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FTM > Cholinergic Agonists > Flashcards

Cholinergic Agonists Flashcards

1
Q

Direct-acting Agonist

A

Bind to and activate Muscarinic or nicotinic receptors

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2
Q

Indirect-acting Agonist

A

Inhibit acetylcholinesterase

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3
Q

Direct effect of Acetylcholine

A

Vasodilation(M3 effect)

Decrease in cardiac rate(M2 effect)

Decrease in rate of conduction in the S.A and AV node (M2 effect)

Decrease in the force of contraction

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4
Q

What is the effect of Acetylcholine on Vasculature/endothelial cells?

A

Release of Nitric Oxide and vasodilation

Decrease in Blood pressure

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5
Q

What is the effect of Acetylcholine on Eye Iris?

A

Miosis- Constriction

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6
Q

What is the effect of Acetylcholine on Ciliary muscle?

A

accommodation of lens to near vision

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7
Q

What is the effect of Acetylcholine on Salivary/sweat/lacrimal glands?

A

inc in secretions

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8
Q

What is the effect of Acetylcholine on Bronchi?

A

constriction

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9
Q

What is the effect of Acetylcholine on heart?

A

Dec. Heart rate Dec conductance velocity

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10
Q

What is the effect of Acetylcholine on GI Tract?

A

Inc tonic and peristaltic activity

relaxation of sphincter

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11
Q

What is the effect of Acetylcholine on Urinary bladder?

A

Contraction of detrusor muscle

relaxation of sphincter

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12
Q

What are the two types of direct acting cholinergic Agonists?

A

Esters of choline and Alkaloids

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13
Q

What are the Choline esters

A

Acetylcholine
methacholine
Bethanecol

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14
Q

properties of Choline esters

A

Quaternary ammoniums

Poorly absorbed and distributed into the CNS

Acetylcholine is rapidly hydrolyzed

Methacholine and bethanecol more resistant to hydrolyzation

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15
Q

uses of Acetylcholine

A

Obtain miosis after delivery of the lens in cataract surgery and other procedures where rapid miosis is required

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16
Q

uses of Methacholine

A

Diagnosis of bronchial airway hyperactivity in subjects who do not have clinically apparent asthma

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17
Q

uses of Bethanecol

A

postoperative urinary retention

atony(lack of physiological tone especially of a contractile organ.) of the urinary bladder

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18
Q

What are the natural alkaloids

A

Pilocarpine and nicotine

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19
Q

Pilocarpine

A

Partial muscarinic agonist

Tertiary amine

stable to hydrolysis by acetylcholinesterase

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20
Q

uses of pilocarpine

A

Glaucoma

Treatment of dry mouth due to radio therapy for cancer of head and neck

21
Q

Adverse effects of muscarinic agonists

A 
sweating
salivation
flushing
low blood pressure 
nausea
abdominal pain
diarrhea 
bronchospasm
22
Q

Nicotine

A

tertiary amine

agonist at nicotinic receptors

depending on the doses can either be stimulating or cause paralysis

23
Q

Nicotinic action at low doses

A

ganglionic stimulation via depolarization

24
Q

Nicotinic action at high doses

A

ganglionic blockade and neuromuscular blockade

25
Q

What are the anticholinesterases?

indirect acting cholinergic agents

A

Edrophonium -binds reversibly to the active site
carbamates- forms a covalent bond with the enzyme
organophosphates- phosphorylate enzyme and covalent bond formed is very stable

26
Q

what is the mechanism of action for anticholinesterases?

A

inhibit cholinesterase.

increase in the concentration of endogenous acetylcholine

27
Q

uses of Edrophonium

A

Diagnosis of myasthenia gravis

reverse the neuromuscular block produced by non-depolarizing muscular blockers

28
Q

uses of Physostigmine

A

Treatment of overdoses of anticholinergic drugs

29
Q

uses of neostigmine

A

urinary retention

cholinesterase inhibitor

reversal of effects of nondepolarizing neuromuscular blockers after surgery

Treatment of myasthenia gravis

30
Q

uses of pyridostigmine

A

treatment of myasthenia gravis

Cholinesterase inhibitor

31
Q

Malathion

A

used in pesticides/insecticides

32
Q

Sarin

A

potent synthetic toxic agents

biowarfare bombs

33
Q

Atropine

A

Reversible competitive antagonist at muscarinic receptors

Tertiary amine: both central and peripheral muscarinic blocker

34
Q

Atropine action on : eye

A

Mydriases(dilation) and cycloplegia(focus on distant objects)

35
Q

Atropine action on : GI

A

reduces gastric motility

36
Q

Atropine action on : Urinary Tract

A

decreases hypermotility of urinary bladder (M3 Blockade)

37
Q

Atropine action on : CV system

A

Atrial M2 Blockade- moderate to high therapeutic doses cause tachycardia

38
Q

Atropine action on : Secretion

A

M3 blockade- Salivary, sweat, and lachrymal glands are blocked.

inhibition of sweat glands can lead to high body temp

39
Q

Atropine uses

A

Antidote for cholinergic agonists

block respiratory tract secretion prior to surgery

40
Q

Atropine adverse effects

A

Drymouth, blurred vision sandy eyes , tachycardia, constipation, urinary retention

effect on CNS: restlessness, confusion, hallucinations, delirium

41
Q

Uses of Scopolamine

A

Prevention of motion sickness

42
Q

Ipratropium

A

used in the treatment of chronic obstructive pulmonary disease and asthma

43
Q

tropicamide

A

used as mydriatic for fundoscopy

produces mydriasis with cycloplegia

44
Q

What is the contraindication of antimuscarinic agent?

A

If the patient has angle-closure glaucoma

if the patient has prostatic hypertrophy and is elderly

45
Q

Ganglionic blocker

A

Remove the dominant control

may occur by prolonged depolarization or antagonism of nicotinic receptors

46
Q

Uses of ganglion blocker

A

Hexamethonium was used for hypertension in the past

Replaced because of their adverse effects

47
Q

Tubocurarine

A

nondepolarizing blocker

competitive agonist

use: as adjuvant drug in anesthesia during surgery to relax skeletal muscle

48
Q

Succinylcholine

A

Depolarizing blocker- done by binding to nicotinic receptor and depolarizing the junction.

leads to flaccid paralysis

Used in rapid endotracheal intubation

49
Q

botulinum toxin

A

injected locally into muscle for treatment of several diseases involving muscle spasm

inhibitor of acetylcholine release

FTM (13 decks)

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