Exluton

Exluton is a medicine containing an artificial progestogen.

[ 1 ], [ 2 ]

Indications Exluton

Indicated as an oral contraceptive (pregnancy prevention).

Release form

Available in tablet form. One blister contains 28 tablets. One package contains 1 blister strip.

Pharmacodynamics

Exluton is an oral contraceptive that contains only progestogen, the substance lynestrenol. This medication is usually prescribed during lactation, as well as to women who do not want or cannot take estrogens.

Lynestrenol is converted into the bioactive decay product norethisterone inside the body. It is synthesized with progesterone receptors inside target organs (for example, inside the myometrium). The contraceptive properties of the drug are primarily associated with increased viscosity of mucus in the cervix, which prevents the passage of sperm. Other properties include a decrease in the absorption function of the endometrium relative to the egg, as well as a violation of movement along the tubes.

Also, 70% of women taking the drug experience suppression of the ovulation process, and in addition, the production of the corpus luteum - this demonstrates the lack of luteinizing hormone reaching its maximum in the middle of the menstrual cycle, and along with this, the absence of a further increase in progesterone levels.

No clinically significant effects on fat and carbohydrate metabolism or hemostasis were observed.

[ 3 ], [ 4 ], [ 5 ], [ 6 ], [ 7 ]

Pharmacokinetics

Lynestrenol is a prodrug that is rapidly absorbed into the body and then metabolized into the pharmacologically active breakdown product norethisterone.

The metabolite reaches its peak plasma concentration 2-4 hours after taking the drug. Bioavailability indicators are 64%.

Norethisterone is synthesized with plasma protein by 96% (most of it with albumin (61%), and a smaller part with globulin (35%), which promotes 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 product of norethisterone decay undergoes a reduction process. Metabolites are synthesized with glucuronides, as well as sulfates.

The mean half-life of norethisterone is approximately 15 hours. The plasma clearance rate is approximately 0.6 L/hour. Lynestrenol and its breakdown products are excreted in the urine (usually as glucuronides with sulfates; a smaller portion is unchanged) and in the feces. The fecal/urine excretion ratio is 1:1.5.

[ 8 ], [ 9 ], [ 10 ], [ 11 ], [ 12 ], [ 13 ], [ 14 ], [ 15 ]

Dosing and administration

Exluton should be taken during the period from day 1 to day 28 of the menstrual cycle (daily at the same time) in the amount of 1 tablet. After finishing the entire package of the medicine, it is necessary to start the next one without interruption.

Women who are predisposed to pigment spots are advised not to go out in the sun while taking the medicine. If 1-2 tablets are missed, their effectiveness may be reduced. Exluton may be taken during lactation.

Diarrhea or vomiting may cause the drug to be excreted from the body – therefore, if these symptoms disappear within 1 day, the tablet should be taken again. If these symptoms continue to occur, other methods of contraception should be used for some time.

In the postpartum period: taking the medicine is permitted from the moment of the first spontaneous menstruation. If it is necessary to start using the medicine earlier (before the first postpartum menstruation), additional precautions must be taken during the first week of use.

The medicine should be taken immediately after abortions or miscarriages, without interruption. In such cases, additional contraceptive measures are not necessary.

[ 23 ]

Use Exluton during pregnancy

Exluton is prohibited for use by pregnant women. If pregnancy occurs, the use of the drug must be stopped immediately.

Contraindications

Among the contraindications:

• suspected or established pregnancy;
• active form of deep vein thrombosis;
• history of severe liver disease in cases where liver function tests have not returned to normal levels;
• progestogen-dependent tumors;
• vaginal bleeding of unknown origin;
• intolerance to the active substance or other components of the drug.

[ 16 ], [ 17 ], [ 18 ], [ 19 ]

Side effects Exluton

Taking the medication may provoke the development of such side effects: the appearance of vaginal candidiasis, bloody discharge from the vagina in the intermenstrual period, and in addition to this, vomiting along with nausea and swelling of the mammary glands.

Occasionally, melasma, cholestatic jaundice, headaches, skin rashes and mood changes develop. In addition, there is a decrease in glucose absorption and fluid retention in the body.

[ 20 ], [ 21 ], [ 22 ]

Overdose

There is no information on the development of serious adverse reactions due to overdose. Since lynestrenol has low toxicity, the simultaneous intake of several tablets of the drug should not cause strong toxic effects.

The following symptoms may develop: vomiting with nausea, as well as slight bleeding from the vagina (in young girls). The drug does not have a specific antidote, treatment is aimed at eliminating unwanted manifestations.

[ 24 ], [ 25 ], [ 26 ], [ 27 ], [ 28 ]

Interactions with other drugs

The properties of the drug are weakened if vomiting or diarrhea begins within the first 4 hours after taking the tablet, as well as in combination with rifampicin, barbiturates, diphenin, as well as laxatives, anticonvulsants and activated carbon.

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

[ 29 ], [ 30 ]

Storage conditions

Exluton should be stored in a place closed to small children and sunlight. It is prohibited to freeze the medicine. The storage temperature is within 2-30°C.

[ 31 ]

Shelf life

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

[ 32 ]