Cholinergic Drugs Flashcards

1
Q

Where are M1 receptors found and what second messenger pathway is activated?

A

CNS and PNS
Gq - activation of PLC which leaves PIP2 to IP3 and DAG - increasing intracellular calcium
*Ganglia

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2
Q

Where are M2 receptors found and what second messenger pathway is activated?

A

Cardiovascular system - lowers HR and BP
Gi - decrease levels of CAMP and increase levels of potassium - this leads to hyperpolarization and decreased action potentials

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3
Q

Where are M3 receptors found and what second messenger pathway is activated?

A

Smooth muscle and glands - urinary release and bronchoconstriction
Gq - activation of PLC which leaves PIP2 to IP3 and DAG - increasing intracellular calcium

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4
Q

What adrenergic receptor behaves similarly to M1 and M3 receptors?

A

Alpha 1 (Gq)

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5
Q

Describe the dose-dependent relationship between ACh concentration and effect and describe the implications

A

Lowest dose - CV effects
Smooth muscle
Ganglia and Adrenal Medulla
NMJ

*Implies that you cannot treat NMJ disease with ACh due to the immense CV effects - HR would go to zero

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6
Q

What distance exists between change centers on muscarinic receptors?

A

4.4A

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7
Q

What distance exists between change centers on nicotinic receptors?

A

5.9A

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8
Q

How are ganglia and NMJ nicotinic receptors differentiated?

A

Ganglia - 6C between N sites

NMJ - 10C between N sites

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9
Q

Describe acetylcholine including the mechanism of action and clinical uses

A

Muscarinic and Nicotinic Agonist - non-specific

Not used due to complete non-specificity and short duration of action (AChE)

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10
Q

Describe metacholine including the mechanism of action and clinical uses

A

Muscarinic agonist - beta methyl group which makes it more specific
Used as a diagnostic for asthma vs COPD
Methyl group prolongs action by hindering hydrolysis by AChE

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11
Q

Describe carbachol including the mechanism of action and clinical uses

A

Muscarinic agonist - terminal NH2 prolongs action by hindering hydrolysis by AChE
Treatment of glaucoma - reduction in intraocular pressure

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12
Q

What do all muscarinic agonists have in common?

A

4.4A between charge centers

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13
Q

What do all nicotinic agonists have in common?

A

5.9A between charge centers

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14
Q

Describe bethanechol including the mechanism of action and clinical uses

A

Muscarinic agonist - beta methyl group and terminal NH2

Treatment of decreased peristalsis after surgery - taken orally and not absorbed due to + charge - impacts intestine

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15
Q

Describe nicotine including the mechanism of action and clinical uses

A

Nicotinic agonist

Used in smoking cessation

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16
Q

What are two other names for muscarinic antagonists?

A

Anti-cholinergic

Anti-muscarinic

17
Q

Describe atropine including the mechanism of action and clinical uses

A

Muscarinic antagonist
Mainly used for CNS effects (nerve / pesticide poisoning)
Given orally or IV due to tertiary nitrogen

18
Q

Describe scopolamine including the mechanism of action and clinical uses

A

Muscarinic antagonist

Used in the treatment of motion sickness

19
Q

Describe homatopine including the mechanism of action and clinical uses

A

Muscarinic antagonist

Used to dilate pupils for retinal exams

20
Q

Describe Ipratroprium including the mechanism of action and clinical uses

A

Muscarinic antagonist - quaternary nitrogen - given via sufflation
Asthma treatment

21
Q

Describe tiotropium including the mechanism of action and clinical uses

A

Muscarinic antagonist - quaternary nitrogen - given via sufflation
Asthma treatment

22
Q

Describe Tolerodine including the mechanism of action and clinical uses

A

Muscarinic antagonist

Used to prevent bladder leakage

23
Q

Describe the general side effects of anti-cholinergic drugs

A

Dry mouth
Constipation
Increased body temperature
Blurred vision - dizziness and headache

24
Q

Describe glycopyrronium including the mechanism of action and clinical uses

A

Muscarinic antagonist

Used to treat excessive sweating

25
Q

Describe curare including the mechanism of action and clinical uses

A

NMJ blocker - muscle relaxant - decreases the EPP which prevents an action potential from firing and prevents muscle contraction
Used as an adjunct to anesthesia

10C between N sites

26
Q

Describe hexamethanium including the mechanism of action and clinical uses

A

Ganglia blockers - block PSNS, SNS, and adrenal medulla
Used historically for HTN crises - now off the market
6C between N sites

27
Q

Describe physostigmine including the mechanism of action and clinical uses

A

Inhibition of AChE - potentiates the effect of ACh

Used in treatment of glaucoma

28
Q

Describe neostigmine including the mechanism of action and clinical uses

A

Inhibition of AChE - potentiates the effect of ACh

Used in treatment of curare-induced paralysis

29
Q

Describe pyridostigmine including the mechanism of action and clinical uses

A

Inhibition of AChE - potentiates the effect of ACh

Used in treatment of myasthenia gravis

30
Q

Describe rivastigmin including the mechanism of action and clinical uses

A

Inhibition of AChE - potentiates the effect of ACh

Used in treatment of Alzheimer’s

31
Q

Describe deonepezil including the mechanism of action and clinical uses

A

Inhibition of AChE - potentiates the effect of ACh

Used in treatment of Alzheimer’s

32
Q

Describe edrophonium including the mechanism of action and clinical uses

A

Reversible Inhibition of AChE - potentiates the effect of ACh
Used in treatment of curare-induced paralysis - competitive inhibitor

33
Q

Describe organophosphates including the mechanism of action and clinical uses. Give an example.

A

Irreversible inhibitors of AChE - PO4 group replaces C=O and covalently binds serine - water cannot break this bond
Echothiophate - Used in treatment of glaucoma

34
Q

How do carbamic acid derivatives affect the cholinergic system?

A

Carbamlyate group vs acetyl group - slower for water to hydrolyze
Reversible inhibitor for AChE - potentiates the effect of ACh