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Pharm > Adrenergic Blockers > Flashcards

Adrenergic Blockers Flashcards

1
Q

Phenoxybenzamine

A
  1. irreversible alpha blocker; insurmountable blockade, forms covalent bond with receptors
  2. non-selective alpha 1 & 2
  3. only therapeutic drug that has noncompetitive antagonism
  4. graphically will level off (flatten on y axis) rather than move to right on x axis
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2
Q

Reversible alpha blockers

A
  1. Phentolamine (nonselective alpha 1 & alpha 2)
  2. Prazosin (alpha 1 selective)
  3. Terazosin (alpha 1 selective)
  4. Doxazosin (alpha 1 selective)
  5. Tamsulosin (alpha 1 selective)
  6. Yohimbine (alpha 2 selective)
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3
Q

alpha 1 selective blockers

A
  1. Prazosin
  2. Terazosin
  3. Doxazosin
  4. Tamsulosin (specific alpha 1A antagonist)

These are all REVERSIBLE blockers

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4
Q

alpha 2 selective blockers

A

Yohimbine

this is a REVERSIBLE blocker

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5
Q

Irreversible alpha blocker

A

phenoxybenzamine; nonselective

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6
Q

CVS effects of alpha blockers

A
  1. decrease PVR & BP

Convert a pressor response of Epi to a depressor response. Called Epinephrine Reversal

Cause orthostatic hypotension & reflex tachycardia, esp with nonselective blockers due to increase release of NE (due to alpha2 blockade)

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7
Q

adverse effects of alpha blockers

A

Cause orthostatic hypotension & reflex tachycardia, esp with nonselective blockers due to increase release of NE (due to alpha2 blockade)

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8
Q

Effects of alpha blockers on urinary bladder

A
  1. alpha 1 receptors are expressed in base of bladder & prostate & blockade–>decrease resistance to flow or urine–> used to tx urinary symptoms in men with BPH

alpha 1A subtype may be the most important subtype in mediating prostate smooth muscle contraction; Tamsulosin=specific alpha 1A antagonist

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9
Q

specific alpha 1A antagonist

A

Tamsulosin

has greater potency than other alpha 1 blockers bc alpha 1A subtype may be the most important subtype in mediating prostate smooth muscle contraction

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10
Q

alpha blockers used to treat pheochromocytoma

A

phenoxybenzamine & phentolamine

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11
Q

Drugs used to treat hypertension

A

prazosin (selective alpha1 blocker)

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12
Q

patient presents with decreased heart rate, sweating, malignant hypertension

A

Dx: pheochromocytoma

increased epi bc tumor–>

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13
Q

alpha blocker used to treat HTN due to clonidine withdrawal, cheese reaction

A

phentolamine

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14
Q

alpha blocker used to treat peripheral vascular disease & Raynauds

A

Prazosin (selective alpha1 blocker)

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15
Q

What’s causing urinary difficulty in BPH?

A

in BPH activation of alpha1A receptors in bladder trigone, prostate & prostatic urethra increases smooth muscle tone

blockade of these receptors relaxes the structures–> increases urinary flow rate & allows more complete emptying of bladder.

DO NOT REVESE THE HYPERPLASIA, only provide symptomatic relief!!

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16
Q

Toxicity of alpha blockers

A
  1. orthostatic hypertension
  2. reflex tachycardia w nonselective blockers (due to increased NE by alpha2 blockade
    * *tachycardia is less common with alpha1 selective blockers
17
Q
  1. drugs with partial agonist activity or “intrinsic sympathomimetic activity
  2. what is this?
A
  1. pindolol & acebutolol

2. advantage of treating patients with asthma bc the drugs are less likely to cause bronchospasm

18
Q
  1. drugs with local anesthetic activity or ‘membrane stabilizing activity
  2. what is this?
A
  1. propranolol

2. the result of blockade of Na channels & can be demonstrated experimentally; no clinical effect

19
Q

longterm use of an agonist has what effect on receptors

A

down regulation of receptors

20
Q

longterm use of an antagonist has what effect on receptors

A

up regulation of receptors

21
Q

why don’t you abruptly stop beta blockers

A

rebound hypertension

22
Q

B1 blockers safe for asthmatics

A
  1. Betaxolol
  2. Esmolol
  3. Atenolol
  4. Metoprolol

“a BEAM of beta blockers”

23
Q

Why is Timolol the preferred beta blocker to treat glaucoma?

A

when used topically in the eye some beta blockers decrease protective reflexes & increase the risk of corneal ulceration. this is ABSENT in Timolol

24
Q

beta blocker used to treat pheochromocytoma

A

Labetalol

25
Q

side effects of beta blockers

A
  1. bradycardia
  2. bronchospasm*
  3. chronic use assoc w increased lipid levels (LDL & TG)
  4. may mask premonitory symptoms of hypoglycemia (tachycardia, tremor, anxiety)
  5. CNS effects: mild sedation, vivid dreams, rarely depression
26
Q

Why should beta blockers be used cautiously in patients with CHF?

A

because beta blockers depress myocardial contractility & excitability

27
Q

premonitory symptoms of hypoglycemia

A

tachycardia, tremor, anxiety

can be masked by beta blockers

28
Q

Beta blockers used to treat heart failure

A
  1. metoprolol
  2. bisoprolol
  3. carvedilol
29
Q

beta blockers used to treat cardiac arrhythmias & MOA

A

Sotalol works by increasing the AV nodal refractory period

has anti arrhythmic effects involving ion channel blockade in addition to its beta blocking action

30
Q

how do beta blockers treat hypertension

A
  1. decreasing CO

2. decrease renin secretion

31
Q

beta blocker used during surgery as an antiarrhythmic

A

Esmolol; half-life = 10m

32
Q

Acebutolol: 1. selectivity 2. side effects 3. uses

A
  1. beta1 selective
  2. sedation
  3. Tx Angina & HTN
33
Q

atenolol: 1. selectivity 2. side effects 3. uses

A
  1. beta1 selective
  2. increases lipid levels
  3. Tx Angina & HTN
34
Q

Metoprolol: 1. selectivity 2. side effects 3. uses

A
  1. Beta1 selective
  2. sedation & increases lipid levels
  3. Angina, HTN, post-MI, antiarrhythmic
35
Q

Pindolol: 1. selectivity 2. side effects 3. uses

A
  1. beta 1 & 2
  2. partial agonist–>less likely to cause bronchospasm in patients with asthma
  3. HTN, Angina
36
Q

epinephrine reversal

A

alpha blockers convert a pressor response of epinephrine to a depressor response

one of the CVS effects of alpha blockers: they cause a lowering of PVR and BP.

Pharm (32 decks)

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