Etinylestradiol, Levonorgestrel | Tri-regol tablets, 63 pcs.

Latin name

Tri regol

Packaging

In 1 blister pack 6 tablets, coated with a pink coating, 5 tablets coated with a coating of white color, 10 tablets coated with a coating of dark yellow color. In a cardboard bundle 3 blisters.

Pharmacological action

Pharmacodynamics

Combined (three-phase) oral contraceptive estrogen-gestagen drug. When taken, inhibits the pituitary secretion of gonadotropic hormones.

Sequential administration of film-coated tablets of the drug, containing different amounts of gestagen (levonorgestrel) and estrogen (ethinyl estradiol) provides concentrations of these hormones in the blood, close to their concentrations during the normal menstrual cycle, and promotes secretory transformation of the endometrium. The contraceptive effect is associated with several mechanisms.

Under the influence of levonorgestrel, there is a blockade in the release of releasing factors (luteinizing and follicle-stimulating hormones) of the hypothalamus, inhibition of pituitary secretion of gonadotropic hormones, which leads to inhibition of maturation and the exit of the egg ready for fertilization (ovulation). Ethinyl estradiol maintains a high viscosity of cervical mucus (it makes it difficult for sperm to enter the uterine cavity). Along with the contraceptive effect, the menstrual cycle is normalized, due to the replenishment of the level of endogenous hormones with the hormonal components of Tri-Regol® tablets. In seven-day periods, when the next break in taking the drug follows, uterine bleeding occurs.

Pharmacokinetics of

Levonorgestrel is rapidly absorbed (less than 4 hours). Levonorgestrel does not have a “first pass” effect through the liver. The elimination half-life makes 8-30 hours (on average 16 hours). Most of the levonorgestrel in the blood binds to albumin and to sex hormone-binding globulin.

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 the “first pass” effect through the liver (the so-called “first pass” effect). Metabolism occurs in the liver and intestines.

When ingested, ethinyl estradiol is excreted within 12 hours from blood plasma.

Ethinyl estradiol metabolites: water-soluble derivatives of sulfate or glucuronide conjugation enter the intestines with bile, where they undergo disintegration using 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, lactation, severe liver disease, liver tumors, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), cholelithiasis, cholecystitis, chronic colitis, the presence or indication of a history of severe cardiovascular (including decompensated heart defects) and cerebrovascular changes, thromboembolism and predisposition to them, phlebitis of the deep veins of the lower extremities, hormone-dependent malignant neoplasms of the genital organs and mammary glands (including suspicion of them), familial forms of hyperlipidemia, arterial hypertension with systolic / diastolic blood pressure of 160/100 mm Hg and above, surgical interventions, surgical operations on the lower extremities, prolonged immobilization, extensive injuries, pancreatitis (including a history), accompanied by severe hypertriglyceridemia and hyperlipidemia, jaundice due to the use of drugs containing steroids, severe diabetes mellitus, sickle cell disease anemia, chronic hemolytic anemia, vaginal bleeding of unknown etiology, migraine, cystic drift, otosclerosis with worsening during the previous pregnancy and (tei) idiopathic jaundice of pregnant women, severe skin itching of pregnant women, herpes of pregnant women with a history of smoking over the age of 35 years, over the age of 40 years, lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the drug contains lactose).

CAUTION

Compensated diabetes mellitus without vascular complications, arterial hypertension with systolic / diastolic blood pressure up to 160/100 mmHg, varicose disease, multiple sclerosis, epilepsy, small chorea, porphyria, tetany, bronchial asthma without regular ovulatory cycles), uterine fibroids, mastopathy, depression, tuberculosis.

Use during pregnancy and lactation

During pregnancy and lactation, taking Tri-RegolВ® is contraindicated.

Composition

active substances:

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 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, sodium carmellose, red iron oxide (E172).

Pills II.

Core: silicon dioxide colloidal, 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, sodium carmellose.

Tablets III.

Core: silicon dioxide colloidal, 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, sodium carmellose, yellow iron oxide (E172).

Dosage and administration

First-time use of the drug:

Take orally, at the same time of the day, if possible in the evening, without chewing and drinking a little liquid.

For the purpose of contraception in the first cycle, Tri-Regol® is prescribed daily at 1 tablet / day. for 21 days, starting from day 1 of the menstrual cycle, then take a 7-day break, during which typical menstrual bleeding occurs. The next pack containing 21 coated tablets should be taken on the 8th day after a 7-day break.

The drug is taken as long as there is a need for contraception.

When switching from another oral contraceptive to taking Tri-Regol®, a similar scheme is used.

After an abortion, taking the drug is recommended to start on the same or the next day after surgery.

After birth, taking the drug is recommended exclusively 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 a woman has not taken Tri-Regol® within the prescribed period, she should take the missed tablet within the next 12 hours. If 36 hours have passed after taking the pill, 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 apply another, non-hormonal method of contraception (for example, barrier).

Side effects

Side effects observed when using 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 1/10000 including individual messages.

Nausea, vomiting, headache, breast engorgement, weight gain, 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 the appointment of any therapy).

Rarely there is an increase in the concentration of triglycerides, glucose in the blood, a decrease in glucose tolerance, an increase in blood pressure, jaundice, hepatitis, liver adenoma, gallbladder diseases (for example, cholelithiasis, cholecystitis), thrombosis and venous thromboembolism, skin rash, hair loss, exacerbation from the vagina, vaginal candidiasis, fatigue, diarrhea.

With prolonged use, it is very rare that generalized itching, cramping of the calf muscles, hearing loss, an increase in the frequency of epileptic seizures, and coarsening of the voice can occur.

Drug interaction

Use with caution while taking:

ampicillin, rifampicin, chloramphenicol, neomycin, polymyxin B, sulfanylamides, tetracyclines, dihydroergotazine, tranquilizers non-hormonal contraceptive method of

anticoagulants, coumarin derivatives or indandion (there may be a need for an extraordinary determination of prothrombin index and change in the dose of anticoagulant) insulin (may need to change their doses)

bromocriptine (decreased effectiveness)

drugs with possible hepatotoxic action, especially dantrolene (risk of increased hepatotoxicity, especially in women older than 35 years).

Overdose

Symptoms: nausea, uterine bleeding.

Treatment: if the first signs of overdose appear in the first 2-3 hours, gastric lavage is recommended.

Symptomatic therapy is shown. There is no antidote.

Storage conditions

The drug should be stored at a temperature of 15 ° to 30 РC.

Expiration

5 years.

dosage form

dosage form

tablets

Gedeon Richter Vengriya