Diecyclene, 2 mg+0.03 mg 21 pcs

Pharmaceutical group:

Contraceptive (estrogen+gestagen).

Pharmic action:

Diecyclene is a low-dose monophasic oral hormonal contraceptive. Contraceptive effect is based on the interaction of various factors, the most important of which is inhibition of ovulation and change of viscosity of cervical mucus, as a result of which it becomes impermeable for sperm, penetration of sperm through the cervical canal is difficult. If used correctly, the Perl Index (a measure of the number of pregnancies per 100 women using the contraceptive in a year) is less than 1. If the pill is missed or used incorrectly, the Perl Index may increase.

In addition to its contraceptive effect, it has other related positive properties. In women taking combined oral contraceptives, the cycle becomes more regular, the pain, intensity and duration of menstrual bleeding decrease, and as a result the risk of iron deficiency anemia decreases. There is also evidence of a decreased risk of endometrial and ovarian cancer.

The active gestagen component of the drug, dienogest, is a derivative of normestosterone with anti-androgenic activity and has a positive effect on the lipid profile by increasing high-density lipoprotein (HDL) concentrations.

Pharmacokinetics:

Ethinylestradiol:
When taken orally, it is rapidly and completely absorbed. The maximum concentration of estradiol in blood plasma (about 67 pg/ml) is reached after 1.5-4 hours. After absorption and the “first pass” effect through the liver, ethinylestradiol is metabolized, its absolute bioavailability with oral administration is about 44%.

Ethinylestradiol binds significantly to serum albumin (approximately 98%) and induces the synthesis of plasma sex hormone hormone binding globulin (hSPH). The volume of distribution of ethinylestradiol is about 2.8-8.6 L/kg.

Ethinylestradiol undergoes presystemic conjugation both in the mucosa of the small intestine and in the liver. The main metabolic pathway is aromatic hydroxylation with the formation of numerous hydroxylated and methylated derivatives in the form of free metabolites, glucuronide metabolites and sulfates. The blood plasma clearance rate is approximately 2.3-7 ml/min/kg.

Up to 30-50% of metabolites of ethinylsistrradiol a is excreted by the kidneys, 30-40% – through the intestine. Half-life of zestradiol (T1/2) does not exceed 10 hours after a single use of 1 tablet and increases to 15 hours after 3 cycles of the drug.
The equilibrium plasma concentration of ethinylsestradiol with regular use is reached in the second half of cyclic use of the drug.

Dienogest:

In oral administration, it is quickly and almost completely absorbed. The maximum concentration of dienogest in blood serum (about 51 pg/ml) is reached after 2.5 hours. Absolute bioavailability of dienogest is 96%, the equilibrium concentration in blood plasma is reached after 4 days with continuous administration.

90% of the total plasma concentration of dienogest is bound to serum albumin, but does not bind to hGH, or corticosteroid-binding globulin. Ten percent of the total plasma concentration of dienogest is unbound. The distribution volume of dienogest is about 37-45 liters.

It is metabolized mainly by hydroxylation, but also by hydrogenation, conjugation and aromatization with formation of inactive metabolites. After a single dose, the total clearance of dienogest is approximately 3.6 L/h.
After a dose of 0.1 mg/kg, the ratio of dienogest excretion as metabolites by the kidneys to the intestine is 3:1. Only a small amount of unchanged dienogest is excreted by the kidneys. The half-life (T1/2) of dienogest is approximately 8.5-10.8 hours. After oral administration 86% of the administered dose of dienogest is excreted within 6 days; a significant portion of it is excreted within the first 24 hours after administration mainly by the kidneys.

The equilibrium concentration. Induction of globulin synthesis by ethinylestradiol does not affect the pharmacokinetics of dienogest with daily use of the drug, the serum concentration of dienogest increases by 1.5 times.

Indications

– oral contraception;
– treatment of mild to moderate acne and seborrhea.

Active ingredient

Composition

1 tablet:

– ethinylestradiol 0.03 mg

– dienogest 2 mg

How to take, the dosage

Enally, daily, preferably at the same time, in the order indicated on the package, with a small amount of water. Take 1 tablet a day continuously for 21 days. Taking pills from each subsequent package begins after a 7-day break, during which there is bleeding “cancellation” (menstrual-like bleeding). It usually starts on 2-3 days after taking the last pill and may last until the beginning of taking the pill from the new package.
If you have not taken any hormonal contraceptives in the previous month, the drug starts on the first day of the menstrual cycle (the first day of menstrual bleeding). It is allowed to start taking the product on days 2-5 of the menstrual cycle, but in this case it is recommended to use an additional barrier method of contraception during the first 7 days of taking the pills from the first package.

