Tri-regol, 21 pcs.

Pharmacodynamics

Combined (three-phase) oral estrogen-gestagen contraceptive drug. When taken it inhibits pituitary gonadotropic hormone secretion.

The sequential administration of coated tablets containing different amounts of gestagen (levonorgestrel) and estrogen (ethinylestradiol) ensures concentrations of these hormones in blood close to their concentrations during normal menstrual cycle and promotes endometrial secretion.

The contraceptive effect is associated with several mechanisms. Under the influence of levonorgestrel there is a blockade of the release of releasing releasing factors (luteinizing and follicle stimulating hormones) of the hypothalamus, inhibition of secretion of gonadotropic hormones by the pituitary gland, which leads to inhibition of maturation and exit of the egg ready for fertilization (ovulation).

Ethinylestradiol maintains high viscosity of cervical mucus (makes it difficult for sperm to enter the uterine cavity). Along with contraceptive effect, menstrual cycle is normalized due to replenishment of endogenous hormone levels by hormonal components of Tri-Regol® tablets. During the seven-day periods when there is another break in taking the drug, uterine bleeding occurs.

Pharmacokinetics

Levonorgestrel is quickly absorbed (less than 4 hours). Levonorgestrel has no “first pass” effect through the liver. The elimination half-life is 8-30 hours (average 16 hours). Most of the levonorgestrel in the blood is bound to albumin and to globulin that binds sex hormones.

Ethinylestradiol is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum plasma concentration is reached between 1-1.5 hours. The elimination half-life is 26±6.8 hours. Ethinylestradiol has an inherent “first pass” effect through the liver (so-called “first pass” effect). Metabolism is carried out in the liver and intestine.

When administered orally, ethinylestradiol is excreted within 12 hours from the blood plasma.

The metabolites of ethinylestradiol: water-soluble derivatives of sulfate or glucuronide conjugation, enter the intestine with the bile, where they undergo disintegration with intestinal bacteria. 60% of levonorgestrel is excreted by the kidneys, 40% through the intestines, 40% of ethinylestradiol is excreted by the kidneys and 60% through the intestines.

Indications

Contraception, Menstrual disorders, Premenstrual syndrome

Oral contraception.

Active ingredient

Levonorgestrel, Ethinylestradiol

Composition

active ingredients:

Table I: contain 0.03 mg ethinylestradiol and 0.05 mg levonorgestrel,
Tablet II: contain 0.04 mg of ethinylestradiol and 0.075 mg of levonorgestrel,
Tablets III: contain 0.03 mg of ethinylestradiol and 0.125 mg of levonorgestrel.

Auxiliary Ingredients

Table I.
Core: colloidal silica, 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).

Tablets II.
Core: colloidal silica, 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: colloidal silica, 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, iron oxide yellow (E172).

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How to take, the dosage

First-time use:

Take orally, at the same time of day, in the evening if possible, without chewing and with a small amount of fluid.

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

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

If you switch from another oral contraceptive to taking Tri-Regol® a similar regimen is used.
After an abortion, it is recommended that the drug be started on the same or next day after surgery.

After childbirth, taking the drug is recommended only for women who are not breastfeeding.
The drug should not be started before the first day of the menstrual cycle.

The use of the drug is contraindicated during lactation.

If a woman does not take Tri-Regol® within the prescribed time, the missed tablet should be taken within the next 12 hours. If 36 hours have elapsed after taking the pill, contraception cannot be considered reliable.

Yet, however, to avoid intermenstrual bleeding, you should continue taking the product from the already started package minus the missed pill(s). At this time, it is recommended to use an additional, non-hormonal method of contraception (e.g., barrier contraception).

Interaction

The drug should be used with caution when taken at the same time:

• ampicillin, rifampicin, chloramphenicol, neomycin, polymyxin B, sulfonamides, tetracyclines, dihydroergotamine, tranquilizers, phenylbutazone because these drugs may weaken the contraceptive effect, another, non-hormonal contraceptive method is recommended;
• anticoagulants, coumarin or indandion derivatives (may require an extraordinary determination of the prothrombin index and a change in the anticoagulant dose);
• tricyclic antidepressants, maprotiline, beta-adrenoblockers (bioavailability and thereby toxicity may increase);
• oral hypoglycemic drugs, insulin (there may be a need to change their doses);
• bromocriptine (decreased effectiveness);
• drugs with possible hepatotoxic effects, particularly dantrolene (risk of increased hepatotoxicity, particularly in women over 35 years).

