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Active ingredients
Levonorgestrel + Ethinyl Estradiol
Release form
Pills
Composition
Ethinyl estradiol 30 mcg, levonorgestrel 150 mcg.
Pharmacological effect
Combined monophasic oral hormonal contraceptive drug. When ingestion inhibits pituitary secretion of gonadotropic hormones. The contraceptive effect is associated with several mechanisms. As a gestagen component (progestin) contains a derivative of 19-nortestosterone - levonorgestrel, surpassing the activity of the corpus luteum hormone progesterone (and the synthetic analogue of the latter - pregnin), acts at the receptor level without prior metabolic transformations. Ethinyl estradiol is an estrogen component. Under the influence of levonorgestrel, a blockade of LH and FSH release from the hypothalamus occurs, suppression of pituitary gonadotropic hormone secretion by the pituitary gland, which leads to inhibition of maturation and release of an egg (ovulation) ready for fertilization. Contraceptive action is enhanced by ethinyl estradiol. Retains a high viscosity of the cervical mucus (makes it difficult for sperm to enter the uterus). Along with the contraceptive effect with regular use, it normalizes the menstrual cycle and helps prevent the development of a number of gynecological diseases, including neoplastic nature.
Pharmacokinetics
Ethinyl estradiol Ethinyl estradiol is rapidly and almost completely absorbed from the intestines. Ethinyl estradiol is exposed to the first passage through the liver, Tmax is 1.5 hours, T1 / 2 is about 26 hours. When ingested, ethinyl estradiol is eliminated from blood plasma for 12 hours, T1 / 2 is 5.8 hours. Ethinyl estradiol is metabolized in the liver and intestines. Ethinyl estradiol metabolites - water-soluble sulfate or glucuronide conjugates, enter the intestine with bile, where they undergo disintegration using intestinal bacteria. Metabolized in the liver, T1 / 2 is 2-7 hours. Ethinyl estradiol is eliminated by the kidneys (40%) and through the intestines (60%) It is excreted with breast milk. LevonorgestrelAfter ingestion, levonorgestrel is rapidly absorbed (in less than 4 hours). Levonorgestrel is not exposed to the first-pass effect through the liver. When combined with the use of levonorgestrel with ethinyl estradiol, there is a relationship between dose and maximum plasma concentration. Tmax (time to reach maximum concentration) of levonorgestrel is 2 h, T1 / 2 - 8-30 h (average 16 h).Most of the levonorgestrel binds to albumin and SHBG (sex hormone-binding globulin) in the blood. Metabolized in the liver. Levonorgestrel is excreted by the kidneys (60%) and through the intestines (40%). It is secreted in breast milk.
Indications
Contraception; Hormone-dependent functional disorders of the menstrual cycle (including dysmenorrhea without an organic cause, menorrhagia without an organic cause, premenstrual syndrome).
Contraindications
Increased individual sensitivity to the components of the drug, pregnancy; breastfeeding period, liver failure, liver tumors; congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes); cholelithiasis; cholecystitis; chronic colitis; the presence or indication in the history of severe cardiovascular and cerebrovascular changes, thromboembolism and predisposition to them, decompensated heart defects; hormone-dependent malignant neoplasms of the genital organs and mammary glands (including suspicion of them), first of all, breast or endometrial cancer; disruption of fat metabolism; congenital hyperlipidemia; uncontrolled arterial hypertension of medium and severe degree with arterial pressure of 160/100 mm Hg. and higher; severe diabetes mellitus (accompanied by retinopathy and microangiopathy); sickle cell anemia; chronic hemolytic anemia; bleeding from the vagina of unknown etiology; migraine; otosclerosis (which worsened during a previous pregnancy); idiopathic jaundice, severe pruritus, herpes pregnant with a history of; pancreatitis (including history), accompanied by severe hyperlipidemia; jaundice due to medication containing steroids; smoking over the age of 35; age over 40 years.
Precautionary measures
Do not exceed the recommended dose. With caution, you should use the drug for diseases of the liver and gallbladder, epilepsy, depression, ulcerative colitis, uterine myoma, mastopathy, tuberculosis, kidney disease, diabetes, cardiovascular diseases, hypertension, and kidney function disorders , varicose veins, phlebitis, otosclerosis, multiple sclerosis, minor trochee, intermittent porphyria, latent tetany, bronchial asthma, in adolescence (without regular ovulatory cycles).
