Naltroxene 50mg

What is naltrexone?

Naltrexone is a prescription medication used to treat alcohol use disorder and opioid use disorder. It helps you stop using these substances and remain off them.

Naltrexone belongs to a class of drugs known as opioid antagonists and works by blocking the mu opioid receptor. It blocks the effects of alcohol and opioid medications, preventing the intoxication these substances cause. Naltrexone 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 comes as an extended-release intramuscular injection (Vivitrol) and as oral tablets. The branded versions of naltrexone tablets (Revia, Depade) have been discontinued, but generic versions are available.

Naltrexone tablets were first approved by the US Food and Drug Administration (FDA) in 1984. In 2006, the FDA also approved Vivitrol, the extended-release intramuscular injection form of naltrexone.

What is naltrexone used for?

Naltrexone is a prescription medication that is used:

• to treat alcohol dependence
• for the blockade of the effects of exogenously administered opioids. To prevent relapse to opioid dependence, after opioid detoxification.

You should stop drinking alcohol or using opioids before starting naltrexone.

Naltrexone hydrochloride should not be used in children and adolescents under 18 years.

Important information

Naltrexone can cause serious side effects, including:

1. 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 naltrexone injection is due
  • if you miss a dose of this medication
  • after you stop naltrexone treatment
    
    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.
      
      Get emergency medical help right away in all cases of known or suspected opioid overdose, even if naloxone is administered.

Some people have had severe injection site reactions, including tissue death (necrosis), while receiving naltrexone 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.

3. 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.

4. Liver damage or hepatitis. Naltrexone 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 that 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).

Who should not use naltrexone?

Do not use naltrexone if you:

• are using or have a physical dependence on/addiction to opioid-containing medicines or opioid street drugs.
  To see whether you have a physical dependence on opioids, your healthcare provider may give you a small injection of a medicine called naloxone. This is called a naloxone challenge test. If you get symptoms of opioid withdrawal after the naloxone challenge test, do not start treatment with naltrexone at that time. Your healthcare provider may repeat the test after you have stopped using opioids to see whether it is safe to start this medication.
• are having opioid withdrawal symptoms. Opioid withdrawal symptoms may happen when you have been taking opioids regularly and then stop.
  Symptoms of opioid withdrawal may include:
  • anxiety
  • sleeplessness
  • yawning
  • fever
  • sweating
  • teary eyes
  • runny nose
  • goose bumps
  • shakiness
  • hot or cold flushes
  • muscle aches
  • muscle twitches
  • restlessness
  • nausea and vomiting
  • diarrhea
  • stomach cramps
    
    Tell your healthcare provider if you have any of these symptoms before taking this medication.
• are taking methadone
• have severe liver problems or acute hepatitis
• have severe kidney problems
• are allergic to naltrexone or any of the ingredients in the formulation of it you use or the liquid used to mix the injectable form (diluent). See below for a complete list of ingredients.

Before you receive naltrexone, tell your healthcare provider if you:

• have liver problems
• use or abuse street (illegal) drugs
• have hemophilia or other bleeding problems
• have kidney problems
• have any other medical conditions
• have alcohol dependence and use opioids

How should I use naltrexone?

Using opioids in the 7 to 14 days before you start receiving naltrexone may cause you to suddenly have symptoms of opioid withdrawal. To avoid this you should not use opioids for a minimum of 7-10 days before starting treatment with naltrexone.

How to take naltrexone tablets

• Always take this medicine exactly as your doctor has told you. Check with your doctor or pharmacist if you are not sure.
• Take this medication once a day by mouth as your doctor tells you to.
• The amount of time you should take this medication for will be decided by your doctor. The usual length of treatment is three months. However, in certain cases, a longer period of treatment may be beneficial.

What happens if I miss a dose?

If you forget to take your naltrexone tablet, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take a double dose to make up for a forgotten dose.

If you miss your appointment for your naltrexone injection, schedule another appointment as soon as possible.

