Product Information
Registration Status: ActiveSIN04784P
DIANE-35 TABLET is approved to be sold in Singapore with effective from 1990-11-06. It is marketed by BAYER (SOUTH EAST ASIA) PTE LTD, with the registration number of SIN04784P.
This product contains Cyproterone 2mg, and Ethinylestradiol 0.035mg in the form of TABLET, SUGAR-COATED. It is approved for ORAL use.
This product is manufactured by BAYER WEIMAR GMBH UND CO. KG in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
An anti-androgen that, in the form of its acetate (cyproterone acetate), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. [Pubchem]
Indication
For the palliative treatment of patients with advanced prostatic carcinoma.
Mechanism of Action
The direct antiandrogenic effect of cyproterone is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. In addition, cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of luteinizing hormone resulting in diminished production of testicular testosterone.
Pharmacokinetics
- Absorption
- Completely absorbed following oral administration.
- Distribution
- Metabolism
- Primarily hepatic. Cyproterone acetate is metabolized by the CYP3A4 enzyme, forming the active metabolite 15beta-hydroxycyproterone acetate, which retains its antiandrogen activity, but has reduced progestational activity.
- Elimination
Active Ingredient/Synonyms
Cyproterone 17-O-acetate | Cyproterone acetate |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.
Description
A semisynthetic alkylated estradiol with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally and is often used as the estrogenic component in oral contraceptives. Ethinyl estradiol is marketed mostly as a combination oral contraceptive under several brand names such as Alesse, Tri-Cyclen, Triphasil, and Yasmin. The FDA label includes a black box warning that states that combination oral contraceptives should not be used in women over 35 years old who smoke due to the increased risk of serious cardiovascular side effects.
Indication
For treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.
Mechanism of Action
Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. This cascade is initiated by initially binding to the estrogen receptors. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).
Pharmacokinetics
- Absorption
- Rapid and complete absorption follows oral intake of ethinyl estradiol (bioavailability 43%).
- Distribution
- Metabolism
- Hepatic. Quantitatively, the major metabolic pathway for ethinyl estradiol, both in rats and in humans, is aromatic hydroxylation, as it is for the natural estrogens.
- Elimination
Toxicity
Oral, mouse LD50: 1737 mg/kg. Symptoms of overdose include nausea and vomiting, and withdrawal bleeding may occur in females. The FDA label includes a black box warning that states that combination oral contraceptives with ethinyl estradiol should not be used in women over 35 years old who smoke due to the increased risk of serious cardiovascular side effects.
Active Ingredient/Synonyms
17-ethinyl-3,17-estradiol | 17-ethinyl-3,17-oestradiol | 17-ethinylestradiol | 17alpha-Ethinyl estradiol | 17α-ethynylestradiol | Ethinylestradiol | Ethinylestradiolum | Ethinyloestradiol | Ethynyl estradiol | Etinilestradiol | Ethinyl Estradiol |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.