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Pharm 12 GABA/Gluta

Pharm

QuestionAnswer
Inhibits GABA transporters in neurons and glia to increase extra/synaptic GABA for epilepsy. metab by CYP3A4. SE: confuse, sedate, amnesia, ataxia Tiagabine
blocks GABA->succinic semialdehyde, leads to high intracell GABA and increased synaptic GABA release for epilepsy. SE: drowsy, confuse, headache, bilateral visual defects Vigabatrin
Bind at single site of GABAa R to increase channel opening and slow receptor deactivation->increased Cl influx. for anxiety (from depression/schizo) and muscle spasms (from MS). use intermittently. metab by CYP3A4 Diazepam (long) also for focal/tonic-clonic seizures, Alprazolam (intermediate)
Bind at single site of GABAa R to increase channel opening and slow receptor deactivation->increased Cl influx. rapid onset/short acting anxiolytic/sedative/amnestic/and for focal/tonic-clonic seizures. metab by CYP3A4 Midazolam (short)
Bind at single site of GABAa R to increase channel opening and slow receptor deactivation->increased Cl influx. for insomnia. Contra: pulm/cardio disease, brain damage/stroke. metab by CYP3A4 Triazolam (short), Estazolam and Temazepam (intermediate), Flurazepam and Quazepam (long)
Bind at single site of GABAa R to increase channel opening and slow receptor deactivation->increased Cl influx. for absence seizures. metab by CYP3A4 Clonazepam
Reduce neuronal excitability by increasing GABA-mediated inhibition by increasing time Cl channel is open. lipid soluble for anesthesia. metab by CYP450s. SE: overdose->hypnosis, coma, resp depress, death. Thiopental and Methohexital (ultrashort mins), Pentobarbital (short, also for insomnia)
Reduce neuronal excitability by increasing GABA-mediated inhibition by increasing time Cl channel is open. for focal and tonic clonic seizures and status epilepticus. metab CYP450s. barbiturate coma, may exacerbate absence seizures. Phenobarbital (long)
Enhance activation of GABAa Rs and are agonists at high conc. For general anesthesia Etomidate (w hemodynamically unstable pts, also inhibits cortisol/aldosterone synth), Propofol (depresses cardiac output and vasc tone)
Selective GABAb R agonist for spasticity (from MS or spinal cord injury). Oral (no tolerance) or intrathecal. SE: sedation, somnolence, ataxia, overdose->blurry vision, hypotense, cardiac/pulm depress, coma, w/drawl->rhabdomyolysis, pruritus, shock Baclofen
Date rape drugs Chloral Hydrate, Gamma-Hydroxybutyric Acid (GHB), Flunitrazepam (Rohypnol)
volt-gated Na channel blocker that prolongs survival and decreases disease progress in ALS. Riluzole
Noncompetitive NMDA receptor antag for Alzheimers dementia Memantine
Noncompetitive NMDA receptor antag for reducing the severity of dyskinesia in Parkinsons in combo w Levodopa Amantadine
Created by: Jakphooey
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