Lindinet 20, pills, 63pcs

Composition

1 tablet contains:

active ingredients:

ethinyl estradiol 20 mcg;

gestodene 75 mcg;

excipients:  

sodium calcium edetate,

magnesium stearate,

colloidal anhydrous silicon,

povidone,

corn starch,

lactose monohydrate;

Shell composition:

D+C yellow N 10 S. I. 47005,

E 104,

povidone,

titanium oxide C. I. 7791,

E 171, macrogol 6000;

talc,

calcium carbonate,

sucrose.

Pharmacological action

Lindinet is a combined remedy, the action of which is due to the effects of the components that make up its composition. It inhibits the pituitary secretion of gonadotropic hormones.

The contraceptive effect of the drug is associated with several mechanisms. The estrogenic component of the drug is a highly effective oral drug — ethinyl estradiol (a synthetic analog of estradiol, which is involved together with the corpus luteum hormone in the regulation of the menstrual cycle). The progestogenic component is a derivative of 19-nortestosterone — gestodene, which surpasses in strength and selectivity of action not only the natural yellow body hormone progesterone, but also modern synthetic progestogens (levonorgestrel). Due to its high activity, gestoden is used in very low dosages, in which it does not show androgenic properties and practically does not affect lipid and carbohydrate metabolism.

Along with these central and peripheral mechanisms that prevent the maturation of a fertilized egg, 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 mucus located 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, including those of a tumor nature.

Pharmacokinetics

Gestoden

Suction. When taken orally, it is rapidly and completely absorbed. After taking a single dose, Cmax in plasma is measured in one hour and is 2-4 ng / ml. Bioavailability is about 99%.

Distribution. It binds to albumin and sex hormone binding globulin (SHBG).1-2% are in the free state,50-75% are specifically bound to SHBG. An increase in SHBG levels due to ethinyl estradiol affects gestodene levels, leading to an increase in the SHBG-related fraction and a decrease in the albumin-related fraction. Gestoden’s Vd is 0.7-1.4 l / kg.

Metabolism. Corresponds to the metabolism of steroids. The average plasma clearance is 0.8-1 ml / min / kg.

Output. The blood level decreases in two stages. The end-phase half-life is 12-20 hours. It is excreted exclusively in the form of metabolites-60% in the urine,40% in the feces. T1 / 2 of metabolites — approximately 1 day.

Stable concentration. The pharmacokinetics of gestodene largely depend on the level of SHBG. Under the influence of ethinyl estradiol, the concentration of SHBG in the blood increases by 3 times; with daily use of the drug, the level of gestodene in plasma increases by 3-4 times and in the second half of the cycle reaches a state of saturation.

Ethinyl Estradiol

Suction. When taken orally, it is absorbed quickly and almost completely. Cmax in the blood is measured after 1-2 hours and is 30-80 pg / ml. Absolute bioavailability ” of 60% (due to presystemic conjugation and primary metabolism in the liver).

Distribution. Easily enters into a non-specific relationship with blood albumin (about 98.5%) and causes an increase in SHBG levels. The average Vd is 5-18 l / kg.

Metabolism. It is mainly carried out by aromatic hydroxylation with the formation of large amounts of hydroxylated and methylated metabolites, which are partly in free, partly in conjugated form (glucuronides and sulfates). Plasma clearance “5-13 ml/min/kg.

Output. The serum concentration is reduced in 2 steps. T1 / 2 in the second phase ” 16-24 hours It is excreted exclusively in the form of metabolites in a ratio of 2: 3 in the urine and bile. T1 / 2 metabolites “1 day.

Stable concentration. It is established by day 3-4, and the level of ethinyl estradiol is 20% higher than after taking a single dose.

Indications

Contraception.

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy.

If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be decided.

The active ingredients of the drug are excreted in small amounts in breast milk, affecting the quantity and quality of milk.

Contraindications

• individual hypersensitivity to the drug or its components;
• the presence of a severe or multiple risk factors for venous or arterial thrombosis (including complicated lesions of valvular apparatus of the heart, atrial fibrillation, vascular diseases of the brain or coronary arteries);
• uncontrolled hypertension moderate or severe AD 160/100 mm Hg. station and more);
• the harbingers of thrombosis (including transient ischemic attack, angina), including in the anamnesis;
• migraine with focal neurological symptoms, including in the anamnesis;
• venous or arterial thrombosis/thromboembolism (including deep vein thrombosis of the leg, pulmonary embolism, myocardial infarction, stroke) in real time or history;
• the presence of venous thromboembolism in relatives;
• major surgery with prolonged immobilization;
• diabetes mellitus (with the presence of angiopathy);
• pancreatitis (including in history), accompanied by severe hypertriglyceridemia;
• dyslipidemia;
• severe liver disease, cholestatic jaundice (including during pregnancy), hepatitis, including history (up to the normalization of functional and laboratory parameters and for 3 months after the return of these parameters to normal);
• jaundice as a result of taking drugs that contain steroids;
• cholelithiasis in real time or history;
• Gilbert syndrome, Dubin-Johnson, Rotor;
• liver tumors (including in history);
• severe itching, otosclerosis or progression of otosclerosis during a previous pregnancy, or if the GCS;
• hormone-dependent malignancies of the genital organs and mammary glands (including suspicion of them);
• vaginal bleeding of unknown etiology;
• the Smoking age 35 years (more than 15 cigarettes a day);
• pregnancy or suspicion of it;
• lactation.

