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STEP 1 Study > Sketchy Autonomic Drugs > Flashcards

Sketchy Autonomic Drugs Flashcards

1
Q

Cholinomimetics

A

mimic the affects of acetylcholine

(Acetylcholine receptor agonist)

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2
Q

Nicotinc Acetylcholine receptors are found where?

A

Autonomic ganglia

motor end plates

adrenal gland

act on ion channels

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3
Q

Muscarinic acetycholine receptors

A

M1 (Gq)

M2 (Gi)

M2 (Gq)

act on G proten coupled receptors

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4
Q

M1 receptors are found . .

A

nervs and CNS

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5
Q

M2 receptors are found where

A

atria

SA node

AV node

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6
Q

M3 receptors are found where?

A

glands

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7
Q

What causes nitric oxide release in vascular smooth muscles -> increased cGMP and vasodilation

A

M3 receptor activation

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8
Q

How does atherosclerosis cause vasodilation?

A

atherosclerosis -> vascular epithelial damage -> direct muscarinic receptor activation -> vasoconstriction

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9
Q

At high dose, muscarinic agonsit are what?

A

Non-selective, can cross to work on other M receptors

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10
Q

Bethanecol

A

Cholinomimetic

Muscarinic agonist

incr. secretion and motor activity of gut

Non onstructive conditions only

(post op ileus, neurogenic ileus)

urinary retention

(neurogenic bladder from spinal cord injury, post pregnancy)

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11
Q

Pilocarpine

A

Cholinomimetic

Muscarinic agonist

increase salivation

lens accomodation (contracts ciliary muscle)

ciliary muscle contraction - increase aqueous humor outflow = glaucoma treatment

activates spinchter pupillar - meiosis = treat acute angle glaucoma

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12
Q

Carbachol

A

Muscarinic and nicotinic agonist

pupilary constriction = acute angle glaucoma tx

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13
Q

Methacholine

A

Instigates asthma on pulmonary testing

contract bronchial smooth muscle = exacerbate asthma and COPD

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14
Q

All cholinomimetics can cause what?

A

peptic ulcers

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15
Q

Varenecline

A

Nicotinic receptor partial agoinst

Smoking cessation

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16
Q

Acetycholineesterase inhibitors

A

indirect cholinomimetics

reversible or irriversible

raise acetycholine or increase hte length of time acetycholine is at the synapse

effects Ach and NMJ

increase activity of NICOTENIC Ach receptors leading to increased strength in contraction

can be used to tx urinary retention (muscarinic activation)

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17
Q

-STIGMINE

A

drug suffix of acetycholinesterase inhibitors

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18
Q

Myasthenia Gravis

A

antibodies against nicotinic Ach receptors at NMJ

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19
Q

What are the sxs of Myasthenia Gravis?

A

progressive muscle weakness

Ptosis

diplopia

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20
Q

Pyridostigmine

A

Acetycholinesterase inhibitor

Long term treatments for Myasthenia Gravis

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21
Q

Neostigmine

A

Acetycholinesterase inhibitor

Used to treat myasthenia gravis

reverse non-depolarizing neuromuscular blockade

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22
Q

Endrophonium

A

acetycholinesterase inhibitor

transiently reverses symptoms of myasthenia gravis in untreated patients who have a positive tensilon test.

(fails to reverse if tensilon test is negative/during cholinergic crisis)

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23
Q

Pyridostigmine, neostigmine, and endrophonium are _______ _______ and do not _______ _____ ______.

A

quaternary amine

Do not penetrate the CNS

(only relieve sxs for 5-15 min)

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24
Q

Tubucuraine, pancuronium, cisatracurium?

A

non-depolarizing neuromuscular blocking agents that cause Curare

(inhibit nicotinic Ach recpetos at NMJ endplate)

25
Q

Succinylcholine

A

Nicotinic Ach receptor Agonist

depolarizing neuromuscular blocking agent

overstimulates NMJ causing the muscle to remain depolarized and unable to respond to stimulus

26
Q

Initial phase 1 of depolarizinf blockade is . . .

irreversible or reversible?

A

irreversible

AchE inhibitors potentiate blockade

27
Q

Physostigmine

A

Acetycholinesterase inhibitor with central effects

Can treat Atopine overdose (Central and peripheral effects)

28
Q

What are the symptoms of Atropine Overdose?

A

MAD as a hatter

HOT as a hare

BLIND as a bat

29
Q

Atropine

A

Muscarinic receptor antagonist (antimuscarinic)
Belladonna flower

Jimsonweed (alkaloid)

“Gardners mydriasis

reverse both peripheral and central muscarinic toxicity from organophosphates poisoning

increase HR (tx for bradycardia)

30
Q

What two things can enter the CNS to cause cholinergic effects?

