Buprenorphine Hydrochloride (HCI)

Drug Class: Buprenorphine Hydrochloride > Buprenorphine > Semi Synthetic Opioid > Opioids > Opioid Agonist > Analgesic.

Uses

Doctors prescribe buprenorphine hydrochloride tablets to treat dependence on opioids, like morphine, heroine and codeine. Use is limited to healthcare providers who meet certain qualifications, such as drug rehabilitation and rapid detox specialists. Clinical trials show that buprenorphine hydrochloride is more effective than clonidine or lofexidine to reduce opioid withdrawal symptoms. Scientists are still studying how buprenorphine rates against methadone for treatment of opioid dependence; while methadone is stronger, buprenorphine hydrochloride may make withdrawal symptoms disappear sooner and increase the likelihood of complete withdrawal from opioid dependence.

Other, off label uses for this medicine

Injectable buprenorphine hydrochloride may be used to treat moderate to severe pain.

Administration/Dosage

Buprenorphine hydrochloride is sold under the trade name of Buprenex and Subutex. Buprenex is available as a 0.3 mg injection. Subutex is sold as 2 mg or 8 mg tablets. The therapeutic dose for drug rehabilitation is 12 mg to 16 mg each day. These tablets are to be taken sublingually, or under the tongue. Allow the medication to dissolve under your tongue; do not chew, swallow or suck on the tablet.

Injectable buprenorphine hydrochloride is indicated for children 13 years or older. Dosage is 0.3 mg deep intramuscular or slow intravenous, administered over a two-minute time period. You may repeat with another 0.3 mg 30 to 60 minutes after the initial dose as needed for pain.

A physician typically prescribes buprenorphine hydrochloride to only be taken when you need relief from pain; therefore missing doses is not an issue. If your doctor told you to take buprenorphine hydrochloride on a regular schedule and you miss a dose, take a dose as soon as you remember. If it is nearly time to take another dose and you can tolerate the pain, skip the missed dose and resume your normal schedule. Do not take extra doses in an attempt to catch up.

Action

The central nervous system transmits messages to the brain, letting it know how things are going around your body. When you are ill or injured, chemicals bind to receptors in nerve endings, encoded with special messages about the location, nature and severity of the pain. There are a few groups of receptors around your body, including the mu, kappa and delta receptors. In contrast, when something makes you feel especially good, naturally-produced endorphins bind to nerve receptor to transmit messages of euphoria and pleasure. An opiate agonist, like morphine or heroine, mimics these endorphins to give users a “high” feeling. An opiate antagonist is a drug that displaces an opiate agonist and then binds to that nerve receptor, thereby inhibiting the intoxicating effect of the opiate.
Buprenorphine hydrochloride is in a group known as opioid agonist/antagonist analgesic. This group of opioids acts like both an agonist and as an antagonist in that buprenorphine competes with other opioids to bind with receptors. Buprenorphine relieves pain and prevents other opiates from making you high.

Precautions

An allergic reaction is a serious medical condition that can result in death. Most allergic reactions to medications occur soon after taking the drug, but allergic reactions may be delayed up to 24 hours. Contact your physician or emergency room immediately if you think you are having an allergic reaction to buprenorphine hydrochloride. Anaphylaxis is a sudden and severe form of allergic reaction that can lead to death within 15 minutes of exposure.

Symptoms of an allergic reaction include hives, itchiness, rashes and watery eyes. Symptoms of a severe reaction may include abdominal pain, difficulty breathing, anxiety, feeling lightheaded or nausea and vomiting.

Your doctor may choose another pain medication or change the dosage of buprenorphine hydrochloride if you have a history of certain medical conditions, including a history of dependence to drugs or alcohol. This medication may worsen certain disorders; some medical conditions can interfere with the way buprenorphine hydrochloride works. Tell your doctor about any serious or chronic illnesses including

Your doctor may order laboratory tests to measure the effectiveness of treatment and look for signs of serious side effects. Keep all doctor and laboratory appointments and alert your physician or laboratory technician to any problems you have with side effects or with buprenorphine hydrochloride.

