Laktinet

General characteristics. Structure:

Active agent: dezogestret 0.075 mg.

Excipients: structure of a kernel of a tablet: DL-α-токоферол, silicon dioxide colloid, stearic acid, magnesium stearate, potato starch, K30 povidone. lactoses monohydrate;
structure of a cover: опадрай the II white (titanium dioxide (EI71). C1 77891, talc, macrogoal 3000, polyvinyl alcohol).

Pharmacological properties:

Pharmacodynamics. Лактинет® is a gestagensoderzhashchy contraceptive for oral administration which active ingredient is dezogestret. As well as of Laktinet® women can accept other hormonal contraceptives which part as active component progestogen is only during feeding by a breast, and also in the presence of contraindications to estrogen or unwillingness to use estrogensoderzhashchy kontraptsetiva.
Unlike other gestagenny contraceptives, contraceptive effect of the drug Laktinet® is explained by braking of process of an ovulation that is confirmed by lack of an ovulatory follicle at ultrasonography and lack of increase in values of the luteotropic hormone (LH) and progesterone in blood serum in the middle of a menstrual cycle. At the same time dezogestret, also. as well as other progestogens, has property to increase viscosity of slime of a neck of uterus, interfering with advance of spermatozoa.
Perl's index (the indicator reflecting approach of pregnancy at 100 women within a year of contraception) makes 0,4 that is comparable to use of the combined hormonal contraceptives for oral administration. Use of the drug Laktinet® leads to decrease in content of oestradiol in a blood plasma to values corresponding to an early follicular phase. Progestagena influence carbohydrate and lipidic metabolism.
 
Pharmacokinetics. Absorption
At intake dezogestret it is soaked up quickly. Average maximum concentration in blood serum is reached in 1,8 hours (Tmax) after reception of a tablet. Bioavailability of an etonogestrel makes about 70%.
Distribution in an organism
Etonogestrel in 95.5-99% contacts proteins of a blood plasma, generally albumine and to a lesser extent the globulin, connecting sex hormones (G,CSH).
Metabolism
Dezogestrel by a hydroxylation and dehydrogenation is metabolized in an active metabolite etonogestret. Etonogestrel is metabolized by formation of sulphatic and glyukuronidny conjugates.
Removal from an organism
Average elimination half-life of an etonogestrel about 30 hours, as at single, and multiple dose. Equilibrium concentration in a blood plasma are established in 4-5 days. Etonogestrel and his metabolites are removed by kidneys and through intestines (in the ratio 1,5:1) in the form of free steroids and conjugates.
At nursing mothers etonogestret milk/blood serum 0,37-0,55 is emitted with breast milk in the ratio. Thus, at approximate consumption of milk of mother in number of 150 mg/kg/day, the newborn can receive 0,01-0,05 mkg of an etonogestrel on body weight kg a day.

Indications to use:

Contraception.

Route of administration and doses:

In the absence of the previous use of hormonal contraceptives (within the last month) reception of tablets is begun from the first day of a menstrual cycle on one tablet a day, whenever possible at the same time days, following in the direction specified on packaging that the break between reception of two tablets made 24 hours, if necessary with a small amount of liquid. This drug does not demand a break in reception. Each following packaging should be begun right after the termination previous.
First administration of drug
Women, which last month not to accept peroral contraceptives:
Reception of the first tablet should be begun from the first day of a menstrual cycle (periods). In this case use of additional methods of contraception is not required.
Reception of tablets it is possible to begin and from 2-5 in the afternoon periods, but in this case in the first cycle it is necessary to apply additional methods of contraception in the first 7 days of reception of tablets.
Women who pass from other the combined oral contraceptive (COC) to Laktinet®

Whenever possible next day after acceptance of the last tablet of the previous PDA. In this case use of additional methods of contraception is not required.
Women who pass from the monocomponent drugs containing only progestogen (mini-saw, the injections, implants or intrauterine contraceptives emitting progestogen)
Upon transition from mini-drank administration of drug it is possible to begin in any day; in case of injections - in day when it would be necessary to do the next injection; in case of an implant - in day after its removal.
In all listed cases use of barrier methods of contraception during the first 7 days is recommended.
Administration of drug after abortion in the first trimester of pregnancy
After abortion in the first trimester of pregnancy administration of drug is recommended to be begun at once after abortion, and in this case there is no need for use of additional methods of contraception.
Administration of drug after the delivery, or after abortion in the second trimester
Administration of drug there begin not early 21-28 days after abortion in the second trimester or after the delivery. If administration of drug is assumed to be begun later, then it is necessary to use a barrier way of contraception for the first 7 days. Besides, if before use of drug unprotected sexual contacts took place, it is necessary to exclude pregnancy or to postpone the beginning of administration of drug to the first day of the following periods (at recovery of a menstrual cycle).

