablets, because in the first 2 weeks It is recommended to use barrier methods of contraception.
Lindinet 20 and Lindinet 30 - what's the difference?
A large number of visitors to pharmaceutical forums for women are asked by the following series of questions: “Lindinet 20 and 30 - what is the difference?”, As well as whether the drugs are interchangeable and, finally, which is the best of the two forms of contraception. The difference in the forms of the same contraceptive lies in concentration one of the active ingredients is ethinyl estradiol. In oral tablets, its level can be 0.02 mg and 0.03 mg, respectively, which in biochemical terms really puts them in different categories.
Lindinet 20 has a milder pharmacological effect and to a lesser extent contributes to an increase in the selective SHBG transporter, which allows it to be used for contraception, however for therapeutic needs , as a rule, a stronger form of the drug is required, therefore Lindinet 30 is used. What distinguishes the more concentrated form of the drug from weaker tablets is not advertised, since sometimes, according to individual indications, even as a contraceptive, it is necessary to use Lindinet 30, which can be perceived by a woman as an unfair load of a hormonal drug.
It is categorically contraindicated to replace pharmaceutical forms of a drug on your own, because a qualified specialist who prescribes contraceptives or therapeutic agents relies on the results of clinical studies, their interpretation and many years of experience in their field, and not on an approximate idea of the biomechanism of the female body. If you experience any side effects or other adverse effects, you should seek advice and resolve this issue on an individual basis.
Since Lindinet is produced in Hungary, its cost in pharmacy kiosks is much lower than that of a drug produced jointly by French and German pharmacists, but this in no way speaks of the effectiveness of the first, because the choice of a contraceptive should be entrusted to a qualified specialist, because he based on individual indicators of hormonal balance and some other medical aspects.
Which is better: Novinet or Lindinet 20?
Novinet - monophasic oral contraceptive, which, in addition to ethinyl estradiol, contains a synthetic progestogen , which somewhat changes the mechanism of action of the contraceptive drug. Like all artificial pharmaceutical components of this nature, desogestrel has a high affinity for progesterone receptors located in the hypothalamic-pituitary region, on which its effects are based. In sufficiently small quantities, it is able to “turn on” the negative feedback mechanism, resulting in a sharp inhibition of the release and production of gonadotropins and complete blocking of ovulation.
Since Novinet includes such a potent pharmaceutical component as one of the active substances, accordingly, its price is almost twice as high as that of Lindinet. However, with certain individual indications or contraindications, a woman does not have the opportunity to use a cheaper contraceptive, which makes it possible to include Novinet in a conservative contraceptive course.
Alcohol and Lindinet
Biochemical studies have shown that alcohol in small quantities does not affect the effectiveness of oral contraception. Moderate dosages of alcoholic beverages are considered to be up to 3 glasses of wine or 50 grams of cognac, but no more, since an increase in the amount of alcohol in the blood increases the risk of a possible pregnancy.
Last update of the description by the manufacturer 07/13/2015
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Active substance:
ATX
Pharmacological group
Nosological classification (ICD-10)
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Compound
| Coated tablets | 1 tab. |
| active substances: | |
| ethinylestradiol | 0.03 mg |
| gestodene | 0.075 mg |
| Excipients | |
| core: sodium calcium edetate - 0.065 mg; magnesium stearate - 0.2 mg; colloidal silicon dioxide - 0.275 mg; povidone - 1.7 mg; corn starch - 15.5 mg; lactose monohydrate - 37.155 mg | |
| shell: quinoline yellow dye (D + C yellow No. 10 - E104) - 0.018 mg; povidone - 0.171 mg; titanium dioxide - 0.448 mg; macrogol 6000 - 2.23 mg; talc - 4.242 mg; calcium carbonate - 8.231 mg; sucrose - 19.66 mg |
pharmachologic effect
pharmachologic effect- estrogen-gestagenic, contraceptive.Dosage and administration
inside, without chewing, drinking plenty of water, regardless of the meal.
