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FA Neuro Pharm Flashcards

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1
Q

Mu-opioid receptor partial agonist and kappa opioid receptor agonist; produces analgesia

A

Butophanol

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2
Q

Very weak opioid agonist; also inhibits serotonin and NE reuptake (used for chronic pain)

A

Tramadol

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3
Q

Facilitates GABAa action by increasing DURATION of Cl- channel opening, thus decreasing neuron firing (barbiturates increase duration). Contraindicated in porphyrias.

A

Barbituates

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4
Q

Facilitate GABAa action by increasing FREQUENCY of Cl- channel opening. Decrease REM sleep,

A

Benzos

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5
Q

Act via the BZ1 subtype of the GABA receptor. Effects reversed by flumazenil.

A

Nonbenzo hypnotics

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6
Q

Block Na+ channels by binding to specific receptors on inner portion of channel. Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons.

A

Local anesthetics

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7
Q

Prevents the release of Ca2+ from the SR of skeletal muscle

A

dantrolene

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8
Q

Selectively inhibits MAO-B, which preferentially metabolizes dopamine over norepinephrine and 5-HT, thereby increasing the availability of dopamine

A

Selegiline

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9
Q

NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca2+)

A

Memantine

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10
Q

AchE inhibitors

A

Donepezil, galantamine, rivastigmine

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11
Q

Inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release

A

Tetrabenzamine, reserpine

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12
Q

5-HT1B/1D agonist. Inhibits trigeminal nerve activation; prevents vasoactive peptide release; induces vasoconstriction. Half-life < 2 hrs

A

Sumatriptan

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13
Q

Increases Na+ channel inactivation, zero-order kinetics

A

Phenytoin

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14
Q

Increases Na+ channel inactivation

A

Carbamazepine

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15
Q

Increases Na+ channel inactivation, increases GABA concentration by inhibiting GABA transaminase