Buprenorphine hydrochloride affects your central nervous system in a way that can make you drowsy. Do not operate heavy machinery or drive a car until you know how you react to this medication. Avoid engaging in risky behavior that requires you to be alert and awake or to make swift decisions. Alcohol and some medications, such as cold or allergy drugs, can enhance this effect.

Do not consume alcohol while taking buprenorphine hydrochloride. Drinking alcohol may worsen side effects. Do not take narcotics or cold and allergy medications while taking buprenorphine hydrochloride; combined use may result in serious side effects or death.

Warnings

The FDA classifies buprenorphine hydrochloride as a pregnancy Category C, which means scientists do not yet know how buprenorphine hydrochloride affects your unborn child. Taking buprenorphine hydrochloride in the last three months of pregnancy may result in your baby experiencing withdrawal symptoms after delivery. Tell your doctor if you are pregnant or plan to become pregnant while taking buprenorphine hydrochloride. If you become pregnant while taking buprenorphine hydrochloride, call your doctor immediately. Buprenorphine hydrochloride is found in breast milk. Do not take buprenorphine hydrochloride while breastfeeding.

Drug Interactions

Buprenorphine hydrochloride may interact in an unfavorable or even dangerous way with other prescriptions, over-the-counter medications and herbal remedies. Give your doctor and pharmacist a complete and updated list of all the prescriptions, remedies and vitamins you take regularly. It is especially important to tell your doctor if you take any of the following drugs:

  • Psychoactive Drugs
  • Sedatives
  • Seizure Medication
  • Antibiotics

Side effects

You may experience side effects while taking buprenorphine hydrochloride. If the more common side effects become intolerable or don’t go away on their own, talk with your doctor. Common side effects include:

  • Shallow or Slowed Breathing.
  • Feeling Light-headed or Fainting.
  • Confusion.
  • Having Unusual Thoughts or Exhibiting Atypical Behavior.
  • Chills.
  • Constipation, Diarrhea, Vomiting, Nausea, Stomach Pain

Some side effects can be severe or life-threatening. Seek medical assistance immediately if you experience severe side effects such as yellowing of your skin or eyes, an allergic reaction, anxiety and nervousness, dark urine, mood changes, pale stools or depressed breathing.

Overdose

Buprenorphine hydrochloride overdose is a serious, life-threatening medical emergency. If you suspect that you or someone you know has taken an overdose of buprenorphine hydrochloride, seek emergency assistance immediately by going to the emergency room or calling an ambulance. If you need immediate help, contact your local poison control center at 1-800-222-1222.
Overdose symptoms include:

  • Excessive Drowsiness
  • Severe Dizziness
  • Very Slow and Shallow Breathing
  • Very Small Pupils

Abuse

The DEA classifies buprenorphine hydrochloride as a Schedule III drug, which means it may lead to moderate or low physical dependence or high psychological dependence. Even though it is typically prescribed to reduce opioid addiction, it carries a low risk for physical dependence. Narcotics are frequently used for recreational purposes and this form of abuse carries an increased risk for dependency and addiction.

Detox

Qualified professionals use buprenorphine hydrochloride to free you from your dependence on opioids. Some in-patient programs offer rapid detox, where you are sedated and anesthetized during the worst parts of the withdrawal syndrome. When you wake up, you do not remember experiencing the withdrawal symptoms that prevented you from quitting opioids on your own. You will start buprenorphine hydrochloride therapy after rapid detox.

Storage

Store this product at room temperature, preferably between the temperatures of 59 degrees to 86 degrees Fahrenheit. Protect from prolonged exposure to light. Do not allow this medication to freeze or to be exposed to heat higher than 104 degrees Fahrenheit.

Miscellaneous information

Buprenorphine hydrochloride was first marketed in the 1980s by the Reckitt & Coleman as a pain reliever. The United States FDA approved its use for detoxification and long-term replacement therapy for opioid addiction in 2002.