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

Oral contraception.

Active ingredient

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®.

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:

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

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.

Contraindications

With caution, the drug is prescribed when:

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.

Overdose

Symptoms: nausea, vomiting, vaginal bleeding.

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

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