Lalinola (Tablets) Instructions for Use

Marketing Authorization Holder

Lupin, Ltd. (India)

ATC Code

G03AC03 (Levonorgestrel)

Active Substance

Levonorgestrel (Rec.INN registered by WHO)

Dosage Form

Lalinola

Tablets 1.5 mg: 1 pc.

Dosage Form, Packaging, and Composition

Tablets from white to almost white, round, biconvex, with an engraving “LV1” on one side and smooth on the other side.

Excipients: lactose monohydrate – 140.1 mg, corn starch – 184 mg, povidone K30 – 8 mg, corn starch – 14 mg, colloidal silicon dioxide – 1.2 mg, magnesium stearate – 1.2 mg.

1 pc. – blisters (1) – cardboard packs.

Clinical-Pharmacological Group

Gestagen

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 suppression of 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 one 1.5 mg tablet orally as a single dose.

Initiate treatment within 72 hours (3 days) after unprotected sexual intercourse or contraceptive failure.

Take the tablet with water; administration is independent of meals.

For maximum efficacy, take the dose as soon as possible after the unprotected event; effectiveness decreases with time.

If vomiting occurs within 3 hours of ingestion, take another 1.5 mg tablet immediately.

This regimen is for occasional use only and does not replace a regular method of contraception.

Menstrual bleeding typically occurs at the expected time or a few days earlier or later.

If your next menstrual period is more than 7 days late or is unusually light or heavy, rule out pregnancy.

For use as an intrauterine system, follow the specific insertion instructions provided with that product; the dosage regimen differs.

Consult a healthcare professional for any questions regarding administration or if a dose is missed post-intake.

Adverse Reactions

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

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 swelling.

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 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, you should consult a doctor 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 processes of oxidative metabolism 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.