TABLE 8.
Neurotransmitter profile
|
Most common side effects (%)
|
||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
Drug | Common trade name | Therapeutic range for pain (mg/24 h) | Half-life (h) | NA | 5-HT | Sedation | Orthostatic hypotension | Weight gain | Dry mouth | Constipation | GI distress, nausea, diarrhea |
Tricyclics | |||||||||||
Amitriptyline | Elavil† | 10–150* | 10–46 | +++ | +++ | >30 | >10 | >30 | >30 | >10 | >2 |
Doxepin | Sinequan‡ | 10–150* | 8–36 | +++ | ++ | >30 | >10 | >10 | >30 | >10 | <2 |
Trimipramine | Surmontil§ | 10–150* | 7–30 | ++ | + | >30 | >10 | >10 | >10 | >10 | <2 |
Imipramine | Tofranil¶ | 10–150* | 4–34 | +++ | +++ | >10 | >30 | >10 | >30 | >10 | >10 |
Clomipramine | Anafranil** | 10–150* | 17–37 | +++ | ++++ | >2 | >10 | >10 | >30 | >10 | >10 |
Desipramine | Norpramin§ | 10–150* | 12–76 | +++++ | ++ | >2 | >2 | >2 | >10 | >2 | >2 |
Nortriptyline | Aventyl†† | 10–100* | 13–88 | ++++ | ++ | >2 | >2 | >2 | >10 | >10 | <2 |
Serotonin/noradrenaline reuptake inhibitors | |||||||||||
Venlafaxine | Effexor‡‡ | 37.5–225 | 3–7 (parent)
9–13 (metabolite) |
++ | ++++ | >10 | >10 | <2 | >10 | >10 | >30 |
Duloxetine | Cymbalta§§ | 60–120 | 10 | ++++ | +++++ | >10 | <10 | <2 | >10 | >10 | >10 |
The therapeutic range for depression is up to 200 mg/24 h for nortriptyline and to 300 mg/24 h for the remaining tricyclic antidepressants; generally, these doses are not required for an analgesic effect and the usual dose will consist of 75 mg/24 h or less;
1560678 Ontario Inc, Canada;
ERFA Canada Inc;
Aventis Pharma Inc, Canada;
Novartis Pharmaceuticals, Canada;
Oryx Pharmaceuticals Inc, Canada;
Pharmel Inc, Canada;
Wyeth Canada;
Lilly, USA. 5-HT 5-Hydroxytryptamine; GI Gastrointestinal; NA Noradrenaline. Adapted from reference 286