AMENA Tibolone 2.5mg Tablet 28's
RXDRUG-DRP-3524
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Used as menopausal therapy in the treatment of menopausal vasomotor symptoms and the prevention of post menopausal osteoporosis.
Dosage/Direction for Use
Tibolone is a steroid derived from noretynodrel that has oestrogenic, progestogenic, and weak androgenic properties. The usual dose is 2.5 mg daily by mouth. Tibolone reduces vasomotor symptoms associated with the use of gonadorelin analogues for endometriosis or fibroids.
Starting Tibolone: Women experiencing a natural menopause should commence treatment with tibolone at least 12 months after their last menstrual bleed. In case of surgical menopause, treatment with Tibolone, may commence immediately.
Switching from a sequential or continuous combined HRT preparation: If changing from a sequential HRT preparation, treatment with Tibolone should start the day following completion of the prior regimen. If changing from a continuous-combined HRT preparation, treatment can start at any time.
Missed dose: A missed dose should be taken as soon as remembered, unless it is 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. Missing a dose may increase the likelihood of breakthrough bleeding and spotting.
Starting Tibolone: Women experiencing a natural menopause should commence treatment with tibolone at least 12 months after their last menstrual bleed. In case of surgical menopause, treatment with Tibolone, may commence immediately.
Switching from a sequential or continuous combined HRT preparation: If changing from a sequential HRT preparation, treatment with Tibolone should start the day following completion of the prior regimen. If changing from a continuous-combined HRT preparation, treatment can start at any time.
Missed dose: A missed dose should be taken as soon as remembered, unless it is 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. Missing a dose may increase the likelihood of breakthrough bleeding and spotting.
Administration
May be taken with or without food.
Contraindications
Presence or history of hormone-dependent tumors, CV or cerebrovascular disorders including thrombophlebitis, thromboembolic processes or undiagnosed vag bleeding & severe liver disorders. Prior to or w/in 12 mth of the natural menopause. Pregnancy & lactation.
Special Precautions
Liver disease; disorders exacerbated by fluid retention eg, history or known kidney dysfunction, epilepsy & migraine; hypercholesterolemia, impaired glucose tolerance. Discontinue use if signs of thromboembolism, cholestatic jaundice, abnormal liver function tests. Stop treatment 4 wk before elective surgery. W/drawal bleed should be induced w/ a progestogen prior to treatment in women transferring from another form of HRT.
Adverse Reactions
Irregular vaginal bleeding or spotting may occur with tibolone, mainly during the first few months of treatment, and particularly in women undergoing a natural menopause who use tibolone within 12 months of their last menstrual period. Unlike cyclical, but similar to continuous, combination HRT, tibolone does not produce regular withdrawal bleeding. Other adverse effects have included changes in body-weight, ankle oedema, dizziness, skin reactions, headache, migraine, visual disturbances, gastrointestinal disturbances, increased growth of facial hair, altered liver function, depression, and arthralgia or myalgia.
Endometrial hyperplasia and endometrial carcinoma have been rarely reported after investigation of uterine bleeding in women receiving tibolone therapy, 1, 2 as has exacerbation of adenomyosis 3. Some of these women had previously received oestrogens. The authors of 1 report concluded that it was unclear whether tibolone was an aetiological agent or a cofactor in these cases, 1 and they emphasized that, although tibolone has progestogenic properties, it cannot be expected to reverse pre-existing endometrial hyperplasia or to protect against the development of endometrial malignancy.
The acute toxicity of tibolone in animals is very low. Therefore, toxic symptoms are not expected to occur, even when several tablets or capsules are taken simultaneously. In cases of acute overdose, nausea, vomiting and vaginal bleeding in females may occur. No specific antidote is known. Symptomatic treatment can be given if necessary.
Endometrial hyperplasia and endometrial carcinoma have been rarely reported after investigation of uterine bleeding in women receiving tibolone therapy, 1, 2 as has exacerbation of adenomyosis 3. Some of these women had previously received oestrogens. The authors of 1 report concluded that it was unclear whether tibolone was an aetiological agent or a cofactor in these cases, 1 and they emphasized that, although tibolone has progestogenic properties, it cannot be expected to reverse pre-existing endometrial hyperplasia or to protect against the development of endometrial malignancy.
The acute toxicity of tibolone in animals is very low. Therefore, toxic symptoms are not expected to occur, even when several tablets or capsules are taken simultaneously. In cases 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 at temperatures not exceeding 30°C. Protect from light.
Action
Pharmacodynamic: Following oral administration, tibolone is rapidly metabolized into three compounds, which all contribute to the pharmacodynamic profile of Tibolone. Two of the metabolites (3αOH-tibolone and 3βOH-tibolone) have estrogenic-like activities, whereas the third metabolite (4-isomer of tibolone) has progestogenic and androgenic-like activities. Tibolone substitutes for the loss of estrogen production in postmenopausal women and alleviates menopausal symptoms. Tibolone prevents bone loss following menopause or ovariectomy.
Pharmacokinetic: After oral administration, peak-plasma concentrations are attained in 1 to 4 hours. Tibolone is rapidly metabolized into 3 active metabolites, 2 of which have predominantly oestrogenic activity while the third, like the parent compound, has predominantly progestogenic activity. Metabolites are excreted in the bile and eliminated in the faeces. A small amount is excreted in the urine.
Pharmacokinetic: After oral administration, peak-plasma concentrations are attained in 1 to 4 hours. Tibolone is rapidly metabolized into 3 active metabolites, 2 of which have predominantly oestrogenic activity while the third, like the parent compound, has predominantly progestogenic activity. Metabolites are excreted in the bile and eliminated in the faeces. A small amount is excreted in the urine.
MedsGo Class
Oestrogens, Progesterones & Related Synthetic Drugs
Features
Brand
Amena
Full Details
Dosage Strength
2.5 mg
Drug Ingredients
- Tibolone
Drug Packaging
Tablet 28's
Generic Name
Tibolone
Dosage Form
Tablet
Registration Number
DRP-3524
Drug Classification
Prescription Drug (RX)
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