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药品详细

Norgestimate(诺孕酯)

化学结构式图
中文名
诺孕酯
英文名
Norgestimate
分子式
C23H31NO3
化学名
(1S,2R,5E,10R,11S,14R,15S)-15-ethyl-14-ethynyl-5-(hydroxyimino)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-yl acetate
分子量
Average: 369.4971
Monoisotopic: 369.230393863
CAS号
35189-28-7
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

Norgestimate is a form of progesterone, which is a female hormone important for the regulation of ovulation and menstruation. Norgestimate is used with estradiol to treat the symptoms of menopause.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Steroids and Steroid Derivatives
    Substructures
    • Steroids and Steroid Derivatives
    • Carboxylic Acids and Derivatives
    • Hydroxy Compounds
    • Alkanes and Alkenes
    • Acetates
    • Alkynes
    • Ethers
    • Imines
    • Cyclohexenes and Derivatives
    • Oximes and Derivatives
    适应症
    药理
    Indication For the prevention of pregnancy
    Pharmacodynamics Norgestimate is used as a female contraceptive. Norgestimate is a progestin or a synthetic form of the naturally occurring female sex hormone, progesterone. In a woman's normal menstrual cycle, an egg matures and is released from the ovaries (ovulation). The ovary then produces progesterone, preventing the release of further eggs and priming the lining of the womb for a possible pregnancy. If pregnancy occurs, progesterone levels in the body remain high, maintaining the womb lining. If pregnancy does not occur, progesterone levels in the body fall, resulting in a menstrual period. Norgestimate tricks the body processes into thinking that ovulation has already occurred, by maintaining high levels of the synthetic progesterone. This prevents the release of eggs from the ovaries.
    Mechanism of action Norgestimate binds to androgen and progestogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Norgestimate will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    GI tract/Hepatic
    Route of elimination Not Available
    Half life 12-30 hours
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 216 °C PhysProp
    logP 4.8 Not Available
    Predicted Properties
    Property Value Source
    water solubility 5.31e-03 g/l ALOGPS
    logP 3.8 ALOGPS
    logP 4.11 ChemAxon
    logS -4.8 ALOGPS
    pKa (strongest acidic) 11.47 ChemAxon
    pKa (strongest basic) 3.11 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 58.89 ChemAxon
    rotatable bond count 3 ChemAxon
    refractivity 105 ChemAxon
    polarizability 42.82 ChemAxon
    药物相互作用
    Drug Interaction
    Artemether Artemether may decrease the effectiveness of norgestimate 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 norgestimate, it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form).
    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.
    Thiopental Thiopental may decrease the effect of Norgestimate. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
    Tretinoin Oral Tretinoin may decrease the effect of oral contraceptive, Norgestimate. An alternate form of contraception should be used during concomitant therapy.
    Warfarin Norgestimate may alter the anticoagulant effect of warfarin. Concomitant therapy should be avoided. Monitor for changes in coagulation status if norgestimate is initiated, discontinued or dose changed.
    食物相互作用
    • Avoid alcohol.
    • Avoid excessive quantities of coffee or tea (Caffeine).
    • Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
    • Take at the same time everyday.
    • Take with food.

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