Take 1 table. per day (if possible at the same time of day) for 21 days. Then, after taking a 7-day break in taking the tablets, resume oral contraception (i.e. 4 weeks after taking the 1st tablet, on the same day of the week). During the 7-day break, uterine bleeding occurs as a result of hormone withdrawal.
First dose of the drug: taking the drug Lindinet 30 should be started from the 1st to the 5th day of the menstrual cycle.
Switching from a combined oral contraceptive to taking Lindinet 30. 1st table. Lindinet 30 is recommended to be taken after taking the last hormone-containing tablet of the previous drug, on the 1st day of withdrawal bleeding.
Switching from progestogen-containing drugs (mini-tablets, injections, implant) to taking Lindinet 30. You can start switching from mini-pills any day of your menstrual cycle; in the case of an implant, the next day after its removal; in case of injections - on the eve of the last injection.
In this case, in the first 7 days of taking the drug Lindinet 30, it is necessary to use an additional method of contraception.
Taking the drug Lindinet 30 after an abortion in the first trimester of pregnancy. The contraceptive can be started immediately after the abortion, without the need for an additional method of contraception.
Taking the drug Lindinet 30 after childbirth or after an abortion in the second trimester of pregnancy. You can start taking a contraceptive on the 21st-28th day after childbirth or abortion in the second trimester of pregnancy. With a later start of taking the contraceptive, in the first 7 days, it is necessary to use an additional, barrier method of contraception. In the case when sexual contact took place before the start of contraception, before you start taking the drug, you should exclude the presence of a new pregnancy or wait for the next menstruation.
Missed pills. If the next scheduled pill was missed, then the missed dose should be replenished as soon as possible. With a delay not exceeding 12 hours, the contraceptive effect of the drug does not decrease, and there is no need to use an additional method of contraception. The remaining tablets are taken as usual.
With more than a 12-hour delay, the contraceptive effect may decrease. In such cases, you should not make up for the missed dose, continue taking the drug as usual, but in the next 7 days, you need to use an additional method of contraception. If at the same time less than 7 tablets remained in the package, then they start taking the tablets from the next package without observing a break. In such cases, uterine withdrawal bleeding occurs only after the completion of the 2nd pack; while taking the tablets from the 2nd package, spotting or breakthrough bleeding is possible.
If there is no withdrawal bleeding at the end of taking the pills from the 2nd pack, then pregnancy should be ruled out before continuing to take the contraceptive.
Measures to be taken in case of vomiting and diarrhoea. If vomiting occurs in the first 3-4 hours after taking the next tablet, the tablet is not completely absorbed. In such cases, you should act in accordance with the instructions described in paragraph Missed pills.
If the patient does not want to deviate from the usual contraceptive regimen, the missed pills should be taken from another package.
Delay of menstruation and acceleration of the onset of menstruation. In order to delay menstruation, they start taking pills from a new package without observing a break. Menstruation can be delayed at will until all the pills from the 2nd package run out. With a delay in menstruation, breakthrough or spotting uterine bleeding is possible. You can return to the usual intake of tablets after observing a 7-day break.
INSTRUCTIONS
on the medical use of drugs
Lindinet 20 and Lindinet 30
(LINDYNETTE 20, LINDYNETTE30)
General characteristics:
international and chemical names: gestodene, ethinyl estradiol;
main physical and chemical properties:
Lindinet 20 - round, biconvex tablets, sugar-coated, pale yellow, without an inscription, with a diameter of approximately 5.6 mm;
Lindinet 30- round, biconvex tablets, sugar-coated, yellow, unlabeled, with a diameter of approximately 5.6 mm;
1 tablet Lindinet 20 contains 0.075 mg gestodene and 0.02 mgetinilest radiol;
1 tablet Lindinet 30contains 0.075 mg of gestodene and 0.03 mgetinilest radiol;
Excipients:
sodium calcium edetate, magnesium stearate silicon colloidal anhydrous povidone; corn starch; lactose; kinoline yellow (E 104); titanium dioxide (E 171); macrogol 6000, talc; calcium carbonate; sucrose.
