Gestarella, 75 mcg+20 mcg 63 pcs

Gestarella is a monophasic low-dose combined gestagen-estrogen (gestoden, a derivative of 19-nortestosterone, and ethinyl estradiol) contraceptive drug.

Acting on central and peripheral mechanisms, the drug inhibits secretion of pituitary gonadotropic hormones, inhibits follicle maturation, prevents ovulation, reduces endometrial susceptibility to blastocysts and increases cervical secretion viscosity making it difficult for sperm to enter the uterine cavity.

With the use of the drug regular menstrual bleeding becomes regular, the pain is less pronounced, the intensity of bleeding decreases, resulting in reduction of one of the risk factors of iron deficiency anemia.

Pharmacokinetics

Ethinylestradiol

Intake

Ethinylestradiol is quickly and completely absorbed when ingested. Cmax is approximately 65 pg/mL and is reached after 1.7 hours. During absorption and “primary passage” through the liver, ethinylestradiol undergoes intensive metabolism, as a result, bioavailability when taken orally is on average 45% with large interindividual variability (about 20-65%).

Distribution

Ethinylestradiol binds almost completely to plasma albumin (approximately 98%) and induces the synthesis of sex hormone binding globulin (hSPH). Vd is about 2.8-8.6 L/kg.

In view of the variability of the T1/2 in the final phase and daily administration of the drug, the plasma Css of ethinylestradiol is reached after approximately 1 week.

Metabolism

Ethinylestradiol undergoes presystemic conjugation both in the small intestinal mucosa and in the liver. The main metabolic pathway is aromatic hydroxylation. Clearance of ethinylestradiol is 2.3-7 ml/min/kg.

Elimination

The decrease in the concentration of ethinylestradiol occurs in two phases, which are characterized by a T1/2 of about 1 h and 10-20 h, respectively. Ethinylestradiol is not excreted unchanged, its metabolites are excreted by the kidneys and through the intestine at a ratio of 4:6, respectively. T1/2 is about 24 hours.

Gestoden

Intake

When taken orally, gestoden is quickly and completely absorbed. Cmax is about 4 ng/mL and is reached approximately 1 h after a single dose. Bioavailability is 99%.

Distribution

Gestoden binds to plasma albumin and HSPH. About 1.3% of the total plasma concentration of the drug is in the form of a free steroid, approximately 68% is specifically bound to HSPH.

The induction of hGH synthesis by ethinylestradiol affects the binding of gestodenol to plasma proteins, resulting in an increase in the hGH-bound fraction and a decrease in the albumin-bound fraction.

The Vd is 0.7 L/kg.

The pharmacokinetics of gestodenone depends on the plasma concentration of hGH, which is increased by a factor of 2 when administered together with ethinylestradiol. After repeated administration, plasma concentration of gestoden increases about 4-fold, and Css of the drug is reached during the second half of the therapeutic cycle.

Metabolism

Gestoden is almost completely metabolized. The metabolic clearance rate from plasma is approximately 0.8 ml/min/kg.

Evacuation

The concentration of gestoden decreases in two phases. The final phase is characterized by a T1/2 of 12-15 h.

Unchanged gestoden is not excreted. Its metabolites are excreted by the kidneys and through the intestine in an approximate ratio of 6:4. T1/2 of metabolites is about 24 hours.

Indications

Contraception

Oral contraception.

Active ingredient

Gestoden, Ethinylestradiol

Composition

Active substances:

Ethinylestradiol20 mcg;

Hestoden 75 mcg;

Excipients:

sodium calcium edetate – 0.14 mg,

lactose monohydrate – 36.865 mg,

corn starch – 16 mg,

povidone 25 – 1.7 mg,

magnesium stearate – 0.2 mg;

Shell:

saccharose – 19.631 mg, povidone 90 F – 0.2 mg, macrogol 6000 – 2.18 mg, calcium carbonate – 8.697 mg, talc – 4.242 mg, glycol wax – 0.05 mg

How to take, the dosage

Gestarella® is taken in the order given on the package at about the same time every day. The tablets are taken orally with a small amount of water. During 21 days one tablet is taken daily in succession.
The pills from the next package should be taken the next day after a 7-day break, during which menstrual bleeding occurs. Bleeding usually starts on the 2nd or 3rd day after taking the last pill and may not end until you start taking the pills from the new package.
How to start taking Gestarella®.

