Persistent Idiopathic Facial Pain Medication
- Author: Stanley J Krolczyk, DO, RPh; Chief Editor: Robert A Egan, MD more...
Medication Summary
The goal of therapy is to manage the pain with anticonvulsants and antidepressants. Narcotics may be appropriate if administered under careful supervision.
Tricyclic antidepressants
Class Summary
A complex group of drugs that has central and peripheral anticholinergic effects and sedative effects. Block the active reuptake of norepinephrine and serotonin.
Amitriptyline (Elavil)
Increases synaptic concentration of serotonin and/or norepinephrine in CNS by inhibiting reuptake by presynaptic neuronal membrane. Useful as analgesic for certain types of chronic and neuropathic pain.
Nortriptyline (Aventyl hydrochloride, Pamelor)
Has demonstrated effectiveness in treatment of chronic pain. Increases synaptic concentration of serotonin and/or norepinephrine in CNS by inhibiting their reuptake by presynaptic neuronal membrane. Additional pharmacodynamic effects, such as desensitization of adenyl cyclase and down-regulation of beta-adrenergic receptors and serotonin receptors, appear to play roles.
Duloxetine (Cymbalta)
FDA approved for diabetic peripheral neuropathic pain. Potent inhibitor of neuronal serotonin and norepinephrine reuptake.
Anticonvulsants
Class Summary
Although useful, their mechanism of action in neuropathic pain is unknown.
Carbamazepine (Tegretol, Carbatrol, Epitol)
Has antineuralgic effects; may depress activity of nucleus ventralis of thalamus or decrease synaptic transmission or summation of temporal stimulation, leading to neural discharge by limiting influx of sodium ions across cell membrane or other unknown mechanisms. Target blood serum concentrations 4-12 mg/L.
Pregabalin (Lyrica)
FDA approved for use in postherpetic neuralgia and painful diabetic peripheral neuropathy. Freynhagen et al describe statistically significant reduction in mean pain score and pain-related sleep interference compared with placebo.
Binds with high affinity to alpha2-delta subunit of voltage-gaited calcium channels, thereby reducing excitatory neurotransmitters. Has half-life of approximately 6 h and is eliminated by renal excretion. Decrease in CrCl results in decreased elimination and, therefore, increase in plasma concentration. Peak plasma concentration occurs at 1 and 1.5 h after oral intake. Bioavailability is 90%. Following repeated dosing, steady-state concentration is achieved at 24-48 h. Can be taken with or without food.
Gabapentin (Neurontin)
Has properties common to other anticonvulsants and antineuralgic effects. Exact mechanism of action not known. Structurally related to GABA but does not interact with GABA receptors. Has efficacy at the alpha2-delta subunit
Phenytoin (Dilantin)
May stabilize neuronal membranes and treat neuralgia by increasing efflux or decreasing influx of sodium ions across cell membranes in motor cortex during generation of nerve impulses. When serum level in or near therapeutic range, adjust dose in 30- to 50-mg increments. Small-dose increments may cause greater than expected increases in serum concentration (ie, Michaelis-Menten drug kinetics). Steady-state serum levels may take up to 3 wk to occur, because half-life is concentration dependent.
Lamotrigine (Lamictal)
Triazine derivative useful in treatment of neuralgia. Inhibits release of glutamate and inhibits voltage-sensitive sodium channels, which stabilizes neuronal membrane. Follow manufacturer's recommendation for dose adjustments.
Topiramate (Topamax)
Precise mechanism unknown, but the following properties may contribute to its efficacy: (1) electrophysiological and biochemical evidence shows blockage of voltage-dependent sodium channels, (2) augments activity of the neurotransmitter GABA at some GABA-A receptor subtypes, (3) antagonizes AMPA/kainate subtype of the glutamate receptor, and (4) inhibits the carbonic anhydrase enzyme, particularly isozymes II and IV.
Valproic acid (Depacon, Depakote, Depakote ER)
Activity may be related to increased brain levels of GABA or enhanced GABA action.
Analgesics
Class Summary
May aid in decreasing severity of pain.
Lidocaine anesthetic (DermaFlex gel, Lidoderm 5% patch)
Several recent studies have advocated topical administration of lidocaine as treatment of postherpetic neuralgia. Lidocaine gel (5%) in placebo-controlled study showed significant relief in 23 patients studied. Lidocaine tape also decreases severity of pain.
Capsaicin topical (Dolorac, Capsin, Zostrix)
Natural chemical derived from plants of Solanaceae family. By depleting and preventing reaccumulation of substance P in peripheral sensory neurons, may render treated areas insensitive to pain. Substance P thought to be chemomediator of pain transmission from periphery to CNS.
Antiemetic, Cannabinoid
Class Summary
Drugs of the cannabinoid class may aid in neuropathic pain.
Dronabinol (Marinol)
Orally active cannabinoid receptor agonist with complex effects on the CNS, including central sympathomimetic activity. Cannabinoid receptors have been discovered in neural tissues. These receptors play a role in mediating the effects of dronabinol and other cannabinoids. It undergoes extensive first-pass hepatic metabolism, by microsomal hydroxylation, yielding both active and inactive metabolites. It has also been shown to be highly plasma protein bound.
Several studies have shown modest effects in treating neuropathic pain and muscle spasticity in individuals with demyelinating disease states.
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