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104 Cards in this Set

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naloxone
mu antagonist used to treat opioid overdose
nalmefene
more potent mu antagonist used for opioid overdose and post operative opioid reversal
naltrexone
mu antagonist PO long half life
methadone
mu agonist similar to morphine. analgesic, oral, LONG half-life, persistent effects on repeat admin so used to treat opioid withdrawal symptoms
diphenoxylate
mu agonist that doesn't get absorbed systemically. used for diahrrea
pentazocine
AGONIST at kappa receptors, PARTIAL agonist/antagonist at mu receptors. used for moderate pain. may have less abuse potential. respiratory depression ceiling at lower dose unlike mu agonists.
nalbuphine
agonist at kappa receptors, COMPLETE antagonist at mu receptors. similar to pentazocine in uses
codeine
methylated morphine (mu agonist) beter PO. weaker because must be demethylated to act.
oxycodone
long acting potent mu agonist given in combo with NSAID or acetaminphen to decrease dose
hydrocodone
potent mu agonist given in combo with NSAID or acetaminphen to decrease dose
dextromethorophan
OTC antitussive, d-isomer of a methylated opioid. no analgesic/addictive properties
morphine
used for: analgesia, cough suppression, acute pulmonary edema. prototypical mu agonist. inhibits release of substance P on presynaptic neurons by decreasing Ca2+ entry. inhibits postsynaptic neurons by increasing K+ efflux and hyperpolarizing them. weak agonist on kappa & delta receptors.
hydromophone
similar to morphine, strong mu agonist and weak kappa and delta agonist
oxymorphone
similar to morphine, strong mu agonist and weak kappa and delta agonist
levorphanol
similar to morphine, strong mu agonist and weak kappa and delta agonist
merperidine
mu agonist. does NOT precipitate biliary colic, so use for patients when you haven't ruled out cholestasis
fentanyl
short-acting IV mu agonist used for anesthesia. also on patches for cancer pain
sufentanil
short-acting IV mu agonist used for anesthesia.
alfentanil
short-acting IV mu agonist used for anesthesia.
remifentanil
short-acting IV mu agonist used for anesthesia.
heroin
derived form morphine. penetrates CNS BBB much faster.
lithium
mood stabilizer. mech unkwn. Treatment of: BIPOLAR. treatment of SIADH (since it causes nephrogenic diabetes insipidus). adjuvant in treatment of severe recurrent depression or schizophrenia
phenytoin
partial (1st line) & tonic-clonic seizures (1st line), prophylaxis for status epilepticus: blocks inactivated Na+ channels and thus inhibits rapidly/repeatedly firing neurons (analagous to class IB antiarrhythmics). can actually be USED as class IB antiarrhythmic (cross-reactivity at heart Na+ channels)
fosphenytoin
water soluble prodrug of phenytoin
lamotrigine
partial and tonic clonic seizures (occaisonally absence/mixed): blocks inactivated Na+ channels and thus inhibits rapidly/repeatedly firing neurons (analagous to class IB antiarrhythmics).
zonisamide
partial, tonic clonic, absence, and myoclonic seizures: blocks inactivated Na+ channels and T-type Ca2+ channels.
carbamazepine
partial (1st line), tonic-clonic (1st line): blocks inactivated Na+ channels and thus inhibits rapidly/repeatedly firing neurons (analagous to class IB antiarrhythmics). ALSO: TRIGEMINAL NEURALGIA (neuropathic pain). ALSO: 2nd line for BIPOLAR
oxcarbazepine
keto-analog of carbamaepine. similar effects but doesn't induce cyt p450 as much so less drug interactions. also keto group prevents epoxide metabolite that causes many of carbamazepine's side effects
topiramate
partial (mono) or tonic-clonic seizures (adjuvant). 1) blocks AMPA/kainate glutamate receptors 2) blocks voltage sensitive Na+ channels (a La phenytoin & carbamazapine) 3) may potenitate GABAergic signaling
felbamate
broad spectrum antiepileptic but in practice only used for severe childhood siezures (due to side effects of anemia hepatotox). 1) inhibits NMDA gluatamate receptors 2) inhibits voltage-sensitive Na+ channels.
