Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Intraperitoneal injection of zymosan in mice induced rapid extravasation and accumulation of plasma protein in the peritoneal cavity. Neutrophils began to appear in the peritoneal cavity after a lag period of approximately 3 hours. The injected mice exhibited a pain response (writhing) during the first 30 minutes after injection, but writhing ceased before protein or cell accumulation had reached maximum levels. The injection of zymosan induced synthesis of PGE2 (measured by RIA) which reached maximum levels at 30 minutes, then declined slowly. Peptido-leukotriene levels (detected by bioassay, RIA and HPLC) increased rapidly after injection, reached a peak within an hour of injection and declined to undetectable levels within 4 hours. The early peptido-LT was predominantly LTC4, while later, LTE4 was the major component. LTD4 levels remained low throughout and no LTB4 was detected at any time. Indomethacin treatment elevated levels of peptido-LTs, reduced PGE2 levels and inhibited writhing. Phenidone reduced peptido-LT levels. In vitro studies demonstrated that zymosan stimulates LTC4 synthesis by peritoneal cells whereas LTE4, LTD4, LTB4 or monoHETES were not detectable (using HPLC methods). The source of enzymes responsible for the in vivo metabolism of LTC4 to LTD4 and LTE4 could not be identified.
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PMID:Intraperitoneal injection of zymosan in mice induces pain, inflammation and the synthesis of peptidoleukotrienes and prostaglandin E2. 300 31

In experimental cholecystitis there is a net fluid secretion into the gallbladder lumen and an increased release of prostaglandins. Indomethacin and opiates are known to inhibit this mucosal fluid secretion. Intraluminal or intra-arterial administration of prostaglandin E2 reduces basal gallbladder fluid absorption or induces a net fluid secretion to the lumen and also contracts the normal gallbladder. The use of a continuous perfusion technique in anaesthetized cats in this study shows that the effects of prostaglandin E2 on gallbladder function are blocked by intravenous morphine and loperamide. Naloxone does not affect the gallbladder responses to PGE2 administration. As a mechanism of action it is suggested that opiates inhibit secretory and contractile nerves that are activated by prostaglandins in the gallbladder wall. The findings suggest that the pain relieving effects of opiates in cholecystitis and biliary pain partly are due to blocking of the effects by prostaglandins on gallbladder function.
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PMID:The influence of morphine, loperamide and naloxone on gallbladder response to prostaglandin E2 in the anaesthetized cat. 346 26

An attempt is made to compile the pharmacological data on the leading non-steroidal anti-inflammatory drugs. They concern the pharmacodynamics, the pharmacokinetics and the unwanted effects of these compounds. From these data a few suggestions for rational use are made: Ibuprofen and diclofenac present as drugs with short and reliable elimination-halflife. The compound with the lower potency namely ibuprofen appears particularly suitable for use in patients suffering from mild inflammatory pain of probably short duration (hours, days). Diclofenac being more potent should be used in more serious painful conditions, the variable bioavailability and the sometimes delayed absorption of diclofenac should be kept in mind if success is not achieved. Ketoprofen may have similar characteristics as diclofenac. The quality of the available data is however limited. Indomethacin and piroxicam are highly potent and reliable in onset; the bioavailability amounts to 100%. Both compounds may owe their effectiveness and reliability to substantial enterohepatic recirculation which may also be responsible for the reported somewhat higher incidence of GI-tract problems in connection with their use. They should hence be used in serious conditions going along with intensive, long-lasting inflammatory pain. Naproxen being less potent than the later two may fall into the same category.
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PMID:[Pharmacologic characteristics as the basis for differential therapy using non-steroidal anti-inflammatory agents]. 359 Oct 20

For the purpose of investigating the clinical efficacy of a newly designed wedged insole, 149 patients with medial osteoarthritis of the knee were followed from one year to five years and five months. A rating system for pain, walking ability, and both were used for evaluation of the clinical results. Comparing two groups consisting of 107 patients with early radiographic stages (Stage I or II), 67 patients (Group I) treated with both a wedged insole and anodyne (Indomethacin 600 mg/day) showed a significantly greater improvement than 40 patients (Group II) treated with anodyne alone. Analyzing the therapeutic efficacy of the wedged insole according to the radiographic stage, the prescription of a wedged insole was significantly more effective for patients with mild osteoarthritis (Stages I, II, and III), and ineffective for those with advanced osteoarthritis (Stage IV). The wedged insole, designed on the basis of an established hypothesis, represents an excellent means of conservative treatment for early medial osteoarthritis of the knee.
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PMID:Clinical evaluation of the treatment of osteoarthritic knees using a newly designed wedged insole. 360 98

Leukotriene D4 (LTD4) increased the blood flow rate in human skin, equipotent to histamine in the dose range of 3.1-200 pmol. The vasodilatation lasted for up to 60 min, and no late reactions occurred. Indomethacin did not affect the LTD4-induced blood flow rate. H1 and H2 antagonists reduced the increase in blood flow rate, but did not abolish the response to LTD4. Local nerve block inhibited the axon reflex-mediated flare component of the LTD4-induced blood flow rate, leaving a local red reaction. This local red reaction was not affected by H1 and H2 antagonists. These results indicate histamine as a mediator of the axon reflex, and show that LTD4 causes a direct vasodilatory effect that is not mediated via histamine or cyclooxygenase products. The laser-Doppler flowmeter was applied for dynamic studies of the vasopressor response in the skin during a Valsalva maneuver, and the relative changes in blood flow were confirmed by control estimates of the blood flow rate by a 133xenon washout method. The pressor response to a Valsalva maneuver was reversed by local nerve block, but not affected by LTD4. Therefore LTD4 did not interfere with the sympathetic activity on the cutaneous vessels. Leukotriene D4 caused a dose-dependent wheal reaction, equipotent to histamine in the dose range of 0.2-200 pmol. Only minor whealing occurred when the vasculature to the test arm was occluded before injection of LTD4 and the circulation restored 30 min later. Most of the LTD4 was apparently metabolized within this period. Subsequent injections of LTD4 into the same sites demonstrated the development of tachyphylaxis with respect to whealing. This evidence suggests that LTD4 cannot mediate sustained inflammation. The injections of LTD4 caused neither pain nor itching. In conclusion, the elucidated properties point to LTD4 as a possible mediator of microvascular changes during acute inflammation.
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PMID:Vascular effects of leukotriene D4 in human skin. 380 52

