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.  
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  
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  
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  
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  
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.  
OXAZEPAM   Mechanism: Increase chloride channel opening frequency through binding to GABAa receptors. Uses: Sleep disorders, anxiety. "Out The Liver" metabolism to inactive compound.  
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.  
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  
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  
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  
ETHYLENE GLYCOL   Anti-freeze. Metabolized to Glycoaldehyde, Glycolic acid and Oxalic acid (toxic). Causes CNS depression, severe metabolic acidosis, deadly nephrotoxicity.  
METHANOL   All toxic metabolites. First formaldehyde, then to formic acid. Causes respiratory failure, severe anion gap metabolic acidosis and ocular damage.  
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.  
ETHOSUXIMIDE   Mechanism: Blocks T-type Ca channels in thalamic n. DOC in absence seizures. Safe in pregnancy. SE: dramatic GI distress.  
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  
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.  
GABAPENTIN   M: increases GABA effects. Use: seizure states, neuropathic pain, BAD. SE: rare, aplastic anemia, liver failure.  
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).  
TOPIRAMATE   (blank)  
TIAGABIN   (blank)  
VIGABATRIN   (blank)  
HALOTHANE   (blank)  
NITROUS OXIDE   (blank)  
SUCCINYLCHOLINE   (blank)  
ATRACURIUM   (blank)  
MIVACURIUM   (blank)  
D-TUBOCURARINE   (blank)  
LIDOCAINE   (blank)  
BUPIVACAINE   (blank)  
MEPIVACAINE   (blank)  
PROCAINE   (blank)  
COCAINE   (blank)  
MORPHINE   (blank)  
MEPERIDINE   (blank)  
METHADONE   (blank)  
FENTANYL   (blank)  
HEROIN   (blank)  
BUPRENORPHINE   (blank)  
CODEINE   (blank)  
NALBUPHINE   (blank)  
NALOXONE   (blank)  
NALTREXONE   (blank)  
CHLORPROMAZINE   (blank)  
FLUPHENAZINE   (blank)  
THIORIDAZINE   (blank)  
HALOPERIDOL   (blank)  
CLOZAPINE   (blank)  
RISPERIDONE   (blank)  
OLANZAPINE   (blank)  
ARIPIPRAZOLE   (blank)  
LEVODOPA   (blank)  
BROMOCRIPTINE   (blank)  
PERGOLIDE   (blank)  
PRAMIPEXOLE   (blank)  
SELEGILINE   (blank)  
CARBIDOPA   (blank)  
BENZTROPINE   (blank)  
TRIHEXIPHENIDYL   (blank)  
TOLCAPONE   (blank)  
AMANTADINE   (blank)  
PHENELZINE   (blank)  
TRANYLCYPROMINE   (blank)  
AMITRIPTYLINE   (blank)  
IMIPRAMINE   (blank)  
CLOMIPRAMINE   (blank)  
FLUOXETINE   (blank)  
PAROXETINE   (blank)  
SERTRALINE   (blank)  
BUPROPION   (blank)  
MIRTAZAPINE   (blank)  
TRAZODONE   (blank)  
VENLAFAXINE   (blank)  
LITHIUM   (blank)  
METHYLPHENYDATE   (blank)  
ATOMOXETINE   (blank)  


   

 
 

 
 

 

 

 
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