Logest tablets p / o, No. 21 * 3

• Contraception.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally according to a special scheme.

When taken as part of fixed combinations, a single dose of gestodene is 75 ?g, ethinylestradiol is 20 mg or 30 mg.

Active ingredients:

gestodene - 75 mcg

ethinylestradiol - 20 mcg

Excipients : lactose monohydrate - 37.155 mg, corn starch - 15.5 mg, povidone 25 - 1.7 mg, magnesium stearate - 0.55 mg.

Shell composition: sucrose - 19.66 mg, povidone 90 - 0.171 mg, macrogol 6000 - 2.18 mg, calcium carbonate - 8.697 mg, talc - 4.242 mg, mountain wax glycolic - 0.05 mg.

• Presence of risk factors for venous thromboembolism;

• the presence of risk factors for the development of arterial thromboembolism;

• severe liver disease (including history) before normalization of liver function indicators;

• liver tumor (including history);

• severe chronic renal failure or acute renal failure;

• known or suspected hormone-dependent malignant tumors (including genital or breast);

• bleeding from the vagina of unclear etiology;

• pregnancy;

• lactation period (breastfeeding).

Trade name: LogestЃ

Composition

Film-coated tablets, white, round.

1 tab.

Active ingredients:

gestodene - 75 mcg

ethinylestradiol - 20 mcg

Excipients : lactose monohydrate - 37.155 mg, corn starch - 15.5 mg, povidone 25 - 1.7 mg, magnesium stearate - 0.55 mg.

Shell composition: sucrose - 19.66 mg, povidone 90 - 0.171 mg, macrogol 6000 - 2.18 mg, calcium carbonate - 8.697 mg, talc - 4.242 mg, mountain wax glycolic - 0.05 mg.

Clinical and pharmacological group: Monophasic oral contraceptive

Pharmaco-therapeutic group: Combined contraceptive (estrogen + gestagen)

pharmachologic effect

Combined oral hormonal contraceptive.

The gestagenic component is a derivative of 19-nortestosterone - gestodene, which surpasses in strength and selectivity of action not only the natural hormone of the corpus luteum progesterone, but also other synthetic gestagens (for example, levonorgestrel). Due to its high activity, gestodene is used in low dosages, in which it does not exhibit androgenic properties and has practically no effect on lipid and carbohydrate metabolism.

The estrogenic component of the combination is ethinyl estradiol, a synthetic analogue of the follicular hormone estradiol, which, together with the corpus luteum hormone, participates in the regulation of the menstrual cycle.

Along with the indicated central and peripheral mechanisms that prevent the maturation of an ovum capable of fertilization, the contraceptive effect is due to a decrease in the susceptibility of the endometrium to the blastocyst, as well as an increase in the viscosity of the mucus in the cervix, which makes it relatively impassable for spermatozoa.

Pharmacokinetics

Gestoden

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract. After a single dose, Cmax is noted after 1 hour and is 2-4 ng / ml. Bioavailability is about 99%. Gestodene binds to albumin and sex hormone binding globulin (SHBG). 1-2% is in plasma in free form, 50-75% specifically binds to SHBG. An increase in the level of SHBG in the blood caused by ethinyl estradiol affects the level of gestodene: the fraction associated with SHBG increases, and the fraction associated with albumin decreases. Average Vd - 0.7-1.4 l / kg. The pharmacokinetics of gestodene depends on the level of SHBG. The concentration of SHBG in the blood plasma under the action of estradiol increases 3 times. With daily intake, the concentration of gestodene in the blood plasma increases by 3-4 times and in the second half of the cycle it reaches a saturation state. It is metabolized in the liver.The average plasma clearance is 0.8-1.0 ml / min / kg. The concentration of gestodene in the blood serum decreases in two phases. T1 / 2 in the? -Phase - 12-20 hours. Gestodene is excreted only in the form of metabolites, 60% - with urine, 40% - with feces. T1 / 2 metabolites - about 1 day.

