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Pharmacology > Adrenoceptor anatagonists > Flashcards

Adrenoceptor anatagonists Flashcards

1
Q

List some of the alpha adrenoceptor antagonists

A
  • Prazosin (alpha 1 >>>> alpha 2)
  • Phenoxy-benzamine (alpha 1> alpha 2)
  • Phentolamine (alpha 1 = alpha 2)
  • Yohimbine (alpha 2>alpha1)
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2
Q

describe the general effects of alpha receptor antagonists

A
  • Decrease blood pressure, orthostatic hypotension
  • Tachycardia
  • reverse the pressor effects of alpha and Beta agonists
  • miosis
  • nasal stuffiness
  • decrease resistance to urine flow
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3
Q

describe some general therapeutic uses for alpha receptor antagonists

A
  • PHEOCHROMOCYTOMA
  • hypertensive emregencies
  • chronic hypertension
  • peripheral ascular dsiease
  • urinary obstruction
  • erectile dysfunction
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4
Q

Phenoxybenzamine (dibenzyline)

A

ALPHA RECEPTOR ANTAGONISTS

  • Irreversibly blocks alpha1 and alpha 2
  • EFFECT = lowers blodd pressure but heart rate rises due to baroreflex activation
  • USED TO TREAT PHEOCHROMOCYTOMA or high catecholamine states
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5
Q

PRAZOSIN (minipress)

A

ALPHA RECEPTOR ANTAGONISTS

  • Alpha 1 selective, but not alpha 2
  • EFFECTS: relaxes arterial, venous and prostate smoth muscle

–> LOWERS BLOOD PRESSURE

  • USES: hypertension, benign prostatic hyperplasia

ADVERSE: can cause orthostatic hypotension (first dose)

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6
Q

TAMSULOSIN (flomax)

A

ALPHA RECEPTOR ANTAGONISTS

  • slightly selective for ALPHA 1a

–> EFFECTS: relax prostatic smooth muscles

  • USES: tx for benign prostatic hyperplasia
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7
Q

Yohimbine

A

ALPHA RECEPTOR ANTAGONIST

  • Blocks alpha2 (increases central sympathetic activity and NE release)

–> RAISES BP and HR

  • uses male erectile dysfunction and hypotension
  • ADVERSE EFFECTS: anxiety
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8
Q

LABETALOL

A
  • Beta Adrenoceptor antagonists (mixed alpha/beta antagonist)

  • BLOCKS Beta > alpha 1

–> EFFECTS: LOWERS BP with limited HR increase

  • USES: tx of HYPERTENSION
  • Side effects = less tachycardia
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9
Q

describe the general cardiovasclar effects of BETA RECEPTOR ANTAGONIST

A
  • decrease inotropic, chronotropic –> DECREASE BLOOD PRESSUE in pts with hypertension (NO EFFECT on NORMOTENSIVE patients)
  • decrease myocardial oxygen consumption
  • decrease renin release
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10
Q

describe the general respiratory effects of BETA RECEPTOR ANTAGONISTS

A
  • Beta 2 blockade –> increase airway resistance
  • UNDESIRABLE IN ASTHMA/COPD
  • No Beta blocker is completely free of BETA2-blocking effect
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11
Q

describe the general effects of BETA RECEPTOR ANTAGONISTS on the eye and metabolism

A

-EYE:

–> decrease aqueous humor production –> DECREASE INTRAOCULAR PRESSURE

  • METABOLIC

–> inhibits lipolysis

–> may decrease glucagon release

–> increase VLDL and decrease HDL

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12
Q

describe the uses of beta receptor antagonists

A
  • hypertension
  • ischemic heart disease
  • cardiac arrhythmias
  • heart failure
  • glaucoma
  • hyperthyroidism
  • neurologic diseases
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13
Q

describe the adverse effects of BETA RECEPTOR ANTAGONISTS

A
  • fatigue
  • worsening peripheral vascular disease
  • worsening bronchospasm
  • decreased sexual functions
  • increased incidence of diabetes
  • masking the symptoms of hypoglycemia (blocks all of the normal symptoms of hypoglycemia EXCEPT FOR SWEATING)
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14
Q

List the nonselective Beta receptor antagonists

A
  • Beta 1 = beta 2

  • PROPRANOLOL
  • nadolol

timolol

pindolol (has intrinsic sympathaminmetic activity (ISA)

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15
Q

describe the SELECTIVE Beta receptor antagonists

A
  • BETA 1 >>>> BETA 2

  • atenolol
  • METOPROLOL
  • ESMOLOL
  • BETAXOLOL
  • ACEBUTOLOL - has ISA

(AMEBA)

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16
Q

describe the vasodilatory Beta receptor antagonists

A
  • B1 = B2 > Alpha 2 > alpha 2
  • LABETALOL
17
Q

PROPRANOLOL

A

Beta adrenergic receptor antagonists

  • Block beta 1 and Beta 2
  • EFFECTS: lower HR and BP; REDUCE RENIN
  • USES: Hypertension, angina pectoris, arrhythmias, migraine
18
Q

METOPROLOL

A

Beta adrenergic receptor antagonists

  • Blocks Beta 1 > Beta 2
  • Effects: lower HR and BP; reduce renin

–> safer in asthma

  • USES: angina pectoris, hypertension, arrhythmias
19
Q

Pindolol and acebutolol

A
  • Beta adrenoceptor antagonists

  • Beta 1 and beta 2 WITH ISA
  • EFFECTS: lowers BP modestly; lowers HR
  • USES: hypertension, arrhythmias, migraine
20
Q

Carvedilol (labetalol)

A

Beta-adrenoceptor antagonists

  • BLOCKS Beta > alpha 1
  • EFFECTS: long half-life; lowers BP with limited HR increase
  • USES: Heart failure/ hypertension
21
Q

What are the properties important for choice of Beta blockers

A
  • Cardioselectivity

–> people with COPD or asthma (lose dose of selective)

  • Intrinsic sympathomimetic activity

–> Used when you don’t want to drop the HR but want to reduce blood pressure

  • lipid solubility]

–> If compound is lipid soluble then the plasma conc will be LESS PREDICTABLE.

–> older people may have kidney/liver disease and unable to metabolize the beta blockers as well.

Pharmacology (19 decks)

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