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Levonorgestrel information from DrugsUpdate  

See Available Brands of Levonorgestrel in India

P - Contraindicated in pregnancy
L - Caution when used during lactation
LI - Lab *

Levonorgestrel (or l-norgestrel or D-norgestrel) is a synthetic progestogen used as an active ingredient in some hormonal contraceptives.

Pharmacodynamics

Information Not Available

Pharmacokinetics

Levonorgestrel, a nortestosterone derivative, is an active isomer of norgestrel. It is a potent inhibitor of ovulation and has androgenic activity.

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).

Levonorgestrel Indications / Levonorgestrel Uses

Information Not Available

Levonorgestrel Adverse Reactions / Levonorgestrel Side Effects

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.

Precautions

Information Not Available

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.

Other Drug Interactions

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

Other Interactions

Information Not Available

Dosage

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

Transdermal
Menopausal hormone replacement therapy
Adult: As combined transdermal patch (releases 10 mcg/24 hours with an oestrogen): Apply once weekly for 2 weeks of a 4-weeks cycle. Alternatively, a patch releasing 7 or 15 mcg/24 hours with an oestrogen is applied once wkly for continuous HRT.

Intrauterine

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

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

Food(before/after)

May be taken with or without food

List of Contraindications

Levonorgestrel and Pregnancy

Contraindicated in pregnancy

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Levonorgestrel and Lactation

Caution when used during lactation

Levonorgestrel and Children

Safety and efficacy before menarche not established

Levonorgestrel and Geriatic

Information Not Available

Levonorgestrel and Other Contraindications

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

Storage

Intrauterine
Store at 25°C (77°F).

Lab interference

Intrauterine
Store at 25°C (77°F).

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