Buprenorphine ®

• A synthetic narcotic analgesic.
• Buprenorphine comes in tablet (sublingual) and transdermal patch form, although some misuse includes intravenous injection and nasal inhalation of crushed tablets.

Adverse effects associated with Buprenorphine ® involved maladministration of sublingual tablets crushed to a powder for nasal inhalation by 3% or dissolved in liquid for intravenous administration by 36% of users. ⁽ⁱ⁾ (Source)

• Injectable formulation under the brand name of Buprenex for the treatment of pain.
• Distribution half-life of 2 to 5 hours.
• Rapid penetration of the blood-brain barrier (highly lipophilic).
• 96% protein bound primarily to alpha and beta globulin.
• Metabolizes in the small intestine and the liver, therefore inappropriate in oral use, but indicated for sublingual (under the tongue) administration.
• Must be taken under the doctor's orders, following instructions since it can be habit forming.
• Increased dosage or frequent period of use, more than prescribed, can lead to dependency.
• Regulated in the U.S. under Controlled Substance oversight on all manufacturing, importing, possession, and especially distribution of the drug, with supportive therapy recommended with prescription.
• DEA review indicates that Buprenorphine ® meets the definition of a Schedule III narcotic under the Controlled Substances Act (CSA).
• Classification per potential to cause moderate or low physical dependence or a high psychological dependence when abused.
• When taken as Suboxone tablets, Buprenorphine ® combined with naloxone in a 4:1 ratio at 4, 8, 16, and 24 mg.
• Indications as an opioid analgesic to manage from chronic moderate to acute pain, and for perioperative conditions.
• International abuse suggests Buprenorphine ® closely resembles Schedule II narcotics, except it demonstrates low-dose distribution and a "ceiling effect''.
• 20% of babies born to mothers in treatment with Buprenorphine substitution (for opioid dependence) have exhibited an abstinence syndrome severe enough to require treatment. ⁽ⁱⁱ⁾
• Buprenorphine-addicted patients have easily returned to heroin use, and vice versa.
• Use with sedatives or alcoholic beverages increases risk of adverse side effects, dizziness, and unconsciousness.
• Maximum recommended first-day dosage of Buprenorphine ® is 8 to 12 mg.
• To stabilize opiate withdrawal, the minimum daily dosage of Buprenorphine/naloxone is 12/3 to 24/6 mg. for most patients.
• In 8 years worldwide production has increased by 13 times, and in France by 31 times within 4 years (United Nations International Narcotics Control Board, UN/INCB).
• A 30-day maintenance supply of 2/0.5 mg Buprenorphine/naloxone tablets costs $200 from a retail pharmacy, or 7 times the cost of Methadone, (not including counseling fees). ⁽ⁱⁱⁱ⁾
• Two common street names are "bupe" and "sub(s)”.
• Of the 6.4 million Americans misusing prescription drugs, more than 73% misused prescription pain relievers (2006, National Household Survey).

Read more about substitution and Buprenorphine addiction.

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