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60 Cards in this Set
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Opioids
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Morphine, fentanyl, codeine, heroin, methadone, meperidine, destromethorphan
agonist at mu rectprs,open K+ channels decreasing vesicle release of ACh, NE, 5-HT, glutamate, substance P |
Use: pain, cough suppressant (dextromethorpan), diarrhea (loperamide and diphenoxylate), acute pulmonary edema. maintenance for addicts (methadone)
Toxicity: addiction, respiratory depression, constipation, miosis, additive CNS depression with other drugs, no tolerance to miosis and constipation. treat with naloxone/naltrexone |
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Butorphanol
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partial agonist at mu receptors and kappa receptors
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Use: pain, causes less respiratory depression than full agonist
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tramodol
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weak opioid agonist and inhibits serotonin and NE reuptake
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use: chronic pain
Toxicity: similar to opioids, decreases the seizure threshold |
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Phenytoin
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increase sodium channel inactivation, increase refractory period, inhibit glutamate release from excitatory neurons
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Use: GTC seizures, class IB antiarrythmics
nystagmus, diploxia, ataxia, sedation, gingival hyperplasia, hirsuitism, megaloblastic anemia (decreased folate absorption), teratogenesis (fetal hydantoin syndrome), SLE like syndrome, P450 inducer, peripheral neuropathy |
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Carbamazepine
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increases sodium channel inactivation
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diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, P450 inducter, SIADH, stevens-johnson syndrome
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Lamotrigine
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blocks voltage gated sodium channels
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stevens-johnson
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gabapentin
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inhibits calcium channels
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sedation, ataxia
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topiramate
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blocks sodium channels, increase GABA action
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sedation, mental dulling, kidney stones, weight loss
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phenobarbital
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increase GABA action by increasing the duration of Cl channel opening
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Use: sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)
Toxicity: sedation, tolerance, dependence, P450 inducer, respiratory or cardiac depression, drug interactions because of induction of liver microsomal enzymes Treat overdose with symptom management |
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valproic acid
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increase sodium channel inactivation, increase GABA concentration
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GI distress, rare but fatal hepatotoxicity, neural tube defects, tremor, weight gain
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diazepam
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facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
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Use: anxiety, spasticity, status epilepticus, detoxification, night terrors, sleep walking, general anesthetic, hypnotic
Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates Treat OD with flumazenil |
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lorazepam
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facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
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Use: anxiety, spasticity, status epilepticus, detoxification, night terrors, sleep walking, general anesthetic, hypnotic
Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates Treat OD with flumazenil |
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triazolam
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facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep, short acting
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Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic
Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates Treat OD with flumazenil |
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oxazepam
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facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep, short acting
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Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic
Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates Treat OD with flumazenil |
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midzolam
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facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep, short acting
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Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic
Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates Treat OD with flumazenil |
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chlordiazepoxide
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facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
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Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic
Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates Treat OD with flumazenil |
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alprazolam
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facilitate GABA action by increasing frequency of Cl channel opening, decreases REM sleep
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Use: anxiety, spasticity, detoxification, night terrors, sleep walking, general anesthetic, hypnotic
Toxicity: dependence, additive CNS depression effects with alochol, less risk of respiratory dpression and coma than with barbituates Treat OD with flumazenil |
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zolpidem
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act via the BZ1 receptor subtye and is reversed by flumazenil
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Use: non-anxiety related insomnia
Toxicity: ataxia, headaches, confusion. short duration with rapid metabolism by liver. only modest day after psychommotor depression and few amnestic effects |
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zaleplon
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act via the BZ1 receptor subtye and is reversed by flumazenil
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Use: non-anxiety related insomnia
Toxicity: ataxia, headaches, confusion. short duration with rapid metabolism by liver. only modest day after psychommotor depression and few amnestic effects |
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eszopiclone
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act via the BZ1 receptor subtye and is reversed by flumazenil
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Use: non-anxiety related insomnia
Toxicity: ataxia, headaches, confusion. short duration with rapid metabolism by liver. only modest day after psychommotor depression and few amnestic effects |
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halothane
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myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
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hepatotoxicity
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enflurane
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myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
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proconvulsant
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isoflurane
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myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
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sevoflurane
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myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
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methoxyflurane
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myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
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nephrotoxicity
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nitrous oxide
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myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreases demand)
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expansion of trapped gas
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thiopental
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IV anesthetic, high potency, high lipid solubility
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induction of anesthesia and short surgical procedures
