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Cholinergic's Flashcards

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1
Q 
Parasympathetic Effects of Acetylcholine: 
Cardiovascular 
GI/GU
Glands
Respiratory 
Ocular
A

Decrease HR/ AV/ contractility
Vasodilation
Increase GI/GU motility, secretion, sphincter relaxation & Increase micturition
Increase glandular secretion
Increase Bronchoconstriction/ respiratory secretions
Miosis/ ciliary muscle contraction – accommodation for near vision

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2
Q

What are the sympathetic and parasympathetic effects elicited by Ach?

A

Sympathetic- vasoconstriction, sweating

Parasympathetic- bradycardia; miosis; GI motility/ urination; glandular secretions

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3
Q

What is the rate limiting step in Ach hydrolysis

A

Quaternary ammonium attracted to anionic site
Acyl O attacked by serine at esteratic site
Ester bond cleavage and liberation of choline (enzyme now acylated)
Acetate removed from AchE–> reactivation **RLS

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4
Q

Tetrodotoxin action

A

Inhibits Na channel/ AP

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5
Q

Saxitoxin action

A

Inhibits Na channel/ AP

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6
Q

Black Widow action

A

Stimulate Ach release

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7
Q

Botulism Toxin action

A

STOPS Ach release

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8
Q

What are the physiologic effects of muscarinic AGONISTS?

A

SLUDE +BBB (salivation, lacrimation, urination, defecation, emesis, bronchoconstriction, bradycardia, blurred vision)

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9
Q

What is that “Bradycardia caveat in “SLUDE BBB”

A
  • Bradycardia at high dose only (Low dose reflex > drug HR in response to vasodilation)
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10
Q

What drug can be used to reverse or block the effects of a muscarinic AGONIST?

A

Atropine

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11
Q

Pilocarpine:
MOA
Specific Use

A

Muscarinic Agonist

Wide angle glaucoma

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12
Q

What are 5 contraindications for all muscarinic agonists

A

1) Asthma
2) COPD
3) CV disease
4) Hyperthyroid
5) peptic ulcer

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13
Q

Carbachol:
MOA
Specific Use

A

Muscarinic Agonist

Wide angle glaucoma

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14
Q

Bethanecol:
MOA
Specific Use

A

Muscarinic Agonist

GI/GU motility–treats urine retention, distention, etc.

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15
Q

Muscarine:
MOA
What’s the story here?

A

Mushrooms, accidental ingestion

Need atropine for reversal

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16
Q 
What are the physiologic effects of Muscarinic ANTAGONISTS: 
CV
GI/GU
Ocular 
Sweating
CNS
A 
Increase CV function
Decrease GI/GU motility
Increase bronchi dilation 
Cyclopedia/ Mydriasis 
Decrease sweating 
CNS Depression
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17
Q

What are 5 ADR’s associated with all Muscarinic ANTAGONISTS? Which Drug is used to reverse them?

A 
Red as a beet 
Dry as a bone 
Blind as a bat 
Hot as a fire 
Mad as a hatter

Reverse with Physostigmine

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18
Q

What are 3 contraindications associated with all Muscarinic ANTAGONISTS?

A
  1. glaucoma (esp narrow angle)
  2. cardiac disease
  3. Prostatic hypertrophy
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19
Q

