Indications |
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. Intrauterine Contraception Adult: 52 mg released at an initial rate of 20 mcg/day. System is effective for up to 5 yr. Intrauterine Menorrhagia Adult: 52 mg released at an initial rate of 20 mcg/day. System is effective for 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. |
Contraindications |
Pregnancy, undiagnosed vaginal bleeding, severe arterial disease; liver adenoma, porphyria; after recent evacuation of hydatidiform mole; history of breast cancer; hepatic impairment. |
Warnings / 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. See Below for More levonorgestrel Drug Interactions |
Lab Interactions |
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. |
Mechanism of Actions |
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). |
Administration |
May be taken with or without food. |
Storage Conditions |
Intrauterine: Store at 25°C (77°F). |
ATC Classification |
G03AC03 - levonorgestrel ; Belongs to the class of progestogens. Used as systemic contraceptives. |
Storage |
Intrauterine: Store at 25°C (77°F). |
Available As |
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Levonorgestrel
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Levonorgestrel Containing Brands
Levonorgestrel is used in following diseases
Drug - Drug Interactions of Levonorgestrel
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