Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0184567 (acute pain)
 3,962 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Zomepirac is an analgesic which is closely related chemically to the nonsteroidal anti-inflammatory agent, tolmetin. In short term studies mainly involving patients with acute pain of moderately severity, zomepirac was at least as effective as usual therapeutic doses of aspirin, codeine alone or with aspirin, phenacetin and caffeine, dextropropoxyphene with paracetamol, or orally administered pentazocine. Additionally, zomepirac may provide analgesia comparable to that with standard doses of intramuscular morphine in patients with acute pain of moderate intensity, but in severe pain states strong analgesics may be more appropriate. Zomepirac has also been studied in patients with chronic orthopaedic pain or osteoarthritic pain for up to several months, without the need for increased doses. It appears to be at least as effective as usual doses of aspirin when used in this way, with a lower incidence of some side effects such as gastrointestinal disturbances and hearing disorders. Preliminary studies suggest that zomepirac may also be effective in patients with chronic cancer pain who have not been previously maintained on strong analgesics, but further experience is needed to clarify its usefulness in this difficult treatment area.
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PMID:Zomepirac: a review of its pharmacological properties and analgesic efficacy. 704 54

A 27-year-old woman developed acute pain, pallor and feeling of cold in her left arm. She had been a smoker of 15-20 cigarettes daily since the age of 15 years, but had not previously had any serious illness. In addition to contraceptives she had had been taking one to several suppositories containing caffeine and ergotamine tartrate (2 mg) daily against migraine. Angiological examination 5 days after onset of symptoms discovered a weak brachial pulse low in the left upper arm, while ulnar and radial pulses were absent. All other pulses were normally palpable. Colour duplex sonography demonstrated occlusion of the brachial artery which angiographically was due to a 5 cm severe narrowing without thrombus, blood flowing distally via collaterals. No improvement was achieved by local injection of 100,000 IU urokinase, 0.5 mg nitroglycerin, 20 mg tolazoline and a 3-hour infusion of alprostadil. On infusion of 560 ml hydroxyethylstarch over 8 hours, 400 mg naftidrofuryl, therapeutic doses of heparin and abstinence from ergotamine (since admission) the vessel diameter increased by 50% within 23 hours and after a further 24 hours to almost 100% of the comparable arterial segment of the right arm while merely on heparin infusion.
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PMID:[Acute ischemia of an arm as an unusual manifestation of ergotism]. 795 78

Adenosine is released from metabolically active cells by facilitated diffusion, and is generated extracellularly by degradation of released ATP. It is a potent biological mediator that modulates the activity of numerous cell types, including various neuronal populations, platelets, neutrophils and mast cells, and smooth muscle cells in bronchi and vasculature. Most of these effects help to protect cells and tissues during stress conditions such as ischaemia. Adenosine mediates its effects through four receptor subtypes: the A1, A2a, A2b and A3 receptors. The A2a receptor (A2aR) is abundant in basal ganglia, vasculature and platelets, and stimulates adenylyl cyclase. It is a major target of caffeine, the most widely used psychoactive drug. Here we investigate the role of the A2a receptor by disrupting the gene in mice. We found that A2aR-knockout (A2aR-/-) mice were viable and bred normally. Their exploratory activity was reduced, whereas caffeine, which normally stimulates exploratory behaviour, became a depressant of exploratory activity. Knockout animals scored higher in anxiety tests, and male mice were much more aggressive towards intruders. The response of A2aR-/- mice to acute pain stimuli was slower. Blood pressure and heart rate were increased, as well as platelet aggregation. The specific A2a agonist CGS 21680 lost its biological activity in all systems tested.
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PMID:Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2a receptor. 926 92

This case report presents a 44-year-old woman with severe arterial ischemia leading to claudicatio and acute pain in rest caused by an ergotism. In the history was an abuse of suppositories containing caffeine and ergotamine induced by chronic headache. The initial angiography showed occlusions of the femoral arteries. After excluding other vascular diseases, intraarterial infusions of prostaglandin E were administered. Additionally, physiotherapeutic treatment followed. An progrediency of the symptoms made a epidural catheter for sympathicolysis and treatment of the acute pain necessary. As the results of this intervention were encouraging, a sympathetic blockade with injection of 96% ethanol at the level of L 2/3 and 3/4 was performed. After treatment, the clinical symptoms and the blood flow measured by Doppler ultrasonography normalised. A final angiography demonstrated a now normal arterial status. Ergotism, indication and methods of sympathetic blockades are discussed.
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PMID:[Normalization of the vascular picture with sympathetic block in severe arterial ischemia from ergotism]. 1054 98