A

Physostigmine and Organophosphates

31
Q

DUMBBEELSS

A

Diarrhea

Urination

Miosis

Bronchospam

Bradycardia

Excitation of skeletal muscle and CNS

Emesis

Lacrimation

Salivation

Sweating

32
Q

Acetylcholinesterase inhibitors toxicity

A

Flaccid Paralysis (overactivation of nicotinic receptor)

33
Q

Organophosphates

A

Insecticides (parathion, maltionm echotiophate)

acetycholinesterase inhibitors

nerve agents and herbicides

can cause acute cholinergic toxicity

34
Q

Pralidoxime

A

Reverse organophosphate toxicity by hydrolyzing the covalent bond (perepheral effects only)

regenerates AchE at muscarinic and nicotinic receptors

reverses flaccid paralysis as well

Side note: ineffective once aginin of organophosphates-cholinesterase complex has occured

35
Q

What are the three acetycholinesterase inhibitors used to treat alzheimer’s?

A

Galantime

Rivastigmine

Donepizil

(all penetrate the CNS )

36
Q

Antimuscarinics

A
  • Block DUMBBEELSS
  • block the action of Ach at M receptors
  • block parasympathetic action of M2 recepetors on the SA and AV node (increase HR and increase conduction) - useful for tx of Heart block (AV block)
  • treat extrapyramidal side effects caused by antipsychotics (dystonia, akathisia, parkinsonism- reestablish dopaminergic-cholinergic balance)
  • inhibit M3 receptors: sweat glands -> decreased sweating -> hyperthermia
  • decrease salivation and lacrimation -> dry mouth and eyes
  • pupilary dilation (mydriasis) and Cycloplegia (inability to accomadate the lens of near vision) -> blurred vision
  • mydriasis -> decreased outflow of aqueous humor -> cause acute angle glaucoma
37
Q

Scopolamine

A

Antimuscarinic

Used to treat motion sickness (vestibular nausea)- needs to be used prior to sickness

transdermal patch

cross blood brain barrier and inhibit central M1 receptors

38
Q

Iprarioprium

A
39
Q

Tiotropium

A

M3 muscarinic antagonist (antimuscarinic)

inhaled = bronchodilation

useful in the management of COPD (antagonize M3 receptor -> bronchodilation, decrease secretion)

dissociated more slowly from the M3 receptor (longer bronchodilation action)

40
Q

Oxybutynin

A

M3 muscarinic antagonist

relieve bladder spasm after urologic surgery

used to treat urge incontinece

(anatgonize M3 receptors -> relax smooth m. in ureters and bladder)

41
Q

Tolterodine

A

M 3muscarinic antagonist

used to treat adult urinary incontinence

(antagonize M3 receptors -> relax smooth muscle in ureters and bladder wall)

42
Q

M1 receptor antagonist can reduce ____ and _____ in Parkinson’s disease

A

tremors

rigidity

43
Q

Centrally acting M1 muscarinic antagonist

A

Benztropine and trihexyphenidyl

treat tremor and rigidity in Parkinson’s (block excess cholinergic activity)

44
Q

Excessive M1 activation is associated with what in PArkinson’s

A

cogwheel rigidity

45
Q

What happens when antimuscarinics cross the BBB?

A

They antagonize central M1 receptors causing sedation, agitation, hallucination, coma (especially in elderly patients)

46
Q

Clonidine

A

alpha 2 agonist

Sympatholytic in the treatment of HTN (reduces sympathetic tone -> reduce CO)

useful in HTN urgency

used to treat ADHD

Useful in the managemtn of Tourette’s syndrome

47
Q

Alpha 2 agonist affect the CNS how?

A

inhibition of sympathetic tone -> reducing blood pressure

48
Q

alphamethyl-dopa

A

alpha 2 receptor agonsit

tx HTN (mainly gestational)

can cause a lupus like syndrome

49
Q

Tizanidine

A

alpha 2 receptor agonist

central acting muscle relaxant

50
Q

phentolamine

A

reversible alpa 1 and alpha 2 antagonist

cause vasodilation (alpha 1 antagonist effect)

used to treat cocaine toxicity (avoid beta blockers due to unopposed alpha constriction)

Tx HTM crisis caused by MAO inhibitors

used preoperatively and interoperatively to control blood pressure with pheochromocytoma

51
Q

Phenosybenzamine

A

irriversible alpha 1 and alpha 2 antagonist

given days before a pheochromcytoma removal

52
Q

Sympathomimetic tyramine

A

in wine and aged cheese

metabolizded by MAO-A

MAO inhibitors prevent metabolism of tyramine causing a HTN crisis (tx with phentolamine)

53
Q

Pheochromocytoma

A

catchecolamine secreting tumor of the adrenal medulla

sxs: headaches, hypertension, palpitation, sweating

tx with phentolamine

54
Q

alpha receptor antagonism can cause what?

A

Orthostatic hypotention

(alpha blocker induced hypotension can cause reflex tachycardia)

55
Q

-OSIN

A

suffix for alpha 1 antagonist

Prazosin

Terazosin

doxazosin

tamsuloisn

cause vasodilation

56
Q

Terazosin

A

alpha 1 antagonist

treat BPH (relax smooth muscle in the urethra and prostate)

57
Q

Prazosin

A

alpha 1 antagonist

used to treat PTSD

increased risk of orthostatic hypotention

58
Q

Mertazipine

A

atypical antidepressent wuth antagonist effects at alpha 2 and other receptors

ehances seretonin release and treats depression

STEP 1 Study (3 decks)

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