neuro pharm Flashcards
alpha1 agonist that decr aq humor synth via vasoconstriction
use: open angle glaucoma
epi
alpha2 agonist that decr aq humor synth
use: open angle glaucoma
brimonidine
beta blockers that decr aq humor synth
use: glaucoma
timolol, betaxolol, carteolol
diuretic that decr aq humor synth via inhib of carbonic anhydrase
use: glaucoma
acetazolamide
direct cholinomimetic that incr outflow of aq humor via contraction of ciliary m. & opening of trabecular meshwork
use: glaucoma
pilocarpine, carbachol
use pilocarpine in emergencies (very effective at opening meshwork into canal of Schlemm)
indirect cholinomimetics that incr outflow of aq humor via contraction of ciliary m. & opening of trabecular meshwork
use: glaucoma
physostigmine, echothiophate
PG that incr outflow of aq humor
use: glaucoma
latanoprost (PGF 2a)
agonists at opioid receptors to modulate synaptic transmission - open K+ channels, close Ca channels - decr synaptic transmission
inhib release of ACh, Norepi, 5HT, glutamate, substanceP
use: pain, cough suppression, diarrhea, acute pulm edema, maintenance for heroin addicts
opioid analgesics: morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate, pentazocine
opioid agonist at mu receptors
morphine
opioid agonist at delta receptors
enkephalin
opioid agonist at kappa receptors
dynorphin
opioid that suppresses cough
dextromethorphan
opioid that tx diarrhea
loperamide, diphenoxylate
opioids used to manage heroin addicts
methadone, buprenorphine + naloxone
kappa opioid receptor agonist & mu opioid receptor partial agonist
use: produce analgesia to tx severe pain, cause less resp depression than full opioid agonists
Butorphanol
weak opioid agonist, also inhib 5HT & Norepi reuptake
use: chronic pain
tramadol
blocks thalamic T type Ca channels
use: 1st line tx of absence generalized sz
EthoSUXimide
Sucks to have Silent/absent Seizures
increases GABAa action
use: 1st line for acute status epilepticus, also for eclampsia sz
benzo’s: diazepam, lorazepam
incr Na+ channel inactivation; zero order kinetics
use: 1st line for tonic clonic generalized sz; 1st line for acute status epilepticus; also used for simple & complex partial sz
phenytoin
incr Na+ channel inactivation
use: 1st line for simple & complex partial sz; 1st line for tonic clonic generalized sz
carbamazepine
incr Na+ channel inactivation, incr GABA conc by inhib GABA transaminase
use: 1st line for tonic clonic generalized sz; also used for simple & complex partial sz; used for absence sz & myoclonic sz as well; bipolar disorder
valproic acid
inhib high voltage activated Ca channels; GABA analog
use: simple & complex partial sz
gabapentin
increases GABAa action, 1st line in neonates
use: simple & complex partial sz, tonic clonic generalized sz
phenobarbital
blocks Na+ channels, incr GABA action
use: simple & complex partial sz, tonic clonic generalized sz
topiramate
blocks voltage gated Na+ channels
use: simple/complex sz, tonic clonic, absence
lamotrigine
unknown- may modulate GABA & glutamate release
use: simple/complex, tonic clonic
levetiracetam
incr GABA by inhib reuptake
use: simple & complex partial sz
tiagabine
incr GABA by irreversibly inhib GABA transaminase
use: simple & complex partial sz
vigabatrin
facilitate GABAa action by incr duration of Cl- channel opening - decr neuron firing
use: sedative for anxiety, sz, insomnia, inducing anesthesia
barbiturates: phenobarbital, pentobarbital, thiopental, secobarbital
facilitate GABAa action by incr frequency of Cl- channel opening, decr REM sleep
shorter acting have higher addictive potential
use: anxiety, spasticity, status epilepticus, detox, night terrors, sleepwalking, general anesthetic, hypnotic
benzo’s: diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide
act via BZ1 subtype of GABA receptor
use: insomnia
non benzo hypnotics: zolpidem, zaleplon, eszopiclone
zzz’s = sleep
inhaled anesthetics that cause myocardial depression, resp depression, nausea/emesis, incr cerebral blood flow (decr cerebral metabolic demand)
halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, N2O
i.v. anesthetic with high potency, high lipid solubility, rapid entry into brain
use: induces anesthesia, for short surg,
effect terminated by rapid re-distribution into tissue
decr cerebral blood flow
barbiturate: thiopental
i.v. anesthetic used for endoscopy, with gaseous anesthetics & narcotics
may cause severe post op resp depression, decr BP, anterograde amnesia
benzo: midazolam
i.v. anesthetic that is a PCP analog - dissociative anesthetic, block NMDA receptors, cardio stimulant
cause disorientation, hallucin, bad dreams
incr cerebral blood flow
arylcyclohexylamines: ketamine
i.v. anesthetic opioids that are used with other CNS depressants during general anesthesia
morphine, fentanyl
i.v. anesthetic used for sedation in ICU, rapid anesthesia induction, short procedures
less post op nausea
potentiates GABAa
propofol
procaine, cocaine, tetracaine
local anesthetic esters
lidocaine, mepivacaine, bupivacaine
local anesthetic amides
block Na+ channels by binding specific receptors on inner portion of channel
preferential to activated Na+ channels (most effective in rapidly firing neurons)
use: minor surg, spinal anesthesia
local anesthetic esters & amides: procaine, cocaine, tetracaine, lidocaine, mepivacaine, bupivacaine
induces muscle paralysis in surg or mechanical ventilation, selective for motor nicotinic receptor
depolarizing Nm blocker - strong ACh agonist w/ sustained depol - prevent m. contraction
succinylcholine
non depolarizing Nm blockers for muscle paralysis in surg or mechanical ventilation, selective to nicotinic motor receptors
competitive antag for ACh receptors
tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium
prevents release of Ca from SR of skel m.
use: malignant hyperthermia, neuroleptic malignant syndrome
dantrolene
inhib GABAa receptors at spinal cord level, induces skel m. relaxation
use: muscle spasms
baclofen
central acting skel m. relaxant
structurally related to TCAs, similar anti cholin SE
use: muscle spasms
cyclobenzaprine
ergot DA agonist that tx Parkinson’s
bromocriptine
non ergot DA agonist that tx Parkinson’s
pramipexole, ropinirole
increases DA release & decr DA reuptake
use: parkinson’s
also used as anti viral for influenza A & rubella
amantadine
prevent periph L-dopa degradation by inhib dopa decarboxylase - incr L-dopa entering CNS - incr central L-dopa avail for conversion to DA
reduces SE of periph L-dopa conversion to DA
use: parkinson’s
levodopa/carbidopa
prevent periph L-dopa degradation into 3-O-methyldopa by inhib COMT
use: parkinson’s
entacapone, tolcapone
act centrally to block breakdown of DA
blocks conversion of DA into 3MT by selectiv inhib MAO-B
use: adjunct to L-dopa to tx parkinson’s
selegiline
act centrally to block DA breakdown by blocking conversion of DA to DOPAC by inhib central COMT
use: parkinson’s
tolcapone
anti muscarinic- improves tremor & rigidity but little effect on bradykinesia
use: parkinson’s
benztropine
NMDA receptor antagon, helps prevent excitotoxicity mediated by Ca
use: Alzheimer’s
memantine
AChE inhibitors
use: Alzheimer’s
donepezil, galantamine, rivastigmine, tacrine
inhib vesicular monoamine transporter, limit DA vesicle packaging & release
use: Huntington’s disease
tetrabenazine, reserpine
D2 receptor antag
use: Huntington’s
Haloperidol
5HT 1b/1d agonists - inhib CN V activation, prevent vasoactive peptide release, induce vasoconstriction
use: acute migraine, cluster HA attacks
Sumatriptan