Release form. Coated tablets.
Pharmacotherapeutic group.
Hormonal contraceptives for systemic use. Gestodene and estrogen. ATC code G03A A10.
pharmacological properties.
Combined oral contraceptives block diugonadotropins. The primary action of these drugs is aimed at inhibiting ovulation. The drug leads to a change in cervical mucus, which makes it difficult for sperm to pass into the uterine cavity and affects the endometrium, thereby reducing the possibility of implantation. All this leads to the prevention of pregnancy.
Oral contraceptives, in addition to preventing pregnancy, may have a number of positive effects.
- Influence on the monthly cycle.
- The monthly cycle becomes regular.
- The amount of blood loss during menstruation is reduced and the loss of iron is reduced.
- Reduced frequency of dysmenorrhea.
- Actions related to inhibition of ovulation.
- The incidence of functional ovarian cysts is reduced.
- The frequency of ectopic pregnancy is reduced.
- Other actions.
- The incidence of fibroadenomas and fibrocysts in the mammary glands is reduced.
- The frequency of occurrence of inflammatory processes in the pelvic organs decreases.
- The incidence of endometrial cancer is reduced.
- Improves the condition of the skin with acne.
Pharmacokinetics
Gestodene.
Oral absorption Gestodene is rapidly and almost completely absorbed. After a single dose, the maximum concentration is observed one hour after administration and is 2-4 ng in 1 ml of blood plasma. The bioavailability of gestodene is approximately 99%.
Distribution in the body:
Gestodene binds to albumin and sex hormone-binding globulin. 1-2% is in the form of a free steroid, 50-75% specifically binds to sex hormone-binding globulin. Ethinyl estradiol-induced globulin elevation affects gestodene levels, while globulin fraction elevation leads to a decrease in albumin-bound fraction. The mean volume of distribution of gestodene is 0.7-1.4 l/kg.
Metabolism:
Gestodene is cleaved by known steroid metabolism. Average clearance values: 0.8-1.0 ml / min / kg (0.8-1.0 ml per quilinone 1 kg of body weight).
Selection:
the level of gestodene in the blood serum is biphasic. In the last phase, the elimination half-life is 12-20 hours.
Gestodene is excreted only in the form of metabolites, 60% in the urine, 40% in the feces. The half-life of metabolite elimination is approximately 1 day.
Saturation stage:
the pharmacokinetics of gestodene depends on the level of globulin that binds sex hormones. The concentration in the blood of globulin, which binds sex hormones under the influence of ethinylest radiol, increases three times. In connection with the daily administration, the level of gestodene in the blood plasma increases by three to four times and is balanced in the second half of the cycle.
Ethinylestradiol.
Absorption of oral administration of ethinyl estradiol is absorbed by Shvydka almost completely. The average maximum concentration in blood serum is 30-80 pg / ml 1-2 hours after taking the drug. The bioavailability of ethinylest radiol through pre-systemic conjugation and primary metabolism is approximately 60%.
Distribution in the body:
ethinylestradiol completely but non-specifically binds to albumin (about 98.5%) and causes an increase in the level of globulin that binds sex hormones in the blood serum. The average volume of rospodiluetinylest radiol is 5-18 l/kg.
Metabolism:
Ethinylestradiol mainly undergoes aromatic hydroxylation, and therefore hydroxyl vanite and ethylated metabolites are formed in large quantities in the form of free metabolites or in formiconjugates (glucuronides and sulfates).
Metabolic clearance of ethinylest radiol from blood plasma is about 5-13 ml/min per 1 kg of body weight.
Excretion from the body:
the concentration of ethinylest radiol in the blood serum is biphasic. The half-life of the second phase is almost 16-24 hours. Ethinylestradiol is excreted only in the form of metabolites, with urine and bile in a ratio of 2:3. The elimination half-life of metabolites is approximately 1 day.
