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Step 1 > Autonomic Drugs > Flashcards

Autonomic Drugs Flashcards

1
Q

Nicotinic ACh receptors - type of receptor?

A

Ligand-gated Na/K channel

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2
Q

What are the two subtypes of nicotinic ACh receptors and where are they found?

A

Nn - autonomic ganglia, adrenal medulla

Nm - NMJ of skeletal muscle

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3
Q

Muscarinic ACh - type of receptor?

A

G-protein-coupled receptors; usually act through 2nd messengers

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4
Q

Where are muscarinic ACh receptors found?

A

Smooth muscle, gland cells, nerve terminals, cardiac muscle, sweat glands (cholinergic sympathetic)

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5
Q

What receptors do NE bind to? Where are these found?

A

A1, A2, B1 (smooth muscle, gland cells, nerve terminals, cardiac muscle, vessels)

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6
Q

What receptors does EPI bind to? Where are these found?

A

A1, A2, B1, B2 (cardiac muscle, vessels)

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7
Q

List the receptors + the G protein class associated with it. (Use the pneumonic)

A

“after QISSeS, you get a QIQ out of SIQ SQS (super qinky sex)”

A1, A2, B1, B2, B3
M1, M2, M3
D1, D2, H1
H2, V1, V2

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8
Q

What are the effects of binding to Gq receptors?

A

Activates PLC
Lipids -> PIP2; PLC converts this to DAG and IP3
DAG activates PKC; IP3 increases intracellular calcium, which leads to smooth muscle contraction (and further activates PKC)

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9
Q

What are the effects of binding to Gs receptors? Gi?

A

Gs activates AC, which converts ATP to cAMP -> PKA -> increased intracellular calcium in the heart and activation of MLCK in smooth muscle; Gi inhibits this

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10
Q

Function of A1

A

Increases contraction of: vascular smooth muscle, pupillary dilator (mydriasis), intestinal/bladder sphincters

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11
Q

Function of A2

A

Decreases sympathetic outflow, insulin release, lipolysis, aqueous humor production

Increases platelet aggregation

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12
Q

Function of B1

A

Increased HR, contractility, renin release, lipolysis

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13
Q

Function of B2

A

Dilation of vascular smooth muscle, bronchi, ciliary muscle (relaxation)

Increases lipolysis, insulin release, aqueous humor production

Decreases uterine tone

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14
Q

Function of B3

A

Increases lipolysis, thermogenesis in skeletal muscle, bladder relaxation

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15
Q

Function of M1

A

Mediates higher cognitive function

Stimulates enteric nervous sytem

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16
Q

Function of M2

A

Decreases HR/atrial contractility

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17
Q

Function of M3

A

Increases exocrine gland secretions, peristalsis, bladder contraction, bronchoconstriction, pupillary sphincter contraction (miosis), ciliary muscle contraction (accommodation), insulin release

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18
Q

Function of D1

A

Relax renal vascular smooth muscle

Activate direct striatum pathway

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19
Q

Function of D2

A

Modulates transmitter release; inhibits indirect striatum pathway

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20
Q

Function of H1

A

Increase nasal/bronchial mucus production, vascular permeability, contraction of bronchioles, pruritis, pain

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21
Q

Function of H2

A

Increase gastric acid secretion

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22
Q

Function of V1

A

Increase vascular smooth muscle contraction

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23
Q

Function of V2

A

Increase water permeability and reabsorption in collecting tubules of kidneys

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24
Q

List the 4 cholinomimetics - direct agonists.

A
  1. Bethanechol
  2. Carbachol
  3. Methacholine
  4. Pilocarpine
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25
Q

List the 5 (+3) cholinomimetics - indirect agonists (anticholinesterase)

A
  1. Galantamine, donepezil, rivastigmine, tacrine
  2. Edrophonium
  3. Neostigmine
  4. Physostigmine
  5. Pyridostigmine
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26
Q

What is the general AE of any cholinomimetic?

A

May exacerbate COPD, asthma, peptid ulcers

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27
Q

MOA and indications of bethanechol

A

Activates bowel and bladder smooth muscle

Postoperative or neurogenic ileus, urinary retention

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28
Q

MOA and indication of methacholine

A

Bronchoconstriction via stimulation of muscarinic receptors; inhaled to diagnose asthma (challenge test)

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29
Q

Edrophonium- indication?

