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Pharmacology > Cholinesrterase drugs > Flashcards

Cholinesrterase drugs Flashcards

1
Q

Nicotinic Receptor location

A

Neuromuscular end plate, Skeletal muscle, Autonomic ganglion cells

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2
Q

Muscarinic Location

A

Nerve, heart and smooth muscle, Gelands and endothelium

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3
Q

Direct Acting CAg

A 
Acetylcholine
Bethanechol
Carbachol
Cevimeline
Nicotine
Pilocarpine
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4
Q

Indirect acting Rev CAg

A 
Ambenonium
Donepezil
Edrophonium
Galantamine
Neostigmine
Physostigmine
Rivastigmine
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5
Q

Indirect Acting Irr CAg

A

Echothiophate

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6
Q

Cholinomimetic (cholinergic) Drugs Short acting

A

Edrophonium

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7
Q

Cholinomimetic (cholinergic) Drugs

Intermediate to long acting

A

Carbamates

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8
Q

Very long acting Cholinomimetic (cholinergic) Drugs

A

Parathion

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9
Q

ACETYLCHOLINE CL Susc, Musc, Nico

A

Very
intermediate
intermediare

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10
Q

Methacholine Susc, Musc, Nico

A

V Little, Very, Intermediate

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11
Q

CARBACHOL CL Susc, Musc, Nico

A

Neg, Little, intermediate

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12
Q

Betanechol Susc, Musc, nico

A

Neg, Little, none

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13
Q

Acetylcholine

A

Direct Acting (Muscarinic)

Metacholine (No nicotinic action, resistant to Ache, like carbachol and
bethanechol

Act on both M and N receptors. Activates M1-M3 receptors in all peripheral tissues

Miotic for Eye surgery

CNS stimulation, miosis, cyclospasm, bronchoconstriction, excessive GI
and GU smooth muscle contraction, increased secretory activity of
sweat gland, airway; vasodilation (arises from M3 activation and
requires intact endothelium – Nitric oxide mediated

Results to increased secretion, smooth muscle contraction (except in
vascular smooth muscles where it causes relaxation) and changes in
heart rate; very short-lived duration of action: 5-30 sec, rapidly
hydrolyzed by AChe

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14
Q

Bethanechol

Carbachol USP 0.01% W/V
1 ml vial
A pack of 1 vial

A

Direct Acting (Muscarinic)

Carbachol (act on both muscarinic and nicotinic receptors)

Act on both M receptors only. Activates M1-M3 receptors

Bladder and bowel atony (post-surgery or spinal cord injury); congenital
megacolon

Cyclospasm, Diarrhea, Urinary urgency, Vasodilation (similar MOA with
Ach), Reflex tachycardia, Sweating

Both are resistant to hydrolysis of Ache – longer duration of action
Carbachol – use for glaucoma as a miotic agent
Neostigmine (an indirect acting cholinomimetic) is also another drug
useful for bladder and bowel atony (non obstructive type)

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15
Q

Pilocarpine

A

Direct Acting (Muscarinic)

Cevimeline (M3 selective)

Activates M3 receptors in ciliary muscle causing contraction of ciliary
body to facilitate aqueous humor outflow and diminish its rate of
secretion; increase salivation

Glaucoma, Sjogren syndrome, Sicca Syndrome, head and neck
irradiation

Miosis, Blurring of vision, increase salivation, Hypertension (after brief
period of hypotension due to activation of sympathetic postganglionic
M1 receptors

No effect of nicotinic receptors

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16
Q

Nicotine

A

Direct Acting (Nicotinic)

Lobeline and Varenicline (selective partial agonist at nicotinic receptor with 12-24
hour duration of action)

Lobeline and Varenicline (selective partial agonist at nicotinic receptor with 12-24
hour duration of action)

Smoking cessation

Generalized ganglionic stimulation (hypertension, tachycardia, nausea, vomiting and diarrhea

Activates all autonomic post ganglionic neurons (both sympathetic and
parasympathetic, hence generalized ganglionic stimulation) and skeletal muscle nm endplates

Nicotine in the CNS is associated with greater release of dopamine in the
mesolimbic system (addicting effect)
Smoke with nicotine (non fatal dose); avoid eating (40mg/2 cigarette)
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17
Q

Low dose and initial high dose Nicotine

A

Stimulate receptors depolarization of membrane and influx of Na and Ca

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18
Q

Large dose Nicotine

A

Stimulation followed by prolonged blockade of repolarization

Receptor: becomes refractory to stimulation

Toxicity: convulsions, fasciculations, and paralysis

Treatment: Atropine for muscarinic; symptomatic
approach

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19
Q

Nicotine: PNS

A

Nicotine – same on both parasympathetic and sympathetic
•CARDIOVASCULAR –SYMPATHOMIMETIC
•GASTROINTESTINAL-PARASYMPATHOMIMETIC

•Prolonged exposure may result in depolarizing
blockade of the ganglia

Primary autoimmune autonomic failure –
example of effect suppression on nicotinic
receptor function at the autonomic ganglia

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20
Q

Nicotine: Abstinence Syndrome

A 
Irritability, restlessness,	anxiety,	
headache, insomnia, GIT upset	
increased appetite, irritability,	
restlessness,	anxiety headache,	
insomnia, GIT	upset, increased	
appetite,	craving to start smoking.

