Buprenorphine/naloxone , sold under the brand name Suboxone among others, is a combination drug that includes buprenorphine and naloxone. In combination with counseling, it is used to treat disorders of opioid use. This reduces withdrawal symptoms for about 24 hours. Buprenorphine/naloxone is available for use in two different forms, under the tongue or on the cheek.
Side effects may include respiratory depression (decreased respiration), small pupils, drowsiness, and low blood pressure. The risk of overdose is lower with buprenorphine/naloxone compared with methadone. However, people are more likely to stop buprenorphine/naloxone treatment than methadone. Methadone is generally preferred when treatment is needed during pregnancy.
Buprenorphine, at lower doses, produces the usual opioid effect; however, high doses beyond a certain limit do not produce a greater effect. This is believed to lead to a lower overdose risk than other opioids. Naloxone is an opioid antagonist that competes with and blocks the effects of other opioids (including buprenorphine) if given by injection. The addition of naloxone is to reduce the risk that people will abuse the drug by injection. Abuse with injections or in the nose, however, still occurs. The level of abuse in the United States appears to be lower than other opioids.
The combination formulation was approved for medical use in the United States in 2002. In the United States the wholesale cost in 2017 is between 2.32 and 3.15 USD per day. In the UK the same dose is subject to NHS 0.90 to 2.72 pounds per day, according to 2015 data.
Video Buprenorphine/naloxone
Medical use
Buprenorphine/naloxone is used for the treatment of opioid use disorders. Long-term outcomes are generally better with the use of buprenorphine/naloxone than attempts to stop simultaneous use of opioids. This includes a lower risk of overdose with the use of drugs. Because of the high affinity of binding and low activation of opioid receptors, cravings and pulling opioids decrease while preventing patients from becoming high and recurring in other opioids. The combination of two drugs is preferred over buprenorphine alone for maintenance treatment due to the presence of naloxone in the formulation, which helps serve as a prevention tool of abuse, especially against intravenous use.
Buprenorphine/naloxone has been found to be effective in treating opioid dependence, and serves as the first recommended line of drugs according to the US National Institute for Drug Abuse. It is an effective maintenance therapy for opioid dependence and generally has the same efficacy as methadone, both of which are much more effective than abstinensia-based treatments.
Because it may be prescribed from office settings (compared to methadone requiring specialized centers), buprenorphine/naloxone allows more freedom in patient administration. It also comes with more risks in this vulnerable population. Buprenorphine/naloxone may be recommended for socially stable opioid users who may not be able to take medication from the center of the day, which may have other conditions requiring regular primary care visits, or who may have work or daily life that requires them to maintain all their abilities and can not take tranquilizers. Buprenorphine/naloxone is also recommended more than methadone in people who may be at high risk of methadone toxicity, such as the elderly, those taking high doses of benzodiazepines or other sedatives, alcohol abuse simultaneously, those with lower opioid tolerance levels, and those at risk high QT prolonged intervals. It is also useful to use drugs in combination with psychosocial support and counseling for patients.
Maps Buprenorphine/naloxone
Contraindications
Contraindications are severe respiratory or liver disorders and acute alcoholism. There are limited accounts of cross reactivity with opioids, but it is possible. Serious CNS and respiratory depression may also occur simultaneously with the use of CNS depressants, ingestion of alcohol, or other CNS suppressor factors when using buprenorphine/naloxone.
Adverse effects
Side effects are similar to buprenorphine and other opioids. In addition, naloxone may induce withdrawal symptoms in opioid-addicted individuals. The most common side effects (in the most common order for the most common) of sublingual tablets include: headache, opioid withdrawal syndrome, pain, increased sweating, low blood pressure, and vomiting. The most common side effects seen in the formulation of the film are tongue pain, decreased sensation and redness in the mouth, headache, nausea, vomiting, excessive sweating, constipation, opioid signs and symptoms, difficulty sleeping, pain, and swelling of the extremities.
Buprenorphine/naloxone has a lighter side effect profile than methadone, and has limited respiratory effects, due to the effects of agonist/antagonist. However, buprenorphine/naloxone may be less safe than methadone in patients with stable liver disease, as it can increase liver enzymes.