effect terminated by redistribution to fat and tissue , decreases cerebral blood flow |
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midazolam
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IV anesthetic, adjunctively with gaseous anesthetics and narcotics
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most common drug for endoscoppy
postoperative respiratory depression, decreased BP (treat OD with flumazenil), and amnesia |
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Ketamine
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IV anesthetic, dissociative anesthetic, blocks NMDA receptors
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cardiovascular stimulant
disorientation, hallucination, bad dreams, increases cerebral blood flow |
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morphine and fentanyl
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IV anesthetic with other CNS depressants during general anasthesia
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propofol
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IV anesthetic, potentiates GABA receptor
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rapid anesthesia induction and short procedures
less post-operative nausea than thiopental |
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Local anesthetics - esters
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procaine, cocaine, tetracaine
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Local anesthetics - amides
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lidocaine, mepivacaine, bupivacaine
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Local anesthetics`
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block Na channels on inner portation of channel preferentially at activated NA channels (rapidly firing neurons)
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in infected tissue, alkaline anesthetics are charged, so they can't penetrate tissue - need more
small diameter nerve fibers blocked more readibly than large, myelin more than non-myelin and size matters more |
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Local anesthetics Use
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minor surgical procedures, spinal anesthesia
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toxicity: CNS excitation, severe CV toxicity (bupicaine), hypertension, hypotension, arrythmias (cocaine)
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Succinylcholine
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selective for motor nicotinic receptor, depolarizing NM blocking drug
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Phase I - prolonged depolarization (no antidote)
Phase II - repolarized but blocked, reverse with neostigmine |
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tubocurarine
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nondepolarizing muscle blocking drugs, compete with ACh for receptors
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reverse blockade with cholinesterase inhibitors
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atracurium
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nondepolarizing muscle blocking drugs, compete with ACh for receptors
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reverse blockade with cholinesterase inhibitors
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mivacurium
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nondepolarizing muscle blocking drugs, compete with ACh for receptors
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reverse blockade with cholinesterase inhibitors
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pancuronium
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nondepolarizing muscle blocking drugs, compete with ACh for receptors
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reverse blockade with cholinesterase inhibitors
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vecuronium
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nondepolarizing muscle blocking drugs, compete with ACh for receptors
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reverse blockade with cholinesterase inhibitors
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rocuronium
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nondepolarizing muscle blocking drugs, compete with ACh for receptors
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reverse blockade with cholinesterase inhibitors
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dantrolene
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prevents release of Ca from sarcoplasmic reticulum of skeletal muscle
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Use: malignant hyperthermia from inhalation anesthetics and succinylcholine & neuroleptic malignant syndrome
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Bromocriptine
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agonize dopamine receptors
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Use: Parkinson's
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pramipexole
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agonize dopamine receptors
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Use: Parkinson's
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ropinirole
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agonize dopamine receptors
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Use: Parkinson's
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amantadine
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agonize dopamine receptors and may increase dopamine levels
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Use: parkinson's and antiviral against influenza A
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L-dopa/Carbidopa
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L dopa can cross BBB and is converted to dopamine in CNS and carbidopa inhibits peripheral conversion
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Use: Parkinsonism
Toxicity: arrhythmias from peripheral conversion, long term can cause dyskinesia after administration and akinesia between doses; these are limited by carbidopa |
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selegiline
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selective MAO B inhibitor which preferentially metabolizes dopamine over NE and serotonin, increasing availability of dopamine
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Use: Parkinson's with L-dopa
Toxicity: may enhance adverse of L-dopa |
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entacapone
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COMT inhibitor, prevents L dopa degredation and increases availability
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Use: Parkinson's
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tolcapone
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COMT inhibitor, prevents L dopa degredation and increases availability
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Use: Parkinson's
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benzotropine
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curb excess cholinergic activity, antimuscarinic
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Parkinson's; improves tremor and rigiditiy but has little effect on bradykinesia
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essential/familial tremors
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beta blockers
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memantine
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NMDA receptor antagonist that helps prevent excitotoxicity
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Use: Alzheimer's
Toxicity: dizziness, confusion, hallucinations |
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donepezil
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acetylcholineresterase inhibitor
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nausea dizziness, insomnia
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galantamine
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acetylcholineresterase inhibitor
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nausea dizziness, insomnia
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rivastigmine
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acetylcholineresterase inhibitor
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nausea dizziness, insomnia
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reserpine and tetrabenazine
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amine depleting
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huntington's
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haloperidol
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dopamine receptor antagonist
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huntington's
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sumatriptan
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5HT1b/1d agpnost. causes vasconstriction and inhibits trigeminal activation and vasoactive peptide release, t1/2 = less than hours
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Use: acute migraine, cluster H/As
Toxicity: coronary vasospasm (contraindicated in patients with CAD and prinzmetal's angina), mild tingling |