Saturation stage:
a stable concentration is established for 3-4 days, when the level of ethinylest radiol in serum is 20% higher than after a single dose.
INDICATIONS
Contraception.
Dosage and administration
The drug should be taken for 21 days, 1 tablet per day (if possible at the same time). Then take a 7-day break. The next 21 tablets should be taken the next day after a 7-day break (in four weeks, on the same day of the week on which the course of taking the drug was started). During a 7-day break, menstrual-like bleeding appears due to discontinuation of the drug.
First dose of the drug
Taking the drug Lindinet 20 or Lindinet 30 should be started from the first day of the menstrual cycle.
Switching to Lindinet 20 or Lindinet 30 from another oral contraceptive.
The first tablet of Lindinet 20 or Lindinet 30 should be taken after taking the last tablet from the previous pack of another oral hormonal contraceptive, on the first day of menstrual bleeding.
Switching to the drug Lindinet 20 or Lindinet 30 from drugs containing only progestogen ("mini-pills", injections, implants).
With a "mini-pill" you can switch to Lindinet 20 or Lindinet 30 on any day of the cycle. From the implant, you can switch to Lindinet 20 or Lindinet 30 the next day after the removal of the implant; from a solution for injection - the day before the injection.
In these cases, additional methods of contraception must be used in the first 7 days.
Taking Lindinet 20 or Lindinet 30 after an abortion in the first trimester of pregnancy
After an abortion, you can start taking the drug immediately, in which case there is no need to use an additional method of contraception.
Taking Lindinet 20 or Lindinet 30 after childbirth or after an abortion in the second trimester of pregnancy
You can take the drug 28 days after childbirth or abortion in the second trimester of pregnancy. In such cases, additional methods of contraception should be used in the first 7 days.
If sexual intercourse has already taken place after childbirth or abortion, pregnancy should be excluded before taking the drug or it is necessary to wait for the first menstruation.
Missed pills.
If a tablet was missed, the missed tablet should be taken as soon as possible. If the interval was less than 12 hours, then the effectiveness of the drug will not decrease, and in this case there is no need to use an additional method of contraception. The remaining tablets should be taken at the usual time.
If the interval is more than 12 hours, then the effectiveness of the drug may decrease. In this case, the woman should not take the missed pill(s), but should take the next pill(s) as normal. In this case, additional methods of contraception must be used for the next 7 days. If there are less than 7 tablets left in the package, the drug from the next package is started without interruption. In this case, there is no menstrual-like bleeding due to discontinuation of the drug before the completion of the drug from the second package, but major breakthrough bleeding may occur.
If menstrual-like bleeding does not occur due to discontinuation of the drug after the completion of taking the drug from the second package, then pregnancy should be excluded before continuing to take the contraceptive
Measures taken in case of vomiting
If vomiting begins within 3-4 hours after taking the drug, then the active substance from the tablet is not completely absorbed. In this case, it is necessary to act according to the item "Missed pills". If the patient does not want to deviate from the regimen, the missed tablets should be taken from an additional package.
Acceleration or delay of the menstrual cycle
There is an opportunity to accelerate the menstrual cycle, with a shortening of the break in taking the drug. The shorter the break in taking the drug, the more likely it is that menstrual-like bleeding will not occur, and breakthrough or spotting bleeding will occur while taking the drug from the next package.
To delay menstruation, the drug should be continued from a new package without interrupting the drug. Menstruation can be delayed for as long as necessary at the end of the last pill from the second package. With a delay in menstruation, breakthrough or spotting bleeding may occur. Regular intake of the drug Lindinet 20 or Lindinet 30 can be restored after the usual 7-day break.
Side effects.
In the first period of taking the drug, 10-30% of women may experience such side effects: tension of the mammary glands, deterioration of health, spotting bleeding. These side effects are usually mild and disappear after 2-4 cycles.