• Begins 24 hrs and last for weeks

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21
Q

Muscarinic Toxicity

A

Seen in overdosage of muscarinic agonist and in types of
mushroom (Inocybe); Amanita muscaria

Atropine (Cholinergic antagonist)

CNS stimulation, miosis, blurring of vision, bronchoconstriction,
excessive gastrointestinal and genitourinary smooth muscle
activity, increase secretory activity of the sweat glands, airway,
gastrointestinal tract, lacrimal glands; vasodilation

Symptoms of muscarinic poisoning is essentially similar with
organophosphate poisoning minus symptoms of nicotinic excess

In organophosphates: they are long acting acetylcholinesterase
inhibitor or indirect acting cholinomimetic

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22
Q

Mushroom Poisoning Rapid oneset

A 
RAPID	ONSET
15-30	MIN	AFTER	INGESTION
SIGNS	OF	MUSCARINIC	EXCESS	OR	MUSCARINIC	
SUPPRESSION
ATROPINE	1-2	MG	IS	RECOMMENDED
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23
Q

MP Delayed onset

A

6-12 HRS

HEPATIC AND RENAL CELL INJURY ATROPINE NOT RECOMMENDED

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24
Q

Edrophonium

A

Cholinomimetic (Indirect acting – Alcohol)

Inhibits acetylcholinesterase. Amplified endogenously released acetylcholine

Myasthenia gravis (diagnosis: tensilon test)
Differentiation of cholinergic crisis and myasthenic crisis
Reversal of neuromuscular blockade

Miosis, Salivation, Nausea, Vomiting, Diarrhea,
Bradycardia

IV, very short lived; 5-15 mins duration of action

25
Q

Neostigmine

A

Cholinomimetic (Indirect acting – Alcohol)

Pyridostigmine, Physostigmine, Ambenonium, echothiophate
(organophosphate)

Indirect acting

Inhibits acetylcholinesterase. Amplifies endogenously released acetylcholine

Myasthenia gravis (treatment); reversal of nondepolarizing neuromuscular
blockade (Neostigmine), Glaucoma (Physostigmine, Echothiophate), Bladder
and Bowel atony (Neostigmine)

Miosis, Salivation, Nausea, Vomiting, Diarrhea, Bradycardia (need to coadministering Atropine in toxicity)

Muscarinic effects are blocked by Atropine
Neostigmine: poor lipid solubility, oral. DOA: 30mins-2 hours
Pyridostigmine: poor lipid solubility, oral. DOA: 4-8 hours
Echothiophate: moderate lipid solubility. DOA: 2-7 days

26
Q

Myasthenia Gravis

A

Autoimmune destruction of nicotinic Ach receptors characterized by
fluctuating muscle weakness, ocular symptoms, bulbar symptoms
and proximal muscle weakness

27
Q

Myasthenic Crisis

A

acute worsening of symptoms due to infection,

stress or undermedication

28
Q

Cholinergic Crisis

A

excessive activation of cholinoceptors (skeletal

muscle weakness and parasympathetic signs) due to overmedication

29
Q

Muscarinic excess:

A

Nausea, vomiting, diarrhea, urinary urgency,
vasodilation, reflex tachycardia, sweating, salivation
and bronchoconstriction

30
Q

Rivastigmine

A

Cholinomimetic (Indirect acting – Alcohol)

Galantamine, Donezepil, Tacrine

Inhibits acetylcholinesterase. Amplifies endogenously released
acetylcholine

Alzheimer’s Disease

Miosis, Salivation, Nausea, Vomiting, Diarrhea, Bradycardia (need
to co-administer Atropine in toxicity)

Rivastigmine as transdermal patch
Donezepil combined with Memantine for Alzheimer’s Disease

31
Q

Organophosphate poisoning

A 
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation (Skeletal muscle	and	CNS)
Lacrimation
Sweating
Salivation
32
Q

Pralidoxime: for Organophosphate Poisoning

A

Cholinesterase regenerator, Antidote

Binds phosphorus of organophosphate. Breaks
organophosphate bond with cholinesterase. (regenerates
active acetylcholinesterase)

