Levonorgestrel: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the local prescribing information.

Generic Medicine Info

Indications and Dosage

Intrauterine
Contraception, Menorrhagia

Adult: 52 mg released at an initial rate of 20 mcg/day. System is effective for up to 5 yr.

Oral
Contraception

Adult: Monotherapy: 30 or 37.5 mcg daily. Monophasic combined oral contraceptive (COC): 150-250 mcg daily. Triphasic COC: 50-125 mcg daily.

Oral
Emergency contraception

Adult: 1.5 mg as soon as possible or within 72 hr of coitus. Alternatively, 750 mcg as soon as possible or within 72 hr of coitus followed by a 2nd dose 12 hr later. Another regimen combines levonorgestrel 500 mcg and ethinylestradiol 100 mcg; may be given within 72 hr of coitus followed by a 2nd dose 12 hr later.

Oral
Menopausal hormone replacement therapy

Adult: As progestogenic component: 75-250 mcg for 10-12 days of a 28-day cycle.

Subcutaneous
Contraception

Adult: Insert 6 implants (36 mg/implant) under the skin within the first 7 days of the menstrual cycle and replace at intervals of up to 5 yr.

Transdermal
Menopausal hormone replacement therapy

Adult: As combined transdermal patch (releases 10 mcg/24 hr with an oestrogen): Apply once wkly for 2 wk of a 4-wk cycle. Alternatively, a patch releasing 7 or 15 mcg/24 hr with an oestrogen is applied once wkly for continuous HRT.

Administration

May be taken with or without food.

Contraindications

Pregnancy, undiagnosed vaginal bleeding, severe arterial disease; liver adenoma, porphyria; after recent evacuation of hydatidiform mole; history of breast cancer; hepatic impairment.

Special Precautions

Sex-steroid dependent cancer, past ectopic pregnancy, malabsorption syndromes, functional ovarian cysts, active liver disease, recurrent cholestatic jaundice, history of jaundice in pregnancy, CV or renal impairment, DM, asthma, epilepsy, migraine, conditions aggravated by fluid retention, depression and thromboembolism (high doses); lactation.

Adverse Reactions

Menstrual irregularities; nausea, vomiting, headache, dizziness, breast discomfort, gynaecomastia, depression, skin disorders, disturbance of appetite, wt changes, fluid retention, oedema, changes in libido, cholestatic jaundice, hair loss or hirsutism. Benign intracranial hypertension, thrombocytopenic purpura.
Potentially Fatal: Thrombocytopenia, stroke.

Drug Interactions

Reduced efficacy with enzyme-inducing drugs; aminoglutethimide. May inhibit ciclosporin metabolism.

Lab Interference

May interfere with laboratory tests e.g. liver, renal, thyroid and adrenal function tests, plasma levels of binding proteins and lipid/lipoprotein fractions, and fibrinolysis and coagulation parameters.

Action

Description: Levonorgestrel, a nortestosterone derivative, is an active isomer of norgestrel. It is a potent inhibitor of ovulation and has androgenic activity.
Pharmacokinetics:
Absorption: Rapid and almost complete from the GI tract (oral).
Distribution: Protein-binding: 42-68% (sex binding globulin), 30-56% (albumin). Distributed into breast milk.
Metabolism: Hepatic; converted to sulfate and glucuronide conjugates.
Excretion: Via urine and via faeces (lesser extent).

Storage

Intrauterine:
Store at 25°C (77°F).
Oral:
Contraception: Store at 20-25°C (68-77°F).

MIMS Class

Oral Contraceptives / Depot Contraceptives / Oestrogens, Progesterones & Related Synthetic Drugs

Disclaimer: This information is independently developed by MIMS based on Levonorgestrel from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com