Overview
11. DESCRIPTION Phentolamine mesylate is phenol,3-[[(4,5-dihydro-1 H -imidazol-2-yl)methyl](4-methyl-phenyl)amino]-,methanesulfonate (salt), a non-specific alpha adrenergic blocker. Phentolamine mesylate USP is a white to off-white, odorless crystalline powder with a molecular weight of 377.46. It is sparingly soluble in water, soluble in alcohol, and slightly soluble in chloroform.
Mechanism of Action
12. CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism by which OraVerse accelerates reversal of soft-tissue anesthesia and the associated functional deficits is not fully understood. Phentolamine mesylate, the active ingredient in OraVerse, produces an alpha-adrenergic block of relatively short duration resulting in vasodilatation when applied to vascular smooth muscle. In an animal model, OraVerse increased local blood flow in submucosal tissue of the dog when given after an intraoral injection of lidocaine 2% with 1:100,000 epinephrine. 12.3 Pharmacokinetics Following OraVerse administration, phentolamine is 100% available from the submucosal injection site and peak concentrations are achieved 10-20 minutes after injection.
Indications
- 1. INDICATONS AND USAGE OraVerse an alpha adrenergic blocker, is indicated for adult and pediatric patients ages 3 years and older for the reversal of soft-tissue anesthesia, i.e., anesthesia of the lip and tongue, and the associated functional deficits resulting from an intraoral submucosal injection of a local anesthetic containing a vasoconstrictor. OraVerse, an alpha adrenergic blocker, is indicated for adult and pediatric patients ages 3 years and older for the reversal of soft-tissue anesthesia, i.e.
Common Doses
- 0.1 mg
- 0.2 mg
- 0.4 mg
- 0.8 mg
Dosage
2. DOSAGE AND ADMINISTRATION Amount of Local Anesthetic Administered Dose of OraVerse 1 / 4 Cartridge 1 / 4 Cartridge (0.1 mg) ½ Cartridge ½ Cartridge (0.2 mg) 1 Cartridge 1 Cartridge (0.4 mg) 2 Cartridges 2 Cartridges (0.8 mg) OraVerse is administered using the same location(s) and same technique(s) (infiltration or block injection) used for the administration of local anesthetic. ( 2.1 ) 2.1 General Dosing information The recommended dose of OraVerse is based on the number of cartridges of local anesthetic with vasoconstrictor administered: Amount of Local Anesthetic Administered Dose of...
Contraindications
- 4. CONTRAINDICATIONS OraVerse is contraindicated in patients with: Hypersensitivity to the active substance or to any ingredients in the formulation OraVerse is contraindicated in patients with: Hypersensitivity to the active substance or to any ingredients in the formulation. ( 4 )
Side Effects
- 6. ADVERSE REACTIONS In clinical trials, the most common adverse reaction with OraVerse that was greater than the control group was injection site pain. The most common adverse reaction with OraVerse (incidence ≥5% and > control) is injection-site pain. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Septodont at 1-888-888-1441 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the...
Interactions
- 7. DRUG INTERACTIONS There are no known drug interactions with OraVerse. 7.1 Lidocaine and Epinephrine When OraVerse was administered as an intraoral submucosal injection 30 minutes after injection of a local anesthetic, 2% lidocaine HCl with 1:100,000 epinephrine, the lidocaine concentration increased immediately after OraVerse intraoral injection. Lidocaine AUC and Cmax values were not affected by administration of OraVerse. OraVerse administration did not affect the PK of epinephrine.