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104 Cards in this Set
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naloxone
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mu antagonist used to treat opioid overdose
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nalmefene
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more potent mu antagonist used for opioid overdose and post operative opioid reversal
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naltrexone
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mu antagonist PO long half life
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methadone
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mu agonist similar to morphine. analgesic, oral, LONG half-life, persistent effects on repeat admin so used to treat opioid withdrawal symptoms
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diphenoxylate
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mu agonist that doesn't get absorbed systemically. used for diahrrea
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pentazocine
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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.
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nalbuphine
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agonist at kappa receptors, COMPLETE antagonist at mu receptors. similar to pentazocine in uses
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codeine
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methylated morphine (mu agonist) beter PO. weaker because must be demethylated to act.
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oxycodone
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long acting potent mu agonist given in combo with NSAID or acetaminphen to decrease dose
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hydrocodone
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potent mu agonist given in combo with NSAID or acetaminphen to decrease dose
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dextromethorophan
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OTC antitussive, d-isomer of a methylated opioid. no analgesic/addictive properties
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morphine
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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.
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hydromophone
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similar to morphine, strong mu agonist and weak kappa and delta agonist
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oxymorphone
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similar to morphine, strong mu agonist and weak kappa and delta agonist
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levorphanol
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similar to morphine, strong mu agonist and weak kappa and delta agonist
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merperidine
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mu agonist. does NOT precipitate biliary colic, so use for patients when you haven't ruled out cholestasis
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fentanyl
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short-acting IV mu agonist used for anesthesia. also on patches for cancer pain
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sufentanil
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short-acting IV mu agonist used for anesthesia.
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alfentanil
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short-acting IV mu agonist used for anesthesia.
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remifentanil
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short-acting IV mu agonist used for anesthesia.
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heroin
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derived form morphine. penetrates CNS BBB much faster.
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lithium
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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
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phenytoin
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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)
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fosphenytoin
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water soluble prodrug of phenytoin
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lamotrigine
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partial and tonic clonic seizures (occaisonally absence/mixed): blocks inactivated Na+ channels and thus inhibits rapidly/repeatedly firing neurons (analagous to class IB antiarrhythmics).
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zonisamide
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partial, tonic clonic, absence, and myoclonic seizures: blocks inactivated Na+ channels and T-type Ca2+ channels.
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carbamazepine
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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
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oxcarbazepine
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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
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topiramate
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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
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felbamate
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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.
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valproic acid
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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
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ethosuximide
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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
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trimethadione
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second-line agent for absence seizures. a metobolite of this drug has same effect on T-type Ca2+ channels as ethosuximide
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gabapentin
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partial, tonic-clonic seizures. NEUROPATHIC PAIN (most common use). treats post-therapeutic neuralgia. UKNOWN MECHANISM but might act at voltage-gated Ca2+ channels
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pregabalin
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similar to gabapentin
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levetiracetam
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broad spectrum antiepileptic. mechanism unkonwn
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tigabine
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adjuvant for parital seizures. blocks neuronal and glial reuptake of GABA from synapses
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phenobarbital
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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)
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primidone
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pro-drug metabolized to phenobarbital
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thiopental
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parenteral preanesthetic sedative or as adjuvant to local anesthesia. largely replaced by benzos. SHORT ACTING barbiturate (same mechanism as phenobarbital)
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thiamylal, methohexital, pentobarbital, secobarbital
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all short acting barbiturates
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propofol
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anesthesia induction: highly lipophilic GABAergic NON-barbiturate with minimal cardiopulmonary side effects. rapid onset and recovery
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etomidate
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emergency procedure anesthesia: GABAergic, NON-barbiturate with minimal cardiopulmonary side effects
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ketamine
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PCP derivative producing dissociative anesthesia. inhibits NMDA gluatmate receptor. disorientation, hallucination, bad dreams (arylcyclohexamine family)
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diazepam
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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.
