Microlut (Dragee) Instructions for Use

Marketing Authorization Holder

Schering, AG (Germany)

ATC Code

G03AC03 (Levonorgestrel)

Active Substance

Levonorgestrel (Rec.INN registered by WHO)

Dosage Form

Microlut

Dragees 30 mcg: 35 pcs. in a calendar pack.

Dosage Form, Packaging, and Composition

35 pcs. – blister calendar packs (1) – cardboard packs.

Clinical-Pharmacological Group

Gestagen for oral contraception

Pharmacotherapeutic Group

Progestogen

Pharmacological Action

Synthetic gestagen with contraceptive action. The emergency contraceptive effect is realized due to pronounced gestagenic and antiestrogenic effects. The main mechanism of action is the inhibition and/or delay of ovulation as a result of suppressing the LH peak.

When used as an emergency contraceptive, Levonorgestrel suppresses ovulation and fertilization if sexual intercourse occurred in the pre-ovulatory phase, when the possibility of fertilization is greatest. Levonorgestrel is not effective if implantation of a fertilized egg has already occurred.

Pharmacokinetics

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract. After taking levonorgestrel at a dose of 1.5 mg, the C_max in plasma is 18.5 ng/ml and is reached in 2 hours. After reaching maximum values, the concentration of levonorgestrel decreases. The absolute bioavailability is 100%.

Levonorgestrel binds to plasma albumin and sex hormone-binding globulin (SHBG). Only 1.5% of the total dose is in free form, 65% is bound to SHBG. Levonorgestrel is excreted in breast milk. The metabolism of levonorgestrel corresponds to the metabolism of sex hormones.

Levonorgestrel is hydroxylated in the liver and metabolites are excreted in the form of conjugated glucuronides. It is excreted exclusively in the form of metabolites, approximately equally by the kidneys and through the intestines. T_1/2 is about 26 hours.

Indications

Emergency (postcoital) contraception within 72 hours after unprotected sexual intercourse or in case of unreliability of the contraceptive method used.

Intrauterine contraception.

ICD codes

Dosage Regimen

For emergency contraception, take a single oral dose of 1.5 mg levonorgestrel as soon as possible.

Administer the dose within 72 hours after unprotected sexual intercourse or contraceptive failure.

Take the tablet with water, with or without food. If vomiting occurs within 3 hours of ingestion, take a replacement dose immediately.

For the intrauterine contraceptive system, follow the specific dosage and insertion instructions for the product used.

Initiate the intrauterine system only after the onset of menarche and a stable menstrual cycle is established.

Note that the contraceptive efficacy of levonorgestrel may be reduced in overweight patients.

This regimen is for emergency use only and is not intended for routine contraception.

Adverse Reactions

From the immune system: very rarely – allergic reaction (skin rash, urticaria, itching, facial edema). If any of these signs occur, seek medical attention immediately.

From the nervous system: very often – headache; often – dizziness.

From the gastrointestinal tract: very often – nausea, pain in the lower abdomen; often – diarrhea, vomiting; very rarely – abdominal pain.

From the genital organs and mammary gland: very often – bleeding not associated with menstruation; often – delay of menstruation by more than 7 days, irregular menstrual bleeding, breast tenderness; very rarely – pelvic pain, dysmenorrhea.

General disorders and administration site conditions: very often – increased fatigue, facial edema.

From the skin and subcutaneous tissues: very rarely – skin rash, urticaria, itching.

Contraindications

Hypersensitivity to levonorgestrel; pregnancy (including suspected); established or suspected malignant neoplasms of the genital organs and mammary gland; uterine bleeding of unknown etiology; history of inflammatory diseases of the pelvic organs or ectopic pregnancy; severe hepatic insufficiency, acute liver diseases, liver tumors; thromboembolic disorders, thrombophlebitis, cerebrovascular diseases, coronary artery diseases; age under 16 years (for dosage forms for emergency contraception).

For the intrauterine contraceptive device – infections of the external genitalia; postpartum endometritis, septic abortion within the last 3 months, cervicitis, cervical dysplasia, congenital or acquired anomalies of the uterus, including fibroids leading to deformation of the uterine cavity.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy (including suspected).

Levonorgestrel passes into breast milk. Use during breastfeeding is not recommended.

Use in Hepatic Impairment

Contraindicated in severe hepatic insufficiency, acute liver diseases, liver tumors. Use with caution in diseases of the liver and biliary tract, jaundice (including in history).

Pediatric Use

Contraindicated for use in children and adolescents under 16 years of age.

The use of levonorgestrel in the form of an intrauterine contraceptive is indicated only after the onset of menarche (establishment of the menstrual cycle).

Special Precautions

Levonorgestrel should be used with caution in patients with diseases of the liver and biliary tract, jaundice (including in history), Crohn’s disease, with a hereditary or acquired predisposition to thrombosis, with congenital heart defects or heart valve diseases (due to the risk of developing septic endocarditis), diabetes mellitus.

When using an intrauterine contraceptive, a doctor should be consulted if any of the following conditions are present or occur for the first time: migraine, focal migraine with asymmetric loss of vision or other symptoms indicating transient cerebral ischemia; unusually severe headache; jaundice; significant arterial hypertension; severe circulatory disorders, including stroke and myocardial infarction.

In patients who are overweight, the contraceptive effect of levonorgestrel is less effective.

If the expected menstruation does not occur within 6 weeks from the start of the previous menstruation or menstruation-like reaction while taking levonorgestrel, pregnancy must be excluded.

In case of prolonged and persistent intermenstrual spotting, additional examination is necessary to verify the diagnosis.

Drug Interactions

With simultaneous use with rifampicin, phenytoin, primidone, barbiturates, the contraceptive effect of levonorgestrel is reduced due to increased metabolism of steroids caused by induction of liver microsomal enzymes.

With simultaneous use with ampicillin, sulfamethoxypyridazine, chloramphenicol, nitrofurantoin, phenoxymethylpenicillin and neomycin, increased intermenstrual bleeding is possible. This is due to the inhibition of the enterohepatic recirculation of sex steroids, which is associated with a change in the intestinal flora.

The following drugs may reduce the effectiveness of levonorgestrel: amprenavir, lansoprazole, nevirapine, oxcarbazepine, tacrolimus, topiramate, tretinoin, barbiturates (including primidone), phenytoin and carbamazepine; preparations containing St. John’s wort (Hypericum perforatum); as well as rifampicin, ritonavir, ampicillin, tetracycline, rifabutin, griseofulvin.

Levonorgestrel reduces the effectiveness of oral anticoagulants, antihypertensive, anticonvulsant and hypoglycemic agents. Increases plasma concentrations of corticosteroids. Women taking these drugs should consult a doctor.

Levonorgestrel may impair the oxidative metabolism processes of diazepam and chlordiazepoxide, leading to their accumulation in plasma.

Preparations containing Levonorgestrel may increase the risk of cyclosporine toxicity due to suppression of its metabolism.

Levonorgestrel may reduce the effectiveness of ulipristal by competitive action on the progesterone receptor, therefore their simultaneous use is not recommended.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.