The passed (forgotten) tablets.
Efficiency of a contraceptive decreases if between receptions of two tablets there passed more than 36 hours. If the break does not exceed 12 hours, the contraceptive effect does not decrease, and use of an additional contraceptive method is not required.
Reception of other tablets is continued according to the usual schedule.
In a case more, than a 12-one-hour break, the contraceptive effect can decrease.
For achievement of effective blocking гипоталамо - pituitary and ovarian system it is necessary to accept daily drug for 7 days. Thus, at a break, exceeding 12 hours, administration of drug is continued in the usual mode, however, in the next 7 days it is necessary to use additional (barrier) methods of contraception. If reception of a tablet was missed on the first week of use of drug and in the previous 7 days unprotected sexual intercourse took place, then it is impossible to exclude probability of approach of pregnancy.

The measures taken in case of vomiting.
If within 3-4 hours after reception of a tablet vomiting develops, then the tablet is soaked up by incompleteness. In this case it is necessary to arrive the same as in case of the passed tablets. The necessary tablet (necessary tablets) should be filled from other packaging.
Observation
Despite regular reception of tablets, there can be disturbances of periods. If periods arise very often and irregularly, it is necessary to consider the possibility of use of other method of contraception. If frustration remain, it is necessary to exclude the organic reason.
Tactics at the amenorrhea which arose during drug use depends on whether a pill according to the instruction was taken or not; test for pregnancy can be required.
If there was pregnancy, administration of drug needs to be stopped.
It is necessary to remember that administration of drug of Laktinet® does not protect from infection of HIV (AIDS) and other diseases, sexually transmitted.

Features of use:

In the presence of any state or risk factor, the doctor has to correlate risk and advantage of use of the drug Laktinet® individually for each woman prior to hormonal contraception. In case of any undesirable effect or risk factor it is necessary to inform at once the attending physician for the solution of a question of expediency of further administration of drug.
Women with a diabetes mellitus have to be under attentive observation for the first months of use of Laktinet®.
Reception of Laktinet® reduces the content of oestradiol of serum to the value corresponding to an early follicular phase.
Protective action only of traditional progestagensoderzhashchy contraceptives in respect of prevention of ectopic pregnancy is not so expressed, as at the combined oral contraceptives that connect with the ovulation which is rather often occurring against the background of reception only of progestagensoderzhashchy drugs.
In spite of the fact that Laktinet®, as a rule, inhibits an ovulation, the possibility of an extrauterine pregnancy needs to be meant at the differential diagnosis at development in the woman of an amenorrhea or abdominal pains.

There can sometimes be a hloazma, especially at women with hloazmy pregnant women in the anamnesis. Women with tendency to a hloazma should avoid solar and ultra-violet radiation during reception of Laktinet®.
Patients with a lactose intolerance need to mean that one film coated tablet Laktinet® contains 67,445 mg of lactose monohydrate. Patients with rare hereditary diseases, such as a lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption should not accept drug.

Influence on ability of driving or other working mechanisms
Does not influence ability to driving and working mechanisms.

Side effects:

Irregular periods were the most frequent undesirable effect about which it was reported in clinical trials. To 50% of the women applying dezogestret, noted acyclic bloody allocations: at 20-30% of women of periods become more frequent while at other 20% - more rare or even completely can stop. Periods can become longer also.
After several months of administration of drug, periods tend to become less frequent. Informing the doctor, medical supervision, and also use of the diary of periods can raise a treatment komplayentnost drug.
The undesirable effects having the established, probable or possible communication using drug are included below.

