Norgestimate resources


DRUG INFO
Norgestimate

Drug Name: Norgestimate

Indication: For the prevention of pregnancy



Pharmacology: 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.

Drug Category: Contraceptives; ATC:G03AA11

Brand Names/Synonyms: Dexnorgestrel Acetime; Ethinylestradiol and Norgestimate; NORGESTIMATE; Norgestimate; Norgestimate [Usan:Ban:Inn]; Norgestimate and Ethinylestradiol; Norgestimato [Inn-Spanish]; Norgestimatum [Inn-Latin]; Ortho Cyclen-21; Ortho Cyclen-28; Ortho Tri-Cyclen; Ortho-Prefest

Dosage Forms: Tablet

Absorption: Not Available

Interactions: Interactions for Norgestimate: Reduced efficacy and increased incidence of breakthrough bleeding and menstrual irregularities have been associated with concomitant use of rifampin. A similar association, though less marked, has been suggested with barbiturates, phenylbutazone, phenytoin sodium, carbamazepine, griseofulvin, topiramate, and possibly with ampicillin and tetracyclines 72. A possible interaction has been suggested with hormonal contraceptives and the herbal supplement St. John's Wort based on some reports of oral contraceptive users experiencing breakthrough bleeding shortly after starting St. John's Wort. Pregnancies have been reported by users of combined hormonal contraceptives who also used some form of St. John's Wort. Healthcare prescribers are advised to consult the package inserts of medication administered concomitantly with oral contraceptives.



Chemical IUPAC Name: (13-ethyl-17-ethynyl-3-hydroxyimino-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl) acetate

Chemical Formula: C23H31NO3

Half Life: 12-30 hours

Drug Type: Approved Drug

# Accession No: APRD00569

CAS Registry Number: 35189-28-7



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