Tibolone Tablets
Sibolone™

Composition:
Each uncoated tablet contains
Tibolone……………………….....2.5 mg

Description: Tibolone is rapidly metabolised into three compounds which contribute to its pharmacological effects and oral administration. Two of these compounds (3α-OH-tibolone and 3ß-OH- Tibolone) have predominantly estrogenic activity, while the third compound (Δ4-isomer of Tibolone) and the parent compound have progestogenic and androgenic activities.

The various effects of Tibolone are issue-specific. It has estrogenic effect on the vagina. On bone and on the thermoregulatory centers in the brain. It 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 haematological 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 favorable 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 liquid, preferably at the same time of a day. Improvement of symptoms generally occurs within a few weeks, but optimal results are seen when therapy is continued for at least 3 months. Tibolone may be used uninterrupted for longer periods.

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

In a woman with a uterus who changes 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 its more than 12 hours overdue. In the latter case, the missed dose should be skipped and the next dose should be taken at the normal time.

Contraindications:

• Pregnancy
• Known or suspected hormone-dependent tumors
• Cardiovascular or cerebrovascular disorders
• Undiagnosed vaginal bleeding
• Severe liver disorders

Warning and precautions:

• Tibolone is not indicated 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 of cholestatic jaundice occurs.
• 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 well with steroids with hormonal activity, yearly medical examination is advisable.
  

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 month of treatment. Other adverse events that have been observed occasionally include: Headache or migraine, oedema, dizziness, pruitus, increase in body weight, nausea, rash, hirsutism and depression.

Over dosage: 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 and vaginal bleeding in females may occur. No specific antidote is known. Symptomatic treatment can be given if necessary.

Storage: Store in cool, dry and dark place.

Presentation: 2 blister packs of 15 tablets each.