Generic Livial, Tibolone Tablet Patient Information Sheet

For the use of a registered medical practitioner or a hospital or a laboratory

Description:

Following oral administration tibolone is rapidly metabolised into three compounds which contribute to the pharmacological effects of tibolone Two of these metabolite (3a - OH - tibotone and 3fi - OH - tibotone) have predominantly estrogenic activity, a third metabolite i.\4 - 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 4 - isomer. Therefore, if vaginal bleeding occurs this usually results from an atrophic endometrium. Tibolone also has effects on certain metabolic and hematological parameter such as a decrease in plasma high density lipoprotein cholesterol, triglycerides and lipoprotein (a), and an increase in blood fibrinolytic activity Finally, tibolone has favourable effects on mood and libido.

Indications:

Complaints resulting from the natural or artificial menopause.

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 ot 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 HPT 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

TIBOFEM

Composition:

Each uncoated tablet contains Tibolone BP ........................ 2.S

2.5 mg

008 IC MK 7

Children:

Not applicable

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

Warning and precautions:

• Tibolone is not intended for contraceptive use

• Risk benefit should be considered when any of the following medical conditions exist

a. Liver disorders or a history of this condition

b. 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 ot 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 ot anticoagulants. This effect has been reported with warfarin

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 ot 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.

Storage:

Store in a cool dry place. Protect form light & moisture

Presentation:

Blister pack of 14 tablets

Cipla