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. Author manuscript; available in PMC: 2015 Sep 15.
Published in final edited form as: Health Aff (Millwood). 2013 Aug;32(8):1462–1469. doi: 10.1377/hlthaff.2012.0846

Exhibit 1.

Characteristics Of Opioid Substitution Treatment Medications And Their Delivery In Canada And The United States

Characteristic Methadone Buprenorphine (B) or buprenorphine and Naloxone (BN)
Description Opioid agonist;a controls opioid craving, eliminating withdrawal symptoms on long-term basis and blocking effects of self-administered opioids B: Partial opioid agonist;b similar characteristics as methadone, but with ceiling effect, which lowers abuse and overdose potential
BN: Partial opioid agonistb paired with opioid antagonist,c which if injected or snorted induces withdrawal symptoms, further discouraging abuse
Administration Oral; liquid form Oral tablet or film; administered under tongue
Prescription source, US Federally regulated drug treatment centers that must adhere to detailed regulations, including on-site counseling and urine toxicology testingd Federally regulated Drug treatment centers, physicians' offices
Prescription source, Canada Drug treatment centers, physicians' offices Drug treatment centers, physicians' offices; available in some jurisdictions with special authority (as second-line therapy)
Dispensing, US On-site at federally-regulated drug treatment centers; take-home doses available only for patients who demonstrate stability in adherence and test negative in urine drug screens Community-based pharmacies or on-site at federally-regulated drug treatment centers
Dispensing, Canada Community-based pharmacies, with ingestion directly observed by pharmacists; take-home doses available only for patients who demonstrate stability in [please provide] Community-based pharmacies
Effectiveness Superior to non-medication based treatment;e more effective than buprenorphine in maintenance treatment of heroin dependencef Superior to non-medication based treatmente
Potential risks and side effects Constipation, excess sweating, drowsiness, decreased libido; irregular heart beat at higher doses
Susceptible to abuse and overdose, particularly during first two weeks
Risk of overdose among opioid-naive individualsg if medication is diverted from intended use
Headache as well as constipation, excess sweating, drowsiness, decreased libido; possible liver problems and stomach pains.
Sublingual buprenorphine can be dissolved, then injected, resulting in possible overdose risk
BN formulated to prevent abuse; naloxone has no effect when taken under the tongue but has unpleasant antagonist properties when injected or snorted

SOURCES Authors' analysis and: (1) Amato L, et al., An overview of systematic reviews of the effectiveness of opiate maintenance therapies (Note 8 in text). (2) Fiellin DA, O'Connor PG. New federal initiatives to enhance the medical treatment of opioid dependence. Ann Intern Med. 2002;137(8):688-92. (3) Mattick RP, et al. Buprenorphine maintenance versus placebo or methadone maintenance for opioid dependence (Note 10 in text).

a

Full opioid agonists bind to opioid receptors and block them, thereby decreasing or eliminating the effect of any subsequent heroin use.

b

Partial agonists bind to receptors and activate them, but not to the same degree as do full agonists. As higher doses and the medication ceiling effects are reached, partial agonists can act like antagonists—occupying receptors but not activating them (or only partially activating them), while at the same time displacing or blocking full agonists from receptors.

c

Opioid antagonists block opioid receptors and thus counteract the effects of opioids.

d

See exhibit source 1.

e

See exhibit source 2.

f

See exhibit source 3.

g

individual has not previously taken any form of opioid.