BUY CODEINE IN USA,UK & CANADA ONLINE

Codeine For Sale In USA,UK & Canada Online

Pronunciation: koe-deen
Generic name: codeine sulfate, codeine phosphate
Brand name: generic only
Dosage form: oral tablet (codeine sulfate: 15 mg, 30 mg, 60 mg), oral solution (discontinued)
Drug classes: Antitussives, Opioids

What is Codeine?

Codeine is used to manage mild to moderate pain, where treatment with an opioid is appropriate, and when other pain treatments such as non-opioid pain medicines do not treat your pain well enough or you cannot tolerate them. Codeine is an opioid and considered a strong prescription pain medicine. It also has cough-suppressing (anti-tussive) properties.

Codeine is available as one of 2 salts: codeine or codeine phosphate:

Codeine phosphate is highly water-soluble and used in oral liquids, tablets, and injections
Codeine sulfate is less soluble and primarily used in tablet form
Codeine sulfate tablets are the only single-ingredient codeine still available in the United States.

An opioid pain medicine that can put you at risk for overdose and death. Even if you take your dose correctly as prescribed, you are at risk for opioid addiction, abuse, and misuse that can lead to death.

Codeine is available in combination with several other ingredients, including acetaminophen, guaifenesin, promethazine, and pseudoephedrine. In products containing guaifenesin, promethazine, or pseudoephedrine, codeine is included specifically for its cough-suppressing properties. Buy Codeine In USA Online

Codeine falls under three different Schedule classifications depending on the product and how much codeine it contains.

Single-ingredient codeine sulfate tablets are Schedule II.
Combination products that contain less than 90 mg of codeine per dosage unit (such as acetaminophen with codeine) are Schedule III
Combination cough preparations containing not more than 200 milligrams of codeine per 100 milliliters, such as codeine and guaifenesin, are Schedule V (although some states have reclassified these as Schedule III).

Codeine has been used for over 100 years and has been classified as generally recognized as safe (GRAS) since 1950. On July 16, 2009, single-ingredient, prescription-only codeine tablets received FDA approval via a new drug application (NDA).

Important Information About Codeine

Get emergency help or call 911 right away if you take too much codeine (overdose). When you first start taking codeine, when your dose is changed, or if you take too much (overdose), serious or life-threatening breathing problems that can lead to death may occur. Ask your healthcare provider about medicines like naloxone or nalmefene that can be used in an emergency to reverse an opioid overdose.

Taking codeine with other opioid medicines, benzodiazepines, gabapentinoids (gabapentin or pregabalin), alcohol, or other central nervous system depressants (including street drugs) can cause severe drowsiness, decreased awareness, breathing problems, coma, and death.

Never give anyone else your codeine. They could die from taking it. Selling or giving away codeine is against the law.

Store codeine securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home.

Important Information Guiding Use in Pediatric Patients

Do not give codeine to a child younger than 12 years of age.
Do not give codeine to a child younger than 18 years of age after surgery to remove the tonsils and/or adenoids.
Avoid giving codeine to children between 12 and 18 years of age who have risk factors for breathing problems, such as obstructive sleep apnea, obesity, or underlying lung problems.

Side Effects

The possible side effects of codeine are constipation, nausea, sleepiness, vomiting, tiredness, headache, dizziness, and abdominal pain. Call your healthcare provider if you have any of these symptoms and they are severe.

Get emergency medical help or call 911 right away if you have:

Trouble breathing, shortness of breath, fast heartbeat, chest pain, swelling of your face, tongue, or throat, extreme drowsiness, light-headedness when changing positions, feeling faint, agitation, high body temperature, trouble walking, stiff muscles, or mental changes such as confusion
If you are a nursing mother taking codeine and your breastfeeding baby has increased sleepiness, confusion, difficulty breathing, shallow breathing, limpness, or difficulty breastfeeding.

These are not all the possible side effects of codeine. Call your healthcare provider for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Before Taking

Do not take codeine if you have:

Severe asthma, trouble breathing, or other lung problems.
A bowel blockage or a narrowing of the stomach or intestines.
An allergy to codeine Tablets or any of the ingredients.

Before taking codeine, tell your healthcare provider if you have a history of:

Head injury, seizures
Problems urinating
Abuse of street or prescription drugs, alcohol addiction, opioid overdose, or mental health problems.
Liver, kidney, thyroid problems
Pancreas or gallbladder problems
Have been told by your healthcare provider that you are a “rapid metabolizer” of certain medicines.

