Norgestimate


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Part of combined oral contraceptive Usual dose in monophasic preparations: 250 mcg/day; triphasic preparations: 180-250 mcg/day. As progestogen component in menopausal HRT; Atrophic vaginitis; Prevention of osteoporosis As a combination preparation: Treatment is cyclical and consists of oestradiol once daily for 3 days, followed by norgestimate 0.09 mg/day w/ oestradiol for the next 3 days; repeat the 6-day cycle continuously.
Dosage Details
Oral
Atrophic vaginitis, Progestogen component in menopausal hormonal replacement therapy, Prophylaxis of osteoporosis
Adult: As a combination preparation: Treatment is cyclical and consists of 1 tablet of oestradiol 1 mg once daily for 3 days, followed by 1 tablet of oestradiol 1 mg and norgestimate 0.09 mg once daily for the next 3 days; repeat the 6-day cycle continuously.

Oral
Part of combined oral contraceptive
Adult: Usual dose in monophasic preparations: 250 mcg/day; triphasic preparations: 180-250 mcg/day.
Contraindications
Undiagnosed abnormal vaginal bleeding; history of or current thrombophlebitis or venous thromboembolic disorders; active or recent (within 1 year) arterial thromboembolic disease (e.g. stroke, MI); breast carcinoma, oestrogen-dependent tumour; hepatic impairment or disease; pregnancy.
Special Precautions
Lactation. CV or renal impairment, DM, asthma, epilepsy and migraine. Conditions which may be made worse by fluid retention. Patients with a history of depression. Large doses should be used with caution in patients who are susceptible to thromboembolism. When used as a contraceptive, its efficacy may be compromised during episodes of vomiting or diarrhoea.
Adverse Reactions
GI discomfort, changes in appetite or wt, fluid retention, oedema, acne, chloasma (melasma), allergic skin rashes, urticaria, mental depression, changes in libido, hair loss, hirsutism, fatigue, drowsiness or insomnia, fever, headache. May alter menstrual cycles. May alter serum lipid levels and LFTs.
Drug Interactions
Enzyme inducers e.g. carbamazepine, griseofulvin, phenobarbital, phenytoin, and rifampicin may increase clearance of progesterone and progestogens. Aminoglutethimide may reduce the serum levels of norgestimate. May inhibit ciclosporin metabolism. May also affect the efficacy of antidiabetic medications thus requiring a change in the antidiabetic dosage.
Action
Description: Norgestimate is a progestogen that is structurally related to levonorgestrel. It binds to androgen and progestogen receptors but not oestrogen receptors. It counters oestrogenic effects by decreasing the number of nuclear oestradiol receptors and suppressing epithelial DNA synthesis in endometrial tissue. It is commonly used as the progestogenic component in combined oral contraceptives and menopausal HRT.
Pharmacokinetics:
Absorption: Largely metabolised in the GI/liver during 1st pass effect; its main active metabolite, 17-deacetylnorgestimate, reaches Cmax at approximately 2 hr after dose.
Distribution: Protein binding of 17-deacetylnorgestimate: Approximately 99%.
Excretion: Half-life of 17-deacetylnorgestimate: About 37 hr. Norgestimate metabolites are excreted via urine and faeces.
Disclaimer: This information is independently developed by MIMS based on Norgestimate 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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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