Gestarelle tabs 75mcg + 20mcg #63

Gestarelle instruction

You can buy Gestarelle here

Composition

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 mg
Packaging
21 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.

Pharmacokinetics

Ethinyl Estradiol

Suction
When 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%) .
Distribution
Ethinyl 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.
Metabolism
Ethinyl 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.
Removal
The 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.

Gestoden

Suction
When 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%.
Distribution
Gestodene 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.
Metabolism
Gestodene is almost completely metabolized. The rate of metabolic clearance from plasma is about 0.8 ml / min / kg.
Removal
The 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

    The states preceding thrombosis (including transient ischemic attacks, angina pectoris) are currently or in history.
    Thrombosis (venous and arterial) and thromboembolism currently or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disorders).
    Identified susceptibility 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 severe risk factors for venous or arterial thrombosis, including complications of cardiac valve apparatus (pulmonary hypertension, atrial fibrillation, subacute bacterial endocarditis), coronary artery disease, smoking after the age of 35, ischemic or hemorrhagic cerebrovascular disorders, expanded cerebral vascular disease, expanded after 35 years of age, ischemic or hemorrhagic cerebrovascular disorders, expanded cerebral vascular disease, expanded after 35 years of age, ischemic or hemorrhagic cerebrovascular disorders, expanded cerebral vascular disease, expanded after 35 years of age, ischemic or hemorrhagic cerebrovascular disorders, expanded cerebral artery disease, expanded after 35 years of age, ischemic or hemorrhagic cerebrovascular disorders, expanded cerebral arteries, expanded cerebrovascular disease, expanded cerebrovascular accident intervention with prolonged immobilization, extensive trauma, surgery on the lower limbs.
    Diabetes mellitus type 1 and 2 with vascular complications (angiopathy, retinopathy)
    Obesity (body mass index (BMI) is above 30 kg / m2).
    Uncontrolled arterial hypertension (blood pressure indicators (BP) 160/100 mm Hg. Art. And above).
    Liver failure and acute or liver disease in history, after which the indicators of functional liver tests were not normalized.
    Benign or malignant liver tumors now or in history.
    Pancreatitis with severe hypertriglyceridemia now or in history.
    Migraine with focal neurological symptoms (currently or in history).
    Epilepsy
    Hormone-dependent malignant diseases of the genital or mammary glands (including a history of), hyperprolactinemia, inflammatory diseases of the female genital organs (salpingoophoritis, endometritis).
    Children and adolescents (before menarche) age.
    Bleeding from the vagina of unknown origin.
    Pregnancy, including the estimated period of breastfeeding.
    Hypersensitivity to Gestarelle.
    Galactose intolerance, Lappa lactase deficiency or impaired absorption of glucose and galactose, fructose intolerance, or sucrase-isomaltase deficiency (the preparation contains lactose monohydrate and sucrose).
With caution, the drug is prescribed for:
    the presence of risk factors for venous or arterial thrombosis: myocardial infarction, thrombosis, thromboembolism, cerebrovascular disorders at a young age in relatives of the 1st degree of kinship in history;
    overweight (BMI ranging from 25.0 to 29.9 kg / m2);
    atherosclerosis and dyslipoproteinemia;
    diabetes without vascular complications;
    controlled arterial hypertension (blood pressure not higher than 160/100 mm Hg);
    migraine without focal neurological symptoms;
    varicose veins;
    impaired renal function;
    fibrocystic mastopathy, uterine myoma;
    otosclerosis;
    multiple sclerosis;
    porphyrias;
    systemic lupus erythematosus;
    Sydenham's chorea;
    chloasma;
    visual impairment and contact lenses intolerance;
    a history of liver diseases with normal liver function tests; jaundice or cholestasis during a previous pregnancy or against the background of a history of taking sex hormones, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes);
    sickle cell anemia, hemolytic-uremic syndrome;
    Crohn's disease and ulcerative colitis;
    tetany;
    phlebitis of superficial veins.

