TABLE 2.
Mu Agonist Opioids and Kappa Opioids
| OPIOID | EXAMPLE BRANDS/PREPARATIONS | SPECIAL PAIN ISSUES | SPECIAL MISUSE ISSUES |
|---|---|---|---|
| Mu Agonist Opioids | |||
| Morphine | MS Contin (12-hour CR), Kadian, Avinza (24-hour CR), Oramorph (IR) | CR mechanism provides relatively stable blood levels | CR mechanism may be altered for misuse |
| Oxycodone | Percocet (IR and acetaminophen), Percodan (IR and aspirin), OxyContin (12-hour CR) | CR mechanism provides relatively stable blood levels | CR mechanism may be altered for misuse |
| Hydrocodone | Vicodin (IR and acetaminophen), Lortab (IR and acetaminophen) | The most commonly prescribed opioid (Hughes, Bogdan, and Dart, 2007) | Most commonly misused opioid |
| Hydromorphone | Dilaudid (IR) | Quick onset; relatively high reward value | |
| Fentanyl | Duragesic (72-hour CR patch), Actiq (IR lozenge) | Patch provides very stable blood levels when used as prescribed | Misuse of patch can be particularly dangerous due to concentrated 3-day supply of opioid |
| Methadone | Methadose, Dolophine | Mu opioid; in addiction, promotes analgesia by a second mechanism: NMDA receptor antagonism; produces tolerance less readily than other mu opioids | Misuse and mortality related to misuse have recently increased; pharmacological properties make misuse particularly risky |
| Tramadol | Ultram (IR), Ultracet (IR with acetaminophen) | Promotes analgesia by a second mechanism: increasing serotonin/norepinephrine; doses are limited due to risk of seizures | Relatively low rates of abuse and reward documented in some persons |
| Buprenorphine | Subutex (used for pain, but not FDA approved for pain) | Partial agonist; ceiling effect; used off label for pain | Approved for treatment of opioid addiction; some IV abuse reported |
| Codeine | Tylenol #3 (IR with acetaminophen) | Metabolism to morphine is a rate-limiting step that creates a ceiling of analgesia in most people | |
| Kappa Opioids | |||
| Butorphanol | Stadol (IV or intranasal) | Rapid onset of intranasal; ceiling analgesic effects | Some patients experience less reward than with mu opioids, but intranasal route is quick onset |
| Nalbuphine | Nubain (IV only) | Ceiling analgesic effects | Some patients experience less reward than with mu opioids |
| Pentazocine | Talwin, Talwin NX (with naltrexone) (oral only) | Ceiling analgesic effects | Some patients experience less reward than with mu opioids; formulated with naltrexone due to IV abuse in 1960s |
Abbreviations: CR, controlled release; FDA, Food and Drug Administration; IR, immediate release; IV, intravenous; NMDA, N-methyl-D-aspartic acid.