valproic acid
VERY BROAD spectrum antiepileptic. partial (1st line), myocloinc (1st line), tonic-clonic (1st line), absence (backup). multiple mechanisms: enhances GABA accumulation 2) inhibits voltage sensitive Na+ channels different from phenytoin and carbamazapine 3) inhibits low threshold, T-type Ca2+ channels. ALSO: USED FOR MANIA and migraine prophylaxis
ethosuximide
absence seizures (1st line). inhibits Ca2+ currents through low-threshold T-type channels. these are present in thalamus and normally activated during sleep to provide rhythmic input to cerebrum in place of sensory input. abnormal hyperpolarization of thalamus during wakefulness triggers these -> absence seizure
trimethadione
second-line agent for absence seizures. a metobolite of this drug has same effect on T-type Ca2+ channels as ethosuximide
gabapentin
partial, tonic-clonic seizures. NEUROPATHIC PAIN (most common use). treats post-therapeutic neuralgia. UKNOWN MECHANISM but might act at voltage-gated Ca2+ channels
pregabalin
similar to gabapentin
levetiracetam
broad spectrum antiepileptic. mechanism unkonwn
tigabine
adjuvant for parital seizures. blocks neuronal and glial reuptake of GABA from synapses
phenobarbital
tonic-clonic and partia seizures in children and pregnant women (not a teratogen). prototypical barbiturate increases efficacy of GABA by increasing duration of Cl- channel opening. will suppress seizures at doses that do not produce hypnosis. suppress reticular activating system (when used as hypnotic)
primidone
pro-drug metabolized to phenobarbital
thiopental
parenteral preanesthetic sedative or as adjuvant to local anesthesia. largely replaced by benzos. SHORT ACTING barbiturate (same mechanism as phenobarbital)
thiamylal, methohexital, pentobarbital, secobarbital
all short acting barbiturates
propofol
anesthesia induction: highly lipophilic GABAergic NON-barbiturate with minimal cardiopulmonary side effects. rapid onset and recovery
etomidate
emergency procedure anesthesia: GABAergic, NON-barbiturate with minimal cardiopulmonary side effects
ketamine
PCP derivative producing dissociative anesthesia. inhibits NMDA gluatmate receptor. disorientation, hallucination, bad dreams (arylcyclohexamine family)
diazepam
sedative-hypnotic, anxiolytic, epilepsy (including status epilepticus), prophylaxis for EtOH withdrawl, muscle relaxant. prototypical benzodiazepine. increases potency of GABA by increasing FREQUENCY of Cl- channel opening. suppress reticular activating system.
flumazenil
benzodiazepine analog that competitively inhibits benzo actions. reverses overdose but can precipitate withdrawl symptoms (especially in alcoholics or chronic benzo abusers)
midazolam
SHORT acting benzodiazepine
oxazepam
SHORT acting benzodiazepine
triazolam
SHORT acting benzodiazepine
alprazolam
MEDIUM acting benzodiazepine
estazolam
MEDIUM acting benzodiazepine
lorazepam
MEDIUM acting benzodiazepine
temazepam
MEDIUM acting benzodiazepine
chlordiazepoxide
LONG acting benzodiazepine
clonazepam
LONG acting benzodiazepine
clorazepate
LONG acting benzodiazepine
dizepam
LONG acting benzodiazepine
flurazepam
LONG acting benzodiazepine
flunitrazepam
LONG acting benzodiazepine
zolpidem
short-term for insomnia, RLS: non-benzodiazepine sedative-hypnotic, stimulates omega1 GABAa receptor
baclofen
spasmolytic in MS patients or spinal cord lesions. intractable hiccups. GABA analog selectively activates GABAb receptors (not-ion channels). acts mostly inhibiting spinal cord transmission of reflexes
dantrolene
treatment of malignant hyperthermia & neuroleptic malignant syndrome. spasmolytic that decouples excitation and contraction by blocking release of Ca2+ from SR
halothane
anesthesia (also last resort for status): increases threshold for CNS firing (mechanism unclear). potency of inhaled anesthetics proportional to their lipid solubility. speed of induction/withdrawl INVERSELY proportional to solubility in blood.
nitrous oxide
used in conjunction with more potent anesthetics. low solubility in blood -> rapid induction of anesthesia. low potency (low lipid solubility) permits close regulation of level of anesthesia (least likely of generals to cause decreased BP or increase pCO2)
procaine
local anesthesia. spinal & epidural anesthesia. blocks the inside of voltage sensitive Na+ channels. blocks: RAPID > slow firing, MYELINATED > unmyelinated, SMALLER > large fibers. therefore pain fibers blocked first. often given in combo with alpha1-adrenoreceptor agonist to vasoconstrict and trap drug in local area
articaine
SHORT ACTING amide local anesthetic.
