Modelle^® 911 (Tablets) Instructions for Use

Marketing Authorization Holder

Teva Pharmaceutical Industries, Ltd. (Israel)

Manufactured By

Laboratorios Leon Farma, S.A. (Spain)

Contact Information

TEVA (Israel)

ATC Code

G03AD01 (Levonorgestrel)

Active Substance

Levonorgestrel (Rec.INN registered by WHO)

Dosage Form

Modelle® 911

Tablets 1.5 mg: 1 pc.

Dosage Form, Packaging, and Composition

Tablets are white, round, biconvex, with an engraving “C” on one side and “1” on the other side.

Excipients: microcrystalline cellulose – 44.4 mg, lactose monohydrate – 43.3 mg, poloxamer 188 – 1.8 mg, croscarmellose sodium – 5 mg, magnesium stearate – 0.5 mg.

1 pc. – PVC-PVDF/Aluminum blister (1) – cardboard packs.

Clinical-Pharmacological Group

Postcoital contraceptive. Gestagen

Pharmacotherapeutic Group

Emergency contraceptive

Pharmacological Action

Levonorgestrel is a synthetic gestagen with a contraceptive effect. It is used as an emergency contraceptive due to its pronounced gestagenic and antiestrogenic effects.

When used at the recommended dosage regimen, Levonorgestrel suppresses ovulation and fertilization if sexual intercourse occurred in the pre-ovulatory phase of the menstrual cycle. It can also cause changes in the endometrium that prevent the implantation of a fertilized egg and increases the viscosity of cervical secretion, which impedes sperm movement. Levonorgestrel is ineffective if implantation has already occurred.

When the recommended dosage regimen is followed, Levonorgestrel does not have a significant effect on blood clotting factors, lipid, or carbohydrate metabolism.

Taking one 1.5 mg levonorgestrel tablet once within 72 hours after unprotected sexual intercourse can prevent an expected pregnancy in 84% of cases (compared to 79% when taking two 750 mcg levonorgestrel tablets with a 12-hour interval).

Pharmacokinetics

Absorption

When taken orally, Levonorgestrel is rapidly and almost completely absorbed. The absolute bioavailability is about 100% of the administered dose. After taking levonorgestrel at a dose of 1.5 mg, the C_max in plasma, equal to 18.5 ng/ml, is reached after 2 hours.

Distribution

Levonorgestrel binds to serum albumin and to sex hormone-binding globulin (SHBG). Only 1.5% of the administered dose is in the free form, and 65% is bound to SHBG. It penetrates into breast milk.

Metabolism

The metabolism of levonorgestrel corresponds to steroid metabolism. It is metabolized in the liver by hydroxylation; metabolites are excreted in the form of conjugated glucuronides. Pharmacologically active metabolites of levonorgestrel are unknown.

Excretion

Levonorgestrel is excreted in approximately equal proportions by the kidneys and through the intestines, exclusively in the form of metabolites. T_1/2 is about 26 hours.

Indications

• Emergency (postcoital) contraception within 72 hours (after unprotected sexual intercourse or failure of the contraceptive method used).

ICD codes

Dosage Regimen

1 tablet should be taken orally as soon as possible, preferably within 12 hours, but no later than 72 hours after unprotected sexual intercourse. If vomiting occurs within 3 hours after taking the Modelle^® 911 tablet, then another 1 tablet of Modelle^® 911 should be taken.

Modelle^® 911 can be used on any day of the menstrual cycle. In case of an irregular menstrual cycle, pregnancy must be preliminarily ruled out.

After taking the emergency contraceptive until the onset of the next menstruation, barrier methods of contraception (for example, condom, vaginal diaphragm, cervical cap) should be used.

Adverse Reactions

The frequency of adverse effects is classified according to WHO recommendations: very common – not less than 10%; common – not less than 1%, but less than 10%; uncommon – not less than 0.1%, but less than 1%; rare – not less than 0.01%, but less than 0.1%; very rare (including isolated cases) – less than 0.01%.

Nervous system disorders: very common – headache; common – dizziness.

Gastrointestinal disorders: very common – nausea, epigastric pain; common – vomiting, diarrhea.

Reproductive system and breast disorders: very common – acyclic spotting (bleeding), lower abdominal pain; common – breast tenderness, delay of menstruation by more than 5-7 days; very rare – dysmenorrhea.

Skin and subcutaneous tissue disorders: very rare – urticaria, skin rash, skin itching, facial edema.

General disorders: very common – feeling of tiredness.

Contraindications

• Hypersensitivity to levonorgestrel or any other component of the drug;
• Children under 16 years of age;
• Severe hepatic impairment;
• Pregnancy;
• Lactose intolerance, lactase deficiency, or glucose-galactose malabsorption.

With caution: liver and biliary tract diseases, jaundice (including in history), Crohn’s disease.

Use in Pregnancy and Lactation

Modelle^® 911 is contraindicated for use during pregnancy. Based on available data, in case of pregnancy occurring with the use of the emergency contraceptive method, no adverse effect of the drug on the fetus has been identified.

Levonorgestrel penetrates into breast milk. Breastfeeding should be discontinued for 24 hours after taking the drug.

Use in Hepatic Impairment

Contraindication: severe hepatic impairment.

Pediatric Use

Contraindication: children under 16 years of age.

Special Precautions

Modelle^® 911 should be used exclusively for emergency contraception. The effectiveness of emergency contraception decreases with delayed use of Modelle^® 911.

The drug does not replace the use of permanent methods of contraception.

Repeated use of Modelle^® 911 within one menstrual cycle is not recommended due to an increased frequency of acyclic spotting/bleeding.

In most cases, Modelle^® 911 does not affect the nature of the menstrual cycle. However, the appearance of acyclic spotting and a delay of menstruation by several days is possible. If menstruation is delayed by more than 5-7 days and its character changes (scanty or heavy discharge), pregnancy must be ruled out. The appearance of lower abdominal pain, fainting may indicate an ectopic pregnancy.

The use of levonorgestrel is not recommended in women at high risk of ectopic pregnancy (with a history of salpingo-oophoritis or ectopic pregnancy).

Emergency contraception does not protect against sexually transmitted diseases.

In case of gastrointestinal tract disorders (for example, Crohn’s disease), the effectiveness of the drug may be reduced.

Use in pediatrics

Experience with the use of levonorgestrel, 1.5 mg tablets, in children under 16 years of age is limited. The use of Modelle^® 911 in them is possible only in exceptional cases (including rape) and only after consultation with a gynecologist. A follow-up consultation with a gynecologist is recommended after emergency contraception.

Effect on ability to drive vehicles and operate machinery

The effect of the drug on the ability to drive vehicles and operate machinery has not been studied. In case of dizziness during the use of Modelle^® 911, caution should be exercised when performing activities requiring increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: nausea, vomiting, withdrawal bleeding.

Treatment: there is no specific antidote. Symptomatic therapy is carried out.

Drug Interactions

Concomitant use with inducers of liver microsomal enzymes accelerates the metabolism of levonorgestrel.

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 hypoglycemic and anticoagulant (coumarin derivatives, phenindione) drugs. It increases plasma concentrations of corticosteroids.

Women taking these drugs should consult a doctor.

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

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

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.