Dependence and tethering
Buprenorphine/naloxone, when taken excessively, can produce dysphoric symptoms for individuals who are independent of opioid/tolerant because buprenorphine is a partial opioid agonist. The sublingual formulation of the buprenorphine/naloxone combination is designed to reduce the potential for abuse via injection route compared with buprenorphine alone. If the combination is taken by sublingual route, as directed, the addition of naloxone does not reduce the effects of buprenorphine. When the combination of sublingual tablets is dissolved and injected by opioid-dependent individuals, the withdrawal effect can be triggered due to the high parenteral bioavailability of the naloxone. While this mechanism has the potential to act to prevent abuse, Suboxone formulations still have the potential to produce "high" opioid agonists if sublingually abused by independent people, leading to dependence on opioids.
Interactions
The effects of buprenorphine sedation/narcotics are elevated by other sedatives such as other opioids, benzodiazepines, first-generation antihistamines, alcohols, and antipsychotics. In addition, opioids and especially benzodiazepines increase the risk of respiratory depression that is potentially lethal.
Strong inhibitors of CYP3A4 liver enzymes, such as ketoconazole, simply increase buprenorphine concentrations; CYP3A4 inducers can theoretically decrease buprenorphine concentrations.
Pharmacology
Action mechanism
Buprenorphine is strongly bound to opioid receptors and acts as a painkiller in the central nervous system (CNS). This binds to a high affinity-opioid receptor that produces analgesic effects on CNS. Is that partial? agonist and it is a weak antioxidant -opioid receptor. As doses of buprenorphine rise, the analgesic effect reaches the plateau, and then begins to act like an antagonist. As a partial agonist, buprenorphine binds and activates opioid receptors, but has only partial effectiveness on receptors relative to full agonists, even in maximal receptor dwellings. It is thus well suited for treating opioid dependence, since it produces a lighter effect on opioid receptors with less dependence and potential abuse.
Naloxone is a pure opioid antagonist that competes with opioid molecules on CNS and prevents it from binding opioid receptors. The affinity of Naloxone binding is highest for receptors? -opioids, then receptors? -opioids, and receptors? lowest -opioid. Naloxone has poor bioavailability, and is rapidly inactivated after oral administration. But when injected, it gives full effect.
Due to the different bioavailability between the two drugs in this combination, buprenorphine/naloxone works as an abstinence prevention tool: when taken sublingually as prescribed, the buprenorphine effect on opioid receptors dominates, while the naloxone effect is negligible due to low oral absorption. However, when a person tries to abuse drugs either by injection or inhalation, naloxone may act as an antagonist and block the opioid euphoric effect or even precipitate withdrawal in those currently dependent on opioids. It has an overall effect helping to reduce the potential for buprenorphine/naloxone abuse.
Society and culture
Access in the United States
Prior to the Drug Addiction Treatment Act of 2000 (DATA), doctors were not allowed to prescribe narcotics to treat opioid dependence. People with narcotic dependence should go to a registered clinic to receive treatment. With DATA, Suboxone is the first approved drug for office based care for opioid dependence. Suboxone has become widely used as a substitute for methadone because it can be prescribed by doctors in their offices, while methadone can only be provided in limited number of specialized addiction centers, often making access difficult. Some doctors also lead a movement to start prescribing it out of the emergency unit (ED), as several small studies have shown ED-initiation of Suboxone to be effective with patients more likely to remain in addiction treatment compared to those referred to addiction treatment. programs or those who receive only short interventions in the department.
Access to Suboxone may be limited due to previous authorization requirements at various insurance companies. Authorizations were previously used by insurance companies to restrict the use of certain drugs by seeking approval before the insurance company would pay for the drugs. This can affect patient's financial access and compliance. Financial access is determined through prior authorization approval, which should be requested by the applicant before the patient can begin treatment. The time required for an approved request may delay the patient in starting treatment. The previous authorization process may also affect compliance, as approval is required for each recipe or every few months. It presents potential gaps in treatment and withdrawal symptoms as patients wait for approval. Several insurance companies, as well as Medicaid in various states, have removed the use of prior authorization for Suboxone in an effort to improve access to this treatment.
See also
- Methadone
- Buprenorphine/samidorphan
- Buprenorphine/naltrexone
References
Source of the article : Wikipedia
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