The influence of total hip replacement (THR) on pain and use of analgesics was evaluated in 511 patients with McKee-Farrar and Brunswik prostheses. The mean age of the patients was 63.8 years and the mean follow-up time 4.2 years. The average grade of pain decreased from 1.8 to 4.9 as evaluated according to Charnley. The proportion of regular users of all analgesics decreased from 75% to 17% (P less than 0.001). Indomethacin was the most common preoperative drug and the proportion of its regular use decreased from 47 to 12% (P less than 0.001). The preoperative association which existed between the grade of pain and the regular drug users in each pain grade decreased more than expected by the preoperative figures. Postoperatively those with previous hip operations, McKee-Farrar prosthesis, one hip replaced, reapplications and removal of the prosthesis gave inferior results with respect to pain than those without previous surgery, with Brunswik prosthesis, both hips replaced and with the original prosthesis in situ. In addition to previous THR operations, type of the hip prosthesis, bilateral or unilateral surgery, primary or secondary coxarthrosis and reapplication of the prosthesis influenced the use of drugs. THR, however, brought a marked drop in the use of analgesics and this effect should be taken into account when assessing the costs and benefits of THR.
Pain 1985 Sep
PMID:The influence of total hip replacement on hip pain and the use of analgesics. 387 66

Indomethacin was recently shown to have a potent analgesic effect on biliary pain. The underlying mechanism is not fully clear, although reduction of increased gallbladder pressure by inhibition of prostaglandin synthesis had been suggested. For further clarification of this mechanism, the effect of intravenous indomethacin on the intraluminal gallbladder pressure was investigated in patients undergoing operation for acute cholecystitis. After laparotomy, gallbladder pressure was measured continuously during 25 min in 20 patients, 10 of whom received 100 mg indomethacin intravenously, while 10 were untreated controls. High intraluminal gallbladder pressure was found in all patients. Indomethacin reduced the average pressure by 11% in 20 min, whereas the corresponding pressure in the controls was constant. The results indicate that acute cholecystitis is associated with substantially raised intraluminal pressure, and that the analgesic action of indomethacin on biliary pain may be attributable to a local effect on gallbladder function, resulting in reduction of intraluminal pressure.
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PMID:Indomethacin reduces raised intraluminal gallbladder pressure in acute cholecystitis. 389 96

The present investigation was designed to study the effect of indomethacin (5 mg kg-1 day-1) on plasma fibrinogen levels in laparotomized rats. Whereas tissue injury significantly increased plasma fibrinogen when compared to normal uninjured rats, indomethacin completely blocked that effect. Conversely, indomethacin did not prevent fibrinogen increase in laparotomized rats injected with epinephrine, with spinal cord transection + epinephrine or with adrenal medullectomy + epinephrine. Indomethacin or epinephrine administration to normal rats did not modify plasma fibrinogen. Taking into account that epinephrine is a key hormone in plasma fibrinogen response in laparotomized rats, and according to our results, prostaglandins might act by two possible pathways: 1) by decreasing of the pain threshold of the sensory nerve endings and stimulating sympathetic adreno-medullar system; 2) by entering into the blood stream and enhancing epinephrine action on plasma fibrinogen. It would appear that indomethacin inhibits both pathways.
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PMID:Effects of indomethacin on plasma fibrinogen levels in rats with tissue injury. 402 61

Adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), adenosine, adenine and inosine were injected intradermally into the backs of human volunteers. ATP, ADP and AMP evoked weal and flare responses in the skin in a dose dependent manner. The rank order of potency was ATP greater than ADP greater than AMP; other metabolites were apparently inactive. The potency of ATP was approximately 0.002 times that of histamine. In the forearm, cross tachyphylaxis was demonstrated between ATP and histamine weals; also the flare due to injected ATP spread beyond a band which was applied to prevent diffusion, indicating that the flare is neurogenic. Injections of ATP and high doses of ADP produced a sensation of persistent pain, unlike histamine which produced transient pain or itch on some occasions, and saline which was without effect. The possible involvement of histamine, mast cells and prostaglandins in the response was examined. The inhibitory actions of systemic pretreatment with diphenhydramine suggests that the erythema and wealing responses to ATP are at least partly due to ATP-evoked histamine release. Indomethacin, doxantrazole and cimetidine did not alter the ATP reaction.
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PMID:Adenosine triphosphate-evoked vascular changes in human skin: mechanism of action. 617 40

The essential clinical features of eight cases of carotidynia are outlined. As little is known about treatment, the effectiveness was evaluated of drugs used in some specific forms of vascular headache with similar pain characteristics. Indomethacin or flurbiprofen were shown to be potent drugs in the treatment of carotidynia.
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PMID:Carotidynia: report of eight cases and prospective evaluation of therapy. 619 74


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