Alvimopan
- Atc Codes:A06AH02
- CAS Codes:156053-89-3#170098-38-1
- PHARMGKB ID:156053-89-3#170098-38-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Entereg.
Drug combinations
Chemistry
Alvimopan: C~25~H~32~N~2~O~4.~ Mw: 424.53. 2-[[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl]-3-phenylpropanoyl]amino]acetic acid. CAS-156053-89-3.
Alvimopan dihydrate: C~25~H~36~N~2~O~6~. Mw: 460.56. 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3, 4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid dihydrate. CAS-170098-38-1.
Pharmacologic Category
GI Drugs, Miscellaneous. Laxatives; Peripheral Opioid Receptor Antagonists. (ATC-Code: A06AH02).
Mechanism of action
Following oral administration, alvimopan antagonizes the peripheral effects of opioids on gastrointestinal motility and secretion by competitively binding to gastrointestinal tract μ-opioid receptors. Alvimopan achieves this selective gastrointestinal opioid antagonism without reversing the central analgesic effects of μ-opioid agonists.
Therapeutic use
Accelerates upper and lower gastrointestinal recovery following partial large or small bowel resection surgery with primary anastomosis.
Pregnancy and lactiation implications
There are no adequate and well-controlled studies in pregnant women. Should be used during pregnancy only if clearly needed. It is unknown whether alvimopan is excreted in human milk. Caution should be exercised when administered to nursing women.
Unlabeled use
Contraindications
Contraindicated in patients who have taken therapeutic doses of opioids for more than 7 consecutive days immediately prior to taking alvimopan.
Warnings and precautions
A higher number of myocardial infarctions was reported in patients treated with alvimopan 0.5 mg twice daily compared with placebo in a 12-month study in patients treated with opioids for chronic pain, although a causal relationship has not been established. Patients recently exposed to opioids are expected to be more sensitive to the effects of alvimopan and therefore may experience abdominal pain, nausea and vomiting, and diarrhea. Not recommended in severe hepatic and/or renal impairment. Not recommended in end stage renal disease. For hospital use only.