Buprenorphine and Naloxone

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

Buprenorphine Hydrochloride and Naloxone Hydrochloride

Uses

People use buprenorphine hydrochloride and naloxone hydrochloride preparations as maintenance treatment for dependence on opioid drugs. Buprenorphine prevents withdrawal symptoms in opioid-dependent people. Naloxone acts as a deterrent to drug use because it reverses the effects of opioids, causing withdrawal symptoms in someone physically dependent on opioids.

General Drug Information

Buprenorphine hydrochloride and naloxone hydrochloride is a generic preparation sold under the brand name Suboxone. Each Suboxone contains a ratio of four parts buprenorphine to one part naloxone.

Administration/Dosage

Physicians should administer buprenorphine hydrochloride and naloxone hydrochloride tablets at least four hours after the patient’s last dose of opioids, preferably when early signs of withdrawal appear. Physicians will adjust the dosage by 2 - 4 mg each day to find a dose that fits the patient’s needs.

The typical dose is 4 to 24 mg per day sublingually, or under the tongue, with the target dose being 16 mg daily. Patients requiring two buprenorphine hydrochloride and naloxone hydrochloride tablets should place one on each side of the tongue rather than on top of one another.

Action

Buprenorphine hydrochloride interacts with the central nervous system, or CNS, in the same way as other opioids but buprenorphine does not produce the euphoric effects that other opioids do.

Naloxone prevents abuse by interfering with the way buprenorphine and other opioids act, reducing their analgesic and euphoric effects. Naloxone causes withdrawal symptoms in opioid-dependent people.

Warnings

Physicians have reported a number of deaths in patients who have used buprenorphine intravenously, often concurrently with benzodiazepines like Librium. Using buprenorphine with other depressants, including alcohol or other opioids, increases the risk for death.

Respiratory Depression

Buprenorphine may cause respiratory depression, a dangerous and sometimes fatal breathing condition where the lungs cannot adequately exchange oxygen for carbon dioxide. Symptoms of respiratory depression include slow, shallow breathing and a bluish tint around the victim’s eyes, lips and fingertips. Intravenous administration of buprenorphine is associated with significant respiratory depression.

Patients with serious breathing problems like COPD, diminished lung capacity, low oxygen levels, high carbon dioxide levels or pre-existing respiratory depression should exercise caution when using buprenorphine hydrochloride and naloxone hydrochloride products, as should individuals with the serious heart condition known as cor pulmonale.

CNS Depression

Like other opioids, buprenorphine acts by depressing the central nervous system, or CNS. Taking buprenorphine with other drugs that depress the nervous system can enhance CNS depression. When a patient needs both buprenorphine and another CNS depressant, the physician should decrease the dose of one or both drugs.

Dependence

Because buprenorphine acts like other opioids, it is possible for someone to become opioid-dependent and experience withdrawal symptoms when he stops taking buprenorphine hydrochloride and naloxone hydrochloride products.

Hepatic Events

Buprenorphine hydrochloride and naloxone hydrochloride consumers have experienced liver problems but researchers are not certain if these hepatic events were associated with this medication or if underlying liver problems caused the illnesses.

Allergic Reactions

A consumer may be hypersensitive to buprenorphine and suffer symptoms of an allergic reaction after taking this drug, including rash, hives and itching. Some patients have experienced breathing problems, swelling under the skin and a dangerous form of an allergic reaction, anaphylaxis, after taking buprenorphine hydrochloride and naloxone hydrochloride products.

Hypotension

Like other opioids, buprenorphine can dilate blood vessels to lower blood pressure and cause hypotension. Buprenorphine hydrochloride and naloxone hydrochloride may cause orthostatic hypotension, or blood pressure that plummets when the patient stands up quickly.

Head Injury and Increased Intracranial Pressure

Buprenorphine and respiratory depression can elevate fluid pressure surrounding the brain and spinal cord; head injuries, brain tumors and pre-existing high pressure inside the skull can enhance these effects. Additionally, buprenorphine can cause pinpoint pupils and changes in consciousness that mimic the effects of a head injury, so using buprenorphine hydrochloride and naloxone hydrochloride products may obscure the presence or healing process of head injuries.

Withdrawal Effects

This combination product contains naloxone, which is likely to cause withdrawal symptoms in opioid-dependent individuals.

