Trade Names:OraVerse- Injection, solution 0.4 mg per 1.7 mL supplied in a dental cartridge
Trade Names:Phentolamine Mesylate- Injection, lyophilized powder for solution 5 mgRogitine (Canada)
Produces an alpha-adrenergic block that results in vasodilatation when applied to vascular smooth muscle and positive inotropic and chronotropic effects on cardiac muscle.
T max is 10 to 20 min ( OraVerse ).
Urine (13% as unchanged drug). Half-life is 19 min (IV) and 2 to 3 h ( OraVerse ).
OraVerse C max 3.5-fold higher in children weighing 15 to 30 kg compared with children weighing more than 30 kg. AUC was similar.
Prevention or control of hypertensive episodes in patients with pheochromocytoma (excluding OraVerse ); pharmacologic test for pheochromocytoma (not method of choice) (excluding OraVerse ); prevention and treatment of dermal necrosis and sloughing following IV administration or extravasation of norepinephrine (excluding OraVerse ); reversal of soft-tissue anesthesia (ie, anesthesia of lip and tongue) ( OraVerse only).
Control of hypertensive crises secondary to MAOI sympathomimetic amine interactions or withdrawal of clonidine, propranolol, or other antihypertensives; in conjunction with papaverine as intracavernous injection for impotence.
Hypersensitivity to phentolamine or related compounds; MI, history of MI, coronary insufficiency, angina, or other evidence suggestive of coronary artery disease.
IM / IV 5 mg.Children
IM/IV 1 mg IV or 3 mg IM.Hypertensive Episodes in PheochromocytomaAdults
IM / IV 5 mg 1 to 2 h before surgery. Repeat if necessary. During surgery, IV 5 mg as indicated.Children
IM / IV 1 mg 1 to 2 h before surgery. Repeat if necessary. During surgery, IV 1 mg as indicated.Prevention of Dermal Necrosis and SloughingAdults
IV Add 10 mg/L of solution containing norepinephrine.Treatment of Dermal Necrosis or Sloughing After Norepinephrine ExtravasationAdults
5 to 10 mg in 10 mL of saline solution in area of extravasation within 12 h.Reversal of Soft-Tissue Anesthesia ( OraVerse only)Adults Intraoral submucosal injection
Based on the amount of local anesthetic administered. One-half cartridge local anesthetic, 0.2 mg (½ cartridge). One cartridge local anesthetic 0.4 mg (1 cartridge). Two cartridges local anesthetic, 0.8 mg (2 cartridges).Children 6 yr of age and older (30 kg or more) Intraoral submucosal injection
See Adults for dosing; do not exceed 0.4 mg (1 cartridge).Children 6 yr of age and older (15 to 30 kg) Intraoral submucosal injection
Max dose is 0.2 mg (½ cartridge).
Store unopened vials between 59° and 86°F. Protect OraVerse from direct heat and light. Do not allow to freeze.
Withhold prior to test for diagnostic of pheochromocytoma; do not perform this test on normotensive patients.Epinephrine, ephedrine
Vasoconstrictive and hypertensive effects of epinephrine and ephedrine are antagonized by phentolamine.
None well documented.
Tachycardia (6%); bradycardia (4%); acute and prolonged hypotensive episodes, cardiac arrhythmias, orthostatic hypotension (postmarketing).
Oral pain (less than 10%) ( OraVerse ).
Postprocedural pain (10%) ( OraVerse ); injection-site pain (6%) ( OraVerse ).
Category C .
OraVerse is not recommended for use in children younger than 6 yr of age or weighing less than 15 kg. Phentolamine injection IM or IV is recommended for children. See Administration and Dosage.
Marked hypotensive episodes and shock-like states may follow use of phentolamine and may lead to MI, cerebrovascular spasm, or cerebrovascular occlusion. Tachycardia and cardiac arrythmias may also occur.
Urinary assays of catecholamines or other biochemical assays have largely supplanted phentolamine and other pharmacologic tests for pheochromocytoma. Phentolamine is usually used as confirmation. Follow specific guidelines for use of phentolamine.
Diarrhea, excitation, headache, hypoglycemia, nausea, pupillary contraction, severe hypotension, shock, sweating, tachycardia, visual disturbances, vomiting.
Copyright © 2009 Wolters Kluwer Health.