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Gestarelle tabs 75mcg + 20mcg #63

Gestarelle tabs 75mcg + 20mcg #63


(In stock)

  • Gestarelle tabs 75mcg + 20mcg #63 Gestarelle tabs 75mcg + 20mcg #63

Gestarelle tabs 75mcg + 20mcg #63

Quick Overview

Active substances: ethinyl estradiol 20 mcg; Gestodene 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: sucrose - 19.631 mg, povidone 90 F - 0.2 mg, macrogol 6000 - 2.18 mg, calcium carbonate - 8.697 mg, talc - 4.242 mg, wax, hot glycolic - 0.05 mgPackaging21 and 63 pcs.

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Gestarelle instruction

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Active substances: ethinyl estradiol 20 mcg Gestodene 75 mcgExcipients: sodium calcium edetate - 0.14 mg, lactose monohydrate - 36.865 mg, corn starch - 16 mg, povidone 25 - 1.7 mg, magnesium stearate - 0.2 mgShell: sucrose - 19.631 mg, povidone 90 F - 0.2 mg, macrogol 6000 - 2.18 mg, calcium carbonate - 8.697 mg, talc - 4.242 mg, wax, hot glycolic - 0.05 mgPackaging21 and 63 pcs.

pharmachologic effect

Gestarelle is a monophasic, low-dose, combined progestogen-estrogen (gestodene, a derivative of 19-nortestosterone, and ethinyl estradiol) contraceptive drug. Influencing the central and peripheral mechanisms, the drug inhibits the secretion of pituitary gonadotropic hormones, inhibits follicle maturation, interferes with the ovulation process, reduces the endometrial susceptibility to the blastocyst and increases the viscosity of the cervix secretion, making it difficult for sperm to enter the uterus.In addition to the contraceptive effect with regular use, the drug also has a therapeutic effect, normalizing hormonal status, and thus, helping to prevent the development of a number of gynecological diseases, including including endometrial cancer and ovarian cancer. Against the background of the drug, regular menstrual bleeding is established, pain is less pronounced, the intensity of bleeding decreases, as a result of which one of the risk factors for the development of iron deficiency anemia is reduced.


Ethinyl Estradiol

SuctionWhen ingestion, ethinyl estradiol is rapidly and completely absorbed. Cmax is approximately 65 pg / ml and is reached after 1.7 hours. During absorption and “initial passage” through the liver, ethinyl estradiol is extensively metabolized, resulting in an average oral bioavailability of 45% with large inter-individual variability (about 20-65%) .DistributionEthinyl estradiol is almost completely bound to plasma albumin (approximately 98%) and induces the synthesis of sex hormone-binding globulin (SHBG). Vd is about 2.8-8.6 l / kg.Taking into account the T1 / 2 variability in the final phase and the daily intake of the Css drug ethinyl estradiol in the blood plasma is reached in approximately 1 week.MetabolismEthinyl estradiol undergoes presystemic conjugation, both in the small intestinal mucosa and in the liver. The main metabolic pathway is aromatic hydroxylation. Ethinyl estradiol clearance is 2.3-7 ml / min / kg.RemovalThe decrease in the concentration of ethinyl estradiol occurs in two phases, which are characterized by T1 / 2 about 1 h and 10-20 h, respectively. Ethinyl estradiol is not excreted unchanged, its metabolites are excreted by the kidneys and through the intestines at a ratio of 4: 6, respectively. T1 / 2 is about 24 hours.


SuctionWhen ingestion, gestodene is quickly and completely absorbed. Cmax is about 4 ng / ml and is reached approximately 1 hour after taking a single dose. Bioavailability is 99%.DistributionGestodene binds to plasma albumin and SHBG. About 1.3% of the total plasma concentration of the drug is in the form of a free steroid, approximately 68% is specifically associated with SHBG.Induction of ethylene estradiol synthesis of SHBG affects the binding of gestodene to plasma proteins, which leads to an increase in the fraction associated with SHBG, and a decrease in the fraction associated with albumin.Vd is 0.7 l / kg.The pharmacokinetics of gestodene depends on the concentration of HSPG in the blood plasma, which increases 2-fold when administered with ethinyl estradiol. After repeated administration, the concentration of gestodene in plasma increases about 4 times, and the Css of the drug is reached during the second half of the therapeutic cycle.MetabolismGestodene is almost completely metabolized. The rate of metabolic clearance from plasma is about 0.8 ml / min / kg.RemovalThe concentration of gestodene decreases in two phases. The final phase is characterized by T1 / 2 12-15 h.In unchanged form, gestodene is not displayed. Its metabolites are excreted by the kidneys and through the intestines in an approximate ratio of 6: 4. T1 / 2metabolites is about 24 hours.

