Table 1.
Pharmacologic treatment | Type | Class | Molecular mechanism(s) | APS 200522 | EULAR 200723 | Approval status |
---|---|---|---|---|---|---|
Standard treatments | ||||||
NSAIDs (eg, aspirin, naproxen, ibuprofen) | N/A | Selective or nonselective | COXb-1,2 inhibition; COXb-2 inhibition | NE | NE | Not approved |
Opioids (eg, morphine, codeine, fentanyl, nalbuphine) | Scheduled or nonscheduled | Agonist, partial agonist, agonist-antagonist, or antagonist | Mu-, kappa-, delta-opioid receptor binding | NE | NE | Not approved |
Tramadol | Nonscheduled opioid analgesic; adjuvant analgesic (antidepressant) | Agonist; SNRI | Mu-opioid receptor binding; norepinephrine/serotonin reuptake inhibition | ME | SE | Not approved |
Amitriptyline | Adjuvant analgesic (antidepressant) | TCA | Na+ ion channel inhibition; NMDA receptor blockade (non-neuroprotective) | SE | SE | Not approved |
Fluoxetine | Adjuvant analgesic (antidepressant) | SSRI | Serotonin reuptake inhibition | ME | SE | Not approved |
Gabapentin | Adjuvant analgesic (anticonvulsant) | N/A | VGCC alpha-2-delta subunit binding | N/A | N/A | Not approved |
S-adenosylmethionine | Adjuvant analgesic (antidepressant) | N/A | Nervous system methylation | WE | N/A | Not approved |
Cyclobenzaprine | Skeletal muscle relaxant | N/A | 5-HT2 receptor antagonist | SE | N/A | Not approved |
Growth hormone | N/A | Hormone | Numerous | WE | N/A | Not approved |
New treatments | ||||||
Pregabalin | Adjuvant analgesic (anticonvulsant) | N/A | VGCC alpha-2-delta subunit binding | ME | SE | FDA-approved (2007) |
Duloxetine | Adjuvant analgesic (antidepressant) | SNRI | Serotonin/norepinephrine reuptake inhibition | ME | SE | FDA-approved (2008) |
Milnacipran | Adjuvant analgesic (antidepressant) | SNRI | Serotonin/norepinephrine reuptake inhibition | ME | SE | FDA-approved (2009) |
Emerging treatments | ||||||
Pramipexole | Adjuvant analgesic | Agonist | Selective non-ergoline D2, D3, and D4 dopamine receptor binding | N/A | SE | Not approved |
Dextromethorphan | Adjuvant analgesic | Antagonist | NMDAR | N/A | N/A | Not approved |
Ketamine | Adjuvant analgesic | Antagonist | NMDAR | N/A | N/A | Not approved |
Sodium oxybate | Adjuvant analgesic | Central nervous system depressant | GABAB and GHB receptors (proposed) | N/A | N/A | Not approved |
Low-dose naltrexone | Opiate analgesia enhancer | Opioid antagonist | Disruption of mu-opioid receptor Gs coupling via filamin A binding | N/A | N/A | Not approved |
Delta-9-THC | Adjuvant analgesic | Psychoactive cannabinoid | Numerous | N/A | N/A | Not approved |
Abbreviations: APS, American Pain Society; COX, cyclooxygenase; EULAR, European League Against Rheumatism; FDA, Food and Drug Administration; FM, fibromyalgia; ME, modest efficacy; NA, not applicable; NE, no evidence of efficacy; NMDAR, N-methyl D-aspartate receptor; NSAID, nonsteroidal anti-inflammatory drug; SE, strong efficacy; SNRI, serotonin/norepinephrine reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor; TCA, tricyclic antidepressant; VGCC, voltage-gated calcium ion channel; WE, weak efficacy.