• If hormonal contraception was not taken in the previous month.
  The intake of pills should be started on the first day of natural menstrual cycle (i.e. the first day of menstrual bleeding). It is also possible to start the intake from day 2 to day 5 of the menstrual cycle, but in this case it is necessary to use a barrier method of contraception during the first 7 days of the first cycle.
• Transition from another combined oral contraceptive medicine, a vaginal ring or a transdermal patch.
  The use of Gestarella® is best started immediately the day after taking the last active pill (the last pill containing the active ingredient) of the previous contraceptive, but in no case later than the day after the usual 7-day break in pills (for products with 21 pills per pack) or after taking placebo pills of the previous contraceptive (for products with 28 pills per pack). In the case of the transdermal patch the woman should start taking the drug the day after it is removed, but never later than the day on which a new ring is to be inserted or the next patch is to be applied.
• Transition from contraceptives containing only progestagens (“mini-pills”, injectables, implant), or an intrauterine system (IUD) releasing the progestagens.
  Transition from the “minipilli” is possible at any time, from the implant or IUD on the day of their removal, from injections on the day when the next injection is due, but in all these cases it is necessary to use an additional barrier method of contraception during the first 7 days of taking Gestarella®.
• Application after abortion in the first trimester of pregnancy.
  A woman may start taking the drug immediately. In this case no additional contraceptive methods are required.
• Application after delivery or abortion in the second trimester of pregnancy.
  The drug is started after childbirth, in the absence of breastfeeding, or abortion in the second trimester of pregnancy. Gestarella® should be started between the 21st and 28th day after childbirth or second trimester abortion. If the woman starts taking it later, she should use an additional barrier method of contraception during the first 7 days of taking the pills. However, if sexual intercourse took place before the start of taking the drug, it is necessary to rule out pregnancy before starting the contraceptive drug, or the woman should wait for her first menstrual bleeding.

The first menstrual cycle after finishing taking the drug is usually prolonged by 1 week. If within 2-3 months the normal cycle is not restored, it is necessary to consult a doctor.
Taking missed pills.
If you are late in taking the pill for less than 12 hours, contraceptive protection is not compromised. The pill should be taken immediately, as soon as the woman remembers the missed pill, the next pill should be taken at the usual time.
If the pill is taken more than 12 hours late, contraceptive protection may be reduced. In this case, the following basic rules should be followed and appropriate measures should be taken:

1. The pill should never be interrupted for more than 7 days.
2. To achieve the necessary suppression of the hypothalamic-pituitary-ovarian system, a 7-day period of continuous pill taking is required.

In accordance with the above rules, the following is recommended.

• First week of taking the drug.
  The woman should take the last missed pill as soon as she remembers it, even if it means taking two pills at the same time. Thereafter, the pills should be taken at the usual time. Additionally, a barrier method of contraception, such as a condom, should be used for the next 7 days. If the woman was sexually active in the previous 7 days, it is necessary to consider the possibility of pregnancy. The greater the number of missed pills and the closer the skip to a break in taking the drug, the higher the risk of pregnancy.
• The second week of taking the drug.
  The woman should take the last missed pill as soon as she remembers it, even if it means taking two pills at the same time. After that, the pills should be taken at regular times. If the pills were taken regularly for 7 days before the first missed pill, no additional contraceptive measures are needed. If the woman took the pills irregularly or missed more than one pill, additional contraceptive measures are required for 7 days.
• The third week of taking the drug.
  There is a high risk of decreased contraceptive reliability because of the upcoming break in taking the pills. However, despite this, by adjusting your medication regimen, a decrease in contraceptive protection can be prevented. If either of the following two instructions is followed, there is no need for other contraceptive measures, provided that the woman has taken the pills correctly for 7 days before the first missed pill. Otherwise, the woman should follow the first recommendation and take other additional contraceptive measures within 7 days.

1. The woman should take the last missed pill as soon as she remembers it, even if it would mean taking two pills at once. After that, the pills should be taken at the usual time. The woman should start taking the next package immediately after she has finished taking the pills from the previous package. In this way, there will be no break between the pills. Bleeding “cancellations” are unlikely until after the second package, but women may experience little or no bleeding from the vagina.
2. Women may also stop taking pills from the current package. In this case, take a break of 7 days, including any missed days, and then restart taking the pills in a new pack.

If a woman has forgotten to take the pills and during the break in taking the pills she has no bleeding “cancellation,” pregnancy must be ruled out.
Intake in case of gastrointestinal disorders
If the woman had vomiting or diarrhea within 4 hours after taking the pills, absorption may be incomplete and additional contraceptive measures should be taken. In these cases, the recommendations for skipping the pill should be followed.
Changing the day of the beginning of the menstrual cycle
If a woman wants to delay the day of the beginning of menstrual bleeding, she should start taking Gestarella® from the next package without interruption. It is possible to continue taking the new pack for as long as the woman wishes (until the pills in the pack are finished). During this period, the woman may have a “breakthrough” bleeding or a period of spotting. After a 7-day break, the woman should resume taking the pills regularly.
If a woman wants to postpone the start of bleeding to another day of the week, she should shorten the nearest break in taking the pills by as many days as she wants. The shorter the interval, the higher the risk of “withdrawal” bleeding and “breakthrough” bleeding and smeary discharge during the second package (just as in the case of postponing the start of bleeding).

Interaction

Barbiturates, some antiepileptic drugs (carbamazepine, phenytoin) can increase the metabolism of the constituent sex hormones.

It can also potentially enhance hepatic metabolism of the sex hormone HIV proteases (e.g., ritonavir) and non-nucleoside reverse transcriptase inhibitors (e.g., nevirapine) and combinations thereof.

