Chapter 2: Cholinergic Pharmacology Flashcards

1
Q

MOA of hemocholinum.

A

blocks uptake of choline

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2
Q

MOA of botulinum toxin.

A

cleaves SNARE proteins involved in exocytosis of ACh

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3
Q

Xerostomia definition and why is this caused? (what is defective)

A

dry mouth
salivary glands don’t produce enough saliva

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4
Q

M1 and M3 correspond with what receptor pathway?

(what coupled pathway or second messenger pathway)

A

Gq coupled

increase phosphliase C > increase IP3, DAG, Ca2+

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5
Q

M2 goes through what coupled receptor pathway?

(what second messenger pathway in other words)

A

Gi coupled

dec. adenylyl cyclase > dec cAMP

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6
Q

Nn and Nm go through what G coupled receptor pathway?

A

trick question

no 2nd messengers

activation through opening of Na/K channels

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7
Q

Stem to remember muscarinic agonist

A

“chol”

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8
Q

Clinical use of bethanechol.

A

Rx: ileus (postop); urinary retention

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9
Q

Use of methacholine.

A

Dx: bronchial hyperactivity (challenge test)

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10
Q

Use of pilocarpine, cevimeline.

A

Rx: xerostomia, glaucoma (pilocarpine)

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11
Q

Stem to help you remember indirect acting cholinomimetics.

A

stigmine

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12
Q

Clinical use for edrophonium

A

Dx myasthenia gravis

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13
Q

Benefits to edrophonium typically being used as a diagnostic tool?

A

short acting

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14
Q

Clinical use of physostigmine?

A

Rx: glaucoma; antidote in atropine overdose

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15
Q

Why can physostigmine be used for atropine overdose? (characteristics that make it suitable)

A

tertiary amine
very lipid soluble
(readily enters CNS)

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16
Q

Neostigmine and pyridostigmine can be used for what?

A

ileus, urinary retention, myasthenia gravis, reversal of non depolarizing NM blockers

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17
Q

Characteristics of neostigmine and pyridostigmine that do not make it suitable for atropine overdose?

A

Quaternary amine so cannot enter CNS

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18
Q

Donepezil clinical use.

A

Rx - Alzheimers

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19
Q

Rivastigmine clinical use.

A

RX - Alzheimers

20
Q

Organophosphate use. (Name some)

A

used as insecticides (malathion, parathion) and sarin ( nerve gas)

21
Q

Some properties of donepezil and rivastigmine that make them ideal for treating Alzeihmers?

A

lipid- solubility

22
Q

Way to remember difference between physostigmine and pyridostigmine.

A

“pyro burns down”

pyro below CNS and physo above so good for atropine overdose

23
Q

DUMBBEELSS acronym use?

A

clues to tell if someone has AChE inhibitor poisoning

24
Q

Use the proper acronym to be able to tell if someone has AChE inhibitor poisoning.

A

DUMBBEELSS

diarrhea
urination
miosis
bradycardia
bronchoconstriction
emesis
excitation (CNS/muscle)
lacrimation
salivation
sweating

25
Q

What is the most deadly S/E of AChE inhibitor poisoning?

A

paralysis of diaphragm

26
Q

Use of pralidoxime.

A

Reversal of irreversible AChE inhibitors

27
Q

What is the prototype of the muscarinic receptor antagonist class?

A

atropine

28
Q

What is the characteristic of atropine that makes it a good antidote for AChE inhibitors?

A

tertiary amine; readily enters CNS

29
Q

What plant atropine derived from?

A

atropa belladonna; Jimsonweed

30
Q

Muscarinic antagonist effects on eyes?

A

mydriasis and cycloplegia

31
Q

Pharamacologic effects of muscarinic receptor anatagonists? (name 2 or 3)

A

*decrease secretions (salivary, bronchiolar, sweat)

*mydriasis and cyclopegia

*hyperthermia (with resulting vasodilation)

*tachycardia

*sedation

*urinary retention and constipation

*Behavioral: excitation and hallucinations

32
Q

Name some classes of drugs with antimuscarinic properties.

A

antihistamine (particularly the 1st generation)

tricyclic antidepressants

antipsychotics

quinidine

amantadine

meperidine

33
Q

Antidote for antimuscarinic drugs?

A

physostigmine

34
Q

Clinical use of atropine.

A

antispasmodic, antisecretory, management of AChE inhibitor OD, antidiarrheal, ophthalmology (but long action)

35
Q

Clinical use of tropicamide.

A

ophthalmology (topical)

36
Q

Clinical use of ipratropium, tiotropium. Also name some important properties to remember about these drugs. (Can they enter CNS) (How do they effect mucus viscosity)

A

asthma and COPD (inhalation) - no CNS entry, no change in mucous viscosity

37
Q

Stem to remember M blockers?

A

“trop”

38
Q

Scopolamine clinical use. Also S/E.

A

motion sickness

causes sedation and short-term memory block

39
Q

Benztropine and trihexyphenidyl clinical use.

A

lipid-soluble (CNS entry) used in Parkinson-ism and in acute extrapyramidal symptoms induced by antipsychotics

40
Q

Clinical use of oxybutinin.

A

used in overactive bladder (urge incontinence

41
Q

What makes tropicamide a more useful drug in eye exams than atropine.

A

causes less sustained dilation of pupils because of its short half-life

42
Q

What are ganglion blockers also typically named?

A

nicotinic receptor antagonist

43
Q

What are 2 ganglion blockers not used today but that this chapter covered?

A

hexamethonium. and mecamylamine

44
Q

Ganglion blockers have what effect that can be useful?

A

they block reflexes

45
Q

Which receptors are stimulated for direct action on HR?

A

M2 and B1

46
Q

What receptors are stimulated for indirect effect on HR causing reflex Brady or tachy?

A

a1 (vasoconstriction) and B2 (vasodilation)