Product Information
Registration Status: ActiveMICROGYNON 30 TABLET is approved to be sold in Singapore with effective from 1990-06-26. It is marketed by BAYER (SOUTH EAST ASIA) PTE LTD, with the registration number of SIN04834P.
This product contains Ethinylestradiol 0.03mg, and Levonorgestrel 0.15mg 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.
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.
Description
A synthetic progestational hormone with actions similar to those of progesterone and about twice as potent as its racemic or (+-)-isomer (norgestrel). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. It is usually supplied in a racemic mixture (Norgestrel, 6533-00-2). Only the levonorgestrel isomer is active. Levonorgestrel is marketed mostly as a combination oral contraceptive under several brand names such as Alesse, Triphasil, and Min-Ovral.
Indication
For the treatment of menopausal and postmenopausal disorders and alone or in combination with other hormones as an oral contraceptive.
Mechanism of Action
Binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like levonorgestrel will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge.
Pharmacokinetics
- Absorption
- Levonorgestrel is not subjected to a "first-pass" effect and is virtually 100% bioavailable.
- Distribution
- * 260 L [Healthy Female Volunteers under Fasting Conditions] * 1.8 L/kg
- Metabolism
- Hepatic
- Elimination
Clearance
* 7.7 +/- 2.7 L/h [Healthy Female Volunteers under Fasting Conditions]
Toxicity
LD50 >5000 mg/kg (orally in rats)
Active Ingredient/Synonyms
(-)-13-Ethyl-17-hydroxy-18,19-dinor-17alpha-pregn-4-en-20-yn-3-one | (8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy- 1,2,6,7,8,9,10,11,12,13,14,15,16, 17- tetradecahydrocyclopenta[a] phenanthren-3-one | 13-beta-Ethyl-17alpha-ethynyl-17beta-hydroxygon-4-en-3-one | 13-Ethyl-17-alpha-ethynyl-17-beta-hydroxy-4-gonen-3-one | 13-Ethyl-17-alpha-ethynylgon-4-en-17-beta-ol-3-one | 17-alpha-Ethinyl-13-beta-ethyl-17-beta-hydroxy-4-estren-3-one | 17-alpha-Ethynyl-13-ethyl-19-nortestosterone | 17-Ethynyl-18-methyl-19-nortestosterone | 17alpha-Ethynyl-13beta-ethyl-3-oxo-4-estren-17beta-ol | 17alpha-Ethynyl-17-hydroxy-18-methylestr-4-en-3-one | 17alpha-Ethynyl-18-homo-19-nortestosterone | 18-Methyl-17-alpha-ethynyl-19-nortestosterone | 18-Methylnorethisterone | d(-)-Norgestrel | Jadelle | Levonelle | Levonorgestrel | Lévonorgestrel | Levonorgestrelum | Levonova | Microlut | Microluton | Microval | NorLevo | Postinor | Levonorgestrel |
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.