Reduction in the local tissue toxicity of chlorpromazine by beta-cyclodextrin complexation.
Effect of beta-cyclodextrin (beta-CyD) on the local tissue toxicity of chlorpromazine (CPZ) was investigated following the intramuscular injection to rabbits. From the gross and histological examinations, beta-CyD was found to alleviate the muscular tissue damage produced by CPZ on M. vastus lateralis in rabbits. The protective effect of beta-CyD may be ascribed to the decrease in affinity of CPZ to the tissue membrane through inclusion complexation. The present data suggest that beta-CyD complexation is particularly useful to reduce the local toxicity of phenothiazine neuroleptics without altering the pharmacological efficacy.
D000818:Animals; D002746:Chlorpromazine / Q000008:administration & dosage* / Q000037:antagonists & inhibitors / Q000633:toxicity; D003505:Cyclodextrins / Q000494:pharmacology*; D003912:Dextrins / Q000494:pharmacology*; D007273:Injections, Intramuscular; D008297:Male; D009132:Muscles / Q000187:drug effects* / Q000473:pathology; D011817:Rabbits; D013213:Starch / Q000494:pharmacology*; D047392:beta-Cyclodextrins
D003505:Cyclodextrins; D003912:Dextrins; D047392:beta-Cyclodextrins; D013213:Starch; C031215:betadex; D002746:Chlorpromazine