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flumazenil
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benzodiazepine analog that competitively inhibits benzo actions. reverses overdose but can precipitate withdrawl symptoms (especially in alcoholics or chronic benzo abusers)
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midazolam
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SHORT acting benzodiazepine
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oxazepam
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SHORT acting benzodiazepine
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triazolam
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SHORT acting benzodiazepine
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alprazolam
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MEDIUM acting benzodiazepine
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estazolam
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MEDIUM acting benzodiazepine
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lorazepam
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MEDIUM acting benzodiazepine
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temazepam
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MEDIUM acting benzodiazepine
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chlordiazepoxide
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LONG acting benzodiazepine
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clonazepam
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LONG acting benzodiazepine
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clorazepate
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LONG acting benzodiazepine
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dizepam
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LONG acting benzodiazepine
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flurazepam
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LONG acting benzodiazepine
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flunitrazepam
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LONG acting benzodiazepine
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zolpidem
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short-term for insomnia, RLS: non-benzodiazepine sedative-hypnotic, stimulates omega1 GABAa receptor
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baclofen
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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
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dantrolene
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treatment of malignant hyperthermia & neuroleptic malignant syndrome. spasmolytic that decouples excitation and contraction by blocking release of Ca2+ from SR
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halothane
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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.
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nitrous oxide
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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)
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procaine
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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
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articaine
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SHORT ACTING amide local anesthetic.
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mepivacaine
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MEDIUM ACTING amide local anesthetic.
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prilocaine
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MEDIUM ACTING amide local anesthetic.
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lidocaine
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MEDIUM ACTING amide local anesthetic
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bupivacaine
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LONG ACTING amide local anesthetic
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etidocaine
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LONG ACTING amide local anesthetic
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levobuprivacaine
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LONG ACTING amide local anesthetic
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ropivacaine
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LONG ACTING amide local anesthetic
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procaine
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SHORT ACTING ester local anesthetic
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chloroprocaine
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SHORT ACTING ester local anesthetic
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dibucaine
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topical amide local anesthetic
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benzocaine
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topical ester local anesthetic
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tetracaine
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topical ester local anesthetic
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memantine
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alzheimers. blocks NMDA glutamate receptor and my prevent excitotoxicity which leads to disease progression
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riluzole
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only drug that helps ALS. reduces gluatamate excitotoxicity
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modafinil
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used for narcolepsy, obstructive sleep apnea. improves wakefulness through unkown mechanism
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sumatriptan
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acute migraine treatment. 5-HT1b & 5-HT1d agonists decrease cerebral blood flow and vasoactive neurpeptides
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ergotamine
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acute migraine treatment. ergot alkaloid: partial 5-HT agonist.
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buspirone
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anxiolytic w/out sedation. selective partial agonist of 5-HT1a receptors
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ondansetron
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antiemetic. 5-HT3 antagonist for receptors at chemoreceptor trigger zone (CTZ) a.k.a. area postrema
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alosetron
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diarrhea-predominant IBS, diarrhea from carcinoid syndrome. 5-HT3 antagonist for receptors in GI tract decreasing motility, electrolyte secretion, increasing fluid resporption
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amitriptyline
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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.
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fluoxetine
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clinical depression. bulimia. OCD. anxiolytic. Prototypical SSRI (minima antihistamine, antimuscarinic, or alpha1 adrenoceptor blockade)
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nefazodone
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clinical depression. Atypical antidepressant, 5-HT and NE reuptake inhibitor. 5-HT2 antagonist.
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mirtazapine
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clinical depression. Atypical antidepressant. Antagonizes 5-HT2 & 5-HT3 receptors. powerful H1 blocker and very sedating. increased apetitie + weight gain
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bupropion
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clinical depression. smoking cessation. blocks DA uptake.
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phenelzine
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clinical depression (third line!). prototypical MAO inhibitor. inhibits both MAO-A (serotonin, epinephrine, NE, tyramine) and MAO-B (dopamine)
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selegiline
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Parkinson's. MAO-B selective inhibitor.
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levodopa + carbidopa
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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)
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encaptone
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Parkinson's. inhibitor of COMT. COMT degrades dopamine. prolongs L-dopa's effects
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tolcapone
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Parkinson's. inhibitor of COMT. COMT degrades dopamine. prolongs L-dopa's effects
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pramipexole
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Parkinson's. Selective D2 and D3 DA receptor agonist.
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prochlorperazine
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antiemetic, motion sickness. D2 receptor antagonist working at chemoreceptor trigger zone (CTZ) a.k.a. area postrema
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chlorpromazine
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neuroleptic. prototypical "low-potency" antipsychotic. useful for "positive" symptoms of schizophrenia. blocks D2 receptors in mesocortical and mesolimbic pathways
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thioridazine
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low-potency neuroleptic (like chlorpromazine)
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haloperidol
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neuroleptic. prototypical "high-potency" antipsychotic. useful for "positive" symptoms of schizophrenia
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clozapine
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neuroleptic. atypical anti-psychotic
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olanzapine
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neuroleptic. atypical anti-psychotic
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risperidone
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neuroleptic. atypical anti-psychotic
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