Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Substance P(SP), the heptapeptide SP and the stable analogue (p-Glu5-MePhe8-MeGly9) SP (DiMe-C7) induce a Ca2+-dependent release of Met5-enkephalin (MET) from slices of periaqueductal gray matter (PAG) and striatum of rats. The MET release from striatal slices is greater than that from PAG slices because of the higher MET content of striatum. Intraventricular injection of SP and of the two related peptides induce analgesia in the rat, and their analgesic potency is in line with their capacity to release MET. Other neuropeptides which possess antinociceptive activity such as bombesin, neurotensin, vasopressin and somatostatin fail to release MET from PAG slices.
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PMID:Substance P-induced release of Met5-enkephalin from striatal and periaqueductal gray slices. 619 90

Opioid analgesia, the selective suppression of pain without effects on other sensations, also distinguishes between different types of pain: severe, persistent pain is potently inhibited by opioids, but they fail to cohceal the sensation of a pinprick. The cellular basis for this specificity was analyzed by means of patch-clamp experiments performed on fluorescently labeled nociceptive neurons (nociceptors) that innervate rat tooth pulp. Activation of the mu opioid receptor inhibited calcium channels on almost all small nociceptors but had minimal effect on large nociceptors. Somatostatin had the opposite specificity, preferentially inhibiting calcium channels on the large cells. Because persistent pain is mediated by slow-conducting, small nociceptors, opioids are thus likely to inhibit neurotransmitter release only at those primary synapses specialized for persistent pain.
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PMID:Selective opioid inhibition of small nociceptive neurons. 748 26

Recent research has demonstrated the increasing importance of the spinal cord in processing and modulating nociceptive input. Different groups of drugs, each acting by a unique mechanism, have been shown to block nociceptive afferent transmission. None of the currently available spinally administered local anesthetics, opioids or non-opioids produce analgesia without side effects. Non-opioids such as alpha-2-adrenergic agonists may be more suited as adjuvants rather than sole analgesic agents and their main role lies in reducing the dose requirements of other analgesics. Spinal somatostatin and ketamine may have neurotoxic potential. The role of these drugs and of midazolam in pain management appears to be limited. Preliminary results suggest that the neuropeptide octreotide has potent analgesic effects. 'Balanced spinal analgesia' using a combination of low doses of drugs, with separate but synergistic mechanisms of analgesia, may produce the best results. The optimal drug combinations and dosages remain to be determined. It is essential that animal neurotoxicity studies followed by controlled clinical trials are performed before widespread spinal administration of new drugs.
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PMID:Spinal antinociception: clinical aspects. 763 24

We have studied the analgesic effects of somatostatin during surgery and its influence on the plasma glucose levels and the liver enzyme profile in 40 ASA 1 or 2 patients undergoing surgery for carcinoma of the gastrointestinal tract. Each patient received either somatostatin bolus 3.5 micrograms.kg-1 intravenously plus an infusion of somatostatin 3.5 micrograms.kg-1.h-1, or sodium chloride 0.9% as a placebo in a double-blind manner. Anaesthesia was induced with propofol 1 mg.kg-1 followed by a continuous infusion of propofol in a stepwise declining regimen. Vecuronium was used for muscular relaxation. Fentanyl 100 micrograms was administered intravenously in bolus doses for analgesia during surgery as required. Blood samples were taken at 10 min pre-induction, 5 min postintubation, 5, 30, 60, 120 min postincision and 30 min post-recovery for plasma glucose levels. Blood samples were also taken at 10 min pre-induction, 120 min postincision and 24 h postoperatively for liver enzymes. The total requirement for fentanyl in the control group was significantly higher (p < 0.001) than in the group that received somatostatin. Eight out of 20 patients in the study group required no additional analgesia intra-operatively. The changes in blood glucose values followed the same pattern in both groups. There was a tendency for liver enzymes to increase in both groups. Although this increase was less in the study group, this change was not statistically significant.
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PMID:Somatostatin and total intravenous anaesthesia. Assessment of analgesic requirements during surgery and the effects on liver enzymes. 765 56

