Peripheral Opioid Analgesia: Mechanisms and Clinical Implications

Stein, Christoph; Cabot, Peter J.; Schäfer, Michael

doi:10.1017/cbo9780511575068.007

Cited by 14 publications

(21 citation statements)

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“…Many conventional opioid agonists have been shown to produce potent opioid receptor mediated analgesia when adminstered locally at small, systemically inactive doses into injured tissue of rodents and humans (75). Recent studies have confirmed these findings in nonhuman primates (31, 32).…”

Section: Analgesic Effects Of Exogenous Peripheral Opioid Agonistsmentioning

confidence: 92%

“…A large number of studies have shown that peripheral analgesic effects of exogenous opioids are enhanced under inflammatory conditions (61,75). One possible underlying mechanism is an upregulation, i. e., an increased number of receptors.…”

Section: Peripheral Opioid Receptors and Inflammationmentioning

confidence: 99%

“…About a decade ago, reports about the existence of opioid receptors outside the central nervous system and the generation of analgesia by these peripheral receptors began to accumulate (70). Such analgesic effects are particularly prominent in painful inflammatory conditions and have been demonstrated both in animals and in humans (75). Opioid receptors are present on peripheral sensory nerves and are upregulated during the development of inflammation.…”

Section: Introductionmentioning

confidence: 99%

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Peripheral analgesic and antiinflammatory effects of opioids

Stein¹,

Machelska²,

Schäfer³

2001

Zeitschrift f�r Rheumatologie

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Traditionally, opioids were considered the prototype of centrally acting analgesics. In the past decade a substantial literature has emerged demonstrating that opioids can produce potent and clinically measurable analgesia by activation of opioid receptors on peripheral terminals of primary sensory neurons. In addition, endogenous ligands of these peripheral receptors were discovered in immune cells. Major recent findings in peripheral opioid analgesia include the relative lack of tolerance under inflammatory conditions, tetrapeptides as novel peripherally restricted compounds, the potent antiinflammatory activity of mu- and kappa-agonists and the identification of selectins as important molecules governing the homing of opioid cells to injured tissue. In addition to the extensively documented efficacy of locally applied morphine in post-surgical pain, clinical studies have now moved into the field of chronic arthritic pain.

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Section: Analgesic Effects Of Exogenous Peripheral Opioid Agonistsmentioning

confidence: 92%

Section: Peripheral Opioid Receptors and Inflammationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Peripheral analgesic and antiinflammatory effects of opioids

Stein¹,

Machelska²,

Schäfer³

2001

Zeitschrift f�r Rheumatologie

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“…One approach employed to circumventing these side effects has been to identify peripherally restricted KOP ligands (Arendt-Nielsen et al 2009;Camilleri 2008;DeHaven-Hudkins and Dolle 2004;Floyd et al 2009;Vanderah et al 2008). The rationale for this approach was that peripherally restricted KOP agonists would be devoid of dysphoria, and sedation seen with centrally acting agents but analgesic efficacy would be maintained given that activation of peripheral KOP receptors also produces antinociception (Stein 1993;Stein et al 1999).…”

Section: Development Of Kop Receptor Agonists As Analgesicsmentioning

confidence: 99%

Kappa opioids and the modulation of pain

2010

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“…These receptors are located on the primary afferents, in the spinal cord, and in the brain. The peripheral receptors are mainly important when inflammation is present (Stein, 1993;Stein et al, 1999;Labuz et al, 2007;Trescot et al, 2008). The receptor is the most abundant in the spinal cord and is the main modulator of the pain system, although ␦ and receptors seem to play a role during, for example, sensitization (Minami and Satoh, 1995).…”

mentioning

confidence: 99%