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Therapeutics I > Cholinergic Agents > Flashcards

Cholinergic Agents Flashcards

1
Q

parasympathetic direct agonist activates what

A

cholinoreceptors

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2
Q

parasympathetic indirect agonist stimulate the release of what

A

acetylcholine

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3
Q

parasympathetic indirect agonists inhibit what

A

acetylcholinesterase

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4
Q

Acetylcholine Biosynthesis & Neurotransmission

how is choline transported into the presynaptic nerve terminal?

A

by a sodium-dependent choline transporter (CHT)

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5
Q

Acetylcholine Biosynthesis & Neurotransmission

what transporter can be inhibited by hemicholinium

A

sodium-dependent choline transporter (CHT)

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6
Q

Acetylcholine Biosynthesis & Neurotransmission

what enzyme synthesizes choline and acetyl-coa into acetylcholine

A

choline acetyltransferase (ChAT)

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7
Q

cholinergic agonists are mostly (muscarinic/nicotinic)

A

muscarinic

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8
Q

what is special about quaternary amines

A

positive charge

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9
Q

State which receptor affects the following:
Bradycardia

A

M2, binds in the heart

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10
Q

State which receptor affects the following:
Nausea, cramps, vomiting, diarrhea

A

M3: bronchiolar smooth muscle

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11
Q

State which receptor affects the following:
visual disturbances

A

M1

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12
Q

T/F: Charged Muscarine has easy access into the BBB

A

F

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13
Q

what are the two main classes of direct acting cholinergic agonists

A

choline esters, alkaloids

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14
Q

what are the four direct acting choline esters

A

ACh, methacholine, carbachol, bethanechol

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15
Q

what are the two direct acting alkaloids

A

muscarine, pilocarpine

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16
Q

what are the 3 reversible indirect-acting cholinergic agonists

A

edrophonium, physostigmine, neostigmine

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17
Q

what is the irreversible indirect-acting cholinergic agonist

A

organophosphates

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18
Q

another name for direct acting cholinergic agonists

A

muscarine receptor agonists

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19
Q

another name for indirect-acting cholinergic agonists

A

AChE inhibitors

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20
Q

what is the effect of M2 activation on the heart

A

Decrease in heart rate, (bradycardia)

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21
Q

what is the effect of M3 activation on exocrine glands

A

increase in secretion

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22
Q

what is the effect of M3 activation on smooth muscles

A

increase in contraction

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23
Q

what is the effect of M3 on sphincters

A

relaxation

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24
Q

CNS effects are mainly mediated by which muscarinic receptor

A

M1

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25
Q

T/F Carbachol (a direct acting cholinoceptor agonist) is resistant AChE

A

True

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26
Q

other name for pilocarbine

A

isoptocarpine

27
Q

pilocarbine is used for the treatment of what

A

glaucoma

28
Q

T/F Pilocarbine cannot cross the BBB

A

F

29
Q

what receptor does pilocarpine target and is it an agonist or antagonist

A

M3, agonist

30
Q

what receptor does brimonidine target and is it an agonist or antagonist

A

alpha2, agonist

31
Q

what receptor does timolol target and is it an agonist or antagonist

A

NE-beta, antagonist

32
Q

what is classified as increased intraocular pressure

A

glaucoma

33
Q

carbachol binds with which receptor(s)

A

muscarinic, nicotinic

34
Q

pilocarpine binds with which receptor(s)

A

muscarinic

35
Q

bethanechol binds with which receptor(s)

A

muscarinic

36
Q

varenicline binds with which receptor(s)

A

nicotinic

37
Q

which drug is used for the following clinical use: Intraocular use for miosis during surgery

A

acetylcholine

38
Q

which drug is used for the following clinical use: intraocular use for miosis during surgery, glaucoma

A

carbachol

39
Q

which drug is used for the following clinical use: glaucoma

A

pilocarpine

40
Q

which drug is used for the following clinical use: urinary retention, post operative ileus

A

bethanechol

41
Q

which drug is used for the following clinical use: smoking cessation

A

varenicline

42
Q

which of the following drugs has cholinesterase sensitivity?
a. acetylcholine
b. carbachol
c. pilocarpine
d. bethanechol
e. varenicline

A

a. acetylcholine

43
Q

M2 effect on cardiovascular

A

fall in blood pressure and heart rate

44
Q

M3 effect on gastrointestinal

A

smooth muscle contraction/ sphincter relax

45
Q

M3 effect on bladder

A

smooth muscle contraction/ sphincter relax

46
Q

M3 effect on eye

A

miosis

47
Q

M3 effect on sweating

A

increase

48
Q

match the drug with the clinical use: open-angle glaucoma; dry mouth due to hypofunction of salivary glands e.g. Sjogren’s or cancer radiotherapy
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol

A

pilocarpine

49
Q

match the drug with the clinical use: GI stimulation or treatment of urinary retention
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol

A

bethanechol

50
Q

match the drug with the clinical use: provocative test for hyperactive airways
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol

A

methacholine

51
Q

match the drug with the clinical use: ocular (surgery, glaucoma)
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol

A

carbachol

52
Q

which cholinoreceptor is found at the skeletal muscle endplate

A

Nm

53
Q

Which cholinoreceptor is found in autonomic ganglia

A

NN

54
Q

which cholinoreceptor is found in the brain

A

NN

55
Q

what does dibasic mean

A

2 nitrogens

56
Q

effects of nicotine in low doses

A

stimulate reticular activating system (alerting) and dopamine release (addictive)

57
Q

effects of nicotine in higher doses

A

CV effects (hypertension, tachycardia)

58
Q

effects of nicotine in toxic doses

A

seizures, loss of receptor selectivity, neuromuscular blockade

59
Q

what drug is often prescribed for intervention of nicotine dependence

A

Varenicline (chantix)

60
Q

mechanism of chantix

A

an α4β2 neuronal nicotinic receptor partial agonist that binds in the central nervous system

61
Q

what is the half life of varenicline (chantix) and how does it get excreted?

A

24 hours, urine

62
Q

what are the adverse effects of varenicline (chantix)

A

nausea, headache, abnormal dreams, constipation, vomiting

63
Q

what are the four forms of nicotine replacement therapy

A

Nicotrol inhaler, nicotrol nasal spray, nicorette gum, nicoderm transdermal patch

64
Q

what disease states are a hypofunction of salivary glands

A

xerostomia and Sjogren’s syndrome

Therapeutics I (4 decks)

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