Journal
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY
Volume 18, Issue 2, Pages 135-149Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/17425255.2022.2057297
Keywords
antidepressive agents; antipsychotic agents; cytochrome P-450 enzyme inducers; cytochrome P-450 enzyme inhibitors; drug interactions; haloperidol; blood; haloperidol; pharmacokinetics; haloperidol; therapeutic use; valproate; smoking
Ask authors/readers for more resources
This article systematically reviews the pharmacokinetic drug-drug interactions of oral haloperidol and summarizes recommendations for clinicians based on current knowledge.
Introduction Pharmacokinetic (PK) drug-drug interactions (DDIs) of oral haloperidol, a first-generation antipsychotic, are systematically reviewed. Areas covered After exclusions, the search for DDIs with oral haloperidol provided 47 articles as victim and 7 as perpetrator. Changes in mean haloperidol concentration-to-dose (C/D) ratios after weighting each study's size were used to calculate the effects of other drugs (inhibitors/inducers) on haloperidol. These changes of haloperidol C/D ratio were used to estimate dose-correction factors (1 for inducers). Expert opinion A box summarizes our recommendations for clinicians regarding our current knowledge of haloperidol PK DDIs, which will need to be updated as new information becomes available. Moderate to strong inducers (carbamazepine, phenobarbital, phenytoin, or rifampin) should be avoided since they required dose-correction factors of 2-5. Smoking appeared to be a weak inducer (dose-correction factor 1.2). Fluvoxamine, promethazine, and combinations of CYP3A4 and CYP2D6 inhibitors should be avoided. There are no long-term studies on fluoxetine to provide a dose correction factor. Limited information suggests that valproate may be an inhibitor (dose-correction factor 0.6). In most patients, haloperidol may not have clinically relevant effects as a perpetrator, but in vitro and clinical studies suggest it is a weak CYP2D6 inhibitor.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available