Laxatives And Buprenorphine: Safe Or Not?

Buprenorphine is an opioid prescription drug used to treat heroin and other opioid dependence. It can cause constipation, which is defined as having fewer than three bowel movements a week. This is because buprenorphine slows down gastric emptying and the smooth muscular propulsion (peristalsis) in the intestines, resulting in increased fluid absorption and harder stools. Opioids also increase anal sphincter tone, impairing the reflex to have a bowel movement. To treat constipation caused by buprenorphine, it is recommended to increase fibre and water intake, and to get more exercise. Doctors may also prescribe laxatives. However, laxatives do not improve the symptoms of opioid-induced constipation and are associated with abdominal symptoms that negatively impact quality of life.

Buprenorphine is an opioid prescription drug

Buprenorphine is a synthetic opioid developed in the 1960s and used to treat pain and opioid use disorder (OUD). It is a synthetic analogue of thebaine, an alkaloid compound derived from the poppy flower. Buprenorphine is a partial opioid agonist, meaning that it produces effects such as euphoria and respiratory depression at low to moderate doses, although these effects are weaker than those of full opioid agonists like methadone and heroin.

Buprenorphine is the first medication to treat OUD that can be prescribed or dispensed in physician offices, significantly increasing access to treatment. It is also the first medication for OUD that does not require treatment in an Opioid Treatment Clinic, making it more convenient for patients. The Drug Enforcement Administration (DEA) and the Department of Health and Human Services (HHS) are committed to ensuring safe and ready access to buprenorphine for individuals who need it.

Buprenorphine has several benefits for those with OUD. It diminishes the effects of physical dependency on opioids, such as withdrawal symptoms and cravings, and it increases safety in cases of overdose. It also has a lower potential for misuse than other opioids. Buprenorphine can be used in agonist substitution treatment, where a more potent full agonist opioid, such as heroin, is substituted with a less potent opioid like buprenorphine. This enables patients to focus on therapy rather than enduring uncomfortable withdrawals.

Buprenorphine is available in various dosage forms and strengths, including buccal film, sublingual tablet, transdermal patch, subdermal or subcutaneous implants, and intravenous or intramuscular injections. It is often combined with naloxone to reduce the potential for misuse and diversion. The recommended initial dose for the treatment of OUD is typically between 2 mg and 4 mg, with a maximum maintenance dosage of 24 mg/day.

Like all medicines, buprenorphine can cause side effects in some people, including constipation, headache, nausea, vomiting, drowsiness, fatigue, muscle aches, blurred vision, and disturbance in attention. Constipation is a common side effect of opioid treatment, and it can be extremely uncomfortable. It occurs because opioids delay the release of hormones that begin digestion, hinder gastric emptying, slow the GI tract, and increase fluid absorption, creating harder stools.

Laxatives are commonly used to treat opioid-induced constipation, but they do not improve symptoms and are associated with abdominal symptoms that negatively impact quality of life. They do not target the underlying mechanisms of opioid-induced constipation and can cause side effects such as gas, bloating, and a sudden urge to defecate. Instead of relieving constipation, laxative use can add to the patient's burden.

If you are experiencing constipation while taking buprenorphine, it is recommended to first try increasing your dietary fibre intake, taking a fibre supplement, and exercising more to improve gut motility. If these measures do not provide relief, your doctor may prescribe laxatives for as-needed use. It is important to speak to your doctor before taking laxatives, especially if you are pregnant or breastfeeding, as they can have side effects and interact with other medications.

Opioids can cause constipation

Opioids slow down digestion in several ways. They can delay the release of hormones that initiate digestion and slow gastric emptying, meaning food takes longer to leave the stomach. They also hinder peristalsis, the wave-like motions that move food through the gastrointestinal tract. This can create harder stools, which are more difficult to pass.

Additionally, opioids increase fluid absorption during digestion, leading to constipation. They can also increase anal sphincter tone, impairing the defecation reflex and leading to blockage due to incomplete bowel movements. Opioids further slow digestion by reducing the emptying of pancreatic juice and bile.

The treatment for OIC includes both lifestyle changes and medications. Increasing dietary fibre, fluid intake, and physical exercise are often recommended. Laxatives are frequently used to treat OIC, and they may be prescribed at the same time as the opioid to prevent constipation. However, laxatives do not always provide complete relief and can have side effects such as abdominal symptoms, gas, and bloating.

For those taking buprenorphine, constipation is a possible side effect. Doctors may prescribe laxatives alongside buprenorphine to prevent or treat constipation. It is important to speak to a doctor or pharmacist about the best way to manage this side effect.

Laxatives are prescribed to treat opioid-induced constipation

Constipation is a common side effect of opioid medications, including buprenorphine. This is known as opioid-induced constipation (OIC). OIC occurs when opioids attach to receptors in the gut, lengthening the time it takes for stool to pass through the gastrointestinal system. This results in hard, dry stools that are difficult to pass. As a result, laxatives are often prescribed to treat OIC.

