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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
Neostigmine
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
Myasthenia Gravis
Autoimmune destruction of nicotinic Ach receptors characterized by fluctuating muscle weakness, ocular symptoms, bulbar symptoms and proximal muscle weakness
27
Myasthenic Crisis
acute worsening of symptoms due to infection, | stress or undermedication
28
Cholinergic Crisis
excessive activation of cholinoceptors (skeletal | muscle weakness and parasympathetic signs) due to overmedication
29
Muscarinic excess:
Nausea, vomiting, diarrhea, urinary urgency, vasodilation, reflex tachycardia, sweating, salivation and bronchoconstriction
30
Rivastigmine
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
Organophosphate poisoning
``` Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation (Skeletal muscle and CNS) Lacrimation Sweating Salivation ```
32
Pralidoxime: for Organophosphate Poisoning
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
Atropine for Organophosphate Poisoning
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
Antimuscarinic Agents
``` Atropine Benztropine Cyclopentolate Darifenacin Fesoterodine Ipratropium Oxybutynin Scopolamine Solifenacin Tiotropium Tolterodine Trihexyphenidyl Tropicamide Trospium chloride ```
35
Ganglionic | Blockers
Nicotine Hexamthonium Mecamylamine
36
Neuromuscular | Blockers
``` Cisatracurium Pancuronium Rocuronium Succinylcholine Vecuronium ```
37
Antimuscarinic M1 selective
Pirenzepine
38
Nonselective Antimuscarinic
Atropine
39
Antinicotinic Ganglionic blocker
Hexamethonium
40
Neuromuscular blockers Antinicotinic
Tubocurarine
41
AChE Regenerator oximes
Pralidoxime
42
Atropine ATROPA BELLADONA DATURA STRAMONIUM
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
Atropine Effects
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
Benztropine
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
Ipratropium
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
Scopolamine
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
Scopolamine: Indication
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
Dicyclomine
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
Oxybutynin
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
Scopolamine: Indication Gut
``` INFLAMMATORY BLADDER DISORDER • BLADDER SPASM(Oxybutinin:M3) • UROLITHIASIS • Involuntary voiding in children • Trospium (nonselective) • Darifenacin and Solifenacin • Tolterodine and Fesoterodine • Urinary incontinence ```
51
Atropine Toxicity
* 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
Hexamethonium
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
Neuromuscular Blocking Drugs
Skeletal muscle relaxants
54
Nondepolarizing Drugs NMB
* Tubocurarine * Pancuronium * Atracurium * Vecuronium
55
Depolarizing Drugs NMB
Succinylcholine
56
Succinylcholine
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
Antimuscarinic Agents
``` Atropine Benztropine Cyclopentolate Darifenacin Fesoterodine Ipratropium Oxybutynin Scopolamine Solifenacin Tiotropium Tolterodine Trihexyphenidyl Tropicamide Trospium chloride ```
58
Ganglionic | Blockers
Nicotine Hexamthonium Mecamylamine
59
Neuromuscular | Blockers
``` Cisatracurium Pancuronium Rocuronium Succinylcholine Vecuronium ```

Pharmacology (19 decks)

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