Tibolone
Indications
Tibolone is used for:
Menopausal vasomotor symptoms [hot flushes, sweating, vaginal dryness & less elasticity, mood disorders, anxiety etc.], postmenopausal and post oophorectomy osteoporosis, improvement of bone-mineral density, Vaginal atrophy, Prevention of frequent UTI and urinary incontinence in postmenopausal women.
Adult Dose
Oral
Menopausal vasomotor symptoms;
Adult: 2.5 mg daily.
Symptomatic relief occurs within few days, but optimal results are obtained minimum after 3 months.
Prophylaxis of postmenopausal osteoporosis
Adult: 2.5 mg daily.
To prevent osteoporosis in post-menopausal women or after oophorectomy an uninterrupted longer (5-10 years) therapy is needed.
Starting Tibolone:
In case of natural menopause: To avoid irregular & abnormal bleeding, Tibolone should be started at least 12 months after last natural bleeding.
In case of artificial menopause: Treatment should be started immediately.
In case of switching over from other conventional HRT: If someone switches from estrogen-only preparation, she should start after a withdrawal bleeding. If someone switches from sequential HRT preparation she should wait for the completion of the progestogen phase. If someone switches from continuous combined HRT, she can start any time.
In case of missed pill: If no more than 12 hours have passed, the pill should be taken immediately. Otherwise the next dose should be continued as before.
Child Dose
Renal Dose
Administration
May be taken with or without food.
Contra Indications
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.
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.
Pregnancy-Lactation
Interactions
Enzyme inducers eg, barbiturates, phenytoin, carbamazepine and rifampicin may accelerate tibolone metabolism. Increased anticoagulant effects of warfarin.
Adverse Effects
Side effects of Tibolone :
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.
Mechanism of Action
Tibolone is a steroid that possesses oestrogenic, progestogenic and weak androgenic properties.