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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Four commercial gel preparations of topical anti-inflammatory agents have been assessed in six animal models commonly used to determine the biological activity of non-steroidal anti-inflammatory agents for systemic administration. Only UV-induced erythema of the skin, adjuvant induced arthritis and the measurement of vascular permeability proved suitable for differentiation of the potency of the four topical agents. Carrageenin-induced paw oedema, the cotton pellet test and the assessment of the pain threshold according to Randall and Selitto were of little value. The effects of the gel preparation of diclofenac (CAS 15307-86-5) diethylammonium (Voltaren Emulgel) were comparable to two preparations containing 1% and 5% active ingredient, respectively. Gel 4 showed low overall activity. The experiments demonstrated that some of the models used for the assessment of anti-inflammatory agent for systemic administration proved suitable for the testing of topical preparations and that percutaneous absorption was insufficient to elicit anti-inflammatory effect in the animals at sites remote from the site of application.
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PMID:Assessment of topical non-steroidal anti-inflammatory drugs in animal models. 229 49

In a single-blind random study, simultaneously carried out by five Pain Therapy and Palliative Care Centres, the analgesic power and side-effects of sodium naproxen (CAS 26159-34-2) and sodium diclofenac (CAS 15307-86-5) by mouth were compared in a group of 100 advanced cancer patients. The patients complained of somatic and/or visceral pain and were treated with non-steroid anti-inflammatories as required. The dose administered amounted to 550 mg every 12 h for sodium naproxen and to 100 mg every 12 h for sodium diclofenac. The study stressed the similar analgesic effect of the two drugs--pain intensity and duration decreased by half in the first week of treatment--and a comparatively low morbidity rate.
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PMID:Sodium naproxen versus sodium diclofenac in cancer pain control. 229 51

Sumatriptan (CAS 103628-46-2, Imigran) has established itself as an important therapeutic agent in the treatment of migraine. Although considerable understanding of, in particular, the vascular pathophysiology of migraine has been gained during the past decade, the pathophysiology and mediators involved in the pain experience during migraine ar during migraine are not yet fully explained. The mechanisms behind the pharmacological effects of sumatriptan are still only partially understood. In the present study the effects of sumatriptan on drug induced cerebral blood flow increases in the baboon model were investigated using 99mTc-HMPAO (hexamethylpropylene amine oxime) and SPECT (single photon emission computed tomography). Sumatriptan selectively reduced drug induced cerebral blood flow increases. The effects of halothane anaesthesia and acetazolamide on cerebral blood flow were not reversed by sumatriptan, while the effect of nimodipine was attenuated by 47% (to the level of cerebral blood flow below the normal flow baseline). These results support multiple mechanisms for sumatriptan involving vascular neurotransmission and neurogenic inflammatory responses via serotonin receptor stimulation and Ca2+ mobilization. Drug-drug interactions are further implicated through this study.
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PMID:Cerebral blood flow effects of sumatriptan in drug combinations in the baboon model. 748 11

The anti-inflammatory and analgesic profile of a new topical foam formulation of ketoprofen lysine salt (CAS 57469-78-0, Artrosilene Schiuma, KLS-foam) was characterized in comparison with marketed gel formulations containing KLS (KLS-gel) or diclofenac diethylammonium salt (DCF-gel). KLS-foam dose-dependently inhibited oedema formation and hyperalgesia induced by subplantar injection of carrageenan or substance P, being more potent than KLS-gel. At equieffective anti-inflammatory doses, KLS-foam provided a more pronounced analgesic effect than DCF-gel. KLS-foam also markedly inhibited exudate formation and prostaglandin production induced by subcutaneous implantation of carrageenan soaked sponges. In carrageenan induced paw inflammation, KLS-foam provided the same anti-inflammatory effect as orally administered KLS, but induced significantly less gastric damages. Oral administration of KLS resulted in sustained systemic absorption of ketoprofen, whereas after topical application of KLS-foam no appreciable ketoprofen plasma levels were detected. These data support the anti-inflammatory and particularly the analgesic effectiveness of the new foam formulation of KLS, a finding that, together with the high gastric tolerability, further emphasizes the usefulness of KLS-foam in the treatment of localized flogistic diseases and associated pain.
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PMID:Effects of a new foam formulation of ketoprofen lysine salt in experimental models of inflammation and hyperalgesia. 754 96

