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Neuro > Analgesics, anesthetics, seizure drugs 0426 > Flashcards

Analgesics, anesthetics, seizure drugs 0426 Flashcards

epilepsy drugs pg 473

1
Q

OPIOID analgesics

A 
morphine
fentanyl
codeine
heroin
methodone
meperidine
dextromethorphan
diphenoxylate
loperamide
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2
Q

OPIOID action

A

agonist at opioid receptors to DECREASE synaptic transmission - open K channel, close Ca channel.

inhibit release of ACh, NE, 5HT, glutamate, substance P

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3
Q

OPIOID receptors

A

mu: morphine
delta: enkephalin
kappa: dynorphin

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4
Q

OPIOID use

A 
pain
acute pulmo edema
cough (dextromethorphan)
diarrhea (loperamide, diphenoxylate)
maintenance program for addicts (methadone)
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5
Q

OPIOID tox

A 
addiction
resp depression
additive CN depression 
constipation
miosis (PINPOINT PUPIL)

*no tolerance to miosis, constipation

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6
Q

OPIOID antidote

A

naloxone or naltrexone - opioid receptor antagonists

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7
Q

butorphanol

A

partial agonist at opioid MU receptor.
agonist at opioid KAPPA receptor.

use: pain.
less resp depression than full agonist.
tox: withdrawal if also on full agonist.

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8
Q

tramadol

A

very weak opioid agonist.
also inhibits 5HT, NE reuptake.

use: chronic pain.
tox: similar to opioids. decrease seizure threshold.

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9
Q

tonic clonic seizures: first line drug

A

phenytoin
carbamazepine
valproic acid

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10
Q

absence seizures: first line drug

A

ethosuximide.

ONLY other tx = valproic acid

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11
Q

status epilepticus: first line drug

A

ACUTE: benzos (diazepam, lorazepam)

PROPHYLAXIS: phenytoin

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12
Q

simple partial seizure: first line drug

A

carbamazepine

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13
Q

complex partial seizure: first line drug

A

carbamazepine

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14
Q

carbamazepine as first line drug for….?

A

simple partial,
complex partial,
tonic-clonic.

*trigeminal neuralgia

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15
Q

CARBAMAZEPINE

A

moa: increase Na channel inactivation

tox: diplopia
ataxia
blood dyscrasias - agranulocytosis, aplastic anemia
liver tox
teratogenesis
cyto P450 induction
SIADH
SJS
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16
Q

LAMOTRIGINE

A

moa: blocks voltage-gated Na channels
tox: SJS

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17
Q

GABAPENTIN

A

moa: mainly inhibits HVA Ca channels.
designed as GABA analog.

  • also used for peripheral neuropathy, bipolar d/o
    tox: sedation, ataxia
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18
Q

TOPIRAMATE

A

moa: blocks Na channels. increase GABA action.

tox: sedation, mental dulling
kidney stones
weight loss

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19
Q

PHENOBARBITAL

A

moa: increase GABA-A action

tox: sedation, tolerance, dependence
cyto P450 induction

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20
Q

VALPROIC ACID

A

moa: increase Na channel inactivation, increase GABA conc
* also used for MYOCLONIC seizures

tox: GI distress
rare but fatal hepatotox
tremor
weight gain
NTD (spina bifida) - CONTRAINDICATED IN PREGNANCY
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21
Q

ETHOSUXIMIDE

A

moa: blocks THALAMIC T-type ca channels

tox: GI distress
fatigue
headache
urticaria
SJS
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22
Q

BENZODIAZEPINES (diazepam, lorazepam) in epilepsy tx

A

moa: increase GABA-A action
tox: sedation, tolerance, dependence

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23
Q

seizures of ECLAMPSIA

A 
#1: MgSO4
#2: benzos (diazepam, lorazepam)
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24
Q

TIAGABINE

A

moa: inhibit GABA reuptake

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25
Q

VIGABATRIN

A

moa: irreversibly inhibit GABA transaminase to increase GABA

26
Q

LEVETIRACETAM

A

moa: unknown, may modulate GABA and glutamate release?

27
Q

epilepsy drugs resulting in SJS

A

carbamazepine
ethosuximide
lamotrigine

28
Q

epilepsy drugs that induce cyto P450

A

carbamazepine
phenobarbital
phenytoin

29
Q

PHENYTOIN tox

A

nystagmus, diplopia, ataxia
sedation
SLE-like syndrome
cyto P450 induction

CHRONIC USE:
gingival hyperplasia 
coarsened facial features
hirsutism
acneiform skin rash
pseudolymphoma
MEGALOBLASTIC ANEMIA
peripheral neuropathy

*teratogenesis (fetal hydantoin syndrome)

30
Q

PHENYTOIN

A

moa: increase Na channel inactivation.
decrease refractory period.
inhibit glutamate release from excitatory presynaptic neuron.