If any of following states / risk factors is observed, it is necessary to weigh carefully expected advantages and risk of use of a contraceptive at consultation with the attending physician throughout the entire period of contraception. At emergence, strengthening, change of any of following states / risk factors, the patient needs to see immediately a doctor for the solution of a question of a possibility of further use of drug.
Often: acne, nausea, changes of mood, decrease in a libido, morbidity of a mammary gland, disturbance of a menstrual cycle, headache, increase in body weight.
Infrequently: an alopecia, fatigue, vomiting, discomfort when carrying contact lenses, a vaginitis, a dysmenorrhea, oothecomas.
Seldom: erubescence, rash, urticaria, knotty erythema.
Though reliable connection with reception of gestagen is not established, at their reception cholestatic jaundice, a skin itch, a cholelithiasis, a chorea, herpes of pregnant women, an otosclerosis, deafness, development of a gemolitiko-uraemic syndrome are possible.

Interaction with other medicines:

Simultaneous use of drugs, inductors of microsomal enzymes of a liver, can cause breakthrough bleeding and decrease in contraceptive effect of drug. Those drugs are hydantoin derivatives (including Phenytoinum), рифабутин, barbiturates, Primidonum, carbamazepine and rifampicin, and also окскарбазепин, топирамат. фелбамат and griseofulvin. Specialized researches regarding interaction of a dezogestrel with other drugs were not conducted. The maximum induction of microsomal enzymes of a liver is reached not earlier than in 2-3 weeks after the beginning of use of the corresponding inductor to 4 weeks after its cancellation.
Antibiotics (e.g., ampicillin and tetracycline) reduce efficiency of perorapny contraceptives.

The women accepting the medicines inducing microsomal enzymes of a liver should recommend temporary additional use of barrier or other non-hormonal methods of contraception.
At simultaneous use. above-mentioned drugs with dezogestrely, use of a barrier method of contraception throughout all course of treatment and within 7 days (for rifampicin - 28 days) after the end of therapy is recommended.
At treatment by absorbent carbon absorption of steroids, and, therefore, and contraceptive efficiency, can decrease. In this case it is necessary to adhere to the recommendations provided in the section "Dosing Mode" on the missed administration of drug.

Contraindications:

- existence now or anamnesis of a venous thromboembolism (including deep vein thrombosis of the lower extremities, thromboembolism of a pulmonary artery;
- a serious illness of a liver now or the anamnesis (before normalization it is indicative functions of a liver);
- liver failure now or anamnesis;
- the established or estimated malignant gormonzavisimy tumors (including a breast cancer);
- liver cancer;
- bleeding from a vagina of not clear etiology;
- the established or alleged pregnancy;
- hypersensitivity to a dezogestrel or any other component of drug.
- lactose intolerance, insufficiency of lactase, glyukozo-galaktozny malabsorption;
- a long immobilization, including connected with operation or a disease (risk of venous - a thromboembolism).

With care
- resistant arterial hypertension. developing against the background of administration of drug, including at inefficiency of anti-hypertensive therapy;
- a hloazma, especially in the presence of a hloazma during pregnancy in the anamnesis;
- a diabetes mellitus (because of possible influence of progestogens on a peripheral nnsulinrezistentnost and tolerance to glucose);
- porphyria;
- system lupus erythematosus (SLE);
- herpes (during pregnancy in the anamnesis).

Pregnancy and period of a lactation
Pregnancy
During pregnancy use of drug is contraindicated.
In preclinical trials. at introduction of very high doses of progestogen observed a masculinization of a female fruit.
In epidemiological researches the increased risk of teratogenic effect and inborn defects of development among children whose mothers accepted oral hormonal contraceptives before pregnancy or inadvertently - in early durations of gestation is not revealed.
Lactation period
As well as other drugs containing only progestogen, Laktinet® does not influence quality and amount of maternal milk, but (etonogestret) a small amount of a metabolite of a dezogestrel it is allocated with maternal milk and makes about 0,01-0,05 mkg/kg/day (at amount of the consumed breast milk of 150 ml/kg/day). Results of 7-month observation did not reveal the increased risks for the children who are on breastfeeding at assessment of their growth, psychomotor and physical development.
Nevertheless, careful dynamic observation of development and growth of the child when breastfeeding is necessary if the woman for the purpose of contraception uses the drug Laktinet®.

Overdose:

Overdose signs: nausea, vomiting, bloody allocations / bleeding from a vagina. There is no specific antidote, a symptomatic treatment.

Storage conditions:

To store in original packaging at a temperature not above 25 °C. To store in the places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets film coated on 0,075mg. 28 tablets, film coated, in the blister from PVH/PVDH - a film and aluminum foil. On 1 or 3 blisters together with the application instruction in a cardboard pack.