adrenergic pharm Flashcards

1
Q

adrenergic receptors

A

GPCRs (like muscarinic ACh receptors)

  • alpha1= vasoconstriction
  • alpha2= inhibit NE release at presynaptic nerve endings and ACh release (heteroreceptor mechanism –> acts on vagal fibers in gut to decrease ACh –> gut relaxation)
  • beta1= increased HR and force of contraction
  • beta2= arteriole dilation in skeletal muscles and bronchodilation
  • beta3= lipolyis D1= dilation of renal, mesenteric and cerebral arterioles
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2
Q

termination of transmitter

A

uptake 1: neuronal uptake - high specificity, low capacity

uptake2: non-neuronal cell - low specificity, high capacity –> metabolism via MAO and COMT mainly in liver

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3
Q

alpha-methyltyrosine

A
  • neuron blocking drug
  • inhibits tyrosine hydroxylase activty (rate limiting step in synthesis of NE) –> decreases noradrenergic response
  • used to treat pheochromocytoma
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4
Q

competing alpha1/ beta2 receptors

A

beta2 have lower threshold –> dilation at low(physiologic) concentrations

alpha1 constriction at higher concentration (seen in shock)

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5
Q

norepinephrine

A

alpha1, beta1

used to treat hypotension

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6
Q

epinephrine

A

released by adrenals, not sympathetic nerve endings (neurohormone!)

alpha1, beta1, beta2

used for anaphylactic shock, local anesthetics, glaucoma

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7
Q

isoproterenol

A

non-selective beta1, beta2 agonist

used for bronchodilator/asthma, shock, heart block

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8
Q

tyramine

A
  • indirect agent
  • tyramine found in fermented foods
  • causes release of NE from cytoplasm (not synaptic vesicles) — no Ca2+ necessary
  • tachyphylaxis: acute tolerance when small cytoplasmic pool of NE is rapidly used up after repeated tyramine injections)
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9
Q

dopamine

A

D1, alpha1, beta1

  • direct and indirect-acting
  • low dose: direct action on D1 –> vasodilation of renal, mesenteric and cerebral vessels
  • medium dose: some direct action on beta1 and indirect action/NE release
  • high dose: direct action on alpha1 and indirect action/NE release
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10
Q

Fenoldopam

A

-Dopamine receptor agonist –> activates D1 receptors only (unlike dopamine)

  • used in hypertensive emergencies and to increase renal perfusion
  • short t1/2
  • **fenolDOPam = DOPamine
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11
Q

ergot alkaloids

A
  • alpha agonists
  • vasoconstriction, uterine smooth muscle contraction, delirium and confusion
  • ergonovine: oxytocic, control post-partum bleeding
  • ergotamine: migraine
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12
Q

clonidine and alpha-methyldopa (pro-drug)

A
  • alpha2 agonists
  • central control of bp (act in brain!) –> decrease central sympathetic output
  • used to treat HTN and withdrawal symptoms from opioids, alcohol
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13
Q

dobutamine

A
  • beta1 selective agonist
  • cardiac stimulation
  • used for cardiac decompensation, shock, heart block
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14
Q

terbutaline and albuterol

A
  • Beta2 selective agonists
  • used to treat asthma, COPD
  • side-effects= cardiac arrhythmia via reflexive response to vasodilation and lowered BP
  • “bute”= asthma and B for bute and beta (as opposed to the other COPD and asthma drugs that are antimuscarinics- Ipatropium and Tiotropium)
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15
Q

amphetamine

A
  • indirect-acting release of NE
  • CNS stimulation
  • used to treat ADHD, narcolepsy
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16
Q

propranolol

A
  • non-selective beta blocker (1st generation)
  • treat HTN, angina, arrhythmia
  • can exacerbate asthma (via beta2 effects)

*old war horse

17
Q

metropolol and atenolol

A
  • beta1-selective blockers (2nd generation)
  • treat HTN, angina, arrhythmia, CHF
  • *only use 2nd or 3rd gen beta-blcoers to treat CHF!
18
Q

carvedilol and labetalol

A

non-selective beta blockers (3rd generation A)

  • also block alpha1 (prevent vasoconstriction)
  • treat HTN and CHF
  • “carve a lab”
  • alpha antagonists have weird endings”ilol” or “alol” whereas beta antagonists end in “olol”
19
Q

betaxolol

A
  • beta1-selective blockers (3rd generation B)
  • treat HTN and CHF

** only use 2nd or 3rd generation to treat CHF!

20
Q

alpha blockers

A
  • phentolamine, phenoxybenzamine, prazosin
  • major application is to treat HTN, peripheral vascular disease (Raynaud’s, frostbite), pheochromocytoma (adrenal tumor), shock, BPH (reduce resistance to urine outflow)
  • ** start with “p”
21
Q

phentolamine and phenoxybenzamine

A
  • non-selective alpha antagonist (alpha 1 and 2)
  • phenoxy = nitrogen-must compound –> forms irreversible covalent bond with receptor)
  • blockade of alpha2 receptors –> loss of feedback inhibition –> excess NE release –> tachycardia
  • used to treat pheocromocytoma, raynaud’s, frostbite
  • ** start with “phen”
22
Q

prazosin

A
  • alpha1 selective blocker
  • less tachycardia
  • used to treat primary HTN and BPH
23
Q

ephedrine

A
  • nasal decongestion
  • alpha1 agonist
  • vasoconstriction –> decrease swollen mucosa
24
Q

phenylephrine

A

alpha1 agonist

nasal decongestion