Ethosuximide (Zarontin)

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Name: Ethosuximide (Zarontin)

Class: Antiepileptic Agent (Absence)

Mechanism: Reduces T-channel Ca2+ currents ® ­ seizure threshold.

Absorption:

Dist.: 0% protein binding.

Metabolism.:

Excretion, : 20-60 hr (adults & kids)

Toxicity/S.E.s: Dose-related—anorexia, nausea, fatigue, headache. Non-dose-rel.—blood-dyscrasia, SLE-like rxn, hepatitis.

Utility: A DOC for uncomplicated absence.

Special Features:

 

Valproate (Depakote, Depakene)

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Name: Valproate (Depakote, Depakene)

Class: Antiepileptic Agent (Absence/Tonic-Clonic/Complex-Partial)

Mechanism: Multiple. Reduces T-channel Ca2+ currents ® ­ seizure threshold. May enhance GABAergic neurotransmission. Inhib. sustained high freq. repetitive neuron firing.

Dist.: 80-95% protein binding.

Excretion, : 6-15 hr (adults), 8-15 hr (kids).

Toxicity/S.E.s: Dose-rel.—GI upset, ­ liver enzymes, tremor, hyperammonemia, initial somnolence, behavioral changes. Non-dose-rel.—weight gain, nausea, hair loss, changes in hair texture. Idiosync.—Reye-like synd,. fetal drug effects, hepatic failure (esp. kids <2 style=""> Drug interactions (¯ w/carbamazepine, phenobarbital, phenytoin; ­ w/felbamate).

Utility: A DOC for uncomp. gen. absence. A DOC for gen. tonic-clonic seizures. DOC for atypical absence, myoclonic & atonic epilepsy. Treat 1° & 2° gen. partial & complex-partial seizures. Treatment of bipolar disorder and mgt. of aggression or violence (off-label).

Special Features:

 

Carbamazepine (Tegretol)

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Name: Carbamazepine (Tegretol)

Class: Antiepileptic Agent (Tonic-Clonic/Complex-Partial)

Mechanism: Blocks voltage-dependent Na+ channels ® inhib. of sustained high-freq repetitive neuron firing.

Absorption:

Dist.: 66-89% protein binding.

Metabolism.:

Excretion, : 14-27 hr (adults), 8-28 hr (kids)

Toxicity/S.E.s: Dose-related—double vision, blurred vision, vertigo, cognitive impairment, lethargy, behavioral changes, dyskinesias, cardiac condxn disturbances. Non-dose-rel.—diarrhea, fluid retention. Idiosync.—granulocyte suppression, allergic dermatitis, Stevens-Johnson synd., aplastic anemia, hepatic & kidney failure. Signif. drug interactions (¯ w/phenobarbital, phenytoin, primidone, felbamate).

Utility: A DOC for generalized tonic-clonic seizures. A DOC for 1° & 2° generalized partial and complex-partial seizures. Treatment of pain assoc. w/true trigeminal neuralgia (off-label). Management of acute mania and maintenance of bipolar affective disorder (off-label).

 

Phenytoin (Dilantin)

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Name: Phenytoin (Dilantin)

Class: Antiepileptic Agent (Tonic-Clonic/Complex-Partial)

Mechanism: Blocks voltage-dependent Na+ channels ® inhib. of sustained high-freq repetitive neuron firing.

Absorption:

Dist.: 69-96% protein binding.

Metabolism.:

Excretion, : 10-34 hr (adults), 5-140 hr (kids).

Toxicity/S.E.s: Dose-related—nystagmus, cognitive impairment, incoordination, dyskinesias, seizure exacerbation. Non-dose-related—hirsutism, coarsening of facial features, exacerbation of acne, gingival hyperplasia, osteopenia, neuropathy, folate deficiency anemia. Idiosync.—allergic dermatitis, fetal drug effects, hepatic failure, serum sickness rxn, SLE-like rxn, hyperglycemia, aplastic anemia, granulocyte suppression. Drug interactions (­ w/carbamazepine, felbamate; ¯ w/valproic acid).

Utility: A DOC for generalized tonic-clonic seizures. A DOC for 1° & 2° generalized partial and complex-partial seizures.

Special Features:

 

Other Migraine Drugs

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Other Migraine Drugs

b Blockers: Propanolol, timolol, nadolol, metoprolol for continuous prophylaxis. S.E.s include fatigue, depression, orthostatic hypotension. C/I in asthmatics & congestive heart failure patients.

Ca2+ Channel Blockers: Verapamil & flunarazine ® moderatey efficacious prophylaxis.

Analgesics: Fiorinal: aspirin + caffeine + butalbital. Midrin: acetaminophen + isometheptene (sympathomimetic) + dichloralphenazone (sedative). NSAIDS, esp. naproxen sodium (but ¯ gastric motility during acute attack may interfere w/absorption). Butorphanol (opioid agonist antagonist) nasal spray. Methadone (IM).

Overuse may cause a headache (“analgesic rebound”).