Acetylsalicylic acid (ASA, CAS 50-78-2) and ibuprofen (IB) are commonly used over-the-counter drugs for short-term treatment of pain of different origin. Ibuprofen lysinate (IBL, CAS 57469-76-8) is a water soluble form of ibuprofen for rapid absorption. This single blind, randomized, controlled study compared the incidence and severity of irritation of gastric and duodenal mucosa in normal healthy subjects (n = 45) following administration of IBL (Dolormin) 800 mg/d, ASA 2000 mg/d or placebo for 3 consecutive days. Gastric and duodenal mucosal injury were assessed endoscopically using a severity scale of 0-4 for mucosal erosions and mucosal hemorrhages. Mean gastric hemorrhage and erosion scores for ASA and IBL were significantly higher than those for placebo. In addition, ASA was found to be significantly more irritating to gastric mucosa than IBL, in both the incidence and severity of gastric erosions. No duodenal hemorrhages were detected in this study. The incidence of duodenal erosions was significantly higher in the ASA group (64%) than in both the IBL (6%) and placebo groups (0%) which were not significantly different. Only one subject (in the placebo group) reported an adverse experience (mild headache) during the study. The data suggest that both active treatments are more injurious to the gastric mucosa than placebo when given for 3 days to normal healthy volunteers, but that IBL 800 mg/d is significantly less injurious to the gastric and duodenal mucosa than ASA 2000 mg/d.
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PMID:Effects of ibuprofen lysinate and acetylsalicylic acid on gastric and duodenal mucosa. Randomized single-blind placebo-controlled endoscopic study in healthy volunteers. 794 19

In a randomized single-blind study carried out simultaneously in five Departments for Pain Therapy and Palliative Care, the analgesic efficacy and side effects of oral ketorolac (ketorolac tromethamine, Tora-Dol, CAS 74103-07-4) and diclofenac sodium were compared in a population of 100 advanced cancer patients suffering from somatic and/or visceral pain. The treatment was carried out in agreement with the first step of the WHO pharmacological strategy in cancer pain. The administered dosage was 10 mg every 6 h for ketorolac and 50 mg every 8 h for diclofenac sodium. The study showed the efficacy of both drugs in cancer pain. A greater number of keterolac patients could pass to the second WHO step later than diclofenac patients. As to the tolerability, both drugs turned out to be similar, except for "sleepiness", which was four times more frequent (p < 0.05) in the diclofenac group.
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PMID:Ketorolac versus diclofenac sodium in cancer pain. 801 Oct 10

Influence of Ranitidine and Famotidine on the Intragastric pH-profile in Healthy Volunteers/Randomised cross-over study of ranitidine effervescent tablets (300 mg) versus famotidine film coated tablets (40 mg). A controlled cross-over trial was carried out to compare the duration of time until the onset of action and its intensity following administration of ranitidine (R, Sostril, CAS 76824-35-6) effervescent tablets (300 mg) and famotidine (F, CAS 76824-35-6) film coated tablets (40 mg). Twelve volunteers (4 female, 8 male) participated in the study. The efficacy of the test medications was assessed by pH-metry during 12 h. The evaluation of the measurements showed that a pH-value 3.5 was reached 100 s after administration of R and 3,392 s (56.5 min) after F (p < 0.01). The median pH-values were significantly higher after R during the first 2 h. The AUC-values (area under the curve; pH-time) for 1, 2 and 4 h were calculated by the trapezoid rule. The intake of R resulted in significantly higher areas than that of F. After reaching the pH-value of 3.5 this value remained stable during the complete period of measurement (R = 12 h, F = 11 h). The faster onset of pH-value elevation could correspond clinically with a faster onset of pain relief.
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PMID:[The effect of ranitidine and famotidine on the intragastric pH profile of healthy subjects. Randomized cross-over trial with ranitidine effervescent tablets (300 mg) versus famotidine film tablets (40 mg) ]. 802 36

