First Line Agents

Gabapentin (Neurontin®)

Pregabalin (Lyrica®)

Lidocaine patch (Lidoderm®)

Imipramine (Torfranil®)

Amitriptyline (Elavil®)

Nortriptyline (Pamelor®)

Desipramine (Norpramin®)

Gabapentin

Neurontin®

Dose: Day 1: 300 mg PO x1, Day 2: 300 mg PO BID, Day 3: 300 mg PO TID,

May titrate to 1800-3600 mg/d

MOA: Structurally related to GABA, modulates the release of excitatory NTs

SE: Somnolence, dizziness, peripheral edema, vasodilation

CI: Hypersensitivity to any component of the formulation

Class: Anticonvulsant

Pregabalin

Lyrica®

Dose: Initial: 150 mg/d in divided doses,

MAX= 300 mg/d

MOA: Inhibits excitatory NT release, exerts antinociceptive & anticonvulsant activity, inhibits voltage gated calcium channels

SE: Peripheral edema, dizziness, somnolence, headache, weight gain, difficulty concentrating

CI: Hypersensitivity to pregabalin or any component of the formulation

Class: Analgesic, Anticonvulsant

Lidocaine patch

Lidoderm®

Dose: Up to 3 patches/application, on 12 hours, off 12 hours

MOA: Blocks both the initiation & conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions

SE: Burning, skin irritation, itching

CI: Hypersensitivity to lidocaine or any component of the formulation

Class: Topical analgesic

Imipramine

Tofranil®

Dose: 0.2-0.4 mg/kg at bedtime

MOA: Increases the synaptic concentration of serotonin and/or NE in the CNS by inhibiting their uptake

SE: Arrhythmias, orthostatic hypotension, HTN, fatigue, seizures, weight gain

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorder & other psychiatric disorders

CI: Hypersensitivity to imipramine or any of the formulation, concurrent use of MAOI (within 14 days), use in a patient during the acute recovery phase of MI, pregnancy

Class: TCA

Amitriptyline

Elavil®

Dose: 0.1 mg/kg at bedtime. May advance as tolerated over 2-3 weeks to 0.5-2 mg/kg at bedtime

MOA: Increases the synaptic concentration of serotonin and/or NE in the CNS by inhibiting their uptake

SE: Arrhythmias, orthostatic hypotension, HTN, fatigue, seizures, weight gain, flushing

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorders & other psychiatric disorders

CI: Hypersensitivity to amitriptyline or any component of the formulation, concurrent use of MAOI (within 14 days), use in a patient during the acute recovery phase of MI

Class: TCA

Nortriptyline

Pamelor®

Dose: Initial: 10-25 mg at bedtime, may increase by 25 mg/d weekly, if tolerated, Maintenance: 75 mg as a single bedtime dose or divided doses

MOA: Increases the synaptic concentration of serotonin and/or NE in the CNS by inhibiting their uptake. Additional receptor effects have been found including desensitization of adenyl cyclase, down regulation of β-adrenergic receptors, & down regulation of serotonin receptors

SE: Arrhythmias, orthostatic hypotension, HTN, fatigue, seizures, weight gain, flushing

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorder & other psychiatric disorders

CI: Hypersensitivity to nortriptyline or any component of the formulation, concurrent use of MAOI (within 14 days), use in a patient during the acute recovery phase of MI

Class: TCA

Desipramine

Norpramin®

Dose: 100-200 mg/d PO (single or divided doses)

MOA: Increases the synaptic concentration of serotonin and/or NE in the CNS by inhibiting their uptake. Additional receptor effects have been found including desensitization of adenyl cyclase, down regulation of β-adrenergic receptors, & down regulation of serotonin receptors

SE: Arrhythmias, orthostatic hypotension, HTN, fatigue, seizures, weight gain, flushing

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorder & other psychiatric disorders

CI: Hypersensitivity to desipramine or any component of the formulation, concurrent use of MAOI (within 14 days), use in a patient during the acute recovery phase of MI

Class: TCA

Second Line Agents

Carbamazepine (Tegretol®)

Phenytoin (Dilantin®)

Clonazepam (Klonopin®)

