Product Information
Registration Status: ActiveESTINOR TABLET 0.75mg is approved to be sold in Singapore with effective from 1991-01-10. It is marketed by DUOPHARMA (SINGAPORE) PTE LTD, with the registration number of SIN06596P.
This product contains Levonorgestrel 0.75mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by DUOPHARMA (M) SDN BHD in MALAYSIA.
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 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.