Other possible side effects
Among women taking Lindinet 20 or Lindinet 30, the following side effects may occur: nausea, vomiting, headache, breast tension, changes in weight and libido, depressed mood, chloasma, bleeding disorders, complaints when wearing contact lenses.
Rarely, increases in the level of triglycerides and blood sugar, decreased glucose tolerance, increased blood pressure, thromboembolism, hepatitis, liver adenoma, gallbladder disease, jaundice, skin rashes, hair loss, changes in the consistency of vaginal discharge, fungal infection of the vagina, unusual fatigue, diarrhea.
Contraindications.
The drug Lindinet 20 or Lindinet 30 should not be taken in the following cases:
during pregnancy or if it is suspected;
with active or history of arterial or venous thromboembolic diseases (for example: deep vein thrombophlebitis, pulmonary thromboembolism, cerebrovascular disorders, myocardial infarction);
if there is a risk of arterial or venous thromboembolism (diseases of the hemostasis system, heart disease, atrial fibrillation);
in the presence of a benign or malignant tumor or severe liver disease,
in the presence of a history of malignant tumors of the uterus or mammary glands;
with bleeding from the vagina of unclear etiology;
in the presence of a history of cholestatic jaundice of pregnancy or itching of pregnant women;
with a history of herpes in pregnant women;
with the progress of otosclerosis bath during a previous pregnancy;
with sickle cell anemia;
with hyperlipidemia;
with severe hypertension;
diabetic angiopathy;
with hypersensitivity to the constituent components of the drug.
Overdose
After taking large doses of Lindinet 20 or Lindinet 30, severe symptoms are unknown. Signs of overdose: nausea, vomiting, in young girls, slight vaginal bleeding. The drug has no specific antidote, treatment is symptomatic.
Application features.
Diseases of the circulatory system.
Oral contraceptives increase the risk of myocardial infarction. The risk of myocardial infarction is higher in smokers and have other risk factors such as hypertension, hypercholesterolemia, obesity and diabetes mellitus.
Lindinet 20 or Lindinet 30 should be administered with caution to women who are at risk of cardiovascular disease.
The use of the drug Lindinet 20 or Lindinet 30 increases the risk of developing cerebrovascular diseases and venous thromboembolic disorders.
The risk of developing venous thromboembolic disease (VTZ) increases in the first year of drug use among those women who have not yet taken such drugs. This risk is much less than the risk of VTS in pregnant women. Out of 100,000 pregnant women, about 60 have VTS and 1-2% of all cases of VTS end in death.
The incidence of VTS among women taking 50 mcg or less of ethinylest radiol in combination with levonorgestrel is approximately 20 cases out of 100,000 women per year. The incidence of VTS among women taking gestodene in combination is approximately 30-40 cases per 100,000 women per year. For those women who have previously observed high blood pressure or conditions associated with high blood pressure, or had kidney disease, it is not recommended to use Lindinet 20 or Lindinet 30. If, despite this, a woman with hypertension wants to take oral contraceptives , it is necessary to keep it under strict control and if there is a significant increase in blood pressure, the drug should be discontinued.
In most women, blood pressure returns to normal with discontinuation of the drug, and in the future, an increased risk of hypertension is uncharacteristic.
An increase in blood pressure was more often observed in older women, as well as with prolonged use.
Smoking significantly increases the risk of cardiovascular complications that may occur when using Lindinet 20 or Lindinet 30. This risk increases with age, so in women over 35 years of age and those who smoke a lot, the risk of cardiovascular complications increases significantly. Women who are taking oral contraceptives are advised to stop smoking.
The risk of arterial venous or thromboembolic diseases increases:
with age;
when smoking (severe burning sensation and age, especially over 35 years old, is an additional risk factor);
with a positive family history (for example: diseases of the father of an abbot, sister at a young age). If there is a congenital tendency to thromboembolic diseases, it is necessary to consult a specialist before using the drug;
with obesity (body mass index above 30 kg/m2);
in violation of fat metabolism (dyslipoproteinemia);
with hypertension;
with diseases of the heart valves;
atrial fibrillation
with prolonged immobilization, severe operations, operations on the lower extremities, severe injuries. Due to the fact that the risk of thromboembolic diseases increases in the postoperative period, it is proposed to stop taking the drug 4 weeks before the planned operation and start taking it 2 weeks after the patient is remobilized.