Lamotrigine (Lamictal®)

Oxcarbazepine (Trileptal®)

Burpropion (Wellbutrin®)

Citalopram (Celexa®)

Paroxetine (Paxil®)

Venlafaxine (Effexor®)

Duloxetine (Cymbalta®)

Carbamazepine

Tegretol®

Dose: 200 mg/d in 2 divided doses

MOA: Limits influx of sodium ions across cell membrane

SE: Arrhythmias, edema, abdominal pain, dizziness, Stevens-Johnson syndrome

BBW: Potentially fatal blood cell abnormalities have been reported

CI: Hypersensitivity to CBZ, TCAs, or any component of the formulation, bone marrow depression, with or within 14 days of MAOI

Class: Anticonvulsant

Phenytoin

Dilantin®

Dose: Initial: 600 mg x1, Maintenance: 300 mg/d

MOA: Stabalizes neuronal membranes and decreases seizure activity by increasing efflux or decreasing influx of sodium ions across cell membranes in the motor cortex during generation of nerve impulses

SE: Nystagmus, ataxia, rash, gingival hyperplasia with long term use

CI: Hypersensitivity to phenytoin, other hydantoins, or any component of the formulation, pregnancy

Class: Anticonvulsant

Clonazepam

Klonopin®

Dose: Initial: 0.25 mg BID, Maintenance: 1 mg/day, MAX= 4 mg/d

MOA: Exact mechanism is unknown but believed to be related to its ability to enhance the activity of GABA

SE: Edema, dizziness, emotional liability, fatigue, nervoisness

CI: Hypersensitivity to clonazepam or any component of the formulation (cross-sensitivity with other Benzos may exist), significant liver disease, narrow-angle glaucoma, pregnancy

Class: Benzodiazepine

Lamotrigine

Lamictal®

Dose: Initial: 25 mg/d, may titrate to 400 mg/d (over 10 weeks)

MOA: A triazine derivative which inhibits release of glutamate (an excitatory amino acid) & inhibits voltage-sensitive sodium channels which stabalizes neuronal membranes

SE: Dizziness, diplopia, ataxia, blurred vision, rhinitis

CI: Hypersensitivity to lamotrigine or any component of the formulation

Class: Anticonvulsant

Oxcarbazepine

Trileptal®

Dose: Initial: 150 mg/d (double weekly x 4 weeks), Maintenance: 600 mg BID, MAX= 1200 mg/d

MOA: Blocks voltage-sensitive sodium channels, stabilizing hyperexcited neuronal membranes inhibiting repetitive firing, and decreasing the propagation of synaptic impulses

SE: Dizziness, diplopia, headache, nausea, vomiting, somnolence, ataxia

CI: Hypersensitivity to oxcarbazepine or any component of the formulation

Class: Anticonvulsant

Bupropion

Wellbutrin®

Dose: 150-300 mg/d

MOA: A relatively weak inhibitor of the neuronal uptake of NE & dopamine & does not inhibit MAO or the reuptake of serotonin

SE: Headache, dry mouth, nausea, weight loss, insomnia

CI: Hypersensitivity to bupropion or any component of the formulation, seizure disorder, anorexia/bulimia, use of MAOI within 14 days

Class: Antidepressant

Citalopram

Celexa®

Dose: 20-30 mg/d, MAX= 60 mg/d

MOA: Selectively inhibits serotinin reuptake in the presynaptic neurons & has minimal effects on NE & dopamine

SE: Dry mouth, nausea, somnolence, sweating, fatigue, tremor

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorder & other psychiatric disorders

CI: Hypersensitivity to citalopram or any component of the formulation, concominant use with MAOI or within 2 weeks of discontinuing MAOIs

Class: SSRI

Paroxetine

Paxil®

Dose: 40 mg/d

MOA: Selective serotonin reuptake inhibitor

SE: Nausea, somnolence, insomnia, dry mouth, headache, constipation, diarrhea, dizziness, ejaculation disorder, sweating

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorder & other psychiatric disorders

CI: Hyersensitivity to paroxetine or any component of the formulation, use with or within 14 days of an MAOI