Tell your healthcare provider if you are:

Noticing your pain is getting worse. If your pain gets worse after you take codeine, do not take more codeine without first talking to your healthcare provider. Talk to your healthcare provider if the pain that you have increases, if you feel more sensitive to pain, or if you have new pain after taking codeine.
Pregnant or planning to become pregnant. Use of codeine for an extended period of time during pregnancy can cause withdrawal symptoms in your newborn baby that could be life-threatening if not recognized and treated.
Breastfeeding. Not recommended; may harm your baby.
Living in a household where there are small children or someone who has abused street or prescription drugs.
Taking prescription or over-the-counter medicines, vitamins, or herbal supplements. Taking codeine with certain other medicines can cause serious side effects that could lead to death.

How do I Take Codeine

Do not change your dose. Take codeine exactly as prescribed by your healthcare provider. Use the lowest dose possible for the shortest time needed.

For acute (short-term) pain, you may only need to take codeine for a few days. You may have some codeine left over that you did not use. See disposal information at the bottom of this section for directions on how to safely throw away (dispose of) your unused codeine.
Take your prescribed dose every 4 hours as needed for pain.
Do not take more than your prescribed dose. If you miss a dose, take your next dose at your usual time.

Call your healthcare provider if the dose you are taking does not control your pain.

If you have been taking codeine regularly, do not stop taking codeine without talking to your healthcare provider.

Dispose of expired, unwanted, or unused codeine by taking your drug to an authorized DEA-registered collector or drug take-back program. If one is not available, you can dispose of codeine by mixing the product with dirt, cat litter, or coffee grounds; placing the mixture in a sealed plastic bag, and throwing the bag in your trash.

What Should I Avoid While Taking Codeine?

While taking codeine, DO NOT:

Drive or operate heavy machinery until you know how codeine affects you. Codeine sulfate can make you sleepy, dizzy, or lightheaded.
Drink alcohol or use prescription or over-the-counter medicines that contain alcohol. Using products containing alcohol during treatment with codeine may cause you to overdose and die.

Dosing information

Adult Dose of Codeine for Pain

Initial dose: 15 to 60 mg orally up to every 4 hours as needed
Maximum dose: 360 mg in 24 hours

Comments:

Initial doses should be individualized, taking into account the severity of pain, response, prior analgesic treatment experience, and risk factors for addiction, abuse, and misuse.
Doses higher than 60 mg have not been shown to improve pain relief and are associated with an increased incidence of adverse effects.
Because of the risks of addiction, abuse, and misuse, the lowest effective dose for the shortest duration consistent with individual patient treatment goals should be used.
Monitor patients closely for respiratory depression within the first 24 to 72 hours after initiating therapy and after any dose increase.

How Does Codeine Work?

Codeine is a mu-opioid receptor agonist, though its affinity for this receptor is considerably weaker than morphine’s. Its analgesic properties depend primarily on its conversion to morphine in the liver, which binds to the mu-opioid receptor with far greater affinity. When opioids bind to these receptors, a cascade of intracellular events occurs, leading to hyperpolarization of neuronal cells and inhibition of nociceptive neurotransmitter release, ultimately reducing the perception of pain. The exact mechanism, however, remains incompletely understood.

What Other Drugs Will Affect Codeine?

You may have breathing problems or withdrawal symptoms if you start or stop taking certain other medicines. Tell your doctor if you also use an antibiotic, antifungal medication, heart or blood pressure medication, seizure medication, or medicine to treat HIV or hepatitis C.

Opioid medication can interact with many other drugs and cause dangerous side effects or death. Be sure your doctor knows if you also use:

cold or allergy medicines, bronchodilator asthma/COPD medication, or a diuretic (“water pill”);
medicines for motion sickness, irritable bowel syndrome, or overactive bladder;
other narcotic medications – opioid pain medicine or prescription cough medicine;
a sedative like Valium – diazepam, alprazolam, lorazepam, Xanax, Klonopin, Versed, and others;
drugs that make you sleepy or slow your breathing – a sleeping pill, muscle relaxer, medicine to treat mood disorders or mental illness; or
drugs that affect serotonin levels in your body– a stimulant, or medicine for depression, Parkinson’s disease, migraine headaches, serious infections, or nausea and vomiting.

This list is not complete. Other drugs may interact with codeine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Popular FAQ

How many hours apart should I take codeine?

You should take codeine tablets at least FOUR hours apart. Do not take them any more frequently than every four hours.

How does codeine interact with the body?

