Regulon, pills, 21pcs

Composition

1 tablet contains:

active ingredients:

ethinyl estradiol 0.03 mg,

desogestrel 0.15 mg,

excipients:

alpha-tocopherol-0.08 mg;

magnesium stearate-0.08 mg;

colloidal silicon dioxide-0.8 mg;

stearic acid-0.8 mg;

povidone-2.4 mg;

potato starch-8 mg;

lactose monohydrate-67.66 mg,

film shell:

propylene glycol-0.03 mg;

macrogol 6000-0.22 mg;

hypromellose-0.75 mg

Pharmacological action

Pharmaceutical group:

contraceptive (estrogen+progestogen).

Pharmaceutical action:  

Regulon is a monophasic oral contraceptive. The main contraceptive effect is to inhibit the synthesis of gonadotropins and suppress ovulation. In addition, by increasing the viscosity of the cervical mucus, the movement of spermatozoa through the cervical canal slows down, and a change in the state of the endometrium prevents the implantation of a fertilized egg.

Ethinyl Estradiol is a synthetic analog of endogenous estradiol.

Desogestrel has a pronounced progestogenic and anti-estrogenic effect, similar to endogenous progesterone, weak androgenic and anabolic activity.

Regulon has a beneficial effect on lipid metabolism: it increases the concentration of HDL in the blood plasma, without affecting the LDL content.

When taking the drug, menstrual blood loss is significantly reduced (with initial menorrhagia), the menstrual cycle is normalized, and a favorable effect on the skin is noted, especially in the presence of vulgar acne.

Pharmacokinetics:

Desogestrelsabsorption Desogestrel is rapidly and almost completely absorbed from the gastrointestinal tract and is immediately metabolized to 3-keto-desogestrel, which is a biologically active metabolite of desogestrel.

Cmax is reached in 1.5 hours and is 2 ng / ml. Bioavailability – 62-81%.

Distribution 3-keto-desogestrel binds to plasma proteins, mainly albumins and sex hormone binding globulin (SHBG). Vd is 1.5 l/kg. Css is set by the second half of the menstrual cycle. The level of 3-keto-desogestrel increases 2-3 times.

Other metabolites are formed in addition to 3-keto-desogestrel (which is formed in the liver and in the intestinal wall): 3α-OH-desogestrel,3β-OH-desogestrel,3α-OH-5α-N-desogestrel (phase I metabolites). These metabolites have no pharmacological activity and are partially converted by conjugation (the second phase of metabolism) to polar metabolites – sulfates and glucuronates. Clearance from blood plasma is about 2 ml / min / kg of body weight.

The elimination of 1/2 3-keto-desogestrel is 30 h. The metabolites are excreted in the urine and feces (in a ratio of 4: 6). – Ethinyl Estradiol

Absorption of ethinyl estradiol is rapidly and completely absorbed from the gastrointestinal tract. Cmax is reached 1-2 hours after taking the drug and is 80 pg / ml. The bioavailability of the drug due to presystemic conjugation and the “first pass” effect through the liver is about 60%.

Distribution Ethinyl estradiol is completely bound to plasma proteins, mainly albumins. Vd is 5 l/kg. Css is established by 3-4 days of use, while the level of ethinyl estradiol in the serum is 30-40% higher than after a single dose of the drug.

Metabolismresystemic conjugation of ethinyl estradiol is significant. Bypassing the intestinal wall (the first phase of metabolism), it undergoes conjugation in the liver (the second phase of metabolism).

Ethinyl estradiol and its conjugates of the first phase of metabolism (sulfates and glucuronides) are released into the bile and enter the enterohepatic circulation. Clearance from blood plasma is about 5 ml / min / kg of body weight.

The elimination of 1/2 ethinyl estradiol is on average about 24 hours. About 40% is excreted in the urine and about 60% in the feces.

Indications

Oral contraception.

Use during pregnancy and lactation

Regulon is contraindicated for use during pregnancy. Regulon should be discontinued 3 months before the planned pregnancy. In case of pregnancy, the drug should be discontinued.

Epidemiological studies have shown that among children born to women who took hormonal contraceptives before pregnancy, the incidence of malformations does not increase. In cases of taking the drug in the early stages of pregnancy, no teratogenic effect was detected.

The use of Regulon is contraindicated during lactation (breastfeeding), because it reduces the secretion of breast milk, changes its composition. In addition, small amounts of active substances are excreted in breast milk.

