Alvimopan
Alvimopan Uses, Dosage, Side Effects, Food Interaction and all others data.
Alvimopan is a peripherally acting μ opioid antagonist. It is used to avoid postoperative ileus following small or large bowel resection and accelerates the gastrointestinal recovery period.
| Trade Name | Alvimopan |
| Availability | Prescription only |
| Generic | Alvimopan |
| Alvimopan Other Names | Alvimopan |
| Related Drugs | lidocaine topical, Xylocaine Jelly, Entereg, Glydo |
| Weight | 12mg |
| Type | Oral capsule |
| Formula | C25H32N2O4 |
| Weight | Average: 424.5326 Monoisotopic: 424.236207522 |
| Protein binding | 80% to 90% bound in after entering systemic circulation. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Alvimopan is an opioid antagonist used to reduce healing time of the upper and lower gastrointestinal tract following surgical procedures that involve bowel resection with primary anastomosis.
Used to accelerate the time to upper and lower gastrointestinal recovery following partial large or small bowel resection surgery with primary anastomosis. Also investigated for use in the treatment of pain (acute or chronic).
Alvimopan is also used to associated treatment for these conditions: Gastrointestinal Recovery
How Alvimopan works
Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract but, unlike methylnaltrexone which relies upon it ionic charge, alvimopan owes its selectivity for peripheral receptors to its pharmacokinetics. Alvimopan binds to peripheral mu-receptors with a Ki of 0.2 ng/mL.
Food Interaction
- Take with or without food. High-fat meals may reduce the Cmax and AUC by 38% and 21%, respectively; however, the clinical significance of this is unknown.
[Minor] Coadministration with a high-fat meal may decrease the rate and extent of alvimopan absorption.
According to the product labeling, alvimopan peak plasma concentration (Cmax) and systemic exposure (AUC) were decreased by approximately 38% and 21%, respectively, and the time to reach peak plasma concentration (Tmax) was prolonged by approximately 1 hour when taken with a high-fat meal.
The clinical significance is unknown.
In postoperative ileus clinical trials, the preoperative dose of alvimopan was administered in a fasting state, and subsequent doses were given without regard to meals.
Alvimopan Drug Interaction
Major: morphine, oxycodone, acetaminophen / oxycodoneUnknown: acetaminophen, aspirin, alprazolam, pseudoephedrine / triprolidine, amoxicillin / clavulanate, carboplatin, multivitamin with iron, clotrimazole, glucose, dalteparin, potassium chloride, metoprolol, ibuprofen, acetaminophen, pantoprazole, tiotropium, docusate
Alvimopan Disease Interaction
Volume of Distribution
- 30±10 L
Elimination Route
Alvimopan's high affinity for the peripheral mu-receptor leads to slower absorption dependent on dissociation from the receptor and subsequently low oral bioavailability of less than 7%.
Half Life
10 to 17 hours (gut metabolite: 10 to 18 hours)
Clearance
- 402 ± 89 mL/min
Elimination Route
Biliary secretion was considered the primary pathway for alvimopan elimination. Unabsorbed drug and unchanged alvimopan resulting from biliary excretion were then hydrolyzed to its ‘metabolite’ by gut microflora. Feces (via biliary excretion) & urine (35%)
Innovators Monograph
You find simplified version here Alvimopan
