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)

Fifty-five women with primary dysmenorrhea were enrolled in a study which each took ibuprofen (400 mg), propoxyphene hydrochloride (64 mg), or a placebo alternately in consecutive menstrual cycles for relief of pain. Fifty-one completed the study during three successive cycles in this triple-blind, crossover, randomized investigation. Ibuprofen was clearly superior to propoxyphene and the placebo in patient preference, degree of relief, and need for supplementary analgesics. In addition, a significantly greater number of patients were able to pursue their normal daily functions during the ibuprofen cycle. Propoxyphene was superior to the placebo but not to the same extent as ibuprofen. Only three side effects were reported during the study, two relative to propoxyphene and one recorded during a placebo cycle. These data show that ibuprofen is an effective agent when used for treatment of dysmenorrhea without organic etiology.
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PMID:Analgesic efficacy of ibuprofen for treatment of primary dysmenorrhea. 699 7

A double-blind randomized clinical trial was conducted in eighty-seven patients with mild, moderate or severe dental surgery pain to evaluate the analgesic activity of a single dose of the following compounds: (i) ibuprofen 400 mg, (ii) ACC-30 (a compound containing ASA 375 mg; codeine phosphate 30 mg; caffeine citrate 30 mg), (iii) placebo. Ibuprofen was significantly better than ACC-30 and placebo on almost all pain intensity, degree of relief and duration of analgesia parameters. ACC-30 was not significantly different from placebo on any analgesic measurement. No serious side-effects were reported with any of the study medications.
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PMID:A double-blind comparison of ibuprofen, ASA-codeine-caffeine compound and placebo in the treatment of dental surgery pain. 702 Dec 62

The chemistry, pharmacokinetics, pharmacology, clinical efficacy, adverse effects, physical dependence and tolerance, drug interactions, dosing, and cost of zomepirac sodium (Zomax, McNeil) are reviewed. Zomepirac is a new nonsteroidal anti-inflammatory agent (NSAIA) approved for the treatment of mild to moderately severe pain. The drug is well absorbed when given orally. It undergoes extensive biotransformation in the liver. Zomepirac shares the pharmacology of the other NSAIAs by decreasing prostaglandin synthesis. The efficacy of zomepirac has been demonstrated primarily in acute forms of pain with associated inflammatory processes including postdental-extraction, postpartum, and postoperative pain. Many of these studies have been single-dose evaluations. Zomepirac sodium 100 mg has been reported to be approximately equivalent to one to two tablets of aspirin-phenacetin-caffeine (APC) with codeine 30 mg. In two studies, zomepirac sodium 100 mg compared favorably with morphine sulfate 8 and 16 mg i.m. It has been shown to be superior to aspirin 650 mg in oral-surgery patients. In osteoarthritis, daily doses of zomepirac sodium 400-600 mg are approximately equivalent to aspirin 3200-4800 mg. Zomepirac has side effects similar to high-dose aspirin. Zomepirac is associated with an increased incidence of urogenital symptoms such as dysuria and pyuria. Because of tumorigenicity in rats, the drug is contraindicated in children, pregnant women, and nursing mothers. The drug has not demonstrated any potential for physical dependence, withdrawal, or tolerance. Zomepirac may provide a suitable alternative to aspirin, narcotic/NSAIA combinations, and narcotics in the treatment of mild to moderately severe pain. It is unlikely that zomepirac will replace narcotics in more severe types of pain.
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PMID:Evaluation of zomepirac sodium. 702 15

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

The acute behavioral cardiopulmonary and pharmacokinetic effects of propoxyphene hydrochloride were studied in seven adult horses. Each horse was given three different dosages of propoxyphene (0.5, 1.0, 2.2 mg/kg) IV. Fourteen days was allotted between each drug administration. The lower IV dosages of propoxyphene (0.5, 1.0 mg/kg) resulted in no changes in indices of cardiopulmonary function. Four horses demonstrated a transient period of muscle fasciculations when given 0.5 mg of propoxyphene/kg. Horses given 1.0 mg/kg demonstrated a brief period of euphoria, ataxia, and muscle fasciculations followed by a period of increased motor activity lasting for approximately 30 minutes. Horses given 2.2 mg of propoxyphene/kg demonstrated significant (P less than 0.05) increases in heart rate and arterial blood pressure and, after a brief period of ataxia and disorientation, displayed increased motor and locomotor activity lasting several hours. These behavioral effects were less apparent in three of four horses 4 hours after their appearance by the IV administration of naloxone. Propoxyphene exhibited a dose dependent half-life of from 61 to 135 minutes and an apparent volume of distribution of from 2.54 to 4.26 L/kg. Total body clearance was 21.9-28.4 ml/min/kg. In the adult pain-free horse, propoxyphene causes dose dependent excitatory effects similar to the narcotic analgesics.
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PMID:Cardiopulmonary, behavioral, and pharmacokinetic effects of propoxyphene in horses. 740 76

