Opioid analgesic: Difference between revisions
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# Morphine | # Morphine | ||
Revision as of 08:20, 22 December 2008
Opioid analgesics, also called narcotics, are drugs usually used for treating pain. Opiod analgesics are defined as "all of the natural and semisynthetic alkaloid derivatives from opium, their pharmacologically similar synthetic surrogates, as well as all other compounds whose opioid-like actions are blocked by the nonselective opioid receptor antagonist naloxone.[1]
Pharmacology
There a several opioid receptors. All are are G-protein-coupled cell surface receptors.
- Mu receptors are responsible for analgesia.
- Delta
- Kappa
Available opioid analgesics
Current opioid analgesics are:[2]
- 18,19-dihydroetorphine
- Alfentanil
- Alphaprodine
- beta-casomorphins
- Buprenorphine
- Butorphanol
- carfentanil
- Codeine
- deltorphin I, Ala(2)-
- dermorphin
- Dextromoramide
- Dextropropoxyphene
- dezocine
- dihydrocodeine
- Dihydromorphine
- Diphenoxylate
- dynorphin (1-13)
- endomorphin 1
- endomorphin 2
- Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
- Enkephalin, D-Penicillamine (2,5)-
- enkephalin-Met, Ala(2)-
- eseroline
- Ethylketocyclazocine
- Ethylmorphine
- Etorphine
- Fentanyl
- Heroin
- Hydrocodone
- Hydromorphone
- ketobemidone
- Levorphanol
- lofentanil
- Meperidine
- Meptazinol
- Methadone
- Methadyl Acetate
- Morphine
- Nalbuphine
- nocistatin
- Opiate Alkaloids
- Opium
- Oxycodone
- Oxymorphone
- paracymethadol
- Pentazocine
- Phenazocine
- Phenoperidine
- Pirinitramide
- Promedol
- protopine
- remifentanil
- Sufentanil
- Tilidine
- Tramadol
- tyrosyl-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-phenylalanyl-phenylalanine
Effectiveness
Narcotics are commonly prescribed for pain, and their usage may be increasing.[3] In emergency rooms, non-Hispanic white patients are more likely to receive narcotics than patients of other ethnicities.[3]
Narcotics are effective for both short (1-16 weeks)[4] and long-term (6-24 months) use[5].
Narcotics, with long-term use, 80% of patients may have drug toxicity, most commonly gastrointestinal. In addition, substrance abuse and "aberrant medication-taking behaviors" may occur.[6] Advice for the treatment of acute pain among patients on chronic methadone is available.[7]
Adverse effects
Constipation
Constipation may be reduced by methylnaltrexone, a mu-opioid receptor antagonist. In a randomized controlled trial, 48% of patients receiving methylnaltrexone had a bowel movement compared to 15% of patients received placebo (number needed to treat = 3.0. Click here to adjust these results for patients at higher or lower risk.)[8] Although mu-receptors provide analgesia, methylnaltrexone is a charged quaternary amine so that it does not well cross the blood-brain barrier.
References
- ↑ Katzung, Bertram G. (2006). Basic and clinical pharmacology. New York: McGraw-Hill Medical Publishing Division, 512. ISBN 0-07-145153-6.
- ↑ Anonymous (2024), Opioid analgesics (English). Medical Subject Headings. U.S. National Library of Medicine.
- ↑ 3.0 3.1 Pletcher MJ, Kertesz SG, Kohn MA, Gonzales R (2008). "Trends in opioid prescribing by race/ethnicity for patients seeking care in US emergency departments". JAMA 299 (1): 70–8. DOI:10.1001/jama.2007.64. PMID 18167408. Research Blogging.
- ↑ Furlan AD, Sandoval JA, Mailis-Gagnon A, Tunks E (2006). "Opioids for chronic noncancer pain: a meta-analysis of effectiveness and side effects". CMAJ 174 (11): 1589–94. DOI:10.1503/cmaj.051528. PMID 16717269. Research Blogging.
- ↑ Kalso E, Edwards JE, Moore RA, McQuay HJ (2004). "Opioids in chronic non-cancer pain: systematic review of efficacy and safety". Pain 112 (3): 372–80. DOI:10.1016/j.pain.2004.09.019. PMID 15561393. Research Blogging.
- ↑ Martell BA, O'Connor PG, Kerns RD, et al (2007). "Systematic review: opioid treatment for chronic back pain: prevalence, efficacy, and association with addiction". Ann. Intern. Med. 146 (2): 116–27. PMID 17227935. [e]
- ↑ Alford DP, Compton P, Samet JH (2006). "Acute pain management for patients receiving maintenance methadone or buprenorphine therapy". Ann. Intern. Med. 144 (2): 127–34. PMID 16418412. [e]
- ↑ Thomas J, Karver S, Cooney GA, Chamberlain BH, Watt CK, Slatkin NE, Stambler N, Kremer AB, Israel RJ. Methylnaltrexone for opioid-induced constipation in advanced illness. N Engl J Med. 2008 May 29;358(22):2332-43. PMID 18509120