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alvimopan

Structure via PubChem · Public domain (PubChem)

EntityQ4738021· pop 14· linked from 739 articles

Also known as ADL 8-2698, Entereg®, alvimopan anhydrous, Alvimopan anhydrous, Anhydrous alvimopan

Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid receptor antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous system, the clinically undesirable effects of centrally acting opioid antagonists (like reversal of opioid-mediated analgesia) are avoided without affecting the intended blockade of μ-opioid receptors in the gastrointestinal tract. It is currently only Food and Drug Administration approved for the treatment of postoperative ileus which it received in May 2008.

Chemical data

Formula
C25H32N2O4
Molecular weight
424.5 g/mol
IUPAC name
2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid
SMILES
C[C@H]1CN(CC[C@@]1(C)C2=CC(=CC=C2)O)C[C@H](CC3=CC=CC=C3)C(=O)NCC(=O)O
InChIKey
UPNUIXSCZBYVBB-JVFUWBCBSA-N
XLogP
1.7
Polar surface area
89.9 Ų
H-bond donors
3
H-bond acceptors
5
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
First approval
2008
Admin. routes
oral
Indications
Constipation, urinary bladder cancer, peritoneum cancer, fallopian tube cancer

via ChEMBL · EBI

Wikidata facts

Mass
424.236
Has use
medication
Show 5 more facts
chemical formula
C₂₅H₃₂N₂O₄
isomeric SMILES
C[C@H]1CN(CC[C@@]1(C)C2=CC(=CC=C2)O)C[C@H](CC3=CC=CC=C3)C(=O)NCC(=O)O
canonical SMILES
CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O
Commons category
Alvimopan
legal status (medicine)
boxed warning
Sources (3)

via Wikidata · CC0

~5 min read

Encyclopedic overview

14 sections
Contents
  • Medical uses
  • Adverse effects
  • Contraindications
  • Interactions
  • Pharmacology
  • Mechanism of action
  • Pharmacokinetics
  • Absorption
  • Distribution
  • Metabolism
  • Elimination
  • Dosing and administration
  • See also
  • References

Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid receptor antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous system, the clinically undesirable effects of centrally acting opioid antagonists (like reversal of opioid-mediated analgesia) are avoided without affecting the intended blockade of μ-opioid receptors in the gastrointestinal tract. It is currently only Food and Drug Administration approved for the treatment of postoperative ileus which it received in May 2008.

== Medical uses == Alvimopan is indicated in people to avoid postoperative ileus following partial large or small bowel resection with primary anastomosis. Alvimopan accelerates the gastrointestinal recovery period as defined by time to first bowel movement or flatus.

Excerpted from Wikipedia’s “alvimopan” article, available under the CC BY-SA 4.0 licence.