Precautions

Elderly or debilitated patients should use buprenorphine hydrochloride and naloxone hydrochloride with caution, as should those with Addison’s disease, CNS depression or serious liver, heart or kidney problems. Patients with acute alcoholism or delirium tremens, sometimes called “DTs,” severe curvature of the spine and some types of prostate, urinary and thyroid problems should exercise caution when taking buprenorphine hydrochloride and naloxone hydrochloride. Healthcare providers should administer buprenorphine hydrochloride and naloxone hydrochloride with caution to comatose patients and to those with the serious mental illness, toxic psychosis.

Buprenorphine hydrochloride and naloxone hydrochloride may cause dizziness and drowsiness and impair the consumer’s physical and mental abilities.

Contraindications

Individuals who are hypersensitive to buprenorphine hydrochloride and naloxone hydrochloride should not use preparations containing these drugs.

Pregnancy, Labor and Delivery, Breastfeeding

Products containing buprenorphine hydrochloride and naloxone hydrochloride are an FDA Pregnancy Category C, there have been no adequately controlled studies to determine how this product will affect the unborn baby or if it affects male or female reproductive capabilities.

Taking buprenorphine hydrochloride and naloxone hydrochloride during pregnancy may cause the baby to be born dependent on opioids, suffering withdrawal symptoms in the first eight days of life. A baby experiencing neonatal withdrawal will suffer stiff muscles, tremors, agitation and muscle twitches.

Buprenorphine hydrochloride passes into human milk and onto a nursing baby. Mothers should not breastfeed while taking buprenorphine hydrochloride and naloxone hydrochloride.

Drug Interactions

Buprenorphine hydrochloride and naloxone hydrochloride preparations can interact with other medications in harmful or unwanted ways.

Drugs known as CYP3A4 inhibitors, including some antifungals, antibiotics and HIV drugs, can increase buprenorphine blood levels. Physicians should monitor these patients and adjust the buprenorphine dosage accordingly.

Physicians should prescribe buprenorphine hydrochloride and naloxone hydrochloride preparations with caution to those already on a CND depressant, including benzodiazepines like Valium or Xanax. Using buprenorphine along with benzodiazepines intravenously may cause death.

Side effects

All drugs, including buprenorphine hydrochloride and naloxone hydrochloride preparations, can cause side effects in some consumers. The most commonly reported side effects are headache, constipation, nausea and vomiting, sweating and insomnia.

Overdose

Buprenorphine hydrochloride and naloxone hydrochloride overdose is a serious and life-threatening situation. Overdose victims require immediate medical treatment.

Symptoms of overdose are respiratory depression, pinpoint pupils, sedation and hypotension. Death may occur.

Unlike in cases involving overdose of other opioids, the respiratory depression caused by buprenorphine may not respond to naloxone; high doses of naloxone between 10 and 35 mg per kilogram of body weight may have limited value in relieving respiratory depression. Some physicians have used the respiratory stimulant, Doxapram, to help the patient breathe.

Abuse

The DEA categorizes buprenorphine hydrochloride and naloxone hydrochloride products as class III drugs, meaning they pose a moderate risk for abuse. To reduce this risk, buprenorphine hydrochloride and naloxone hydrochloride is available only with a prescription.

Withdrawal

While doctors usually prescribe buprenorphine hydrochloride and naloxone hydrochloride preparations to treat opioid-dependence, some individuals become physically dependent on buprenorphine and suffer withdrawal symptoms when they stop using it. Buprenorphine withdrawal symptoms start later than with other types of opioid withdrawal. Withdrawal from buprenorphine is less severe than withdrawal from other types of opioids.

If misused, naloxone will lower buprenorphine levels and cause withdrawal symptoms.

To avoid withdrawal symptoms, doctors recommend tapering buprenorphine hydrochloride and naloxone hydrochloride over the course of several days.

Detox

Tapering works for many people, but persistent and strong withdrawal symptoms prevent some from discontinuing buprenorphine hydrochloride and naloxone hydrochloride at the appropriate time. Some local healthcare institutions offer detoxification services to help these individuals overcome withdrawal. During detoxification, the patient receives drugs to lower buprenorphine levels along with medications to ease withdrawal symptoms.

Many informed patients choose the more humane and efficient option - rapid detox. During rapid detox, patients receive anesthesia and sedatives before doctors administer the standard detoxification and anti-withdrawal drugs. The rapid detox patient dozes in a comfortable “twilight sleep” rather than struggling with the protracted detoxification experience.

Storage

Buprenorphine hydrochloride and naloxone hydrochloride products are best stored at 77 degrees Fahrenheit but can tolerate temperatures ranging from 59 to 86 degrees Fahrenheit.