Laxatives are medications that help to soften stools and stimulate bowel activity, making it easier to have a bowel movement. Common types of laxatives used to treat OIC include:

• Stimulant laxatives: These include biscacodyl (Ducodyl, Dulcolax) and senna-sennosides (Senokot). They induce bowel activity by increasing intestinal contractions.
• Stool softeners: Such as docusate (Colace) and docusate calcium (Surfak). They increase the amount of water in the colon, helping stools to pass more easily.
• Osmotics: Such as oral magnesium hydroxide (Phillips Milk of Magnesia) and polyethylene glycol (MiraLAX). They help fluid move through the colon.
• Mineral oil: A lubricant laxative that helps stool move through the colon and is available in oral and rectal forms.

While laxatives can be effective in treating constipation, they may not always improve OIC. In some cases, laxatives may even worsen OIC by causing side effects such as abdominal symptoms, gas, bloating, and a sudden urge to defecate. These side effects can negatively impact a person's quality of life and may interfere with their work and social activities.

Therefore, it is important for patients taking buprenorphine or other opioids to discuss their options for managing constipation with their doctor or pharmacist. In addition to laxatives, there are also prescription medications specifically designed to treat OIC, such as lubiprostone (Amitiza), methylnaltrexone (Relistor), naloxegol (Movantik), and naldemedine (Symproic). Lifestyle changes, such as increasing fibre intake, staying hydrated, and exercising regularly, can also help prevent and manage OIC.

Laxatives are ineffective in treating opioid-induced constipation

Constipation is a common side effect of taking buprenorphine. This is because opioids, including partial opioid agonists like buprenorphine, can change your digestive system in several ways, causing constipation, bloating and more. Opioids can delay the release of hormones that begin digestion, slow down contractions of the intestinal walls, hinder gastric emptying and peristalsis, and increase the absorption of water from bowel contents, creating harder stool and constipation.

Laxatives are commonly used to treat opioid-induced constipation, but they are ineffective. They do not target the underlying mechanism of opioid-induced constipation, as they do not impact binding to µ-opioid receptors in the gastrointestinal tract. Many patients will not have their constipation resolved with this therapeutic approach. In one survey of patients with chronic noncancer pain, 54% of those treated for opioid-induced constipation with laxatives did not achieve the desired effect even half of the time. In another survey, 96% of patients taking one laxative and 38% taking two laxatives had an inadequate response to treatment.

The multinational Prevalence, Severity, and Impact of Opioid-Induced Bowel Dysfunction (PROBE1) survey assessed opioid-induced bowel dysfunction in 322 patients who were receiving opioids for chronic pain and taking laxatives. Eighty-one percent of patients reported that they experienced constipation despite taking laxatives, and more than half said that constipation had a “moderate-to-great” or “great” impact on their quality of life. Patients also reported a number of other symptoms, such as bloating and gas, which negatively impacted their quality of life.

Laxatives are associated with abdominal symptoms that negatively impact quality of life. Three-quarters of patients currently taking opioids reported side effects with their use. The most common side effects were gas, bloating or fullness, and sudden urge to defecate. Side effects were more common in younger patients: 83% of patients younger than 40 years reported at least one side effect, compared with 73% of older patients. Approximately half of the patients surveyed reported that laxatives interfered with their work or social lives.

Instead of relieving the burden of opioid-induced constipation, laxative use is associated with a negative impact. There is a need to develop evidence-based treatment guidelines, which, combined with better education for health care professionals and patients, would be likely to shift prescribing away from multiple courses of laxatives and toward treatments that target the underlying cause of opioid-induced constipation.

Buprenorphine can be taken in different forms

• Sublingual tablets: These are placed under the tongue and allowed to dissolve slowly. This method ensures rapid absorption and helps to bypass the first-pass metabolism by the liver.
• Buccal film: This is a thin, flexible film that is applied inside the cheek or between the gum and teeth. Similar to sublingual tablets, buccal films also allow for rapid absorption.
• Transdermal patch: Buprenorphine patches are applied to the skin and provide a slow, continuous release of the drug over an extended period, typically used for chronic pain relief.
• Parenteral routes: Buprenorphine can also be administered through subdermal or subcutaneous implants, as well as intravenous, intramuscular, or subcutaneous injections. However, these routes are not commonly used.
• Extended-release injection: This is an injectable form of buprenorphine that provides long-lasting effects and is typically used for the treatment of opioid use disorder.

It is important to note that the availability of these different forms may vary depending on the region and country-specific regulations. Additionally, the choice of buprenorphine formulation depends on the patient's specific needs, medical condition, and the recommendations of their healthcare provider.

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