Opiates and Opioids
Opiates are a group of naturally occurring compounds derived from the juice of the poppy Papaver somniferum. Morphine is the classic opiate derivative used widely in medicine; heroin (diacetylmorphine) is a well-known, highly addictive street narcotic. The term opioids refers to these and other derivatives of naturally occurring opium (eg, morphine, heroin, codeine, and hydrocodone) as well as new, totally synthetic opiate analogs (eg, fentanyl, butorphanol, meperidine, and methadone [Table II–43]). A wide variety of prescription medications contain opioids, often in combination with aspirin or acetaminophen. Dextromethorphan (See Dextromethorphan) is an opioid derivative with potent antitussive but no analgesic or addictive properties. Tramadol (Ultram) is an analgesic that is unrelated chemically to the opiates but acts on mu-opioid receptors and blocks serotonin reuptake. Butorphanol is available as a nasal spray with rapid absorption. Buprenorphine is a partial opioid agonist that is approved for treatment of opioid addiction. Suboxone is a sublingual tablet containing buprenorphine plus naloxone to reduce intravenous abuse. Tapentadol (Nucynta) is a new mu-opioid agonist that also inhibits the reuptake of norepinephrine.
Drug | Type of Activity | Usual Adult Dosea (mg) | Elimination Half-life (h) | Duration of Analgesia (h) |
---|---|---|---|---|
Buprenorphine | Agonistb | 2–8 | 20–70 | 24–48 |
Butorphanol | Mixed | 2 | 5–6 | 3–4 |
Codeine | Agonist | 60 | 2–4 | 4–6 |
Fentanyl | Agonist | 0.2 | 1–5 | 0.5–2 |
Heroinc | Agonist | 4 | N/Ac | 3–4 |
Hydrocodone | Agonist | 5 | 3–4 | 4–8 |
Hydromorphone | Agonist | 1.5 | 1–4 |