Ethinylestradiol

After oral administration, ethinyl estradiol is rapidly and completely absorbed. Cmax in serum, equal to about 65 pg / ml, is achieved in 1-2 hours. During absorption and 'first pass' through the liver, ethinyl estradiol is metabolized, as a result of which its oral bioavailability averages about 45%. Ethinylestradiol is almost completely (approximately 98%), albeit nonspecifically, bound to albumin. Ethinylestradiol induces the synthesis of SHBG. The apparent Vd of ethinyl estradiol is 2.8-8.6 l / kg. Undergoes presystemic conjugation, both in the mucous membrane of the small intestine and in the liver. The main metabolic pathway is aromatic hydroxylation. The clearance rate from blood plasma is 2.3-7 ml / min / kg. The decrease in the concentration of ethinyl estradiol in the blood serum is biphasic;T1 / 2 in the first phase is about 1 hour, in the second phase - 10-20 hours. It is not excreted from the body unchanged. Ethinyl estradiol metabolites are excreted in the urine and bile in a ratio of 4: 6 with a T1 / 2 of about 24 hours.

Indications

• Oral contraception.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally according to a special scheme.

When taken as part of fixed combinations, a single dose of gestodene is 75 ?g, ethinylestradiol is 20 mg or 30 mg.

Side effect

On the part of 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.

From the senses: hearing loss due to otosclerosis.

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

From the digestive system: epigastric pain, nausea, vomiting, Crohn's disease, ulcerative colitis, the onset or exacerbation of jaundice and / or itching associated with cholestasis, cholelithiasis, hepatitis, liver adenoma.

On the part of the skin and its appendages: erythema nodosum, exudative erythema, rash, chloasma, increased hair loss.

From the neurological system: headache, migraine, mood lability, depression.

From the senses: hearing loss, increased sensitivity of the cornea (when wearing contact lenses).

From the side of metabolism: fluid retention in the body, change (increase) in body weight, decreased tolerance to carbohydrates, hyperglycemia, increased TG levels.

Others: allergic reactions, hemolytic uremic syndrome, porphyria; rarely - exacerbation of reactive systemic lupus erythematosus; very rarely - Sydenham's chorea.

Contraindications for use

• Presence of risk factors for venous thromboembolism;

• the presence of risk factors for the development of arterial thromboembolism;

• severe liver disease (including history) before normalization of liver function indicators;

• liver tumor (including history);

• severe chronic renal failure or acute renal failure;

• known or suspected hormone-dependent malignant tumors (including genital or breast);

• bleeding from the vagina of unclear etiology;

• pregnancy;

• lactation period (breastfeeding).

Application during pregnancy and lactation

Use during pregnancy and lactation (breastfeeding) is contraindicated.

special instructions

The benefits of hormonal contraception should be assessed individually for each woman and discussed with her before starting hormonal contraceptive use.

Combined hormonal contraceptives should be used with caution, incl. fixed combinations of gestodene / ethinylestradiol for conditions that increase the risk of developing venous or arterial thrombosis / thromboembolism: age over 35 years, smoking, hereditary predisposition to thrombosis (thrombosis, myocardial infarction or cerebrovascular accident at a young age in one of the closest relatives), hemolytic uremic syndrome, hereditary angioedema, liver disease, diseases that first appeared or worsened during pregnancy or against the background of previous use of sex hormones (including porphyria, herpes of pregnant women, chorea minor, Sydenham's chorea, chloasma), obesity (BMI more than 30 kg / m2), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valvular heart disease,atrial fibrillation, prolonged immobilization, major surgery, lower limb surgery, severe trauma, varicose veins and superficial thrombophlebitis, postpartum period (non-lactating women / 21 days postpartum /; lactating women after the end of lactation), severe depression , (including history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.major surgery, surgery on the lower extremities, severe trauma, varicose veins and superficial thrombophlebitis, postpartum period (non-breastfeeding women / 21 days after childbirth /; breastfeeding women after the end of lactation), severe depression, (incl. history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus, not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.major surgery, surgery on the lower extremities, severe trauma, varicose veins and superficial thrombophlebitis, postpartum period (non-lactating women / 21 days after childbirth /; lactating women after the end of lactation), severe depression, (incl. history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus, not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.surgery on the lower extremities, severe trauma, varicose veins and superficial thrombophlebitis, the postpartum period (non-lactating women / 21 days after childbirth /; lactating women after the end of the lactation period), the presence of severe depression (including a history) , changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease , ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.surgery on the lower extremities, severe trauma, varicose veins and superficial thrombophlebitis, the postpartum period (non-lactating women / 21 days after childbirth /; lactating women after the end of the lactation period), the presence of severe depression (including a history) , changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease , ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.postpartum period (non-lactating women / 21 days after childbirth /; lactating women after the end of the lactation period), the presence of severe depression (including history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (incl. family history), acute and chronic liver disease.postpartum period (non-lactating women / 21 days after childbirth /; lactating women after the end of the lactation period), the presence of severe depression (including history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (incl. family history), acute and chronic liver disease.antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, incl. antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.antithrombin III deficiency, protein C or S deficiency, antiphospholipid antibodies, incl. antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver diseases.