If you are switching from a previous use of other combined oral contraceptives, it is preferable to start the product the day after taking the last active pill in the previous package, but no later than the day after the usual 7-day gap in intake (for products containing 21 pills) or after taking the last inactive pill (for products containing 28 pills in a package).

When switching from a vaginal ring to a transdermal patch, it is preferable to start Diecyclene on the day the ring or patch is removed, but no later than the day the new ring or patch is to be inserted.
When switching from contraceptives containing only gestagens (“mini-pills”, injectable forms, implant) the drug is taken: from “mini-pills” – on any day (without a break), from the implant – on the day of its removal, from the injectable form – from the day when the next injection should have been made. In all cases, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the pills.

After an abortion in the first trimester of pregnancy, it is possible to start taking immediately. No additional contraceptive protection is necessary if this condition is met.

After childbirth or a second trimester abortion, it is recommended that Diecyclene be started 21-28 days after childbirth or abortion If started later, an additional barrier method of contraception should be used during the first 7 days of taking the pills. However, if a woman has already been sexually active, before starting to take the drug, pregnancy should be excluded or it is necessary to wait for the first menstruation.

Recommendations in case of irregular use of Diecyclen:

In case of missing the drug if the delay in taking the pill was less than 12 hours, contraceptive protection is not reduced. It is necessary to take the pill as soon as possible, the next pill is taken at the usual time. If the delay in taking the pill was more than 12 hours, contraceptive protection may be reduced.

In the first 2 weeks of taking the drug, if the interval from taking the last pill is more than 36 hours: it is necessary to take the last missed pill as soon as possible (even if this means taking 2 pills at once). The next tablet is taken at the usual time. In addition, a barrier method of contraception (condom) must be used for the next 7 days. If there was sexual intercourse within 1 week before skipping the pill, it is necessary to consider the possibility of pregnancy. The more pills you miss and the closer you miss to a 7-day break in your medication, the greater the risk of pregnancy.

In the 3rd week of taking the drug, if the interval since the last pill is more than 36 hours: you should take the last missed pill as soon as possible (even if this means taking 2 pills at the same time). The next tablet is taken at the usual time. Additionally, a barrier method of contraception (condom) must be used for the next 7 days. In addition, the pill from the new pack should be started as soon as the current pack is finished, i.e. without interruption. It is likely that there will be no bleeding “cancellation” until the end of the pills from the second pack, but there may be a “smeary” discharge or uterine bleeding “breakthrough” on the days of taking the pills.

If a woman misses taking the pill and then has no bleeding “withdrawal” during a break in the medication, pregnancy must be ruled out.

In gastrointestinal disorders:

If a woman had vomiting or diarrhea within 3 to 4 h after taking Diecyclene, absorption may be incomplete. In this case, it is necessary to be guided by the recommendations regarding skipping taking the pill. If a woman does not want to change the normal regimen of taking the drug, she should take an additional tablet from the spare package, if necessary.

Change the day of the beginning of menstrual bleeding:

To delay the start of menstrual-like bleeding, you must continue taking pills from the new pack immediately after taking all pills from the previous pack, without interruption of intake. The pills from the new pack may be taken until the pack is finished. While taking the pills from the second package, a woman may have “masticatory” discharge or “breakthrough” uterine bleeding.

Resume taking the drug from the new pack after the usual 7-day break.
In order to postpone the day of menstrual bleeding to another day of the week, you should shorten the nearest break in taking Dietsiklen tablets by as many days as necessary to postpone the day of the beginning of menstrual bleeding. The shorter the interval, the higher the risk of no “cancellation” bleeding and the subsequent occurrence of “smeary” discharge and “breakthrough” bleeding while taking pills from the second pack (just as in the case of delaying the start of menstrual-like bleeding).

Interaction

Some drugs can increase the rate of metabolic clearance of sex hormones and lead to significant bleeding or to a decrease in the contraceptive effect of the drug. Such effects are characteristic of drugs that induce microsomal liver enzymes: hydantoin, barbiturates, primidone, carbamazepine and rifampicin. There are also suggestions for rifabutin, efavirenz, nevirapine, oxcarbazenine, topiramate, felbamate, ritonavir, nelvinafir, fiseofulvin, and drugs containing St. John’s wort (Hypericum perforatum).
Some antibiotics that reduce intestinal hepatic circulation of estrogen (such as ampicillin or tetracycline) reduce the effectiveness of combined oral contraceptives.

Women taking short courses (maximum 1 week) of the above drugs should use additional contraceptive measures (e.g., barrier methods) during concomitant use of the drugs and in the following 7 days.

In case of concomitant use of oral contraceptives with rifampicin, additional contraceptive measures (e.g., barrier method) should be used during concomitant use of the drugs and in the next 4 weeks after discontinuation of treatment. If the package of oral contraceptives ends before the end of the course of other drugs, the pills from the next package of the drug should be started without a break.