Codeine acts on your brain and nervous system to lessen the way you feel pain. Codeine works by weakly binding to a specific opioid receptor, known as the mu-opioid receptor, but with much less affinity than morphine, which means its pain-relieving effects are not as strong as morphine’s.

What is codeine actually used for?

Codeine is an oral prescription opioid (narcotic) drug most commonly used to treat mild-to-moderate pain, as a cough suppressant, and to help relieve pain from tension headaches. It is often combined with other medications for these or other uses and can be habit-forming.

Is tramadol stronger than codeine?

Both tramadol and codeine are prescription painkillers used to treat moderate pain, and they are generally considered comparable in terms of pain relief. Tramadol is sometimes considered slightly more effective for moderate to moderately severe pain due to its dual mechanism of action, but both are classified as “weak” opioids.

Codeine is an opiate derived from the poppy plant, similar to morphine. Tramadol is a synthetic (man-made) opioid with a chemical structure similar to codeine but manufactured in a lab. While opiates are drugs derived directly from opium, opioids are a broader class of opiate analogues with morphine-like activity. Opioid medications, such as tramadol and codeine, should only be used to treat moderate to moderately severe chronic pain in adults, when other pain treatments such as non-opioid pain medicines do not treat your pain well enough, or you cannot tolerate them.

Position on the Analgesic Ladder

On the analgesic ladder, tramadol sits alongside codeine and dihydrocodeine as a prescribing option. Research has suggested tramadol’s effectiveness at relieving acute pain after dental surgery was similar to 60 milligrams of codeine, but less than a recommended dose of NSAIDs or a codeine combination such as acetaminophen/codeine.

A large retrospective study of over one million patients found that tramadol, compared with codeine, was associated with a higher risk of cardiovascular events, fractures, and mortality, but no difference in the risk of opioid abuse or dependence. The authors urged caution when interpreting the results due to potential confounding factors.

Codeine Requires Conversion to Morphine to Work

One key pharmacological difference is that codeine requires conversion to morphine by the liver via the CYP2D6 enzyme, and this conversion varies by individual. Tramadol also relies on CYP2D6 for conversion to its active form, meaning patients taking CYP2D6 inhibitors such as fluoxetine or bupropion may experience reduced effectiveness. Tramadol’s additional mechanism of increasing serotonin and norepinephrine levels can offer better relief in cases where codeine is ineffective, but also introduces additional risks.

Codeine Vs. Tramadol: Differences in Side Effects

There are notable differences between the two drugs’ side effect profiles. Tramadol carries a lower risk of respiratory depression and generally causes less constipation than codeine, but has an increased risk of serotonin toxicity, particularly when combined with other medications that raise serotonin levels. Symptoms of serotonin toxicity may include sweating, shaking, and headaches. Tramadol can also lower the seizure threshold, meaning it should not be used by people with a history of seizures or taken alongside monoamine oxidase inhibitors (MAOIs).
In addition to pain relief, codeine is also used as a cough suppressant. Both medications may be combined with other ingredients such as acetaminophen. It is not recommended to take tramadol and codeine together, as combining two opioids can amplify side effects and increase the risk of overdose.

Side effects common to both drugs include potential for addiction, dizziness, confusion, sedation, and constipation. Although both are considered weaker than other opioids, both are habit-forming and can cause severe withdrawal symptoms if stopped abruptly. Tramadol withdrawal is particularly complex, combining opioid withdrawal symptoms such as sweating and gastrointestinal distress with symptoms resembling SSRI withdrawal, including anxiety, confusion, and in some cases hallucinations. There is always a risk with opioid pain medicines that even if you take your dose correctly as prescribed, you are at risk for opioid addiction, abuse, and misuse that can lead to death.

Key Takeaways: Tramadol Vs. Codeine

Effectiveness: Tramadol is often preferred for more persistent or moderate to severe pain. Codeine’s effectiveness depends on individual liver enzyme activity for conversion to morphine. A study of hand surgery patients found tramadol prescriptions were refilled at a higher rate than codeine, suggesting it may be less effective for some patients in acute postoperative settings.
Usage: Tramadol (Ultram, ConZip, Rybix ODT) is commonly used for both acute and chronic pain. Codeine is more often paired with acetaminophen (for example, Tylenol with Codeine) for acute pain and as a cough suppressant.
Risks: Tramadol carries a higher risk of serotonin syndrome and seizures. Codeine carries a higher risk of constipation and respiratory depression. Both carry risks of addiction, dependence, and withdrawal.
Pharmacology: Codeine is an opiate medicine and tramadol is a synthetic (man-made) opioid. Opiates are drugs derived directly from opium (eg, morphine, codeine, and heroin); while opioids are a broad class of opiate analogues that have morphine-like activity.

