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CPR > Pharmacology: Autonomic Drugs > Flashcards

Pharmacology: Autonomic Drugs Flashcards

1
Q

alpha1

A

G-protein: q
Fcn: ^vascular smooth muscle contraction, ^pupillary dilator muscle contraction (mydriasis), ^intestinal and bladder sphincter muscle contraction

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2
Q

alpha2

A

G-protein: i*inhibitory
Fcn: v-sympathetic (adrenergic) outflow, v-insulin release, v-lipolysis, ^platelet aggregation, v-aqueous humor production

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3
Q

beta1

A

G-protein: s
Fcn: ^HR, ^contractility, ^renin release, ^lipolysis
(#1 in my heart)

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4
Q

beta2

A

G-protein: s
Fcn: vasodilation, bronchodilation, ^lipolysis, ^insulin release, v-uterine tone (tocolysis), ciliary muscle relaxation, ^aqueous humor production

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5
Q

beta3

A

G-protein: s

Fcn: ^lipolysis, ^thermogenesis in skeletal muscle

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6
Q

D1

A

G-protein: s

Fcn: relaxes renal vascular smooth muscle

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7
Q

D2

A

G-protein: i *inhibitory

Fcn: modulates transmitter release, especially in brain

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8
Q

G-protein q

A

Gq –> phospholipase C, which cleaves PIPs –> DAG and IP3. DAG activates PKC. IP3 increases intracellular Ca –> smooth muscle contraction.

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9
Q

G-protein s

A

activates adenylyl cyclase, which causes ATP–>cAMP. cAMP–>PKA–> increases intracellular Ca in heart

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10
Q

G-protein i

A

inhibits adenylyl cyclase; inhibits release of NE and DA

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11
Q

Tyramine

A

Normally degraded by MAO, but if patient on MAO inhibitor, tyramine levels rise (from cheese, wine). Displaces neurotransmitters (NE) from their presynaptic vesicles, meaning there is more NE active –> ^sympathetic stimulation. Classically results in HTN crisis.

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12
Q

Albuterol, salmeterol

A

direct sympathomimetics
b2>b1
Albuterol for acute asthma or COPD
Salmeterol for long-term asthma or COPD control

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13
Q

Dobutamine

A

direct sympathomimetic
b1>b2, a
heart failure (inotropic>chronotropic)
cardiac stress testing

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14
Q

Dopamine (DA)

A

direct sympathomimetic
D1=D2>b>a
unstable bradycardia, heart failure, shock
inotropic and chronotropic effects at lower doses due to b effects; vasoconstriction at high doses due to a effects.

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15
Q

Epinephrine (EPI)

A 
direct sympathomimetic
b>a
anaphylaxis, asthma, open-angle glaucoma
a effects predominate at high doses
significantly stronger effect at b2 receptor than norepinephrine
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16
Q

Fenoldopam

A 
direct sympathomimetic 
D1
postoperative HTN, HTN crisis, vasodilator (coronary, peripheral, renal, and splanchnic)
promotes natriuresis 
can cause hypotension and tachycardia
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17
Q

Isoproterenol

A

direct sympathomimetic
b1=b2
electrophysiological evaluation of tachyarrhythmias
can worsen ischemia
causes b2-mediated vasodilation –> v-MAP and ^HR through b1 and reflex activity

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18
Q

Midodrine

A

direct sympathomimetic
a1
autonomic insufficiency and postural hypotension
may exacerbate supine HTN

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19
Q

Norepinephrine

A

direct sympathomimetic
a1>a2>ba
hypotension, septic shock
a1-mediated vasoconstriction –> ^systolic and diastolic pressures –> ^MAP –> reflex bradycardia

20
Q

Phenylephrine

A

direct sympathomimetic
a1>a2
hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant)

21
Q

Amphetamine

A

indirect general agonist, reuptake inhibitor, releases stored catecholamines (^NE)
use: narcolepsy, obesity, ADHD

22
Q

Cocaine

A

indirect general agonist, reuptake inhibitor
causes vasoconstriction and local anesthesia
never give b-blocker if cocaine intoxication suspected (–> unopposed a1 activation and extreme HTN)

23
Q

Ephedrine

A

indirect general agonist, releases stored catecholamines (^NE)
use: nasal decongestion, urinary incontinence, hypotension

24
Q

Clonidine, guanfacine

A

sympatholytics
a2-agonists
HTN urgency, ADHD, Tourette syndrome
Adverse effects: CNS depression, bradycardia, hypotension, respiratory depression, miosis

25
Q

a-methyldopa

A

sympatholytic
a2-agonist
HTN in pregnancy
Adverse effects: direct Coombs positive hemolysis, SLE-like syndrome

26
Q

Phenoxybenzamine

A

nonselective a-blocker
irreversible
pheochromocytoma (used preoperatively) to prevent catecholamine (HTN) crisis
Adverse effects: orthostatic hypotension, reflex tachycardia

27
Q

Phentolamine

A

nonselective a-blocker
reversible
give to patients on MAO inhibitors who eat tyramine-containing foods
Adverse effects: orthostatic hypotension, reflex tachycardia

28
Q

Prasozin, terazosin, doxazosin, tamsulosin (-osin!)

