Haloperidol kinetics after oral and intravenous doses

Holley, F. O.; Magliozzi, Joseph R.; Stanski, Donald R.; Lombrozo, Leon; Hollister, Leo E.

doi:10.1038/clpt.1983.65

Cited by 66 publications

(27 citation statements)

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“…The clearance and elimination half-life of haloperidol in Chinese schizophrenic patients are similar to those from previous studies (Holley et al 1983). Reduced haloperidol is a more polar molecule, and it would thus be expected that its kinetic profile differs from haloperidol.…”

Section: Discussionsupporting

confidence: 79%

Reversible metabolism of haloperidol and reduced haloperidol in Chinese schizophrenic patients

1990

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Haloperidol disposition has been associated with reversible metabolism: it is reversibly reduced to its metabolite, reduced haloperidol, which has less pharmacologic activity than the parent compound. To characterize the interconversion process, six healthy male schizophrenics were administered a single dose of 10 mg haloperidol or reduced haloperidol in a randomized crossover manner. Using a general pharmacokinetic model for the interconversion process, the clearances of haloperidol and reduced haloperidol are 1.15 +/- 0.32 l/h/kg and 0.76 +/- 54 l/h/kg, respectively. These clearances are similar to that obtained by the usual mammillary model analysis. With a single 10 mg dose administration of either drug, about 23% of the biotransformation of haloperidol involves the reduction pathway. Back conversion from the reduced metabolite to the parent drug through oxidation contributes even less to the total biotransformation of reduced haloperidol. This action of interconversion or saturation under chronic drug administration is unknown. Reversible metabolism of haloperidol could partially account for the wide therapeutic range for haloperidol as reported in the literature.

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Section: Discussionsupporting

confidence: 79%

Reversible metabolism of haloperidol and reduced haloperidol in Chinese schizophrenic patients

1990

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“…First, bioavailability of haloperidol after oral administration is about 65% (Holley et al 1983). Second, haloperidol dissolved in drinking water was taken by animals little by little many times at night-time.…”

Section: Discussionmentioning

confidence: 99%

Chronic treatment with haloperidol diminishes the phencyclidine-induced sensorimotor gating deficit in rats

Pietraszek

Ossowska

1998

Naunyn-Schmiedeberg's Arch Pharmacol

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Prepulse inhibition is a model in which a weak subthreshold stimulus (prepulse), presented to an individual before a strong stimulus (pulse), inhibits a startle response to the latter. A deficit of prepulse inhibition induced by dopaminomimetics and antagonists of NMDA receptors has been suggested as an animal model of the sensorimotor deficit in schizophrenia. The aim of the present study was to examine the effect of chronic treatment with the classic neuroleptic haloperidol on the disruption of prepulse inhibition induced by the uncompetitive antagonist of NMDA receptors phencyclidine (PCP, 5 mg/kg sc). Haloperidol in a dose of 1 mg/kg/day was given to rats in drinking water for 3 months. The PCP-induced reduction in prepulse inhibition was not reversed by short-term (4-day) haloperidol administration. In contrast, long-term treatment with haloperidol (6 weeks or 3 months) diminished the PCP-induced effect. The present study suggests that the improvement in sensorimotor gating in the PCP model in rats by prolonged treatment with haloperidol may reflect its antipsychotic action.

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“…With regard to the haloperidol, recordings began during the probable rising phase of blood levels and before the attainment of peak blood concentration levels [9].…”

Section: Methodsmentioning

confidence: 99%

The effects of levodopa and haloperidol on flash and pattern ERGs and VEPs in normal humans

et al. 1990

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We investigated the effects of single doses of the dopamine agonist levodopa and the dopamine antagonist haloperidol on pattern and flash electroretinograms (ERGs) and visual evoked potentials (VEPs) in normal subjects. A placebo and two treatment regimens were administered in a randomized double-masked design. No significant intertreatment differences in the pattern ERGs and VEPs were noted. Although not statistically significant, a clearly discernible tendency was found for increased flash ERG b-wave amplitudes after levodopa administration compared with placebo. In comparison with placebo and levodopa, haloperidol was associated with significantly prolonged flash ERG b-wave implicit times, including each oscillatory potential, which also showed increased duration, particularly in the O1-O3 interpeak implicit time. The failure of pattern ERGs and VEPs to show changes after haloperidol may have been related to the timing of the recordings, which took place during the presumed phase of rising blood levels and before the flash ERG and VEP recordings. Our findings further demonstrated the reliability of the flash ERG in revealing changes in dopaminergic status in the visual system and suggest that steady-state (flicker) ERGs, cone ERGs, and oscillatory potentials have particular use in this regard.

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Haloperidol kinetics after oral and intravenous doses

Cited by 66 publications

References 0 publications

Reversible metabolism of haloperidol and reduced haloperidol in Chinese schizophrenic patients

Reversible metabolism of haloperidol and reduced haloperidol in Chinese schizophrenic patients

Chronic treatment with haloperidol diminishes the phencyclidine-induced sensorimotor gating deficit in rats

The effects of levodopa and haloperidol on flash and pattern ERGs and VEPs in normal humans

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