Instruction for use: Lactinette

Active substance Desogestrel

ATX code G03AC09 Desogestrel

Pharmacological group

Estrogens, gestagens; Their homologues and antagonists

Nosological classification (ICD-10)

Z30 Monitoring contraceptive use

Local Contraception, Contraception oral, Local contraception, Episodic prevention of pregnancy, Hormonal Contraception, Contraception, Prevention of Pregnancy, Prevention of unwanted pregnancy, Contraceptive intrauterine, Contraception in women with androgenization phenomena, Installation and removal of the intrauterine device, Prevention of pregnancy (contraception)

Z30.0 General advice and advice on contraception

Safe sex, Intrauterine device contraception, Contraception, Contraceptive intrauterine, Oral contraception, Oral contraception during lactation and with estrogen contraindications, Postcoital contraception, Prevention of Pregnancy, Prevention of unwanted pregnancy, Emergency Contraception, Episodic prevention of pregnancy, Contraception in adolescents, Prevention of pregnancy (contraception)

Composition

Tablets, coated with a film membrane 1 tab.

active substance:

Desogestrel 0.075 mg

Excipients

Nucleus: D, L-α-tocopherol - 0.08 mg; Silicon dioxide colloidal - 0.8 mg; Stearic acid - 0.8 mg; Magnesium stearate - 0.4 mg; Potato starch - 8 mg; Povidone K30 - 2.4 mg; Lactose monohydrate - 67.445 mg

Film sheath: Opadry II white (titanium dioxide (E171) Cl 77891 0.25 mg, talc 0.148 mg, macrogol 3000 0.202 mg, polyvinyl alcohol 0.4 mg) 1 mg

Description of dosage form

Tablets are round, biconvex, covered with a film shell of white or almost white color, labeled "D" on one side and "75" on the other.

pharmachologic effect

Pharmacological action - contraceptive.

Pharmacodynamics

Lactinette® is a gestagen-containing contraceptive for oral use, the active ingredient of which is desogestrel. Like other hormonal contraceptives, which contain an exclusively progestogen as an active ingredient, Lactinette® can be taken by women during lactation, as well as by contraindications to estrogens or unwillingness to use estrogen-containing contraceptives.

Unlike other gestagen contraceptives, the contraceptive effect of Lactinette® is explained by the inhibition of the ovulation process, as evidenced by the absence of an ovulatory follicle in ultrasound (ultrasound) and the absence of an increase in the values of LTG (luteotropic hormone) and progesterone in the serum in the middle of the menstrual cycle. At the same time, desogestrel, as well as other progestogens, has the property of increasing the viscosity of the cervical mucus, preventing the progress of spermatozoa. Perl index (the indicator reflecting the onset of pregnancy in 100 women during the year of contraception) is 0.4, which is comparable with the use of combined hormonal contraceptives for oral use. The use of the drug Lactinette® leads to a decrease in the content of estradiol in the blood plasma to values corresponding to the early follicular phase. Progestogens affect carbohydrate and lipid metabolism.

Pharmacokinetics

Suction

When ingestion, desogestrel is absorbed quickly. Tmax is achieved 1.8 hours after taking the tablet. Bioavailability of etonogestrel is about 70%.

Distribution

Etonogestrel is 95.5-99% bound to blood plasma proteins, mainly with albumin and to a lesser extent with sex hormone binding globulin (GLB (globulin binding sex hormones)).

Metabolism

Desogestrel by hydroxylation and dehydrogenation is metabolized to the active metabolite ethonogestrel. Ethonogestrel is metabolized by the formation of sulfate and glucuronide conjugates.

Excretion

The mean T1 / 2 (half-life) of etonogestrel is about 30 hours, both with single and multiple administration. Css (equilibrium concentration) in the blood plasma are established after 4-5 days. Etonogestrel and its metabolites are excreted by the kidneys and through the intestine (in a ratio of 1.5: 1) in the form of free steroids and conjugates. In lactating mothers, etonogestrel is excreted in breast milk in a milk / serum ratio of 0.37-0.55. Thus, with an approximate milk consumption of the mother in the amount of 150 mg / kg / day, the newborn can receive etonogestrel in an amount of 0.01-0.05 μg / kg / day.

Indications

Contraception.

Contraindications

Increased sensitivity to desogestrel or any other component of the drug;

The present or previous history of venous thromboembolism (including deep vein thrombosis of the lower extremities, thromboembolism of the pulmonary artery);

Severe liver disease at present or history (before the normalization of liver function);

Hepatic insufficiency at present or anamnesis;

Established or suspected malignant hormone-dependent tumors (including breast cancer);

liver cancer;

Bleeding from the vagina of an unclear etiology;

Established or suspected pregnancy;

Lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

Prolonged immobilization, incl. Associated with surgery or disease (risk of venous thromboembolism).

