Escapelle. Escapel ® (Escapelle ®) Escapel 1.5 mg

Postcoital contraceptive with a pronounced gestagenic and antiestrogenic effect. With the recommended dosing regimen, it suppresses ovulation and fertilization if sexual intercourse occurred in the preovulatory phase of the menstrual cycle, i.e. during the period of greatest probability of fertilization. In addition, the regression of endometrial proliferation caused by the drug prevents the implantation of a fertilized egg. When implantation has taken place, the drug is ineffective.

It is recommended to start taking Escapel® as soon as possible (but no later than 72 hours) after sexual intercourse, if no protective measures have been taken. The more time elapsed between sexual intercourse and taking the drug, the lower its effectiveness (95% during the first 24 hours, 85% - from 24 to 48 hours, and 58% - from 48 to 72 hours).

Pharmacokinetics

Suction

After oral administration, levonorgestrel is rapidly and completely absorbed from the gastrointestinal tract. Cmax of the active substance in plasma is reached after 2 hours and is 18.5 ng / ml. Absolute bioavailability is 100%.

Distribution

Levonorgestrel binds to albumin and sex hormone-binding globulin (SHBG). 1.5% of the total amount in plasma is in the form of a free steroid, 65% is specifically associated with SHBG.

Metabolism

Biotransformation of levonorgestrel corresponds to the metabolism of steroids. Levonorgestrel is hydroxylated in the liver and metabolites are excreted in the form of conjugated glucuronides. Pharmacologically active metabolites of levonorgestrel are unknown.

breeding

After reaching Cmax, the concentration of levonorgestrel in plasma decreases. T1 / 2 is 26 hours. Levonorgestrel is excreted approximately equally by the kidneys and through the intestines exclusively in the form of metabolites.

Pharmacokinetics in special clinical situations

Diseases of the gastrointestinal tract, occurring with impaired absorption, reduce the absorption of the drug, which may affect its effectiveness.

Release form

Tablets white or almost white, flat, round, chamfered and engraved "G00" on one side.

Excipients: potato starch, anhydrous colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate.

1 PC. - blisters (1) - packs of cardboard.

Dosage

The drug is taken orally at 1.5 mg (1 tab.) As soon as possible, but no later than 72 hours after unprotected intercourse (the effectiveness of emergency contraception with delayed use of the drug is significantly reduced). If vomiting occurs within 3 hours after ingestion, then Escapel should be taken again at a dose of 1.5 mg (1 tab.).

The drug can be used at any time of the menstrual cycle. In case of an irregular menstrual cycle, pregnancy must be excluded.

After taking the drug Escapelle ® before the onset of the next menstruation, local barrier methods of contraception (for example, a condom) should be used. The use of the drug during repeated unprotected intercourse during one menstrual cycle is not recommended due to an increase in the frequency of acyclic spotting / bleeding.

Overdose

Symptoms: increased severity of side effects.

Treatment: symptomatic therapy, there is no specific antidote.

Interaction

With the simultaneous use of the drug Escapel ® with inducers of liver enzymes, the metabolism of levonogestrel is accelerated.

The contraceptive effect of the drug Escapel ® is reduced when used simultaneously with the following drugs: amprenavir, lansoprazole, nevirapine, oxycarbazepine, tacrolimus, topiramate, tretinoin, barbiturates, including primidone, phenytoin and carbamazepine, preparations containing St. John's wort, as well as rifampicin, ritonavir, ampicillin , tetracycline, rifabutin, griseofulvin.

Escapel ® reduces the effectiveness of hypoglycemic and anticoagulant (coumarin derivatives, phenindione) drugs.

Levonorgestrel increases plasma concentrations of corticosteroids.

Preparations containing levonorgestrel may increase the risk of cyclosporine toxicity due to the suppression of its metabolism.

Side effects

Allergic reactions: possibly - urticaria, rash, itching, swelling of the face.

The following are transient adverse reactions that occur with varying frequency and do not require drug therapy: very often (≥1/10), often (≥1/100,<1/10).

From the digestive system: very often - nausea; often - vomiting, diarrhea.

From the side of the central nervous system: very often - fatigue; often - headache, dizziness.

