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Step 1 Andre > Pharmacology - Autonomic drugs > Flashcards

Pharmacology - Autonomic drugs Flashcards

1
Q

Cholinomimetics (4)

A
  1. Bethane.chol
  2. Carba.chol
  3. Pilo.car.pine
  4. Metha.choline
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2
Q

GPCR’s

- list them, and which G-protein

A 
Adrenergics: QISS
Muscarinics: QIQ
Dopamine: SI
Histamine: QS
Vasopressin: QS
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3
Q

actions of alpha-1

A
  • vascular smooth muscle contraction
  • pupillary dilator muscle contraction (mydriasis)
  • intestinal and bladder sphincted muscle

Gq, so muscle contractions

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4
Q

actions of alpha-2

A
  • decrease sympathetic outflow
  • decrease insulin release
  • decrease lipolysis
  • decrease blood flood 2/2 plt aggregation

Gi, so decreases stuff

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5
Q

actions of beta-1

A
  • increase HR and contractility
  • increases renin
  • increase lipolysis

Gs, so increase stuff

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6
Q

actions of beta-2

A
  • increase HR and contractility
  • increase blood flow (vasodilation)
  • increase breathing (bronchodilation)
  • increase lipolysis
  • increase insulin release
  • increase aqueous humor production
  • increase intraocular pressure (relaxing ciliary muscle)
  • decrease uterine tone

Gs, so increases stuff … beta-2, so more than beta-1

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7
Q

actions of M1

A

CNS and enteric NS

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8
Q

actions of M2

A
  • decrease HR
  • decrease atrial contractility

anti-beta-2
Gi, so decrease stuff

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9
Q

actions of M3

A
  • exocrine gland muscle contraction –> secretions
  • intestinal muscle contraction –> peristalsis
  • bladder muscle contraction
  • broncho muscle contraction (broncoconstriction)
  • pupillary sphincter muscle contraction (miosis)
  • ciliary muscle contration (accomodation and decreases IOP by allowing humor flow)

Gq, so contraction stuff

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10
Q

actions of D1

A

relaxes renal vascular smooth muscle

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11
Q

actions of D2

A

modulates NT release, esp brain

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12
Q

actions of H1

A
  • nasal and bronchial mucus production
  • increase vascular permeability
  • bronchoconstriction
  • pruritis
  • pain

Gq, so contraction stuff

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13
Q

actions of H2

A
  • increases gastric acid secretion by parietal cells

Gs, so increases stuff

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14
Q

actions of V1

A

increase vascular smooth muscle contraction

Gq, so muscle contraction

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15
Q

actions of V2

A

increase water permeability and reabsorption at collecting tubules

Gs, so increases stuff (v2, b/c 2 kidneys)

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16
Q

choline transporter inhibitor

A

Hemicholinium

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17
Q

Ach vescile loading inhibitor

A

Ves.ami.col

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18
Q

Ach release inhibitor

A

botilinum

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19
Q

Tyrosine hydroxylase inhibitor

A

Metyrosine

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20
Q

Dopamine vesicle loading inhibitor

A

Reserpine

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21
Q

vesicular NE release inhibitor

A

Bretylium

Guanethidine

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22
Q

vesicular NE release stimulator

A

amphetamine

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23
Q

Direct agonist Cholinomimetic agents (4)

A
  1. Bethane.chol
  2. Carb.a.chol
  3. Pilo.car.pine
  4. Metha.choline
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24
Q

Cholinomimetic agents (4)

A
  1. Bethane.chol
  2. Carb.a.chol
  3. Pilo.car.pine
  4. Metha.choline
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25
Q

Carb.a.chol

  • action
  • clinical application
A
  • Carbon copy of Ach
  • Glaucoma, pupillary constriction, relief of IOP

via M3

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26
Q

Pilocarpine

  • action
  • clinical application
A
  • contracts ciliary muscle (allows flow of humor), contracts pupillary sphincter (miosis), stimulates glands (sweat, tears, saliva)
  • open and close angle glaucoma; used to dx CF

via M3

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27
Q

Metha.choline

  • action
  • clinical application
A
  • stimulates muscarinic receptors in airway when inhaled

- constricts bronchioles… used as the challenge test for asthma

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28
Q

Metha.choline

  • action
  • clinical application
A
  • stimulates muscarinic receptors in airway when inhaled

- constricts bronchioles… used as the challenge test for asthma

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29
Q

Indirect agonist Cholinomimetic drugs (via AchE inhibition) (5 of them)

A
  1. Neo.stig.mine
  2. Pryido.stig.mine
  3. Physo.stig.mine
  4. Donepezil, Riva.stig.mine, Galantamine
  5. Edrophonium
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30
Q

Neo.stig.mine

  • action
  • clinical application
A
  • increases endogenous Ach; NO cross BBB

- post-op and neurogenic ileus, urinary retention, myasthenia gravis, reversal or NMJ blockade (post-op)

