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Pharmacology S1 Exam 2 > Adrenergic Antagonists (8-19/20/21-15) > Flashcards

Adrenergic Antagonists (8-19/20/21-15) Flashcards

1
Q

Propanolol

A
  • Indication: HTN, angina due to atherosclerosis, MI
  • MOA: B1, B2 blocker (non-selective)
  • Toxicity/side-effects: B1/2: bronchospasm (esp in asthmatics), mask hypoglycemia symptoms, increases triglycerides, bradycardia; CNS: insomnia, depression
  • Contraindications: DO NOT GIVE TO ASTHMATICS; sinus bradycardia, heart block, cardiogenic shock

*Drug action: B1: decreases HR and contractility, decreases renin release which leads to decreased vasoconstriction, decreases aqueous humor production (topical); B2: bronchiole constriction (problem in asthma and COPD), inhibits effects of EPI (hyperglycemia, anxiety, sweating) so masks symptoms of hypoglycemia (normally due to EPI release)
Elimination: Liver
*1/2 life: 4 hrs
*Note: Nadolol has longer 1/2 life (20-24hr) so has once-daily dosing advantage over propranolol; timolol given topically in eye for glaucoma

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2
Q

Timolol

A
  • Indication: Glaucoma
  • MOA: B1, B2 blocker (non-selective)
  • Toxicity/side-effects: B1/2: bronchospasm (esp in asthmatics), mask hypoglycemia symptoms, increases triglycerides, bradycardia; CNS: insomnia, depression
  • Contraindications: DO NOT GIVE TO ASTHMATICS; sinus bradycardia, heart block, cardiogenic shock

*Drug action: B1: decreases HR and contractility, decreases renin release which leads to decreased vasoconstriction, decreases aqueous humor production (topical); B2: bronchiole constriction (problem in asthma and COPD), inhibits effects of EPI (hyperglycemia, anxiety, sweating) so masks symptoms of hypoglycemia (normally due to EPI release)
Elimination: Liver
*1/2 life: 4 hrs
*Note: Nadolol has longer 1/2 life (20-24hr) so has once-daily dosing advantage over propranolol; timolol given topically in eye for glaucoma

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3
Q

Nadolol

A
  • Indication: Long-term angina, HTN
  • MOA: B1, B2 blocker (non-selective)
  • Toxicity/side-effects: B1/2: bronchospasm (esp in asthmatics), mask hypoglycemia symptoms, increases triglycerides, bradycardia; CNS: insomnia, depression
  • Contraindications: DO NOT GIVE TO ASTHMATICS; sinus bradycardia, heart block, cardiogenic shock

*Drug action: B1: decreases HR and contractility, decreases renin release which leads to decreased vasoconstriction, decreases aqueous humor production (topical); B2: bronchiole constriction (problem in asthma and COPD), inhibits effects of EPI (hyperglycemia, anxiety, sweating) so masks symptoms of hypoglycemia (normally due to EPI release)
Elimination: Urine
*1/2 life: 20-24 hrs
*Note: Nadolol has longer 1/2 life (20-24hr) so has once-daily dosing advantage over propranolol; timolol given topically in eye for glaucoma

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4
Q

Atenolol

A
  • Indication: HTN, angina, MI
  • MOA: B1 blocker (cardioselective)
  • Toxicity/side-effects: depression, insomnia, HYPOtension, bradycardia
  • Contraindications: heart block, cardiogenic shock

*Drug action: B1: decreases heart rate & contractility, decreases renin release (less vasoconstriction via RAA system); Metoprolol crosses BBB; Atenolol does not (so give to pt with CNS side effects (depression))
Elimination: urine
1/2 life: 6-7 hrs
*Note: All of the B-Blockers are “olol” but the cardioselectives have an E in the name

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5
Q

Metoprolol

A
  • Indication: HTN, long-term angina rx
  • MOA: B1 blocker (cardioselective)
  • Toxicity/side-effects: depression, insomnia, HYPOtension, bradycardia
  • Contraindications: heart block, cardiogenic shock

*Drug action: B1: decreases heart rate & contractility, decreases renin release (less vasoconstriction via RAA system); Metoprolol crosses BBB; Atenolol does not (so give to pt with CNS side effects (depression))
Elimination: liver
1/2 life: 3-7 hrs
*Note: All of the B-Blockers are “olol” but the cardioselectives have an E in the name

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6
Q

Esmolol

A
  • Indication: Supraventricular tachycardia (SVT)
  • MOA: B1 blocker (cardioselective)
  • Toxicity/side-effects: depression, insomnia, HYPOtension, bradycardia
  • Contraindications: heart block, cardiogenic shock

