Topogin (Topogin)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceMisoprostolMisoprostol
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    • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    Active substance: misoprostol - 0.200 mg.

    Excipients: cellulose microcrystalline - 175.8 mg, hypromellose - 20.0 mg, sodium carboxymethyl starch (type A) 3.0 mg, castor oil ordinary oil - hydrogenated 1.0 mg.

    Description:Tablets are flat-cylindrical, round, with a risk on one side and a facet on both sides, white or almost white. Above the risk in the form of a dent print is the letter "M", under the risk - the number "200".
    Pharmacotherapeutic group:Generic activity stimulant - prostaglandin E1 analogue synthetic
    ATX: & nbsp

    G.02.A.D.06   Misoprostol

    G.02.A.D.   Prostaglandins

    Pharmacodynamics:

    Misoprostol is a synthetic derivative of prostaglandin E1. Misoprostol induces contraction of smooth muscle fibers of myometrium and expands the cervix, which facilitates the removal of the contents of the uterine cavity. Increases the frequency and strength of contractions of the myometrium, has a weak stimulating effect on the smooth muscles of the gastrointestinal tract (GIT).

    Pharmacokinetics:

    Suction

    When administered orally misoprostol quickly absorbed. Taking misoprostol with food does not change the bioavailability of the active metabolite (misoprostol acid), but reduces the maximum concentration in the plasma due to slower adsorption. The time to reach the maximum concentration of misoprostol acid is approximately 30 minutes, maximum concentration (Cmax) - 1 μg / l, half-life (T1/2) - 20-40 minutes. In case of impaired renal function FROMmax may increase in 2 times, extend T1 / 2.

    Distribution

    In blood plasma, misoprostol acid binds to proteins by less than 90%. Do not cumulate.

    Metabolism

    Metabolism of misoprostol occurs in the walls of the gastrointestinal tract and liver to pharmacologically active misoprostol acid.

    Excretion

    It is excreted by the kidneys - 64-73% during the first 24 hours (56% within the first 8 hours) and with bile (15% within the first 24 hours).

    Indications:

    The drug interruption of developing uterine pregnancy in the early stages (duration of amenorrhea not more than 42 days) in combination with mifepristone.

    Contraindications:- hypersensitivity to misoprostol and / or to any other component of Topogin and other prostaglandin preparations;

    - cardiovascular diseases;

    - diseases associated with prostaglandin dependence, or contraindications to the use of prostaglandins: glaucoma, bronchial asthma, arterial hypertension;

    - endocrinopathy and endocrine system diseases, including diabetes mellitus, adrenal insufficiency;

    - acute or chronic renal and / or liver failure;

    - hormone-dependent tumors;

    - anemia;

    - disturbance of homeostasis;

    - pregnancy for more than 42 days amenorrhea;

    - pregnancy, which is not confirmed by ultrasound or biological test;

    - the period of breastfeeding;

    - children's age till 18 years;

    - use of intrauterine contraceptives (IUDs) (before removal it is necessary to remove IUD);

    - suspicion of ectopic pregnancy;

    - contraindications to the use of mifepristone.

    Carefully:

    The risk of cardiovascular disorders

    Rare but severe cases of cardiovascular disorders (myocardial infarction and / or coronary artery spasm or severe pressure reduction) were noted with intravaginal or intramuscular injection of a large dose of prostaglandin analog, including misoprostol. For this reason, women with a risk factor for cardiovascular diseases (for example, age over 35, chronic smoking, hyperlipidemia) should apply Topogin with caution.

    Rhesus alloinimization

    In case of medical abortion, it is necessary to determine Rh and then to take measures to prevent Rh-alloimulation, as well as other general measures that are usually taken with any other method of abortion.

    The use of contraception after drug abortion

    In clinical trials, it was found that the next pregnancy occurs between embryo release and the resumption of menstruation. For this reason, it is recommended that you start taking the contraceptive immediately after the medical confirmation of the abortion, carried out by the medication method.

    Other

    Also, follow the precautionary measures that apply to the use of mifepristone.

    Pregnancy and lactation:

    Pregnancy

    Misoprostol can be used during pregnancy ONLY to interrupt it. The use of mifepristone and misoprostol or only misoprostol during pregnancy can lead to the formation of birth defects / deformities.Prenatal exposure to misoprostol is associated with the development of Mobius syndrome (congenital impairment of facial nerve functions that can be accompanied by limb defects) and amniotic constriction syndrome (limb deformities / amputations, especially clubfoot, Achaea, oligochtilia and, among other things, wolf mouth). Women who decide to terminate the pregnancy with a medication method should receive detailed advice about the risk of teratogenic effects on the fetus (see section "Special instructions") if the abortion is not completed and the repeated termination of pregnancy is undesirable.

