Tri-regol, 63 pcs.

Pharmacodynamics

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

The sequential administration of the coated tablets of the drug containing different amounts of gestagen (levonorgestrel) and estrogen (ethinylestradiol) provides concentrations of these hormones in blood close to their concentrations during normal menstrual cycle and promotes endometrial secretory conversion. The contraceptive effect is associated with several mechanisms.

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

Ethinylestradiol keeps cervical mucus highly viscous (makes it difficult for sperm to enter the uterine cavity). In addition to the contraceptive effect, the menstrual cycle is normalized by replenishing endogenous hormone levels with the hormonal components of the Tri-Regol ^® tablets. During the seven-day periods when another break in taking the drug follows, uterine bleeding occurs.

Pharmacokinetics

Levonorgestrel is rapidly 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 taken 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 the help of intestinal bacteria. 60% of levonorgestrel is excreted by the kidneys, 40% is excreted through the intestines, 40% of ethinylestradiol is excreted by the kidneys and 60% is excreted 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 substances

Pills 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).

Pills 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.

Pills 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).

How to take, the dosage

First-time use of the drug:

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

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 the typical menstrual bleeding occurs. Taking the next package containing 21 coated tablets should be started on the 8th day after the 7-day break.

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

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

After an abortion, it is recommended that the drug be started the same day or the day after surgery.

After childbirth, taking the drug is recommended only for women who are not breastfeeding.

The intake 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 elapse after taking the pill, contraception cannot be considered reliable. 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 concomitant administration:

• ampicillin, rifampicin, chloramphenicol, neomycin, polymyxin B, sulfonamides, tetracyclines, dihydroergotamine, tranquilizers, phenylbutazone because these drugs may weaken the contraceptive effect, a different, non-hormonal contraceptive method is recommended in addition;
• 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 rule out pregnancy, to do a general medical and gynecological examination (breast examination, cytological smear test).

At the time of taking the drug regular gynecological examination every 6 months is required.

The use of oral contraceptives is allowed not earlier than 6 months after previous viral hepatitis and under condition of normalization of liver functions.

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

In case of acyclic bleeding it is possible to continue taking Tri-Regol^® after excluding organic pathology by the attending physician.

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

In case of vomiting or diarrhea, the drug should be continued and another, non-hormonal method of contraception is recommended.

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 change some laboratory parameters (functional parameters of the liver, kidneys, adrenal glands, thyroid gland, blood clotting and fibrinolytic factors, levels of lipoproteins and transport proteins).

The drug should be discontinued 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 infarction is suspected;
– In 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 onset of pregnancy;
– 6 weeks before the planned surgery, in long-term immobilization (eg, after trauma).

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

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

Contraindications

– severe liver disease;
– liver tumors;
– congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes);
– cholelithiasis;
– cholecystitis;
– chronic colitis;
– presence or previous history of severe cardiovascular diseases (including decompensated malformations).
– severe cardiovascular (including decompensated heart disease) and cerebrovascular changes, thromboembolism and predisposition to them;
– phlebitis of deep veins of lower limbs;
– hormonedependent malignant neoplasms of genitals and mammary glands (including the suspicion of such neoplasms);
– any signs of neoplasia or syndrome.
– family forms of hyperlipidemia;
– arterial hypertension with systolic/diastolic BP 160/100 mm Hg. Individuals with hypertension – arterial hypertension with systolic/adiastolic blood pressure 160/100 mm Hg and higher;
– surgical interventions, surgical operations on lower extremities;
– prolonged immobilization;
– extensive trauma;
– pancreatitis (incl. In anamnesis), accompanied by significant hypertriglyceridemia and hyperlipidemia;
– jaundice due to taking medicines containing steroids;
– severe forms of diabetes;
– sickle-cell anemia;
– chronic hemolytic anemia;
– vaginal bleeding of unknown etiology;
– migraine;
– bulla;
– otosclerosis with worsening course during previous pregnancy(s);
– idiopathic jaundice of pregnant women, severe skin pruritus of pregnant women, herpes of pregnant women in the history;
– smoking over 35 years old, age over 40 years old;
– Lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the drug form contains lactose);
– pregnancy;
– lactation;
– hypersensitivity to any component of the preparation Tri-Regol.
With caution
Compensated diabetes 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.

Side effects

The side effects observed with the use of the drug are classified into categories according to their frequency of occurrence:

Very common ≥1/10; common >1/100, ≤1/10, sometimes ≥1/1000, ≤1/100; rare ≥1/10000, ≤1/1000; very rare ≤1/10000 including individual reports.

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

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

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

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