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31
Q

Pyrido.stig.mine

  • action
  • clinical application
A
  • increase endogenous Ach; NO cross BBB

- long acting Myasthenia Gravis relief of weakness

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32
Q

Physo.stig.mine

  • action
  • clinical application
A
  • increases engodenous Ach; CAN cross BBB

- fixes anticholinergic toxicity b/c can cross BBB (e.g. atropine overdose)

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33
Q

Donepezil

  • action
  • clinical application
A
  • increases endogenous Ach

- Alzheimers

34
Q

Edrophonium

  • action
  • clinical application
A
  • increases endogenous Ach

- extremely short-acting relief of Myasthenia Gravis (historically used to dx it)

35
Q

Cholinesterase Inhibitor poisoning leads to:

A

DUMBBELSS
- Diarrhea/Diaphoresis, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of CNS and skeletal muscle/Emesis, Lacrimation, Sweating, Salivation

CNS excitation is by nAchR

36
Q

Cholinesterase Inhibitor poisoning leads to:

A

DUMBBELSS

- Diarrhea/Diaphoresis, Urination, Miosis, Bronchospasm, Bradycardia, Emesis, Lacrimation, Sweating, Salivation

37
Q

antidote for cholinesterase inhibitor poisoning?

A

Atropine (comp inhibitor) + Pralidoxine (releases AchE is given early)

38
Q

antidote for cholinesterase inhibitor poisoning?

A

Atropine (comp inhibitor) + Pralidoxine (releases AchE is given early)

39
Q

Muscarinic antagonists used on eye (3)

- what action

A
  1. Atropine
  2. Homatropine
  3. Tropicamide
  • mydriasis and cyclopegia
40
Q

Muscarinic antagonist used for CNS (2)

A
  1. Benz.tropine for PD and EPS

2. Scopolamine for motion sickness

41
Q

Muscarinic antagonist used for respiratory (2)

A
  1. Ipra.tropium
  2. Tio.tropium

for COPD and asthma

42
Q

Muscarinic antagonist used for GU (3)

A
  1. Oxy.buty.nin
  2. Dari.fenacin
  3. Soli.fenacin
  • Reduce urgency in mild cystitis and reduce bladder spasms
43
Q

Muscarinic antagonist used for GI and respiratory

A

Glyco.pyrro.late

IV: pre-op use to reduce airway secretions
PO: drooling, peptic ulcer

44
Q

Atropine toxicity results in?

A

“Hot as a hare, Dry as a bone, Red as a beet, Blind as a bat, Mad as a hatter”

  • Hot b/c can’t sweat and tachycardic
  • Dry mouth and skin
  • Red skin
  • Blind b/c cyclopegia and acute angle glaucoma (2/2 mydriasis)
  • Mad b/c disorientation
45
Q

Atropine toxicity results in?

A

“Hot as a hare, Dry as a bone, Red as a beet, Blind as a bat, Mad as a hatter”

  • Hot b/c can’t sweat and tachycardic
  • Dry mouth and skin
  • Red skin
  • Blind b/c cyclopegia and acute angle glaucoma (2/2 mydriasis)
  • Mad b/c disorientation
46
Q

What garden plant leads to mydriasis

A

Jimson weed (Datura) 2/2 plant alklaloids

47
Q

Direct Sympathomimetics (8)

A
  1. Epi
  2. NE
  3. Iso.pro.terenol
  4. Dopamine
  5. Dobutamine
  6. Phenylephrine
  7. Albuterol, Salmetrol
  8. Terbutaline
48
Q

Epi

  • what receptors (at high doses which one more)
  • applications
A
  • beta > alpha (but at high doses, alpha more)

- anaphylaxis, open-angle glaucoma (not closed angle) w/alpha, asthma, hypotension

49
Q

NE

  • what receptors
  • applications
A
  • alpha-1 > alpha-2 > beta- 1

- treats hypotension by contraction of vascular smooth muscle, but causes decrease in renal perfusion

50
Q

Iso.pro.terenol

  • what receptors
  • applications
A
  • beta-1 = beta-2

- used in electrophysiological evaluation of tachyarrhythmias, but can worsen ischemia

51
Q

Dopamine

  • what receptors
  • applications
A
  • D1 = D2 > beta > alpha

- unstable bradycardia, HF, shock; inotropic and chronotropic alpha effects predominante ate higher doses

52
Q

Dobutamine

  • what receptors
  • applications
A
  • beta-1 > beta-2

- HF (inotropic > chronotropic); cardiac stress testing

53
Q

Phenylephrine

  • what receptors
  • applications
A
  • alpha-1 > alpha-2

- hypotension (by vasoconstriction); ocular procedures (b/c mydriatic); rhinitis (decongestant)

54
Q

terbutaline

  • what receptors
  • applications
A
  • beta-2 > beta-1

- reduce premature uterine contractions

55
Q

terbutaline

  • what receptors
  • applications
A
  • beta-2 > beta-1

- reduce premature uterine contractions

56
Q

Indirect Sympathomimetics (3)

A
  1. Amphetamine
  2. Ephedrine
  3. Cocaine
57
Q

Amphetamine

  • effect
  • applications
A
  • indirect general agonist, reuptake inhibitor, release of stored catecholamines
  • Narcolepsy, obesity, ADD
58
Q

Ephedrine

  • effect
  • applications
A
  • indirect general agonist releases stored catecholamines

- Nasal decongestant, urinary incontinence, hypotension

59
Q

what should you never give suspected cocaine intoxication? and why?