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Special Instructions

Before starting to use the drug it is necessary to exclude pregnancy, to conduct a general medical and gynecological examination (breast examination, cytological smear test).

When taking the drug it is necessary to have regular gynecological examinations every 6 months.
The use of oral contraceptives is allowed not earlier than 6 months after the last viral hepatitis and under condition of normalization of liver functions.

In case of severe pain in the upper abdomen, hepatomegaly or signs of intra-abdominal hemorrhage, the presence of liver tumor can be suspected. In this case, the drug should be discontinued.

If acyclic bleeding occurs, Tri-Regol® may be continued after excluding organic pathology by the physician.

If liver function abnormalities are detected during the use of the drug, the appropriateness of continuing the use of Tri-Regol® should be considered.

In case of vomiting or diarrhea, the drug should be continued and an alternative, non-hormonal method of contraception should be used.

At least 3 months before the planned pregnancy, the use of the drug should be stopped.

The effects of oral contraceptives (due to the estrogenic component) may alter some laboratory parameters (functional parameters of the liver, kidneys, adrenal glands, thyroid gland, blood clotting and fibrinolytic factors, lipoprotein and transport proteins levels).

The drug should be stopped immediately in the following cases:

– if migraine-like or unusually severe headache occurs for the first time or worsens, if visual acuity deteriorates, if thrombosis or heart attack is suspected;
– In case of a sharp increase in blood pressure, the appearance of jaundice or hepatitis without jaundice, the occurrence of generalized itching or increased frequency of epileptic seizures;
– In the beginning of pregnancy;
– 6 weeks before the planned surgery, in case of prolonged immobilization (for example, after injuries).

The effect of the drug on the ability to drive and operate vehicles

The use of the drug does not affect the ability to drive and operate other mechanisms.

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; presence or mention in the anamnesis of severe cardiovascular (including decompensated cardiac defects) and cerebrovascular disorders.history of severe cardiovascular (including decompensated heart disease) and cerebrovascular changes, thromboemboli and predisposition to them, phlebitis of deep veins of the lower extremities, hormone-dependent malignancies of the genitals and mammary glands (including suspected malignancies).including suspected), familial forms of hyperlipidemia, arterial hypertension with systolic/diastolic blood pressure 160/100 mmHg or higher, surgical interventions, lower extremity surgeries, prolonged immobilization, extensive trauma, pancreatitis (incl.ч. history) accompanied by marked hypertriglyceridemia and hyperlipidemia, jaundice due to the administration of drugs containing steroids, severe forms of diabetes mellitus, sickle cell anemia, chronic hemolytic anemia, vaginal bleeding of unknown etiology, migraine, bladder disease, otosclerosis with worsening course during the previous pregnancy(s); idiopathic jaundice in pregnant women, severe pruritus in pregnant women, herpes in pregnancy; smoking over 35 years of age, age over 40 years; lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the drug contains lactose in its dosage form).

WARNING

Compensated diabetes mellitus without vascular complications, arterial hypertension with systolic/diastolic blood pressure up to 160/100 mm Hg, varicose veins, multiple sclerosis, epilepsy, minor chorea, porphyria, tetany, bronchial asthma, adolescence (without regular ovulatory cycles), uterine myoma, mastopathy, depression, tuberculosis.

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Side effects

The side effects observed with the drug are classified into categories according to their frequency of 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 reports.

Nausea, vomiting, headache, mammary gland engorgement, weight gain, decreased libido, depressed mood, chloasma, intermenstrual bleeding, in some cases – eyelid edema, conjunctivitis, visual disturbances, discomfort when wearing contact lenses (these phenomena are temporary and disappear after cancellation without any therapy).

. Increases in triglycerides, blood glucose, decreased glucose tolerance, increased blood pressure, jaundice, hepatitis, liver adenoma, gall bladder disorders (e.g., cholelithiasis, cholecystitis) thrombosis and venous thromboembolism, skin rash, hair loss, increased vaginal discharge, vaginal candidiasis, increased fatigue, diarrhea are rare.

Long-term use may very rarely cause generalized itching, calf cramps, decreased hearing, increased frequency of epileptic seizures, coarsening of the voice.

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Overdose

Symptoms: nausea, uterine bleeding.

Treatment: gastric lavage is recommended at the first signs of overdose during the first 2-3 hours.

Symptomatic therapy is indicated.

There is no antidote.

Pregnancy use

Tri-Regol® is contraindicated during pregnancy and lactation.

Similarities

Rigavidon, Microgynon