TABLE 9.
Agent | Dose range (mg/day) | Mechanism of action | Indications supported by at least one RCT* | Side effects | Comments |
---|---|---|---|---|---|
Gabapentin (Neurontin†) | 1200–3600 | N-type calcium channel blocker | PHN, DN, mixed neuropathic pain | Sedation, dizziness ataxia, confusion | Does not require metabolism in liver, so is a better choice in liver dysfunction; clearance will be diminished in renal dysfunction |
Pregabalin (Lyrica†) | 150–600 | α2-δ protein of voltage- gated calcium channels | PHN, DN | Dizziness, somnolence | Analgesic effect is seen within first three days; does not require liver metabolism; renal excretion primary route of elimination |
Carbamazepine (Tegretol‡) | 200–2000§ | Sodium channel blockade | TN | Sedation, dizziness, ataxia, diplopia, hepatitis, rash, hyponatremia | CBC, electrolyte and liver function studies pretreatment and every two weeks for three months, then less frequently§ (the hyponatremia may result in a confusional state); most serious potential side effects are aplastic anemia, hepatitis, serious dermatological reactions¶ |
Lamotrigine (Lamictal**) | 200–400 | Sodum channel blockade | TN, DN, poststroke pain, spinal cord injury | Mild rash to serious dermatological reactions†† | CBC and liver function studies pretreatment and at four weeks |
Oxcarbazepine (Trileptal‡) | 600–1200 | Sodium channel blockade | TN | Sedation, headache, dizziness, rash¶, vertigo, ataxia, nausea, diplopia, hyponatremia | CBC, electrolyte and liver function studies pretreatment and at four weeks
Serious dermatological reactions and multiorgan hypersensitivity reactions have been reported |
Topiramate (Topamax‡‡) | 50–200 | Sodium channel blockade, ↑ GABA inhibition, ↓ glutamate excitation, modulates calcium channels | Migraine prophylaxis | Paresthesia, fatigue, nausea, anorexia, weight loss, changes in taste | Effect is modest; topiramate was associated with approximately one less migraine per month than placebo in three large RCTs |
For details see section relating to the specific agent in the text;
Pfizer Canada Inc;
Novartis Pharmaceuticals Canada Inc;
Doses of up to 2000 mg/day may be required in trigeminal neuralgia (TN) (116);
Life threatening dermatological reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis and lupus may be serious and require discontinuation of carbamazepine and oxcarbazepine;
GlaxoSmithKline Inc, Canada;
Rash ranging from simple morbilliform type to potentially serious rashes, including Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported (283);
Janssen-Ortho Inc, Canada. CBC Complete blood count; DN Diabetic neuropathy; GABA Gamma-aminobutyric acid; PHN Postherpetic neuralgia; RCT Randomized, placebo-controlled trial; ↑ Increases; ↓ Decreases