Phentolamine

  • Phentolamine is a non-selective alpha-adrenergic antagonist (alpha-blocker) used primarily to manage and treat hypertensive emergencies, particularly those caused by pheochromocytoma.
  • Phentolamine works by blocking alpha-1 and alpha-2 adrenergic receptors, leading to vasodilation, reduced blood pressure, and improved blood flow.

Chemical Structure & Formula:

  • Contains an imidazoline fragment linked to a substituted aromatic moiety (often an indanyl derivative) with a urea or carbamoyl linkage.
  • Approximate Formula: C₁₇H₂₇N₅O₂
  • Chemical Structure of Phentolamine
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Mechanism of Action:

  • Acts as a competitive, nonselective antagonist at both α₁ and α₂ receptors.
  • Blocks the actions of norepinephrine and epinephrine on vascular smooth muscle, leading to vasodilation and blood pressure reduction.
  • Its rapid onset makes it useful in acute settings.

Side Effects of Phentolamine:

  • Marked hypotension
  • Reflex tachycardia
  • Headache
  • Potential arrhythmias due to abrupt vasodilation
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Clinical Uses of Phentolamine:

  • Employed in hypertensive emergencies, particularly in pheochromocytoma, and used in certain diagnostic procedures related to erectile dysfunction

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