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

    If in the previous month hormonal contraception was not carried out.
    Pills should be taken on the first day of the natural menstrual cycle (that is, on the first day of menstrual bleeding). You can also start the reception from the 2nd to the 5th day of the menstrual cycle, but it is necessary to use a barrier method of contraception during the first 7 days of the first cycle.
    Transfer from another oral oral contraceptive pill, vaginal ring or transdermal patch.
    It is best to start taking Gestarelle immediately the next day after taking the last active pill (last tablet containing the active substance) of the previous contraceptive drug, but in no case later than the next day after the usual 7-day break in taking the pills (for drugs with 21 tablets per pack) or after taking the placebo tablets of the previous contraceptive preparation (for drugs with 28 tablets per pack). In the case of a transdermal patch, a woman should start taking Gestarelle the day after it was removed, but in no case no later than the day when it is necessary to inject a new ring or stick the next patch.
    The transition from contraceptives containing only progestogens ("mini-pilli", injections, implant), or the intrauterine system (IUD), releasing the prostate gene.
    Switching from “mini-saws and” is possible at any time, from an implant or an IUD on the day of their removal, from injections on the day when the next injection is to be given, but in all these cases it is necessary to use an additional barrier method of contraception during the first 7 days taking the drug Gestarelle.
    Application after abortion in the first trimester of pregnancy.
    A woman can start taking the drug immediately. In this case, the use of additional contraceptive methods is not required.
    Use after childbirth or abortion in the second trimester of pregnancy.
    Gestarelle is started after delivery, in the absence of breastfeeding of the child, or abortion in the second trimester of pregnancy. Reception of the drug Gestarelle should begin between the 21st and 28th day after childbirth or abortion during the second trimester. If a woman starts later, she needs to use an additional barrier method of contraception during the first 7 days of taking the pills. However, if sexual contact was before the start of the drug, it is necessary to exclude pregnancy before using the contraceptive drug, or the woman should wait for her first menstrual bleeding.
Usually, the first menstrual cycle after the end of taking the drug is extended by 1 week. If within 2-3 months the normal cycle is not restored, it is necessary to consult a doctor.

Acceptance of missed pills

If you are late in taking the pill for less than 12 hours, contraceptive protection is not impaired. The pill must 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 late for more than 12 hours, contraceptive protection may be reduced. In this case, you must follow the following basic rules and take appropriate measures:
    Taking pills should never be interrupted for more than 7 days.
    To achieve the necessary inhibition of the hypothalamic-pituitary-ovarian system requires a 7-day period of continuous administration of tablets.
In accordance with the above rules, the following is recommended.
    The first week of taking the drug.
    A woman should take the last missed pill as soon as she remembers, even if it means taking two pills at the same time. After that, tablets should be taken at the usual time. Additionally, over the next 7 days, you should use a barrier method of contraception, for example, a condom. If a woman had sex in the previous 7 days, it is necessary to take into account the possibility of pregnancy. The greater the number of missed pills and the closer the pass to a break in taking Gestarelle, the higher the risk of pregnancy.
    The second week of taking the drug.
    A woman should take the last missed pill as soon as she remembers, even if it means taking two pills at the same time. After that, tablets should be taken at the usual time. If the pill is taken regularly for 7 days before the first missed pill, no additional contraceptive measures are required. If the woman took the pills irregularly or missed more than one pill, additional contraceptive measures should be taken within 7 days.
    The third week of taking the drug.
    Due to the upcoming break in the pill there is a high risk of reducing the reliability of contraception. However, despite this, adjusting the regimen of Gestarelle, a decrease in contraceptive protection can be prevented. When one of the following two guidelines 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 adhere to the first recommendation and take other additional contraceptive measures within 7 days.
    A woman should take the last missed pill as soon as she remembers, even if it means taking two pills at the same time. After that, tablets should be taken at the usual time. A woman should start taking from the next pack immediately after completing taking the pills from the previous pack. Thus, the break between the packages will be absent. “Cancellation” bleeding is unlikely until the second package ends, but there may be scant bleeding or profuse bleeding from the vagina.
    A woman may also stop taking pills from the current package. In this case, you need to take a break for 7 days, including the days of skipping, then start taking pills from a new package.
If a woman has forgotten to take pills and during a break in taking pills she has no “withdrawal” bleeding, it is necessary to exclude pregnancy.

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.

Interaction

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 contraception
A 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).

Overdose

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.