Structure |
Amino amide anesthestic |
Gamma-aminobutyric acid (GABA) analog |
Dibenzocycloheptene tricyclic antidepressant (TCA) |
Mu opioid receptor agonist |
Gamma-aminobutyric acid (GABA) analog |
Mu opioid agonist and serotonin and norepinephrine reuptake inhibitor |
Kinetics |
Very little systemic absorption |
Renal elimination; prolonged half-life with renal impairment |
Hepatic metabolism; higher levels of active metabolites in the elderly |
Hepatic metabolism and renal elimination |
Renal elimination; prolonged half-life with renal impairment |
Hepatic metabolism and renal elimination |
Standard Dosing |
Up to 3 patches applied over the affected area for 12 hours a day |
Start at 100-300 mg at night; increase by 100-300 mg a day every 1-7 days as tolerated in tid dosing; maximum dose 3600 mg/day |
Start 10 mg at night; increase by 10 mg every 4-7 days by the same amount until reduction in pain; maximum dose 75-150 mg day |
In morphine equivalents start 2.5-15 mg every four hours; after 1-2 weeks, convert total daily dosage to long-acting opioid analgesic and continue short-acting medication as needed |
150 mg/day given in 2 or 3 divided doses; may increase to 300 mg/day, given in 2 or 3 divided doses, within 1 week; maximum dosage 600 mg/day |
Start 50 once daily; increase by 50 mg daily in divided doses every 3-7 days as tolerated; maximum dose 400 mg daily; in patients over 75 years of age, 300 mg daily in divided doses |
Benefit: % Significant Improvement* |
≥50% reduction in pain scores: 31% lidocaine patch vs. 8% placebo patch |
Moderate or much pain improvement: 41-43% gabapentin vs. 12-23% placebo |
Moderate to good pain relief: 44-67% TCAs vs. 5-19% placebo or control drug |
Masked preference: 67% oxycodone vs. 11% placebo |
≥50% reduction in pain scores: 50% pregabalin vs. 20% placebo |
≥50% reduction in pain scores 77% tramadol vs. 56% placebo |
Adverse Events |
Skin redness or rash |
Somnolence, dizziness, ataxia, peripheral edema |
Arrhythmia, cardiac conduction block, orthostatic hypotension, urinary retention, constipation, cognitive impairment |
Constipation, sedation, nausea/vomiting, respiratory depression, nervous system symptoms, pruritis |
Somnolence, dizziness, ataxia, peripheral edema |
Constipation, sedation, nausea/vomiting, respiratory depression, nervous system symptoms, seizures |
Main Drug-Drug Interactions |
Class I antiarrythmics |
Opioids |
Antipsychotics, anticholinergics, selective serotonin reuptake inhibitors (SSRI), sedative-hypnotics, antiarrhythmics, MAO inhibitors |
Anticholinergics, sedative-hypnotics, anxiolytics, CYP2D6 inhibitors, TCAs, muscle relaxants |
Opioids |
Anticholinergics, sedative-hypnotics, anxiolytics, CYP2D6 inhibitors, SSRIs, TCAs, muscle relaxants |
Main Drug-Disease Interactions |
None |
Dementia, ataxia, falls |
Myocardial infarction, QT prolongation, AV block, bundle branch block, ileus, prostatic hypertrophy, seizure disorder, glaucoma, dementia |
Ileus, chronic obstructive pulmonary disease, dementia, prostatic hypertrophy |
Dementia, ataxia, falls |
Ileus, chronic obstructive pulmonary disease, dementia, prostatic hypertrophy, seizure disorder |
How Supplied |
10 by 14 cm. lidocaine patch contains 5% lidocaine base on polyester backing |
100 mg, 300 mg, 400 mg capsules; 600 mg, 800 mg tablets |
10 mg, 25 mg, 50 mg, 75 mg capsules; 10 mg/5ml solution |
Multiple drugs and dosage forms |
25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, 300 mg capsules |
50 mg tablet |