Naltrexone

Naltrexone is a prescription medication used to treat alcohol use disorder (AUD) and opioid use disorder (OUD) to reduce cravings and help control physiological dependence. Naltrexone works by blocking the effects of alcohol and opioid medications, preventing the euphoria and intoxication (the “buzz”) these substances cause, and it also helps reduce the urge or cravings to use alcohol or opioids. For alcohol use disorder, naltrexone helps people lessen their drinking behaviors and avoid relapses, and over time, cravings for alcohol will decrease. For opioid use disorder, naltrexone prevents euphoria and reduces physiological dependence on opioids such as heroin, morphine, and codeine to help people avoid relapses and remain opioid-free. Low dose naltrexone (LDN) is used for conditions such as fibromyalgia, Crohn’s disease, multiple sclerosis, and complex regional pain syndrome, as it may work as an anti-inflammatory agent in the central nervous system. Use of low dose naltrexone is an off-label use and is not FDA-approved for these conditions. Naltrexone is available as an intramuscular injection (Vivitrol) and as oral tablets. The branded tablets ( Revia , Depade) have been discontinued, but generic versions are available. Naltrexone is an opioid antagonist. Its mechanism of action (MOA) is blocking the mu opioid receptor. This medicine also modifies how the hypothalamus, pituitary gland, and adrenal gland (hypothalamic-pituitary-adrenal axis, HPA axis) interact to suppress the amount of alcohol consumed.

Naltrexone is a prescription medication used to treat alcohol use disorder (AUD) and opioid use disorder (OUD) to reduce cravings and help control physiological dependence. Naltrexone works by blocking the effects of alcohol and opioid medications, preventing the euphoria and intoxication (the “buzz”) these substances cause, and it also helps reduce the urge or cravings to use alcohol or opioids. For alcohol use disorder, naltrexone helps people lessen their drinking behaviors and avoid relapses, and over time, cravings for alcohol will decrease. For opioid use disorder, naltrexone prevents euphoria and reduces physiological dependence on opioids such as heroin, morphine, and codeine to help people avoid relapses and remain opioid-free. Low dose naltrexone (LDN) is used for conditions such as fibromyalgia, Crohn’s disease, multiple sclerosis, and complex regional pain syndrome, as it may work as an anti-inflammatory agent in the central nervous system. Use of low dose naltrexone is an off-label use and is not FDA-approved for these conditions. Naltrexone is available as an intramuscular injection (Vivitrol) and as oral tablets. The branded tablets ( Revia , Depade) have been discontinued, but generic versions are available. Naltrexone is an opioid antagonist. Its mechanism of action (MOA) is blocking the mu opioid receptor. This medicine also modifies how the hypothalamus, pituitary gland, and adrenal gland (hypothalamic-pituitary-adrenal axis, HPA axis) interact to suppress the amount of alcohol consumed.

You should not be treated with  this medicine if you are allergic to it, or if: you are currently addicted to opioids; you are having withdrawal symptoms from opioid addiction; you are using any opioid pain medicine (including fentanyl, Vicodin, OxyContin, and many others); you have failed the naloxone challenge test or have a positive urine screen for opioids or you have used any opioid medicine such as methadone, buprenorphine, tramadol, and other opioids within 7 to 14 days. Also, tell your doctor if you have or have ever had: bleeding problems such as hemophilia; or liver or kidney disease. have alcohol dependence and use opioids.

The severe or irreversible adverse effects of Naltrexone, which give rise to further complications include Hepatic damage, Thrombocytopenic purpura. The signs and symptoms that are produced after the acute overdosage of Naltrexone include Liver dysfunction. The symptomatic adverse reactions produced by Naltrexone are more or less tolerable and if they become severe, they can be treated symptomatically, these include Tiredness, Headache, Diarrhea, Anxiety, Restlessness, Abdominal cramps, Skin rashes, GI adverse effects, Somnolence, Nausea and vomiting, Muscle aching, Decreased appetite, Anxiety, Arthralgia, Depression, Alopecia, Edema, Dyspnea.