Dosage and administration
One tablet per day, preferably at the same time of day.If the woman in the previous cycle did not take a contraceptive, and the doctor did not prescribe otherwise, the first pill should be taken on the first day of menstruation and the pills should be continued for 21 days. Then taking the drug is recommended to continue reddish-brown pills for 7 days, during which menstrual-like bleeding occurs. After that, you should continue to take the next package containing 21 white pills, and then 7 pills of a reddish-brown color without a break. Thus, each cycle of administration begins on the same day of the week. In the event that a woman took a contraceptive in the previous cycle, and in the previous package was 21 pills, the drug should be taken after a 7-day break, on the eighth day. The composition of pills of different colors is not the same. Therefore, the beginning and the correct sequence of administration - first 21 white pills, then 7 reddish-brown pills - are indicated on the packaging with numbers and arrows. When switching to Rigevidon 21 + 7 from another contraceptive, you should use the above scheme. Taking the drug after childbirth or after an abortion can begin no earlier than the first day of the menstruation of the first two-phase cycle. The first biphasic cycle is usually shortened due to premature ovulation. If the drug begins already at the first spontaneous bleeding, the drug cannot successfully prevent premature ovulation, therefore, contraception may be unreliable in the first two weeks of the cycle. If the pill was missed within the prescribed period, then the missed pill should be taken within the next 12 hours. In this case, there is no need to use additional methods of contraception. The remaining pills are recommended to be taken at the usual time. If more than 12 hours have passed, you should take the last missed pill (skipping the rest of the unaccepted pills) and continue taking the drug as normal. In this case, in the next 7 days it is necessary to apply additional methods of contraception (barrier methods, spermicides). This does not apply to pills of a reddish-brown color, since they do not contain hormones. For therapeutic purposes, the dose of the drug and the scheme of use are selected by the doctor for each patient individually.
Side effects
Nausea, vomiting, headache, breast engorgement, weight gain and libido, depressed mood, intermenstrual bleeding, in some cases - eyelid edema, conjunctivitis, blurred vision, discomfort when wearing contact lenses (these phenomena are temporary and disappear after abolition without any therapy). With prolonged use, chloasma, hearing loss, generalized itching, jaundice, cramps of the gastrocnemius muscles, an increase in the frequency of epileptic seizures may very rarely occur. Rarely: an increase in triglycerides, blood glucose, decreased glucose tolerance, increased blood pressure, pulmonary embolism, thromboembolism, myocardial infarction, cardiovascular disorders, for example: cerebral vascular embolism, stroke, retinal thrombosis, mesenteric thrombosis, thrombosis of the brain, retinal thrombosis, mesenteric thrombosis, thrombosis of the brain, retinal thrombosis, retinal thrombosis, mesenteric thrombosis, cerebral thrombosis, retinal thrombosis, retinal thrombosis, mesenteric thrombosis, thrombosis, thrombosis pelvic, lower extremities, thrombophlebitis of the deep veins of the lower extremities, hepatitis, jaundice, skin rashes, hair loss, increased vaginal discharge, candida vagina, fatigue, diarrhea. Fumarate iron, which is part of the reddish-brown sugar-coated pills, can cause irritation of the mucous membrane of the gastrointestinal tract, nausea, vomiting, diarrhea, constipation and dye black in feces.
Overdose
Cases of toxic effects due to overdose are unknown.
Interaction with other drugs
Barbiturates, some antiepileptic drugs (carbamazepine, phenytoin), sulfonamides, pyrazolone derivatives can enhance the metabolism of steroid hormones that make up the drug. Reduced contraceptive efficacy can also be observed when administered concomitantly with some antimicrobial agents (including ampicillin, rifhymphymes, and simultaneous administration with some antimicrobial agents (including ampicillin, rifhymphymes, and concomitant administration with certain antimicrobial agents (including ampicillin, rifhymphyrme, and rifhymphycene). , neomycin, polymyxin B, sulfonamides, tetracyclines), which is associated with changes in the intestinal microflora. When used simultaneously with anticoagula Tami, coumarin derivatives or indandiona may require additional identification of prothrombin index and change in dose antikoagulyanta.Pri use of tricyclic antidepressants, maprotiline,beta-blockers may increase their bioavailability and toxicity. When using oral hypoglycemic drugs and insulin, it may be necessary to change their dose. When combined with bromocriptine, its effectiveness decreases. hepatotoxicity, especially in women over 35 years old.
special instructions
Cases of toxic effects due to overdose are unknown.