With caution: resistant arterial hypertension, developing against the background of taking the drug, incl. With ineffectiveness of antihypertensive therapy; Chlamydia, especially if there is a history of chloasma during pregnancy; Diabetes mellitus (due to possible effects of progestogens on peripheral insulin resistance and glucose tolerance); Porphyria; Systemic lupus erythematosus; Herpes (during pregnancy in anamnesis).

pregnancy and lactation

During pregnancy, the use of the drug is contraindicated. In preclinical studies with the introduction of very high doses of progestogen, masculinization of the female fetus was observed. In epidemiological studies, there was no increased risk of teratogenic and congenital developmental defects among children whose mothers took oral hormonal contraceptives prior to pregnancy or unintentionally - in early pregnancy.

Like other preparations containing only progestogen, Lactinette® does not affect the quality and quantity of mother's milk, but a small amount of the metabolite of desogestrel (etonogestrel) is excreted in the mother's milk and is approximately 0.01-0.05 μg / kg / day (with an amount Of consumed breast milk is 150 ml / kg / day). The results of a 7-month follow-up showed no increased risks for breastfed infants when assessing their growth, psychomotor and physical development. Nevertheless, careful monitoring of the development and growth of the infant with breastfeeding is necessary if the woman uses Lactinette® for contraceptive use.

Side effects

The most frequent undesirable effect reported in clinical studies was irregular menstruation. Up to 50% of women who used desogestrel, noted acyclic spotting: in 20-30% of women, menstruation becomes more frequent, while in others 20% - more rare or even completely can stop. Menstruation can also become more prolonged.

After several months of taking the drug, menstruation tends to become less frequent. Informing a doctor, seeing a doctor, and using a diary of menstruation can increase compliance with medication.

Below are the undesirable effects that have an established, probable or possible relationship with the use of the drug.

In the event that any of the following conditions / risk factors are observed, the expected benefits and risk of contraceptive use should be carefully weighed in consultation with the attending physician throughout the contraceptive period. If any of the following conditions / risk factors appear, increase or change, the patient should immediately consult a doctor to decide whether to continue using the drug.

Often - acne, nausea, mood changes, decreased libido, breast tenderness, menstrual irregularity, headache, weight gain.

Infrequently - alopecia, fatigue, vomiting, discomfort when wearing contact lenses, vaginitis, dysmenorrhea, ovarian cysts.

Rarely - redness of the skin, rash, hives, erythema nodosum.

Although there is no reliable connection with the use of gestagens, cholestatic jaundice, pruritus, cholelithiasis, chorea, pregnant herpes, otosclerosis, deafness, development of hemolytic-uremic syndrome are possible with their reception.

Interaction

Simultaneous use of inducers of microsomal liver enzymes can cause breakthrough bleeding and a decrease in the contraceptive effect of the drug. Such drugs are derivatives of hydantoin (including phenytoin), rifabutin, barbiturates, primidone, carbamazepine and rifampicin, as well as oxcarbazepine, topiramate, felbamate and griseofulvin. Specialized studies for the interaction of desogestrel with other drugs have not been conducted. The maximum induction of microsomal liver enzymes is achieved not earlier than 2-3 weeks after the start of the application of the corresponding inducer and lasts up to 4 weeks after its cancellation. Antibiotics (eg, ampicillin and tetracycline) reduce the effectiveness of oral contraceptives.

Women taking medications that induce microsomal enzymes of the liver should be recommended temporary additional use of barrier or other nonhormonal methods of contraception. With the simultaneous use of the above drugs with desogestrel, use of the barrier method of contraception throughout the course of treatment and for 7 days (for rifampicin - 28 days) after the end of therapy is recommended. In the treatment of activated charcoal, the absorption of steroids, and hence the contraceptive effectiveness, may decrease. In this case, you should follow the recommendations in the section "Method of administration and dose" for the missed intake of the drug.

Dosing and Administration

Inside.

In the absence of prior application of hormonal contraceptives (during the last month), the taking of tablets starts from the first day of the menstrual cycle according to 1 table. In a day, if possible at the same time of day, following in the direction indicated on the package, so that the interval between taking 2 table. Was 24 hours, if necessary with a small amount of liquid. This drug does not require a break in admission. Each next package should be started immediately after the end of the previous one.

Procedure for taking the drug

Women who in the previous month did not take oral contraceptives. Reception of the first table. Should start from the first day of the menstrual cycle (menstruation). In this case, no additional methods of contraception are required.

