The opioid peptide dimmer biphalin [(Tyr-D-Ala-Gly-Phe-NH-)(2)] has high potency both in vivo and in vitro. Its antinociceptive activity depends on the route of administration: the lowest potency is after subcutaneous, and the highest after intrathecal or inracerebroventricular administration. We tested the analgesic activity of biphalin in a wide range of doses after intrathecal administration...

UNLABELLED Over the past five years our pain practice encountered eight patients (5 female, 3 male) with chronic non-malignant pain syndromes, in whom any meaningful pain reduction via opioid analgesics (either by oral or systemic and/or intraspinal route) had resulted in profound nausea and/or vomiting despite generous use of available and/or affordable anti-emetics. After obtaining proper con...

Loperamide, a mu opioid receptor agonist, which is commonly used as an antidiarrhoeal agent has been reported to possess analgesic activity after intrathecal administration. However, the exact analgesic profile, i.e., onset, duration and intensity of analgesia in relation to morphine is not fully known. In the present study, the acute analgesic effect of loperamide (5 microg) was compared with ...

BACKGROUND Intrathecal morphine is commonly used for post caesarean analgesia. However, their use is frequently associated with the incidence of troublesome side effects such as nausea, vomiting and pruritus. Various mechanisms have been postulated for the opioid-induced pruritus, with a variety of medications with different mechanisms of actions formulated for the prevention and treatment. But...

OBJECTIVE To demonstrate the efficacy and safety of the addition of bupivacaine in restoring pain control and improving quality of life and activity level in patients with chronic nonmalignant pain refractory to intrathecal opioids. DESIGN Retrospective study. SETTING Outpatient clinics. PATIENTS Seventeen patients with inadequate pain relief while receiving intrathecal opioids alone. Int...

Chen, Shao-Rui and Hui-Lin Pan. Loss of TRPV1-expressing sensory neurons reduces spinal opioid receptors but paradoxically potentiates opioid analgesia. J Neurophysiol 95: 3086–3096, 2006. First published February 8, 2006; doi:10.1152/jn.01343.2005. Systemic administration of resiniferatoxin (RTX), an ultrapotent capsaicin analogue, removes transient receptor potential vanilloid type 1 (TRPV1)-...

BACKGROUND Neuropathic pain is associated with several sensory abnormalities, including allodynia as well as spontaneous pain. Opioid intake in neuropathic pain patients is motivated by alleviation of both pain and allodynia. However, laboratory animal studies rely almost exclusively on reflexive withdrawal measures of allodynia. The authors examined the pharmacology of self-regulated intake of...

BACKGROUND Despite decades of intense research efforts, actions of acute opioids are not fully understood. Increasing evidence suggests that in addition to well-documented antinociceptive effects opioids also produce paradoxical hyperalgesic and excitatory effects on neurons. However, most studies focus on the pronociceptive actions of chronic opioid exposure. Matrix metalloproteinase 9 (MMP-9)...

Pain is prevalent in advanced malignancies; however, some patients cannot get adequate pain relief by conservative routes of analgesic administration or experience serious side effects related to high dose of opioids. For those who have exhausted multimodal conservative analgesic, intrathecal drug delivery is an alternative intervention for truly effective pain management. The objective of this...