Assessment of the drug metabolism capacity of the liver.

Park, BK

doi:10.1111/j.1365-2125.1982.tb04950.x

Cited by 102 publications

(33 citation statements)

References 193 publications

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“…A number of compounds administered either as a single dose or chronically, (reviewed by Park, 1982) have previously been shown to inhibit antipyrine metabolism in man (as judged by a percentage increase in half-life) to varying extents, e.g. allupurinol (167%, Vesell et al, 1970), aminopyrine (75%, Vesell et al, 1976), cimetidine (35%, Serlin et al, 1979, delta-9-tetrahydrocannabinol (22%, Benowitz & Jones, 1977), oral contraceptive steroids (57%, Homeida et al, 1978), levodopa plus L-a-methyl dopa hydrazine, ( 8% Vesell et al, 1971) metoprolol andpropranolol (21% and64% respectively, Bax et al, 1981).…”

Section: Resultsmentioning

confidence: 99%

Effect of chloroquine and primaquine on antipyrine metabolism.

Back¹,

Purba²,

Park³

et al. 1983

Brit J Clinical Pharma

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1 The effects of two antimalarial drugs, chloroquine and primaquine on antipyrine kinetics and metabolism have been studied in volunteers. 2 Chloroquine (250 mg) given 2 h before antipyrine (600 mg orally) had no effect on salivary kinetics of antipyrine or on the urinary recovery of metabolites. Primaquine (45 mg) given 2 h before antipyrine (300 mg orally), increased antipyrine half-life (calculated from 0-24 h) from 12.7 + 3.2 (mean + s.d.) to 25.3 + 3.9hand decreased clearance from3.01 + 0.67 to 1.32 + 0.321 h-. There was no change in the apparent volume of distribution. Antipyrine half life changed with time in the presence of primaquine and when calculated between 24 and 48 h had returned to control. 3 After primaquine, the metabolic clearance (calculated from 0-24 h) of antipyrine to its three main metabolites, 3-hydroxymethylantipyrine, 4-hydroxyantipyrine and norantipyrine was significantly reduced. There was no selective effect on a particular metabolic pathway.4 There was no change in 6,8-hydroxycortisol excretion (expressed as a ratio of total 17-hydroxycorticosteroids) in the period 0-48 h following primaquine administration. 5 The inhibition of hepatic metabolism by primaquine but not the structurally related chloroquine may be an example of a structure activity phenomenon and could be of clinical significance.

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Section: Resultsmentioning

confidence: 99%

Effect of chloroquine and primaquine on antipyrine metabolism.

Back¹,

Purba²,

Park³

et al. 1983

Brit J Clinical Pharma

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“…Antipyrine (AP) serum clearance (CL) and half-life (t½,) are useful indices of hepatic enzyme activity (Park, 1982;Boobis et al, 1981). Oral AP is rapidly and completely absorbed and the CL of oral and intravenously administered AP is very similar in epileptic patients taking enzymeinducing AEDs (Rimmer et al, 1986).…”

Section: Introductionmentioning

confidence: 99%

Effect of the removal of individual antiepileptic drugs on antipyrine kinetics, in patients taking polytherapy.

Patsalos

Duncan

Shorvon

1988

Brit J Clinical Pharma

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1 Antipyrine (AP) clearance, half-life and volume of distribution were determined in 52 patients, taking one or more antiepileptic drug (AED), before and 4 weeks after the complete removal of phenytoin (PHT, n = 20), carbamazepine (CBZ, n = 15) and sodium valproate (VPA, n = 17). 2 PHT removal was associated with a mean 13% fall in AP clearance and a mean 16% increase in AP half-life, in patients who were also taking CBZ with or without barbiturates. There was no significant difference between patients who did, and did not, take barbiturates, in addition to CBZ. 3 CBZ removal was associated with a mean 45% fall in AP clearance and a mean 69% increase in AP half-life, if there was no inducing AED comedication, but had no effect on AP clearance and half-life if PHT and/or barbiturates were also being taken. 4 Removal of VPA had no effect on AP clearance or half-life. 5 The removal of PHT, CBZ and VPA had no significant effect on AP volume of distribution. 6 PHT appears to be a more powerful inducer of hepatic enzyme activity, as measured by the AP test, than is CBZ.

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“…Therefore, within the limits of the indices used in this study (Park, 1982), there is no evidence that cisapride at a daily dose of 30 mg for 28 days has either an inducing or inhibitory effect on hepatic microsomal enzymes.…”

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confidence: 69%