Rigevidone, pills, 21pcs

Composition

Active ingredients:  

ethinyl estradiol: 0.03 mg,

levonorgestrel; 0.15 mg

Auxiliary substances:

in the core of the tablet:

colloidal silicon dioxide,

magnesium stearate,

talc,

corn starch,

lactose monohydrate;

coated tablets:

sucrose,

talc,

calcium carbonate,

titanium dioxide,

copovidone,

macrogol 6000,

colloidal silicon dioxide,

povidone,

sodium carmellose.

Pharmacological action

Pharmacodynamics

Rigevidone is an oral monophasic combined estrogen-progestogen contraceptive. When taken orally, it inhibits the pituitary secretion of gonadotropic hormones.

The contraceptive effect is associated with several mechanisms. As a progestogen component (progestin), it contains a derivative of 19-nortestosterone – levonorgestrel, which is superior in activity to the yellow body hormone progesterone (and a synthetic analog of the latter-pregnin), acts at the level of receptors without preliminary metabolic transformations. The estrogenic component is ethinyl estradiol.

Under the influence of levonorgestrel, the release of releasing hormones (LH and FSH) of the hypothalamus is blocked, and the pituitary gland secretes gonadotropic hormones, which leads to inhibition of maturation and release of an egg ready for fertilization (ovulation). The contraceptive effect is enhanced by ethinyl estradiol. Preserves the high viscosity of cervical mucus (makes it difficult for spermatozoa to enter the uterine cavity). Along with the contraceptive effect, when taken regularly, it normalizes the menstrual cycle and helps prevent the development of a number of gynecological diseases, including those of a tumor nature.

Pharmacokinetics

Levonorgestrel is rapidly absorbed (in less than 4 hours). Levonorgestrel has no first-pass effect through the liver. When levonorgestrel is co-administered with ethinyl estradiol, there is a relationship between the dose and the maximum plasma concentration. TCmax (time to reach the maximum concentration) of levonorgestrel is 2 hours, T 1/2 (half-life) is 8-30 hours. (an average of 16 hours). Most of levonorgestrel is bound in the blood to albumin and SHBG (Sex Hormone binding Globulin).

Ethinyl estradiol is rapidly and almost completely absorbed from the intestine. Ethinyl estradiol has the effect of primary passage through the liver, TCmax is 1.5 hours, and the half-life is about 26 hours.

When taken orally, ethinyl estradiol is released from the blood plasma within 12 hours, the half-life is 5.8 hours. Ethinyl estradiol is metabolized in the liver and intestines. Metabolites of ethinyl estradiol – water-soluble products of sulfate or glucuronide conjugation, enter the intestine with bile, where they are disintegrated by intestinal bacteria. Both components (levonorgestrel and ethinyl estradiol) are excreted in breast milk. Active substances are metabolized in the liver, T 1/2 is 2-7 h

. levonorgestrel is absorbed by the kidneys (60%) and through the intestines (40%); ethinyl estradiol – by the kidneys (40%) and through the intestines (60%).

Indications

Oral contraception, functional disorders of the menstrual cycle (including dysmenorrhea without an organic cause, dysfunctional metrorrhagia, premenstrual syndrome).

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Contraindications

-Severe liver diseases (including congenital hyperbilirubinemia-Gilbert’s, Dubin-Johnson and Rotor syndromes). – Cholecystitis. – The presence or indication in the anamnesis of severe cardiovascular and cerebrovascular diseases. – Thromboembolism and predisposition to them. – Malignant tumors (primarily breast or endometrial cancer). – Liver tumors. – Familial forms of hyperlipidemia. – Severe forms of arterial hypertension. – Endocrine diseases (including severe forms of diabetes mellitus). – Sickle cell anemia. – Chronic hemolytic anemia. – Vaginal bleeding of unknown etiology. – Bubble drift. – Migraines. – Otosclerosis. – A history of idiopathic jaundice in pregnant women. – Severe pruritus of pregnant women. – Herpes of pregnant women. – Age over 40 years. – Pregnancy. – The period of lactation (breastfeeding). – Hypersensitivity to the components of the drug.

The drug should be used with caution when: :

– Diseases of the liver and gallbladder. – Epilepsy. – Depression. – Ulcerative colitis. – Uterine fibroids. – Mastopathy. – Tuberculosis. – Kidney diseases. – For diabetes mellitus. – Diseases of the cardiovascular system. – Arterial hypertension. – Impaired renal function. – Varicose veins. – Phlebite. – Multiple sclerosis. – Little chorea. – In adolescence (without regular ovulatory cycles).

Side effects

The drug is usually well tolerated.

Possible side effects of a transient nature that pass spontaneously: nausea, vomiting, headache, breast engorgement, changes in body weight and libido, mood changes, acyclic spotting, in some cases – eyelid edema, conjunctivitis, visual impairment, discomfort when wearing contact lenses (these phenomena are temporary and disappear after discontinuation without any therapy).

With prolonged use, chloasma, hearing loss, generalized itching, jaundice, calf muscle cramps, and an increase in the frequency of epileptic seizures may very rarely occur.

Hypertriglyceridemia, hyperglycemia, decreased glucose tolerance, increased blood pressure (BP), thrombosis and venous thromboembolism, jaundice, skin rashes, changes in the nature of vaginal secretion, vaginal candidiasis, increased fatigue, diarrhea are rarely observed.

