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Active ingredients
Levonorgestrel + Ethinyl Estradiol
Release form
Pills
Composition
Tablets I: contain 0.03 mg of ethinyl estradiol and 0.05 mg of levonorgestrel, Tablets II: contain 0.04 mg of ethinyl estradiol and 0.075 mg of levonorgestrel, Tablets III: contain 0.03 mg of ethinyl estradiol and 0.125 mg of levonorgestrel. Excipients: Tablets I. Core: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate (33.0 mg). Shell: sucrose, talc, calcium carbonate, titanium dioxide (E171), copovidone, macrogol 6000, colloidal silicon dioxide, povidone, carmellose sodium, iron red oxide (E172). Tablets II. Core: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate (33.0 mg). Shell: sucrose, talc, calcium carbonate, titanium dioxide (E171), copovidone, macrogol 6000, colloidal silicon dioxide, povidone, carmellose sodium. Tablets III. Core: colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate (33.0 mg).
Pharmacological effect
Combined (three-phase) oral contraceptive estrogen-progestin drug. When taking inhibits pituitary secretion of gonadotropic hormones. Sequential administration of coated pills, a preparation containing different amounts of progestogen (levonorgestrel) and estrogen (ethinyl estradiol) provides blood concentrations of these hormones close to their concentrations during the normal menstrual cycle and contributes to the secretory transformation of the endometrium. The contraceptive effect is associated with several mechanisms. Under the influence of levonorgestrel, the release of releasing factors (luteinizing and follicle-stimulating hormones) of the hypothalamus, suppression of secretion by the pituitary gonadotropic hormones, which leads to inhibition of maturation and release of the egg (ovulation) ready for fertilization, occurs. Ethinyl estradiol maintains a high viscosity of the cervical mucus (makes it difficult for sperm to enter the uterus). Along with the contraceptive effect, the menstrual cycle is normalized, thanks to the completion of the level of endogenous hormones with the hormonal components of the Tri-Regol pills ;. In the seven-day periods, when there should be another break in taking the drug, uterine bleeding occurs.
Pharmacokinetics
Levonorgestrel is rapidly absorbed (less than 4 hours). Levonorgestrel lacks the “first pass” effect through the liver. The half-life is 8-30 hours (average 16 hours). Most of the levonorgestrel in the blood binds to albumin and the globulin that binds sex hormones. Ethinyl estradiol is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum plasma concentration is reached in the range of 1-1.5 hours. The half-life is 26 ± 6.8 hours. Ethinyl estradiol has an effect of “first pass” through the liver (the so-called “first pass” effect). Metabolism is carried out in the liver and intestines. When ingestion, ethinyl estradiol is released within 12 hours from blood plasma. Metabolites of ethinyl estradiol: water soluble derivatives of sulfate or glucuronide conjugation, enter the intestine with bile, where they are disintegrated by intestinal bacteria. 60% of levonorgestrel is excreted by the kidneys, 40% through the intestines, 40% of ethinyl estradiol is excreted by the kidneys and 60% through the intestines.
Indications
Oral contraception.
Contraindications
Hypersensitivity to any component of the drug. Pregnancy, breastfeeding, severe liver disease, liver tumors, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), cholelithiasis, cholecystitis, chronic colitis; the presence or indication in the history of severe cardiovascular (including decompensated heart defects) and cerebrovascular changes, thromboembolism and predisposition to them, phlebitis of the lower veins of the lower extremities, hormone-dependent malignant tumors of the genitals and mammary glands (including suspicion of them), familial forms of hyperlipidemia, arterial hypertension with a systolic / diastolic arterial pressure of 160/100 mm Hg. and above, surgery, surgery on the lower extremities, prolonged immobilization, extensive injuries, pancreatitis (including a history of), accompanied by severe hypertriglyceridemia and hyperlipidemia, jaundice due to medications containing steroids, severe diabetes, sickle cell disease anemia, chronic hemolytic anemia, vaginal bleeding of unknown etiology, migraine, cystic swelling,otosclerosis with worsening of the course during the previous pregnancy (s); idiopathic jaundice in pregnant women, severe pruritus in pregnant women, herpes of pregnant women in history; smoking over the age of 35, age over 40; lactase deficiency, lactose intolerance, glucose-galactose malabsorption (in the medicinal form of the drug contains lactose).
Precautionary measures
Compensated diabetes mellitus without vascular complications, arterial hypertension with systolic / diastolic arterial pressure up to 160/100 mm Hg, varicose disease, multiple sclerosis, epilepsy, minor chorea, porphyria, tetany, asthma, adolescence (without regular ovulatory cycles ), uterine fibroids, mastopathy, depression, tuberculosis.
Use during pregnancy and lactation
During pregnancy and lactation, taking the drug Tri-Regol; contraindicated.
