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Benzocaine is indicated for local anesthesia in dentistry, minor trauma, and as preparation for infiltrative anesthesia. 4 Benzocaine products are indicated for topical anesthesia in a wide variety of conditions including skin irritation, 13 oral pain, 14 and hemorrhoids. 15
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Benzocaine is indicated for use as a topical anesthetic. 4 It has a duration of action of approximately 10 minutes 9 and a wide therapeutic window. 4 Patients should be counselled regarding the risks of methemoglobinemia. 4 , 5 , 6 , 8
Benzocaine diffuses into nerve cells where it binds to sodium channels, preventing the channels from opening, and blocking the influx of sodium ions. 2 , 3 , 4 Nerve cells unable to allow sodium into cells cannot depolarize and conduct nerve impulses. 3 , 4
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Benzocaine binds to both serum albumin and alpha-1-acid glycoprotein. 7
Benzocaine undergoes ester hydrolysis to form 4-aminobenzoic acid, acetylation to form acetylbenzocaine, or N-hydroxylation to form benzocaine hydroxide.1 4-aminobenzoic acid can be acetylated or acetylbenzocaine can undergo ester hydrolysis to form 4-acetaminobenzoic acid.1
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