Clinical pharmacology of opioids for pain Journal Article
| Author: | Inturrisi, C. E. |
| Article Title: | Clinical pharmacology of opioids for pain |
| Abstract: | The pharmacological effects of the opioid analgesics are derived from their complex interactions with three opioid receptor types (μ, δ, and κ; morphine is an agonist at the μ opioid receptor). These receptors are found in the periphery, at presynaptic and postsynaptic sites in the spinal cord dorsal horn, and in the brain stem, thalamus, and cortex, in what constitutes the ascending pain transmission system, as well as structures that comprise a descending inhibitory system that modulates pain at the level of the spinal cord. The cellular effects of opioids include a decrease in presynaptic transmitter release, hyperpolarization of postsynaptic elements, and disinhibition. The endogenous opioid peptides are part of an endogenous pain modulatory system. A number of opioids are available for clinical use, including morphine, hydromorphone, levorphanol, oxymorphone, methadone, meperidine, oxycodone, and fentanyl, and their advantages and disadvantages for the management of pain are discussed. An understanding of the pharmacokinetic properties, as well as issues related to opioid rotation, tolerance, dependence, and addiction are essential aspects of the clinical pharmacology of opioids for pain. |
| Keywords: | drug tolerability; mortality; review; unindexed drug; pain; classification; opiate; brain cortex; withdrawal syndrome; neuromodulation; physiology; risk assessment; drug receptor binding; chronic disease; narcotic analgesic agent; pethidine; paracetamol; comorbidity; psychological rating scale; psychiatric status rating scales; drug bioavailability; methadone; morphine; drug half life; analgesics, opioid; opioid-related disorders; psychosis; hydromorphone; morphine sulfate; levomepromazine; drug tolerance; euphoria; brain stem; mu opiate receptor; phenytoin; drug induced disease; carbamazepine; fentanyl; opiate receptor; gabapentin; levorphanol; oxycodone; opiate addiction; opioid receptor; dexamphetamine; codeine; oxymorphone; caffeine; amitriptyline; pentazocine; analgesic; desipramine; thalamus; neurotransmission; buprenorphine; neurotransmitter release; spinal cord dorsal horn; nalbuphine; nortriptyline; kappa opiate receptor; hydroxyzine; imipramine; psychotic disorders; opioid rotation; receptors, opioid; hyperpolarization; endogenous opioid; humans; human; priority journal; article; dihydromorphine; support, u.s. gov't, p.h.s.; postsynaptic membrane; morphinelike agonist; butorphanol tartrate; nomorphan; nubain n; oramorph sr; oxy ir; sigma opiate receptor; presynaptic membrane; substance withdrawal syndrome |
| Journal Title: | Clinical Journal of Pain |
| Volume: | 18 |
| Issue: | 4 Suppl. |
| ISSN: | 0749-8047 |
| Publisher: | Lippincott Williams & Wilkins |
| Date Published: | 2002-07-01 |
| Start Page: | S3 |
| End Page: | S13 |
| Language: | English |
| DOI: | 10.1097/00002508-200207001-00002 |
| PUBMED: | 12479250 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Export Date: 14 November 2014 -- Source: Scopus |
