药品详细
Norethindrone(炔诺酮)
化学结构式图
中文名
炔诺酮
英文名
Norethindrone
分子式
C20H26O2
化学名
(1S,2R,10R,11S,14R,15S)-14-ethynyl-14-hydroxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
分子量
Average: 298.4192
Monoisotopic: 298.193280076
Monoisotopic: 298.193280076
CAS号
68-22-4
ATC分类
G03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
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. [PubChem]
生产厂家
- Barr laboratories inc
- Duramed research inc
- Glenmark generics ltd
- Glenmark generics ltd india
- Ortho mcneil janssen pharmaceuticals inc
- Parke davis div warner lambert co
- Warner Chilcott
- Watson laboratories inc
封装厂家
- A-S Medication Solutions LLC
- Barr Pharmaceuticals
- Breckenridge Pharmaceuticals
- Bristol-Myers Squibb Co.
- Dept Health Central Pharmacy
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Duramed
- Glenmark Generics Ltd.
- Innovative Manufacturing and Distribution Services Inc.
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Murfreesboro Pharmaceutical Nursing Supply
- Novartis AG
- Noven Pharmaceuticals Inc.
- Novo Nordisk Inc.
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Ortho-McNeil-Janssen Pharmaceuticals Inc.
- Patheon Inc.
- Pfizer Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmaceutics International Inc.
- Pharmacia Inc.
- Physician Partners Ltd.
- Physicians Total Care Inc.
- Qualitest
- Quality Care
- Redpharm Drug
- Southwood Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- Warner Chilcott Co. Inc.
- Watson Pharmaceuticals
- WC Pharmaceuticals
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
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适应症
药理
| Indication | For use as an oral contraceptive in the prevention of pregnancy. |
| Pharmacodynamics | Norethindrone is a synthetic oral progestin. It is used for contraception or to treat such conditions as secondary amenorrhea, abnormal uterine bleeding, and endometriosis. As an oral contraceptive, norethindrone is available as either a single agent or in combination with an estrogen. |
| 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. |
| Absorption | Absolute oral bioavailability approximately 64% |
| Volume of distribution | Not Available |
| Protein binding | >95% |
| Metabolism |
Hepatic
|
| Route of elimination | Not Available |
| Half life | 7 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acitretin | Acitretine may cause a loss of contraceptive effect |
| Amobarbital | This product may cause a slight decrease of contraceptive effect |
| Aprobarbital | This product may cause a slight decrease of contraceptive effect |
| Artemether | Artemether may decrease the effectiveness of norethindrone by increasing its metabolism via CYP3A4. Consider an alternate non-hormonal means of contraception during artemether therapy. |
| Bexarotene | Bexarotene may decrease the serum concentration of Contraceptives (Progestins). Since bexarotene is teratogenic and can lower serum concentrations of norethindrone, it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form). |
| Bosentan | Bosentan may decrease the contraceptive effect of norethindrone. Hormonal contraception should not be relied on alone during concomitant therapy with bosentan. |
| Butabarbital | This product may cause a slight decrease of contraceptive effect |
| Butalbital | This product may cause a slight decrease of contraceptive effect |
| Butethal | This product may cause a slight decrease of contraceptive effect |
| Carbamazepine | This product may cause a slight decrease of contraceptive effect |
| Colesevelam | Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Progestins). Administer oral progestin-containing contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Consider alternatives in order to avoid this combination when possible, due to the risk for impaired contraceptive effectiveness. |
| Ethotoin | This product may cause a slight decrease of contraceptive effect |
| Fosphenytoin | This product may cause a slight decrease of contraceptive effect |
| Griseofulvin | This product may cause a slight decrease of contraceptive effect |
| Heptabarbital | This product may cause a slight decrease of contraceptive effect |
| Hexobarbital | This product may cause a slight decrease of contraceptive effect |
| Lamotrigine | The oral contraceptive decreases the effect of lamotrigine |
| Mephenytoin | This product may cause a slight decrease of contraceptive effect |
| Methohexital | This product may cause a slight decrease of contraceptive effect |
| Methylphenobarbital | This product may cause a slight decrease of contraceptive effect |
| Pentobarbital | This product may cause a slight decrease of contraceptive effect |
| Phenobarbital | This product may cause a slight decrease of contraceptive effect |
| Phenytoin | This product may cause a slight decrease of contraceptive effect |
| Pioglitazone | Possible loss of contraceptive effect |
| Primidone | This product may cause a slight decrease of contraceptive effect |
| Rifabutin | Rifabutin may decrease the contraceptive effect of norethindrone. Hormonal contraception should not be solely relied on alone during concomitant therapy with rifabutin. |
| Rifampin | This product may cause a slight decrease of contraceptive effect |
| Rifapentine | This product may cause a slight decrease of contraceptive effect |
| Rufinamide | Rufinamide decreases plasma concentrations of norethindrone, thus consider therapy modification |
| Secobarbital | This product may cause a slight decrease of contraceptive effect |
| St. John's Wort | St. John's Wort could reduce the contraceptive effect |
| Talbutal | This product may cause a slight decrease of contraceptive effect |
| Thiopental | Thiopental may decrease the effect of Norethindrone. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy. |
| Tizanidine | The contraceptive increases the effect of tizanidine |
| Tretinoin | Oral Tretinoin may decrease the effect of oral contraceptive, Norethindrone. An alternate form of contraception should be used during concomitant therapy. |
| Troglitazone | Possible loss of contraceptive effect |
| Warfarin | Norethindrone may alter the anticoagulant effect of warfarin. Concomitant therapy should be avoided. Monitor for changes in coagulation status if norethindrone is initiated, discontinued or dose changed. |
食物相互作用
- Take without regard to meals.
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