You can start taking pills from the 2nd-5th day of menstruation, but in this case you need to apply additional contraceptive methods in the first cycle in the first 7 days of taking the pills.

Women who switch from another combined oral contraceptive (PDA) to Lactinette®. If possible, the day after the last tablet of the previous PDA. In this case, no additional methods of contraception are required.

Women who switch from monocomponent drugs containing only progestogen (mini-pili, injections, implants or intrauterine contraceptives releasing progestogen). When switching from minipilli, the drug can be taken any day; In the case of injections - the day that the next injection should be given; In the case of an implant, the day after it is removed.

In all of these cases, the use of barrier methods of contraception is recommended for the first 7 days.

Taking the drug after an abortion in the first trimester of pregnancy. After abortion in the first trimester of pregnancy, it is recommended to start taking the drug immediately after the abortion, and in this case there is no need for additional methods of contraception.

Reception of the drug after childbirth or after termination of pregnancy in the second trimester. Admission of the drug begins not earlier than 21-28 days after the termination of pregnancy in the second trimester or after childbirth. If the drug is supposed to start later, then it is necessary to use a barrier method of contraception during the first 7 days. In addition, if unprotected sex has occurred before starting the use of the drug, pregnancy should be excluded or the beginning of the drug on the 1st day of the next menstruation (during the restoration of the menstrual cycle) be postponed.

Missed (forgotten) tablets. The effectiveness of the contraceptive decreases, if between the methods of 2 table. More than 36 hours have passed. If the break does not exceed 12 hours, the contraceptive effect does not decrease, and the use of an additional contraceptive method is not required. The intake of the remaining tablets is continued according to the usual schedule.

In the case of more than 12 hours of interruption, the contraceptive effect may decrease. To achieve an effective blockade of the hypothalamic-pituitary-ovarian system, it is necessary to take the drug daily for 7 days. Thus, with a break of more than 12 hours, the drug is continued in normal mode, but additional (barrier) methods of contraception must be used in the next 7 days. If the intake of the tablet was missed for the first week of the drug and in the previous 7 days there was an unprotected sexual intercourse, it is impossible to exclude the possibility of pregnancy.

Measures taken in case of vomiting. If vomiting develops within 3-4 hours after taking the pill, then the tablet is not fully absorbed. In this case, you should do the same as in the case of missed tablets. The necessary tablet (the necessary pills) should be replenished from another package.

Observation. Despite the regular intake of tablets, there may be irregular menstruation. If menstruation occurs very often and irregularly, consider using another method of contraception. If the disorder persists, it is necessary to exclude the organic cause.

Tactics with amenorrhea that occurs during the use of the drug depend on whether the tablets were taken according to the instructions or not; A pregnancy test may be required.

If a pregnancy occurs, the drug should be discontinued.

It must be remembered that taking Lactinette® does not protect against the infection of HIV (AIDS) and other sexually transmitted diseases.

Overdose

Symptoms: nausea, vomiting, spotting / bleeding from the vagina.

Treatment: symptomatic, there is no specific antidote.

special instructions

If there is any condition or risk factor, the physician should correlate the risk and benefit of using Lactinette ® individually for each woman before hormonal contraception begins. In case of occurrence of any undesirable effect or risk factor it is necessary immediately to put the attending physician in the notice for the decision of a question on expediency of the further reception of a preparation. Women with diabetes should be monitored carefully during the first months of use of the Lactinette® drug. Taking Lactinette® reduces the serum estradiol to a value corresponding to the early follicular phase. The protective effect of traditional only progestogen-containing contraceptives in terms of preventing ectopic pregnancy is not as pronounced as in combined oral contraceptives, which is associated with a relatively common occurrence when taking progestogen-only preparations by ovulation. Despite the fact that Lactinette®, as a rule, inhibits ovulation, the possibility of an ectopic pregnancy should be borne in mind when a differential diagnosis occurs when a woman develops amenorrhea or abdominal pain. Sometimes there may be a chloasma, especially in women with a history of pregnant women with chloasma. Women with a tendency to chloasma should avoid sunlight and ultraviolet irradiation while taking Lactinette®. Patients with lactose intolerance should bear in mind that one film-coated tablet of Lactinette® contains 67.445 mg of lactose monohydrate. Patients with rare hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug.

Impact on the ability to drive or other working mechanisms. Does not affect the ability to control the car and working mechanisms.

Form of issue

Tablets coated with a film coating, 0.075 mg. In the blister of PVC / PVDH-film and aluminum foil for 28 pcs. 1 or 3 blisters in a pack of cardboard.

Terms of leave from pharmacies

On prescription.

storage conditions

At temperatures not higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

shelf life

3 years.

Do not use after the expiry date printed on the package.