Cholinergic Pharmacolgy II Flashcards

0
Q

What nicotinic antagonist historically was used extensively for chronic hypertension largely supplanted by adrenergic receptor-selective agents, some limited specific uses in CV regulation?

A

Hexamethonium

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1
Q

What drug blocks ANS functioning by deducing which branch SNS or PNS exercises dominant control of various organs?

A

Hexamethonium

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2
Q

What nicotinic antagonist was used for centuries along the amazon and Orinoco rivers to immobilize and paralyze wild animals and cause death from paralysis of skeletal muscle? (Not well absorbed through GI tract so possible to use it for hunting and then eat animal)

A

Curare

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3
Q

What nicotinic receptor antagonist blocks function at the NMJ, active components of curare extracts, and has a very long duration of action?

A

D-tubocurarine

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4
Q

What nicotinic antagonist causes motor weakness giving way to total flaccid paralysis, effects small rapidly moving muscles first (eyes, jaws, larynx), then limbs and trunk and then intercostal muscles and diaphragm, after drug removal recovery goes in reverse order?

A

D-Tubocurarine

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5
Q

What depolarizing blocking agent is essentially to ACh molecules linked together, actively excites receptor but has no way of turning signal off so results in flaccid paralysis, not degraded by AChE but is rapidly degraded by BChE?

A

Succinylcholine

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6
Q

What drugs can be used in surgery for relaxation of skeletal muscle to facilitate operative manipulations particularly abdominal and short duration blockers for intubation, bronchoscopy, esophagoscopy?

A

Tubocurarine derivatives and succinylcholine

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7
Q

What drug us used to treat focal dystonia by persistent inhibition of ACh release from neurons supplying skeletal muscle?

A

Botulinum toxin (Botox)

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8
Q

What is an example of a quaternary alcohol AChE inhibitor that uses electrostatic binding, short lived for 2-10min and used in the diagnoses of MG?

A

Edrophonium

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9
Q

What are the 3 groups of AChE inhibitors?

A

Quaternary alcohol, carbamate esters, organophosphates

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10
Q

What are 3 examples of carbamate ester AChE inhibitors that use covalent bonding and are long lived up to 6hr?

A

Neostigmine, physostigmine, pyridostigmine

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11
Q

What are 3 examples of organophosphate AChE inhibitor, that are extremely stable and can bind as long as 100hrs and are irreversible after aging?

A

Malathion, parathion, echothiophate

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12
Q

What agent can push and organophosphate AChE inhibitor off the binding cleft before aging?

A

Pralidoxime

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13
Q

What are some therapeutic uses of AChE inhibitors?

A

MG, atony or urinary bladder, paralytic ileus, glaucoma, muscarinic antagonist poisoning

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14
Q

What is used to differentiate between MG and cholinergic crisis?

A

Endrophonium

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15
Q

Skeletal muscle weakness due to depolarization of motor end plate by high concentrations of ACh (ex: ChE inhibitor overdose) describes what?

A

Cholinergic crisis

16
Q

If edrophonium causes further weakness then what is the prognosis?

A

Cholinergic crisis

17
Q

If edrophonium improves muscle strength than what is the prognosis?

A

MG

18
Q

What two drugs can be used to treat MG and increase response to myasthenic muscle to repetitive nerve impulses, preservation of endogenous ACh and step wise increase of dosage to find optimal dosage?

A

Neostigmine, pyridostigmine

19
Q

What are 3 possible ways to be exposed to AChE inhibitor toxicity?

A

Side effect of ChE inhibitor therapy, accidental exposure (insecticide spraying), warfare agents

20
Q

What are 3 AChE inhibitor warfare agents?

A

Sarin, Vx, Soman

21
Q

What warfare agent is volatile and mainly has inhalation exposure?

A

Sarin

22
Q

What warfare agent is very persistent can remain on the body, terrain for extended periods of time, mainly has skin exposure but also through inhalation?

A

Vx

23
Q

What warfare agent is moderately volatile inhalation or skin contact very rapid “aging” occurs in minutes?

A

Soman

24
Q

In general what kind of effects do AChE inhibitors amplify?

A

PNS

25
Q

What drug helps alleviate symptoms of AChE inhibitor toxicity by binding reversibly to AChE molecules and releasing them when it’s effects wear off, protects from irreversible binding of nerve gas agents (used extensively as prophylactic agents during 1990-1991 gulf war)?

A

Pyridostigmine

26
Q

What are 4 treatments of AChE inhibitor toxicity?

A

Pyridostigmine, heroic doses of atropine, pralidoxime, artificial respiration and anticonvulsants

27
Q

What drug is effective for PNS effects induced by nerve gas agents but is ineffective against skeletal muscle neuromuscular effects?

A

Atropine

28
Q

What drug will effectively reverse all symptoms by regenerating AChE has been used as prophylactic agent for agricultural workers however must be applied before aging or organophosphate inhibitors?

A

Pralidoxime

29
Q

What can be used incase of several AChE inhibitor intoxication?

A

Artificial respiration and anticonvulsants