Prazosin (Minipress) (alpha1-Arenoceptor Antagonis); Terazosin (Hytrin) (alpha1-Adrenoceptor Antagonist)
  • Prazosin (Minipress), terazosin (Hytrin), and doxazosin (Cardura) reduce arteriolar resistance and increase venous capacitance as a consequence of alpha1 adrenergic receptor blockade.
    • Normal inhibition of norepinephrine-mediate inhibition through alpha2 receptors remain-- prazosin (Minipress) is a selective postsynaptic alpha1 adrenergic receptor blocker
    • The short-term increase in heart rate and plasma renin levels do not persist although the vasodilation continues.
    • Prazosin (Minipress) monotherapy --less effective than thiazide diuretics
    • Prazosin (Minipress) in combination with other agents: quite effective in young patients with moderately severe hypertension
    • Good patient compliance
  • Cardiovascular Effects: --
    • Prazosin (Minipress) reduces systemic vascular resistance without:
      • causing reflex-mediated tachycardia
      • causing increases in plasma renin {as seen with minoxidil/hydralazine}
        • absence of changes in plasma renin reflect continued alpha2 receptor function which normally inhibits renin release {recall that prazosin is an alpha1 selective antagonist}
    • Prazosin (Minipress) -- greater affinity for venular alpha receptors compared to arteriolar alpha receptors; resultant hemodynamics effect (orthostatic hypotension) --an action more similar to nitroglycerin than hydralazine (Apresoline).
  • Renal blood flow is maintained.
  • Retention of salt and water occurs.
  • Alpha1-adrenergic receptor blockers reduce plasma triglycerides, total and LDL-cholesterol, and increase HDL-cholesterol.
  • Other Therapeutic Uses:
    • Congestive heart failure: valuable for reducing afterload
    • Preoperative preparation of patients with pheochromocytoma
    • Treatment of benign prostatic hypertrophy in older males (drug decreases prostate size)
  • Adverse Effect
    • Inital-dose marked orthostatic hypotension is seen in about 50% of cases-- (sudden syncope; dosage dependence)
    • Fluid retention, vertigo
    • dry mouth, urinary frequency, lethargy, sexual dysfunction, nasal congestion, nightmares
  • Anesthetic Implications:
    • Prazosin (Minipress)-induced alpha1 blockade may cause exaggerated hypotension during epidural anesthesia (alpha receptor--blockade prevents compensatory vasoconstriction)
      • Prazosin (Minipress)-exacerbated hypotension may not be responsive to typical alpha1 adrenergic agonists (e.g. phenylephrine) dosage; epinephrine may be required to increase systemic vascular resistance & BP in this setting
      •  The combination of prazosin (Minipress) and a beta-blocker could result in nearly refractory hypotension during regional anesthesia (diminished response to both b and alpha1 agonists)
Stoelting, R.K., "Antihypertensive Drugs", in Pharmacology and Physiology in Anesthetic Practice, Lippincott-Raven Publishers, 1999, 302-312.