Rogitine


phentolamine mesylate

Rogitine (CA) (UK)

Therapeutic class: Diagnostic agent, antihypertensive agent in pheochromocytoma

Pregnancy risk category C

Action

Competitively blocks postsynaptic (alpha1) and presynaptic (alpha2) adrenergic receptors. Acts on arterial tree and venous bed, reducing total peripheral resistance and lowering venous return to heart.

Availability

Powder for injection: 5 mg

Indications and dosages

➣ To prevent or control hypertensive episodes before or during pheochromocytomectomy

Adults: 5 mg I.V. or I.M. 1 to 2 hours before surgery, then 5 mg I.V. during surgery as indicated

Children: 1 mg I.V. or I.M. 1 to 2 hours before surgery, then 1 mg I.V. during surgery as indicated

➣ To aid pheochromocytoma diagnosis

Adults: 2.5 or 5 mg (in 1 ml of sterile water) by I.V. injection; record blood pressure q 30 seconds for 3 minutes, then q minute for next 7 minutes. Or 5 mg (in 1 ml sterile water) I.M.; record blood pressure q 5 minutes for 30 to 45 minutes.

➣ To prevent or treat dermal necrosis after norepinephrine extravasation

Adults: For prevention, add 10 mg to each liter of I.V. solution containing norepinephrine. For treatment, inject 5 to 10 mg in 10 ml of normal saline solution into extravasated area within 12 hours.

Off-label uses

• Hypertensive crisis caused by MAO inhibitors

• Rebound hypertension caused by withdrawal of clonidine, propranolol, or other antihypertensives

• Erectile dysfunction (given with papaverine)

Contraindications

• Hypersensitivity to drug

• Coronary artery disease

• Myocardial infarction (MI) or history of MI

• Coronary insufficiency

• Angina

Precautions

Use cautiously in:

• patients receiving cardiac glycosides concurrently

• pregnant or breastfeeding patients.

Administration

• Reconstitute powder by diluting with 1 ml of sterile water for injection.

• For pheochromocytoma diagnosis, withhold sedatives, analgesics, and nonessential drugs for 24 to 72 hours before test (until hypertension returns). Keep patient supine until blood pressure stabilizes; then rapidly inject drug I.V. Maximum effect usually occurs within 2 minutes of dosing.

Adverse reactions

CNS: weakness, dizziness

CV: tachycardia, acute and prolonged hypotension, orthostatic hypotension, arrhythmias

EENT: nasal congestion

GI: nausea, vomiting, diarrhea

Skin: flushing

Interactions

Drug-drug. Ephedrine, epinephrine: antagonism of these drugs' effects

Drug-herbs. Ephedra (ma huang): antagonism of vasoconstrictive effects

Patient monitoring

• When using for norepinephrine extravasation, monitor injection site closely and assess blood pressure, heart rate, and respiratory rate.

• For pheochromocytoma diagnosis, monitor blood pressure. In pheochromocytoma, systolic and diastolic pressures drop immediately and steeply. Monitor and record blood pressure immediately after injection, at 30-second intervals for first 3 minutes, and at 1-minute intervals for next 7 minutes. Systolic decrease of 60 mmHg and diastolic decrease of 25 mmHg within 2 minutes after I.V. administration indicates a positive reaction for pheochromocytoma.

Patient teaching

• Explain drug administration procedure.

See Instruct patient to promptly report adverse reactions. Assure him he'll be monitored closely.

• Tell patient to withhold other drugs (especially sedatives and analgesics) for at least 24 hours before pheochromocytoma testing, if appropriate.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and herbs mentioned above.

phentolamine

(fen-tole-a-meen) phentolamine,

Oraverse

(trade name),

Regitine

(trade name),

Rogitine

(trade name)

Classification

Therapeutic: agents pheochromocytoma
Pharmacologic: alpha adrenergic blockers
Pregnancy Category: C

Indications

Intravenous: 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. Intramuscular: Intravenous: 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.

Action

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.

Therapeutic effects

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).

Pharmacokinetics

Absorption: Well absorbed following IM administration; completely available after local injection.Distribution: Unknown.Metabolism and Excretion: 10% excreted unchanged by kidneys.Half-life: 19 min (IV); 2–3 hr (local injection).

Time/action profile (alpha-adrenergic blockade)

ROUTEONSETPEAKDURATION
IMunknown20 min30–45 min
IVimmediate2 min15–30 min
Localrapid10–20 minunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Coronary or cerebral arteriosclerosis;Renal impairment.Use Cautiously in: Peptic ulcer disease; Obstetric / Lactation: Safety not established; Pediatric: Children <6 yr or <15 kg (Oraverse) (safety not established); Geriatric: More susceptible to hypotensive effects; ↓ dose recommended.

Adverse Reactions/Side Effects

With parenteral use

Central nervous system

  • cerebrovascular spasm (life-threatening)
  • dizziness
  • weakness

Ear, Eye, Nose, Throat

  • nasal stuffiness

Cardiovascular

  • hypotension
  • mi (life-threatening)
  • angina (most frequent)
  • arrhythmias (most frequent)
  • tachycardia (most frequent)

Gastrointestinal

  • abdominal pain (most frequent)
  • diarrhea (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • aggravation of peptic ulcer

Dermatologic

  • flushing

Local

  • injection site pain (local)

Interactions

Drug-Drug interaction

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.

Route/Dosage

Hypertension Associated with Pheochromocytoma—Before/During SurgeryIntravenous (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.Intravenous Intramuscular (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 DopamineIntravenous (Adults) Add 10 mg phentolamine to every 1000 mL of fluid containing norepinephrine.Treatment of Dermal Necrosis Following Extravasation of Norepinephrine, Phenylephrine, or DopamineInfiltrate: (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 ≥6 yr and >30 k g) 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 ≥6 yr and 15–30 kg) Do not exceed dose of 0.2 mg (1/2 cartridge).

Availability (generic available)

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

Nursing implications

Nursing assessment

  • 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.

Potential Nursing Diagnoses

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

Implementation

  • Patient should remain supine throughout parenteral administration.
  • Intravenous Administration
  • pH: 4.5–6.5.
  • Intravenous: 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.
  • Syringe Compatibility: papaverine
  • 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, ticarcillin/clavulanate, tirofiban, tobramycin, tolazoline, trimethophan, vancomycin, vasopressin, verapamil, vinorelbine, voriconazole
  • Y-Site Incompatibility: amphotericin B colloidal, cefazolin, cefoperazone, cefotetan, cefoxitin, cefuroxime, chloramphenicol, clindamycin, dantrolene, dexamethasone, diazepam, diazoxide, furosemide, ganciclovir, insulin, ketorolac, moxalactam, penicillin G, pentobarbital, phenobarbital, phenytoin, trimethoprim/sulfamethoxazole
  • Additive Compatibility: dobutamine, norepinephrine
  • 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.

Patient/Family Teaching

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

Evaluation/Desired Outcomes

  • 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.

Rogitine

A brand name for PHENTOLAMINE.