Taking the drug Lindinet 20 or Lindinet 30 should be stopped immediately if such signs of thromboembolism appear: chest pain, radiating to the left arm, unusually severe pain in the legs, swelling of the legs, stabbing pain when inhaling or coughing, bloody discharge from the bronchi.
Biochemical indicators indicating a tendency to thromboembolic diseases: resistance to activated protein C (APC), hyperhomocysteinemia, deficiency of antithrombin III, protein C and protein S, the presence of antiphospholipid antibodies (anticardiolipin, lupus anticoagulant).
Tumors.
Some studies have reported an increase in cervical cancer among women who have taken oral contraceptives for a long time, but the results are mixed. The likelihood of developing cervical cancer depends on sexual behavior and other factors (for example: human papillomavirus).
Identified cases of breast cancer in women taking oral contraceptives were clinically at an earlier stage than in women who did not take these drugs.
There are isolated reports of the development of a benign liver tumor in women who have been taking hormonal contraceptives for a long time.
Among women who take oral contraceptives for a long time, the development of a malignant tumor of the liver has occasionally been observed.
Other pathological conditions.
When using oral contraceptives, retinal thrombosis can sometimes form. The drug should be discontinued in case of loss of vision (complete or partial), exophthalmos, diplopia or swelling of the nipple of the optic nerve or disturbances in the vessels of the retina.
With the appearance or intensification of migraine attacks, with the appearance of a constant or repeated unusually severe headache, the drug should be discontinued.
Taking the drug Lindinet 20 or Lindinet 30 should be stopped immediately if itching occurs, or with the onset of an epileptic seizure.
Studies show that the relative risk of developing gallstones increases with age among women taking oral contraceptives or drugs containing estrogens. Recent studies have shown that the risk of gallstone disease is low when using drugs with a low dose of hormones.
Influence on the metabolism of carbohydrates and lipids
Among women taking Lindinet 20 or Lindinet 30, there may be a decrease in carbohydrate tolerance. In this regard, women with diabetes who take Lindinet 20 or Lindinet 30 should be closely monitored.
In some women, when using oral contraceptives, an increase in the level of three glycerides in the blood was found. A number of progestogens reduce the level of cholesterol HDL) HDL in blood plasma. Due to the fact that estrogen increases the level of cholesterol HDL) HDL in blood plasma, the effect of Lindinet 20 or Lindinet 30 on lipid metabolism depends on the ratio of estrogens and progestogen and on the dose and form of progestogen.
Careful monitoring of women who have hyperlipidemia and who, despite this, decide to take contraceptives should be carried out carefully.
Among those women who have hereditary hyperlipidemia and who took the drug with estrogen, a sharp increase in plasma triglycerides was found, which could lead to the development of pancreatitis.
Bleeding.
When using the drug Lindinet 20 or Lindinet 30, especially in the first three months, irregular (breakthrough) bleeding may occur. If such bleeding is present for quite a long time or appears after regular cycles have formed, their cause is usually non-hormonal and an appropriate gynecological examination should be performed to rule out pregnancy or malignant tumors. If a non-hormonal cause can be excluded, it is necessary to switch to another drug.
In some cases, menstrual-like bleeding after discontinuation of the drug during a 7-day break does not appear. If the regimen of taking the drug was violated before the absence of bleeding or if there is no bleeding after taking the second package, then pregnancy must be excluded to continue the course of taking the drug.
Conditions requiring special care
Before starting the use of the drug Lindinet 20 or Lindinet 30, it is necessary to collect a detailed family history, conduct a general medical and gynecological examination. These studies should be repeated regularly. At physical examination, blood pressure should be measured, breast examination, abdominal palpation, gynecological examination with a cytological smear, and laboratory tests.
