Autonomic drugs Flashcards

0
Q

What are symptoms of “cholinergic syndrome”, or cholinesterase inhibitor poisoning? Tx?

A

MS: weakness, confusion, drowsiness –> coma, seizures
Pupils: miosis (small, fixed or sl reactive)
Bradycardia, paralysis, muscle fasciculations
SLUDGE: salivation/sweating, lacrimation, urination, defecation, GI hyperactivity, emesis.
Tx: atropine (muscarinic antagonist), pralidoxime (regenerates AChE)

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1
Q

What are cholinomimetics? What are the two types?

A

Drugs that increase acetylcholine signaling

1) Direct cholinergic agonists
2) Anti-cholinesterases

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2
Q

Name 4 cholinergic direct agonists

A

Bethanechol, carbachol, pilocarpine, methacholine

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3
Q

Name 7 acetylcholinesterase inhibitors

A

Neostigmine, pyridostigmine, physostigmine, Donepezil, rivastigmine, galantamine, edrophonium

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4
Q

Bethanechol

A

Cholinergic direct agonist
Activates badder and bowel smooth muscle
Resistant to AChE
Used for post-op ileus, neurogenic ileus, urinary retention

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5
Q

Carbachol

A

Direct cholinergic, ACh mimic

Used for relief of intraocular pressure, glaucoma pupillary constriction

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6
Q

Pilocarpine

A

Direct cholinergic agonist
Contracts ciliary muscle of eye and pupillary sphincter, resistant to AChE
Used for glaucoma, stimulator of sweat and tears

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7
Q

Methacholine

A

Direct cholinergic agonist

Works in airway to constrict airways, used as asthma challenge

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8
Q

Neostigmine

A

Anticholinesterase

Used for post-op and neurogenic ileus, urinary retention, myasthenia gravis, reversal of NMJ blockade

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9
Q

Pyridostigmine

A

Anticholinesterase
Used as long-acting to improve strength in myasthenia gravis
Does not penetrate CNS

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10
Q

Physostigmine

A

Anticholinesterase
Used for anticholinergic toxicity (eg atropine OD)
Penetrates CNS

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11
Q

Donepezil, rivastigmine, galantamine

A

Anticholinesterase

Used for Alzheimer’s disease

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12
Q

Edrophonium

A

Anticholinesterase

Historically used for diagnosis of myasthenia gravis

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13
Q

Treatment for cholinesterase inhibitor poisoning

A

Atropine (competitive inhibitor) and pralidoxime (regenerates AChE)

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14
Q

Muscarinic Antagonist Effects

A

Oppose cholinergics. Dilate eyes, decrease secretions (airways, GI), decrease GI motility, decrease bladder urgency.

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15
Q

Muscarinic antagonist toxicity

A

Hot as a hare (no sweating), dry as a bone (no secretions), red as a beet (flushing), blind as a bat (cycloplegia), mad as a hatter (disorientation), bloated as a toad (constipation and urinary retention

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16
Q

Atropine

A

Muscarinic antagonist

Mydriasis and cycloplegia in eye

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17
Q

Homatropine

A

Muscarinic antagonist

Mydriasis and cycloplegia in eye

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18
Q

Tropicamide

A

Muscarinic antagonist

Mydriasis and cycloplegia in eye

19
Q

Benztropine

A

Muscarinic antagonist

CNS, used for Parkinson

20
Q

Scopolamine

A

Muscarinic antagonist

CNS, used for motion sickness

21
Q

Ipratropium, tiotropium

A

Muscarinic antagonist

Respiratory system, used for COPD

22
Q

Oxybutynin, darifenacin, solifenacin

A

Muscarinic antagonist

Reduces urinary urge in cystitis

23
Q

Glycopyrrolate

A

Muscarinic antagonist

GI and respiratory

24
Q

Drugs for urinary urge/incontinence

A

Oxybutynin, darifenacin, solifenacin

25
Q

Other meds with anticholinergic side effects

A

H1 antihistamines (1st gen), neuroleptics, TCAs, Jimson weed

26
Q

Anticholinergics contraindicated in

A

BPH, hyperthermia, acute angle glaucoma, GI obstruction, elderly

27
Q

Epinephrine

A

Sympathomimetic, b > a (a predominates at high doses)

Used for anaphylaxis, open angle glaucoma, asthma, hypotension

28
Q

Norepinephrine

A

Sympathomimetic, a1 > a2 > b1 (HR actually decreases by reflex)

Used for hypotension, except it decreases renal perfusion

29
Q

Isoproterenol

A

Beta agonist, b1 = b2

Decreases mean arterial pressure, increases HR

30
Q

Dopamine

A

Sympathomimetic, D > b > a (can adjust dosage for effects)

31
Q

Dobutamine

A

Sympathomimetic, b1 > b2, a

32
Q

Phenylephrine

A

Sympathomimetic, a1 > a2

Used for hypotension

33
Q

Albuterol, salmeterol, terbutaline

A

Sympathomimetic, b2 > b1

Can be used for asthma and to reduce premature uterine contractions

34
Q

Amphetamine

A

Indirect sympathomimetic, general agonist and reuptake inhibitor. Used for narcolepsy, obesity, ADD

35
Q

Ephedrine

A

Indirect sypathomimetic, releases stored catecholamines. Used for nasal decongestion, urinary incontinence, hypotension

36
Q

Cocaine

A

Indirect sympathomimetic general agonist, reuptake inhibitor. Causes vasoconstriction and local anesthesia.

37
Q

Beta blockers plus cocaine?

A

Bad idea! Can lead to unopposed alpha activation, massive hypertension.

38
Q

Clonidine

A

a2 agonist, can be used for hypertensive emergency, ADHD, pain. CNS depression, bradycardia, rebound hypertension, small pupils.

39
Q

a-methyldopa

A

a2 agonist, used for hypertension in pregnancy. Can cause hemolytic anemia, SLE type syndrome

40
Q

Phenoxybenzamine

A

Irreversible alpha blocker. Used for pheochromocytoma to prevent hypertensive crisis. Can cause orthostatic hypertension, reflex tachycardia

41
Q

Phentolamine

A

Reversible alpha blocker

42
Q

Prazosin (-zosin)

A

a1 blocker, used for BPH, hypertension, PTSD (prazosin). Can cause first dose orthostatic hypotension.

43
Q

Tamsulosin

A

Selective a1 blocker for prostate, BPH

44
Q

Mirtazapine

A

Selective a2 blocker, used for depression. Can cause sedation, high cholesterol, increased appetite

45
Q

Effect of each receptor on blood pressure

A

a1: increases (especially diastolic)
b1: increases (especially systolic)
b2: decreases (especially diastolic)