From the reproductive system: very often - pain in the lower abdomen, acyclic spotting (bleeding); often - soreness of the mammary glands, delayed menstruation (no more than 5-7 days). If menstruation is delayed for a longer period, pregnancy must be excluded.

Indications

Emergency (postcoital) contraception (after unprotected intercourse or unreliability of the contraceptive method used).

Contraindications

severe liver failure;
use in adolescents under 16 years of age;
pregnancy;
lactose intolerance, lactase deficiency or glucose/galactose malabsorption;
hypersensitivity to the components of the drug.

With caution, the drug should be used in patients with diseases of the liver or biliary tract, with jaundice (including history), Crohn's disease, during lactation.

Application features

Use during pregnancy and lactation

Escapel ® is contraindicated for use during pregnancy. Based on the available data, there was no adverse effect of the drug on the fetus in the event of pregnancy against the background of the use of an emergency method of contraception.

Levonorgestrel is excreted in breast milk. After taking the drug, breastfeeding should be stopped for 24 hours.

Application for violations of liver function

Contraindicated in liver diseases.

special instructions

This medicine is for emergency contraception only and does not replace regular contraception. Repeated use of the drug Escapel ® during one menstrual cycle is not recommended.

Escapel should be taken as soon as possible, but no later than 72 hours after unprotected intercourse. The effectiveness of emergency contraception with delayed use of the drug is significantly reduced.

In most cases, Escapel ® does not affect the nature of the menstrual cycle. However, there may be acyclic spotting and a delay in menstruation for several days. With a delay in menstruation for more than 5-7 days and a change in its nature (scanty or heavy discharge), pregnancy must be excluded. The appearance of pain in the lower abdomen, fainting may indicate an ectopic (ectopic) pregnancy.

Adolescents under 16 in exceptional cases (including rape) need to consult a gynecologist to confirm pregnancy. After emergency contraception, a consultation with a gynecologist is recommended to select the most appropriate method for permanent contraception.

Emergency contraception does not protect against sexually transmitted diseases.

With violations of the function of the gastrointestinal tract (for example, with Crohn's disease), the effectiveness of the drug may decrease.

Influence on the ability to drive vehicles and control mechanisms

The effect of the drug on the ability to drive vehicles and other mechanisms has not been studied.

Postcoital contraceptive. Gestagen

Active substance

Levonorgestrel (levonorgestrel)

Release form, composition and packaging

Pills white or almost white, flat, round, chamfered and engraved "G00" on one side.

Excipients: potato starch, colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate.

1 PC. - blisters (1) cardboard packs.

pharmachologic effect

Levonorgestrel is a synthetic progestogen with a contraceptive effect, pronounced progestogenic and antiestrogenic properties. With the recommended dosing regimen, levonorgestrel suppresses ovulation and fertilization if sexual contact occurs in the pre-ovulatory phase, when the possibility of fertilization is greatest. It can also cause changes in the endometrium that prevent implantation. The drug is not effective if implantation has already occurred.

Efficiency: it is recommended to start taking Escapel as soon as possible (but no later than 72 hours) after sexual intercourse, if no protective measures have been taken. The more time elapsed between sexual intercourse and taking the drug, the lower its effectiveness (95% during the first 24 hours, 85% - from 24 to 48 hours, and 58% - from 48 to 72 hours). At the recommended dose, levonorgestrel does not have a significant effect on blood coagulation factors, fat and carbohydrate metabolism.

Pharmacokinetics

Suction

After oral administration, levonorgestrel is rapidly and completely absorbed from the gastrointestinal tract. After taking one tablet of the drug Escapel, Cmax of the active substance is reached after 2 hours and is 18.5 ng / ml. Absolute bioavailability is 100%.

Distribution

Levonorgestrel binds to albumin and sex hormone-binding globulin (SHBG). 1.5% of the total amount in plasma is in the form of a free steroid, 65% is specifically associated with SHBG.

Metabolism

breeding

After reaching Cmax, the concentration of levonorgestrel in plasma decreases. T1 / 2 is about 26 hours. Levonorgestrel is excreted approximately equally by the kidneys and through the intestines exclusively in the form of metabolites.

Pharmacokinetics in special clinical situations

Diseases of the gastrointestinal tract, occurring with impaired absorption, reduce the absorption of the drug, which may affect its effectiveness.