*parenteral: fosphenytoin

31
Q

PHENYTOIN use

A

tonic-clonic seizures.
partial.
status epilepticus prophylaxis.

*class IB antiarrhythmic

32
Q

barbiturates

A

phenobarbital
pentobarbital
thiopental
secobarbital

33
Q

barbiturate moa

A

facilitate GABA-A action by increase DURATION of Cl channel opening, decrease neuron firing

34
Q

barbiturate use

A

sedative for seizures, anxiety, insomnia.

*thiopental: induction of anesthesia

35
Q

barbiturate tox

A

dependence.
additive CNS depression WITH ALCOHOL.
resp or cardio depression leading to DEATH.
drug interactions (P450)

36
Q

barbiturate antidote

A

sx management - assist resp, increase BP

37
Q

barbiturate contraindicated in….?

A

porphyria

38
Q

benzodiazepines

A

short-acting: triazolam, oxazepam, midazolam, alprazolam

intermediate: lorazepam, temazepam

long-acting: diazepam, chlordiazepoxide

39
Q

benzodiazepine moa

A

facilitate GABA-A action by increase FREQUENCY of Cl channel opening.

decreases REM sleep.

40
Q

benzodiazepine use

A

anxiety
spasticity
detox, esp for ALCOHOL WITHDRAWAL, DELIRIUM TREMENS
night terror
sleepwalking
general anesthetic (amnesia, muscle relaxation)
insomnia (hypnotic)

41
Q

benzodiazepine tox

A

dependence
additive CNS depression with ALCOHOL
less risk of resp depression and coma than barbiturates

42
Q

benzodiazepine antidote

A

treat OD with flumazenil - competitive antagonist at GABA benzo receptor

43
Q

common receptor for benzodiazepine, barbiturates, alcohol

A

GABA-A receptor (ligand gated chloride channel)

44
Q

addiction potential with benzodiazepine

A

highest with short-acting benzos

45
Q

non-benzodiazepine HYPNOTICS

A

zolpidem, zaleplon, eszopiclone

moa: act at BZ1 receptor subype.
reversed by flumazenil.
for INSOMNIA.
lower dependence risk than benzos.
short duration due to rapid metab by liver.
modest day-after psychomotor depression.
few amnestic effects.

tox: ataxia, HA, confusion

46
Q

inhaled anesthetics

A 
halothane
enflurane
isoflurane
sevoflurane
methoxyflurane
NITROUS OXIDE
47
Q

inhaled anesthetics moa

A

unknown.

effects:
myocardial depression
resp depression
nausea, emesis
increase cerebral bld flow (decrease cerebral metab demand)
48
Q

inhaled anesthetics tox

A

halothane: hepatotox
enflurane: pro-convulsant
methoxyflurane: nephrotox
nitrous oxide: expansion of trapped gas

*rare: malignant hyperthermia

49
Q

IV anesthetics

A 
barbiturates
benzodiazepines
arylcyclohexylamines (ketamine)
opiates
propofol
50
Q

IV anesthetics - barbs

A

THIOPENTAL
high potency, high lipid solubility.
rapid entry into brain.
decrease cerebral bld flow.

for induction and short surg.
rapid redistribution to tissue (skel mm) and fat.

51
Q

IV anesthetics - benzos

A

MIDAZOLAM for endoscopy.
adjunct with gaseous anesthetics and narcotics.

tox: severe postop resp depression
amnesia
hypotension (treat with flumazenil)

52
Q

IV anesthetics - ketamine

A

PCP analog.
acts as dissociative anesthetics.
block NMDA receptor.

CV stimulant.
increase cerebral bld flow.
cause disorientation, hallucination, bad dreams.

53
Q

IV anesthetics - opiates

A

MORPHINE, FENTANYL.

with other CNS depressants during general anesthesia

54
Q

IV anesthetics - propofol

A

potentiates GABA-A.
for rapid anesthesia induction and short procedures.
less postop nausea than thiopental.

55
Q

local anesthetics

A

ESTERS
procaine
cocaine
tetracaine

AMIDES
lidocaine
mepivacaine
bupivacaine

56
Q

local anesthetics moa

A

block Na channels by binding specific receptors on INNER portion of channel.

prefer activated Na channels = most effective in rapidly firing neurons.

57
Q

local anesthetics use

A

minor surg procedures

spinal anesthesia

58
Q

local anesthetics tox

A

CNS excitation
severe CV tox (bupivacaine)
hyper/hypotension
arrhythmias (cocaine)

59
Q

neuromuscular blocking drugs - depolarizing

A

SUCCINYLCHOLINE

60
Q

neuromuscular blocking drugs - nondepolarizing

A 
tubocurarine 
atracurium
mivacurium 
pancuronium 
vecuronium
rocuronium

*compete with ACh for receptors

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