Levonorgestrel

Левоноргестрел Constitutional formula

The description is actual on 02.12.2015

  • Latin name: Levonorgoestrelum
  • ATH code: G03AC03
  • Chemical formula: C21H28O2
  • CAS code: 797-63-7

Chemical name

(–) - 13-etil-17-etinil-17-gidroksi-1,2,6,7,8,9,10,11,12,13,14,15,16, 17-tetradecahydrocyclopenta [a] phenanthrene - 3 - it

Chemical properties

Levonorgestrel what substance is?

Levonorgestrel is the synthetic progestogen which is actively applied as active component of hormonal contraceptives. The molecular mass of hormone = 312,4 grams on mol. Medicine is a part of oral contraceptives separately or combinations with other synthetic hormones.

Pharmacological action

Contraceptive, gestagenny.

Pharmacodynamics and pharmacokinetics

This substance causes structural changes in an endometria and brakes an ovulation therefore the oospore cannot normally be implanted. Also hormone exerts impact on viscosity of tserkvialny slime and slows down advance of spermatozoa.

If medicine is a part of intrauterine therapeutic system, then it makes direct local impact on growth of an endometria, uterine tubes and slime in the cervical channel.

At drugs on the basis of Levonorgestrel of high 100% bioavailability. After penetration inside medicine is completely and quickly enough soaked up through walls of a gastrointestinal tract and gets into a system blood stream.

The single dose of 0,75 mg of means provides achievement of the maximum concentration of substance in blood in 1-2,3 hours. At synthetic hormone high extent of linkng with proteins of a blood plasma – about 55% (albumine and globulin).

The metabolism of drug proceeds in liver tissues, as a result form pharmacological inactive metabolites. The elimination half-life of means makes about one days. Medicine in the form of inactive metabolites with urine is removed and it is insignificant – with a fecal masses.

After installation of Naval Forces the speed of release of hormone in a cavity of the uterus makes 20 mkg a day in the beginning, during 5 flyings decreases approximately to 11 mkg a day. Women who receive hormonal replacement therapy in combination with transdermalny or oral estrogen, without gestagenny component can use intrauterine therapeutic system.

Indications to use

Levonorgestrel is used:

  • for the emergency post-coital contraception at women after the unprotected sexual intercourse;
  • as intrauterine therapeutic system for long contraception, at an idiopathic menorrhagia;
  • for Naval Forces for prevention of a hyperplasia of an endometria during replacement therapy by estrogen.

Contraindications

Medicine is contraindicated:

  • in the presence of reactions of individual intolerance;
  • to pregnant women or at suspicion on pregnancy;
  • to patients with a serious illness of a liver or zhelchevyvodyashchy ways (intake);
  • after jaundice;
  • at teenage age;
  • to the nursing women.

Also there are additional restrictions to use at Naval Forces:

  • recurrent or acute inflammatory diseases of bodies of a small pelvis;
  • cervicitis;
  • endometritis after the delivery;
  • infections of urinogenital system;
  • the septic abortion which is carried out to currents of the last 3 months;
  • dysplasia or malignant tumors of a neck of uterus or uterus;
  • the tumors depending on progestogen (breast cancer);
  • uterine bleeding of an unknown origin;
  • the anomalies of development of a uterus acquired or inborn (deformation of a cavity of the uterus, a fibromyoma);
  • tumor of a liver or other serious illness of a liver.

Side effects

During clinical tests the following side reactions resulting from use of synthetic hormone were revealed:

  • nausea, fatigue, painful feelings in the bottom of a stomach;
  • headaches, plentiful or, on the contrary, scanty menstrual bleedings, failures in a menstrual cycle;
  • dizziness, swelling and morbidity in mammary glands;
  • diarrhea, vomiting.

Side effects of Levonorgestrel when using Naval Forces:

Application instruction (Way and dosage)

Depending on the used dosage form the dosing mode strongly differs. Medicine is appointed in or as a part of an intrauterine contraceptive.

The instruction on Levonorgestrel at an emergency contraception

Inside. Synthetic hormone is accepted in the form of tablets within 96 hours after the unprotected sexual intercourse. On average the dose fluctuates from 0,75 to 1,5 mg of drug.

Substance can be used once. Extremely it is not recommended to take a pill for an emergency contraception more often than 1 time in 4-6 months.

The instruction on Levonorgestrel at Naval Forces

Procedure of installation of Naval Forces happens under control of the doctor. Substance is entered into a cavity of the uterus and there is not term there till 5 flyings. Periodic control of a condition of the patient is necessary.

Overdose

There are no data on overdose cases drug.

Interaction

Levonorgestrel at a combination to rifampicin, Primidonum, Phenytoinum and barbiturates has smaller contraceptive effect because of acceleration of processes of a metabolism of steroids.

The combined reception of Ampicillin, hloramfenikolya, phenoxymethylpenicillin, Sulphamethoxypyridazinum, nitrofurantoin, Neomycinum and medicine intermenstrual bleedings can strengthen. It happens because of oppression of enterogepatichesky circulation of sexual steroids owing to change of flora of intestines.

Substance reduces efficiency of anticoagulants for oral administration, anticonvulsant, hypoglycemic and anti-hypertensive means.

Means breaks processes of a metabolism of diazepam and chlordiazepoxide that can lead to accumulation of these of substance in a blood plasma.

Terms of sale

The recipe is necessary.

Special instructions

At patients with a big weight medicine has smaller pharmacological activity.

At implantation of substance under skin to patients with a serious illness of a liver there is a need to carry out monitoring of work of a liver each 8-12 weeks.

If within 6 weeks against carrying out therapy there did not come the periods (6 weeks from previous), then it is necessary to exclude pregnancy.

In the presence of periodic long and plentiful bloody allocations between periods it is necessary to make in addition additional inspections to confirm or correct the diagnosis.

To children

It is impossible to appoint medicine aged till 18 flyings.

At pregnancy and a lactation

Drug is contraindicated to pregnant women.

Substance in large numbers is emitted with breast milk therefore breastfeeding is recommended to be stopped.

Drugs in which contains (Analogues)

Coincidence on the ATH code of the 4th level:

Structural analogs of medicine: Mirren, Postinor, Eskinor-F, Mikrolyut, Norplant, Escapelle.

What it is better, Dezogestrel or Levonorgestrel?

Both drugs possess high pharmacological activity and are rather effective. Depending on specific features of an organism and portability of substances the attending physician has to pick up the corresponding synthetic hormone.

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance Levonorgestrel use surely consult with the attending physician.