Indications

- emergency (postcoital) contraception (after unprotected sexual intercourse or unreliability of the contraceptive method used).

Contraindications

- hypersensitivity to the components of the drug;

- severe liver failure;

- use in adolescents under 16 years of age;

- pregnancy;

- lactose intolerance, lactase deficiency or malabsorption / galactose.

Carefully the drug should be used in patients with diseases of the liver or biliary tract, with jaundice (including history), during lactation.

Dosage

The drug can be used at any time of the menstrual cycle. In case of an irregular menstrual cycle, pregnancy must be excluded.

After taking the drug Escapelle before the onset of the next menstruation, local barrier methods of contraception (for example, a condom) should be used. The use of the drug during repeated unprotected intercourse during one menstrual cycle is not recommended due to an increase in the frequency of acyclic spotting / bleeding.

Side effects

Allergic reactions: possibly - urticaria, rash, itching, swelling of the face.

The following are transient adverse reactions that occur with varying frequency and do not require drug therapy: very often (≥1/10), often (≥1/100,<1/10).

From the digestive system: very often - nausea; often - vomiting, diarrhea.

From the nervous system: very often - fatigue; often - headache, dizziness.

From the reproductive system: very often - pain in the lower abdomen, acyclic spotting (bleeding); often - soreness of the mammary glands, delayed menstruation (no more than 5-7 days). If menstruation is delayed for a longer period, pregnancy must be excluded.

Overdose

Symptoms: increased severity of side effects.

Treatment: symptomatic therapy, there is no specific antidote.

drug interaction

With the simultaneous use of the drug Escapel with inducers of liver enzymes, the metabolism of levonogestrel is accelerated.

The contraceptive effect of the drug Escapelle is reduced when used simultaneously with the following drugs: amprenavir, lansoprazole, oxcarbazepine, tacrolimus, topiramate, tretinoin, barbiturates, including primidone, phenytoin and carbamazepine, drugs containing St. John's wort , as well as rifampicin, ritonavir, ampicillin, tetracycline, griseofulvin.

Escapel reduces the effectiveness of hypoglycemic and anticoagulant (coumarin derivatives, phenindione) drugs.

Levonorgestrel increases plasma concentrations of corticosteroids.

Preparations containing levonorgestrel may increase the risk of toxicity due to the suppression of its metabolism.

special instructions

Escapel should only be used for emergency contraception. Repeated use of the drug Escapel during one menstrual cycle is not recommended.

Escapelle should be taken as soon as possible, but no later than 72 hours after unprotected intercourse. The effectiveness of emergency contraception with delayed use of the drug is significantly reduced.

The drug does not replace the use of permanent methods of contraception.

In most cases, Escapelle does not affect the nature of the menstrual cycle. However, there may be acyclic spotting and a delay in menstruation for several days. With a delay in menstruation for more than 5-7 days and a change in its nature (scanty or heavy discharge), pregnancy must be excluded. The appearance of pain in the lower abdomen, fainting may indicate an ectopic (ectopic) pregnancy.

After emergency contraception, a consultation with a gynecologist is recommended to select the most appropriate method for permanent contraception.

Emergency contraception does not protect against sexually transmitted diseases.

With violations of the function of the gastrointestinal tract (for example, with Crohn's disease), the effectiveness of the drug may decrease.

Teenagers under 16 in exceptional cases (including rape), a gynecologist's consultation is necessary to confirm pregnancy.

The effect of the drug on the ability to drive vehicles and mechanisms

The effect of the drug on the ability to drive a car and other machines has not been studied.

Pregnancy and lactation

Escapelle is contraindicated for use during pregnancy. Based on the available data, there was no adverse effect of the drug on the fetus in the event of pregnancy against the background of the use of an emergency method of contraception.

Description of Vidal 2007

Representation:

GEDEON RICHTER A/O

Registration certificate holder:

GEDEON RICHTER Ltd.

ATX code: G03AC03

Release form, composition and packaging

Tablets white or almost white, flat, round, chamfered and engraved "GOO" on one side. 1 tab.

levonorgestrel 1.5 mg

Excipients: potato starch, anhydrous colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate.