Somatostatin 1-14, a natural occurring neuropeptide (Somiaton), has been reported to have analgesic effects in humans in different painful conditions. The aim of the present study was to investigate if epidural somatostatin produced clinical analgesia to postoperative pain after upper abdominal surgery. In a randomized double-blind controlled study, 40 patients received either 125 micrograms of epidural somatostatin infusions every hour (using a continuous infusion pump: CADD-PCA model 5200 PCX, Pharmacia) or placebo: mannitol (somatostatin inactif ingredient) 2.5 mg during the first 3 postoperative days (plus additional pulses of either substance, 250 micrograms or 5 mg, respectively, according to the level of analgesia needed by the patient). Additional subcutaneous analgesic treatment with 1 mg/kg pethidine chlorhydrate was administered at the patient's request. The degree of pain was quantified with visual analogue scale at baseline, 1 h after the operation and at every 4 h for the next 3 days. Arterial blood gases and spirometry values were determined at different intervals throughout the study period. Somatostatin was significantly better than placebo for pain relief (P < 0.01) and respiratory function preservation (P < 0.05). The total consumption (and ranges) of somatostatin at 24, 48 and 72 h were: 5.2 +/- 1.4 mg (4.0-6.25 mg), 4.2 +/- 0.8 mg (2.2-5.0 mg) and 3.7 +/- 0.4 mg (2.2-4.7 mg) respectively. During the whole study the need for complementary analgesia (pethidine chlorhydrate) was significantly higher in the placebo group: 5.4 +/- 3.5 vs. 2.7 +/- 1.9 (mean +/- SD) P < 0.01, dose/72 h. Side effects were irrelevant and scarce in both groups. The sustained pain relief combined with the respiratory function preservation in the somatostatin group suggests an important role of this drug in postoperative analgesia.
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PMID:Epidural somatostatin as an analgesic in upper abdominal surgery: a double-blind study. 865 41

Amongst the spinal peptide candidates believed to be involved in the mediation of analgesia, only somatostatin fulfills the criterium of a real analgesia substance. Spinal somatostatin specifically blocks the transmission of painful stimuli. Spinal calcitonin may lower the opioid dose requirement in patients with bone metastases but it fails to relieve acute pain. The usefulness of ACTH and CRF for treatment of pain remains to be established. The role of CCK-8, vasopressin and neurotensin is unclear. The contradictory findings on antinociception using simple rodent withdrawal reflex tests (e.g. the tail flick test), or more complex behavioral tests in which supraspinal sensory processing is involved, (e.g. the hot plate test), indicate that these tests are inappropriate when neuropeptides are employed. Furthermore, due to their inability to predict analgesia in humans, they do not fulfill the guidelines proposed by the IASP that animal test procedures have to be for the benefit of humans.
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PMID:Non-opioid peptides for analgesia. 831 62

Somatostatin is distributed in the substantia gelatinosa in the dorsal horn of the spinal cord, and its application has been found to produce an inhibitory effect on nociceptive neurons. Although intraspinal administration of somatostatin-14 produces pain relief in patients with cancer and in postoperative patients, its short half-life limits its clinical usefulness. Octreotide, a synthetic analog of somatostatin, is more stable and not been associated with neurodegenerative changes when administered intrathecally in dogs. Intrathecal octreotide provides analgesia without adverse drug effects when administered chronically for cancer pain; however, treatment periods have been limited. This article describes the 5-year clinical course of two patients receiving intrathecal octreotide for severe, intractable nonmalignant pain. Included in this description are the results of blinded, randomized "N of 1" trials conducted in each of these patients.
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PMID:Intrathecal octreotide for relief of intractable nonmalignant pain: 5-year experience with two cases. 874 73

The purpose of this study was to verify the role of somatostatin (Som) of brain in analgesia of electroacupuncture (EA). Intracerebroventricular (icv) injection of Som caused a more marked elevation of pain threshold and of EA analgesic effect, but the activity of Ca(2+)-APTase in hippocampus was significantly decreased; The Som and GABA levels in hippocampus and brain stem were decreased by EA analgesia. The Som in hippocampus and brain stem were obviously depleted by icv injection of cycteamine, but without any change of pain threshold and analgesic effect of EA. These results indicated that the exogenous Som of brain potentiated the analgesic effect of EA, however, the decrease of endogenous of some brain regions took part in the process of EA analgesia.
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PMID:[Effect of brain somatostatin on electroacupuncture analgesia of rat]. 875 23

