Depression of ventilation | Nausea and vomiting |
Sedation | Itching |
Dysphoria | Constipation |
Hypotension, bradycardia | Delayed gastric emptying |
Increased skeletal muscle tone | Urinary retention |
Suppression of cough | Biliary spasm |
Suppression of immune function | Addiction |
Characteristic | Methylnaltrexone | Alvimopan |
---|---|---|
Approved indication | Opioid-induced constipation in patients with advanced illness receiving palliative care, when response to laxatives has not been sufficient | Facilitation of gut function after bowel resection and primary anastomosis |
Dosage | 8 mg every other day (body weight, 38-62 kg) | 12 mg twice daily, starting preoperatively (limit, 15 doses total) |
12 mg every other day (body weight, 63-114 kg) | ||
Administration | Subcutaneous | Oral |
Adverse effects | Flatulence | Anemia |
Abdominal cramping | Dyspepsia | |
Nausea | Hypokalemia | |
Vomiting | Back pain Urinary retention | |
Contraindications | Mechanical bowel obstruction | Opiate use >1 wk Restricted to hospitals |
Wholesale cost/dose | $38.54 | $61.88 |
GASTROINTESTINAL EFFECTS OF OPIOIDS
PHARMACOTHERAPY FOR OPIOID GASTROINTESTINAL EFFECTS
Methylnaltrexone



Alvimopan


- Wolff BG
- Michelassi F
- Gerkin TM
- et al.
- Viscusi ER
- Goldstein S
- Witkowski T
- et al.
- Wolff BG
- Michelassi F
- Gerkin TM
- et al.
- Viscusi ER
- Goldstein S
- Witkowski T
- et al.
Time to GI-2 | ||||||||
---|---|---|---|---|---|---|---|---|
Study No. | Treatment | No. of patients | 50th percentile (d) | Change from placebo (d) | 75th percentile (d) | Change from placebo (d) | HR (95% CI) | P value |
302 60 | Placebo | 99 | 4.8 | −0.7 | 5.9 | −0.8 | 1.40 (1.04-1.89) | .029 |
Alvimopan | 98 | 4.1 | 5.1 | |||||
308 63
Alvimopan, a peripherally acting μ-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study [published correction appears in Surg Endosc. 2006;20 (3): 537]. Surg Endosc. 2006; 20 (Epub 2005 Dec 7.): 64-70 | Placebo | 142 | 4.9 | −0.5 | 6.3 | −0.9 | 1.37 (1.06-1.76) | .017 |
Alvimopan | 139 | 4.4 | 5.4 | |||||
313 59
Alvimopan Postoperative Ileus Study Group. Alvimopan, a novel, peripherally acting μ opioid antagonist: results of a multicenter, randomized, double-blind, placebo-controlled, phase III trial of major abdominal surgery and postoperative ileus. Ann Surg. 2004; 240: 728-734 | Placebo | 142 | 4.9 | −0.9 | 6.3 | −1.2 | 1.63 (1.26-2.10) | <.001 |
Alvimopan | 160 | 4.0 | 5.1 | |||||
001 62 | Placebo | 229 | 4.0 | −0.1 | 5.7 | −0.8 | 1.30 (1.07-1.58) | .008 |
Alvimopan | 238 | 3.9 | 4.9 | |||||
314 61 | Placebo | 312 | 4.0 | −0.7 | 5.5 | −0.9 | 1.53 (1.29-1.82) | <.001 |
Alvimopan | 317 | 3.3 | 4.6 |
- Wolff BG
- Michelassi F
- Gerkin TM
- et al.
- Viscusi ER
- Goldstein S
- Witkowski T
- et al.
Study No. | Treatment | No. of patients | Time to discharge 75th percentile (d) | Change from placebo (d) | HR (95% CI) | P value |
---|---|---|---|---|---|---|
302 60 | Placebo | 99 | 4.7 | 1.52 (1.11-2.09) | ||
Alvimopan | 98 | 4.1 | −0.6 | .010 | ||
308 63
Alvimopan, a peripherally acting μ-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study [published correction appears in Surg Endosc. 2006;20 (3): 537]. Surg Endosc. 2006; 20 (Epub 2005 Dec 7.): 64-70 | Placebo | 142 | 4.9 | 1.40 (1.09-1.78) | ||
Alvimopan | 139 | 4.6 | −0.3 | .008 | ||
313 59
Alvimopan Postoperative Ileus Study Group. Alvimopan, a novel, peripherally acting μ opioid antagonist: results of a multicenter, randomized, double-blind, placebo-controlled, phase III trial of major abdominal surgery and postoperative ileus. Ann Surg. 2004; 240: 728-734 | Placebo | 142 | 4.7 | 1.54 (1.20-1.96) | ||
Alvimopan | 160 | 4.0 | −0.7 | <.001 | ||
001 62 | Placebo | 229 | 5.7 | 1.11 (0.92-1.35) | ||
Alvimopan | 238 | 5.7 | 0.0 | .287 | ||
314 61 | Placebo | 312 | 3.8 | 1.38 (1.17-1.63) | ||
Alvimopan | 317 | 3.4 | −0.4 | <.001 |
- Wolff BG
- Michelassi F
- Gerkin TM
- et al.
- Viscusi ER
- Goldstein S
- Witkowski T
- et al.
- Wolff BG
- Michelassi F
- Gerkin TM
- et al.
- Viscusi ER
- Goldstein S
- Witkowski T
- et al.
- Webster L
- Jansen JP
- Peppin J
- et al.
- Webster L
- Jansen JP
- Peppin J
- et al.
EFFICACY OF PAMORAS IN ATTENUATING OTHER OPIOID-INDUCED ADVERSE EFFECTS
Delayed Gastric Emptying
Nausea and Vomiting
Urinary Retention

The Cough Reflex
Pruritus
CELLULAR EFFECTS
Human Immunodeficiency Virus
Angiogenesis

Vascular Permeability
Bacterial Opioid Receptors
THE NEW DRUGS: FINAL THOUGHTS
CONCLUSION
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Footnotes
Dr Moss has patent interests in methylnaltrexone and serves as a consultant to Progenics Pharmaceuticals, which has the license for methylnaltrexone's development. Wyeth Pharmaceuticals entered into an agreement with Progenics in December 2005 to develop and commercialize methylnaltrexone for the treatment of patients with opioid-induced adverse effects. Dr Rosow has received research support from Progenics Pharmaceuticals.
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