In case of suspected or established venous or arterial thromboembolism, the use of combined hormonal contraceptives should be discontinued. If anticoagulant therapy is initiated, adequate alternative contraception should be initiated to avoid the teratogenic effects of anticoagulant therapy (coumarins).

The use of any combined oral contraceptive pill increases the risk of venous thromboembolism.

The results of epidemiological studies have made it possible to associate the use of combined hormonal contraceptives with an increased risk of arterial thromboembolism (myocardial infarction) or cerebrovascular accident (for example, transient ischemic attack, stroke). Arterial thromboembolic complications can be fatal.

Some epidemiological studies have noted an increased risk of cervical cancer in women who have been receiving combined oral contraceptives for more than 5 years. However, there is no common point of view about the degree of influence on this disease of sexual behavior and other factors, such as the human papillomavirus.

In women with hypertriglyceridemia or a hereditary predisposition to it, the risk of pancreatitis may be increased when taking combined oral contraceptives.

Although a small increase in blood pressure was observed in many women taking combined oral contraceptives, a clinically significant increase was rare. Only in these rare cases is the immediate discontinuation of combined oral contraceptives justified. If, when taking combined oral contraceptives in patients with concomitant arterial hypertension, blood pressure constantly increases or significantly increased pressure cannot be corrected with antihypertensive drugs, the use of combined oral contraceptives should be discontinued. After normalization of blood pressure with antihypertensive drugs, the use of combined oral contraceptives can be resumed.

While taking combined oral contraceptives, there was an increase in endogenous depression, epilepsy, Crohn's disease and ulcerative colitis.

Drug interactions

Interaction with drugs that induce microsomal enzymes of the cytochrome P450 system is possible, as a result of which the clearance of sex hormones can increase, which, in turn, can lead to acyclic 'breakthrough' uterine bleeding and / or a decrease in the contraceptive effect.

Substances that increase the clearance of a fixed combination of gestodene / ethinylestradiol (decrease in effectiveness due to the induction of liver enzymes): barbiturates, bosentan, carbamazepine, phenytoin, primidone, rifampicin, drugs for the treatment of HIV - ritonavir, nevirapine, efavirenz and possibly also oxcarbamatazepine and preparations containing St. John's wort (Hypericum perforatum).

When used together with a fixed combination of gestodene / ethinyl estradiol, many inhibitors of HIV or hepatitis C virus proteases and non-nucleoside reverse transcriptase inhibitors can both increase and decrease the concentration of hormonal components of the combination in blood plasma. In some cases, this effect may be clinically significant.

When combined with a fixed combination of gestodene / ethinyl estradiol with perampanel, vemurafenib, dabrafenib, modafinil or rufinamide, the likelihood of a decrease in contraceptive effectiveness due to an accelerated metabolism of sex hormones should be taken into account. It is recommended to use additional methods of contraception (intrauterine devices or condoms) throughout the course of joint drug intake and for 2-6 months after its termination.

Strong to moderate inhibitors of the CYP3A4 isoenzyme, such as antifungal agents, azole derivatives (eg, itraconazole, voriconazole, fluconazole), verapamil, macrolides (eg, clarithromycin, erythromycin), diltiazem and grapefruit juice can increase plasma concentrations of estrogen, or both.

NSAIDs reduce the effectiveness of a fixed combination of gestodene / ethinyl estradiol.

Combined oral contraceptives can affect the metabolism of other drugs, so their plasma and tissue concentrations may increase (for example, cyclosporine) or decrease (for example, lamotrigine).

Storage conditions
At a temperature not exceeding 25 ? — in places inaccessible to children

Shelf life is
4 years. Cannot be used after the expiration date!

Terms of dispensing from pharmacies
Prescription. List B.