A

Diagnose myasthenia gravis (historically)

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30
Q

Neostigmine - indication?

A

Postoperative/neurogenic ileus
Urinary retention
Myasthenic gravis
Reversal of NMJ blockade postoperatively

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31
Q

Physostigmine - indication?

A

Anticholinergic toxicity antidote (ie, atropine overdose)?

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32
Q

Pyridostigmine - indication?

A

Myasthenia gravis (long-acting)

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33
Q

List the muscarinic antagonists.

A
  1. Atropine (homatropine, tropicamide)
  2. Benztropine, trihexyphenidyl
  3. Glycopyrrolate
  4. Hyoscyamine/dicyclomine
  5. Ipratropium/tiotropium
  6. Oxybutynin, solifenacin/tolterodine
  7. Scoplamine
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34
Q

Which muscarinic antagonists decrease ACh activity in the CNS primarily?

A
  1. Benztropine/trihexyphenidyl

2. Scopolamine

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35
Q

Which muscarinic antagonists decrease ACh activity in the GI system?

A
  1. Glycopyrrolate (and respiratory)

2. Hyoscyamine, dicyclomine

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36
Q

Which muscarinic antagonists decrease ACh activity in the respiratory system?

A
  1. Glycopyrrolate

2. Ipratropium/tiotropium

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37
Q

Which muscarinic antagonists decrease ACh activity in the GU system?

A

Oxybutynin, solifenacin, tolterodine

38
Q

Indications for atropine?

A

Cholinesterase inhibitor poisoning (too much ACh), bradycardia, ophthalmic uses to produce mydriasis and cycloplegia

39
Q

What are the key AE of atropine?

A

Hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter (increased body temperature, decreased sweating, rapid pulse, dry mouth, dry flushed skin, cycloplegia (paralysis of ciliary muscle), constipation, disorientation

40
Q

What specific AE can atropine have on the elderly, men with prostatic hyperplasia, and hyperthermia in infants?

A

Elderly - acute angle-closure glaucoma (mydriasis)

Men - prostatic hyperplasia

Infants - hyperthermia

41
Q

Indications - glycopyrrolate?

A

Parenteral - reduce airway secretions pre-op

Oral - drooling, peptic ulcer disease

42
Q

Indication - oxybutynin, solifenacin, tolterodine

A

Reduce bladder spasms and urge incontinence by inhibiting M3 receptors on smooth muscle in the bladder (decreases involuntary detrusor contraction)

43
Q

Indication - scopolamine?

A

Motion sickness

44
Q

Sympathomimetic effect of albuterol/salmeterol?

A

B2 > B1

45
Q

Sympathomimetic effect of dobutamine?

A

B1 > B2, A1, A2

Inotropic > chronotropic (contractility increases more than HR)

46
Q

Indication of dobutamine?

A

Heart failure, cardiac stress testing

47
Q

Sympathomimetic effect of dopamine (low dose vs. high dose)?

A

D1 = D2 > B1, B2 > A1, A2
Low - inotropic and chronotropic
High - vasoconstriction

48
Q

Indications of dopamine?

A

Unstable bradycardia, HF, shock

49
Q

Sympathomimetic effect of epinephrine?

A

B1, B2 > A1, A2

50
Q

Which receptor effect predominates at a higher dose of EPI?

A

Alpha

51
Q

Indications of epinephrine?

A

Anaphylaxis, asthma, open-angle glaucoma

52
Q

Sympathomimetic effect of fenoldopam?

A

D1

53
Q

Sympathomimetic (direct) effect of isoproterenol?

A

B1 = B2 (non-selective)

54
Q

Indication of isoproterenol?

A

Electrophysiologic evaluation of tachyarrhythmias (caution, as it can worsen ischemia)

55
Q

Sympathomimetic (direct) effectof midodrine?

A

A1 agonist

56
Q

Indications of midodrine?

A 
Autonomic insufficiency
Postural hypotension (may exacerbate supine HTN)
57
Q

Sympathomimetic (direct) effect of mirabegron?

A

B3

58
Q

Indication of mirabegron?

A

Urge incontinence

59
Q

Sympathomimetic (direct) effect of NE?