A woman should be warned that the drug does not protect her from sexually transmitted infections, in particular from AIDS.
In acute or chronic hepatic impairment, the drug should be discontinued until normalization of liver enzymes. In violation of the function of liver enzymes, the metabolism of steroid hormones may be disturbed.
For those women who develop depression while taking contraceptives, it is advisable to stop the drug and temporarily switch to another method of contraception to determine the cause of the depressive state. Women with a history of depression should be closely monitored and oral contraceptives should be discontinued if depression returns.
When using oral contraceptives, the level of folic acid in the blood may decrease. This is of clinical significance only if conception occurs shortly after completion of the oral contraceptive course.
In addition to the conditions listed above, you need to pay special attention to the stanzhinki in the presence of the following diseases: otosclerosis, multiple sclerosis, epilepsy, chorea minor, intermittent porphyria, tetanic conditions, renal failure, obesity, systemic lupus erythematosus, uterine fibroids.
Pregnancy, breastfeeding.
The use of the drug immediately before pregnancy or in the early stages of pregnancy does not affect the development of the fetus.
The use of hormonal contraceptives during breastfeeding is not recommended, as these drugs reduce milk secretion, change its composition, and also penetrate milk in small amounts.
Interaction with other drugs.
With the simultaneous use of rifampicin and Lindinet 20 or Lindinet 30, the effect of the hormonal drug is reduced. The incidence of breakthrough bleeding and bleeding disorders is increased. There is a similar interaction between the drug Lindinet 20 or Lindinet 30 and barbiturates, phenylbutazone, phenytoin, griseofulvin, ampicillin, tetracycline. Those women who receive such drugs at the same time as an oral contraceptive are encouraged to use additional non-hormonal (condom, spermicidal gels) methods of contraception. Such methods of contraception should be used when using the above drugs and within 7 days after the completion of the course. When using rifampicin, additional methods of contraception should be used within 4 weeks after completing the course of taking it.
Interactions associated with the absorption of the drug. With diarrhea, intestinal motility increases and the absorption of hormones decreases. Any drug, by its action, reduces the time of the presence of a hormonal drug in the large intestine, reduces the level of the hormone in the blood.
Interactions associated with drug metabolism.
Intestinal wall: ethinylest radiol sulfation occurs in the intestinal wall. Drugs (for example: ascorbic acid), which are also amenable to sulfation in the intestinal wall, inhibit this process, increase the bioavailability of ethinylest radiol.
Metabolism in the liver: drugs that activate microsomal liver enzymes, and thereby reduce the level of ethinylest radiol in blood plasma (for example: rifampicin, barbiturates, phenylbutazone, phenytoin, griseofulvin, topiramate). Liver enzyme inhibitors (itraconazole, fluconazole) and thus increase the level of ethinylest radiol in blood plasma.
Effects on intrahepatic circulation: Some antibiotics (ampicillin, tetracycline) inhibit the intrahepatic circulation of estrogen, thereby reducing plasma rivenetinylest radiol.
Influence on the metabolism of other drugs: ethinylestradiol can affect the metabolism of other drugs by blocking liver enzymes or accelerating conjugation (primarily glucuronidation). Therefore, the level of other drugs in the blood may increase or decrease (for example: cyclosporine, theophylline).
The use of other drugs or St. The reason for this is the inducing effect of St. John's wort on liver enzymes, which lasts another 2 weeks after the completion of St. John's wort.
With the simultaneous use of riton ver and an oral contraceptive, a drug with a higher dose of etinilest radiol should be used or non-hormonal methods of contraception should be used.
Under the influence of oral contraceptives, the level of some laboratory parameters (indicators of the function of the liver, kidneys, adrenal glands, thyroid gland, blood coagulation system and fibrinolytic factors, lipoproteins and transport proteins) may change. Despite this, the indicators remain within the normal range.
Storage conditions.
Store at a temperature of 15 - 300C.
Best before date- 3 years.
