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Stack #138478
PHARMACOLOGY
| 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) |
Created by:
drjosefrancisco
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