PHARMACOLOGY
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| 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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