Alvimopan
Drug Info:
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Alvimopan
Brand names: Entereg™
- Espa�ol:
- Alvimopan, Cápsula oral
Alvimopan Oral capsule
What is this medicine?
ALVIMOPAN (AL vi MOE pan) is used to help the gut function after having gut surgery.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•heart disease
•kidney disease
•liver disease
•taking pain medications (e.g., codeine, morphine)
•undergoing surgery for stomach or intestinal blockage
•an unusual or allergic reaction to alvimopan, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. It will only be given to you by a health care professional while you are in the hospital.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•amiodarone
•bepridil
•cyclosporine
•diltiazem
•itraconazole
•narcotic medicines for pain
•quinidine
•quinine
•spironolactone
•verapamil
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Your condition will be monitored carefully while you are receiving this medicine.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing difficulties
•dizziness
•unusually weak or tired
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•back pain
•constipation
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
This does not apply.
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Wikipedia on Answers.com:
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Alvimopan
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| Systematic (IUPAC) name | |
| 2-([(2S)-2-([(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl) -3-phenylpropanoyl]amino)acetic acid | |
| Clinical data | |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a608051 |
| Licence data | US FDA:link |
| Pregnancy cat. | ? |
| Legal status | ? |
| Routes | Oral |
| Identifiers | |
| CAS number | 156053-89-3  |
| ATC code | A06AH02 |
| PubChem | CID 5488548 |
| DrugBank | DB06274 |
| ChemSpider | 4589864  |
| UNII | Q153V49P3Z |
| ChEMBL | CHEMBL270190 |
| Synonyms | Alvimopan, Entereg |
| Chemical data | |
| Formula | C25H32N2O4 |
| Mol. mass | 424.53 g/mol |
| SMILES | eMolecules & PubChem |
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 (what is this?) (verify) |
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Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid antagonist. With limited ability to cross the blood–brain barrier, many of the undesirable side-effects of the opioid agonists such as constipation are minimized without affecting analgesia or precipitating withdrawals.[1][2] The Food and Drug Administration reviewed the safety and efficacy data for alvimopan and approved its use in May 2008.[3]
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Contents
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Indication
Alvimopan is indicated in patients 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.[4]
Mechanism of action
Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract. Unlike methylnaltrexone (another peripherally acting mu-receptor antagonist) that bears a quaternary amine, alvimopan owes its selectivity for peripheral receptors to its kinetics. Alvimopan binds to peripheral mu-receptors with a Ki of 0.2 ng/mL and dissociates slower than most other ligands.[4]
Pharmacokinetics
Absorption
Peak plasma concentration (Cmax) of alvimopan is reached approximately 2 hours after oral dosing, while the Cmax for metabolite occurs 36 hours after an oral dose. Alvimopan's high affinity for the peripheral mu-receptor results in an absolute bioavailability less than 7%. [4]
Distribution
80% to 90% of systemically available alvimopan is bound to plasma protein. At steady state, the volume of distribution is approximately 30 liters.[4]
Metabolism
Alvimopan undergoes no significant hepatic metabolism, but is metabolized by intestinal flora. Gut metabolism produces an active metabolite with no clinically significant contribution to drug effect.[4]
Elimination
Alvimopan undergoes 35% renal excretion and greater than 50% biliary excretion. Drug metabolized by intestinal flora is excreted in the feces. Alvimopan's half-life of elimination is 10 to 17 hours, while that of the gut metabolite is 10 to 18 hours.[4]
Dosing and administration
Alvimopan is only approved for short term use of no more than 15 doses. It is available on an inpatient basis at institutions approved by and registered with the Entereg Access Support and Education (E.A.S.E.) program. The drug is a 12 mg blue hard gelatin capsule. The recommended adult dose is to administer 12 mg 30 minutes to 5 hours preoperatively and 12 mg twice daily for seven days postoperatively. A patient should receive no more than 15 doses.[4]
Adverse effects
The most common side effects associated with alvimopan are:[1]
| Adverse Effect | Frequency (%) with placebo | Frequency (%) with alvimpoan |
|---|---|---|
| Dyspepsia | 4.6 | 7.0 |
| Hypokalemia | 8.5 | 9.5 |
| Back Pain | 1.7 | 3.3 |
| Delayed Micturition | 2.1 | 3.2 |
Contraindications
Alvimopan is absolutely contraindicated in patients who have taken therapeutic doses of opioids for more than seven consecutive days immediately prior to when alvimopan would be initiated because individuals with recent exposure to opioids are expect to be more sensitive to the effects of mu-opioid receptor antagonists. The peripheral site of action of alvimopan suggests that such a heightened sensitivity would precipitate gastrointestinal effects beyond dyspepsia.[4]
Warnings
Myocardial infarction
During clinical trials, a 12 month study of alvimopan dosed at 0.5 mg twice daily reported observed more myocardial infarction in the treatment group compared to placebo. The majority of these events occurred between months one and four of treatment. No causal relationship between alvimopan and myocardial infarction was ever established, and this effect has not been reproduced in subsequent studies.
Severe hepatic impairment
During clinical trials, one patient with severe hepatic impairment appreciated a 10-fold increase in Cmax compared to healthy volunteers. Two other patients with a similar Child-Pugh score (class C) did not experience this same phenomenon.
End-stage renal disease
Alvimopan has not been studied in patients with end-stage renal disease.
Bowel obstruction
It is not recommended to use alvimopan in surgical candidates for correction of a complete bowel obstruction.
Drug interactions
Alvimopan is not substrate for the cytochrome P450 enzyme system. Therefore, no interactions are expected with hepatically metabolized drugs. Alvimopan is substrate for p-glycoprotein. Expect interactions with known p-glycoprotein inhibitors such as amiodarone, depridil, diltiazem, cyclosporine, itraconazole, quinine, quinidine, spironolactone, and verapamil.[4]
References
- ^ a b Neary P, Delaney P (2005). "Alvimopan". Expert Opin Investig Drugs 14 (4): 479–88. doi:10.1517/13543784.14.4.479. PMID 15882122.
- ^ Schmidt WK (2001). "Alvimopan* (ADL 8-2698) is a novel peripheral opioid antagonist". Am J Surg 182 (5A Supp): 27S–38S. doi:10.1016/S0002-9610(01)00784-X. PMID 11755894.
- ^ FDA press release - FDA Approves Entereg to Help Restore Bowel Function Following Surgery
- ^ a b c d e f g h i Alvimopan Product Label as approved by the FDA on May 20, 2008.
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