Class: SSRI

Venlafaxine

Effexor®

Dose: 75-225 mg/d

MOA: Potent inhibitor of neuronal serotonin & NE reuptake & weak inhibitor of dopamine reuptake

SE: Headache, nausea, insomnia, dizziness, ejaculation disorder, somnolence, dry mouth, sweating

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorder & other psychiatric disorders

CI: Hypersensitivity to venlafaxine or any component of the formulation, use of MAOI with or within 14 days, initiation of MAOI within 7 days of discontinuing venlafaxine

Class: SNRI

Duloxetine

Cymbalta®

Dose: 60 mg 1-2 times/d

MOA: Potent inhibitor of neuronal serotonin & NE reuptake & a weak inhibitor of dopamine reuptake, no significant activity for muscarinic cholinergic, H1-histaminergic or α2-adrenergic receptors, no MAOI activity

SE: Fatigue, dizziness, headache, insomnia, nausea, xerostomia, diarrhea, constipation, decreased appetite

BBW: Antidepressants increase the risk of suicidal thinking & behavior in children, adolescents, & young adults with major depressive disorder & other psychiatric disorders

CI: Use with or within 14 days of MAOI, uncontrolled narrow-angle glaucoma

Class: SNRI

Other Agents

Amantadine (Symmetrel®)

Capsacin (Capzacin® P, Zostrix®)

Clonidine (Catapres-TTS®)

Oxycondone (Oxycontin®)

Mexelitine (Mexitil®)

Tramadol (Ultram®)

Amantadine

Symmetrel®

Dose: 200 mg IV

MOA: N-methyl-D-aspartate (NMDA) receptor antagonist that may block pain transmission in the dorsal horn

SE: Orthostatic hypotension, peripheral edema, agitation, anxiety, confusion, delirium, depression, dizziness, constipation, nausea, xerostomia

CI: Hypersensitivity to amanradine or any component of the formulation

Class: Antiparkinson's agent, Dopamine agonist, Antiviral

Capsaicin

Capzacin® P, Zostrix®

Dose: Apply to affected area 3-4 times daily for 3-4 weeks, MAX= 4 applications/d

MOA: Affects the synthesis, storage, transport, and release of substance P

SE: Transient increased pain at application site (stops with continuous use), application site redness, itching

CI: Hypersensitivity to capsaicin or any component of the formulation

Class: Topical analgesic

Clonidine

Catapres-TTS®

Dose: 0.1-0.3 mg/d

MOA: Stimulates α2-adrenorceptors in the brain stem, thus activating an inhibitory neuron, resulting in reduced sympathetic outflow from the CNS

SE: Drowsiness, dizziness, transient localized skin reactions, dry mouth

CI: Hypersensitivity to clonidine or any component of the formulation

Class: α2 adrenergic agonist

Oxycodone

Oxycontin®

Dose: 10-30 mg every 12 hours

MOA: Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of & response to pain, produces generalized CNS depression

SE: Somnolence, dizziness, pruritis, nausea, constipation, vomiting, respiratory depression

CI: Hypersensitivity to oxycodone or any component of the formulation, significant repsiratory depression, acute or severe bronchial asthma

Class: Opioid analgesic

Mexelitine

Mexitil®

Dose: 600 mg/d

MOA: Structurally related to lidocaine, which inhibits inward sodium current

SE: Dizziness, nervousness, nausea, vomiting, unsteady gait

CI: Hypersensitivity to mexelitine or any component of the formulation, cardiogenic shock, 2nd or 3rd degree AV block (except in patients with functioning artificial pacemaker)

Class: Class Ib antiarrhythmic

Tramadol

Ultram®

Dose: 210 mg/d

MOA: Binds to Mu receptors in the CNS causing inhibiton of ascending pain pathways, altering the perception of & response to pain, also inhibits the reuptake of NE & serotonin which also modifies the ascending pain pathway

SE: Flushing, dizziness, headache, insomnia, fatigue, nausea, vomiting, constipation

CI: Hypersensitivity to tramadol, opioids, or any component of the formulation, opioid dependent patients, acute intoxication with alcohol, hypnotics, or psychotropic drugs

Class: Opioid analgesic