Homotropine:
MOA
Therapeutic use

A

Bind Muscarinic receptors and INHIBIT Ach effects

Optho Exam: mydriasis, cycloplegia

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20
Q

Cyclopentolate:
MOA
Therapeutic Use

A

Bind Muscarinic receptors and INHIBIT Ach effects

Optho Exam: mydriasis, cycloplegia

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21
Q

Tropicamide:
MOA
Therapeutic Use

A

Bind Muscarinic receptors and INHIBIT Ach effects

Optho Exam: mydriasis, cycloplegia

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22
Q

Atropine:
MOA
Therapeutic Use

A

Bind Muscarinic receptors and INHIBIT Ach effects

Reverses anticholinesterases (AchEi) + muscarinic agonist

Note: toxic dose stimulates CNS,
> toxic dose will depress CNS

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23
Q

Glycopyrrolate:
MOA
Therapeutic Use

A

Bind Muscarinic receptors and INHIBIT Ach effects

Reverses Anticholinesterases

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24
Q

Benztropine:
MOA
Therapeutic Use

A

Bind Muscarinic receptors and INHIBIT Ach effects

Parkinsonism

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25
Trihexylphenidyl: MOA Therapeutic Use
Bind Muscarinic receptors and INHIBIT Ach effects Parkinsonism
26
Scopolamine: MOA Therapeutic Use
Bind Muscarinic receptors and INHIBIT Ach effects Administered as transdermal patch to prevent motion sickness Note: CNS Depressant in therapeutic doses
27
Ipratropium: MOA Therapeutic Use
Bind Muscarinic receptors and INHIBIT Ach effects COPD, Asthma
28
Tiotropium: MOA Therapeutic Use
Bind Muscarinic receptors and INHIBIT Ach effects COPD, Asthma
29
Darifenacin: MOA Therapeutic Use
Bind Muscarinic receptors and INHIBIT Ach effects Overactive bladder in children
30
Amitriptyline
Has significant anti-muscarinic activity and can cause anti-muscarinic toxicity
31
H1 Receptor antagonists
Has significant anti-muscarinic activity and can cause anti-muscarinic toxicity
32
Phenothiazines
Has significant anti-muscarinic activity and can cause anti-muscarinic toxicity
33
What is the MOA for all non-depolarizing (competitive) NMJ Blockers?
Bind Nm Receptor at NMJ--> Displace Ach--> Induce Paralysis without polarization
34
What is the therapeutic indication for all Non-Depolarizing/ Competitive NMJ Blockers?
Induce muscle paralysis as an adjunct to anesthetic during surgery
35
What 3 drugs enhance the effects of non-depolarizing/ competitive NMJ blockers
* Halogenated Hydrocarbon Anesthetics * Aminoglycoside Antibiotics * Ca++ Channel Blockers
36
Which drugs can be used to reverse the effects of non-depolarizing/ Competitive NMJ Blockers?
Anticholinesterase Drugs (*NEOSTIGMINE, EDROPHONIUM, PYRIDOSTIGMINE)
37
What are three commonalities amongst all non-depolarizing/ Competitive NMJ blockers? BBB? Molecular structure? Administration?
- NO CROSS BBB - Quaternary Ammonium Salts - IV admin only
38
Curare: MOA Duration of activity
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER Long acting
39
``` Tubocurarine: MOA Duration of activity Metabolism* ADR* ```
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER - Long acting - Hepatic metabolism, renal excretion ADR: Partial ganglionic block (histamine release--> bronchospasm, hypotension)
40
Doxacurium: MOA Duration of activity
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER | - Long acting
41
Panacuronium: MOA Duration of activity
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER | - Long acting
42
Gallamine: MOA Duration of activity ADR*
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER - Long acting ``` ADR: Blocks cardiac Vagus N - Tachycardia - ~HTN - ^ Cardiac Output "Galloping Heart!" ```
43
Cisatracurium: MOA Duration of action Metabolism*
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER - Intermediate duration Metabolized by plasma esterase; has fast onset
44
Rocuronium: MOA Duration of Action
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER | - Intermediate duration
45
Vecuronium: MOA Duration of Action
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER | - Intermediate duration