A 
a1-selective blocker
urinary symptoms of BPH
prazosin - PTSD
HTN (except tamsulosin) 
Adverse effects: 1st-dose orthostatic hypotension, dizziness, headache
29
Q

Mirtazapine

A

a2-selective blocker
depression
Adverse effects: sedation, ^serum cholesterol, ^appetite

30
Q

b-blocker applications and actions

A

Angina pectoris - v HR and contractility, resulting in v O2 consumption
MI - v mortality
SVT - metoprolol, esmolol - v AV conduction velocity
HTN - v CO, v renin secretion (due to b1-receptor blockade on JGA cells)
HF - bisoprolol, carvedilol, metoprolol - v mortality
Glaucoma - timolol - v secretion of aqueous humor
Variceal bleeding - nadolol, propanolol - v hepatic venous pressure gradient and portal HTN

31
Q

b-blocker adverse effects

A

Erectile dysfunction
Cardiovascular - bradycardia, AV block, HF
CNS - seizures, sedation, sleep alterations
Dyslipidemia (metoprolol)
Asthma/COPD exacerbations
Risk of unopposed a-adrenergic receptor agonist activity in cocaine users

32
Q

b1-selective antagonists

A

A-M 1st half alphabet

acebutolol (partial agonist), atenolol, betaxolol, esmolol, metoprolol

33
Q

nonselective b antagonists

A

N-Z 2nd half alphabet

nadolol, pindolol (partial agonist), propranolol, timolol

34
Q

nonselective a and b-antagonists

A

carvedilol, labetalol

35
Q

Nebivolol

A

combines cardiac-selective b1-adrenergic blockade with stimulation of b3-receptors, which activate NO synthase in the vasculature

36
Q

M1

A

Parasympathetic receptor
G-protein q
CNS, enteric nervous system

37
Q

M2

A

Parasympathetic receptor
G-protein i (*inhibitory)
v HR and contractility of atria

38
Q

M3

A

Parasympathetic receptor
G-protein q
^ exocrine gland secretions (lacrimal, sweat, salivary, gastric acid), ^ gut peristalsis, ^ bladder control, bronchoconstriction, ^ pupillary sphincter muscle contraction (miosis), ciliary muscle contraction (accommodation), vasodilation (NO release in vascular smooth muscle endothelial cells)

39
Q

Bethanechol

A

ACh/muscarinic/cholinomimetic agonist
Activates Bowel and Bladder smooth muscle
resistant to AChE
Used: postoperative ileum, neurogenic ileum, urinary retention

40
Q

Carbachol

A

muscarinic and nicotinic agonist
CARBon copy of AcetylCHOLine
Constricts pupil and relieves intraocular pressure in open-angle glaucoma

41
Q

Methacholine

A

muscarinic agonist
Stimulates muscarinic receptors in airway when inhaled
Challenge test for diagnosis of asthma

42
Q

Pilocarpine

A

muscarinic agonist
Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma)
Resistant to AChE
Potent stimulator of sweat, tears, and saliva
Xerostomia (Sjogren Syndrome)

43
Q

Atropine

A

Muscarinic antagonist
Treats bradycardia and ophthalmic applications
Blocks cholinesterase inhibitor poisoning
^pupil dilation, cycloplegia
v airway secretions
v stomach acid secretions
v gut motility
v bladder urgency in cystic
Adverse effects: Hot as hare, dry as bone, red as beet, blind as bat, mad as hatter; constipation, rapid pulse, glaucoma in elderly, urinary retention in men with prostatic hyperplasia, hyperthermia in infants

44
Q

Benztropine

A

Muscarinic antagonist
CNS
Use: Parkinson’s disease, acute dystonia

45
Q

Ipratropium, tiotropium

A

Muscarinic antagonist

Use: COPD, asthma

46
Q

Scopolamine

A

Muscarinic antagonist
CNS
Use: motion sickness

47
Q

Muscarinic agonists

A

v HR (reflex tachycardia due to vBP)
v tone in arterioles and small blood vessels (due to NO release) –> v TPR and v BP
other smooth muscle ^tone and contraction
^salivation and mucous secretions
pupil constriction (miosis)
^ tone GI tract, contractions, peristalsis
bronchoconstriction
v bladder capacity

CPR (8 decks)

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