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PNP Drug Mechanisms Flashcards

1
Q

Tetrodotoxin (TTX)

A

Presynaptic neuromuscular agent

blocks voltage gated Na channels

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2
Q

Mg2+, cations

A

presynaptic agent

competition/blocker of ca2+ channels

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3
Q

aminoglycosides

A

presynaptic agent

reduces Ca entry through channels

Note: do not use these antibiotics with myasthenia gravis patients

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4
Q

black widow spider venom

a-latrotoxin

A

presynaptic agent

adds Ca channels to membrane, leads to barrage and exocytosis creating loss of Ach vesicles and increased surface area (results in transmission block)

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5
Q

botulinum toxin A

A

presynaptic agent

cleaves SNAP-25 (SNARE complex), reducing calcium sensitivity and preventing secretion

Note: blocks ANS as well, not just muscles

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6
Q

botulinum toxin B

A

presynaptic agent

cleaves synaptobrevin SNARE protein

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7
Q

hemicholinium

A

presynaptic agent

interferes with choline uptake, leads to less Ach available for secretion

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8
Q

tubocurarine

A

postsynaptic non-depolarizing blocker

competitive inhibition of Ach at nicotinic receptors

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9
Q

pancuronium

A

postsynaptic non-depolarizing blocker

competitive inhibition of Ach, selective for neuromuscular junction

Note: do not use with aminoglycosides (similar to MG)
Note: renal clearance

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10
Q

vecuronium

A

postsynaptic non-depolarizing blocker

competitive inhibition of Ach, similar to pancuronium but faster action (intermediate duration)

Note: no CV effects, eliminated by liver

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11
Q

rocuronium

A

postsynaptic non-depolarizing blocker

competitive inhibition of Ach

Note: very rapid onset, similar duration to vecuronium

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12
Q

acetylcholine

A

post-synaptic depolarizing blocker

nicotinic receptor agonist, can block at high exogenous concentrations

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13
Q

succinylcholine

A

post-synaptic depolarizing blocker

nicotinic receptor agonist, causes sustained depolarization/desensitization

Notes: rapidly reversible, can cause muscle fasciculations and damage, hydrolyzed by cholinesterases

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14
Q

nicotine

A

post-synaptic depolarizing blocker

depolarizing blocker at neuromuscular junction

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15
Q

sugummadex

A

reversal agent of non-depolarizing blocker

encapsulates blockers to eliminate actions (specifically rocuronium, vecuronium)

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16
Q

neostigmine

A

anti-cholinesterase

binds to cholinesterase to prevent degradation

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17
Q

edrophonium

A

anti-cholinesterase

binds to cholinesterase, short-acting and rapid onset

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18
Q

physostigmine

A

anti-cholinesterase

Notes: can cross BBB

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19
Q

pyridostigmine bromide

A

anti-cholinesterase

neostigmine but long lasting slow release form

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20
Q

DFP

A

anti-cholinesterase

irreversible phosphorylation of esteratic site of acetylcholinesterase

Notes: well absorbed in all routes

21
Q

sarin

A

anti-cholinesterase

irreversible phosphorylation of esteratic site of acetylcholinesterase

22
Q

parathion

A

anti-cholinesterase

irreversible phosphorylation of esteratic site of acetylcholinesterase

Notes: metabolized into a toxic form that inhibits ChE

23
Q

malathion

A

anti-cholinesterase

irreversible phosphorylation of esteratic site of acetylcholinesterase

Notes: slightly safer than malathion (easier metabolism)

24
Q

chlorpyifos

A

anti-cholinesterase

irreversible phosphorylation of esteratic site of acetylcholinesterase

25
Q

VX

A

anti-cholinesterase

irreversible phosphorylation of esteratic site of acetylcholinesterase

Notes: almost impossible to remove, deadliest of nerve gases

26
Q

rivastigmine, galantamine, donepezil, tacrine

A

anti-cholinesterase

cholinesterase inhibitor

27
Q

oximes, pralidoxime

A

anticholinesterase antagonist

remotes phosphorylation from ache to restore cholinesterase activity

28
Q

dantrolene

A

peripheral muscle relaxant

ryanodine receptor blocker, preventing release of Ca

29
Q

methacholine

A

parasympathomimetic

muscarinic receptor agonist

30
Q

bethanechol

A

parasympathomimetic

muscarinic receptor agonist

Notes: resistant to hydrolysis by cholinesterases

31
Q

pilocarpine

A

parasympathomimetic

muscarinic receptor agonist

Notes: not hydrolyzed by cholinesterases

32
Q

cevimeline

A

parasympathomimetic

muscarinic receptor agonist

Notes: only used in Sjogren’s

33
Q

atropine

A

muscarinic receptor blocker

competitive inhibitor of Ach at muscarinic receptors

Notes: associated with toxicity syndrome

34
Q

homatropine

A

muscarinic receptor blocker

competitive inhibitor of Ach at muscarinic receptors, like atropine but shorter acting

35
Q

scopolamine

A

muscarinic receptor blocker

competitive inhibitor of Ach at muscarinic receptors

Notes: causes more CNS depressant effects compared to atropine

36
Q

glycopyrrolate

A

muscarinic receptor blocker

Notes: prevents excessive muscarinic effects after removal of blocker

37
Q

tolterodine

A

muscarinic receptor blocker

Notes: has active metabolite

38
Q

fesoterodine

A

muscarinic receptor blocker

Notes: needs to be metabolized to active version

39
Q

solifenacin

A

muscarinic receptor blocker

like tolterodine but better

40
Q

darifenacin

A

muscarinic receptor blocker

41
Q

oxybutynin

A

muscarinic receptor blocker

42
Q

tropicamide

A

muscarinic receptor blocker

ocular effects

43
Q

ipratropium

A

muscarinic receptor blocker

SAMA, bronchiolar dilation, blocks both presynaptic inhibitory and postsynaptics

44
Q

tiotropium

A

muscarinic receptor blocker

LAMA, bronchiolar dilation, more effective than ipratropium (postysnaptics only)

45
Q

norepinephrine

A

non-selective adrenergic agonist

activity: all a, B1, B3
No B2

46
Q

epinephrine

A

non-selective adrenergic agonist

activity: all a and B
notes: metabolized by MAO

47
Q

isoproterenol

A

non-selective adrenergic agonist

activity: all B, No a

48
Q

phenylephrine

A

selective a1 agonist

longer duration than epi,, selective but not potent

49
Q

imidazolines

A

selective a1 agonist

long acting

Notes: may cause depressant effects in kids

Neuro (2 decks)

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