Clomiphene dihydrogen citrate

• Estrogen Antagonists
• Fertility Agents, Female
• Selective Estrogen Receptor Modulators
• ATC:G03GB02

• Chlomaphene
• Chloramifene
• Chloramiphene
• Cisclomiphene
• Clomid
• Clomid (TN)
• Clomifene citrate
• Clomifene citrate (JP14)
• Clomifeno
• Clomiphene
• Clomiphene B
• Clomiphene Citrate
• Clomiphene citrate (Z,E)
• Clomiphene dihydrogen citrate
• Clomivid
• Clomphid
• Clostilbegyt
• Dyneric
• Genozym
• Ikaclomin
• Milophene
• Omifin
• Racemic clomiphene citrate
• Serophene
• Serophene citrate
• Zuclomiphene citrate

• No information avaliable

C₂₆H₂₈ClNO

http://www.rxlist.com/cgi/generic/clomiph.htm

No information avaliable

405.959 g/mol

No information avaliable

Slightly soluble

Solid

7.496

Capsule; Liquid; Powder; Tablet; Tablet (effervescent)

Used mainly in female infertility due to anovulation (e.g. due to polycystic ovary syndrome). In some countries, it is also registered for use in men.

Clomifene (previously clomiphene) is an orally administered, non steroidal, ovulatory stimulant that acts as a selective estrogen receptor modulator (SERM). Clomifene can lead to multiple ovulation, and hence increasing the risk of twins. In comparison to purified FSH, the rate of ovarian hyperstimulation syndrome is low. There may be an increased risk of ovarian cancer, and weight gain. Clomifene is capable of interacting with estrogen-receptor-containing tissues, including the hypothalamus, pituitary, ovary, endometrium, vagina, and cervix. It may compete with estrogen for estrogen-receptor-binding sites and may delay replenishment of intracellular estrogen receptors. Clomifene initiates a series of endocrine events culminating in a preovulatory gonadotropin surge and subsequent follicular rupture. The first endocrine event in response to a course of clomifene therapy, is an increase in the release of pituitary gonadotropins. This initiates steroidogenesis and folliculogenesis resulting in growth of the ovarian follicle and an increase in the circulating level of estradiol. Following ovulation, plasma progesterone and estradiol rise and fall as they would in a normal ovulatory cycle.

Based on early studies with 14 C-labeled clomifene, the drug was shown to be readily absorbed orally in humans.

The acute oral LD₅₀ of clomifene is 1700 mg/kg in mice and 5750 mg/kg in rats. The toxic dose in humans is not known. Toxic effects accompanying acute overdosage of clomifene have not been reported. Signs and symptoms of overdosage as a result of the use of more than the recommended dose during clomifene therapy include nausea, vomiting, vasomotor flushes, visual blurring, spots or flashes, scotomata, ovarian enlargement with pelvic or abdominal pain.

No information avaliable

Humans and other mammals