A

Valproic acid

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16
Q

Primarily inhibits high-voltage-activated Ca2+ channels; designed as GABA analog

A

Gabapentin

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17
Q

Blocks thalamic T-type Ca2+ channels

A

Ethosuximide

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18
Q

Increases GABAa action

A

Phenobarbital

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19
Q

Blocks Na+ channels and increases GABA action

A

Topiramate

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20
Q

Blocks voltage-gated Na+ channels

A

Lamotrigine

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21
Q

Unknown; may modulate GABA and glutamate release

A

Levetiracetam

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22
Q

Increases GABA by inhibiting reuptake

A

Tiagabine

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23
Q

Increases GABA by irreversibly inhibiting GABA transaminase

A

Vigabatrin

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24
Q

Decreases aqueous humor synthesis via vasoconstriction

A

Epinephrine

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25
Tox: Mydriasis; do NOT use in closed-angle glaucoma
Epinephrine
26
Alpha2 agonist that decreases aqueous humor synthesis
Brimonidine
27
Tox: Blurry vision, ocular hyperemia, foreign body sensation, ocular allergic run, ocular pruritus
Brimonidine
28
5 classes of drugs that can be used for glaucoma
1. alpha agonists 2. beta blockers 3. diuretics 4. cholinomimetics (direct and indirect) 5. prostaglandin
29
What beta blockers can be used for glaucoma?
Timolol, betaxolol, carteolol
30
What diuretic can be used for glaucoma?
Acetazolamide
31
What alpha agonists can be used for glaucoma?
Epinephrine, brimonidine
32
Decreases aqueous humor synthesis via inhibition of carbonic anhydrase
Acetazolamide
33
Two direct cholinomimetics that can be used for glaucoma
pilocarpine and carbachol
34
two indirect cholinomimetics that can be used for glaucoma
physostigmine and chothiophate
35
What drug do you use in a glaucomic emergency?
pilocarpine - very effective at opening meshwork into canal of Schlemm
36
What is the mechanisms of cholinomimetics in treatment of glaucoma?
Increased outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshwork
37
What are the side effects of cholinomimetics in treatment of glaucoma?
miosis and cyclospasm (contraction of ciliary muscle)
38
What prostaglandin is useful in glaucoma treatment?
Latanoprost (PGF2alpha)
39
what is the mechanism of latanoprost?
increased outflow of aqueous humor
40
tox latanoprost
darkens color of iris
41
agonist at mu receptors
morphine
42
agonist at delta receptors
enkephalin
43
agonist at kappa receptors
dynorphin
44
what opioid is used for cough suppression?
dextromethorphan
45
what opioid is used for diarrhea
loperamide, diphenoxylate
46
opioid analgesic mechs
act as agonists at opioid receptors to (open K+ channels, close Ca2+ channels) --> decreased synaptic transmission Inhibit release of ACh, NE, 5-HT, glutamate, substance P
47
opioid antidote
naloxone or naltrexone
48
Butorphanol mech
mu opioid PARTIAL receptor agonist and kappa opioid receptor agonist; produces analgesia
49
CU butorphanol
severe pain (migraine, labor); causes less respiratory depression that full opioid agonists
50
Butorphanol Tox
can cause opioid withdrawal sx is pt is also taking full opioid agonist (competition for opioid receipts). OD not easily reversed w. naloxone
51
Tramadol mech
very weak opioid agonst; also inhibits serotonin and NE reuptake (works on multiple NTs - "tram it all" in with tramadol).
52
CU tramadol
chronic pain
53
Tramadol tox
opioid tox, decreases seizure threshold, serotonin syndrome
54
ethosuximide mech
blocks thalamic T-type Ca2+ channels
55
Tox ethosuximide
EFGHIJ | Ethosuximide causes Fatigue, GI distress, Headache, Itching, stevens-Johnson
56
barbiturate mech
facilitate GABA(A) action by increasing the DURATION of chloride channel opening, thus decreasing neuron firing (barbiDURATes increase DURATion). Contraindicated in porphyria
57
barbiturate CU
sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)
58
barbiturate tox
respiratory and CV depression (can be fatal!); CNS depression (exacerbated by EtOH); dependence; drug interaxns (INDUCES P450!).
59
barbituate AD?
none! supprotive - assist respiration and maintain BP
60
phenobarbital, pentobarbital, thiopental, secobarbital
barbiturates
61
benzo mech
facilitate GABA(A) action by increasing FREQUENCY of chloride channel opening, decrease REM sleep
62
highest addictive potential, shortest acting benzos
Triazolam Oxazepam Midazolam
63
status epilepticus tx
lorazepam, diazepam
64
benzo AD
flumazenil
65
flumazenil mech
competitive antagonist at GABA benzo receptor
66
Non benzo hypnotic examples
Zolpidem Zaleplon Eszopiclone
67
Zolpidem mech
act via the BZ1 subtype of the GABA receptor
68
MAC =
miminal alvelolar concentration required to prevent 50% of subjects from moving in response to noxious stimulus (e.g. skin incision)
69
inhaled anesthetic with hepatotoxicity
halothane
70
inhaled anesthetic with nephrotoxicity
methoxyflurane
71
inhaled anesthetic that is proconvulsant
enflurane
72
inhaled anesthetic that can cause expansion of trapped gas in a body gravity?
nitrous oxide
73
the one inhaled anesthetic that doesn't cause malignant hyperthermia
nitrous oxide
74
what besides inhaled anesthetics can cause malignant hyperthermia
succinylcholine
75
tx malignant hypertension
dantolene
76
dantrolene mech
prevents the release of Ca2+ from SR of skeletal muscle
77
what causes neuroleptic malignant syndrome?
antipsychotic drugs
78
IV anesthetic barbiturate
thiopental
79
IV anesthetic benzo
midazolam
80
PCP analogs that act as dissociative anesthetics, Block NMDA receptors. CV stimulants. Cause disorientation, hallucination, and bad dreams. Increases cerebral BF
arylcyclohezylamines (ketamine)
81
Used for sedation in ICU, rapid anesthesia induction, and short procedures. Less post operative nausea than thiopental. Potentiates GABA(A).
Propofol
82
local anesthetic esters
procaine, cocaine, tetracaine
83
local anesthetic amides
lidocaine, mepivacaine, bupivacaine,
84
local anesthetic mechanism
blocks Na+ channels by binding to specific receptors on inner portion of channel. Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons. Teritiary amine local anesthetics penetrate membrane in uncharted form, then bind to ion channels in charged form.
85
Strong ACh receptor agonist; produces sustained depolarization and prevents muscle contraction
succinylcholine (depolarizing nueromuscular blocking drug)
86
reversal of non depolarizing neuromuscular blockade?
neostigmine (must be given with atropine to prevent muscarinic effects such as bradycardia), edrophonium, and other cholinesterase inhibitors)
87
How to treat Parkinson dz?
``` BALSA Bromocriptine Amantadine Levodopa w/ carbidopa Selegiline (and COMT inhibitors) Antimuscarinics ```
88
levodopa tox
arrythmias from increased peripheral formation of catecholamines. long term use can lead to dyskinesia following administration ("on off phenomenon"), akinesia between doses
89
how to treat alzheimers?
``` memantine (NMDA receptor antagonist) AChE inhibitors (donepezil, galantamine, rivastigmine) ```
90
memantine tox
dizziness, confusion, hallucinations
91
AChE inhibitor tox
nausea, dizziness, insomnia
92
NT changes in HD?
decreased GABA and ACh, | Increased dopamine
93
HD tx
tetrabenazamine and reserpien; | haloperidol
94
tetrabenazine and reserpine mech
inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release
95
haloperidol mech
dopamine receptor antagonist
96
sumatriptan mech
5HT1b/1D agonist. INhibts trigeminal nerve activation; prevents vasoactive peptide release; induces vasoconstriction. Half-life < 2 hours
97
sumatriptan CU
acute migraine, cluster headache
98
sumatriptan tox
coronary vasospasm (contraindicated in pts with CAD or Prinzmetal), mild tingling.

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