Codeine, levopropoxyphene: Similar to dextromethorphan • Naltrexone, nalmefene: Like naloxone but longer durations of action (10 h); naltrexone is used in maintenance programs and can block heroin effects for up to 48 h; naltrexone is also used for alcohol and nicotine dependence; when combined with bupropion, may be effective in weight-loss programs • Alvimopan, methylnaltrexone bromide: Potent μ antagonists with poor entry into the central nervous system; can be used to treat severe opioid-induced constipation without precipitating an abstinence syndrome •TapentadolModerate μ agonist, strong NET inhibitor Analgesia Moderate pain Duration4–6h•Toxicity:Headache; nausea and vomiting; possible dependence •TramadolMixed effects: weak μagonist, moderate SERT inhibitor, weak NET inhibitor Analgesia Moderatepain•adjuncttoopioids in chronic pain syndromes Duration4–6h•Toxicity: Seizures •riskofserotoninsyndromeOTHER ANALGESICS USED IN MODERATE PAIN
NET, norepinephrine reuptake transporter; SERT, serotonin reuptake transporter.
Buprenorphine Buprenex, others, Butrans (transdermal)
Fentanyl Generic, Duragesic (transdermal). Fentanyl Buccal, Fentanyl Actiq (lozenge)
Hydromorphone Generic, Dilaudid, others
Oral, rectal, parenteral Generic
Oral sustained-release capsules Avinza, Kadian
Nalbuphine Generic, Nubain
Oxycodone Generic, OxyContin (sustained release) Pentazocine Talwin Sufentanil Generic, Sufenta
Oxymorphone Generic, Numorphan, others
Remifentanil Generic, Ultiva
Codeine/aspirin Generic, Empirin Compound, others
Naloxone Generic, Narcan *Antidiarrheal opioid preparations are listed in Chapter 62.
†Orphan drug approved only for the treatment of narcotic addiction.
‡Dozens of combination products are available; only a few of the most commonly prescribed are listed here. Codeine combination products available in several strengths are usually denoted No. 2 (15 mg codeine), No. 3 (30 mg codeine), and No. 4 (60 mg codeine). Prescribers should be aware of the possible danger of renal and hepatic injury with acetaminophen, aspirin, and nonsteroidal anti-inflammatory drugs contained in these analgesic combinations.
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