Buprenorphine chemical structure
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Buprenex

Buprenorphine, also colloquially referred to as bupe, is an opioid drug with partial agonist and antagonist actions. Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, yet is now primarily used for the treatment of opioid addiction. It is a Schedule III drug under the Convention on Psychotropic Substances. more...

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Commercial preparations

Britsh firm Reckitt & Colman (now Reckitt Benckiser) first marketed buprenorphine under the trade names Temgesic (sublingual/parenteral preparations, no active additives) and Buprenex (parenteral, no active additives). Two more recent formulations from Reckitt Benckiser have been approved for opioid addiction treatment in the U.S.: Subutex (lemon-lime flavored sublingual, no active additives; in 2mg and 8mg dosages) and Suboxone (orange-tang flavored sublingual, one part naloxone for every four parts buprenorphine; hexagon shaped tablet in 2mg and 8mg dosages). Suboxone contains the opioid antagonist naloxone to deter illicit intravenous preparation of the tablet, this is intended to attenuate the effects of buprenorphine on opioid-naive users should this formulation be injected - however no human studies have been done demonstrating the efficacy of this approach with buprenorphine and a growing number of street reports indicate that the naloxone is ineffective. It must also be noted that buprenorphine in and of itself will induce a precipitated withdrawal syndrome if ingested by an acutely opioid dependent individual via any route.

Buprenorphine is also delivered transdermally in 25, 50 and 75 mcg/hour. The trade name in the UK is Transtec, and manufactured by Napp. A new 5, 10 and 20 mcg/hour patch marketed as Bu'7rans (Bu-trans), where the 7 indicates its once weekly dosage for pain in osteoarthritis.

Pharmacology and pharmacokinetics

Buprenorphine is a thebaine derivative, and its analgesic effect is due to partial agonist activity at μ-opioid receptors. The partial agonist activity means that opioid receptor antagonists (e.g. naloxone) only partially reverse the effects of buprenorphine. Buprenorphine is also a κ-opioid receptor partial agonist/antagonist, and partial/full agonist at the recombinant human ORL1 nociceptin receptor. (Huang et al., 2001)

Buprenorphine hydrochloride is administered by intramuscular injection, intravenous infusion, via a transdermal patch, or as a sublingual tablet. It is not administered orally, due to very high first-pass metabolism. Buprenorphine is metabolised by the liver, via the CYP3A4 isozyme of the cytochrome p450 enzyme system, into norbuprenorphine (by N-dealkylation) and other metabolites. The metabolites are further conjugated with glucuronic acid and eliminated mainly through excretion into the bile. The elimination half-life of buprenorphine is 20.4–72.9 hours (mean 34.6).

The main active metabolite, norbuprenorphine, is a δ-opioid receptor and ORL1 receptor agonist, μ- and κ-opioid receptor partial agonist. (Huang et al., 2001)

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Treating acute pain in addicted patients
From Nursing, 1/1/01 by Compton, Peggy

QUESTION. My postoperative patient acknowledges active abuse of opioids. How can I effectively treat his acute pain without reinforcing his addiction?

ANSWER: Never withhold opioids from someone with acute pain who's suffering from addictive disease. No scientific evidence exists to show that providing opioid analgesia to these patients in any way worsens the disease-or that withholding opioid analgesia increases the likelihood of recovery.

To treat your patient's acute postoperative pain, determine the types and amount of opioid drugs to which he's addicted. Although addiction generalizes across substances, try to avoid exposing the patient to the drug he's been abusing.

Always treat severe pain immediately. Start with opioids. In addition, use nonopioid and adjuvant analgesics and nonpharmacologic pain-relief measures when appropriate.

When possible, therapy should involve just one opioid, not several. Avoid a mixed opioid agonistantagonist, such as butorphanol (Stadol) or a partial agonist such as buprenorphine (Buprenex), because these may precipitate withdrawal symptoms.

Provide analgesia around the clock to maintain opioid blood levels and prevent withdrawal symptoms. Use supplemental doses to handle breakthrough pain.

Keep in mind that a patient who's tolerant to opioids will need much higher dosages to manage pain control than an opioid-naive patient would.

With the patient's participation, consider a written agreement or treatment plan. This may reassure him of your commitment to pain relief and encourage him to cooperate with treatment.

Although controversial for treating addicted patients, patientcontrolled analgesia (PCA) may improve pain control and reduce drugseeking behavior, according to limited research. Include guidelines and expectations for appropriate PCA use in the patient's treatment agreement.

As acute pain decreases, plan with the patient to taper the analgesic gradually to prevent withdrawal symptoms, which can exacerbate pain and lead to drug-seeking behavior or illicit drug use. Use oral long-acting opioid formulations to treat the pain and provide stable blood levels.

Monitor the patient at least every 4 hours for withdrawal symptoms such as yawning, tearing, gastrointestinal symptoms, and anxiety/ dysphoric mood. If these symptoms emerge, treat symptoms aggressively with a more gradual taper of the opioid and consider the addition of clonidine to reduce sympathetic hyperactivity.

Assess the patient's motivation for drug addiction treatment, but only after his pain is under control. Have treatment referral references on hand.

Source: Pain: Clinical Manual, 2nd edition, M. McCaffery and C. Pasero, Mosby, Inc., 1999.

BY PEGGY COMPTON, RN, PhD

Assistant Professor - University of California, Los Angeles School of Nursing - Los Angeles, Calif.

MARGO McCAFFERY, RN, MS, FAAN

Consultant in the Nursing Care of Patients with Pain - Los Angeles, Calif.

Copyright Springhouse Corporation Jan 2001
Provided by ProQuest Information and Learning Company. All rights Reserved

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