When Gestarella is used concomitantly with liver microsomal enzyme inducers and for 28 days after their withdrawal, an additional barrier method of contraception must be used. A decrease of the effective concentration of the Gestarella drug is observed during concomitant administration of some antibiotics (ampicillin, tetracycline) due to changes in the microflora in the intestine; during therapy and for 7 days after their withdrawal an additional barrier method of contraception must be used.

NSAIDs reduce the effectiveness of Gestarella.

The dosing regimen of hypoglycemic drugs may need to be adjusted. Oral contraceptive drugs may affect the metabolism of other drugs, so their plasma and tissue concentrations may increase (e.g., cyclosporine) or decrease (e.g., lamotrigine).

Contraindications

• Conditions preceding thrombosis (including transient ischemic attacks, angina pectoris), current or history.
• Thrombosis (venous and arterial) and thromboembolism (including deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disorders).
• Discovered 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 (antibodies to cardiolipin, lupus anticoagulant).
• .Multiple or pronounced risk factors for venous or arterial thrombosis, including complicated heart valve lesions (pulmonary hypertension, atrial fibrillation, subacute bacterial endocarditis), coronary artery disease, smoking over age 35, ischemic or hemorrhagic cerebrovascular disorders, extended surgical intervention with prolonged immobilization, extensive trauma, lower extremity surgery.
• Diabetes mellitus type 1 and 2 with vascular complications (angiopathy, retinopathy)
• Obesity (body mass index (BMI) above 30 kg/m2).
• Uncontrolled arterial hypertension (blood pressure (BP) 160/100 mmHg or higher)
• Hepatic failure and acute liver disease or a history of liver disease after which liver function test values have not normalized.
• Pancreatitis with significant hypertriglyceridemia, current or history
• Migraine with focal neurologic symptoms (current or history).
• Epilepsy
• Hormone-dependent malignant diseases of the genitals or mammary glands (including history), hyperprolactinemia, inflammatory diseases of the female reproductive organs (salpingo-oophoritis, endometritis).
• Childhood and adolescence (before menarche).
• Vaginal bleeding of unclear genesis.
• Pregnancy or presumed pregnancy, breast-feeding
• High sensitivity to medicine’s components.
• Galactose intolerance, Lapp intolerance or impaired glucose or galactose absorption, fructose intolerance or sucrase-isomaltase deficiency (the drug contains lactose monohydrate and sucrose).

With caution, the drug is prescribed when:

• the presence of risk factors for venous or arterial thrombosis: myocardial infarction, thrombosis, thromboembolism, cerebrovascular disorders at a young age in a 1st degree relative with a history;
• overweight (BMI between 25.0 and 29.9 kg/m2);
• atherosclerosis and dyslipoproteinemia;
• diabetes mellitus without vascular complications;
• controlled arterial hypertension (BP no higher than 160/100 mm Hg.mbar).
• migraine without focal neurologic symptoms
• varian veins

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• renal dysfunction
• fibrotic cystic mastitis, uterine fibroids
• otosclerosis;
• Missile sclerosis;
• porphyria;
• ystemic lupus erythematosus;
• Missile Sidengam’s choreaSydenham’s chorea;
• chloasma;
• vision impairments and contact lens intolerance;
• Hepatic disorders with a history of normal liver function tests; jaundice or cholestasis in a previous pregnancy or history of taking sex hormones, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson, and Rotor syndromes);
• ser sickle cell anemia, hemolytic-uremic syndrome;
• Cron’s disease and ulcerative colitis;
• tetany;
• phlebitis of superficial veins.

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Side effects

The digestive system: frequently – nausea, abdominal pain; infrequently – vomiting, diarrhea; rarely – cholestasis; very rarely – pancreatitis, cholestasis, hepatocellular adenoma.

Reproductive system and mammary glands: often – feeling of tension, painful mammary glands, acyclic bloody discharge or bleeding from the vagina during the first few months of use, painful menstrual-like bleeding; no menstrual-like bleeding; infrequent – increase of the breast; rarely – discharge from the breast, vaginal dryness, increased libido.

Nervous system disorders: frequently – headache; infrequently – migraine.

Cardiovascular system disorders: very rarely – thrombophlebitis, thromboembolism.

Sensory system disorders: very rarely – hearing loss; rarely – visual impairment, poor tolerance of contact lenses.

Skin and subcutaneous tissue: infrequent – skin rash, including ureticaria; rare – erythema nodosum, erythema multiforme; very rare – with long-term use – chloasma (focal pigmentation).

Others: often – weight gain, anxiety, depression; infrequent – decreased libido, edema, increased blood lipid concentration; rare – allergic reactions (oedema of eyelids, conjunctivitis), dizziness, weight loss; very rare – disorders of sodium and calcium ion exchange.

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Overdose

Symptoms: nausea, vomiting, vaginal bleeding.

Treatment: symptomatic therapy is carried out. There is no specific antidote.

Similarities

Logest, Femoden, Lindinet 30