A

A1 > A2 > B1

60
Q

Indications of NE?

A

Hypotension, septic shock

61
Q

Sympathomimetic (direct) effect of phenylephrine?

A

A1 > A2

62
Q

List the 3 indirect sympathomimetics.

A
  1. Amphetamine
  2. Cocaine
  3. Ephedrine
63
Q

MOA - amphetamine; what other sympathomimetic has the same MOA?

A

Uses the NE transporter to enter the presynaptic terminal, uses VMAT to enter vesicles, which displaces NE, increasing the [NE] in the terminal, leading to transporter reversal; ultimately increases release and inhibits reuptake

Same as ephedrine

64
Q

Three indications for amphetamines?

A

ADHD
Narcolepsy
Obesity

65
Q

MOA - cocaine?

A

Inhibits reuptake of NE

66
Q

What is strongly contraindicated if cocaine intoxication is suspected and why?

A

Beta-blockers - can lead to unopposed A1 activation and extreme hypertension

67
Q

Indications - ephedrine?

A

Nasal decongestion (pseudoephedrine)
Urinary incontinence
Hypotension

68
Q

MOA - clonidine, guanfacine, alpha-methyldopa

A

A2 agonist (sympatholytic)

69
Q

Indications - clonidine, guanfacine?

A 
Hypertensive urgency (limited situations)
ADHD, Tourette syndrome
70
Q

Indication - alpha-methyldopa?

A

Hypertension in pregnancy

71
Q

Major AE - clonidine, guanfacine?

A

Rebound hypertension with abrupt cessation

CNS depression, bradycardia, hypotension, respiratory depression, miosis

72
Q

What are the two non-selective alpha antagonists? Which is irreversible?

A

Phenoxybenzamine - irreversible

Phentolamine - reversible

73
Q

Indication - phenoxybenzamine?

A

Pre-operatively in pheochromocytoma to prevent catecholamine (hypertensive) crisis

74
Q

Indication - phentolamine?

A

Given to patients on MAOIs who eat tyramine containing food

75
Q

AE - non-selective alpha blockers?

A

Orthostatic hypotension, reflex tachycardia

76
Q

List the 4 alpha-1-selective blockers.

A

Prazosin
Terazosin
Doxazosin
Tamsulosin

77
Q

What are the 3 indications of alpha-1-selective blockers?

A

Urinary symptoms of BPH
PTSD (prazosin)
HTN (except tamsulosin)

78
Q

What AE may occur with the first dose of an A1 selective blocker?

A

Orthostatic hypotension

79
Q

What is the one A2 blocker?

A

Mirtazapine

80
Q

List the 6 beta blockers with B1 selectivity (B1>B2).

A
  1. Acebutolol
  2. Atenolol
  3. Betaxolol
  4. Bisoprolol
  5. Esmolol
  6. Metoprolol

(A-M)

81
Q

List the major indications of beta-blockers.

A
  1. Angina pectoris
  2. MI
  3. SV tachycardia
  4. HTN
  5. Glaucoma
  6. Variceal bleeding
  7. Decrease mortality of heart failure (some)
82
Q

How do beta-blockers address angina pectoris?

A

Decrease HR and contractility, resulting in decreased O2 consumption

83
Q

What is the MOA of beta-blockers in treating HTN?

A

Decreases CO, decreases renin secretion via blockade on JGA cells

84
Q

How do beta-blockers treat variceal bleeding?

A

Decrease hepatic venous pressure gradient and portal hypertension

85
Q

Which three beta-blockers decrease mortality of heart failure?

A

Bisoprolol
Esmolol
Metoprolol

86
Q

List the non-selective beta blockers (4).

A
  1. Nadolol
  2. Pindolol
  3. Propranolol
  4. Timolol
    (N-Z)
87
Q

What is the unique indication/mechanism of propranolol?

A

Inhibits 5’ monodeiodinase in peripheral tissue, reducing the conversion of T4 to T3; treats thyroid storm

88
Q

List the two non-selective alpha and beta blockers.

A

Carvedilol

Labetalol

89
Q

List the two partial beta agonists.

A

Acebutolol

Pindolol

90
Q

List the B1 blocker/B3 agonist.

A

Nebivolol

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