Which drugs cause opioid-induced constipation?

Any drug that is classified as an “opioid” can cause constipation. Examples of commonly prescribed opioids (narcotics) that may cause this side effect include hydrocodone, oxycodone, morphine, fentanyl, methadone, codeine and tramadol.

hydrocodone (Hysingla ER)
oxycodone (Oxycontin, Roxicodone)
morphine (MS Contin, Kadian)
fentanyl (Duragesic, Actiq)
methadone
codeine
tramadol (ConZip)

How common is opioid-induced constipation?

Opioids, often used for pain control can be responsible for many side effects including sedation, nausea, and drug tolerance. An opioid is sometimes called a narcotic, and they are used for varying degrees of moderate-to-severe pain. They came in various forms, like oral tablets, injections and even skin patches.

One of the most common and troubling side effects with opioids is Opioid-Induced Constipation (OIC). In fact, 40% to 80% of patients taking opioids over the long-term may suffer from this side effect.

Talking about constipation can be embarrassing, but it can be a serious side effect and deserves your attention. Opioid-Induced Constipation (OIC) can occur among patients with chronic non-cancer pain, such as:

Musculoskeletal pain like severe back pain
Osteoarthritis like knee pain
Fibromyalgia
Headache
Other degenerative joint pain

While many opioid side effects such as drowsiness, nausea and vomiting, and respiratory depression (slowed breathing) may lessen over time due to the development of tolerance, the constipating effects of opioids can last throughout the entire period of treatment.

Guidelines state opioids should not be used first-line as treatment for chronic, non-cancer pain, but opioid-induced constipation can happen quickly — in a matter of days. This can result in more serious complications, like fecal impaction, anal fissures, rectal bleeding or prolapse, stomach pain, hemorrhoids, or perforation. It’s nothing to laugh about, and it is important you discuss constipation concerns with your doctor.

What are the symptoms of opioid-induced constipation?

Frequent symptoms of opioid-induced constipation include:

Difficulty passing stools
Hard, dry or infrequent (less than at least 3 per week) bowel movements
Pain during bowel movement
Straining, incomplete evacuation of stool
Bloating or distention in the stomach

Constipation and infrequent bowel movements can lead to more serious complications. Opioid-induced constipation should be addressed or prevented to help avoid issues such as stool impaction or bowel perforation.

If you’ve recently started an opioid, and notice these symptoms above, contact your doctor to discuss treatment options. If you are being prescribed a medicine for pain, ask your doctor if it causes constipation and how you should prevent this side effect.

What causes opioid-induced constipation?

Opioids work well for pain but are known for causing stomach and bowel side effects, in addition to a high risk for tolerance and addiction. Opioid-Induced Constipation (OIC) is one of the most common side effects of opioid use, and can start quickly and last as long as the patient takes the opioid.

Opioids attach to special receptors, called μ (mu) receptors in the central nervous system to help block pain. Opioids like codeine or hydrocodone are used for pain because they block these pain signals in the brain. But μ receptors are also found in the bowel, and when the opioid attaches here, it can slow down bowel movement and lead to opioid-induced constipation.

Pain and chronic illness can also lead to immobility and infrequent exercise, which can worsen constipation.

Other contributing factors include:

Dehydration; the elderly may be more likely to get dehydrated due to lack of fluids.
Certain medications, like tricyclic antidepressants or other anticholinergic drugs, can worsen constipation
Hypercalcemia (high blood calcium levels)
Bowel obstruction
Certain chemotherapy regimens.

How do I treat opioid-induced constipation?

Opioid-induced constipation (OIC) results in bowel movements that are infrequent or incomplete due to a side effect of opioid medications.

Prevention of opioid-induced constipation is always preferred over waiting to treat it due to the possibility of complications from unaddressed constipation. For example, changing your diet, increasing fluids like water, adding dietary fiber, stool softeners, or other laxatives to help prevent constipation from opioids is a common and accepted practice.

This may be especially important in the elderly, those with limited mobility, or those who take other drugs that also cause constipation (such as tricyclic antidepressants, antihistamines, calcium or iron supplements, and aluminum-containing antacids). If you are not sure if your medicine causes constipation, ask your doctor or pharmacist.

