Composition

Each uncoated tablet contains Tibolone 2.5 mg

Description

Following oral administration tibolone is rapidly metabolised into three compounds which contribute to the pharmacological effects of tibolone. Two of these metabolite (3µ - OH - tibolone and 3b - OH - tibolone) have predominantly estrogenic activity, a third metabolite (D4 - isomer of tibolone) and the parent compound have progestagenic and androgenic activities.

Tibolone has various tissue-specific effects. It has estrogenic effect on the vagina, on bone and on the thermoregulatory centres in the brain (hot flushes). Tibolone has predominantly progestagenic effects on the breast. Tibolone does not induce endometrial proliferation, due to local conversion to the D4 - isomer. Therefore, if vaginal bleeding occurs this usually results from an atrophic endometrium. Tibolone also has effects on certain metabolic and haematological parameter such as a decrease in plasma high densiy lipoprotein cholesterol, triglycerides and lipoprotein (a), and an increase in blood fibreinolytic activity. Finally, tibolone has favourable effects on mood and libido.

Indications

Complaints resulting from the natural or artificial menopause.

Contraindications

• Pregnancy
• Known or suspected hormone - dependent tumours
• Cardiovascular or cerebrovascular disorders e.g. thrombophlebitis, thrombo-embolic processes or a history of these conditions
• Undiagnosed vaginal bleeding
• Severe liver disorders

Dosage and Administration

The dosage is 2.5 mg per day. The tablet should be swallowed with some water or other drink, preferably at the same time of day. Improvement of symptoms generally occurs within a few weeks, but optimal results are obtained when therapy is continued for at least 3 months. At the recommended dosage, tibolone may be used uninterrupted for longer periods.

Starting Tibolone

Women experiencing a natural menopause should commence treatment with tibolone 12 months after their last natural bleed. If tibolone is taken sooner than this, irregular menstrual bleeding may occur. In the case of artifical menopause, treatment with tibolone may commence immediately switching from conventional hormone replacement therapy (HRT).

In women with a uterus who change from an estrogen - only preparation, a withdrawal bleed should be induced before starting tibolone. If changing from sequential HRT preparation treatment with tibolone should start after the progestagen phase has been completed. If changing from a continuous - combined HRT preparation, treatment can start at any time. If abnormal vaginal bleeding is the reason for switching from conventional HRT, it is advised to investigate the cause of bleeding before starting tibolone.

Missed tablets

A missed dose should be taken as soon as remembered, unless it is more that 12 hours overdue. In the latter case, the missed dose should be skipped and the next dose should be taken at the normal time.

Warning and Precautions

• Tibolone is not intended for contraceptive use
• Risk and benefits should be considered when have had any liver disorder or disturbances of the lipid and Lipoprotein profile
• Treatment should be discontinued if signs of thromboembolic processes occur, if results of liver function tests become abnormal, or of cholestatic jaundice appears
• The occurrence of vaginal bleeding or spotting soon after starting treatment with Tibolone may be due to the residual effects of endogenous or exogenous estrogens. Bleeding commencing after three months of treatment, or persistent bleeding should be appropriately investigated; however, in most cases no apparent cause of bleeding is found.
• As with all steroids with hormonal activity, yearly medical examination is advisable

Interactions

Since Tibolone may increase blood fibrinolytic activity, it may enhance the effect of anticoagulants. This effect has been reported with warafin.

Pregnancy and Lactation

Tibolone is contraindicated in pregnancy and lactation

Adverse reactions

Occasionally, vaginal bleeding or spotting, vaginal discharge, breast pain or abdominal pain may occur, mainly during the first months of treatment. Other adverse events that have been observed occasionally include: headache or migraine, oedema, dizziness, pruritus, increase in body weight, nausea, rash, hirsutism and depression.

Overdosage

The acute toxicity if 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 and vaginal bleeding in females may occur. No specific antidote is known. Symptomatic treatment can be given if necessary.

Presentation

Blister pack of 14 tablets