A series of aryl tropanyl esters and amides related to 1H-indole-3-carboxylic acid endo 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester (ICS 205930, CAS 89565-68-4) were synthesized and evaluated for antinociceptive activity using the hot-plate test. Of these, the benzofurane-3-carboxylic ester of tropine (1) was found powerfully to increase the pain threshold, with a cholinergic mechanism of action. Despite the structural similarity with ICS 205930, the analgesia induced by 1 seems not to be due to 5-HT3 receptor interaction, and there is evidence of involvement of the central 5-HT4 receptor.
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PMID:Synthesis and biological activity of a series of aryl tropanyl esters and amides chemically related to 1H-indole-3-carboxylic acid endo 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester. Development of a 5-HT4 agonist endowed with potent antinociceptive activity. 821 52

To investigate the combined analgesic and spasmolytic effect of metamizole (dipyrone, Novalgin, CAS 68-89-3) this drug was compared with an opioid analgesic (tramadol) and a pure spasmolytic drug (butylscopolamine). In a multicentre, observer-blind, parallel-group study conducted in five German centres 74 patients suffering from "severe" or "excruciating" colic pain caused by a calculus in the bile duct were randomized to receive intravenously 2.5 g metamizole (25 patients), 100 mg tramadol (25 patients), or 20 mg butylscopolamine (24 patients). The three treatment groups were homogeneous for age, sex, height, weight and baseline pain intensity. Metamizole was significantly more effective in reducing pain than tramadol and butylscopolamine for the primary endpoint, pain intensity on a visual analogue scale (VAS) when evaluated as the area under the curve (AUC) from baseline to onset of analgesic action (p < 0.05) and the sum of pain intensity differences (SPID) for the observation period of 2 h (p < 0.005). The mean time until the onset of analgesic action occurred was shortest (p < 0.005) for metamizole (10.9 +/- 5.8 min) compared with tramadol (15.8 +/- 11.7 min) and butylscopolamine (25.6 +/- 24.3 min). Metamizole was also more effective for the secondary efficacy endpoint, pain intensity on a 5-point ordinal scale. In the patient's overall assessment of treatment efficacy at the end of the trial, metamizole was rated as the most effective drug (p < 0.005). Fewer patients in the metamizole (3) and the tramadol (1) groups than in the butylscopolamine group (8) needed a second injection of the "rescue" medication (p < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Observer-blind study with metamizole versus tramadol and butylscopolamine in acute biliary colic pain. 829 68

In a double-blind study, 198 patients experiencing recurrent herpes orofacialis were randomly assigned to treatment with either tromantadine hydrochloride (ViruMerz Serol, CAS 53783-83-8) or aciclovir. All patients performed an up to 5-day course of topical treatment beginning on average within 2 h after the first signs of recurrence. The herpes efflorescences and symptoms were assessed daily by the same physician for 14 days, except on weekends, and by the patients each day during the whole observation time. Rapid healing was achieved with both medications. Efficacy was assessed by rating the course of vesicle eruptions, duration until beginning of incrustation and the clinical course of the symptoms (burning, tension, pain). Equivalence between the medication groups was shown by comparative analysis of all evaluation criteria. The global efficacy and tolerability of both medications was rated by the physician as well as by the patients as "good" or "very good" in more than 80% of the cases. The results of this trial show equivalence of both medications in the treatment of recurrent herpes orofacialis, and confirm the good dermal tolerability of the drugs.
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PMID:Efficacy of tromantadine and aciclovir in the topical treatment of recurrent herpes orofacialis. Comparison in a clinical trial. 849 82


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