Drospirenone

• 产品号: DB01395
• CAS号: 67392-87-4
• 分子式: C24H30O3
• 分子量: 366.4932

产品别名

• 标题: Drospirenone
• IUPAC标准名: (1R,2R,4R,10R,11S,14S,15S,16S,18S,19S)-10,14-dimethylspiro[hexacyclo[9.8.0.0^{2,4}.0^{5,10}.0^{14,19}.0^{16,18}]nonadecane-15,2'-oxolan]-5-ene-5',7-dione
• IUPAC传统名: drospirenone
• 别名: Drospirenonum [inn-latin]; DRSP; Drospirenona [inn-spanish]; 6β,7β,15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17 carbolactone

产品登记号

• PubChem CID: 68873
• CAS号: 67392-87-4
• PubChem SID: 46507653

产品详细信息

详细说明 (English)

• Drug Groups: approved
• Description: Drospirenone is a synthetic progestin that is an analog to spironolactone. It is found in a number of birth control formulations. Drospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. As such it has anti-mineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and is not androgenic.
• Indication: For the prevention of pregnancy in women who elect an oral contraceptive.
• Pharmacology: Drospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. As such it has anti-mineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and is not androgenic.
• Affected Organisms: Humans and other mammals
• Biotransformation: Extensively metabolized following oral or intravenous administration. The two major metabolites are inactive and are formed independent of the CYP450 enzyme system. The metabolites are the acid form of drospirenone formed by opening of the lactone ring and the 4,5-dihydro-drospirenone-3-sulfate.
• Absorption: Oral bioavailability is approximately 76%.
• Half Life: 30 hours
• Protein Binding: 97%
• References: Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception. 2000 Jul;62(1):29-38. [Pubmed]
• External Links: Wikipedia

参考文献

• Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception. 2000 Jul;62(1):29-38. Pubmed