46
Mivacurium: MOA Duration of action Metabolism
NONDEPOLARIZING/ COMPETATIVE NMJ BLOCKER - Short duration of action Metabolized by pseudocholinesterase (plasma cholinesterase)
47
Common ADR Associated with all Non-Depolarizing/Competative NMJ Blockers
Prolonged muscle paralysis & apnea
48
Succinylcholine: MOA Therapeutic Use
Depolarizing NMJ Blocker: Prolonged binding to Nm (Stable Nm Agonist) Phase I Depolarization block--> muscle paralysis--> ~Phase II depolarization block (low butrylcholinesterase; too high dose) Rapid muscle paralysis for endotracheal intubation
49
Succinylcholine: Metabolism Route of administration BBB?
Butrylcholinesterase IV Admin Does not cross BBB
50
Succinylcholine ADR***
* Malignant hypepyrexia - Muscle rigidity - Hyperthermia - HTN - Tachycardia - Genetic predisposition - Tx. DANTROLINE
51
2 Drugs that prolong/ exaggerate action of succinylcholine
1. Anticholinesterases (Neostigmine) | 2. Halothane anesthetics
52
What are two DEPOLARIZING NMJ BLOCKING Drugs?
1. Succinylcholine | 2. Nicotine
53
Nicotine: MOA Physiologic effects
Low Dose: STIMULATES Nn, Nm High Dose: BLOCKS Nn, Nm Excessive SLUDE BB, Tachy, HTN, muscle fasciculation's
54
Acute Nicotine Poisoning: Manifestation Drug for reversal
Excessive SLUDE BB (stimulation)--> Brain stem Depression--> Respiratory Failure Reverse with ATROPINE
55
Edrophonium: MOA Therapeutic Use Does it cross BBB?
Reversible Anticholinesterase - Reverse effects of competitive non-depolarizing NMJ blockers (not succinylcholine) - Quaternary Ammonium, no cross BBB
56
Tacrine MOA Therapeutic Use
Reversible Anticholinesterase | Alzheimers--crosses BBB
57
Rivastigmine MOA Therapeutic Use
Reversible Anticholinesterase | Alzheimers--crosses BBB
58
Donepezil MOA Therapeutic Use
Reversible Anticholinesterase | Alzheimers--crosses BBB
59
Physostigmine MOA Therapeutic Use Cross BBB?
``` Reversible Anticholinesterase CARBAMOYL ESTER LINKAGES Carbamylate esteric site on AchE causes increase in Ach - Reverse atony of smooth muscle - Reverse non-depolarizing NMJ blockers - Crosses BBB ```
60
Neostigmine MOA Therapeutic Use Cross BBB?
``` Reversible Anticholinesterase CARBAMOYL ESTER LINKAGES Carbamylate esteric site on AchE causes increase in Ach - Reverse atony of smooth muscle - Reverse non-depolarizing NMJ blockers - No cross BBB ```
61
Pyridostigmine MOA Therapeutic Use
Reversible Anticholinesterase CARBAMOYL ESTER LINKAGES Carbamylate esteric site on AchE causes increase in Ach - Reverse non-depolarizing NMJ blockers
62
Isoflurophate MOA Therapeutic Use
Anticholinesterase IRREVERSIBLE!!!! ORGANOPHOSPHATE INHIBITORS Phosphorylate esteratic site of AchE
63
Echothiophate MOA Therapeutic Use
Anticholinesterase IRREVERSIBLE!!!! ORGANOPHOSPHATE INHIBITORS Phosphorylate esteratic site of AchE - Second Line Tx. Chronic wide angle glaucoma /Acute angle glaucoma (short term tx)
64
Insecticides MOA Therapeutic Use
Anticholinesterase IRREVERSIBLE!!!! ORGANOPHOSPHATE INHIBITORS Phosphorylate esteratic site of AchE
65
Nerve Gas MOA Therapeutic Use
IRREVERSIBLE!!!! ORGANOPHOSPHATE INHIBITORS | Phosphorylate esteratic site of AchE
66
Pralidoxime (2-PAM): MOA Therapeutic Use
Cholinesterase Reinactivator: Pulls organic phosphate off esteratic site of AchE Administer soon after poisoning to beat aging
67
What happens when organophosphate inhibitors age?
Loss of alkyl or alkoxyl group makes phosphorylated enzyme more stable--> Increases irreversible properties
68
How does Anticholinesterase poisoning present and what drugs can be used to reverse it?
Excessive SLUDE BBB; delayed neurotoxicity REVERSE: ATROPINE, PRALIDOXIME
69
Which drug is used to identify whether patient has Myasthenia Gravis or Cholinergic Crisis?
Edrophonium, then look for muscle strength: MG: Increase muscle strength, give pt more AchEi Cholinergic Crisis: Decrease Muscle Strength, give patient less anti cholinesterase
70
How do you treat myasthenia gravis?
Neostigmine, Pyridostigmine

Nervous System Pharmacology (3 decks)

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