Sex hormones and modulators
A synthetic nonapeptide analogue of the hypothalamic peptide gonadorelin. It is obtained by chemical synthesis and is available as an acetate. Store in airtight containers at a temperature not exceeding 30°.
Practically insoluble in water sparingly soluble in alcohol and in methyl alcohol soluble in acetone freely soluble in chloroform slightly soluble in ether and in fixed oils. A white to pale yellow crystalline powder. Practically insoluble in water soluble 1 in 40 of alcohol, 1 in 2 of chloroform, and 1 in 200 of ether.
Practically insoluble in water and in hexane sparingly soluble in alcohol and in ethyl acetate soluble in methyl alcohol and in acetone freely soluble in dichloromethane. Store in airtight containers at a temperature of 20° to 25°, excursions permitted between 15° and 30°. As for progestogens in general (see Progesterone).
In a few countries, gonadotrophins derived from cadaver pituitary glands have been used in the treatment of infertility, and a small number of patients are reported to have acquired Creutzfeldt-Jakob disease from such preparations.l However, most countries have preferred to use gonadotrophins derived from urine, and these in their turn are being replaced with recombinant products such preparations appear to carry negligible risk of transmitting prion disease. Follitropins alfa and beta are slowly absorbed after subcutaneous or intramuscular injection, with an absolute bioavailability of about 70 to 80%.
International Nonproprietary Names (INNs) in main languages (French, Latin, and Spanish): Acetato de cetrorelix; Cetrorelix, Acetate de; Cetrorelixi Acetas; D-20761; NS-75A; SB-75 (cetrorelix); SB-075 (cetrorelix). N-Acetyl-3-(2-naphthyl)-D-alanyl-p-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L-tyrosyl-N5-carbamoyl-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaniriamide acetate.
Practically insoluble in water sparingly soluble in dehydrated alcohol freely soluble in acetone very soluble in dichloromethane soluble in methyl alcohol. When given to men cyproterone reduces libido, inhibits spermatogenesis, reduces the volume of ejaculate, and causes infertility.
A purified extract of human postmenopausal urine containing follicle-stimulating hormone (FSH) and lutein-ising hormone (LH) the relative in-vivo activity is expressed as a ratio. Human menopausal gonadotrophins with a ratio of FSH:LH of 1:1 are known as menotrophin (see below). A dry preparation containing glycoprotein gonadotrophins possessing follicle-stimulating and luteinising activities.