What happens if I overdose?

If you take more naltrexone tablets than you should, tell your Doctor or Pharmacist or contact your nearest hospital emergency department immediately.

What should I avoid while using naltrexone?

Do not drive a car, operate machinery, or do other dangerous activities until you know how this medication affects you. Naltrexone may make you feel dizzy and sleepy.

Tablets:

• Alcoholism: The recommended dose is 1 tablet (50 mg) once a day
• Opioid dependence: Start with half a tablet (25 mg) and if no withdrawal signs occur increase to the dose to 1 tablet (50 mg) a day from then on

Intramuscular injection:

• The recommended dose is naltrexone 380 mg delivered intramuscularly (IM) as a gluteal injection, every 4 weeks or once a month, alternating buttocks for each subsequent.

See the full prescribing information for further details about naltrexone dosing.

What are the side effects of naltrexone?

Serious side effects of naltrexone include:

• See 'Important information' above
• Depressed mood. Sometimes this leads to suicide, or suicidal thoughts, and suicidal behavior. Tell your family members and people closest to you that you are taking this medication.
  You, a family member, or the people closest to you should call your healthcare provider right away if you become depressed or have any of the following symptoms of depression, especially if they are new, worse, or worry you:
  • You feel sad or have crying spells.
  • You are no longer interested in seeing your friends or doing things you used to enjoy.
  • You are sleeping a lot more or a lot less than usual.
  • You feel hopeless or helpless.
  • You are more irritable, angry, or aggressive than usual.
  • You are more or less hungry than usual or notice a big change in your body weight.
  • You have trouble paying attention.
  • You feel tired or sleepy all the time.
  • You have thoughts about hurting yourself or ending your life.
  • You have hallucinations.
• Pneumonia. Some people receiving this treatment have had a certain type of pneumonia that is caused by an allergic reaction. If this happens to you, you may need to be treated in the hospital. Tell your healthcare provider right away if you have any of these symptoms during treatment with naltrexone:
  • shortness of breath or wheezing
  • coughing that does not go away
• Serious allergic reactions. Serious allergic reactions can happen during or soon after an injection of naltrexone. Tell your healthcare provider or get medical help right away if you have any of these symptoms of a serious allergic reaction.
  • skin rash
  • swelling of your face, eyes, mouth, or tongue
  • trouble breathing or wheezing
  • chest pain
  • feeling dizzy or faint

Common side effects of naltrexone include:

• nausea. Nausea may happen when you first start this medication, but it can improve overtime.
• vomiting
• sleepiness
• anxiety
• headache
• restlessness
• nervousness
• abdominal pain
• painful joints
• muscle pain and muscle cramps
• weakness
• decreased appetite
• heart palpitations
• increased heart rate
• ECG changes
• libido disorders
• thirst
• dizziness
• increase tear secretion
• chest pain
• diarrhea
• constipation
• rash
• delayed ejaculation and erectile dysfunction
• increased energy
• irritability
• increased sweating
• affective disorders
• cold symptoms
• trouble sleeping
• toothache

These are not all the side effects of this medication. For more information, ask your healthcare provider or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Interactions

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.

Pregnancy and breastfeeding

Tell your doctor if you are pregnant or plan to become pregnant. It is not known if naltrexone will harm your unborn baby. This medication should only be used during pregnancy if the potential benefits justifies the potential risk to the fetus.

Tell your doctor if you are breastfeeding. It is not known if naltrexone passes into your milk when it is administered by IM injection, and it is not known if it can harm your baby. Naltrexone from tablets passes into breast milk. Talk to your healthcare provider about whether you will breastfeed or take this medication. You should not do both.

Keep out of sight and reach of children.

What are the ingredients in naltrexone?

Active ingredient: Naltrexone hydrochloride (tablets)

Inactive ingredients vary among the different generic tablet formulations of naltrexone. Check the product label for your particular formulation for a complete list of inactive ingredients.