If opioid-induced constipation does occur, the basic principles of treating OIC are similar to the methods used to handle most other opioid side effects:

Your healthcare provider may lower your opioid dose (which may not always be possible dependent upon pain levels).
You may be able to manage the side effects with other medications or lifestyle changes.
Your healthcare provider may change the prescribed opioid to a different class of pain medication that is less constipating.

Which lifestyle changes help prevent opioid-induced constipation?

It’s important to address opioid-induced constipation (OIC) with dietary and lifestyle changes, even if medications are still needed. Prevention is preferred over treatment, when possible; however, it is unlikely that dietary and lifestyle changes alone will prevent or treat OIC. It’s best to start OIC prevention strategies when the opioid is initiated.

Nondrug actions that can be added to OIC drug therapy to help prevent constipation when an opioid is started include:

Increased fluid intake, especially water; drink at least eight 8-ounce glasses of water daily.
Increased dietary soluble fiber intake (but not if dehydrated, debilitated or a bowel obstruction). Fiber supplements and/or bulk-forming laxatives (eg, psyllium) require good oral hydration; but effectiveness is generally modest in patients with OIC.
Daily exercise and activity, when able and approved by your doctor
Timely toileting habits
Bathroom privacy.

How do I prevent opioid-induced constipation?

Exercise, added fiber in the diet with whole grains, fruits and leafy vegetables, and plenty of fluids can be helpful, but may not work for everyone.

In these cases, typical first-line agents used in OIC (many available over-the-counter) may be effective. If you have OIC, you should contact your healthcare provider for advice to determine the best diet and over-the-counter medicine regimen and dose, based on your health history.

Senna (Senokot, Senokot-S)

Intermittent or daily use of an oral stimulant laxative (senna, 2 tablets at bedtime) usually given with a stool softener like docusate (100 mg orally twice a day), increases the movement of stool through the gut and helps to keep stool softer by reducing water absorption out of the intestines.
There are few risks with short-term use. It is often the first-line choice for prevention of OIC when pain treatment is started. One disadvantage is that its effectiveness may wane over time.

Bisacodyl (Dulcolax)

A stimulant laxative that is also available without a prescription.
It can be used intermittently (every 2 to 3 days) orally or as a rectal suppository for constipation, but can cause some cramping and explosive diarrhea.
Bisacodyl suppositories usually produce a bowel movement within 1/2 to 1 hour, while tablets usually take 6 to 12 hours.

Docusate (Colace)

Daily use of a common surfactant stool softener available over-the-counter (OTC). As noted above, docusate is probably best combined with senna (Senokot S) for treatment or prevention of OIC in patients with hard, dry stools. Used by itself, docusate is often not effective.

Osmotic cathartics

Osmotic cathartics such as lactulose (Cholac, Constilac, Enulose, Generlac) or polyethylene glycol (MiraLax) increase water in the bowel and help to move the bowel movement more quickly through the intestine.

Polyethylene glycol (MiraLax) is not absorbed into the bloodstream and can be used longer-term, if needed. Your doctor may suggest you take it daily as a preventive for OIC – (17 grams or one heaping teaspoonful), or can be used intermittently (every 2 or 3 days). Check with your healthcare provider for the best dose regimen.
Lactulose can be given in a daily dose of 30 mL as a preventive for OIC. It can lead to excessive gas, cramping and bloating, and may need to be avoided in patients who are lactose-intolerant and those who require a low galactose diet.

Which drugs are FDA-approved for opioid-induced constipation?

Peripheral opioid receptor antagonists

Opioid antagonists work peripherally (in the gut, not in the brain) binding to the opioid receptor and prevent the constipating effect from narcotics. Unlike laxatives, peripherally acting μ-opioid receptor antagonists directly affect how opioids cause constipation; however, the pain-relieving effect of the opioid is not blocked.

FDA-approved regimens include:

methylnaltrexone (Relistor)
naloxegol (Movantik)
naldemidine (Symproic)
alvimopan (Entereg; brand name discontinued in U.S)

Relistor

Relistor (methylnaltrexone), a derivative of naltrexone, is classified as a mu-opioid receptor antagonist, and blocks receptors in the bowel that can interact with pain medications and lead to constipation. However, Relistor does not block the pain receptors in the brain, so the pain-relieving action of the opioid medication still takes effect, and does not induce opioid withdrawal symptoms.

Relistor was originally approved in 2008 as a subcutaneous (under the skin) injection in various strengths. In 2016, the 150 mg oral tablets were also approved.