Gestarelle, indications for use

Oral contraception.

Contraindications for Gestarelle

Dosage and administration

Gestarelle is taken in a certain order, indicated on the package, every day at about the same time. Tablets are taken orally with a small amount of water. For 21 days, take one pill daily.Taking the pills from the next pack should be started the next day after a 7-day break, during which menstrual-like bleeding occurs. Bleeding usually starts 2-3 days after taking the last pill and may not end before taking the pills from a new package.

How to start taking Gestarelle

Acceptance of missed pills

Reception in case of gastrointestinal disturbances

If a woman has vomiting or diarrhea within 4 hours after taking the pills, absorption may not be complete and additional contraceptive measures should be taken. In these cases, you should focus on the recommendations when skipping the pill.

Change the day of the beginning of the menstrual cycle

If a woman wants to delay the day of the onset of menstrual bleeding, she should start taking Gestarelle from the next package without interruption. It is possible to continue taking the drug from the new package as long as the woman wants (up to the end of the tablets in the package). During this period, "breakthrough" bleeding or spotting may occur. After a 7-day break, a woman should resume regular drug intake.If a woman wants to postpone the onset of bleeding to another day of the week, then the nearest pause in taking the pills should be reduced to as many days as she wants. The shorter this interval, the higher the risk of bleeding "cancellation" and the appearance of "breakthrough" bleeding and spotting during the reception of the second package (as well as in the case of transfer of the onset of bleeding).

Side effects

On the part of the digestive system: often - nausea, abdominal pain infrequently - vomiting, diarrhea rarely - cholestasis very rarely - pancreatitis, cholestasis, hepatocellular adenoma.On the part of the reproductive system and the mammary gland: often - a feeling of tension, tenderness of the mammary glands, acyclic bleeding or bleeding from the vagina during the first few months of administration, painful menstrual-like bleeding no menstrual bleeding infrequently - an increase in the mammary glands rarely - discharge from the mammary glands, vaginal dryness, increased libido.From the nervous system: often - headache infrequently - migraine.Since the cardiovascular system: very rarely - thrombophlebitis, thromboembolism.From the senses: very rarely - loss of hearing rarely - blurred vision, poor tolerance to contact lenses.On the part of the skin and subcutaneous tissues: infrequently - skin rash, incl. urtikarnaya rarely, erythema nodosum, erythema multiforme very rarely - with prolonged use - chloasma (focal pigmentation).Others: often - weight gain, anxiety, depression infrequently - decreased libido, edema, increased concentration of lipids in the blood rarely - allergic reactions (eyelid edema, conjunctivitis), dizziness, weight loss very rarely - metabolic imbalance of sodium and calcium.


Barbiturates, some antiepileptic drugs (carbamazepine, phenytoin) can increase the metabolism of sex hormones that make up Gestarelle.Prolonged use of drugs that induce microsomal liver enzymes, which increases the clearance of sex hormones, may cause breakthrough bleeding and / or decrease the contraceptive efficacy of Gestarelle. Such drugs include: phenytoin, barbiturates, primidone, carbamazepine and rifampicin there are also suggestions regarding oxcarbazepine, topiramate, felbamate, ritonavir, griseofulvin and preparations containing St. John's wort.The hepatic metabolism of the sex hormones of HIV protease (for example, ritonavir) and non-nucleoside reverse transcriptase inhibitors (for example, nevirapine) and their combinations can also potentially increase.With the simultaneous use of the drug Gestarelle with drugs-inducers of microsomal liver enzymes and within 28 days after their withdrawal, you must additionally use a barrier method of contraceptionA decrease in the effective concentration of the drug Gestarelle is observed with the simultaneous prescription 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 method of contraception must be used.NSAIDs reduce the effectiveness of the drug Gestarelle.May require correction dosage regimen hypoglycemic drugs. Oral contraceptive drugs can affect the metabolism of other drugs, so their concentrations in plasma and tissues may increase (for example, cyclosporine) or decrease (for example, lamotrigine).


Symptoms: nausea, vomiting, vaginal bleeding.Treatment: conduct symptomatic therapy. There is no specific antidote.Shelf life - 3 years

Storage conditions

Gestarelle should be stored out of the reach of children at a temperature not higher than 25 ° C.

Terms of sell

You can buy Gestarelle without a prescription.


Additional Information

SKU fh2618
The purpose of the medication Contraception
Weight kg. 0.05

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