fen-TOLE-a-meen

Therapeutic Classification: agents for pheochromocytoma

Pharmacologic Classification: alpha adrenergic blockers

• IV: Control of BP during surgical removal of a pheochromocytoma.

IV, Infiltration:

• Prevention and treatment of dermal necrosis and sloughing following extravasation of norepinephrine, phenylephrine, or dopamine.

Local:

• Reversal of soft-tissue anesthesia (of lip and tongue) resulting from an intraoral submucosal injection of a local anesthetic containing a vasconstrictor.

Unlabeled Use:

• IM, IV: Treatment of hypertension associated with pheochromocytoma or adrenergic (sympathetic) excess, such as administration of phenylephrine, tyramine-containing foods in patients on MAO inhibitor therapy, or clonidine withdrawal.

• Produces incomplete and short-lived blockade of alpha-adrenergic receptors located primarily in smooth muscle and exocrine glands.
• Induces hypotension by direct relaxation of vascular smooth muscle and by alpha blockade.
• Increases blood flow to submucosal tissue through blockade of alpha receptors.

• Reduction of BP in situations in which hypertension is due to adrenergic (sympathetic) excess.
• When infiltrated locally, reverses vasoconstriction caused by norepinephrine or dopamine.
• Reverses local anesthetic effects (restores normal lip and tongue sensation).

Absorption: Well absorbed following IM administration; completely available after local injection.

Distribution: Unknown.

Metabolism/Excretion: 10% excreted unchanged by kidneys.

Half-life: 19 min (IV); 2–3 hr (local injection).

(alpha-adrenergic blockade)

Contraindicated in:

• Hypersensitivity
• Coronary or cerebral arteriosclerosis
• Renal impairment.

Use Cautiously in:

• Peptic ulcer disease
• OB: Lactation: Safety not established
• Pedi: Children <3 yr or <15 kg (Oraverse) (safety and effectiveness not established)
• Geri: More susceptible to hypotensive effects; ↓ dose recommended.

With IV use

CNS: CEREBROVASCULAR SPASM, dizziness, weakness.

EENT: nasal stuffiness.

CV: hypotension, MI, angina, arrhythmias, tachycardia.

GI: abdominal pain, diarrhea, nausea, vomiting, aggravation of peptic ulcer.

Derm: flushing.

Local: injection site pain (local).

Drug-Drug:

• Antagonizes the effects of alpha-adrenergic stimulants.
• May ↓ pressor response to ephedrine or phenylephrine.
• Severe hypotension may occur with concurrent use of epinephrine or methoxamine.
• ↓peripheral vasoconstriction from high doses of dopamine.

Hypertension Associated with Pheochromocytoma — Before/During Surgery

• IV (Adults): 5 mg given 1–2 hr preop, repeated as necessary. May be infused at a rate of 0.5–1 mg/min during surgery.
• IV, IM (Children): 1 mg or 0.1 mg/kg (3 mg/m²) given 1–2 hr preop, repeated IV as necessary during surgery.

Prevention of Dermal Necrosis during Infusion of Norepinephrine, Phenylephrine, or Dopamine

• IV (Adults): Add 10 mg phentolamine to every 1000 mL of fluid containing norepinephrine.

Treatment of Dermal Necrosis Following Extravasation of Norepinephrine, Phenylephrine, or Dopamine

• Infiltrate (Adults): 5–10 mg.
• Infiltrate (Children): 0.1–0.2 mg/kg (up to 10 mg).

Reversal of Intraoral Submucosal Anesthesia Following Dental Procedures (Oraverse)

• Infiltrate or Block Injection (Adults and Children 3 yr and >30 kg): Dose administered is based on number of cartridges of local anesthetic with vasoconstrictor administered: 1/2 cartridge local anesthetic — 0.2 mg phentolamine (1/2 cartridge); 1 cartridge local anesthetic — 0.4 mg phentolamine (1 cartridge); 2 cartridges local anesthetic — 0.8 mg phentolamine (2 cartridges).
• Infiltrate or Block Injection (Children 3 yr and 15–30 kg): Do not exceed dose of 0.2 mg (1/2 cartridge).

(Generic available)

• Powder for injection: 5 mg/vial;
• Injection for local infiltration/block injection: 0.4 mg/cartridge;

• Monitor BP, pulse, and ECG every 2 min until stable during IV administration. If hypotensive crisis occurs, epinephrine is contraindicated and may cause paradoxic further decrease in BP; norepinephrine may be used.

• Patient should remain supine throughout parenteral administration.