Antidote for early stage cholinesterase inhibitor poisoning
(organophosphate poisoning and nerve gas poisoning); can
relieve skeletal muscle and endplate block

Address both muscarinic and nicotinic symptoms
Must be administered before 6-8 hours of
organophosphate bond with cholinesterase occurs (before
the bond has aged (AGING) or turned into covalent bond:
Has oxime group which has high affinity for phosphorus

33
Q

Atropine for Organophosphate Poisoning

A

Cholinergic antagonist (muscarinic)

Competitively blocks all muscarinic receptors

Mydriatic, cycloplegic, antidote for organophosphate poisoning
(first choice), Bradycardia, Hypersalivation, Decreased airway
secretion during general anesthesia

Mydriasis, Tachycardia, Cycloplegia, Skin Flushing, Delirium,
Hallucinations, Urinary retention, Constipation

Only muscarinic symptoms are reversed. No effect on the nicotinic
signs of toxicity
Notorious for causing hyperthermia in susceptible patients because
Atropine suppressed thermoregulatory sweating

34
Q

Antimuscarinic Agents

A 
Atropine
Benztropine
Cyclopentolate
Darifenacin
Fesoterodine
Ipratropium
Oxybutynin
Scopolamine
Solifenacin
Tiotropium
Tolterodine
Trihexyphenidyl
Tropicamide
Trospium chloride
35
Q

Ganglionic

Blockers

A

Nicotine
Hexamthonium
Mecamylamine

36
Q

Neuromuscular

Blockers

A 
Cisatracurium
Pancuronium
Rocuronium
Succinylcholine
Vecuronium
37
Q

Antimuscarinic M1 selective

A

Pirenzepine

38
Q

Nonselective Antimuscarinic

A

Atropine

39
Q

Antinicotinic Ganglionic blocker

A

Hexamethonium

40
Q

Neuromuscular blockers Antinicotinic

A

Tubocurarine

41
Q

AChE Regenerator oximes

A

Pralidoxime

42
Q

Atropine

ATROPA BELLADONA
DATURA STRAMONIUM

A

Cholinergic antagonist (muscarinic)

Homatropine, Cyclopentolate, Tropicamide

Competitively blocks all muscarinic receptors (salivary, bronchial
and sweat glands)

Mydriatic – from unopposed sympathetic dilator activity

Cycloplegia – due to weakness of ciliary muscle contraction; loss of
accommodation – no near vision focus

Antidote for organophosphate poisoning (1st choice, addressing
muscarinic excess), Bradycardia, Hypersalivation

Mydriasis, Tachycardia, Cycloplegia, Skin Flushing, Delirium,
Hallucinations, Urinary retention, Constipation, Dry eyes “Sandy
Eyes”

Cross BBB, just like physostigmine (an indirect-acting cholinomimetic)

43
Q

Atropine Effects

A

CVS
• Low doses: Initial bradycardia (autoreceptors, M3)
• Moderate to high: tachycardia
• Little effect on blood pressure

LUNGS
• Limited use: Block of M2 receptors in postganglionic
parasympathetic fibers versus block in the M3
receptors in airway smooth muscle
• Valuable in some patients with asthma and in many
COPD patients

44
Q

Benztropine

A

Cholinergic antagonist (muscarinic)

Biperiden, Trihexylphenidyl

Competitive blocks all muscarinic receptors
Restores neurotransmitter balance in the basal ganglia

Parkinson’s Disease

Blurring of vision, Dry eyes, Constipation, Dry mouth, Urinary
retention

The tremors associated with Parkinson disease is a result of relative
excess of cholinergic activity due to the deficiency of dopamine
activity in the basal ganglia stratum system. The role of cholinergic
antagonism is for tremor/rigidity improvement

45
Q

Ipratropium

A

M receptor antagonist
Tiotropium, Glycopyrronium, Aclidinium, Umeclidinium

Blocks muscarinic receptors in bronchial smooth muscle.
Prevents vagal-stimulated bronchoconstriction

Acute asthma, COPD

Dry mouth, Blurred vision, includes all anti-cholinergic effects

Less toxic than beta agonist
Tiotropium and Umeclidinium have longer DOA.
Has no effect of the chronic inflammation aspect of asthma
Glycopyrronium – for COPD; anti-spasmodic and reduce salivation
Tiotropium – adjunct in pulmo rehab (increase exercise tolerance)

46
Q

Scopolamine

A

Cholinergic antagonist (muscarinic)

Competitively blocks all muscarinic receptors Antagonizes histamine and serotonin

Motion sickness (M3 and M4 receptors), Decrease acid secretion in the GIT, Nausea and Vomiting