The antinociceptive, anti-inflammatory and gastric effects of trimetazidine (2,3,4-trimethoxybenzyl-piperazine dihydrochloride), a novel anti-ischaemic compound, were evaluated in various animal models. In acute pain models, namely acetic acid-induced writhing, hot-plate assay, tail electric stimulation test, capsaicin-induced pain and the formalin test, trimetazidine (1.8-7.2 mg/kg, i.p.) showed marked antinociceptive effects. Trimetazidine did not produce any behavioural impairment as revealed by the mouse rotarod. The inhibition of writhing response by trimetazidine was reduced by yohimbine, theophylline (and to a certain extent by sulpiride) but not by prazosin, guanethidine, naloxone, atropine, propranolol, haloperidol, domperidone, clozapine, glibenclamide or caffeine. The carrageenan-evoked acute paw oedema was reduced by 19.2-21.2 and 17-18.6% by 3.6 and 7.2 mg/kg trimetazidine, respectively. The drug did not alter the oedema-suppressive effect of indomethacin or dexamethasone, but reduced that of rofecoxib. Trimetazidine at 7.2 mg/kg reduced immobility time in Porsolt's forced-swimming test by 28.9%. The acute gastric mucosal lesions evoked by indomethacin in the rat were inhibited in a dose-dependent manner by co-administration of trimetazidine. In anesthetized rats, trimetazidine potentiated the gastric acid secretory response. This study indicates that trimetazidine possesses antinociceptive and gastric protective properties. The antinociceptive properties of trimetazidine are likely to be centrally mediated, but do not involve opioid pathways.
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PMID:Pharmacological investigation of trimetazidine in models of inflammation, pain and gastric injury in rodents. 1615 71

Acupuncture is now accepted as a complementary analgesic treatment. Auricular acupuncture is a distinct form of acupuncture. Electrical stimulation of acupoints (electroacupuncture) increases the effects of acupuncture. Recently, an auricular electroacupuncture device, the P-Stim, has become available. Clinical studies in outpatients have investigated the P-Stim in chronic musculoskeletal pain and its use for minor surgery. In chronic cervical or low back pain, auricular electroacupuncture was more effective than conventional auricular acupuncture. The results in acute pain were controversial. Auricular electroacupuncture reduced pain and remifentanil consumption during oocyte aspiration when compared with conventional auricular acupuncture or a sham treatment. However, after third molar tooth extraction, auricular electroacupuncture and auricular acupuncture failed to reduce either postoperative pain or analgesic consumption. Further large-scale studies are required to evaluate the analgesic efficacy of auricular electroacupuncture.
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PMID:P-Stim auricular electroacupuncture stimulation device for pain relief. 1718 68

Based on 19 studies (7,238 participants) a Cochrane review concludes that the addition of caffeine to an analgesic drug provides superior analgesia compared with the analgesic drug alone. The benefit is small, with a number needed to treat of approx. 16. The use of analgesics containing caffeine is associated with an increased risk of the development of physical dependence, overuse headache, and withdrawal symptoms upon abrupt discontinuation. Combination analgesics with caffeine should only be used temporarily and exclusively for the treatment of acute pain conditions.
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PMID:[Caffeine as adjuvant analgeticum for treating acute pain]. 2462 15

Reflex-based procedures are important measures in preclinical pain studies that evaluate stimulated behaviors. These procedures, however, are insufficient to capture the complexity of the pain experience, which is often associated with the depression of several innate behaviors. While recent studies have made efforts to evidence the suppression of some positively motivated behaviors in certain pain models, they are still far from being routinely used as readouts for analgesic screening. Here, we characterized and compared the effect of the analgesic ibuprofen (Ibu) and the stimulant, caffeine, in assays of acute pain-stimulated and pain-depressed behavior. Intraperitoneal injection of acetic acid (AA) served as a noxious stimulus to stimulate a writhing response or depress saccharin preference and locomotor activity (LMA) in mice. AA injection caused the maximum number of writhes between 5 and 20 minutes after administration, and writhing almost disappeared 1 hour later. AA-treated mice showed signs of depression-like behaviors after writhing resolution, as evidenced by reduced locomotion and saccharin preference for at least 4 and 6 hours, respectively. Depression-like behaviors resolved within 24 hours after AA administration. A dose of Ibu (40 mg/kg) - inactive to reduce AA-induced abdominal writhing - administered before or after AA injection significantly reverted pain-induced saccharin preference deficit. The same dose of Ibu also significantly reverted the AA-depressed LMA, but only when it was administered after AA injection. Caffeine restored locomotion - but not saccharin preference - in AA-treated mice, thus suggesting that the reduction in saccharin preference - but not in locomotion - was specifically sensitive to analgesics. In conclusion, AA-induced acute pain attenuated saccharin preference and LMA beyond the resolution of writhing behavior, and the changes in the expression of hedonic behavior, such as sweet taste preference, can be used as a more sensitive and translational model to evaluate analgesics.
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PMID:Changes in saccharin preference behavior as a primary outcome to evaluate pain and analgesia in acetic acid-induced visceral pain in mice. 2650 5