After suffering some setbacks since its introduction in 1967, stimulation of the spinal and peripheral nervous systems has undergone rapid development in the last ten years. Based on principles enunciated in the Gate Control Hypothesis that was published in 1968, stimulation-produced analgesia [SPA] has been subjected to intensive laboratory and clinical investigation. Historically, most new clinical ideas in medicine have tended to follow a three-tiered course. Initial enthusiasm gives way to a reappraisal of the treatment or modality as side-effects or unanticipated problems arise. The last and third phase proceeds at a more measured pace as the treatment is refined by experience. This review is divided into three parts as it traces the progress of spinal cord stimulation [SCS] and peripheral nerve stimulation [PNS]. The review commences with a discussion of the theory of SCS and PNS, and is followed by early reports during which it became apparent that the modality is essentially only effective in the treatment of neuropathic pain. The last section describes the modern experience including efficacy in specific types of pain and concludes with recent accomplishments that dramatize the relief of pain which can be achieved in nonoperable peripheral vascular disease or myocardial ischemia. Over the years, a search for those transmitters that might be influenced by spinal cord stimulation focused on somatostatin, cholecystokinin (CCK), vasoactive intestinal polypeptide (VIP), neurotensin and other amines, although only substance "P" was implicated. More recently, in animal studies, evidence that GABA-ergic systems are affected may explain the frequent successful suppression of allodynia that follows spinal cord stimulation. During the past eight years, much attention has been directed to studies that use a chronic neuropathic pain model. While PNS held significant promise as a pain relieving modality, early electrode systems and their surgical implantation yielded variable results due to evolving technical and surgical skills. These results dramatically reduced the continued development of PNS, which then gave way to a preoccupation with SCS. Modern development of SCS with outcome studies, particularly in relation to failed back surgery syndrome [FBSS] and the outcome of peripheral nerve surgery for chronic regional pain syndromes, has earned both modalities a place in the ongoing management of patients with intractable neuropathic pain. The last section, dealing with pain of peripheral vascular and myocardial ischemia, is perhaps one of the more exciting developments in stimulation produced analgesia and as the papers discussed demonstrate, can provide a level of analgesia and efficacy that is unattainable by other treatment modalities. SCS and PNS has an important role to play in the management of conditions that are otherwise refractory to conservative or other conventional management.
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PMID:Stimulation of the central and peripheral nervous system for the control of pain. 901 59

Certain types of cancer pain fail to respond well either to systemic drug therapy or to spinal opioids because of the occurrence of intolerable adverse effects. In addition to spinal opioids other drugs may produce an antinociceptive effect when administered by the spinal route, such as local anesthetics, NSAID, alpha 2-agonists, calcium-channel blockers, NMDA antagonists, cholinergic drugs, peptides such as somatostatin, octreotide or calcitonin, adenosine agonists, benzodiazepines, neurokinin and cholecystokinin antagonists, nitric oxide synthase inhibitors, corticosteroids, and enkephalinase inhibitors. All these drugs may be administered in combination between them, realising the so called balanced spinal analgesia. The aim of this study is to analyse: the available methods for the evaluation of pharmacological interactions, the types of interaction between different spinal antinociceptive drugs and the role of balanced spinal analgesia in the treatment of cancer pain. Analysis of the presented data shows that the spinal synergism between opioids-local anesthetics and opioids-alpha 2-agonists can be useful in the treatment of opioid refractory cancer pain. Furthermore, the use of cholinergic drugs combined with opioids and alpha 2-agonists may be promising. Finally, even if the synergism between NSAID or NMDA antagonists with opioids or alpha 2-agonists have been proved, at the moment their use in man by the spinal route is not advisable because of the absence of adequate studies on their neurotoxicity and adverse effects.
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PMID:[Balanced spinal analgesia in the treatment of oncologic pain. Review of the literature]. 910 86


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