The dose of contraceptives should be increased during a long-term course of treatment with drugs that induce microsomal liver enzymes. If side effects develop (e.g., irregular menstruation) or if the drug is ineffective, other non-hormonal contraceptives should be used additionally. Peroral contraceptives can affect the metabolism of some other drugs. Accordingly, this may lead to an increase (cyclosporine) or decrease (lamotrigine) in their plasma or tissue concentrations.

Dienogest is a cytochrome P450 (CYP3A4) substrate. Known CYP3A4 inhibitors such as antifungal drugs (e.g., ketoconazole), cimetidine, verapamil, macrolides (e.g., erythromycin), diltiazem, antidepressants and grapefruit juice may increase plasma concentrations of dienogest.

Special Instructions

Ingregular use may lead to acyclic bleeding and reduce the contraceptive effectiveness of the drug.
Before starting or resuming use of the drug, it is recommended to perform a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical scrape), exclude pregnancy. In addition, blood clotting system disorders should be excluded. When using the drug at least once every 6 months it is necessary to conduct preventive control examinations.

Dietsiklen does not protect against HIV infection (AIDS) and other sexually transmitted diseases.

Cardiovascular diseases:

Possible venous thromboembolism (VTE) in the form of deep vein thrombosis and/or pulmonary embolism when using hormonal contraceptives. The estimated incidence of VTE in women taking low-dose estrogen oral contraceptives (less than 50 mcg ethinyl estradiol) is up to 4 per 10,000 women per year, compared with 0.5-3 per 10,000 women not using oral contraceptives. However, the incidence of VTE developing while taking combined oral contraceptives is lower than the incidence of pregnancy-related VTE (6 per 10,000 pregnant women per year).
In women taking combined oral contraceptives, extremely rare cases of thrombosis of other blood vessels, such as hepatic, mesenteric, renal arteries and veins or vein and retinal arteries, have been described. The association of these cases with the use of combined oral contraceptives has not been proven. A woman should stop taking the drug and consult a physician if she develops symptoms of venous or arterial thrombosis, which may include unilateral lower extremity pain and/or swelling; sudden severe chest pain; with or without irradiation into the left arm; sudden shortness of breath; sudden bouts of cough; any unusual, severe, prolonged headache increased frequency and severity of migraine; sudden partial or total loss of vision; diplopia; slurred speech or aphasia; dizziness; collapse with or without partial seizure; weakness or very significant loss of sensation, suddenly appearing on one side or in one part of the body; motor disorders; “acute” abdomen.

The risk of thrombosis (venous and/or arterial) and thromboembolism increases: with age, in smokers (with increasing number of cigarettes smoked or increasing age the risk further increases, especially in women over 35), with a family history (i.e. venous or arterial thromboembolism ever in a close relative or parent at a relatively young age), obesity dyslipoproteinemia, arterial hypertension, heart valve disease, prolonged immobilization, extensive surgery, any lower extremity surgery or extensive trauma, atrial fibrillation.

In case of prolonged immobilization, major surgery, any lower extremity surgery, or extensive trauma, it is advisable to discontinue the drug (if surgery is planned, at least 4 weeks before) and not resume for 2 weeks after the end of immobilization.

The possible role of varicose veins and superficial thrombophlebitis in venous thromboembolism remains controversial. An increased risk of thromboembolism in the postpartum period should be considered.

Microcirculatory disorders may also be seen in diabetes mellitus, SLE, hemolytic-uremic syndrome, Crohn’s disease, ulcerative colitis and sickle cell anemia.

Tumors:

The most significant risk factor for cervical cancer is persistent papillomavirus infection. There have been reports of some increased risk of cervical cancer with long-term use of combined oral contraceptives. However, the association with taking combined oral contraceptives has not been proven. The possibility of an association of these findings with cervical disease screening and with patterns of sexual behavior (less frequent use of barrier methods of contraception) is discussed.

A meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk of breast cancer diagnosed in women currently taking combined oral contraceptives (relative risk 1.24). The increased risk gradually disappears within 10 years of stopping these drugs. Because breast cancer is rare in women under 40 years of age, the increase in breast cancer diagnoses in women currently taking the combined oral contraceptives or who have recently taken them is small relative to the overall risk of the disease. The relationship between the development of breast cancer and taking the combined oral contraceptives has not been proven. The observed increase in risk can also be a consequence of careful observation and earlier diagnostics of breast cancer in women using combined oral contraceptives. Women who have ever used combined oral contraceptives are detected earlier stages of breast cancer than women who have never used them.

