Alpha blockers and adrenergic blockers Flashcards

1
Q

types of Alpha receptor antagonists

A

Nonselective, a1-selective, a2-selective

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2
Q

Nonselective Alpha blockers

A
  • phenoxybenzamine
  • Phentolamine
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3
Q

Selective alpha 1 blockers

A

More systemic affects:
- Prazosin
- terazosin
- Doxazosin

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4
Q

local side effects of non-selective alpha antagonists

A

Nasal congestion and difficulty in ejaculation

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5
Q

systemic side effects of non-selective alpha antagonists

A
  • reflex tachycardia
  • systemic extracellular fluid retention
  • orthostatic hypotensive symptoms
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6
Q

pharmacokinetics of phenoxybenzamine

A

Long acting irreversible inhibitor of Alpha receptors

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7
Q

Phenoxybenzamine clinical use

A

Main benefit is to treat pheochromocytoma
- treats sweating and hypertension associated with pheochromocytoma

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8
Q

benefit of phenoxybenzamine versus other alpha antagonists

A

blocks both alpha receptors and is a non competitive inhibitor

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9
Q

pharmacokinetics of phentolamine

A

nonselective(reversibly inhibits both alpha receptors)
- short acting

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10
Q

clinical use of phentolamine

A

blocks epi release during adrenal gland removal
- reverses necrosis when missing vein with NE

Historically diagnosis of phenochromocytoma

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11
Q

phentolamine adverse effects

A

gastrointestinal

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12
Q

prazosin clinical use

A

treat mild to moderate hypertension
- also treats Raynaud phenomenon (excessive vasoconstriction) if CCB doesn’t work
- off label PTSD and sleep disruption treatment

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13
Q

why is prazosin not used as a mono therapy

A

the ALLHAT study found that mono therapy did not protect against cardiovascular end points

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14
Q

what is prazosin attractive for

A

male patient with both hypertension and BPH because it treats both at the same time

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15
Q

what is the initial therapy for Raynaud phenomenon

A

calcium channel blockers

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16
Q

prazosin adverse effects

A
  • orthostatic hypotension while standing.
    (dose titration helps)
  • Edema occurs as well
  • tachycardia
17
Q

differences of doxazosin and terazosin with Prazosin

A

Prazosin has a much smaller half life

18
Q

doxazosin and terazosin clinical use

A
  • Similar to Prazosin +
  • treats BPH
  • induces apoptosis in prosthetic smooth muscle cells
19
Q

symptoms of Benign prosthetic hyperplasia (BPH)

A

with BPH the prostate becomes larger which cause obstructive urinary symptoms. Which in turn a person cannot void their bladder. so must go to the bathroom often

20
Q

Benign prosthetic hyperplasia (BPH) long acting alpha-1 antagonists

A

Doxazosin, terazosin, Alfuzosin,

21
Q

skip

A

skip

22
Q

skip

A

skip

23
Q

tamsulosin adverse side effects

A

abnormal ejaculation

24
Q

alfluzosin

A

Demonstrates functional uroselectivity
a1 blocker for BPH

25
Q

centrally acting sympathetic neuronal blockers

A
  1. methyldopa
  2. clonidine
  3. Guanfacine (Intuniv)
26
Q

centrally acting adrenergic neuronal inhibitors function

A

a2- receptor agonists
prominent effects at CNS a2 sites.

27
Q

centrally acting adrenergic neuronal inhibitors act on vasomotor centers

A

Decreases sympathetic outflow to peripheral organs such as heart and kidney
- no reflex mediated only CNS effects

28
Q

Methyldopa mechanism of action

A

prodrug that convert dopa to dopamine to NE to methylnorepinephrine
- decreases renin release, decreased heart rate, and decreased peripheral resistance
- decreases sympathetic nervous system

29
Q

Methyldopa clinical use

A

treats hypertension in pregnancy
- longest clinical data

30
Q

Methyldopa adverse effects

A
  • sedation
  • edema
  • dry mouth
  • autoimmune disorder causes positive Coombs test
  • hemolytic anemia
    -abnormal liver tests
31
Q

Clonidine mechanism of action

A

Decreases sympathetic outflow from CNS

32
Q

Clonidine clinical use

A
  • primary hypertension
  • not for initial treatment
    -oral or transdermal for BP control
  • ADHD
  • Epidural
  • withdrawal
  • menopause
  • lower intraocular pressure
33
Q

Clonidine adverse effects

A
  • Sedation
  • 50% of patients get dry mouth
  • sexual dysfunction
  • rebound hypertension with abrupt stop
34
Q

Guanfacine clinical use

A
  • primary hypertension (not desirable)
  • Primarily ADHD if stimulants don’t work