1 PC. - blisters (1) cardboard packs.

Clinico-pharmacological group: Postcoital contraceptive for oral administration

Registration Nos.:

tab. 1.5 mg: 1 pc. - P No. 015924/01, 10/21/04

pharmachologic effect

Postcoital contraceptive with a pronounced gestagenic and antiestrogenic effect. Causes inhibition of ovulation if sexual intercourse takes place in the preovulatory phase of the menstrual cycle, i.e. during the period of greatest probability of fertilization. In addition, the regression of endometrial proliferation caused by the drug prevents the implantation of a fertilized egg. When implantation has taken place, the drug is ineffective.

The effectiveness of contraception decreases as the time elapsed between intercourse and taking the drug increases. Subject to the recommended dosing regimen, levonorgestrel does not have a significant effect on blood coagulation factors, fat and carbohydrate metabolism.

The risk of pregnancy is on average 1.1%.

Pharmacokinetics

Suction

After oral administration, levonorgestrel is rapidly and completely absorbed from the gastrointestinal tract. Cmax of the active substance in plasma is reached after 2 hours and is 18.5 ng / ml.

Distribution

Levonorgestrel binds to albumin and sex hormone-binding globulin (SHBG). 1.5% of the total amount in plasma is in the form of a free steroid, 65% is specifically associated with SHBG.

After taking 1 tab. Escapela average concentration of SHBG in the blood is approximately 40 nmol / l. Within 24 hours, the concentration of SHBG in the blood remains unchanged or slightly increases, then begins to decrease and after 190 hours is approximately 30 nmol / l. Absolute bioavailability is 100% of the dose taken.

It is allocated with breast milk; when breastfeeding, about 0.1% of the dose taken with breast milk enters the child's body.

Metabolism

Levonorgestrel is metabolized in the liver by hydroxylation. Pharmacologically active metabolites of levonorgestrel are unknown.

breeding

The decrease in the concentration of levonorgestrel in the blood plasma has a two-phase character. T1 / 2 is 2-7 hours. 60% is excreted in the urine as metabolites and 40% in the feces.

Pharmacokinetics in special clinical situations

Diseases of the gastrointestinal tract, occurring with impaired absorption, reduce the absorption of the drug, which may affect its effectiveness.

Indications

Emergency (postcoital) contraception.

Dosing regimen

The drug is prescribed at a dose of 1.5 mg (1 tab.) during the first 96 hours after intercourse.

Side effect

On the part of the endocrine system: rarely - a feeling of tension in the mammary glands, menstrual irregularities (a temporary change in the nature of the menstrual cycle is possible in the form of a delay in menstruation, usually not exceeding 5-7 days).

From the digestive system: rarely - nausea, vomiting, diarrhea.

From the side of the central nervous system: rarely - fatigue, headache, dizziness.

Other: rarely - pain in the lower abdomen.

Contraindications

Diseases of the liver or biliary tract;

Jaundice (including history);

puberty;

Pregnancy;

Hypersensitivity to the components of the drug.

Pregnancy and lactation

Escapelle is contraindicated for use during pregnancy.

If necessary, the use of the drug during lactation after taking Escapel should stop breastfeeding for 36 hours.

special instructions

This medicine is for emergency contraception and does not replace regular contraception. It is recommended to ensure regular contraception after using Escapelle: either use barrier contraceptives, such as a condom, until the next menstruation, or continue taking an oral hormonal contraceptive if started earlier.

It is not allowed to use Escapel as a means of permanent and continuous contraception, because. this leads to a decrease in the effectiveness of the drug and an increase in adverse reactions. With regular sexual activity, permanent methods of contraception should be used.

Levonorgestrel does not prevent fertilization in all cases. In the case when the time of sexual intercourse is not exactly known, or when more than 96 hours have passed since intercourse without contraception, the probability of fertilization is high. If menstruation is delayed by more than 7 days, as well as in the case when the timely onset of menstruation is unusual, or there is a suspicion of pregnancy for any other reason, a gynecological examination should be performed to exclude pregnancy.

In cases where Escapel was used due to an error in regular hormonal contraception, and there is no menstruation in the subsequent seven-day break, pregnancy should be excluded.

If vomiting occurs within 3 hours after taking the tablet, the effectiveness of Escapel is reduced.

Diseases of the gastrointestinal tract, occurring with violations of the absorption process, reduce the absorption of the drug, which may also affect its effectiveness.

