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NS Receptors & Drugs > Drugs & Receptors > Flashcards

Drugs & Receptors Flashcards

1
Q

Muscarinic effects on:heart

A

decrease HR, contractility, conduction at AV node

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2
Q

M on blood vessels

A

vasodilation, not innervated

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3
Q

m on blood pressure

A

hypotension

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4
Q

m on lungs

A

bronchoconstrictionsecretions

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5
Q

m on eye

A

miosis, accomodation, increase aqueous humour outflow (good for glaucoma), tears

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6
Q

m on GI/GU

A

increase salivationopen sphincter and increase detrusorincrease motilitystimulates erection

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7
Q

nicotinic on NMJ

A

muscle contraction

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8
Q

m on CNS

A

memory, cognition, movement

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9
Q

a1 on eye

A

pupil dilates

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10
Q

b2 on trachea and bronchioles

A

dilates

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11
Q

b1 on kidney

A

increases secretion of renin

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12
Q

a1 on kidney

A

decreases secretion of renin

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13
Q

a1/b2 on bladder

A

contraction of trigone and sphincter, relaxes detrusor

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14
Q

a1 on male genetalia

A

stimulates ejaculation

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15
Q

a1 on salivary glands

A

thick, viscous secretion

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16
Q

b1 on heart

A

increased rate, increased contractility

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17
Q

B2/A1 on GI

A

decrease in muscle motility and tone, contraction of sphincters

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18
Q

b2 on female genetalia

A

relaxation of uterus

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19
Q

B2 on blood vessels

A

skeletal vasodilation

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20
Q

a1 on blood vessels

A

constriction

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21
Q

a2 on blood pressure

A

decreases via central effect at vasomotor center

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22
Q

a1 on eye

A

mydriasis for eye examsmydriasis = dilation of pupil

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23
Q

b on eye

A

increase humour production (increases intraocular pressure)maintains glaucoma pathophysiology

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24
Q

a1 on GU

A

close sphincter

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25
Q

b2 on female genetalia

A

uterine relaxation to prevent premature labour

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26
Q

b2 on NMJ

A

causes muscle tremors = bad

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27
Q

adrenergic on CNS

A

increases vigilance and focus for ADHD

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28
Q

b inhibition on cns

A

used to treat stage fright, essential tremor

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29
Q

What are the main direct cholinergic agonists?

A

bethanachol, pilocarpine

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30
Q

what do physostigmine and neostigmine do?

A

AchE inhibitors

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31
Q

What are main muscarinic receptor antagonists

A

atropine, scopolamine, tropicamide (all tertiary)ipratropium

32
Q

what is donepezil?

A

tertiary ACHEi- crosses BBB, used in seizures

33
Q

what is pralidoxime used for?

A

organophosphate poisiningDetaches organophosphates from AChE

34
Q

How does botulinum toxin work?

A

Blocks ACh release.It lyses synapto- brevin, thereby preventing synaptic vesicle fusion and Ca2+-dependent release; used clinically to prevent spasms and reduce pain in ocular/facial muscles and to reduce severe underarm sweating (axillary hyperhidrosis); used cosmetically to lessen wrinkles; has a 2-4 mo duration/local injection.Leads to respiratory failure

35
Q

How does black widow toxin work?

A

Promotes ACh releaseIt results in excessive clumping of vesicles and “explosive release”. Also leads to respiratory failure.

36
Q

What is edrophonium?

A

Ultra short acting AChEi

37
Q

What is the action of nicotine?

A

nAChr agonist

38
Q

What is the action of curare?

A

Non-depolarizing blocker at muscle type nAChr’scompetitive antagonists at nAChRs at the NMJCauses flaccid paralysis of skeletal musclesrenal elimination

39
Q

What is atracurium?

A

Non-depolarizing blocker at muscle-type nAChRs competitive antagonists at nAChRs at the NMJCauses flaccid paralysis of skeletal musclesCompared to curare: faster onset, shorter duration of action, fewer side effectsEliminated via spontaneous hydrolysis and hydrolysis by plasma ChEs$$$

40
Q

WHat is Rocuronium?

A

Non-depolarizing blocker at muscle typenAChr’s competitive antagonists atnAChRs at the NMJCauses flaccid paralysis of skeletal musclesCompared to atracurium: faster onset, similar duration of action(2) None of curare’s side effects(3) Eliminated via hepatic metabolism$$$

41
Q

What is succinylcholine?

