Generic Name
TiboloneTherapeutic Class: Bone and Joint Disorder
Indications:
Tibolone is indicated for the following conditions:
Tibolone: Each tablet contains Tibolone INN 2.5 mg.
Description:
Tibolone is a synthetic steroid with tissue-specific estrogenic, progestogenic, and androgenic effects. Following oral administration, tibolone is rapidly metabolized into three compounds, which contribute to the pharmacological effects of tibolone. Two of these metabolites (3 alpha-hydroxide-tibolone and 3 beta-hydroxide-tibolone) have predominantly estrogenic activity, a third metabolite (delta 4-isomer of tibolone) and the parent compound have progestogenic and androgenic activities.
Dosage & Administration:
Climacteric symptoms & other post-menopausal problems in adults and elderly women: The dosage is 2.5 mg tablet per day, preferably at the same time of the day. Symptomatic relief occurs within few days, but optimal results are obtained minimum after 3 months.
Osteoporosis: To prevent osteoporosis in post-menopausal women or after oophorectomy an uninterrupted longer (5-10 years) therapy of 2.5 mg daily is needed.
StartingTibolone:
In case of natural menopause: To avoid irregular & abnormal bleeding, Tibolone should be started at least 12 months after the 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 the 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.
Side Effects:
Generally, tibolone is well tolerated. However, a few adverse reactions have been observed like headache, pre-tibial oedema, change in body mass, dizziness, rash, and abdominal pain. Vaginal bleeding may occur mainly during the first 1-3 months of treatment.
Precautions:
Renal dysfunction.
Epilepsy or migraine.
Impaired carbohydrate metabolism.
Hypercholesterolemia.
Liver diseases.
With anticoagulants.
Use in Pregnancy & Lactation:
Tibolone is contraindicated in pregnancy and lactation.
Interaction:
Since tibolone may increase blood fibrinolytic activity, it may enhance the effect of anticoagulants. This effect has been reported with warfarin.
Drugs that induce hepatic microsomal enzymes or other enzyme-inducing drugs may accelerate the metabolism of tibolone and thus lower its activity.
Overdose:
The acute toxicity of tibolone in animals is very low. Therefore, toxic symptoms are not expected to occur, even when several tablets are taken simultaneously. In case of acute overdose nausea, vomiting, withdrawal bleeding, etc. may occur. Symptomatic treatment can be given if necessary.
Storage:
Keep in a cool & dry place. Protect from light. Keep out of the reach of children.
Tibolone is indicated for the following conditions:
- Treatment of the climacteric symptoms [hot flushes, sweating, vaginal dryness & less elasticity, mood disorders, anxiety, etc.] resulting from natural or artificial menopause.
- Prevention of postmenopausal and post oophorectomy osteoporosis and improvement of bone mineral density in patients with established postmenopausal osteoporosis.
- Vaginal atrophy.
- Prevention of frequent UTI and urinary incontinence in postmenopausal women.
Tibolone: Each tablet contains Tibolone INN 2.5 mg.
Description:
Tibolone is a synthetic steroid with tissue-specific estrogenic, progestogenic, and androgenic effects. Following oral administration, tibolone is rapidly metabolized into three compounds, which contribute to the pharmacological effects of tibolone. Two of these metabolites (3 alpha-hydroxide-tibolone and 3 beta-hydroxide-tibolone) have predominantly estrogenic activity, a third metabolite (delta 4-isomer of tibolone) and the parent compound have progestogenic and androgenic activities.
Dosage & Administration:
Climacteric symptoms & other post-menopausal problems in adults and elderly women: The dosage is 2.5 mg tablet per day, preferably at the same time of the day. Symptomatic relief occurs within few days, but optimal results are obtained minimum after 3 months.
Osteoporosis: To prevent osteoporosis in post-menopausal women or after oophorectomy an uninterrupted longer (5-10 years) therapy of 2.5 mg daily is needed.
StartingTibolone:
In case of natural menopause: To avoid irregular & abnormal bleeding, Tibolone should be started at least 12 months after the 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 the 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.
Side Effects:
Generally, tibolone is well tolerated. However, a few adverse reactions have been observed like headache, pre-tibial oedema, change in body mass, dizziness, rash, and abdominal pain. Vaginal bleeding may occur mainly during the first 1-3 months of treatment.
Precautions:
Renal dysfunction.
Epilepsy or migraine.
Impaired carbohydrate metabolism.
Hypercholesterolemia.
Liver diseases.
With anticoagulants.
Use in Pregnancy & Lactation:
Tibolone is contraindicated in pregnancy and lactation.
Interaction:
Since tibolone may increase blood fibrinolytic activity, it may enhance the effect of anticoagulants. This effect has been reported with warfarin.
Drugs that induce hepatic microsomal enzymes or other enzyme-inducing drugs may accelerate the metabolism of tibolone and thus lower its activity.
Overdose:
The acute toxicity of tibolone in animals is very low. Therefore, toxic symptoms are not expected to occur, even when several tablets are taken simultaneously. In case of acute overdose nausea, vomiting, withdrawal bleeding, etc. may occur. Symptomatic treatment can be given if necessary.
Keep in a cool & dry place. Protect from light. Keep out of the reach of children.
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