In rare cases, development of benign, and in extremely rare cases, malignant liver tumors have been observed during the use of combined oral contraceptives, which in some cases led to life-threatening intra-abdominal bleeding. If severe abdominal pain, liver enlargement, or signs of intra-abdominal bleeding occur, this should be considered when making a differential diagnosis.

Other conditions:

Women with hypertriglyceridemia or a family history of it may have an increased risk of developing pancreatitis when taking combined oral contraceptives.

While small increases in blood pressure (BP) have been described in many women taking combined oral contraceptives, clinically significant increases have rarely been reported. However, if persistent, clinically significant arterial hypertension develops while taking the combined oral contraceptives, discontinuation of the combined oral contraceptives and treatment of arterial hypertension is appropriate. The combined oral contraceptives may be continued if normal BP values are achieved with hypotensive therapy.

Impacts on the menstrual cycle:

In the background of combined oral contraceptives, irregular (acyclic) bleeding (“mastic” bleeding or “breakthrough” bleeding) may occur, especially during the first months of use. Therefore, any irregular bleeding should be evaluated only after an adjustment period of approximately 3 cycles.

If irregular bleeding recurs or develops after previous regular cycles, a thorough evaluation should be performed to rule out malignancy or pregnancy.

Some women may not develop “withdrawal” bleeding during a break in the pill. However, if the combined oral contraceptive has not been taken consistently before, or if there have not been two consecutive “withdrawal” bleeds, pregnancy should be ruled out before continuing the medication.

The effect on laboratory test values:

The use of oral combination contraceptives may affect the results of some laboratory tests, including blood chemistry (indicators of liver, thyroid, kidney, and adrenal function, plasma transport protein concentrations (such as HSPG), carbohydrate metabolism, lipid/lipoprotein fractions), and coagulation and fibrinolysis parameters. However, changes in these indicators remain within normal values.

Impact on the ability to drive vehicles and mechanisms:

There are no data on the negative effect of the drug Diecyclen on the ability to drive vehicles and engage in potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

– hypersensitivity to any of the ingredients of Dietsiklen;
– thrombosis (venous and arterial) and thromboembolism at present or in the anamnesis (including deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke, cerebrovascular disorders);
– Conditions preceding thrombosis (including transient ischemic attacks, angina pectoris), current or anamnesis;
– Multiple or expressed risk factors for venous or arterial thrombosis, including complicated heart valve lesions, atrial fibrillation, diseases of the brain vessels or coronary arteries; Uncontrolled arterial hypertension, massive surgery with prolonged immobilization, smoking over 35 years of age, obesity with a body mass index of 30 kg/m2;
– Diabetes mellitus with diabetic angiopathy;
– diagnosed predisposition to venous or arterial thrombosis, including resistance to activated protein C, antithrombin III deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia, antibodies to phospholipids, lupus antigen;
– severe liver diseases (prior to restoration and normalization of laboratory liver function parameters);
– benign or malignant liver tumors, including in anamnesis.In the anamnesis;
– severe forms of arterial hypertension with blood pressure >160/100 mm Hg;
– detected hormone-dependent malignant diseases of genitals or mammary glands or suspicion of them, including in the anamnesis. In anamnesis;
– vaginal bleeding of unknown genesis;
– migraine with focal neurological symptoms at the present moment or in the anamnesis;
– pancreatitis accompanied with expressed hypertriglyceridemia at the present moment or in the anamnesis;
– severe and/or acute renal insufficiency;
– pregnancy or suspected pregnancy;
– lactation period;
– hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome or hypersensitivity to peanuts or soy (due to the presence of lactose and soy lecithin in the preparation Dietsiklen).
With caution:
Risk factors for thrombosis and thromboembolism: Obesity, smoking, dyslipoproteinemia, arterial hypertension, migraine without focal neurological symptoms, heart valve defects, prolonged immobilization, major surgery, extensive trauma, hereditary predisposition to thrombosis (thrombosis, myocardial infarction or cerebral circulation disorder at a young age in any of the immediate family members).
Other diseases in which peripheral circulatory disorders may be noted: diabetes without diabetic angiopathy, surface vein phlebitis, systemic lupus erythematosus (SLE), hemolytic-uremic syndrome, Crohn’s disease, ulcerative colitis, sickle cell anemia.
Illnesses that first occurred or worsened during pregnancy or on previous sex hormone administration, such as jaundice and/or pruritus with cholestasis, gallbladder disease, porphyria, Sydenham’s chorea, herpes in pregnancy history, hearing impairment (associated with otosclerosis).
Endogenous depression, epilepsy; hereditary angioedema; hypertriglyceridemia; liver disease; postpartum period.

Overdose

Possible symptoms of overdose of the drug Diecyclen: nausea, vomiting, irregular bloody discharge, absence of menstrual bleeding.

If necessary, symptomatic therapy is carried out.

Similarities