A

Depolarizing blocker at muscle type nAChr’s(1) Like ACh, succinylcholine interacts with nAChRs to increase Na+ permeability; the resulting depolarization leads to a short burst of action potentials; this initial stimulation (1-5 min) is associated with muscle fasciculations and soreness.(2) Since succinylcholine is not as rapidly eliminated as ACh, depolarization at the NMJ is prolonged and depolarization block, as well as desensitization, produce flaccid skeletal muscle paralysis.Used to facilitate intubation and to allow controlled ventilation in ICU and as an adjuvant to surgical anesthesia

42
Q

What is the tensilon test?

A

In myasthenia gravis, Ab to muscle type nAChr often result in skeletal muscle weakness and fatiguability. Endrophonium (tensilon) is an ultra-short acting AChEi that is used for diagnosis. The person would get a little stronger.

43
Q

What is the depolarization blockade?

A

Prolonged stimulation of nAChRs, for example caused by AChE inhibitors increas- ing the lifetime of synaptic ACh, results in(1) depolarization blockade”

44
Q

How do you usually treat myasthenia gravis?

A

reversible, long acting AChEi’s like pyridostigmine (quaternary)SteroidsThymectomy

45
Q

nicotine on nAChr in NMJ

A

blockade (depolarization block and nAChr desensitization)

46
Q

n on periperal sesnsory receptors

A

stimulation(stretch receptors, chemo- receptors (carotid and aortic bodies), thermal receptors (skin and tongue), and pain receptors)

47
Q

n on ANS ganglia

A

initial stimulation followed by blockade (depolarization block & nAChr desensitization)

48
Q

n on CV system

A

increase HR and BP

49
Q

n on CNS

A

stimulation followed by depression and addiction

50
Q

What are the monoamines?

A

DA, NE, 5HT

51
Q

What does MAO do?

A

Mitochondrial enzyme, converts catecholamines to aldehydes, isozymes with different substrate specificities exist (MAO A: norepinephrine, serotonin, tyramine; MAO B: dopamine).

52
Q

What are MAOi’s used for?What are some common MAOi’s?

A

Depression:Phenylzine, tranylcypromine = irreversible inhibitors of MAO A, Bmoclobemide = reversible inhibitor MAO AParkinson’s:Selegiline = irreversible MAO B

53
Q

How would you stop premature labor?

A

B2 agonist

54
Q

What receptors are on the eye?What do they do?

A

Muscarinic:Miosis, accomodation, increase aqueous humour outflowa1: mydriasisb: increases humor production

55
Q

What receptors are involved in peeing?

A

Muscarinic: contracts detrusor, opens sphinctera1: closes sphincter,b2: relaxes detrusor

56
Q

What receptors does propranolol work on?

A

B1, B2 antagonist

57
Q

How do you treat Alzheimer’s?

A

Overall goal is to increase ACh activityGive donepezil (AChEi)and memantine (NMDA-R antagonist)

58
Q

Tell me about actions of B2 receptors.

A

Skeletal blood vessels: vasodilationBronchodilationSmooth muscle relaxation in GI tractUterine relaxationMuscle tremors @NMJDetrusor relaxationIncreases aqueous humour (B nonspecific)

59
Q

What are 2 important muscarinic agonists?

A

bethanacol, pilocarpine, and ACh of course

60
Q

What are the nicotinic receptor agonists?

A

ACh, nicotine

61
Q

What are the muscarinic receptor antagonists?

A

Atropine, scopolamine, tropicamide

62
Q

What are the AChE inhibitors?

A

Neostigmine, physostigmine, donepezil, edrophonium, organophosphates (irreversible)

63
Q

What is an irreversible AChEi?What is the one drug you can use to reverse it?

A

OrganophosphatesPralidoxime

64
Q

Adrenergic agonists at a1, b1, b2

A

EpinephrinePseudophedrine, Tyramine (indirect)

65
Q

a1, b1 agonists

A

Ephedrine (indirect)NE

66
Q

a1 selective agonist

A

phenylephrine

67
Q

a2 selective agonist

A

clonidine

68
Q

b1 selective agonist

A

dobutamine

69
Q

a1 selective antagonist

A

prazosintamsulosin (flomax)

70
Q

a1, a2 antagonist

A

phentolamine (reversible)phenoxybenzamine (irreversible)

71
Q

b1 selective antonist

A

metoprolol, atenolol

72
Q

b1,b2 antagonist

A

propranolol

73
Q

b1, b2 agonist

A

isoproterenol

74
Q

a1, b1, b2 antagonist

A

labetalolcarvedilol

75
Q

b2 selective agonist

A

albuterol

76
Q

Main COMT inhibitor

A

entacapone

NS Receptors & Drugs (1 decks)

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