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Non-selective alpha-adrenoceptor antagonist Pregnancy: There is very limited data on the use of phentolamine in pregnant women. Animal studies have shown reproductive toxicity. Phentolamine mesilate is not recommended during pregnancy. Breast-feeding: it is not known whether phentolamine is excreted in human milk; as a precautionary measure, breastfeeding should be discontinued during treatment. Fertility: there are no available data on the effect of phentolamine on fertility in animals or humans.

Phentolamine

Brand names: Rogitine

Phentolamine is a short-acting alpha-adrenoceptor antagonist used to control hypertension in catecholamine excess such as phaeochromocytoma crises and to treat catecholamine extravasation.

Adult dose

Dose: Reversal of paroxysmal hypertension in phaeochromocytoma (hypertensive crisis) - THIS ROUTE/INDICATION ONLY: 2-5 mg phentolamine mesilate intravenously, for hypertensive crises occurring before surgery or during the induction of anaesthesia, intubation, or surgical tumour removal
Route: Intravenous. The SPC's method of administration states only: 'This medicinal product is administered intravenously or intramuscularly.'
Frequency: 'This administration is repeated if necessary, while monitoring blood pressure.' The dosage should be further adjusted based on the clinical condition
Max: No maximum or cumulative ceiling is stated in this SPC for the hypertensive-crisis indication. The quoted per-administration range is 2-5 mg intravenously, repeated if necessary under blood-pressure monitoring. Do not treat the 5 mg diagnostic-test dose below as a ceiling for this indication - it belongs to a different indication
SCOPE - THIS DRAFT COVERS ONE OF THE PAGE'S TWO ROUTES ONLY. The page is titled 'IV (crisis) or local infiltration (extravasation)'. The IV crisis route is sourced above. THE EXTRAVASATION / LOCAL INFILTRATION ROUTE IS NOT COVERED BY THIS SOURCE: this SPC contains no subcutaneous or local-infiltration regimen for extravasation of a vasopressor, and its §4.2 method of administration admits only the intravenous and intramuscular routes. Do not infer an infiltration dose or dilution from the figures above - that regimen needs its own source. DIAGNOSTIC USE IN PHAEOCHROMOCYTOMA (recorded for completeness, a separate indication from the crisis dose): intravenous test - adults 5 mg (0.5 ml), children 1 mg (0.1 ml), injected quickly with blood pressure measured immediately after injection at 30-second intervals for the first 3 minutes and 60-second intervals for the next 7 minutes; intramuscular test - adults 5 mg (0.5 ml), children 3 mg (0.3 ml), with blood pressure measured every 5 minutes for 30-45 minutes. The SPC cautions that 'the diagnostic use of phentolamine mesilate is not the first choice and should only be used if the other specific tests are not available', having 'largely been replaced by the commonly available urinalysis of catecholamines or other biochemical tests'. BETA-BLOCKADE: during surgical tumour removal a hypertensive crisis may occasionally occur even if the patient has received phentolamine as premedication; in such cases beta-blockade may be indicated, using a beta-1-selective beta blocker such as metoprolol administered as a slow IV injection. RENAL IMPAIRMENT: no pharmacokinetic studies have been performed in patients with renal impairment; caution is advised.

Paediatric dose

Route: Intravenous
Frequency: Repeated if necessary, while monitoring blood pressure
Max: Not stated in this SPC for the paediatric hypertensive-crisis dose
FIXED DOSE, NOT WEIGHT-BASED - dosePerKg is deliberately null because this SPC expresses the paediatric figure as a flat milligram dose, not per kilogram. Do not derive a per-kg figure. HYPERTENSIVE CRISIS, verbatim: 'For children over 8 years old, the minimum effective dose is 1 mg. The dosage should be further adjusted based on the clinical condition.' Note this is stated as a MINIMUM EFFECTIVE dose, not a recommended or maximum dose, and the SPC gives no figure at all for children aged 8 years or under for this indication. DIAGNOSTIC TEST DOSES IN CHILDREN (a different indication): intravenous test 1 mg (0.1 ml); intramuscular test 3 mg (0.3 ml).

Dose independently re-sourced from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — clinician-reviewed. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to phentolamine and related compounds
  • Hypersensitivity to sulphites
  • Hypotension
  • Myocardial infarction, history of myocardial infarction, coronary insufficiency, angina, or other evidence of coronary artery disease

Side effects

  • Tachycardia
  • Angina pectoris and arrhythmias
  • Orthostatic hypotension
  • Acute or prolonged hypotensive episodes - myocardial infarction, cerebrovascular spasm and cerebrovascular occlusion may occur
  • Flushing
  • Dizziness
  • Nasal congestion
  • Nausea, vomiting, diarrhoea
  • Asthenia
  • Chest pain
  • Severe hypersensitivity reactions and bronchospasm - rarely, from the sodium metabisulphite content (0.5 mg per 1 ml of solution)

Monitoring

  • Blood pressure should be monitored regularly to ensure that dosage and duration of therapy are carefully adjusted to the patient
  • Monitor for tachycardia and cardiac arrhythmias, which may occur with the use of phentolamine mesilate
  • Be alert to myocardial infarction, cerebrovascular spasm and cerebrovascular occlusion, which have been reported after administration, usually in association with severe hypotensive episodes
  • In overdose (manifesting as a significant drop in blood pressure and tachycardia) treatment should be symptomatic, based on the patient's clinical condition and the physician's judgment
  • Use with caution in patients with gastritis and peptic ulcers, due to the stimulating effect on the gastrointestinal tract including gastric acid secretion
  • Use with caution in renal impairment - no pharmacokinetic studies have been conducted in these patients

Clinical monograph

How it works

It is a competitive, non-selective alpha-1 and alpha-2 adrenoceptor blocker, producing vasodilatation that lowers blood pressure and counteracts the vasoconstriction caused by extravasated sympathomimetics.

Prescribing in practice

  • Because it can cause abrupt hypotension and reflex tachycardia, administer with continuous blood pressure and cardiac monitoring and have measures to manage haemodynamic swings.
  • In phaeochromocytoma it is used for acute hypertensive episodes and to provide alpha-blockade before any beta-blocker is introduced, never beta-blockade first.
  • Local infiltration is used to reverse the dermal ischaemia of noradrenaline or other vasopressor extravasation.

Monitoring

Monitor blood pressure and heart rate closely and continuously during and after intravenous administration.

Counselling the patient

  • Explain that this medicine rapidly lowers a dangerously high blood pressure or relieves a leaked drug at a drip site.
  • Warn the patient they may feel dizzy, flushed or experience a fast heartbeat.
  • Advise the team to be alert for sudden drops in blood pressure.

Evidence & guidelines

Phentolamine is an established agent for catecholamine-mediated hypertension and for treating vasopressor extravasation, as reflected in its SPC and toxicology references.

Reference: Endocrine Society Phaeochromocytoma Guidelines; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.