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RENAL II - Pharm Exam > Cholinergic Agonists and Antagonists > Flashcards

Cholinergic Agonists and Antagonists Flashcards

1
Q

Direct acting cholinergic agonists

A

Stimulate muscarinic or nicotinic receptors directly

Alkaloids and Choline esters

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2
Q

Indirect acting cholinergic agonists

A

Increase the amount of ACh available to act on mAChR and nAChR
Stimulate effector organs
Stimulate (followed by depression) muscle and ganglia
Stimulate (sometimes depress) receptors in the brain
(Reversible and irreversible)

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3
Q

Choline esters

A

Quaternary ammonium groups - not absorbed to CNS
Hydrolyzed by AChE: ACh > methacholine > carbachol > bethanechol (longest lasting)
MOA: direct cholinergic agonists

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4
Q

Alkaloids

A

Uncharged tertiary - well absorbed, can go to CNS
Basic (acidification of urine helps elimination)
MOA: direct cholinergic agonists

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5
Q

Muscarine (in mushrooms)

A

Quaternary amine
Highly toxic
Can enter CNS

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6
Q

M1

A

Nerves

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7
Q

M2

A

Heart, nerves, smooth muscle

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8
Q

M3

A

Glands, smooth muscle, endothelium

Predominates in most organs

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9
Q

M4

A

CNS (brain > SC)

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10
Q

M5

A

CNS (brain > SC)

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11
Q

Nm

A

Skeletal muscle and NMJ

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12
Q

Nn

A

Postganglionic cell body, dendrites, CNS (SC > brain)

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13
Q

IP3 and DAG cascade

A

M1, M3, M5

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14
Q

Inhibition of cAMP production

A

M2 and M4

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15
Q

Activation of K+ channels

A

M2

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16
Q

Na+ and K+ depolarizing ion channel

A

Nm and Nn

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17
Q

Skeletal muscle receptors

A 
ONLY nAChR (nicotinic)
Binding these receptors with agonist leads to depolarizing blockade
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18
Q

Depolarizing blockade

A

Binding AChR with greater affinity cause disorganized depolarization and doesn’t allow muscle cell to repolarize
Leads to flaccid paralysis/muscle relaxation
Ex. Succinylcholine

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19
Q

Prolonged presence of nAChR agonist

A

Abolishes effector response - postganglionic neuron stops firing
Skeletal muscle cells relax

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20
Q

General parasympathetic effects

A

Pupil constriction, accommodation, salivation, bronchiole constriction, lung secretions, gastric secretions, increase motility, diarrhea, urination
**INCREASE with agonist

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21
Q

PS and Eye

A

Constrict sphincter, increase aqueous humor flow

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22
Q

PS and Cardio

A

Only M2 mAChR
Reduce peripheral resistance
Atria > Ventricle - decrease rate and contractile strength
Release EDRF - relax SM around blood vessels
Small dose - slight BP decrease, increase HR reflex
Large dose - bradycardia and hypotension

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23
Q

PS and GI

A

Increase glandular secretions (salivary and gastric especially)
M3 - direct contraction
M2 - indirection contraction
Sphincter relaxation

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24
Q

PS and GU

A

Sphincter relaxation

Increase voiding

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25
Q

CNS - excitatory mAChRs

A

Increased cognitive function

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26
Q

CNS - inhibitory mAChRs

A

Tremors, hypothermia, and analgesia

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27
Q

CNS - nAChR activation

A

Dose dependent

Can have severe CNS consequences

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28
Q

PNS - nAChR activation

A

Simultaneously fire parasympathetics and sympathetics
Cardio - sympathetic dominates
GI/GU - parasympathetic dominates

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29
Q

Direct agonist use in Eye

A

Glaucoma - Increase flow via contraction (Replaced by beta blockers and prostaglandin derivatives)

Accommodative estropia - Cross eyed from accommodation error

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30
Q

Direct agonist for GI/GU

A 
Bethanechol:
Increase tone of stomach and intestines
Increase tone of lower esophageal sphincter
Fix urinary retention
**Beware of bowel obstruction

Pilocarpine and Cevimeline:
Increase salivary secretions

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31
Q

Muscarinic direct agonist overdose

A

Treat with Atropine

N/V/D, urination, salivation, sweating, cutaneous vasodilation, bronchial constriction

