Levonorgestrel

Brand Gedeon Richter

In stock 1836 Items

Available since: 2019-09-19

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Clinical Pharmacology

Postinor - a synthetic drug with a contraceptive effect, pronounced progestogenic and antiestrogenic properties. With the recommended dosing regimen, levonorgestrel suppresses ovulation and fertilization, if sexual intercourse occurs during the pre-ovulation 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.

Efficacy: using Postinor pills can prevent pregnancy in approximately 85% of cases. The more time elapsed between 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). Thus, it is recommended to start taking Posinor pills as soon as possible (but not later than 72 hours) after sexual intercourse, if no protective measures have been applied. At the recommended dose, levonorgestrel does not significantly affect blood clotting factors, fat and carbohydrate metabolism.

Pharmacokinetics

When oral Postinor drug quickly and almost completely absorbed. Absolute bioavailability is almost 100% of the dose. After administration of 0.75 mg of levonorgestrel Cmax in serum, equal to 14.1 ng / ml, is reached after 1.6 h. After reaching Cmax, the content of levonorgestrel 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. Biotransformation of levonorgestrel corresponds to the metabolism of steroids. Levonorgestrel is hydroxylated in the liver, metabolites are excreted in the form of conjugated glucuronides. Pharmacologically active metabolites of levonorgestrel are unknown. Levonorgestrel binds to serum albumin and sex hormone-binding globulin (SHBG). Only 1.5% of the entire dose is in free form, and 65% is associated with SHBG.

Indications

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

Composition

active substance: levonorgestrel 0.75 mg;

Excipients: colloidal silicon dioxide - 0.5 mg; magnesium stearate - 1 mg; talc - 2.5 mg; corn starch - 23.5 mg; potato starch - 0.5 mg; lactose monohydrate - 71.25 mg

Levonorgestrel is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Postinor	Gedeon Richter	Hungary	pills
Escapelle®	Gedeon Richter	Hungary	pills
Mirena	Bayer Pharma AG	Germany	Other

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Dosage and Administration

For oral use You must take 2 pills in the first 72 hours after unprotected intercourse: the 2nd pill should be taken 12 hours (but no later than 16 hours) after taking the 1st pill.

To achieve a more reliable effect, both pills should be taken as soon as possible after unprotected intercourse (no later than 72 hours).

If vomiting occurs within 3 hours after the 1st or 2nd dose of a postinor pill, 1 more pill should be taken.

Postinor can be used at any time during the menstrual cycle. In the case of an irregular menstrual cycle, you must first exclude pregnancy.

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

Adverse reactions

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

Transient side effects that occur with varying frequency and do not require drug therapy:sometimes (1-10%) - vomiting, diarrhea, dizziness, headache, breast tenderness, menstruation delay (no more than 5-7 days; if menstruation is delayed for a longer period, it is necessary to exclude pregnancy); often (more than 10%) - nausea, fatigue, abdominal pain, acyclic bleeding (bleeding).

Contraindications

WITHcaution: diseases of the liver and biliary tract, jaundice (including history), Crohn's disease, lactation.

Drug interactions

With simultaneous administration of liver enzyme inducer drugs, levonorgestrel metabolism accelerates.

Others may reduce the effectiveness of levonorgestrel: amprekavil, lansoprazole, nevirapine, oxcarbazepine, tacrolimus, topiramate, tretinoin, barbiturates, including primidone, phenytoin, and carbamazepine, preparations that contain St. John's wort (Hypericum perforatum, and others, and the same,), with carbamazepine. rifabutin, griseofulvin. Levonorgestrel reduces the effectiveness of hypoglycemic and anticoagulant (coumarin derivatives, phenindione) drugs. Increases plasma concentrations of GCS. Women taking these drugs should consult a doctor.

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

Pregnancy and Lactation

Postinor is contraindicated for use during pregnancy. If pregnancy has arisen while applying an emergency method of contraception, then on the basis of the available data, no adverse effect of the drug on the fetus has been identified.

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

Special instructions

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

The effectiveness of postinor pills after unprotected intercourse, in which contraceptives were not used, decreases with time:

The time between intercourse and taking postinor pills (h)	Efficiency (%)
24 or less	95
25-48	85
49-72	58

The drug does not replace the use of permanent methods of contraception. In most cases, Postinor does not affect the nature of the menstrual cycle. However, the appearance of acyclic bleeding and delayed menstruation for several days is possible. With a delay of menstruation for more than 5-7 days and a change in its nature (scanty or heavy discharge), it is necessary to exclude pregnancy. The appearance of lower abdominal pain, fainting states may indicate ectopic (ectopic) pregnancy.

Adolescents under 16 in exceptional cases (incl.for rape) a gynecologist's consultation is required to confirm pregnancy.

After emergency contraception, a gynecologist's consultation is recommended to select the most appropriate method of permanent contraception.

Emergency contraception does not protect against sexually transmitted diseases.

In cases of dysfunction of the gastrointestinal tract (for example, Crohn’s disease), the effectiveness of the drug may decrease.

Influence on ability to drive motor transport and control mechanisms

The influence of Postinor on the ability to drive vehicles and machinery has not been studied.