| 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) |