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32
Q

Muscarinic direct agonist contraindications

A

**Asthma
Hyperthyroidism
Coronary insufficiency
Acid-peptic disease

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33
Q

Nicotinic direct agonist acute toxicity

A 
Nicotine only common source
CNS simulation
Skeletal muscle depolarization blockade
Respiratory paralysis
HTN and cardiac arrhythmias
Treat with atropine and diazepam (no muscle recovery)
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34
Q

Acetylcholine use

A

Intraocular during surgery

Rarely systemically given

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35
Q

Methacholine use

A

Treat airway hyperreactivity if no asthma

Rarely used due to risk of bronchospasm

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36
Q

Bethanechol use

A

Urinary retention and heartburn
**selective mAChR
Little cardiovascular effect

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37
Q

Carbachol

A

Glaucoma or miosis during surgery

38
Q

Cevimeline

A

Treat xerostomia

*Metabolized with p450 pathway and eliminated in urine

39
Q

Pilocarpine

A

Treat xerostomia
Glaucoma or miosis as well
**selective mAChR

40
Q

Varenicline (Chantix)

A 
Smoking cessation
**selective nAChR alpha4beta2 in brain
Reduce craving and withdrawal
90% eliminated unchanged in urine
Potential psych side effects :(
41
Q

Indirect agonists MOA

A

Inhibiting cholinesterase and allowing more ACh to interact with receptors therefore increase parasympathetic effects

42
Q

Alcohol AChE Inhibitors

A

Positively charged quaternary
Reversible binding to AChE (electrostatic interactions and H bonding)
Ex. Endrophonium

43
Q

Carbamic acid esters AChE inhibitors

A

Positive or neutral, quaternary or tertiary
Reversible binding to AChE (covalent bonds that are later hydrolyzed)
**Ex. Neostigmine, pyridostigmine, physostigmine

44
Q

Organophosphate AChE inhibitors

A

Insecticides, nerve gases
Neutral and lipid soluble - CNS toxicity, readily absorbed everywhere including skin and lungs
Irreversible binding to AChE (very stable bond, aging increase phosphorus-enzyme bond)
Little excretion/metabolism
**Need to regenerate AChE as well as counteract ACh overload

45
Q

Quaternary and charged AChE inhibitors

A 
Poor absorption, insoluble in lipids (NO CNS)
Parenteral preferred
Act preferentially at NMJ
Duration determined by complex stability
**Neostigmine, pyridostigmine
Edrophonium, echothiophate, ambenonium
46
Q

Tertiary and uncharged AChE inhibitors

A

Well absorbed - including CNS
More toxic
**Physostigmine
Donepezil, tacrine, rivastigmine, galantamine

47
Q

Eye, GI, GU and Respiratory + AChE inhibitors

A

Same effect as direct cholinomimetics

48
Q

Cardio and AChE inhibitors

A

Parasympathetic tone dominates

Modest bradycardia, fall in CO, little or no decrease in BP

49
Q

NMJ and AChE inhibitors

A

Therapeutic levels can increase strength of contraction

Too much can cause blockade

50
Q

Reversal of pharmacologic paralysis using AChE inhibitors

A

Reverse effects of nondepolarizing nerve blockers
**Neostigmine and edrophonium
Treat atony of GI and GI

51
Q

AChE inhibitor and Glaucoma

A

Same effect as direct agonist but not commonly used

52
Q

AChE inhibitor and dementia

A

Tacrine came first
Donepezil, rivastigmine, galantamine, and physostigmine preferred
Parkinsonian dementia also benefits

53
Q

Compounds with anticholinergic properties

A

Atropine, antihistamines, tricyclic antidepressents, sleep aids, cold preparations

54
Q

Antidote for anticholinergic compounds

A

AChE inhibitor

**Physostigmine (can cross BBB)

55
Q

AChE inhibitor with nondepolarizing neuromuscular blocking agents

A

Blockade will diminish

Exception: mivacurium

56
Q

AChE inhibitor with Succinylcholine

A

Enhance phase 1 block

Antagonize phase 2 block

57
Q

AChE inhibitor with direct agonists

A

Enhance the effects

58
Q

AChE inhibitor with beta blockers

A

May enhance bradycardic effects

59
Q

AChE inhibitor with systemic corticosteroids

A

May enhance muscle weakness

60
Q

AChE inhibitor acute intoxication

A

Increased parasympathetics
Ex. pesticides, veterinary vermifuges
Ingestion - GI first
Skin - sweating and muscle fasciculations
Lipid soluble agents have serious CNS involvement
TOD can be quick