Contraindications

• the presence of severe and/or multiple risk factors for venous or arterial thrombosis (including hypertension severe or moderate AD ≥ 160/100 mm Hg. St. )
• the presence or provision in the history of the harbingers of thrombosis (including transient ischemic attack, angina);
• migraine with focal neurological symptoms, including in the anamnesis;
• venous or arterial thrombosis/thromboembolism (e. g. myocardial infarction, stroke, deep vein thrombosis of the leg, pulmonary embolism) in the present or in history;
• the presence of venous thromboembolism in history;
• diabetes mellitus (with angiopathy);
• pancreatitis (including in history), accompanied by severe hypertriglyceridemia;
• dyslipidemia;
• severe liver disease, cholestatic jaundice (including pregnancy), hepatitis, including history (up to the normalization of functional and laboratory parameters and for 3 months after the normalization of them);
• jaundice in GCS;
• gallstone disease currently or in history;
• syndrome Gilbert syndrome, Dubin-Johnson syndrome Rotor;
• liver tumors (including in the anamnesis);
• severe itching, otosclerosis or progression during a previous pregnancy or GCS;
• hormone-dependent malignancies of the genital organs and mammary glands (including if you suspect them);
• vaginal bleeding of unknown etiology;
• the Smoking age 35 years (more than 15 cigarettes a day);
• pregnancy or suspicion of it;
• lactation;
• hypersensitivity to the components of the drug.

Caution should be exercised when prescribing the drug for conditions that increase the risk of venous or arterial thrombosis/thromboembolism: age over 35 years, smoking, family history, obesity (body mass index more than 30 kg/m2), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valvular heart disease, atrial fibrillation, prolonged immobilization, extensive surgery, lower limb surgery, severe pain trauma, varicose veins and superficial thrombophlebitis, postpartum period, presence of severe depression (including in the anamnesis), changes in biochemical parameters (activated protein C resistance, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including cardiolipin antibodies, including lupus anticoagulant), diabetes mellitus, uncomplicated cardiovascular disorders, SLE, Crohn’s disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.

Side effects

Side effects that require discontinuation of the drug

From the cardiovascular system: arterial hypertension; rarely-arterial and venous thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary embolism); very rarely-arterial or venous thromboembolism of the hepatic, mesenteric, renal, retinal arteries and veins.

Sensory disorders: hearing loss due to otosclerosis.

Others: hemolytic-uremic syndrome, porphyria; rarely-exacerbation of reactive systemic lupus erythematosus; very rarely-Sydenham’s chorea (passing after drug withdrawal).

Other side effects that are more common but less severe. The expediency of continuing to use the drug is decided individually after consultation with a doctor, based on the benefit/risk ratio.

From the genital system: acyclic bleeding/spotting from the vagina, amenorrhea after discontinuation of the drug, changes in the state of vaginal mucus, development of inflammatory processes of the vagina, candidiasis, tension, pain, breast enlargement, galactorrhea.

From the digestive system: nausea, vomiting, Crohn’s disease, ulcerative colitis, occurrence or exacerbation of jaundice and / or itching associated with cholestasis, cholelithiasis.

Dermatological reactions: erythema nodosum, exudative erythema, rash, chloasma.

From the central nervous system: headache, migraine, mood lability, depression.

From the side of the organ of vision: increased sensitivity of the cornea (when wearing contact lenses).

From the side of metabolism: fluid retention in the body, changes (increase) in body weight, decreased tolerance to carbohydrates.

Other: allergic reactions.

Interaction

When using Regulon concomitantly with antispasmodics, phenobarbital derivatives, antibiotics (tetracycline, ampicillin, rifampicin, isoniazid, neomycin, penicillin, chloramphenicol), carbamazepine, phenylbutazone, analgesics, anxiolytics, activated carbon, sulfonamides, nitrofurans, anti-migraine drugs, griseofulvin, laxatives, and some medicinal plants (for example, St. John’s wort) can change the nature of menstruation and reduce the contraceptive effect of Regulon.When used concomitantly, Regulon reduces the effectiveness of oral anticoagulants, anxiolytics (diazepam), tricyclic antidepressants, guanethidine, theophylline, caffeine, vitamins, clofibrate, glucocorticosteroids, and paracetamol. When Regulon is co-administered with oral hypoglycemic drugs or insulin, it is possible to disrupt the control of carbohydrate metabolism, since Regulon can reduce carbohydrate tolerance and increase the need for insulin or oral hypoglycemic agents, which may require dose adjustment.

How to take, course of use and dosage

The drug is prescribed for 1 tab. /day (if possible at the same time), starting from the 1st day of the menstrual cycle for 21 days. This is followed by a 7-day break, during which menstrual-like bleeding occurs. Then the tablets are taken again from the next package (even if the bleeding has not stopped yet). If the rules of admission are observed, the contraceptive effect is maintained for the duration of the 7-day break.

If the first pill is taken on the 1st day of the menstrual cycle, then additional methods of contraception are not required. You can start taking pills from 2-5 days of menstruation, but in this case, in the first cycle, you need to use additional methods of contraception in the first 7 days of taking pills.

If more than 5 days have passed since the start of menstruation, you should postpone the start of taking the drug until the next menstruation.

– After giving birth to non-lactating women, the drug can be prescribed in 21 days. In this case, there is no need to use other methods of contraception. If the drug is prescribed later than 21 days after delivery, then additional methods of contraception should be used in the first 7 days of admission. If in the postpartum period, sexual contact was preceded by oral contraception, then taking pills should wait until the first menstruation appears. In women who continue to breastfeed, the use of combined oral contraceptives is not recommended, since taking the drug can reduce the release of milk.

