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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
VIGABATRIN
moa: irreversibly inhibit GABA transaminase to increase GABA
26
LEVETIRACETAM
moa: unknown, may modulate GABA and glutamate release?
27
epilepsy drugs resulting in SJS
carbamazepine ethosuximide lamotrigine
28
epilepsy drugs that induce cyto P450
carbamazepine phenobarbital phenytoin
29
PHENYTOIN tox
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
PHENYTOIN
moa: increase Na channel inactivation. decrease refractory period. inhibit glutamate release from excitatory presynaptic neuron. *parenteral: fosphenytoin
31
PHENYTOIN use
tonic-clonic seizures. partial. status epilepticus prophylaxis. *class IB antiarrhythmic
32
barbiturates
phenobarbital pentobarbital thiopental secobarbital
33
barbiturate moa
facilitate GABA-A action by increase DURATION of Cl channel opening, decrease neuron firing
34
barbiturate use
sedative for seizures, anxiety, insomnia. *thiopental: induction of anesthesia
35
barbiturate tox
dependence. additive CNS depression WITH ALCOHOL. resp or cardio depression leading to DEATH. drug interactions (P450)
36
barbiturate antidote
sx management - assist resp, increase BP
37
barbiturate contraindicated in....?
porphyria
38
benzodiazepines
short-acting: triazolam, oxazepam, midazolam, alprazolam intermediate: lorazepam, temazepam long-acting: diazepam, chlordiazepoxide
39
benzodiazepine moa
facilitate GABA-A action by increase FREQUENCY of Cl channel opening. decreases REM sleep.
40
benzodiazepine use
anxiety spasticity detox, esp for ALCOHOL WITHDRAWAL, DELIRIUM TREMENS night terror sleepwalking general anesthetic (amnesia, muscle relaxation) insomnia (hypnotic)
41
benzodiazepine tox
dependence additive CNS depression with ALCOHOL less risk of resp depression and coma than barbiturates
42
benzodiazepine antidote
treat OD with flumazenil - competitive antagonist at GABA benzo receptor
43
common receptor for benzodiazepine, barbiturates, alcohol
GABA-A receptor (ligand gated chloride channel)
44
addiction potential with benzodiazepine
highest with short-acting benzos
45
non-benzodiazepine HYPNOTICS
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
inhaled anesthetics
``` halothane enflurane isoflurane sevoflurane methoxyflurane NITROUS OXIDE ```
47
inhaled anesthetics moa
unknown. ``` effects: myocardial depression resp depression nausea, emesis increase cerebral bld flow (decrease cerebral metab demand) ```
48
inhaled anesthetics tox
halothane: hepatotox enflurane: pro-convulsant methoxyflurane: nephrotox nitrous oxide: expansion of trapped gas *rare: malignant hyperthermia
49
IV anesthetics
``` barbiturates benzodiazepines arylcyclohexylamines (ketamine) opiates propofol ```
50
IV anesthetics - barbs
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
IV anesthetics - benzos
MIDAZOLAM for endoscopy. adjunct with gaseous anesthetics and narcotics. tox: severe postop resp depression amnesia hypotension (treat with flumazenil)
52
IV anesthetics - ketamine
PCP analog. acts as dissociative anesthetics. block NMDA receptor. CV stimulant. increase cerebral bld flow. cause disorientation, hallucination, bad dreams.
53
IV anesthetics - opiates
MORPHINE, FENTANYL. | with other CNS depressants during general anesthesia
54
IV anesthetics - propofol
potentiates GABA-A. for rapid anesthesia induction and short procedures. less postop nausea than thiopental.
55
local anesthetics
ESTERS procaine cocaine tetracaine AMIDES lidocaine mepivacaine bupivacaine
56
local anesthetics moa
block Na channels by binding specific receptors on INNER portion of channel. prefer activated Na channels = most effective in rapidly firing neurons.
57
local anesthetics use
minor surg procedures | spinal anesthesia
58
local anesthetics tox
CNS excitation severe CV tox (bupivacaine) hyper/hypotension arrhythmias (cocaine)
59
neuromuscular blocking drugs - depolarizing
SUCCINYLCHOLINE
60
neuromuscular blocking drugs - nondepolarizing
``` tubocurarine atracurium mivacurium pancuronium vecuronium rocuronium ``` *compete with ACh for receptors

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