With caution: conditions that increase the risk of venous or arterial thrombosis/thromboembolism (age over 35 years, smoking, hereditary predisposition to thrombosis — thrombosis, myocardial infarction or cerebral circulation disorders at a young age in one of the closest relatives); hemolytic uremic syndrome; hereditary angioedema; liver diseases; diseases that first occurred or worsened during pregnancy or against the background of previous use of sex hormones (including porphyria pregnancy herpes, chorea minor-Sydenham’s disease, Sydenham’s chorea, chloasma); obesity (body mass index more than 30); dyslipoproteinemia; arterial hypertension; migraine; epilepsy; valvular heart defects; atrial fibrillation; prolonged immobilization; extensive surgery; surgery on the lower extremities; severe trauma; varicose veins and superficial thrombophlebitis; postpartum period (non — lactating women — 21 days after delivery; lactating women — after the end of lactation); presence of severe depression, including in the anamnesis; changes in biochemical parameters (activated protein C resistance, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant); diabetes mellitus, not complicated by vascular disorders; systemic lupus erythematosus (SLE); Crohn’s disease; ulcerative colitis; sickle cell anemia; hypertriglyceridemia (including family history); acute and chronic liver diseases.

Side effects

Side effects that require immediate discontinuation of the drug:

– arterial hypertension;

– hemolytic-uremic syndrome;

– porphyria;

– hearing loss due to otosclerosis.

Rare-arterial and venous thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary embolism); exacerbation of reactive SLE.

Very rare-arterial or venous thromboembolism of the hepatic, mesenteric, renal, retinal arteries and veins; Sydenham’s chorea (passing after discontinuation of the drug).

Other side effects, less severe, but more common — the expediency of continuing to use 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 of the vagina (for example, candidiasis), changes in libido.

From the mammary glands: tension, pain, enlargement of the mammary glands, galactorrhea.

From the gastrointestinal tract and hepatobiliary system: nausea, vomiting, diarrhea, epigastric pain, Crohn’s disease, ulcerative colitis, hepatitis, liver adenoma, occurrence or exacerbation of jaundice and / or itching associated with cholestasis, cholelithiasis.

Skin disorders: nodular / exudative erythema, rash, chloasma, increased hair loss.

From the central nervous system: headache, migraine, mood swings, depressive states.

Metabolic disorders: fluid retention in the body, changes (increase) in body weight, increased triglycerides and blood sugar, decreased tolerance to carbohydrates.

From the sensory organs: hearing loss, increased sensitivity of the cornea of the eye when wearing contact lenses.

Other: allergic reactions.

Interaction

The contraceptive effect of oral contraceptives decreases with the simultaneous use of rifampicin, breakthrough bleeding and menstrual disorders become more frequent. A similar, but less well-understood, interaction exists between contraceptives and carbamazepine, primidone, barbiturates, phenylbutazone, phenytoin, and presumably griseofulvin, ampicillin, and tetracyclines. During treatment with the above drugs, it is recommended to use an additional method of contraception (condom, spermicidal gel) simultaneously with oral contraception. After completing the course of treatment, the use of an additional method of contraception should be continued for 7 days, in the case of rifampicin treatment – for 4 weeks.

Interactions associated with drug absorption

During diarrhea, the absorption of hormones decreases (due to increased intestinal motility). Any drug that shortens the time that a hormone is present in the large intestine leads to low concentrations of the hormone in the blood.

Interactions related to drug metabolism

The intestinal wall. Drugs that undergo sulfation in the intestinal wall like ethinyl estradiol (for example, ascorbic acid) inhibit metabolism and increase the bioavailability of ethinyl estradiol.

Metabolism in the liver. Inducers of microsomal liver enzymes reduce the level of ethinyl estradiol in blood plasma (rifampicin, barbiturates, phenylbutazone, phenytoin, griseofulvin, topiramate, hydantoin, felbamate, rifabutin, oxcarbazepine). Liver enzyme blockers (itraconazole, fluconazole) increase the level of ethinyl estradiol in the blood plasma.

Effect on intrahepatic circulation. Some antibiotics (for example ampicillin, tetracycline), interfering with the intrahepatic circulation of estrogens, reduce the level of ethinyl estradiol in plasma.

Effect on the metabolism of other drugs

By blocking liver enzymes or accelerating conjugation in the liver, mainly increasing glucuronidation, ethinyl estradiol affects the metabolism of other drugs (for example, cyclosporine, theophylline), leading to an increase or decrease in their plasma concentrations.

