Adrenergic Antagonists Flashcards

1
Q

List the conditions that are most commonly treated with B-blockers. What is the mechanism by which B-blockers produce their beneficial effects?

A
use: HTN, (angina, arrhythmia)
mechanisms
- cardioselective (B1 blockers)
- nonselective (B1 and B2 blockers)
- partial agonists (B1 and B2 agonists)
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2
Q

Identify the 6 beta-adrenergic antagonists and the commonly recognized category of beta-blockers to which they belong.

A

NONSELECTIVE

  • propranolol
  • timolol
  • nadolol

CARDIOSELECTIVE

  • atenolol
  • metoprolol

PARTIAL AGONISTS
- pindolol

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3
Q

Describe how toxic side effects of the beta antagonist drugs differ with their receptor subtype selectivity.

A

NONSELECTIVE

  • bronchospasm
  • symptoms of hypoglycemia
  • raise triglycerides
  • bradycardia

CARDIOSELECTIVE (B1)

  • hypotension
  • bradycardia
  • mild, transient

PARTIAL AGONISTS
- same as non-selective

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4
Q

List the 5 prominent alpha-adrenergic antagonists. Identify the following for each:

  • receptor subtype selectivity
  • conditions they are used for
A

NON-SELECTIVE
- phenoxybenzamine (irreversible)
- phentolamine (reversible)
=> USE: HTN in relation to perioperative tx of pheochromocytoma, dermal necrosis, vasoconstrictor extravasation

A1 SELECTIVE
- prazosin
- doxazosin
- terazosin
=> USE: HTN, benign prostatic hyperplasia
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5
Q

List the most serious side effects produced by selective and non-selective alpha-adrenergic receptor antagonists.

A

NONSELECTIVE: prolonged hypotension, reflex tachycardia

SELECTIVE A1: orthostatic hypotension

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6
Q

Explain why selective alpha-1-adrenergic receptor antagonists are more preferable for use in hypertension than non-selective alpha-adrenergic receptor antagonists.

A

because there is less cardiac stimulation b/c A2 functions are preserved

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7
Q

Describe the following for non-selective beta antagonists:

  • drug names
  • effects
  • use
  • toxicity
  • contraindications
A

NAMES: propranolol, nadolol, timolol

EFFECTS

  • reduced heart rate and contractility
  • reduced renin release
  • reduced vasoconstriction
  • bronchiole constriction in patients with asthma or COPD

USE

  • HTN
  • angina
  • glaucoma
  • heart failure
  • arrhythmia

TOXICITY

  • bronchospasm
  • hypoglycemia
  • increased triglycerides
  • bradycardia

CONTRAINDICATIONS

  • side effects in patients with respiratory diseases
  • asthma
  • sinus bradycardia
  • heart block
  • cardiogenic shock
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8
Q

Describe the following for cardioselective beta antagonists:

  • drug names
  • effects
  • use
  • toxicity
  • contraindications
A

NAME: atenolol, metoprolol, esmolol (reduced respiratory side effects)

EFFECT

  • reduced heart rate and contractility
  • reduced renin release

USE

  • HTN
  • angina
  • arrhythmia (only esmolol; only transient b/c short half-life)

TOXICITY

  • mild, transient
  • hypotension
  • bradycardia

CONTRAINDICATIONS

  • sinus bradycardia
  • heart block
  • cardiogenic shock
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9
Q

Describe the following for partial beta agonists:

  • drug names
  • effects
  • use
  • toxicity
  • contraindications
A

NAME: pindolol

EFFECT

  • reduced heart rate and contractility
  • reduced renin release
  • reduced vasoconstriction
  • bronchiole constriction in patients with asthma or COPD

USE

  • when HTN is due to sympathetic output
  • in those less tolerant of bradycardia
  • in those with less tolerance for exercise

TOXICITY

  • less bradycardic effect
  • bronchospasm
  • hypoglycemia
  • increased triglycerides

CONTRAINDICATION

  • asthma
  • sinus bradycardia
  • heart block
  • cardiogenic shock
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10
Q

If you have a patient with respiratory disease, what beta blocker category would you recommend?

A

cardioselective: atenolol, esmolol, metoprolol

non-selective and partial agonists will still have respiratory issue

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11
Q

If you have a patient that has bradycardia, which beta blocker category would you recommend?

A
  • partial agonists b/c have less bradycardic effect
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12
Q

If you have a patient with high sympathetic output, which beta blocker category would you recommend?

A
  • partial agonists b/c block high output
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13
Q

Describe the following for non-selective alpha antagonists:

  • drug names
  • effects
  • use
  • toxicity
  • contraindications
A

NAMES

  • phenoxybenzamine
  • phentolamine

EFFECTS

  • inhibit vasoconstriction
  • block presynaptic A2 receptor => increased NT release => increased ionotropy and cronotropy => increased CO and contractility
  • vasodilation

USE

  • HTN associated with perioperative pheochromocytoma
  • dermal necrosis
  • vasoconstrictor extravasation

TOXICITY

  • prolonged hypotension
  • reflex tachycardia

CONTRAINDICATIONS
- CAD

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14
Q

Describe the following for selective A1 antagonists:

  • drug names
  • effects
  • use
  • toxicity
  • contraindications
A

NAME

  • prazosin
  • doxazocin
  • terazocin

EFFECTS

  • inhibit vasoconstriction
  • preserves A2 function

USE

  • HTN
  • benign prostatic hyperplasia

TOXICITY
- orthostatic hypOtension
CONTRAINDICATIONS

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