    Consequently:

    - Women should be warned that, because of the risk of failure of drug-induced abortion and the risk to the fetus, a follow-up visit to the doctor is mandatory.

    - When diagnosing the failure of the method during a follow-up visit to the doctor (viable continuation of the pregnancy) and with the patient's consent, the abortion must be completed with the procedure of repeated termination of pregnancy.

    - If the patient wishes to keep the pregnancy, it is necessary to conduct a thorough ultrasound scan in a specialized center.

    Breast-feeding

    Mifepristone is a lipophilic compound and, theoretically, can be excreted into the mother's breast milk. However, there is no data on this. Misoprostol can also be excreted into breast milk and, therefore, women should avoid breast-feeding while using mifepristone or misoprostol.

    Breastfeeding should be discontinued for 7 days after medical abortion (starting from the moment of taking mifepristone).

    Dosing and Administration:

    Inside. Misoprostol is taken orally for 2 tablets 200 mcg (400 mcg) after 36-48 hours after a single dose of 200 mg or 600 mg of the drug mifepristone. Information on doses of mifepristone can be found in the instructions for use of mifepristone.

    A vomiting attack within the first 30 minutes after taking Topogin can lead to a decrease in the effectiveness of misoprostol.

    The patient should be under the supervision of medical personnel, at least within 3 hours after taking Topogin.

    Side effects:

    Undesirable phenomena classified by organs and systems are listed below in order of decreasing frequency of detection: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1000 to <1 / 100), rarely (from> 1/10 000 to <1/1 000), very rarely (<1/10 000), the frequency is unknown (to establish the frequency of which the data not enough).

    Infectious and parasitic diseases: often due to an abortion.

    Immune system disorders: frequency unknown - anaphylactic shock, hypersensitivity.

    Impaired nervous system: rarely - a headache.

    Vascular disorders: rare, but severe, cases of cardiovascular disorders (myocardial infarction and / or spasm of the coronary arteries or a strong decrease in pressure) were noted, mainly with the prohibited intravaginal route of misoprostol tablets.

    Disorders from the gastrointestinal tract: very often - nausea, vomiting, diarrhea; often - spasms.

    Disturbances from the skin and subcutaneous tissues: infrequent skin rash; rarely - an allergic rash, erythroderma, erythema nodosum, toxic epidermal necrolysis; very rarely - Quincke's edema.

    Disturbances from the musculoskeletal and connective tissue: frequency unknown - back pain.

    Violations of the genitals and breast: very often - contractions of the uterus or spasms in the first hours after taking misoprostol; often - heavy bleeding.

    General disorders and disorders at the site of administration: rarely - malaise, symptoms of vagal nerve damage (hot flashes, dizziness, chills), high fever.

    Overdose:

    Symptoms: sedation, tremor, cramps, dyspnoea, abdominal pain, diarrhea, fever, bleeding, coronary artery spasm, hypotension and bradycardia.

    Treatment: symptomatic, hemodialysis is ineffective.

    Interaction:

    Antacids can reduce the bioavailability of misoprostol.

    Antacids containing magnesium can increase diarrhea caused by the use of misoprostol.

    The decrease in the effectiveness of misoprostol can theoretically occur due to the anti-prostaglandin properties of non-steroidal anti-inflammatory drugs, including acetylsalicylic acid. Limited data suggest that the combined use of non-steroidal anti-inflammatory drugs on the day of misoprostol administration does not adversely affect the effects of mifepristone or misoprostol on cervical ripening or uterine contractions and do not reduce the clinical effectiveness of drug-induced abortion.

    The use for a long time of rifampicin, isoniazid, anticonvulsants, antidepressants, cimetidine, indomethacin and barbiturates, smoking more than 10 cigarettes a day stimulates the metabolism of misoprostol, reducing its concentration in the blood serum.

    Special instructions:

    In combination with mifepristone misoprostol should be applied only to the appointment and supervision of an obstetrician and gynecologist and only in medical obstetric and gynecological institutions related to the public health system, as well as in municipal and private property, licensed for this type of activity and appropriately trained medical personnel and necessary equipment.