61
Q

AChE inhibitor antidote

A

Atropine
Cholinesterase regenerators needed for NMJ
Can add benzodiazepine (anticonvulsant) as well

62
Q

Cholinesterase regenerator

A

Pralidoxime

Must be given before aging occurs

63
Q

AChE inhibitor prophylaxis

A

Pyridostigmine in low doses

64
Q

Antinicotinic drugs

A

Effect NMJ and ganglia

Not as clinically useful

65
Q

mAChR blockers

A

Parasympatholytic - block the effects of parasympathetic discharge
**Think everything opposite of parasympathetics
Prototype - Atropine

66
Q

Tertiary antimuscarinics

A

Used for eye or CNS
More readily absorbed and distributed
Atropine, tropicamide, benztropine

67
Q

Quaternary antimuscarinics

A

Elicit effects in periphery

Ipratropium, glycopyrrolate

68
Q

Metabolism/excretion of antimuscarinics

A

Effect usually declines rapidly
Excreted in the urine
Except - long lasting in the eye

69
Q

MOA of atropine

A

Reversible antagonist of mAChRs
Most sensitive are salivary, bronchial, and sweat (gastric is the least sensitive)
**Does not distinguish between types of receptors

70
Q

CNS and antimuscarinics

A

Low dose: minimal stimulant effect on CNS, mild sedative to brain
Reduce Parkinson tremor
Reduce motion sickness (scopolamine)

71
Q

Eye and antimuscarinics

A

Dilate, can’t accommodate, reduce tears

72
Q

Cardio and antimuscarinics

A

Mild tachycardia
Prevent CV effects of direct muscarinic agonists
Low dose - initial bradycardia (reflex)
High dose - tachycardia (vagal block)

73
Q

Respiratory and antimuscarinics

A

Bronchodilation and reduced secretion

74
Q

GI and antimuscarinics

A

Decreased saliva
Decreased gastric secretions to a lesser degree
Gastric emptying is prolonged and GI transit time prolonged

75
Q

GI and antimuscarinics

A

Treat urinary incontinence - slow voiding, relax muscle

76
Q

Sweat glands and antimuscarinics

A

Reduce thermocontrol/sweating even though they are only innervated by sympathetics
*Atropine fever

77
Q

Antimuscarinics and Parkinsons

A

Reduce tremor

Benztropine, trihexyphenidyl, procyclidine

78
Q

Antimuscarinics and Motion sickness

A

Antihistamines

*Scopolamine

79
Q

Antimuscarinics in anesthesia

A

Atropine blocks vagal reflexes

Atropine paired with neostigmine when reversing skeletal muscle relaxation (block increase in parasympathetics)

80
Q

Antimuscarinics in opthalmologic disorders

A

Mydriasis for long periods

Prevent synechia formation in uveitis and iritis

81
Q

Antimuscarinics in respiratory disorders

A

Treat asthma and COPD
Ipratropium
**Tiotropium

82
Q

Antimuscarinics in cardio disorders

A

Rarely used

Can alter vagal reflex

83
Q

Antimuscarinics and GI disorders

A

Treat traveler’s diarrhea

Can be combined with opioid agent to discourage abuse (Lomotil)

84
Q

Antimuscarinics and urinary urgency

A

Oxybutynin
Trospium
Darifenacin, solifenacin, and tolterodine - selective for M3, less xerostomia and constipation

85
Q

Cholinergic poisoning

A

No effective treatment for muscarinic effects

Treat with antimuscarinic and AChE regenerator

86
Q

Pralidoxime

A

Cholinesterase regenerator

Charged - only works at NMJ

87
Q

Rapid onset cholinergic poisoning

A

Adequately treated with Atropine

Shows signs of DUMBBELLS

88
Q

High concentration of atropine

A

Dry, blind, red, mad, hot

89
Q

Atropine overdose

A

Treat with cholinesterase inhibitor

or treat symptomatically

90
Q

Antimuscarinic contraindications

A

Glaucoma
History of prostatic hyperplasia (risk for acute urinary retention)
Acid peptic disease (slowed emptying increases discomfort)

91
Q

Pirenzepine

A

M1 selective antimuscarinic used in other countries for peptic ulcer disease

92
Q

Ganglion blocking drugs

A

Synthetic amines
*Mecamylamine - can cross BBB
Blocks both - Parasympathetic tone dominates
Use is infrequent

RENAL II - Pharm Exam (7 decks)

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