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Phentolamine

    Brands

    DEA Class;  Rx

    Common Brand Names; Regitine, OraVerse

    • Alpha Blockers, Antihypertensives; 
    • Extravasation Antidotes

    Has positive inotropic and chronotropic effect on the heart

    Blocks alph-adrenergic receptors to briefly antagonize circulating epinephrine and norepinephrine to reduce hypertension caused by alpha effects of the endogenous catecholamines

    Indicated For the treatment of Pheochromocytoma

    Treatment of hypertension during pheochromocytoma surgery

    Epinephrine or norepinephrine extravastation treatment

    Indicated for reversal of soft-tissue anesthesia associated with functional deficits from intraoral local anesthesia containing a vasoconstrictor

    Hypersensitivity; MI or other CAD

    • Nasal congestion (10% )
    • Post-treatment pain (up to 10% )
    • Injection site pain (4% to 6% )
    • Diarrhea (<3% )
    • Cardiac dysrhythmia
    • Chest pain
    • Hypotension
    • Myocardial infarction
    • CVA – cerebrovascular accident due to cerebral artery occlusion

    First dose effect may occur, causing a sudden and drastic fall in blood pressure after administering the first dose.

    Hypotension/syncope with first few doses or with increase in dose; minimize by using small first dose at bedtime

    Increase dose slowly

    Myocardial infarction, cerebrovascular spasm, and cerebrovascular occlusion reported following parenteral administration of phentolamine; these events usually occurred in association with marked hypotensive episodes producing shock-like states

    Tachycardia and cardiac arrhythmias may occur with use of phentolamine or other alpha-adrenergic blocking agents; although such effects are uncommon after administration, clinicians should be alert to signs and symptoms of these events, particularly in patients with a prior history of cardiovascular disease; discontinue if angina occur or worsen

    Pregnancy Category: C

    Lactation: not known if excreted in breast milk; not recommended

    Adults

    Pheochromocytoma

    Diagnosis: 5 mg IV/IM

    Test for pheochromocytoma is positive if decrease SBP >35 mmHg & decrease DBP >25 mmHg

    Pheochromocytoma Surgery Use

    5 mg IV/IM 1-2 hr preoperative, repeat if necessary q2-4hr

    Extravasation Treatment

    Epinephrine or norepinephrine extravastation treatment

    Treatment: 5-10 mg in 10 mL NS local injection within 12 hr

    Prevention: 10 mg for each liter of IV fluids (pressor effect of NE is unaffected)

    Dental Anesthesia Reversal (OraVerse)

    Administer using same locations and techniques (infiltration or block injection) as local anesthetic

    1/2 cartridge local anesthetic: OraVerse 1/2 cartridge (0.2 mg)

    1 cartridge local anesthetic: OraVerse 1 cartridge (0.4 mg)

    2 cartridges local anesthetic: OraVerse 2 cartridges (0.8 mg)

    Hypertensive Crises (Off-label)

    Secondary to catecholamine excess: 5-15 mg IV

    Pediatric

    Pheochromocytoma, Diagnosis

    0.1-0.2 mg/kg IV/IM, OR 1 mg IV OR 3 mg IM 

    Pheochromocytoma Surgery Use

    Treatment of hypertension during surgery

    0.05-0.1 mg/kg/dose OR 1 mg IV/IM 1-2 hr preoperative, repeat q2-4hr until hypertension is controlled; not to exceed 5 mg/dose 

    Dental Anesthesia Reversal (OraVerse)

    <6 years or <15 kg: Safety and efficacy not established

    Dose based on amount of local anesthetic administered

    6-12 years (15-30 kg)

    • For 1/2 cartridge local anesthetic, use OraVerse 1/2 cartridge (0.2 mg)

    6-12 years (>30 kg)

    • 1/2 cartridge local anesthetic: OraVerse 1/2 cartridge (0.2 mg)

    • 1 cartridge local anesthetic: OraVerse 1 cartridge (0.4 mg)

    Other Information

    Extravasation of epinephrine/norepinephrine:0.1-0.2 mg/kg to no more than 10 mg

    Phentolamine mesylate

    powder for injection

    • 5mg

    injectable solution

    • 0.4mg/1.7mL