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Neuro II > Cholinergic Agonists and Antagonists > Flashcards

Cholinergic Agonists and Antagonists Flashcards

1
Q

Acetycholine

A

Direct acting cholinomimetic

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2
Q

Bethanechol

A

direct acting cholinomimetic

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3
Q

Carbachol

A

direct acting cholinomimetic

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4
Q

Civemeline

A

direct acting cholinomimetic

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5
Q

Methacholine

A

direct acting cholinomimetic

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6
Q

Pliocarpine

A

direct acting cholinomimetic

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7
Q

Varenicline (Chantix)

A

direct acting cholinomimetic

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8
Q

Ambenonium

A

Cholinisterase inhibitor

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9
Q

Donepezil

A

Cholinesterase inhibitor

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10
Q

Echothiophate

A

Cholinesterase inhibitor

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11
Q

Edrophonium

A

Cholinesterase inhibitor

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12
Q

Galantamine

A

Cholinesterase inhibitor

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13
Q

Neostimine

A

Cholinesterase inhibitor

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14
Q

Physostigmine

A

Cholinesterase inhibitor

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15
Q

Pyridostigmine

A

Cholinesterase inhibitor

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16
Q

Rivastimine

A

Cholinesterase inhibitor

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17
Q

Tacrine

A

Cholinesterase inhibitor

18
Q

Pralidoxime

A

Cholinesterase regenerator

19
Q

Antimuscarinic drugs used for motion sickness

A

Scopolamine

20
Q

Antimuscarinic drugs for GI disorders

A

Atropine
Dicyclomine
Glycopyrrolate
Hyoscyamine

21
Q

Antimuscarinic drugs used in ophthamology

A 
Atropine
Cyclopentolate
Homatopine
Scopolamine
Tropicamide
22
Q

Antimuscarinic drugs used for respiratory disorders (asthma, COPD)

A

Ipratropium

Tiotropium

23
Q

Antimuscarinic drugs used for urinary disorders

A 
Darifenacin
Fesoterodine
Oxybutynin
SOlifenacin
Tolterodine
Trospium
24
Q

Antimuscarinic drugs used for cholinergic poisoning

A

Atropine (+ pralidoxime)

25
Q

Antimuscarinic Drugs used for movement disorders

A 
Benztropine
Biperiden
Orphenadrine
Procyclidine
Trihexyphenidyl
26
Q

Ganglion blockers

A

Mecamylamine

27
Q

Choline esters and alkaloids are what type of drugs

A

Direct acting cholinergic agonists

28
Q

Choline esters MOA

A

Act as agonists on cholinergic receptors

29
Q

Choline esters eg

A

acetylcholine

carbachol, bethanechol

30
Q

Choline esters absorption, distribution and metabolism

A

permanently charged quartenary ammonium groups that result in poor absorption and distribution into the CNS

Hydrolyzed in the GI tract, less active when given by mouth

Hydrolysed by cholinesterase but at different rates –> varrying durations of action

31
Q

Alkaloid MOA

A

acts as agonist on cholinergic receptors

32
Q

Alkaloids eg

A

muscarine, nicotine, pliocarpine

33
Q

Hydrolyzation speeds of choline esters by cholinesterase

A

most rapid: acetylcholine > methacholine> carbachol=bethanechol : least rapid

34
Q

Alkaloids absorption, distribution and metabolism

A

uncharge tertiary amines (muscarine is an exception). well absorbed from most sites of administration

muscarine is a quartenary amine, is highly toxic when ingested, and can enter the brain (musrooms)

Cheifly excreted by the kidneys; acidification of the urine accelerates clearance.

35
Q

M1, M3, M5

A

Gq, stimulatory, Ip3 DAG cascade
Nerves (M1)
Glands, smooth muscle, endothelium, (M3)
CNS (M5)

36
Q

M2, M4

A

Gi, inhibitory, inhibition of cAMP production (activation of K+ch in M2)
M2 - heart, nerves, smooth muscle
M4 - CNS

37
Q

Nicotinic receptors

A

Nm - skeletal NMJ
Nn - postganglionic cell body, dendrites, cns

Na, K depolarizing ion channel

38
Q 
Organ system effects of the direct acting cholinergic agonists
Skeletal muscle (somatic effects)
A

only nACHRs ar on skeletal muscle, so only those agents that activate nACHR will produce any effect (muscle contraction)

Prolonged agonist occupancy of the nACHr abolishes the effector response: the postganglionic neuron stops firing and the skeletal muscle cell relaxes (similar to succiylcholine)

Eventually a state of depolarizing blockade is produced (flaccid paralysis)

Nicotine itself has a greater affinity for neuronal nACHRs than skeltal muscle nACHRs

39
Q

Organ system effects of the direct acting cholinergic agonists
Eye

A

Contraction of iris sphincter and ciliary muscle –> increased aqueous humor outflow into canal of Schlemm

40
Q

Organ system effects of the direct acting cholinergic agonists
Cardiovascular system

A

M2 mACHR

reduction in peripheral vascular resistance and changes in HR

Neuro II (10 decks)

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