Self-catalyzed destruction of cytochrome P-450: covalent binding of ethynyl sterols to prosthetic heme.

PR Ortiz de Montellano, KL Kunze… - Proceedings of the …, 1979 - National Acad Sciences
The hepatic pigment accumulated as a consequence of the self-catalyzed destruction of
cytochrome P-450 by norethisterone (17-hydroxy-19-nor-17 alpha-pregn-4-en-20-yn-3-one) …

The presence of dl-, d-and l-norgestrel and their metabolites in the plasma of women

SF Sisenwine, HB Kimmel, AL Liu, HW Ruelius - Contraception, 1975 - Elsevier
Women of childbearing potential were given single 1.5 mg oral doses of 14C-dl-, d-or l-
norgestrel (Ng). Blood specimens were obtained at selected time intervals. Drug related …

Metabolism of 2-3H-and 4-14C-17α-Ethynylestradiol 3-methyl ether (mestranol) by women

JG Williams, KIH Williams - Steroids, 1975 - Elsevier
A mixture of 2-3 H and 4-14 C-mestranol was administered orally to five women and 2-3 H-
mestranol alone to one woman. Reactions involving position 2 were extensive as judged by …

Enantioselectivity in drug metabolism

LK Low, N Castagnoli Jr - Annual reports in medicinal chemistry, 1978 - Elsevier
Publisher Summary This chapter is primarily concerned with the recent reports on substrate
dependent enantioselective metabolism of chiral CNS agents, autonomic, and …

The conversion of d-norgestrel-3-oxime-17-acetate to d-norgestrel in female rhesus monkeys

SF Sisenwine, AL Liu, HB Kimmel, HW Ruelius - Contraception, 1977 - Elsevier
Abstract Single intragastric 0.5 mg/kg doses of 14 Cd-norgestrel-3-oxime-17-acetate were
given to female rhesus monkeys. Rapid absorption was evidenced by peak concentrations …

Structural modifications in contraceptive steroids altering their metabolism and toxicity

HM Bolt - Archives of Toxicology, 1977 - Springer
Norethisterone and, to a lesser extent, d-norgestrel are metabolically activated by rat liver
microsomal enzymes to intermediates which are capable of irreversibly binding to proteins …

The metabolic disposition of norgestrel in female rhesus monkeys.

SF Sisenwine, HB Kimmel, AL Liu… - Drug Metabolism and …, 1979 - ASPET
Following single intragastric doses of d-and dl-[24C] norgestrel (Ng), rhesus monkeys
excreted 29.5+/-2.0 (SE) and 52.6+/-5.4% of the administered radioactivity in urine. Fecal …

The metabolic fate of chlormadinone acetate in the baboon

H Honjo, M Ishihara, Y Osawa, RY Kirdani… - Steroids, 1976 - Elsevier
The metabolic fate of chlormadinone acetate (17α-acetoxy-6-chloro-4, 6-pregnadiene-3, 20-
dione; CAP) was studied in intact and biliary fistula baboons. The steroid was labeled with 3 …

In vitro metabolism of 17α-ethynylsteroids

FS Khan, K Potherby - Journal of Steroid Biochemistry, 1979 - Elsevier
The rates of metabolism of synthetic gestagens derived from 19-nortestosterone by rabbit
liver tissue in vitro were compared. Over a period of 1 h norethisterone was metabolised as …

Interaction of drug metabolism with the other elements of drug safety evaluation

HW Ruelius - Drug Metabolism Reviews, 1975 - Taylor & Francis
The title of this article expresses a position: It implies that drug metabolism is part of drug
safety evaluation. To those in the pharmaceutical industry this may appear quite natural …