– After an abortion, it is recommended to start taking the drug immediately after surgery, and in this case there is no need to use additional methods of contraception.

– When switching to Regulon after taking another estrogen-progestogen hormonal contraceptive, the first tablet of Regulon should be taken the next day after completing the course of the previous drug. There is no need to use additional methods of contraception. When switching to Regulon after taking another hormonal contraceptive containing only progestogen, the first tablet of Regulon should be taken on the first day of the menstrual cycle; there is no need to use additional methods of contraception. If menstruation does not occur when taking the previous drug, you can start taking Regulon on any day of the cycle, but in this case, additional methods of contraception should be used in the first 7 days of taking it. As additional methods of contraception, it is recommended to use a cervical cap with spermicidal gel, a condom, or abstinence from sexual contact. The use of the calendar method as an additional method of contraception is not recommended.

– If it is necessary to delay menstruation, taking tablets should be continued without a 7-day break. In this case, intermenstrual bleeding may occur, but this does not reduce the contraceptive effect of the drug. Regular use of Regulon can be restored after the usual 7-day break.

– If you miss taking the drug if the delay in taking the pill was not more than 12 hours, then you need to take the missed pill and then continue taking it at the usual time. If the delay in taking a pill is more than 12 hours, this is considered a missed pill. The reliability of contraception in this cycle is not guaranteed and the use of additional methods of contraception is recommended. If you skip 1 tab. in the first or second week of the cycle, you need to take 2 tablets the next day and then continue regular intake, using additional methods of contraception until the end of the cycle. If you skip 1 tab. on the third week of the cycle, in addition to the measures listed, a 7-day break is excluded. If vomiting or diarrhea occurs after taking the drug, the absorption of the drug may be incomplete. If the symptoms stopped within 12 hours, then you need to take another 1 tab in addition. After that, you should continue taking the pills in the usual way. If the symptoms continue for more than 12 hours, then it is necessary to use additional methods of contraception in the next 7 days.

Overdose

Symptoms: metrorrhagia. Taking the drug in high doses was not accompanied by the appearance of severe symptoms. Treatment: in the first 2-3 hours after taking the drug in a high dose, gastric lavage is recommended. There is no specific antidote, and the treatment is symptomatic.

Special instructions

Before starting to use the drug, it is necessary to conduct a general medical (detailed family and personal history, blood pressure measurement, laboratory tests) and gynecological examination (including examination of the mammary glands, pelvic organs, cytological analysis of a cervical smear). A similar study during the period of taking the drug is carried out regularly, every 6 months.

The effectiveness of the drug Regulon decreases in the case of skipping pills, vomiting and diarrhea, as well as when taken simultaneously with other medications.

The effectiveness of Regulon may decrease if intermenstrual bleeding occurs after several months of its use. If menstrual-like bleeding does not occur during the break, taking pills can be continued only after pregnancy is excluded.

The risk of arterial or venous thromboembolic disease increases with age, while Smoking, the presence of a family history of thromboembolic disease, obesity (body mass index above 30 kg/m 2 ), the dyslipidemias, hypertension, diseases of the heart valves, atrial fibrillation, diabetes, prolonged immobilization (after the big surgery, after surgery on the lower limbs, after a serious injury).

In the presence of congenital or acquired biochemical defects (resistance to activated protein C, hyperchromocysteinemia, protein C and S deficiency, antithrombin III deficiency, presence of antiphospholipid antibodies) it also increases the risk of developing thromboembolic diseases. Targeted treatment of the above conditions reduces the risk of blood clots.

Pregnancy poses a greater risk of blood clots than taking hormonal contraceptives.

Regulon should be discontinued immediately in the following cases::

– The occurrence of a severe headache for the first time or an increase in the usual migraines. – Acute deterioration of visual acuity. – Suspected myocardial infarction or thrombosis. – A sharp increase in blood pressure. – The appearance of jaundice or hepatitis without jaundice, intense generalized pruritus. – The occurrence of epilepsy or increased frequency of epileptic seizures. – 4 weeks before the planned surgical intervention and in case of prolonged immobilization (taking the drug Regulon can be resumed after 2 weeks from the moment of remobilization). – Development of pregnancy.

– Use in patients with impaired liver function: Contraindicated in patients with hepatic insufficiency.

– Use in patients with impaired renal function: With caution and only after a thorough assessment of the benefits and risks of use, the drug should be prescribed for patients with renal insufficiency (including in the anamnesis).

– Influence on the ability to drive vehicles and manage mechanisms: Studies on the effect of the drug Regulon on the abilities necessary for driving a car and industrial mechanisms have not been conducted.

Form of production

Film-coated tablets

Storage conditions

At a temperature of 15-30 °C

Shelf life

3 years

Active ingredient

Desogestrel, Ethinyl Estradiol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For women of childbearing age, For adults as prescribed by a doctor

Indications

Contraception