Table 2.
Compound class | Drug | Route | Dose | Experimental pain effect | Neuropathic pain effect | Postoperative pain effect | Reference(s) |
---|---|---|---|---|---|---|---|
Opioid | Alfentanil | IV | 75 ng/mL | Positive | Positive as a class | Positive as a class | [50, 51, 61–64] |
Remifentanil | IV | 0.1 μg/kg/min | Positive | ||||
Hydromorphone | PO | 8 mg | Positive | ||||
Morphine | PO | 30 mg | Positive | ||||
Morphine | IV | 10 mg | Positive | ||||
Alfentanil | IV | 50 ng/mL | Negative | ||||
Alfentanil | IV | 200 ng/mL | Positive | ||||
NMDA antagonist | Ketamine | IV | 150 ng/mL | Positive | Disappointing as a class | Positive only in combination with an opioid | [49, 50, 52, 61] |
Dextromethorphan | PO | 30 mg | Negative | ||||
Ketamine | IV | 0.1 mg/kg then 7 μg/kg/min | Positive | ||||
Magnesium | IV | 0.2 mmol/kg then 0.2 mmol/kg/min for 90 min | Negative | ||||
Alpha 2 agonist | Clonidine | Intrathecal | 150 μg | Positive | Positive | Positive only in combination with an opioid | [65] |
Clonidine | IV | 150 μg | Negative | ||||
Alpha 2 delta ligand | Gabapentin | PO | 1,200 mg | Positive | Positive as a class | Positive only in combination with an opioid | [49–52, 66–69] |
Gabapentin | PO | 2,400 mg/day | Positive | ||||
Gabapentin | PO | 1,800 mg/day | Negative | ||||
Pregabalin | PO | 300 mg | Positive | ||||
Antihistamine | Diphenhydramine | PO | 50 mg | Negative | Negative | Negative | [49] |
Diphenhydramine | IV | 25 mg | Negative | [61, 65] | |||
Tricyclic antidepressant | Desipramine | PO | 225 mg/day | Negative | Positive | Negative | [65–67] |
Amitriptyline | IM | 25 mg | Negative | ||||
GABA-A agonist | Midazolam | IM | 4 mg | Negative | Negative as a class | Negative as a class | [65] |
Na-channel block | Lidocaine | IV | 3 μg/mL | Negative | Disappointing as a class | Disappointing as a class | [65] |
Lidocaine | IV | 2 mg/kg then 3 μg/kg/h | Positive (but limited) | [68] | |||
Lidocaine | IV | 5 mg/kg over 50 min | Positive | [69] | |||
Mexiletine | PO | 859 mg/day | Positive (but limited) | [70] | |||
Lamotrigine | PO | 300 mg | Negative | [53] | |||
Lamotrigine | PO | 400 mg | Negative | [63] | |||
Adenosine agonist | Adenosine | IV | 65 μg/kg/min for 85 min | Negative | Negative | Positive (spinal) | [72] |
Cannabinoids | Cannabis | Inhaled | 3 doses (2%, 4%, 6%) | Positive 4%, negative 2 % and 6% | Positive 6%, negative 2 and 4% | Modest benefit | [55] |
Cannabis | Inhaled | 4% | Positive | Positive (low dose) | [73] | ||
THC/Cannabidiol | Inhaled | 3.56% THC | Equivocal | Negative (high dose) (sativex) | |||
TRPV1 antagonist | REN-1654 | PO | Oral 100 mg | Negative | Negative | N/aa | [74] |
AMPA antagonist | NGX426 | PO | 10 mg/cc | Positive | N/ab | N/ab | [75] |
Magnesium | Magnesium | IV | 0.2 mmol/kg−1 | Negative | N/ab | N/ab | [76] |
AMPA α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid, GABA γ-aminobutyric acid, IM intramuscularly, IV intravenously, NMDA N-methyl-d-aspartic acid, PO orally, THC tetrahydrocannabinol, TRPV1 transient receptor potential cation channel, subfamily V, member 1
a The patients in this study had a neuropathic component to their pain, but not post-surgical
b This study was done in healthy subjects without neuropathic or postoperative pain