Dosage and administration
Use of the drug for the first time: Take inside, at the same time of the day, if possible in the evening, without chewing and washing it down with a small amount of liquid. For the purpose of contraception in the first cycle Tri-Regol; appoint daily on 1 tab. / day. for 21 days, starting from day 1 of the menstrual cycle, then a 7-day break is taken, during which typical menstrual bleeding occurs. Reception of the next package containing 21 coated pills should be started on the 8th day after the 7-day break. The drug is taken as long as there is a need for contraception. In the transition from another oral contraceptive to receive the drug Tri-Regol; apply a similar pattern. After an abortion, it is recommended to start taking the drug on the same or the next day after surgery. After delivery, the drug is recommended only for women who are not breastfeeding. Reception should begin no earlier than the first day of menstruation, cycle. During lactation, the use of the drug is contraindicated. If the woman did not take Tri-Regol; within the prescribed period, you should take the missed pill within the next 12 hours. If after taking the pill 36 hours have passed, contraception cannot be considered reliable. However, in order to avoid intermenstrual bleeding, it is necessary to continue taking the drug from the already started packaging minus the missed tablet (s). At this time, it is recommended to additionally use another, non-hormonal method of contraception (for example, barrier).
Side effects
The side effects observed with the use of the drug are classified into categories depending on the frequency of their occurrence: very often ≥1 / 10; often> 1/100, ≤1 / 10, sometimes ≥1 / 1000, ≤1 / 100; rarely ≥1 / 10000, ≤1 / 1000; very rarely ≤1 / 10,000 including individual messages. Nausea, vomiting, headache, engorgement of the mammary glands, increased body weight, decreased libido, depressed mood, chloasma, intermenstrual bleeding, in some cases - eyelid edema, conjunctivitis, blurred vision, discomfort when wearing contact lenses (these phenomena are temporary and disappear after cancellation without any therapy). Increased concentrations of triglycerides, blood glucose, decreased glucose tolerance, increased blood pressure, jaundice, hepatitis, liver adenoma, gallbladder disease (for example, cholelithiasis, cholecystitis) thrombosis and venous thromboembolism, skin rash, hair loss, increased excretion of vagina, vaginal candidiasis, fatigue, diarrhea. With prolonged use, very rarely, generalized itching, convulsions of the gastrocnemius muscles, hearing loss, an increase in the frequency of epileptic seizures, and coarsening of the voice may occur.
Overdose
Symptoms: nausea, uterine bleeding. Treatment: when the first signs of overdose appear in the first 2-3 hours, gastric lavage is recommended. Symptomatic therapy is indicated. There is no antidote.
Interaction with other drugs
The drug should be used with caution while taking: ampicillin, rifampicin, chloramphenicol, cahr, necrcr, nemitsin, polymyxin B, sulphonamides, tetracycline, rn, chenquilizers, phenylbutazone, since these drugs can weaken the contraceptive effect, it is recommended to cure, chenquilizers, phenylbutazone. coumarin or indandione (it may be necessary to determine the prothrombin index in an extraordinary manner and change the dose of the anticoagulant); antidepressants, maprotiline, beta-blockers (may increase bioavailability and therefore toxicity), oral hypoglycemic drugs, insulin (you may need to change their doses), bromocriptine (reduced efficacy), drugs with possible hepatotoxic effects, especially dantrolen (risk of increased hepatotoxicity, especially in women over 35).
special instructions
Before starting to use the drug, it is necessary to exclude pregnancy, conduct a general medical and gynecological examination (breast examination, cytological smear analysis). While taking the drug requires regular gynecological examination every 6 months. The use of oral contraceptives is allowed no earlier than 6 months after suffering viral hepatitis and subject to the normalization of hepatic functions. If a sharp pain in the upper abdomen, hepatomegaly or signs of intra-abdominal hemorrhage appears, a liver tumor may be suspected. In this case, the drug should be discontinued. With the appearance of acyclic bleeding, it is possible to continue taking Tri-Regol; after exclusion of organic pathology by the attending physician. In identifying abnormal liver functions during the use of the drug, the question of whether to continue taking Tri-Regol should be decided; In the case of vomiting or diarrhea, the drug should be continued, it is recommended to additionally use a different, non-hormonal method of contraception. At least 3 months before the planned pregnancy, the drug should be stopped. Under the action of oral contraceptives (due to the estrogen component), some laboratory parameters (liver, kidney, adrenal gland, thyroid gland, blood clotting and fibrinolytic factors, lipoprotein and transport protein levels) can change. The drug should be stopped immediately in the following cases : - in the case of a new or aggravated migraine-like or unusually severe headache, acute visual acuity, suspected thrombosis or nfarkt; - With a sharp increase in blood pressure, the appearance of jaundice or hepatitis without jaundice, the occurrence of generalized itching or increased epileptic seizures; - upon the occurrence of pregnancy; - 6 weeks before the planned operation, with prolonged immobilization (for example, after injuries). The effect of the drug on the ability to drive a car and other mechanisms Taking the drug does not affect the ability to drive a car and work with other mechanisms.