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ph78antiepileptics
pharm78
| Question | Answer |
|---|---|
| side effect of Na channel blockers | Diplopia, Nystagmus, Ataxia, VErtigo, sleepiness, lethargy, cognitive slowing |
| phenytoin | -not for im -no active metabolites -oral dose produce cerebellar-vestibular disturbance -chronic pdm: gingival hyperplasia, hirsutism, osteopenia |
| fosphenytoin | prodrug of pheytoin okay for im |
| carbamazepine | -slow oral abs -induce P450, inc porphyrin formation -epoxide, active metabolite -chronic use cause water retention -NOT FOR acute intermittent porphyria -inc toxicity with LAMOTRIGINE |
| oxcarbazepine | -FDA app for partial seizure -better tolerated at higher levels -MHD metabolite -hyponatremia -no effect on hepatic microsomal ez |
| Valproic acid | -FDA app partial and absence -off-labeled for tonic-clonic -no active metabolites -"fat, shaky, bald, yellow" - acute pancreatitis - hyperammonemia - hepatic tox - inhibit metabolism of phenobarbital and lamotrigine (high protein binding) |
| lamotrigine | -FDA partial seizure -GTC, depression with epilepsy, bipolar depression -metabolized by glucuronidation, good oral abs -t1/2 reduced by phenytoin, carbamazepine, phenobarbital -blood conc dec with oral contraceptives -plasma conc inc with valproic ac |
| topiramate | -FDA partial and GTC -no metabolites -activate hyperpolarizing K current -enhance postsynaptic GABA -limits activation of AMP A kainate (glutamate receptors) -acute myopia w angle closure glaucoma -dec oral contraceptives conc |
| zonisamide | -FDA partial and GTC -metabolized by cyp3a4 -kidney stone!! |
| lacosamide | -cyp2c19 -serine like -inc PR interval, cause conductance pbm |
| rufinamide | new, nothing significant... |
| use of voltage gated Na channel stabilizers | partial and GTC |
| drugs that enhance GABA channel | Benzo, Barbiturate, Topiramate, Flebamate |
| Flabamate not used b/c | hepatic failure, aplastic anemia |
| enhance GABA synthesis | Gabapentin |
| Block GABA reuptake | Tiagabine-marginal benefit |
| Reduce GABA metabolism | Valproic acid, Vigabatrin |
| severe SE of vigabatrin | constrit visual fields |
| clonazepam | for partial, GTC, absence, atonic, myoclonic. |
| diazepam | only, DOC for emergency treatment of status epilepticus |
| phenobarbital | long t1/2, no activate metabolites, inc duration of GABA Cl channel, NOT for AI porphyria |
| primidone | metabozed to PEMA and phenobarbital, with more severe SE |
| what's T type Ca channel | low threshold activated Ca currents, generate rhythmic pacemaker activity in thalamus |