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PHARMACOLOGY

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CNS DRUG LIST
Key Information
PHENOBARBITAL   Mechanism: Prolong GABAa activity therefore increase Chloride channel opening. GABA mimetic at high doses. Used for seizure states. No antidote in OD. Safest anticonvulsant during pregnancy for general tonic-clonic seizures and partial seizures.  
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ALPRAZOLAM   Mechanism: Increase the frequency of Cl channel opening. No GABA mimetic activity. BZ1 mediates sedation, hypnotic while BZ2 mediates antianxiety, impairment of cognitive functions, muscle relaxant, etc. Uses: anxiety, panic, phobias Most widely used BZ  
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DIAZEPAM(VALIUM)   Mechanism: GABAa binding to increase frequency of chloride channel opening. No GABA mimetic activity. Uses: Muscle relaxation, withdrawal states (cross-dependence), status epilepticus  
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LORAZEPAM(ATIVAN)   Mechanism: Bind to GABAa BZ binding site to increase frequency of chloride channel opening. No GABA mimetic activity. Uses: Status epilepticus(IV), preop sedation. Metabolized "Out The Liver" to non active compounds  
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MIDAZOLAM(DORMICUM/VERSED)   Mechanism: Bind to GABAa BZ binding site to increase Chloride channel opening frequency. No GABA mimetic activity. Uses: Preop sedation, anesthesia(IV) because of anterograde amnesia and sedation  
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TEMAZEPAM   Mechanism: Bind to BZ binding site on GABAa receptor to increase frequency of Chloride channel opening. No GABA mimetic activity. Uses: Sleep disorders. "Out The Liver" metabolism to inactive compound.  
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OXAZEPAM   Mechanism: Increase chloride channel opening frequency through binding to GABAa receptors. Uses: Sleep disorders, anxiety. "Out The Liver" metabolism to inactive compound.  
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BUSPIRONE   Mechanism: 5HT1a partial agonist with no effect on GABA (non-sedative). Uses: Generalized anxiety disorders (not for situational anxiety disorders). PK: Takes around 1-2 weeks for effects.  
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ZOLPIDEM / ZALEPLON   Mechanism: BZ1 receptor agonist with less effect on BZ2 mediated functions. Uses: Sleep disorders. Less tolerance and abuse liability. Overdose reversed by flumazenil  
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FLUMAZENIL   Mechanism: Blocks the BZ1 or BZ2 binding sites on GABA receptors. Uses: To reverse CNS depression caused by BZs overdose. PK: Very short duration of action  
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ETHANOL   CNS depressant, causes metabolic acidosis (ketones). Acetaldehyde toxicity. FAS: growth restriction, midfacial hypoplasia, microcephaly, frequent mental retardation. Disulfiram like: Metronidazole, Cefamandole, Cefoperazone, Cefotetan, Chlorpropamide  
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ETHYLENE GLYCOL   Anti-freeze. Metabolized to Glycoaldehyde, Glycolic acid and Oxalic acid (toxic). Causes CNS depression, severe metabolic acidosis, deadly nephrotoxicity.  
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METHANOL   All toxic metabolites. First formaldehyde, then to formic acid. Causes respiratory failure, severe anion gap metabolic acidosis and ocular damage.  
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CARBAMAZEPINE   Mechanism: Blocks Na channels in their inactivated state. Used in seizure states. DOC for trigeminal neuralgia. PK induces CYP450. SE: CNS depression, osteomalacia, megaloblastic anemia, increased ADH secretion, exfoliative dermatitis, aplastic anemia.  
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ETHOSUXIMIDE   Mechanism: Blocks T-type Ca channels in thalamic n. DOC in absence seizures. Safe in pregnancy. SE: dramatic GI distress.  
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VALPROIC ACID   Mechanism: Blocks axonal Na channels, inhibition of GABA transaminase, T-type Ca channel block. Use: Broadspectrum antiepileptic, BAD, migraine (prophylaxis) SE: LT Hepatotoxicity and Pancreatitis, Thrombocytopenia, alopecia. Spina Bifida  
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PHENYTOIN   M: Blocks axonal Na channels inactive state. Use: in seizure states. PK: variable absorption, CYP450 induction, zero-order kinetic elimination SE: CNS depression, gingival hyperplasia, hirsutism, acne, osteomalacia, megaloblastic anemia, aplastic anemia.  
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GABAPENTIN   M: increases GABA effects. Use: seizure states, neuropathic pain, BAD. SE: rare, aplastic anemia, liver failure.  
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FELBAMATE/LAMOTRIGINE   M: Block Na channel and glutamate receptors. Use: in seizure states. SE: LT hepatotoxicity and aplastic anemia (mostly FELBAMATE). Stevens Johnson syndrome (lamotrigine).  
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TOPIRAMATE   (blank)  
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TIAGABIN   (blank)  
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VIGABATRIN   (blank)  
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HALOTHANE   (blank)  
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NITROUS OXIDE   (blank)  
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SUCCINYLCHOLINE   (blank)  
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ATRACURIUM   (blank)  
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MIVACURIUM   (blank)  
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D-TUBOCURARINE   (blank)  
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LIDOCAINE   (blank)  
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BUPIVACAINE   (blank)  
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MEPIVACAINE   (blank)  
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PROCAINE   (blank)  
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COCAINE   (blank)  
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MORPHINE   (blank)  
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MEPERIDINE   (blank)  
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METHADONE   (blank)  
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FENTANYL   (blank)  
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HEROIN   (blank)  
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BUPRENORPHINE   (blank)  
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CODEINE   (blank)  
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NALBUPHINE   (blank)  
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NALOXONE   (blank)  
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NALTREXONE   (blank)  
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CHLORPROMAZINE   (blank)  
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FLUPHENAZINE   (blank)  
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THIORIDAZINE   (blank)  
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HALOPERIDOL   (blank)  
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CLOZAPINE   (blank)  
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RISPERIDONE   (blank)  
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OLANZAPINE   (blank)  
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ARIPIPRAZOLE   (blank)  
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LEVODOPA   (blank)  
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BROMOCRIPTINE   (blank)  
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PERGOLIDE   (blank)  
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PRAMIPEXOLE   (blank)  
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SELEGILINE   (blank)  
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CARBIDOPA   (blank)  
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BENZTROPINE   (blank)  
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TRIHEXIPHENIDYL   (blank)  
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TOLCAPONE   (blank)  
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AMANTADINE   (blank)  
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PHENELZINE   (blank)  
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TRANYLCYPROMINE   (blank)  
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AMITRIPTYLINE   (blank)  
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IMIPRAMINE   (blank)  
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CLOMIPRAMINE   (blank)  
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FLUOXETINE   (blank)  
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PAROXETINE   (blank)  
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SERTRALINE   (blank)  
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BUPROPION   (blank)  
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MIRTAZAPINE   (blank)  
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TRAZODONE   (blank)  
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VENLAFAXINE   (blank)  
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LITHIUM   (blank)  
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METHYLPHENYDATE   (blank)  
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ATOMOXETINE   (blank)  
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