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).
Full opioid agonists bind to opioid receptors and block them, thereby decreasing or eliminating the effect of any subsequent heroin use.
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.
Opioid antagonists block opioid receptors and thus counteract the effects of opioids.
See exhibit source 1.
See exhibit source 2.
See exhibit source 3.
individual has not previously taken any form of opioid.