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Active ingredients
Levonorgestrel + Ethinyl Estradiol
Release form
Pills
Composition
Active ingredient: 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, Active ingredient concentration (mg): 0.08 mg, 0.115 mg, 0.155 mg
Pharmacological effect
Combined (three-phase) oral contraceptive estrogen-progestin drug. Inhibits pituitary secretion of gonadotropic hormones. Sequential administration of pills containing different amounts of gestagen (levonorgestrel) and estrogen (ethinyl estradiol) provides these blood levels 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 (LH and FSH) of the hypothalamus occurs, the secretion of pituitary gonadotropic hormones is inhibited by the pituitary gland, which leads to inhibition of maturation and release of the ovum (ovulation) ready for fertilization. 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 7-day periods, when there should be another break in taking the drug, uterine bleeding occurs.
Pharmacokinetics
LevonorgestrelSuctionLevonorgestrel is rapidly absorbed (less than 4 hours). Not affected by first pass through the liver. Distribution and excretion Most of the levonorgestrel in the blood is associated with albumin and globulin that binds sex hormones. T1 / 2 is 8-30 hours (average 16 hours). 60% of levonorgestrel is excreted by the kidneys, 40% through the intestines. Ethinyl estradiol Absorption and metabolism Ethinyl estradiol is rapidly and almost completely absorbed from the gastrointestinal tract. Cmax in plasma is achieved in the range of 1-1.5 h. Ethinyl estradiol is subject to the effect of the first passage through the liver. Metabolism is carried out in the liver and intestines. Withdrawal When ingested, 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. 40% of ethinyl estradiol is excreted by the kidneys and 60% through the intestines. T1 / 2 is 26 ± 6.8 h.
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, gallbladder, otosclerosis with worsening of the course during the previous pregnancy and (tey); 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
With care: compensated diabetes mellitus without vascular complications, arterial hypertension with systolic / diastolic blood pressure up to 160/100 mm Hg, varicose disease, multiple sclerosis, epilepsy, minor chorea, porphyria, tetany, bronchial asthma, teenage age (without ovulatory cycles), uterine myoma, mastopathy, depression, tuberculosis.
Use during pregnancy and lactation
In pregnancy and lactation, the use of the drug Tri-Regol is contraindicated.
Dosage and administration
To accept inside, without chewing and washing down with a small amount of liquid. From the first day of menstruation, for 28 days, take one coated tablet each day, preferably at the same time of day. Menstrual-like bleeding occurs while taking red-brown coated pills. The reception of pills from the next package should be started without observing the interval between the two packages, i.e. 4 weeks after the start of the drug, on the same day of the week. It is important to observe the following order of taking the pills: first 6 pink follow, then 5 white, then 10 dark yellow, and 7 reddish brown at the end. In order to ensure the necessary priority on the package numbers and arrow are indicated. With good portability, take the drug as long as there is a need for contraception. The transition to the drug Tri-Regol 21 + 7 from another oral contraceptive is carried out according to the same scheme. After an abortion, it is recommended to start taking the drug on the day of the abortion or the day after the operation. After birth, the drug can be recommended only to women who are not breastfeeding; Reception should begin no earlier than the first day of menstruation. During lactation, the use of the drug is contraindicated. Missed pills: missed pills should be taken within the next 12 hours. If 36 hours have passed since the last pill was taken, contraception is unreliable. In such cases, to prevent possible intermenstrual bleeding, the drug should be continued from the already started packaging, with the exception of the missed tablet (s). In the case of skipping the timely taking of pills, it is recommended to use another, additional, non-hormonal method of contraception (for example, barrier). This rule does not apply to pills of reddish-brown color, since they do not contain hormones.
Side effects
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. Usually the drug is well tolerated. Possible side effects that are transient in nature and do not require treatment: nausea,vomiting, headache, engorgement of the mammary glands, weight gain, decreased 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 withdrawal without appointment of any therapy). Increase in the concentration of triglycerides, blood glucose, decreased glucose tolerance, increased blood pressure, hepatitis, liver adenoma, gallbladder disease (eg, cholelithiasis, cholecystitis), thrombosis and venous thromboembolism, jaundice, skin rash, hair loss, increased secretions from the vagina, vaginal candidiasis, fatigue, diarrhea. Very rarely, with a longer reception: chloasma. Iron fumarate, which is a part of reddish-brown sugar-coated pills, can cause irritation of the gastrointestinal tract mucosa, nausea, vomiting, diarrhea, constipation and dye black in feces.
Overdose
Symptoms: nausea, uterine bleeding. Treatment: when the first signs of overdose appear in the first 2-3 hours, gastric lavage and symptomatic treatment are recommended. There is no antidote.
Interaction with other drugs
With simultaneous use with the drug Tri-Regol ampicillin, rifampicin, chloramphenicol, neomycin, polymyxin B, sulfonamides, tetracyclines, dihydroergotamine, tranquilizers, phenylbutazone can weaken the contraceptive effect. These combinations should be used with caution; It is recommended to use a different, non-hormonal method of contraception. When using the drug Tri-Regol with anticoagulants derived from coumarin or indandion, an extraordinary determination of the prothrombin index and changing the dose of the anticoagulant may be needed. possible increase in bioavailability and therefore increased toxicity. With simultaneous use of the drug Tri-Regol and ne pill hypoglycemic drugs, insulin may need to change their dosage. With the simultaneous use of the drug Tri-Regol and bromocriptine, the effectiveness of the latter decreases. With simultaneous use of the drug Tri-Regol and drugs with a possible hepatotoxic effect, primarily dantrolene, the risk of increasing hepatotoxicity increases,especially in women over 35 years old.
special instructions
Before starting the drug, it is necessary to exclude pregnancy, conduct a general medical and gynecological examination (examination of the mammary glands, smear cytology). A regular gynecological examination is required every 6 months while taking the drug. The use of oral contraceptives is allowed not earlier than 6 months after suffering viral hepatitis and on condition of normalization of hepatic functions. In case of severe pain in the upper abdomen, hepatomegaly or intra-abdominal symptoms In a hemorrhage, a liver tumor may be suspected. In this case, taking the drug should be discontinued. If acyclic bleeding occurs, it is possible to continue taking Tri-Regol after excluding the organic pathology by the attending physician. In identifying abnormal liver functions during the use of the drug, decide whether to continue taking Tri-Regol. vomiting or diarrhea, the drug should be continued, it is recommended to additionally use another, non-hormonal method of contraception. Not less than 3 months before we plan During pregnancy, taking the drug must be discontinued. Under oral contraceptives (due to the estrogen component), some laboratory parameters (liver, kidney, adrenal, thyroid, blood clotting and fibrinolytic factors, lipoprotein levels and transport proteins) may change. Reception the drug should be immediately discontinued in the following cases: when a migraine-like or unusually severe headache first arises or intensifies, with acute impairing its correct visual acuity, with suspected thrombosis or heart attack; 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 long-term immobilization (for example, after injuries). Impact on the ability to drive vehicles and control mechanisms Reception of the drug does not affect the ability to drive and work with other mechanisms.