Both the injection and tablets are approved to treat Opioid-Induced Constipation in adults with chronic non-cancer pain.

Relistor injection (but not the oral tablets) is approved for Opioid-Induced Constipation in adults with advanced illness.

Common side effects include abdominal (stomach area) pain or distention, diarrhea, excessive sweating, chills, gas, and nausea.

Do not use Relistor if you have a blockage in your stomach or intestines, or are at risk, due to a possible perforation (tear). The use of Relistor injection longer than 4 months has not been studied in patients with advanced illness.

Learn more: Side effects with Relistor (in more detail)

Movantik

In September, 2014 the FDA cleared AstraZeneca’s Movantik (naloxegol) to treat opioid-induced constipation (OIC) in adults with long-lasting (chronic) pain that is not caused by active cancer. This includes patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation.

Movantik may be more effective in people who have been taking opioid pain medicine for at least 4 weeks.

Like Relistor, Movantik is a peripherally acting mu-opioid receptor antagonist that blocks opioid receptors in the intestines with little penetration into the the brain.

In clinical studies, 1,352 participants received 12.5 milligrams (mg) or 25 mg of Movantik or a placebo (sugar pill) once daily for 12 weeks. Results showed that 41% to 44% of participants experienced an increase in bowel movements per week, compared to 29% of participants receiving placebo.

Do not take Movantik if you have a bowel blockage (intestinal obstruction) or a history of bowel blockage.

It’s important to avoid eating grapefruit or drinking grapefruit juice during treatment with Movantik, as this can increase drug levels in your blood, which may worsen side effects. Take Movantik on an empty stomach at least 1 hour prior to the first meal of the day or 2 hours after the meal.

Symproic

In March of 2017, the FDA approved Shionogi’s Symproic (naldemedine), another peripherally-acting mu-opioid receptor antagonist. Symproic treats OIC without reducing the pain-relieving effects of the narcotic.

Symproic is indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation.

Those who have received opioids for less than 4 weeks may be less responsive to Symproic.

If your opioid pain medication is stopped, your doctor will also stop your use of Symproic.

Symproic is usually taken by mouth once a day, with or without food. Your pharmacist or doctor should review your medicines, including non-prescription drugs, for drug interactions including possible CYP 450 3A drug interactions.

Most common adverse reactions (≥2%) are: abdominal (stomach area) pain, diarrhea, nausea and gastroenteritis.

Symproic approval was based on the COMPOSE I and II randomized trials: two 12-week, randomized efficacy studies and one 52-week safety study conducted in adult patients with OIC and chronic non-cancer pain. Symproic met its primary and key secondary endpoints in both COMPOSE I and II.

Entereg / Alvimopan

Note: The brand name product Entereg has been discontinued in the U.S. but the generic product, alvimopan, is still available by prescription and via a REMS program.

Alvimopan is a peripherally-acting mu opioid receptor antagonist used to help patients regain gastrointestinal (GI) function earlier following surgeries that include bowel resection (surgery to remove a portion of your intestine) with primary anastomosis (when the ends of the intestines are surgically connected during surgery).

Alvimopan is only approved for short-term use (15 doses) in patients in a hospital enrolled in the Alvimopan REMS program, due to the potential risk of heart attack with long-term use. It is NOT used to treat Opioid-Induced Constipation on an outpatient basis.

Alvimopan is for short-term use after bowel resection surgery only. Patients should not receive more than 15 doses of Alvimopan or use it for longer than 7 days.

Alvimopan should not be used (is contraindicated) in patients who have received therapeutic doses of opioids for more than 7 consecutive days immediately prior to taking Entereg due to possible side effects such as stomach pain, nausea, vomiting, and diarrhea.

The most common adverse reaction (in at least 1.5% of patients) include dyspepsia (heartburn).

A Boxed Warning, the FDA’s most stringent safety warning, is found on the labeling for alvimopan. Warnings include:

Increased incidence of myocardial infarction (heart attack) was seen in a clinical trial of patients taking alvimopan for long-term use.
Alvimopan capsules are available only through a restricted program for short-term use (15 doses) called the Alvimopan REMS Program.

In studies, there was a greater incidence of myocardial infarction (heart attack) in alvimopan-treated patients compared to placebo-treated patients in a 12-month clinical trial, although a causal relationship has not been established. In short-term trials with alvimopan, no increased risk of myocardial infarction was observed.

Discuss any questions or concerns about alvimopan use with your doctor or other healthcare provider