IV Administration:

• IV:
  Diluent: Reconstitute each 5 mg with 1 mL of sterile water for injection or 0.9% NaCl. Discard unused solution.Concentration: 5 mg/mL.
• Rate: Inject each 5 mg over 1 min.
• Continuous Infusion: Dilute 5–10 mg in 500 mL of D5W.
• Rate: Titrate infusion rate according to patient response.
  • May also add 10 mg to every 1000 mL of fluid containing norepinephrine for prevention of dermal necrosis and sloughing. Does not affect pressor effect of norepinephrine.
• Y-Site Compatibility:
  • alfentanil
  • amikacin
  • aminophylline
  • amiodarone
  • ascorbic acid
  • atropine
  • aztreonam
  • benztropine
  • bumetanide
  • buprenorphine
  • butorphanol
  • calcium chloride
  • calcium gluconate
  • ceftazidime
  • ceftriaxone
  • chlorpromazine
  • cimetidine
  • cyanocobalamin
  • cyclosporine
  • dactinomycin
  • daptomycin
  • digoxin
  • diltiazem
  • diphenhydramine
  • dobutamine
  • docetaxel
  • dobutamine
  • docetaxel
  • dopamine
  • doxycycline
  • enalaprilat
  • epinephrine
  • epoetin
  • ertapenem
  • erythromycin
  • esmolol
  • etoposide phosphate
  • famotidine
  • fenoldopam
  • fentanyl
  • fluconazole
  • fludarabine
  • folic acid
  • gemcitabine
  • gentamicin
  • glycopyrrolate
  • granisetron
  • heparin
  • hydrocortisone sodium succinate
  • imipenem-cilastatin
  • isoproterenol
  • labetalol
  • lidocaine
  • linezolid
  • lorazepam
  • magnesium sulfate
  • mannitol
  • mechlorethamine
  • meperidine
  • metaraminol
  • methoxamine
  • methyldopa
  • metoclopramide
  • metoprolol
  • metronidazole
  • midazolam
  • minocycline
  • mitoxantrone
  • morphine
  • multivitamin injection
  • nafcillin
  • naloxone
  • nesiritide
  • nitroglycerin
  • nitroprusside
  • norepinephrine
  • octreotide
  • ondansetron
  • oxaliplatin
  • oxytocin
  • paclitaxel
  • palonosetron
  • pantoprazole
  • pemetrexed
  • pentamidine
  • pentazocine
  • phenylephrine
  • phytonadione
  • piperacillin/tazobactam
  • potassium chloride
  • procainamide
  • prochlorperazine
  • promethazine
  • propranolol
  • protamine
  • pyridoxime
  • quinidine
  • ranitidine
  • sodium bicarbonate
  • streptokinase
  • succinylcholine
  • sufentanil
  • tacrolimus
  • teniposide
  • theophylline
  • thiamine
  • thiotepa
  • tirofiban
  • tobramycin
  • tolazoline
  • trimethaphan
  • vancomycin
  • vasopressin
  • verapamil
  • vinorelbine
  • voriconazole
• Y-Site Incompatibility:
  • amphotericin B colloidal
  • cefazolin
  • cefotetan
  • cefoxitin
  • cefuroxime
  • chloramphenicol
  • clindamycin
  • dantrolene
  • dexamethasone
  • diazepam
  • diazoxide
  • furosemide
  • ganciclovir
  • insulin
  • ketorolac
  • moxalactam
  • penicillin G
  • pentobarbital
  • phenobarbital
  • phenytoin
  • trimethoprim/sulfamethoxazole
.
• Infiltration: Dilute 5–10 mg of phentolamine in 10 mL of 0.9% NaCl. For children, use 0.1–0.2 mg/kg up to a maximum of 10 mg. Infiltrate site of extravasation promptly. Must be given within 12 hr of extravasation to be effective.

• Advise patient to change positions slowly to minimize orthostatic hypotension.
• Instruct patient to notify health care professional if chest pain occurs during IV infusion.

• Decrease in BP.
• Prevention of dermal necrosis and sloughing in extravasation of norepinephrine, dopamine, and phenylephrine.
• Restoration of normal lip and tongue sensation following local anesthesia.

Oraverse

Rogitine

• Ineffective tissue perfusion (Indications).
• Risk for injury (Indications).

NDC Code^*

• 0143- West-Ward Pharmaceuticals Corp
  • 0143-9564- Phentolamine Mesylate
    • 0143-9564-01- 1 VIAL in 1 BOX (0143-9564-01) > 1 mL in 1 VIAL

• 0143- West-Ward Pharmaceuticals Corp
  • 0143-9564- Phentolamine Mesylate
    • 0143-9564-10- 10 VIAL in 1 BOX (0143-9564-10) > 1 mL in 1 VIAL

• 0362- Septodont, Inc.
  • 0362-0101- Oraverse
    • 0362-0101-10- 10 CARTRIDGE in 1 CARTON (0362-0101-10) > 1.7 mL in 1 CARTRIDGE

• 51224- TAGI Pharma, Inc.
  • 51224-012- Phentolamine Mesylate
    • 51224-012-10- 10 CARTON in 1 TRAY (51224-012-10) > 1 VIAL in 1 CARTON (51224-012-20) > 1 INJECTION in 1 VIAL

• 68094- Precision Dose Inc.
  • 68094-101- PHENTOLAMINE MESYLATE
    • 68094-101-10- 10 CARTON in 1 TRAY (68094-101-10) > 1 VIAL in 1 CARTON (68094-101-20) > 1 INJECTION in 1 VIAL