Escapela tablet can be taken on any day of the menstrual cycle, provided that the previous menstruation was normal.

The use of the drug, as a rule, does not violate the regularity and normal nature of menstruation. Sometimes earlier or late (about 2 days) appearance of menstruation is possible.

Repeated use of Escapel tablets during the same menstrual cycle should be avoided in order to avoid its violations.

In patients with a history of ectopic pregnancy, fallopian tube surgery, pelvic inflammatory disease, the use of levonorgestrel may be an additional risk factor for ectopic pregnancy. If there is pain in the lower abdomen, fainting, a history of ectopic pregnancy, surgery on the pelvic organs or their inflammation, an ectopic pregnancy should be excluded.

Postcoital administration of Escapel does not protect against sexually transmitted diseases.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Pills white or almost white, flat, round, chamfered and engraved "GOO" on one side.

Excipients: potato starch, anhydrous colloidal silicon dioxide, magnesium stearate, talc, corn starch, lactose monohydrate.

1 PC. - blisters (1) cardboard packs.

Clinical and pharmacological group

Postcoital oral contraceptive

pharmachologic effect

Pharmacokinetics

Suction

Distribution

Levonorgestrel binds to albumin and sex hormone-binding globulin (SHBG). 1.5% of the total amount in plasma is in the form of a free steroid, 65% is specifically associated with SHBG.

Metabolism

breeding

Pharmacokinetics in special clinical situations

Diseases of the gastrointestinal tract, occurring with impaired absorption, reduce the absorption of the drug, which may affect its effectiveness.

Indications for the use of the drug

- emergency (postcoital) contraception (after unprotected sexual intercourse or unreliability of the contraceptive method used).

Dosing regimen

The drug can be used at any time of the menstrual cycle. In case of an irregular menstrual cycle, pregnancy must be excluded.

Side effect

Allergic reactions: possibly - urticaria, rash, itching, swelling of the face.

The following are transient adverse reactions that occur with varying frequency and do not require drug therapy: very often (≥1/10), often (≥1/100, 1/10).

From the digestive system: very often - nausea; often - vomiting, diarrhea.

From the side of the central nervous system: very often - fatigue; often - headache, dizziness.

Contraindications to the use of the drug

- severe liver failure;

- use in adolescents under 16 years of age;

- pregnancy;

- lactose intolerance, lactase deficiency or malabsorption of glucose / galactose;

- Hypersensitivity to the components of the drug.

WITH caution the drug should be used in patients with diseases of the liver or biliary tract, with jaundice (including history), Crohn's disease, during lactation.

The use of the drug during pregnancy and lactation

Levonorgestrel is excreted in breast milk. After taking the drug, breastfeeding should be stopped for 24 hours.

Application for violations of liver function

Contraindicated in liver diseases.

special instructions

This medicine is for emergency contraception only and does not replace regular contraception. Repeated use of the drug Escapel ® during one menstrual cycle is not recommended.

Emergency contraception does not protect against sexually transmitted diseases.

With violations of the function of the gastrointestinal tract (for example, with Crohn's disease), the effectiveness of the drug may decrease.

Influence on the ability to drive vehicles and control mechanisms

The effect of the drug on the ability to drive vehicles and other mechanisms has not been studied.

Overdose

Symptoms: increased severity of side effects.

Treatment: symptomatic therapy, there is no specific antidote.

drug interaction

With the simultaneous use of the drug Escapel ® with inducers of liver enzymes, the metabolism of levonogestrel is accelerated.

The contraceptive effect of the drug Escapel ® is reduced when used simultaneously with the following drugs: amprenavir, lansoprazole, nevirapine, oxycarbazepine, tacrolimus, topiramate, tretinoin, barbiturates, including primidone, phenytoin and carbamazepine, preparations containing St. John's wort , as well as rifampicin, ritonavir, ampicillin, tetracycline, rifabutin, griseofulvin.

Escapel ® reduces the effectiveness of hypoglycemic and anticoagulant (coumarin derivatives, phenindione) drugs.

Levonorgestrel increases plasma concentrations of corticosteroids.

Preparations containing levonorgestrel may increase the risk of cyclosporine toxicity due to the suppression of its metabolism.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

List B. The drug should be stored out of the reach of children at a temperature of 15 ° to 25 ° C. Shelf life - 5 years.