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At least 127 records · Page 7Linked to original sources
PubMed1983

Effects of oral contraceptive steroids on acetaminophen metabolism and elimination.

Plasma acetaminophen elimination was examined in women taking low-dose estrogen oral contraceptive (OC) steroids and in age-matched control women. Fractional rates of elimination and fractional clearances were calculated for each of the metabolic pathways, including oxidation, sulfation, and glucuronidation. The cysteine adduct and mercapturic acid derivative of acetaminophen were used as an index of oxidative biotransformation, a potentially toxic route of metabolism for acetaminophen. Plasma acetaminophen clearance rose from 287 +/- 13 ml/min to 470 +/- 51 ml/min in women taking OC steroids, whereas elimination t1/2 decreased from 2.40 +/- 0.14 hr to 1.67 +/- 0.16 hr. The fractional clearance and rate of elimination of acetaminophen by glucuronidation increased in women taking OC steroids, whereas the clearance and elimination by sulfation did not differ significantly from values in control subjects. Fractional clearance of the cysteine adduct also increased significantly, but clearance of acetaminophen mercapturic acid did not change. These data suggest that the increased clearance of acetaminophen from plasma in women taking OC steroids results from increased glucuronidation of the drug, although the mechanism is not known.

Acetaminophen↗
PubMed1984

"The pill" and rheumatoid arthritis: benefits for the future?

The paper firstly reviews the recent epidemiological literature on the apparently protective effect of oral contraceptive use on the onset of rheumatoid arthritis. This epidemiological evidence is then placed in the wider context of both old and recent clinical observations on the influence of pregnancy, the menstrual cycle and exogeneous sex hormones on the course of rheumatoid arthritis. Finally, possible hints for underlying biological mechanisms are discussed.

Arthritis, Rheumatoid↗
PubMed1976

Estrogen-receptor binding: relationship to estrogen-induced responses.

The relationship between nuclear binding of the receptor-estrogen complex (R-E) and estrogenic responses was examined. Nuclear-bound R-E was measured by the [3H] estradiol exchange assay, which permits the quantification of R-E as a function of either endogenous or non labeled estrogen. The quantity of nuclear R-E fluctuated as a function of blood levels of estrogen during the estrous cycle in the rat. This indicates that the accumulation of the R-E complex by the nucleus of uterine cells may be of physiologic significance and under the control of endogenous estrogen.

Animals↗
PubMed1980

Studies on Nonoxynol-9. II. Intravaginal absorption, distribution, metabolism and excretion in rats and rabbits.

Some pharmacological aspects of Igepal CO-630, used by some pharmaceutical companies as the source of nonylphenoxypoly (ethyleneoxy) ethanol (Nonoxynol-9, N-9) in various spermicidal formulations, were studied. It was found that Igepal CO-630 contains at least 13 components, 70% having molecular weights near that of N-9. After intravaginal administration, the detergent is rapidly and quantitatively absorbed through the vaginal wall into the systemic circulation. The rate of vaginal absorption of N-9 depends on the vehicle in which the detergent is carried. Once in the blood, N-9 is excreted by liver-bile-feces and the kidney-urine routes, the first being more effective in rats, the latter in rabbits. Following intravaginal or intraperitoneal injection of radioactive N-9, the highest content of radioactivity was found in the liver and kidney. The detergent was detected in the milk of lactating rats and the serum of their pups within two hours after the intravaginal dose.

Absorption↗
PubMed1983

Mitochondrial respiration inhibitors and human sperm motility: implication in the development of spermicides.

Three inhibitors of the mitochondrial respiratory chain, rotenone, antimycin A, potassium cyanide and the uncoupler of oxidative phosphorylation, 2,4-dinitrophenol, were tested for their sperm immobilizing effects with a trans-membrane migration method. None of these drugs inhibited human sperm motility at the concentrations of 10(-6), 10(-5), 10(-4) and 10(-3) M. The suggestion to develop spermicidal contraceptives from mitochondrial respiration inhibitors could not be substantiated; and the theory that motility inhibiting drugs act primarily on the sperm membrane was reconfirmed.

Antimycin A↗
PubMed1976

Outcome of pregnancy after clomiphene therapy.

Of 159 pregnancies conceived after clomiphene therapy, 141 ended in childbirth, including seven sets of twins. There was a probable increase in the number of infants born with major malformations. These were exclusively to women who had not previously borne a normal infant. The incidence of malformed infants compares well with that published after gonadotropin therapy. The possibly higher incidence of malformations seen after drug-induced ovulation would therefore seem to be due to the underlying subfertility state and thus not a direct drug effect.

Abnormalities, Drug-Induced↗