This medicine can cause serious side effects, including: Risk of opioid overdose. You can accidentally overdose in two ways. Naltrexone blocks the effects of opioid drugs. Do not take large amounts of opioids, including opioid-containing medicines, such as heroin or prescription pain pills, to try to overcome the opioid-blocking effects of this medication. This can lead to serious injury, coma, or death. After you receive a dose of the extended-release injection form of this medication, its blocking effect slowly decreases and completely goes away over time. If you have used opioid street drugs or opioid-containing medicines in the past, using opioids in amounts that you used before treatment can lead to overdose and death. You may also be more sensitive to the effects of lower amounts of opioids: after you have gone through detoxification when your next injection is due if you miss a dose of this medication after you stop treatment with this medicine It is important that you tell your family and the people closest to you of this increased sensitivity to opioids and the risk of overdose. You or someone close to you should call 911 or get emergency medical help right away if you: have trouble breathing become very drowsy with slowed breathing have slow, shallow breathing (little chest movement with breathing) feel faint, very dizzy, confused, or have unusual symptoms Talk to your healthcare provider about naloxone, a medicine that is available to patients for the emergency treatment of an opioid overdose. Call 911 or get emergency medical help right away in all cases of known or suspected opioid overdose, even if naloxone is administered. Severe reactions at the site of the naltrexone injection (injection site reactions). Some people have had severe injection site reactions, including tissue death (necrosis), while receiving injections. Some of these injection site reactions have required surgery. This medication must be injected by a healthcare provider. Call your healthcare provider right away if you notice any of the following at any of your injection sites: intense pain the area feels hard large area of swelling lumps blisters an open wound a dark scab Tell your healthcare provider about any reaction at an injection site that concerns you, gets worse over time, or does not get better by two weeks after the injection. Sudden opioid withdrawal Anyone who receives naltrexone must not use any type of opioid (must be opioid-free), including street drugs, prescription pain medicines, cough, cold, or diarrhea medicines that contain opioids, or opioid dependence treatments, buprenorphine or methadone, for at least 7 to 14 days before starting this medication. Using opioids in the 7 to 14 days before you start receiving treatment may cause you to suddenly have symptoms of opioid withdrawal when you receive treatment. Sudden opioid withdrawal can be severe, and you may need to go to the hospital. You must be opioid-free before receiving naltrexone unless your healthcare provider decides that you don't need to go through detox first. Instead, your doctor may decide to give this medication in a medical facility that can treat you for sudden opioid withdrawal. Liver damage or hepatitis . This medicine can cause liver damage or hepatitis. Tell your healthcare provider if you have any of the following symptoms of liver problems during treatment with this medication: stomach area pain lasting more than a few days dark urine yellowing of the whites of your eyes tiredness Your healthcare provider may need to stop treating you with this medication if you get signs or symptoms of a serious liver problem. You must inform every doctor who treats you that you are taking Naltrexone. Non-opiate based anesthetics should be used if you require an anesthetic in an emergency situation. If you have to use opiate-containing anesthetics, you may need higher doses than usual. You may also be more sensitive to the side-effects (breathing difficulties and circulatory problems).

This medicine can cause serious side effects, including: Risk of opioid overdose. You can accidentally overdose in two ways. Naltrexone blocks the effects of opioid drugs. Do not take large amounts of opioids, including opioid-containing medicines, such as heroin or prescription pain pills, to try to overcome the opioid-blocking effects of this medication. This can lead to serious injury, coma, or death. After you receive a dose of the extended-release injection form of this medication, its blocking effect slowly decreases and completely goes away over time. If you have used opioid street drugs or opioid-containing medicines in the past, using opioids in amounts that you used before treatment can lead to overdose and death. You may also be more sensitive to the effects of lower amounts of opioids: after you have gone through detoxification when your next injection is due if you miss a dose of this medication after you stop treatment with this medicine It is important that you tell your family and the people closest to you of this increased sensitivity to opioids and the risk of overdose. You or someone close to you should call 911 or get emergency medical help right away if you: have trouble breathing become very drowsy with slowed breathing have slow, shallow breathing (little chest movement with breathing) feel faint, very dizzy, confused, or have unusual symptoms Talk to your healthcare provider about naloxone, a medicine that is available to patients for the emergency treatment of an opioid overdose. Call 911 or get emergency medical help right away in all cases of known or suspected opioid overdose, even if naloxone is administered. Severe reactions at the site of the naltrexone injection (injection site reactions). Some people have had severe injection site reactions, including tissue death (necrosis), while receiving injections. Some of these injection site reactions have required surgery. This medication must be injected by a healthcare provider. Call your healthcare provider right away if you notice any of the following at any of your injection sites: intense pain the area feels hard large area of swelling lumps blisters an open wound a dark scab Tell your healthcare provider about any reaction at an injection site that concerns you, gets worse over time, or does not get better by two weeks after the injection. Sudden opioid withdrawal Anyone who receives naltrexone must not use any type of opioid (must be opioid-free), including street drugs, prescription pain medicines, cough, cold, or diarrhea medicines that contain opioids, or opioid dependence treatments, buprenorphine or methadone, for at least 7 to 14 days before starting this medication. Using opioids in the 7 to 14 days before you start receiving treatment may cause you to suddenly have symptoms of opioid withdrawal when you receive treatment. Sudden opioid withdrawal can be severe, and you may need to go to the hospital. You must be opioid-free before receiving naltrexone unless your healthcare provider decides that you don't need to go through detox first. Instead, your doctor may decide to give this medication in a medical facility that can treat you for sudden opioid withdrawal. Liver damage or hepatitis . This medicine can cause liver damage or hepatitis. Tell your healthcare provider if you have any of the following symptoms of liver problems during treatment with this medication: stomach area pain lasting more than a few days dark urine yellowing of the whites of your eyes tiredness Your healthcare provider may need to stop treating you with this medication if you get signs or symptoms of a serious liver problem. You must inform every doctor who treats you that you are taking Naltrexone. Non-opiate based anesthetics should be used if you require an anesthetic in an emergency situation. If you have to use opiate-containing anesthetics, you may need higher doses than usual. You may also be more sensitive to the side-effects (breathing difficulties and circulatory problems).

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No neonatal dosage information is recorded for this medicine yet.

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you take any opioid-containing medicines for pain, cough or colds, or diarrhea. If you are being treated for alcohol dependence but also use or are addicted to opioid-containing medicines or opioid street drugs, it is important that you tell your healthcare provider before starting naltrexone to avoid having sudden opioid withdrawal symptoms when you start treatment. Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

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