A

beta blockers
this would lead to unopposed alpha-1 activation and extreme hypertension b/c of loss of beta-2 which vasodilates and counteracts it

60
Q

what should you never give suspected cocaine intoxication? and why?

A

beta blockers
this would lead to unopposed alpha-1 activation and extreme hypertension b/c of loss of beta-2 which vasodilates and counteracts it

61
Q

NE vs. Isoproterenol

- BP and HR effects

A

NE is more alpha and Isoproterenol is beta

NE: alpha-1 –> increases BP –> reflex bradycardia
Isoproterenol: beta -2 –> decrease BP –> reflex tacycardia + beta-1 tachycardia

62
Q

Sympatholytics (alpha-2 agonists) (2)

A
  1. clonidine

2. alpha-methyldopa

63
Q

Clonidine

  • what receptors
  • applications
  • toxicity
A
  • alpha-2 agonist (decrease sympathetic outflow)
  • HTN emergency (doesn’t decrease renal flow); ADHD, severe pain, ethanol/opioid withdrawal
  • toxic: CNS depression, bradycardia, hypotension, respiratory distress, miosis
64
Q

alpha-methyldopa

  • what receptors
  • application
  • toxicity
A
  • alpha 2 agonist
  • HTN in pregnancy b/c safe in pregnancy
  • Direct Coombs + hemolytic anemia; SLE-like syndrome
65
Q

Non-selective alpha blockers (2)

A
  1. Phenoxybenzamine (irreversible)

2. Phentolamine (reversible)

66
Q

Alpha-1 selective alpha blocker (4)

A
  1. Praz.osin
  2. Teraz.osin
  3. Doxaz.osin
  4. Tamsul.osin`
67
Q

Alpha-2 selective alpha blockers (1)

A

Mirtazapine

68
Q

Phen.oxy.benz.amine

  • what receptors
  • applications
  • toxicity
A
  • nonselective irreversible alpha blockade
  • pheochromocytoma (used pre-op) to prevent catecholamine crisis
  • orthostatic hypotension, reflex tachycardia
69
Q

Phen.tol.amine

  • what receptors
  • applications
  • toxicity
A
  • nonselective reversible alpha blockade

- give to pts on MAO-I’s who eat tyramine containing foods

70
Q

Mirtazapine (Remeron)

  • what receptors
  • applications
  • toxicity
A
  • selective alpha-2 antagonism
  • depression
  • sedation, increase serum cholesterol and increase appetite
71
Q

Epinephrine vs. Phenylephrine on BP

  • before and after alpha-blockade
A

Epi at high doses acts more on alphas, so acts as a pressor… however, if administered after alpha-blockade, will have beta response of vasodilation and decrease in BP

Phenylephrine is a pure alpha-agonist, so acts as a pressor… so after alpha-blockade, will have no effect on BP

72
Q

Beta-1 selective Beta Blocker (5)

A
  1. Ace.but.olol
  2. A.ten.olol
  3. Bet.ax.olol
  4. Esm.olol
  5. Metopr.olol

beta-1 .. first 1st half of alphabet

73
Q

Non-selective Beta blocker (4)

A
  1. Nad.olol
  2. Pind.olol
  3. Propran.olol
  4. Tim.olol

both beta 1- and 2 … second half of alphabet

74
Q

non-selective alpha AND beta antagonism (2)

A
  1. Carvedi.lol
  2. Labeta.lol

these are not -olol’s, but just -lol’s

75
Q

Special beta blocker that blocks beta-1 and activates beta-3

what does it lead to?

A

Nebiv.olol

cardiac selective beta-1 blockade with beta-3 agonism
- beta-3 stimualtes activation of NO synthase in vasculature

76
Q

How does BB work to treat: angina pectoris

A

decreases HR and contractility, resulting in decrease O2 consumption

77
Q

How does BB work to treat: MI

- which ones

A

metoprolol, carvedilol, bisoprolol

decreases mortality

78
Q

How does BB work to treat: SVT

- which ones

A 
metoprolol and esmolol
- class II antiarrhythmics that decrease AV conduction velocity
79
Q

How does BB work to treat: HTN

- which ones

A
  • decreases CO by decreasing HR and contractility

- decreases renin secretion by blocking beta-1 on JGA cells

80
Q

How does BB work to treat: CHF

A
  • slows progression of chronic failure
81
Q

How does BB work to treat: glaucoma

- which one

A

Timolol

decreases secretion of aqueous humor (beta-2 blockade)

82
Q

Toxicity of beta blockers (5)

A
  1. impotence
  2. CV ADRs (brady, AV block, CHF)
  3. CNS ADRs (sz, sedation, sleep alteration)
  4. Dyslipidemia (w/metoprolol)
  5. Exacerbation of COPD and asthma

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