Product Information
Registration Status: ActiveNORETHISTERONE TABLET 5mg is approved to be sold in Singapore with effective from 1990-06-28. It is marketed by BEACONS PHARMACEUTICALS PTE LTD, with the registration number of SIN04889P.
This product contains Norethisterone 5mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by BEACONS PHARMACEUTICALS PTE LTD in SINGAPORE.
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
Norethisterone (INN, BAN), also known as Norethindrone (USAN), is a synthetic progestational hormone with actions similar to those of progesterone but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for contraception.
Indication
For the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer.
Mechanism of Action
Progestins diffuse freely into target cells and bind to the progesterone receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.
Pharmacokinetics
- Absorption
- Norethindrone acetate is completely and rapidly deacetylated to norethindrone (NET) after oral administration, and the disposition of norethindrone acetate is indistinguishable from that of orally administered norethindrone. Norethindrone is rapidly absorbed from norethindrone acetate, in which maximum plasma concentration occur 2 hours post-dose (Tmax). When a single dose is given to healthy women, the Cmax is 26.19 ± 6.19 hours. The AUC (0-inf) is 166.90 ± 56.28 ng/mL*h. Absolute oral bioavailability is approximately 64%. The effect of food on the pharmacokinetics of norethindrone acetate is unknown.
- Distribution
- * 4 L/kg
- Metabolism
- Hepatic. Norethindrone is extensively metabolized, primarily via reduction. It also undergoes sulfate and glucuronide conjugation. The majority of metabolites in the circulation are sulfates, with glucuronides accounting for most of the urinary metabolites.
- Elimination
Clearance
* 0.4 L/hr/kg [plasma clearance]
Active Ingredient/Synonyms
(17alpha)-17-Ethynyl-17-hydroxyestra-4,8(14),9-trien-3-one | 17-alpha-Ethynyl-17-hydroxy-4-estren-3-one | 17-alpha-Ethynyl-19-norandrost-4-en-17-beta-ol-3-one | 17-alpha-Ethynyl-19-nortestosterone | 17-alpha-Ethynyl-4-estren-17-ol-3-one | 17-beta-Hydroxy-19-norpregn-4-en-20-yn-3-one | 17-Hydroxy-19-nor-17-alpha-pregn-4-en-20-yn-3-one | 17-Hydroxy-19-nor-17alpha-pregn-4-en-20-yn-3-one | 17alpha-Ethinyl-19-nortestosterone | 17alpha-Ethinylestra-4-en-17beta-ol-3-one | 17alpha-Ethynyl-17-hydroxy-4-estren-3-one | 17alpha-Ethynyl-17beta-hydroxy-19-norandrost-4-en-3-one | 17alpha-Ethynyl-19-nor-4-androsten-17beta-ol-3-one | 17alpha-Ethynyl-19-norandrost-4-en-17beta-ol-3-one | 17alpha-Ethynyl-19-nortestosterone | 17alpha-Ethynyl-4-estren-17-ol-3-one | 17beta-Hydroxy-19-norpregn-4-en-20-yn-3-one | 17α-ethinyl-19-nortestosterone | 19-Nor-17-alpha-ethynyl-17-beta-hydroxy-4-androsten-3-one | 19-Nor-17-alpha-ethynylandrosten-17-beta-ol-3-one | 19-Nor-17-alpha-ethynyltestosterone | 19-Nor-17alpha-ethynyl-17beta-hydroxy-4-androsten-3-one | 19-Nor-17alpha-ethynylandrosten-17beta-ol-3-one | 19-Nor-17alpha-ethynyltestosterone | 19-nor-17α-ethynyltestosterone | 19-Nor-ethindrone | 19-Norethisterone | 4-Estren-17alpha-ethynyl-17beta-ol-3-one | Norethindrone | Norethisteron | Norethisteronum | Noretisterona | Norethisterone |
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.