Metabolism of benzocaine during percutaneous absorption in the hairless guinea pig: Acetylbenzocaine formation and activity

Skin Pharmacology and Physiology

Volumn 9, Issue 3, 1996, Pages 221-230

  Kraeling, Margaret E K ^a   Lipicky, Raymond J ^a   Bronaugh, Robert L ^a  

^a CENTER FOR DRUG EVALUATION AND RESEARCH   (United States)

Author keywords

Benzocaine; Hairless guinea pig; Metabolism; Percutaneous absorption

Indexed keywords

ACYLTRANSFERASE; BENZOCAINE;

ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG ACETYLATION; DRUG METABOLISM; ENZYME INHIBITION; FEMALE; GUINEA PIG; NONHUMAN; PRIORITY JOURNAL; SKIN ABSORPTION; SKIN CELL;

ACETYLATION; ANESTHETICS, LOCAL; ANIMALS; BENZOCAINE; DECAPODIFORMES; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTRIC CONDUCTIVITY; FEMALE; GUINEA PIGS; NERVE FIBERS; PATCH-CLAMP TECHNIQUES; POTASSIUM CHANNELS; SKIN; SKIN ABSORPTION; SODIUM CHANNELS;

EID: 0029874101     PISSN: 16605527     EISSN: 16605535     Source Type: Journal    
DOI: 10.1159/000211419     Document Type: Article

References (12)

1. Kao J, Carver MP: Skin metabolism; in Marzulli FN, Maibach HI (eds): Dermatotoxicology, ed 4. New York, Hemisphere Publishing, 1991, pp 143-200.
2. Kawakubo Y, Manabe S, Yamazoc Y, Nishikawa T, Kato R: Properties of cutaneous acetyltransfcrasc catalyzing N- and O-acetylation of carcinogenic arylamines and N-hydroxyl-amine. Biochem Pharmacol 1988; 37:265-270.
3. Kawakubo Y, Yamazoe Y, Kato R, Nishikawa T: High capacity of human skin for N-acetylation of arylamines. Skin Pharmacol 1990;3: 180-185.
4. Nathan D, Sakr A, Lichtin JL, Bronaugh RL: In vitro skin absorption and metabolism of benzoic acid, p-aminobenzoic acid, and benzocaine in the hairless guinea pig. Pharm Res 1990;7:1147-1151.
5. Vogel AI: A Text Book of Practical Organic Chemistry Including Qualitative Organic Analysis, ed 3. London. Longman Group. 1972.
6. Bronaugh RL, Stewart RF: Methods for in vitro percutaneous absorption studies. IV. The flow-through cell. J Pharm Sei 1985;74:64-67.
7. Collier SW, Sheikh NM, Sakr A, Lichtin JL, Stewart RF. Bronaugh RL: Maintenance of skin viability during in vitro percutaneous absorption/metabolism studies. Toxicol Appl Pharmacol 1989;99:522-533.
8. Lipicky RJ, Gilbert DL, Ehrcnstcin G: Effects of yohimbine on squid axons. BiophysJ 1978;24:405-422.
9. Elliott JR, Haydon DA, Hendry BM: Local anaesthetic effects of benzene and structurally related molecules, including bcnzocainc, on the squid giant axon. Pflügers Arch 1987;409:589-595.
10. Elliott JR, Haydon DA, Hendry BM: The mechanisms of sodium current inhibition by benzocaine in the squid giant axon. Pflügers Arch 1987;409:596-600.
11. Altman RS, Smith-Coggins R, Ampel LL: Local anesthetics. Ann EmergMed 1985;14:1209-1217.
12. Neal RA: Metabolism of toxic substances; in Doull J, Klaassen CD, Amdur MO (eds): Casarett and Doull’s Toxicology, the Basic Science of Poisons, ed 2. New York, Macmillan Publishing, 1980, pp 56-69