Antiepileptics Flashcards by Robert Stuver

Voltage-gated Na blockers (stabilizers of inactive state)?

Carbamazepine, Oxcarbamazepine, Phenytoin, Lamotrigine

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Carbamazepine class?

Sodium channel blocker

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Carbamazepine for?

Complex partial epilepsy (versus primary generalized), bipolar affective disorder, neuropathic pain

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Carbamazeipine toxicity?

Sedation, ataxia, diplopia

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Carbamazepine adverse reactions?

Rash (rarely, Stevens-Johnson), mild increase in LFTs, mild myelosuppression, contraceptive failure

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Toxicity of carbamazepine is due to?

Epoxide metabolite

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Pharmacologic considerations of carbamazepine?

Highly protein bound; Autoinduction & heteroinduction occur (so much so that increased dose is needed 1-2 weeks into treatment); Short half-life

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`Phenytoin class?

Sodium channel blocker

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Phenytoin for?

Tonic-Clonic seizures of Primary Generalized Epilepsy or Partial onset and Secondary Generalized Seizures. Effective for acute seizures.

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Phenytoin is less effective for what seizures?

Absence, myoclonic, atonic

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Phenytoin toxicity?

Dizziness, nystagmus, ataxia, incoordination

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Phenytoin adverse reactions?

Mild hepatotoxicity, myelosuppression, gingival hyperplasia, rash, hersutism, Lupus-like reaction, contraceptive failure, & (with long term use) cerebellar degeneration, peripheral neuropathy, osteoporosis

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IV infusion of Phenytoin limited by?

Hypotension

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IV Phenytoin for?

Status epilepticus

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Phenytoin half-life?

Longer, can be used for once daily dosing

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Oxcarbazepine class?

Sodium channel blocker

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Oxcarbazepine has the same…

efficacy & indications as Carbamazepine

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How is oxcarbazepine better than carbamazepine?

Less protein bound, less autoinduction, fewer interactions, less toxic, longer half-life

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Oxcarbazepine for?

Complex partial epilepsy (versus primary generalized), bipolar affective disorder, neuropathic pain

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Oxcarbazepine toxicity?

Sedation, ataxia, diplopia

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Oxcarbazepine adverse reactions?

Rash (rarely, Stevens-Johnson), mild increase in LFTs, mild myelosuppression, contraceptive failure

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Lamotrigine class?

Sodium channel blocker

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Lamotrigine for?

Primary Generalized, Partial Complex, Secondary Generalization, Absence. Also: Bipolar Affective, Neuropathic pain

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Unique about Lamotrigine?

Indication for use in children

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Lamotrigine is less effective and may exacerbate?

Myoclonic seizures

Lamotrigine toxicity?

Dizziness, sedation, ataxia, diplopia, can cause contraceptive failure (more so than others)

Lamotrigine adverse reactions?

Rash (rarely, Stevens-Johnson) -- rash is dose related, and slow initial titration is important.

Lamotrigine pharmacological considerations?

Less protein bound, hepatic metabolism, hepatic enzyme inducer

Lamotrigine competes with excretion with?

Valproic acid

Synergistic action with Lamotrigine?

Valproate (Depakote)

Benzodiazepines for?

Status Epilepticus, Anasthesia

Benzodiazepines class?

GABA-A receptor agonists

Benzodiazepine dose limited by?

Sedation. Long term use limited by tolerance

Benzodiasepine timing?

Short acting due to distribution

Name 3 benzodiazepines.

Lorazepam (Ativan) & Diazepam (Valium) & Midazolam (versed)

Midazolam for?

Anasthesia or refractory status epilepticus

Iv half-life of midazolam?

minutes (orally, 1 hr)

Valproate mxn?

Unknown, probably Na channel and GABA system actions

Valproate for?

Broad spectrum. Absence, myoclonic, Tonic-Clonic of Primary Generalized Epilepsy, partial onset, and secondary generalized. IV for status epilepticus. Bioplar affective. Migraine prophylaxis.

5 pharmacoligical considerations of valproate?

Highly protein bound, hepatic mets, rapidly absorbed & metabolized, short half-life, extended release preparations

Valproate toxicity?

Sedation, tremor

Valproate adverse effects?

Nausea, weight gain, hair loss, hyperammonemia, teratogenic. Still, this won't affect BC effectiveness and is considered a "very safe drug"

Phenobarbitol and Benzodiazepines do what?

Bind to GABA receptor

GABA transaminase binder?

Vigabatrine (slows intracellular breakdown of GABA)

GABA reuptake inhibitor?

Tiagabine

GABA channels use what ion?

Chloride

GABA analogs?

Gabapentin & Pregabalin

What do GABA analogs do?

Inhibit Ca current

Gabapentin class?

GABA analog

Pregabalin class?

GABA analog

GABA analogs used for?

Adjunctive treatment for partial complex epilepsy, but especially more commonly for neuropathic pain

What limits gapapentin absorption?

Amino acid transporter in the intestin

Toxicity of gabapentin?

Sedation, but in general NO major organ toxicity

Gabapentin binds proteins? Interacts with other drugs?

Limitedly, no interaction with other drugs

Is gabapentin metabolized by the body?

No evidence of metabolism in humans, eliminated unchanged in urine

Ethosuximide class?

T-type Ca-channel blocker in thalamo-cortical circuits

Ethosuximide for?

Absence seizures only

Ethosuximide side effects?

Transient nausea, sedation, irritability

Ethosuximide absorption and metabolism?

Readily absorbed, minimal first pass metabolism, not protein bound

Topiramate class?

AMPA & Kainate Ca channel blocker; also activity at Na and GABA channels

Topiramate for?

Partial onset, secondarily generalized, primary generalized, migraine prophylaxis.

Topiramate activates what enzyme, causing what?

Carbonic anhydrase --> mild met acidosis --> respiratory compensation --> mild alkalosis --> calcium ionization --> tingling

How can tingling from topiramate be counteracted?

Vitamin C

Besides tingling, adverse reactions of topiramate?

modest weight loss, kidney stones, (rarely) acute glaucoma

Levitiracetam class?

Synaptic vesicle protein 2 binder resulting in less neurotransmitter release

Levetiracetam for?

Partial onset & Secondarily Generalized seizures, maybe primary generalized.

How is levetiracetam tolerated?

Well

Levetiracetam toxicity?

Sedation

Levetiracetam adverse reactions?

Irritability, aphasia, thrombocytopenia

Lithium for?

Bipolar affective mood stabilization, cluster headache

Lithium is cleared how?

Renal

Lithium alters transport of? Where?

Sodium re-absorption in th eproximal tubule

Lithium is contraindicated in?

Those with arrythmia or prone to dehydration

Drug interactions of lithium?

Diuretics, ARB, NSAID

Toxicity of lithium at low levels?

Sedation, dizzy, thirst, inc. urination, fine tremor

Toxicity of lithium at high levels?

Giddiness, ataxia, blurred vision, large amt of dilute urine

Cautions with lithium?

arrythmia, family Hx of sudden death < 45, Brugada syndrome

Antiepileptics Flashcards

(77 cards)