Sympathomimetic drugs Flashcards

1
Q

Midodrine

(Phenylephrine)

A
  • α1 agonist
  • MOA
  • activates phospholipase C→increased intracellular Ca and vasoconstriction
  • Effects
  • vascular smooth muscle contraction increasing BP
  • Clinical
  • orthostatic hypotension
  • Kinetics, tox, int.
  • oral prodrug converted to active drug with 1-h peak effect
  • tox: supine hypertension, piloerection (goose bumps), urinary retention
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2
Q

Clonidine
(α-methyldopa, guanfacine, guanabenz)
(dexomedetomidine, tizanidine, apraclonidine & brimonidine)

A
  • α2 agonist
  • MOA
  • inhibits adenylyl cyclase and interacts with other intracellular pathways
  • Effects
  • vasoconstriction is masked by central sympatholytic effect, which lowers BP
  • Clinical
  • hypertension
  • Kinetics, tox, int.
  • oral, transdermal
  • peak effect 1-3h, t1/2 of oral drug approx 12h
  • xerostomia, sedation
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3
Q

Dobutamine

A
  • β1 agonist (and other actions)
  • MOA
  • activates adenylyl cyclase increasing myocardial contractility
  • Effects
  • positive inotropic effect
  • Clinical
  • cardiogenic shock, acute heart failure
  • Kinetics, tox, int.
  • IV, requires titration to desired effect
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4
Q

Albuterol

A
  • β2 agonist
  • MOA
  • activates adenylyl cyclase
  • Effect
  • bronchial smooth muscle dilation
  • Clinical
  • asthma
  • Kinetics, tox, int.
  • inhalation
  • duration 4-6h
  • tox: tremor, tachycardia
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5
Q

Mirabegron

A
  • β3 agonist
  • MOA
  • activates adenylyl cyclase
  • Effects
  • reduces bladder tone
  • Clinical
  • urinary urgency
  • Kinetics, tox, int.
  • oral
  • duration 50h
  • tox: possible hypertension
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6
Q

Fenoldopam

A
  • D1 agonist
  • MOA
  • activates adenylyl cyclase
  • Effects
  • vascular smooth muscle relaxation
  • Clinical
  • hypertension
  • Kinetics, tox, int.
  • requires dose titration
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7
Q

Bromocriptine

A
  • D2 agonist
  • MOA
  • inhibits adenylyl cyclase and interacts with other intracellular pathways
  • Effects
  • mimics dopamine actions in CNS
  • Clinical
  • Parkinson’s
  • prolactinemia
  • Kinetics, tox, int.
  • oral
  • tox: nausea, headache, orthostatic hypotension
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