Analgesic Options Using Antiepileptic Medication

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June 1, 2002

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Table: Antiepileptic Drugs for Pain Management
Drug	Mechanism of Action	Side Effects	Maximum*

Carbamazepine	Slows recovery rate of voltage gated Na+ channels	drowsiness, diplopia, unsteadiness aplastic anemia (1:200,000)	1600 mg/d
Phenytoin	Similar to carbamazepine	nausea, diplopia, dizziness, confusion, gingival hyperplasia, Stevens-Johnson syndrome	600 mg/d
Valproic Acid	Similar to carbamazepine, also increases levels of GABA by decreasing degradation	nausea, vomiting, sedation ataxia, rash, alopecia, appetite stimulation elevated transaminases in 40%	60 mg/kg/d
Clonazepam	Enhancement of the GABA-induced increase in chloride conductance	sedation, lethargy, ataxia, dizziness	20 mg/d
Gabapentin	Uncertain, may have its effect at a central voltage dependent L-type Ca++ channel	drowsiness, somnolence, fatigue	3600 mg/d
Pregabalin	gabapentin analog	not yet approved for clinical use
Lamotrigine	Inhibitor of voltage gated Na+ channels; may suppress glutamate release; may inhibit serotonin reuptake	dizziness, diplopia, drowsiness, rash	900 mg/d
Topiramate	Potentiates GABA responses, increasing CNS GABA levels, blocks the AMPA kainate excitatory receptor, weak carbonic anhydrase inhibitor	abnormal thinking, psychotic thinking, delusional	400 mg/d
Oxcarbezapine	Similar to carbamazepine, may modulate voltage activated Ca++ currents	drowsiness, diplopia, unsteadiness	2400 mg/d
Felbamate	Decreases glutamate synthesis, blocks NMDA receptors	rare hepatotoxicity, aplastic anemia	3600 mg/d
Zonisamide	Na+ channel blockade; T-type Ca++ channel blockade; carbonic anhydrase inhibitor		600 mg/d
Tiagabine	GABA reuptake inhibitor; future potential for the treatment of painful conditions		60 mg/d
Vigabatrin	GABA metabolism inhibitor; future potential for the treatment of painful conditions		4000 mg/d

N.B. Only carbamazepine, phenytoin, gabapentin, and lamotrigine have been evaluated in double-blind trials (JAMA.* 1998;280:1837-1842; Pain. 1997; 73:223-230). Always begin with a low dose, preferably at bedtime. Increase gradually until side effects occur. Maximum dose may be exceeded if patient is tolerant. Pain relief may be gradual; wait 4-8 weeks at therapeutic dosage before moving to a different agent.

Analgesic Options Using Antiepileptic Medication

Analgesic Options Using Antiepileptic Medication

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