*Drug action: B1: decreases heart rate & contractility, decreases renin release (less vasoconstriction via RAA system)
Elimination: esterases in RBC
*1/2 life: ~9 mins (so IV given for hypertensive crisis, angina, or arrhythmias–when a long acting beta blocker is a bad idea)
*Note: All of the B-Blockers are “olol” but the cardioselectives have an E in the name

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7
Q

Pindolol

A
  • Indication: HTN, esp when due to high sympathetic tone (and in pt who are less tolerant of bradycardia and reduced exercise capacity)
  • MOA: B1, B2 blocker (non-selective; WITH PARTIAL AGONIST ACTIVITY)
  • Toxicity/side-effects: dizziness, depression, insomnia, HYPOtension
  • Contraindications: heart block, cardiogenic shock
  • Drug action: B1: decrease heart rate & contractility, decrease renin release (less vasoconstriction via R-A-A system)
  • Elimination: urine
  • 1/2 life: 3-4 hrs
  • Note: beneficial when SYMPATHETIC activity is high; has less bradycardia due to partial agonist activity
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8
Q

Phenoxybenzamine

A
  • Indication: HTN associated with preoperative pheochromocytoma; dermal necrosis (vasoconstrictor extravasation)
  • MOA: a1, a2 blocker (non-selective; IRREVERSIBLE)
  • Toxicity/side-effects: prolonged HYPOtension, reflex tachycardia, nasal congestion
  • Contraindications: Coronary artery disease

*Drug action: inhibit vasoconstriction (decreases BP), increases inotropy and chronotropy due to blockade of presynaptic A2 (and resulting increase in NE release), unmasks vasodilatory effects of EPI
Elimination: conjugates to receptor
1/2 life: 24 hrs (IV given); long-acting bc IRREVERSIBLE!
*Note: Pheochromocytoma massive NE/EPI release could overcome a reversible block–why you need an irreversible blocker

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9
Q

Phentolamine

A
  • Indication: Test for pheochromocytoma; rx for pheo before surgery; catecholamine extravasation
  • MOA: a1, a2 blocker (non-selective; REVERSIBLE)
  • Toxicity/side-effects: prolonged HYPOtension, reflex tachycardia, nasal congestion
  • Contraindications: pts with poor cardiac blood flow or coronary artery disease (due to reflex tachycardia)

*Drug action: inhibit vasoconstriction (decreases BP), increases inotropy and chronotropy due to blockade of presynaptic A2 (and resulting increase in NE release), unmasks vasodilatory effects of EPI
Elimination: urine
1/2 life: 19 mins (IV given); shorter acting than phenoxy bc REVERSIBLE!
*Note: adding an alpha blocker to EPI can switch the net pressor response to a more B2 mediated depressor response–called an “epinephrine reversal”; don’t see with NE or Phenyleph b/c those don’t do B2

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10
Q

Prazosin

A

Indication: benign prostatic hyperplasia; HTN

  • MOA: a1 blocker (selective)
  • Toxicity/side-effects: orthostatic hypotension (syncopy)
  • Contraindications: ???

*Drug action: inhibits A1 mediated vasoconstriction of vessels (vasodilation, decreases BP), relaxes smooth muscle of prostate to help urinary flow
Elimination: liver
1/2 life: 2.3 hrs (given orally); SLOW onset, LONG duration of action (10 hrs!!); extensive 1st pass metabolism (50% metabolized in liver!!)
*Note: less reflex tachycardia–less cardiac stimulation than non-selective A blockers due to preservation of A2 function

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11
Q

Doxazosin

A

Indication: benign prostatic hyperplasia; HTN

  • MOA: a1 blocker (selective)
  • Toxicity/side-effects: orthostatic hypotension (syncopy)
  • Contraindications: ???

*Drug action: inhibits A1 mediated vasoconstriction of vessels (vasodilation, decreases BP), relaxes smooth muscle of prostate to help urinary flow
Elimination: liver
1/2 life: 22 hrs
*Note: less reflex tachycardia–less cardiac stimulation than non-selective A blockers due to preservation of A2 function

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12
Q

Terazosin

A
  • Indication: benign prostatic hyperplasia; HTN
  • MOA: a1 blocker (selective)
  • Toxicity/side-effects: orthostatic hypotension (syncopy)
  • Contraindications: ???

*Drug action: inhibits A1 mediated vasoconstriction of vessels (vasodilation, decreases BP), relaxes smooth muscle of prostate to help urinary flow
Elimination: urine and fecal
1/2 life: 12 hrs
*Note: less reflex tachycardia–less cardiac stimulation than non-selective A blockers due to preservation of A2 function

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Pharmacology S1 Exam 2 (12 decks)

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