Tibolone


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Menopausal vasomotor symptoms; Prevention of postmenopausal osteoporosis 2.5 mg/day.
Dosage Details
Oral
Menopausal vasomotor symptoms, Prophylaxis of postmenopausal osteoporosis
Adult: 2.5 mg daily.
Administration
May be taken with or without food.
Contraindications
Known or suspected oestrogen dependent tumours in women, present or history of breast cancer, undiagnosed vaginal bleeding, severe liver disease, history or current CV or cerebrovascular disorders, untreated endometrial hyperplasia, porphyria, pregnancy and lactation, premenopausal women.
Special Precautions
Liver disease, history or risk factors of thromboembolic disorder, impaired glucose tolerance, hypercholesterolaemia, hypertriglyceridaemia, hypertension, cholelithiasis, SLE, uterine fibroids, endometriosis and history of endometrial hyperplasia. Disorders that may be worsened by fluid retention, eg. renal dysfunction, migraine, epilepsy. Discontinue in the event of thromboembolic or abnormal liver function results, significant increase in BP, new onset of migraine-type headache. Not recommended in women within 1 yr of menopause because of irregular vaginal bleeding. Stop tibolone 4 wk before elective surgery especially when prolonged immobilisation after surgery is expected. Adjustment of antidiabetic medications may be needed.
Adverse Reactions
Weight gain; dizziness; rash; pruritus; headache; migraine; visual disturbances; GI symptoms; facial hair growth; altered liver function; ankle oedema; depression; arthralgia or myalgia; irregular vaginal bleeding.
Potentially Fatal: Breast or endometrial cancer and stroke.
Drug Interactions
Enzyme inducers eg, barbiturates, phenytoin, carbamazepine and rifampicin may accelerate tibolone metabolism. Increased anticoagulant effects of warfarin.
Action
Description: Tibolone is a steroid that possesses oestrogenic, progestogenic and weak androgenic properties.
Pharmacokinetics:
Absorption: Rapidly and extensively absorbed after oral admin. Peak plasma concentrations after 1-1.5 hr (oral).
Metabolism: Converted into 3 active metabolites with 2 having predominantly oestrogenic property and 1 with progestogenic and androgenic property.
Excretion: Faeces (via the bile); via the urine (about 30% of a dose). The 2 main metabolites have an elimination half-life of about 7 hr.
Disclaimer: This information is independently developed by MIMS based on Tibolone 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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