Interaction

Barbiturates, some antiepileptic drugs (carbamazepine, phenytoin ), sulfonamides, pyrazolone derivatives can increase the metabolism of the steroid hormones included in the drug.

A decrease in contraceptive effectiveness can also be observed when prescribed simultaneously with some antimicrobials (including ampicillin, rifampicin, chloramphenicol, neomycin, polymyxin B, sulfonamides, tetracyclines), which is associated with changes in the intestinal microflora.

When used concomitantly with anticoagulants, coumarin derivatives or indandione, additional determination of the prothrombin index and a change in the dose of the anticoagulant may be required.

When using tricyclic antidepressants, maprotilin, beta-blockers, their bioavailability and toxicity may increase.

When using oral hypoglycemic drugs and insulin, it may be necessary to change their dose.

When combined with bromocriptine, its effectiveness decreases.

When combined with drugs with potential hepatotoxic effects, such as dantrolen, there is an increase in hepatotoxicity, especially in women over 35 years of age.

Rigevidone should be used with caution in combination with the drugs listed above.

How to take, course of use and dosage

Apply orally, without chewing and with a small amount of liquid.

If during the previous menstrual cycle hormonal contraception was not performed, contraception with Rigevidone is started from the first day of menstruation, taking 1 tablet daily for 21 days, at the same time of day.

This is followed by a 7-day break, during which menstrual-like bleeding occurs. The next 21-day cycle of taking tablets from a new package containing 21 tablets should be started the next day after a 7-day break, i. e. on the eighth day, even if the bleeding has not stopped. Thus, the start of taking the drug from each new package falls on the same day of the week.

When switching to taking Rigevidone from another oral contraceptive, a similar scheme is used. The drug is taken as long as there is still a need for contraception.

After an abortion, it is recommended to start taking the drug on the day of the abortion or the day after the operation.

After childbirth, the drug can only be prescribed to women who are not breast-feeding; the contraceptive should be started no earlier than the first day of menstruation. During lactation, the use of the drug is contraindicated.

Missed pills; the missed pill should be taken within the next 12 hours. If 36 hours have passed since the last pill was taken, contraception is unreliable. To avoid intermenstrual spotting, the drug should be continued from the already started package, with the exception of the missed tablet (s). In cases of missing pills, it is recommended to additionally use a different, non-hormonal method of contraception (for example, barrier). For therapeutic purposes; the dose of Rigevidone and the scheme of application are selected by the doctor in each case individually.

Overdose

Cases of toxic effects due to overdose are unknown.

Special instructions

Before using hormonal contraception and every 6 months thereafter, a general medical and gynecological examination is recommended, including cytological analysis of a smear from the cervix, assessment of the condition of the mammary glands, determination of blood glucose, cholesterol and other indicators of liver function, blood pressure monitoring, and urine analysis).

The use of Rigevidone in women with thromboembolic diseases at a young age and a family history of increased blood clotting is not recommended.

The use of oral contraception is allowed no earlier than 6 months after the transfer of viral hepatitis, provided that liver functions are normalized.

If there is severe pain in the upper abdomen, hepatomegaly, and signs of intra-abdominal bleeding, a liver tumor may be suspected. If necessary, the drug should be discontinued.

If liver function is impaired while taking Rigevidone, consult a therapist.

If acyclic (intermenstrual) bleeding occurs, Rigevidone should be continued, since in most cases these bleeds stop spontaneously. If acyclic (intermenstrual) bleeding persists or recurs, a medical examination should be performed to rule out organic pathology of the reproductive system.

In case of vomiting or diarrhea, the drug should be continued using a different, non-hormonal method of contraception.

Women who smoke and take hormonal contraceptives have an increased risk of developing cardiovascular diseases with serious consequences (myocardial infarction, stroke). The risk increases with age and depending on the number of cigarettes smoked (especially in women over 35 years of age).

The drug should be discontinued in the following cases::

– When a migraine-like headache appears for the first time or increases. – The appearance of an unusually strong headache. – When early signs of phlebitis or phlebothrombosis appear (unusual pain or swelling of the veins on the legs). – If jaundice or hepatitis occurs without jaundice. – For cerebrovascular disorders. – When there are stabbing pains of unclear etiology when breathing or coughing, pain and tightness in the chest. – With acute deterioration of visual acuity. – If a thrombosis or heart attack is suspected. – With a sharp increase in blood pressure. – When generalized itching occurs. – With increased frequency of epileptic seizures. – 3 months before the planned pregnancy. – Approximately 6 weeks before the planned surgical intervention. – With prolonged immobilization. – In case of pregnancy.

– Use in patients with impaired liver function: Contraindicated use in severe liver diseases (including congenital hyperbilirubinemia-Gilbert’s, Dubin-Johnson and Rotor syndromes; liver tumors).

– Use in patients with impaired renal function: Caution is required when prescribing the drug to patients with impaired renal function.

– Influence on the ability to drive vehicles and manage mechanisms: Taking the drug does not affect the ability to drive vehicles and manage other mechanisms that are associated with an increased risk of injury.

Form of production

coated tablets

Storage conditions

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

Shelf

life is 5 years.

Active ingredient

Ethinyl Estradiol, Levonorgestrel

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For women of childbearing age, For adults

Indications

Contraception, Premenstrual Syndrome, Menstrual disorders