phentolamine (Regitine, OraVerse)
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Introduction
Tradename: Regitine.
Indications
- used in diagnosis of pheochromocytoma & associated hypertension
- prevention of dermal necrosis due to extravasation of vasoconstrictors
- reversal of soft-tissue anesthesia
- erectile dysfunction[4]
Dosage
- pheochromocytoma:
- extravasation:
- 5-10 mg in 10 mL normal saline in & around the site of extravasation
- best if given immediately, but may be effective if given within 12 hours
Injection: 5 mg/mL (1 mL), OraVerse may be different
Pharmacokinetics
- response to IV administration is within 2 minutes
- duration of action 15-30 minutes
elimination via plasma
Adverse effects
- common (> 10%)
- orthostatic hypotension, abdominal pain, nausea, reflex tachycardia, anginal pain, diarrhea
- less common (1-10%)
- weakness, fainting, flushing of face, nasal congestion
- uncommon (< 1%)
- myocardial infarction, severe headache, exacerbation of peptic ulcer
- other
Mechanism of action
- competitively blocks alpha adrenergic receptors
- decreases peripheral resistance
- induces peripheral vasodilation
- stimulates beta adrenergic receptors
- positive inotropic effects
- positive chronotropic effects
- increases cardiac output
- dilates bronchial smooth muscle
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 Deprecated Reference
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=91430
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5775
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4772
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=66147
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4774
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=657359
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=517293