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The FDA has approved the use of phentolamine mesylate as the first-ever drug for reversing local anesthesia, the company announced today.
Phentolamine, an alpha-adrenergic blocking agent, does not reverse anesthetics themselves. Instead, it competes with epinephrine for receptors. Epinephrine and neocobefrin are included in most dental anesthetic formulations as vasoconstrictors to keep the anesthetic in the targeting area. If blood vessels dilate, blood can wash the anesthesia away. By blocking the vasoconstrictors, phentolamine accelerates this clearance.
Phentolamine has been used since the 1950s as an antihypertensive in a 5- to 10-mg dose, and can cause fainting and other side effects in these doses. A 1.7-mL cartridge of OraVerse contains only 0.4 mg of phentolamine. Dentists can inject OraVerse as a cartridge in the same manner and in the same site as anesthetics.
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