Drowsiness, Amnesia, Sedation, Blurring of vision, Dry
eyes, Constipation, Dry mouth, Urinary retention

For motion sickness, available in patch
Other name: hyoscine
Highest propensity to cause CNS symptoms compared to
all other anticholinergics

47
Q

Scopolamine: Indication

A

MOTION SICKNESS

  • Certain vestibular disorder and production of endolymph
  • Scopolamine is one of the oldest remedies
  • Given by IV or oral
  • Patch with 48 to 72 hr effect
  • Sedation and dry mouth
  • OPHTHALMOLOGIC DISORDER
  • EXAMINATION OF RETINA (Mydriasis)
  • FUNDOSCOPIC EXAM (Cycloplegia)
  • Eye drops or ointment
  • RESPIRATORY
  • Pre medication: atropine or scopolamine
  • Ipratropium: synthetic analog of atropine
  • tiotropium
48
Q

Dicyclomine

A

Cholinergic antagonist (muscarinic)

Hyoscyamine, Glycopyrrolate

Competitively blocks muscarinic (M3) receptors

Inflammatory bowel disease, diarrhea, decrease acid secretion in GIT

Tachycardia, confusion, urinary retention, relative contraindicated
in patients with Glaucoma (increase intraocular pressure)

Quarternary amines, action remains on the periphery Unlike tertiary amines, like atropine, scopolamine can act centrally
as the cross the BBB

49
Q

Oxybutynin

A

Cholinergic antagonist (muscarinic)

Darifenacin, Solifenacin, Tolterodine, Trospium, Imipramine, Fesoterodine

Slightly blocks M3 receptors
Reduces detrusor muscle tone

Urge incontinence, Post-operative bladder spasms (Prostatectomy)

Tachycardia, Constipation, Xerostomia, Increased IOP

May cause pruritus (available in patch)
Imipramine – tricyclic antidepressant with strong antimuscarinic Darifenacin and Solifenacin – M3 greater selectivity

50
Q

Scopolamine: Indication Gut

A 
INFLAMMATORY	BLADDER	DISORDER
• BLADDER	SPASM(Oxybutinin:M3)
• UROLITHIASIS
• Involuntary	voiding	in	children
• Trospium	(nonselective)
• Darifenacin	and	Solifenacin
• Tolterodine	and	Fesoterodine
• Urinary	incontinence
51
Q

Atropine Toxicity

A
  • Signs/Symptoms – Hot as a hare, Dry as a bone, Red as a beet, blind as a bat and Mad as a hatter
  • Caution use in infants (sensitive to atropine, hyperthermia effect)
  • Can aggravate acute angle-closure glaucoma (mydriasis effect)

• Can precipitate further retention in patients with benign prostatic hyperplasia (relaxation of smooth muscle of
ureter and bladder wall

52
Q

Hexamethonium

A

Cholinergic antagonist (Nicotinic)

Trimetaphan (blocks the receptor), Mecamylamine

Competitively blocks Nn nicotinic receptors

Hypertension (obsolete), Hypertensive emergencies

Postural hypotension, Dry mouth, Blurred vision,
Constipation, Sexual dysfunction, Tachycardia

Hemicholinium – blocks choline uptake (synthesis)
Hexamethonium – blocks the ion channel

53
Q

Neuromuscular Blocking Drugs

A

Skeletal muscle relaxants

54
Q

Nondepolarizing Drugs NMB

A
  • Tubocurarine
  • Pancuronium
  • Atracurium
  • Vecuronium
55
Q

Depolarizing Drugs NMB

A

Succinylcholine

56
Q

Succinylcholine

A

Depolarizing neuromuscular blocker

Short acting
6-11 mins in duration; 60-90 seconds in onset

Agonist at Ach-N receptors causing initial twitch (transient

contractions) then persistent depolarization (flaccid
paralysis) then followed by repolarization (paralysis)

Skeletal muscle relaxant during intubation and GA

Postop muscle pain, increased intragastric pressure
(aspiration risk) increased IOP; Malignant Hyperthermia

Dantrolene - antidode

57
Q

Antimuscarinic Agents

A 
Atropine
Benztropine
Cyclopentolate
Darifenacin
Fesoterodine
Ipratropium
Oxybutynin
Scopolamine
Solifenacin
Tiotropium
Tolterodine
Trihexyphenidyl
Tropicamide
Trospium chloride
58
Q

Ganglionic

Blockers

A

Nicotine
Hexamthonium
Mecamylamine

59
Q

Neuromuscular

Blockers

A 
Cisatracurium
Pancuronium
Rocuronium
Succinylcholine
Vecuronium

Pharmacology (19 decks)

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