mepivacaine
MEDIUM ACTING amide local anesthetic.
prilocaine
MEDIUM ACTING amide local anesthetic.
lidocaine
MEDIUM ACTING amide local anesthetic
bupivacaine
LONG ACTING amide local anesthetic
etidocaine
LONG ACTING amide local anesthetic
levobuprivacaine
LONG ACTING amide local anesthetic
ropivacaine
LONG ACTING amide local anesthetic
procaine
SHORT ACTING ester local anesthetic
chloroprocaine
SHORT ACTING ester local anesthetic
dibucaine
topical amide local anesthetic
benzocaine
topical ester local anesthetic
tetracaine
topical ester local anesthetic
memantine
alzheimers. blocks NMDA glutamate receptor and my prevent excitotoxicity which leads to disease progression
riluzole
only drug that helps ALS. reduces gluatamate excitotoxicity
modafinil
used for narcolepsy, obstructive sleep apnea. improves wakefulness through unkown mechanism
sumatriptan
acute migraine treatment. 5-HT1b & 5-HT1d agonists decrease cerebral blood flow and vasoactive neurpeptides
ergotamine
acute migraine treatment. ergot alkaloid: partial 5-HT agonist.
buspirone
anxiolytic w/out sedation. selective partial agonist of 5-HT1a receptors
ondansetron
antiemetic. 5-HT3 antagonist for receptors at chemoreceptor trigger zone (CTZ) a.k.a. area postrema
alosetron
diarrhea-predominant IBS, diarrhea from carcinoid syndrome. 5-HT3 antagonist for receptors in GI tract decreasing motility, electrolyte secretion, increasing fluid resporption
amitriptyline
clinical depression. neuropathic and chronic pain. Prototypical tricyclic antidepressant (TCA). Inhibits NE and 5-HT reuptake. Also block histamine receptors, muscarinic receptors, a1 and a2 adrenoceptors.
fluoxetine
clinical depression. bulimia. OCD. anxiolytic. Prototypical SSRI (minima antihistamine, antimuscarinic, or alpha1 adrenoceptor blockade)
nefazodone
clinical depression. Atypical antidepressant, 5-HT and NE reuptake inhibitor. 5-HT2 antagonist.
mirtazapine
clinical depression. Atypical antidepressant. Antagonizes 5-HT2 & 5-HT3 receptors. powerful H1 blocker and very sedating. increased apetitie + weight gain
bupropion
clinical depression. smoking cessation. blocks DA uptake.
phenelzine
clinical depression (third line!). prototypical MAO inhibitor. inhibits both MAO-A (serotonin, epinephrine, NE, tyramine) and MAO-B (dopamine)
selegiline
Parkinson's. MAO-B selective inhibitor.
levodopa + carbidopa
Parkinson's. Precursor that crosses BBB and converted to dopamine by dopa decarboxylase. Carbidopa is a decarboxylase inhibitor (doesn't cross BBB) preventing peripheral conversion of L-Dopa to dopamine (maximizing delivery to CNS)
encaptone
Parkinson's. inhibitor of COMT. COMT degrades dopamine. prolongs L-dopa's effects
tolcapone
Parkinson's. inhibitor of COMT. COMT degrades dopamine. prolongs L-dopa's effects
pramipexole
Parkinson's. Selective D2 and D3 DA receptor agonist.
prochlorperazine
antiemetic, motion sickness. D2 receptor antagonist working at chemoreceptor trigger zone (CTZ) a.k.a. area postrema
chlorpromazine
neuroleptic. prototypical "low-potency" antipsychotic. useful for "positive" symptoms of schizophrenia. blocks D2 receptors in mesocortical and mesolimbic pathways
thioridazine
low-potency neuroleptic (like chlorpromazine)
haloperidol
neuroleptic. prototypical "high-potency" antipsychotic. useful for "positive" symptoms of schizophrenia
clozapine
neuroleptic. atypical anti-psychotic
olanzapine
neuroleptic. atypical anti-psychotic
risperidone
neuroleptic. atypical anti-psychotic