Exluent

Exluent is a medicine containing an artificial progestogen.

[1], [2], [3], [4]

Indications Exluent

It is indicated as a means of oral contraception (prevention of pregnancy).

Release form

Produced in tablet form. One blister contains 28 tablets. In one package - 1 blister plate.

Pharmacodynamics

Eksluton - oral contraceptive, which contains exclusively progestagen - a substance of linestrone. This medication is usually prescribed during lactation, as well as to women who do not want or can not take estrogens.

Linestrenol inside the body is converted into a bioactive product of the decay of norethisterone. It is synthesized with progesterone receptors inside target organs (for example, inside the myometrium). The contraceptive properties of drugs are primarily associated with an increase in the viscosity of mucus in the uterine neck, which prevents the passage of sperm. Other properties - a decrease in the absorbing function of the endometrium relative to the ovule, and in addition a disruption of movement along the tubes.

Also, 70% of women taking the drug are suppressed ovulation, and in addition to this production of the yellow body - this demonstrates the lack of achievement of luteinizing hormone its maximum in the middle of the menstrual cycle, and with it the lack of further increases in progesterone.

There was no clinically significant effect on the metabolism of fats and carbohydrates, as well as hemostasis.

[5], [6], [7], [8], [9], [10], [11], [12], [13], [14]

Pharmacokinetics

Linestrenol is a prodrug that is quickly absorbed into the body, and then metabolized to the pharmacologically active degradation product of norethisterone.

Peak plasma concentrations of metabolite reaches 2-4 hours after drug use. Bioavailability indicators are 64%.

Norethisterone is synthesized with a plasma protein by 96% (most - with albumins (61%), and the smaller - with globulin (35%), which contributes to the synthesis of sex hormones).

In the first phase of metabolism of the active component, 3-hydroxylation occurs, followed by dehydrogenation. After this, the active degradation product of norethisterone undergoes the reduction process. Metabolites are synthesized with glucuronides, as well as sulfates.

The average indicator of the half-life of norethisterone is approximately 15 hours. The coefficient of cleansing from the plasma is approximately 0.6 l / h. Excretion of linestrenol together with the products of disintegration occurs with urine (usually in the guise of glucuronides with sulfates, a smaller part in unchanged form), and also with feces. The ratio of excretion to feces / urine is 1k1.5.

[15], [16], [17], [18], [19], [20], [21], [22], [23], [24]

Dosing and administration

Eksluton should be drunk during the 1-28th days of the menstrual cycle (daily at the same time) in the amount of 1 tablet. After completing the use of the whole package of medicine, it is required to start the next without a break.

Women who have a predisposition to the appearance of age spots, during the period of drug use, it is recommended not to appear in the sun. If the intake of 1-2 tablets was missed, it is possible that their effectiveness is weakened. The exlujutton is allowed to be taken during lactation.

Diarrhea or vomiting can lead to excretion of the drug from the body - because of this, if these symptoms disappear within 1 day, you need to re-use the pill. If these manifestations continue to occur even further, some other methods of contraception should be used for some time.

In the postpartum period: taking medication is allowed from the moment of the first appearance of spontaneous menstruation. If it is necessary to start using drugs earlier (before the onset of the first postpartum menstruation), additional precautions should be taken during the first week of use.

Take medication after abortion or miscarriage should be immediately, without interruption. In such cases, additional contraceptive measures are not needed.

[35], [36]

Use Exluent during pregnancy

It is forbidden to use exlutton for pregnant women. In case of pregnancy it is required to immediately cancel the use of the medicine.

Contraindications

Among the contraindications:

• suspected or established pregnancy;
• active form of deep vein thrombosis;
• presence in the anamnesis of severe hepatic pathology in cases when the parameters of the hepatic function did not return to the normal level;
• progestogen-dependent tumors;
• bleeding from the vagina of an unknown genesis;
• intolerance of the active ingredient or other components of the drug.

[25], [26], [27], [28], [29], [30]

Side effects Exluent

Taking medication can trigger the development of such side effects: the appearance of vaginal candidiasis, blood vaginal discharge in the intermenstrual period, and in addition to this vomiting along with nausea and swelling of the mammary glands.

Occasionally, melasma develops, cholestatic form of jaundice, headaches, rashes on the skin and changes in mood. In addition, there is a decrease in glucose uptake and a delay in the body's fluid.

[31], [32], [33], [34]

Overdose

There is no information about the development of serious adverse reactions due to an overdose. Because linestrenol has a weak toxicity, the simultaneous administration of several tablets of drugs should not cause severe poisoning manifestations.

Perhaps the development of such symptoms: vomiting with nausea, as well as weak bleeding from the vagina (in young girls). The medicine does not have a specific antidote, the treatment is aimed at eliminating unwanted manifestations.

[37], [38], [39], [40], [41], [42], [43]

Interactions with other drugs

Properties of drugs are weakened if vomiting or diarrhea, and also in combination with rifampicin, barbiturates, diphenin, and also laxatives, anticonvulsants and activated charcoal, begins in the first 4 hours after the use of the tablet.

Oral contraception can impair glucose uptake by the body and increase its need for insulin or other hypoglycemic drugs in patients with diabetes mellitus.

[44], [45], [46], [47]

Storage conditions

Exluent should be kept in a place that is closed from small children and sunlight. Do not freeze the medicine. Storage temperature is within 2-30 ° C.

[48], [49]

Shelf life

Exluent is suitable for use for 5 years from the date of manufacture of the medicine.

[50]