    When the pregnancy is interrupted, the patients should be informed:

    - the need to combine the use of misoprostol with the use of mifepristone, which should be taken 36-48 hours before taking Topogin; application of the drug outside the established regime entails ALL relevant risks;

    - about the need to visit again for 14-21 days after taking misoprostol to confirm the complete expulsion of the fetal egg (clinical examination, ultrasound of pelvic organs and determination of the concentration of β-hCG in the blood plasma);

    - that in case of ineffectiveness of application of Topogin on day 14 (incomplete abortion or continuing pregnancy) pregnancy must be interrupted by an operative route (the possibility of congenital malformations in the fetus);

    - on the decrease in the effectiveness of the method with increasing age of the woman;

    - about the possibility of prolonged bleeding from the vagina (on average about 12 days or more after taking Topogin), up to profuse bleeding that lasts more than 12 days and / or is more abundant than normal menstrual bleeding (in this connection it is not recommended to go to long trips until the full abortion is confirmed).

    A woman should receive clear instructions as to where to apply if she heavy bleeding or any other problems. Continuing bloody vaginal discharge may indicate incomplete abortion or undiagnosed ectopic pregnancy, to exclude these conditions appropriate examination and treatment should be carried out. In the case of heavy bleeding (1.4% of cases) may require scraping of the uterine cavity with gemostaticheskoy goal, in this regard, special attention should be paid to patients with disorders of hemostasis and anemia. The decision to use Topogin in such cases should be taken in conjunction with specialists, depending on the type of hemostasis disorder and the severity of anemia.

    Risks associated with the use of the drug

    The effectiveness of the drug abortion method is reduced:

    - when the specified mode of application of the drug Topogin is not observed,

    - in the presence of twins.

    Bleeding

    Bleeding occurs in almost all cases, but it is not an indisputable confirmation of the complete termination of pregnancy.

    Bleeding occurs almost immediately after taking Topogin, but sometimes occurs later:

    - in 60% of cases, abortion occurs within 4 hours after taking Topogin;

    - in 40% of cases, abortion occurs within 24-72 hours after taking Topogin. In rare cases, bleeding can begin before taking Topogin (about 3% of cases). This DOES NOT cancel a check-up visit to the doctor to confirm a complete termination of the pregnancy and complete liberation of the uterus.

    Infections

    Severe cases (including fatal) of toxic or septic shock due to infections caused by atypical pathogens (Clostridium sordellii and Clostridium perfringens, Klebsiella pneumoniae, Escherichia coli, streptococcus group A), were observed with medical abortions, produced through a prohibited vaginal or buccal method of using misoprostol tablets. Doctors should be aware of the possibility of deadly complications.

    Cardiovascular disorders

    Rare, but serious complications from the cardiovascular system were recorded after intramuscular injection of the prostaglandin analog. In this regard, it should be treated with extreme caution to patients with risk factors for development or established cardiovascular diseases. During the admission and within 3 hours after taking prostaglandin, the patient should be in a medical institution in order not to miss possible acute conditions caused by the use of prostaglandin.

    Teratogenicity

    Patients who decide to remain pregnant after a medical interruption should be informed of the risk of teratogenicity.This risk is an inherent consequence of the use of mifepristone and misoprostol and occurs when treatment regimens are used other than the only acceptable regimen specified in the section "Dosing and Administration". The effects of misoprostol and mifepristone on the fetus increase the risk of Moebius syndrome and / or amniotic constriction syndrome. It is necessary to take measures for the re-termination of pregnancy. If pregnancy persists, a thorough ultrasound scan at a specialized center should be carried out (see "Application in pregnancy and during breastfeeding").

    Ability to childbearing

    Misoprostol does not affect fertility. A woman can again conceive as soon as the previous pregnancy is completely interrupted. Therefore, it is important to warn the patient about the need to use contraceptives right after confirmation of complete termination of pregnancy.

    Effect on the ability to drive transp. cf. and fur:

    Data on the effect on the ability to drive a vehicle are unknown. As a side effect, dizziness may occur.When driving a vehicle and using various mechanisms, it is necessary to take into account the possibility of this side effect.

    Form release / dosage:Tablets, 200 mcg.
    Packaging:

    For 4 tablets in PVC / PTFE / A1-blister or A1 / A1-blister.

    For 1 blister, along with instructions for medical use, put in a pack of cardboard.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Leave conditions

    The drug can be supplied only in medical obstetrics and gynecology institutions related to the public health system, as well as to institutions of municipal and private property that have licenses for this type of activity.

    Shelf life:

    18 months - for PVC / PTFE / Al-blasters.

    2 years - for Al/Al-blasters.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:For hospitals
    Registration number:LP-004275
    Date of registration:28.04.2017
    Expiration Date:28.04.2022
    The owner of the registration certificate:ExceleljinExceleljin France
    Manufacturer: & nbsp
    Representation: & nbspIZVARIN PHARMA LLC IZVARIN PHARMA LLC Russia
    Information update date: & nbsp05.06.2017
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