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Products

Amena

Comfort from menopausal discomforts


Amena's generic name is Tibolone. Tibolone is an effective therapy for vasomotor symptoms -- Hot flushes, Night Sweats; Improves mood, vaginal dryness and sexual well-being; Reduces risk of vertebral and non-vertebral fractures; Lowers total cholesterol and triglyceride levels; Mitigates menopause related decline in muscle strength; Helps protect against Coronary Artery Disease; May reduce incidence of diabetes; Aids in reducing incidence of breast cancer






Tibolone




Brand Name, Dosage Format and Strength
Amena  2.5 mg 

Therapeutic Category


Sub Therapeutic


Class


Marketing Division





CLINICAL PHARMACOLOGY

Pharmacodynamics 

Tibolone is a synthetic steroid compound characterized as a selective tissue estrogenic activity regulator (STEAR). Tibolone itself has no biological activity; its effects are the results of the activity of its metabolites on various tissues. The 3αOH and 3βOH metabolites of tibolone act like estrogen in the thermoregulatory centers in the brain (preventing hot flushes), bone (preventing bone loss) and vaginal tissue (preventing dryness and soreness). In endometrial tissue, the ?4-isomer acts like progesterone in the womb to prevent overgrowth of the endometrium and subsequent bleeding.

In breast tissue, the main actions of the progestogenic ?4-isomer of tibolone are strong inhibition of sulfatase activity and weak inhibition of 17α-hydroxysteroid dehydrogenase activity which result in blocking the conversion of estrone sulfate to the active hormones estrone and 17β-estradiol. Tibolone inhibits human breast cell proliferation and stimulates apoptosis. Unlike classical hormone replacement therapy, the incidence of breast tenderness is low and mammographic density does not increase with tibolone,

Tibolone has androgenic effects on certain metabolic and hematological parameters such as decrease in plasma high density lipoprotein cholesterol, triglycerides and lipoprotein(a), and may increase blood fibrinolytic activity.

Tibolone improves vaginal dryness and vaginal atrophy. Tibolone has testosterone-like activity that appears to play a role in enhancing women’s mood and libido, although response is variable.

 

Pharmacokinetics

Tibolone is rapidly and extensively absorbed after oral administration. It is rapidly metabolized by the liver into two estrogenic metabolites (3α- and     3β-OH-tibolone), which bind to the estrogen receptor, and a third metabolite, the ?4-isomer, which binds to the progesterone and androgen receptors. Some of the pharmacokinetic parameters of tibolone cannot be determined due to its very low plasma levels. There is no significant effect on the extent of absorption when taken with food.

Peak concentrations of tibolone and its metabolites occur about 1 to 1.5 hours after oral administration; the two main metabolites have an elimination half-life of about 7 hours. Metabolites are excreted in the bile and eliminated in the feces. About 30% of a dose is excreted in the urine.

The pharmacokinetic parameters for tibolone and its metabolites were found to be independent of renal function.


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