Concomitant use of St. John’s wort (Hypericum perforatum) with Lindinet 20 tablets is not recommended (due to a possible decrease in the contraceptive effect of the active substances of the contraceptive, which may be accompanied by the appearance of breakthrough bleeding and unwanted pregnancy). St. John’s wort activates liver enzymes; after stopping taking St. John’s wort preparations, the effect of enzyme induction may persist for the next 2 weeks.

Concomitant use of ritonavir and a combined contraceptive is accompanied by a 41% decrease in the average ethinyl estradiol AUC. During treatment with ritonavir, it is recommended to use a drug with a high content of ethinyl estradiol or a non-hormonal method of contraception. It may be necessary to adjust the dosage regimen when using hypoglycemic agents, since oral contraceptives can reduce carbohydrate tolerance, increase the need for insulin or oral antidiabetic agents.

How to take, course of use and dosage

Inside, without chewing, with a sufficient amount of water, regardless of the meal.

Take 1 table each. per day (if possible at the same time of day) for 21 days. Then, after taking a 7-day pill break, resume oral contraception (i. e. 4 weeks after taking the 1st pill, 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 20 should be started from the 1st to the 5th day of the menstrual cycle.

Switching from a combined oral contraceptive to taking the drug Lindinet 20. The 1st table of the drug Lindinet 20 is recommended to be taken after taking the last hormone-containing tablet of the previous drug, on the 1st day of withdrawal bleeding.

Transition from progestogen-containing drugs (mini-tablets, injections, implants) to taking Lindinet 20. The transition from mini-pills can be started on any day of the menstrual cycle; in the case of an implant, on the day after its removal; in the case of injections, on the eve of the last injection.

At the same time, in the first 7 days of taking the drug Lindinet 20, an additional method of contraception should be used.

Taking the drug Lindinet 20 after an abortion in the first trimester of pregnancy. You can start taking a contraceptive immediately after an abortion, and there is no need to use an additional method of contraception.

Taking the drug Lindinet 20 after childbirth or after an abortion in the second trimester of pregnancy. You can start taking a contraceptive on the 21st-28th day after giving birth or having an abortion in the second trimester of pregnancy. At a later start of taking a contraceptive, in the first 7 days, it is necessary to use an additional, barrier method of contraception. In cases where sexual contact took place before the start of contraception, before starting 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 intake was missed, then you should make up for the missed dose as soon as possible. If the delay does not exceed 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, the drug is continued as usual, but in the next 7 days it is necessary to use an additional method of contraception. If at the same time there were less than 7 tablets left in the package, then they start taking tablets from the next package without observing a break. In such cases, uterine withdrawal bleeding occurs only at the end of the 2nd package; while taking tablets from the 2nd package, smearing or breakthrough bleeding is possible.

If withdrawal bleeding does not occur at the end of taking tablets from the 2nd package, then the presence of pregnancy should be excluded before continuing to take the contraceptive.

Measures taken in case of vomiting and diarrhea. If vomiting occurs in the first 3-4 hours after taking the next tablet, the tablet is not completely absorbed. In such cases, follow the instructions described in Missed Pills.

If the patient does not want to deviate from the usual contraceptive regimen, the missed pills should be taken from a different package.

Delayed menstruation and accelerated timing of menstruation. In order to delay menstruation, taking tablets from a new package is started without taking a break. Menstruation can be delayed at will until all the tablets from the 2nd package run out. If menstruation is delayed, breakthrough or spotting uterine bleeding is possible. You can return to the usual pill intake after observing a 7-day break.

In order to prevent the onset of menstrual bleeding earlier, you can shorten the 7-day break by the desired number of days. The shorter the break, the more likely it is that breakthrough or spotting bleeding will occur while taking pills from the next package (similar to cases with delayed menstruation).

Overdose

High-dose contraceptive use was not associated with the development of severe symptoms.

Symptoms: nausea, vomiting, small vaginal bleeding in young girls.

Treatment: symptomatic, no specific antidote.

Special instructions

Before starting to use the drug, it is recommended to collect a detailed family and personal history and then undergo a general medical and gynecological examination every 6 months (examination by a gynecologist, cytological smear examination, examination of mammary glands and liver function, blood pressure monitoring, cholesterol concentration in the blood, urine analysis). These studies should be repeated periodically due to the need for timely identification of risk factors or contraindications.

The drug is a reliable contraceptive drug-the Pearl index (an indicator of the number of pregnancies that occurred during the use of the method of contraception in 100 women within 1 year) when used correctly is about 0.05. Due to the fact that the contraceptive effect of the drug from the start of use is fully manifested by the 14th day, then 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 taking them are individually evaluated. This issue should be discussed with the patient, who, after receiving the necessary information, will make a final decision on the preference for hormonal or any other method of contraception. A woman’s health status should be carefully monitored.

If any of the following conditions/diseases appear or worsen while taking the drug, you should stop taking the drug and switch to another, non-hormonal, method of contraception:

– diseases of the hemostatic system;

– conditions/diseases of, predisposing to the development of cardiovascular, renal failure;

– epilepsy;

– migraine;

– the risk of estrogen-dependent tumors or estrogen-dependent gynecological diseases;

diabetes mellitus that is not