Hemorrhoids are a common source of anorectal symptoms, which are determined by their size. A helpful measure in small hemorrhoids is a high-fiber diet; in moderate lesions, ligature therapy is effective. Surgery should be reserved for large hemorrhoids. Anal fissures, probably caused by trauma to the anal canal during defecation, may persist because of a cycle of hard stools, pain, and reflex spasm. A high-fiber diet and sitz baths relieve acute fissures. Lateral partial internal sphincterotomy is usually effective when they become chronic. Perianal abscess is often caused by acute infection of the anal glands; fistula is the result of chronic infection. Swelling and induration may be present. Pain is throbbing and continuous, and perianal examination may require use of an anesthetic. Incision and drainage with follow-up to ensure resolution of infection is required. Pruritus ani may result from several contributing conditions or may be idiopathic. Restoration of dry, intact perianal skin is the treatment goal. Patients should be taught gentle hygiene and drying methods and advised to avoid caffeine or other dietary items that seem to exacerbate symptoms. Condylomata acuminata cause bleeding and pain if allowed to progress. Biopsy should be considered in patients at risk of dysplasia. Repeated application of caustic topical agents may help small lesions. Large, extensive, and persistent lesions require surgical ablation.
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PMID:Anorectal disorders. Five common causes of pain, itching, and bleeding. 747 60

Sumatriptan is a potent and selective agonist at a vascular serotonin1 (5-hydroxytryptamine1; 5-HT1) receptor subtype (similar to 5-HT1D) and is used in acute treatment of migraine and cluster headache. Following administration of sumatriptan 100mg orally, relief of migraine headache (at 2 hours) was achieved in 50 to 67% of patients compared with 10 to 31% with placebo in controlled clinical trials. In a comparative study, oral administration of sumatriptan 100mg consistently achieved significantly greater response rates than a fixed combination of ergotamine 2mg plus caffeine 200mg during 3 consecutive migraine attacks (66 vs 48% for first attack). Oral sumatriptan 100mg was also more effective than aspirin 900mg plus metoclopramide 10mg orally in a similar study. In the majority of controlled clinical trials, headache relief (at 1 hour after administration) was achieved in 70 to 80% of patients with migraine receiving sumatriptan 6mg subcutaneously compared with 18 to 26% of placebo recipients. Approximately 40% of patients who initially responded to oral or subcutaneous sumatriptan experienced recurrence of their headache, usually within 24 hours, but the majority of these patients responded well to a further dose of sumatriptan. Patients with cluster headache were treated for acute attacks with sumatriptan 6mg subcutaneously or placebo in 2 crossover trials. Headache relief was achieved within 15 minutes in 74 and 75% of patients receiving sumatriptan in these studies compared with 26 and 35%, respectively, with placebo. Patients receiving sumatriptan 12mg had a similar response rate as those receiving 6mg, but the higher dose was associated with an increased incidence of adverse events. Based on extensive safety data pooled from controlled clinical trials, sumatriptan is generally well tolerated and most adverse events are transient. The most frequently reported adverse events following oral administration include nausea, vomiting, malaise, fatigue and dizziness. Injection site reactions (minor pain and redness of brief duration) occur in approximately 40% of patients receiving subcutaneous sumatriptan, although the incidence appears to be markedly reduced when patients self-administer the drug with an auto-injector. Chest symptoms (mainly tightness and pressure) occur in 3 to 5% of sumatriptan recipients, but have not been associated with myocardial ischaemia except in a few isolated cases. Sumatriptan is contraindicated in patients with ischaemic heart disease, angina pectoris including Prinzmetal (variant) angina, previous myocardial infarction and uncontrolled hypertension, but is not contraindicated in patients with migraine and asthma. Data from long term studies in acute treatment of migraine and cluster headache suggest that sumatriptan remains effective and well tolerated over several months.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Sumatriptan. A reappraisal of its pharmacology and therapeutic efficacy in the acute treatment of migraine and cluster headache. 751 61

To investigate the interaction at the spinal level of endogenously released substance P with the effects of endogenously released adenosine, extracellular single-unit activity was recorded from dorsal horn neurons in the anesthetized cat. Vibration to the skin inhibited on-going activity of nociceptive neurons; 20 mg/kg caffeine reversibly blocked this inhibition, indicating mediation via adenosine receptors. In half of the cases, this inhibition was potentiated by iontophoretic application of substance P. High-intensity electrical stimulation to a sensory nerve produced excitation which was blocked by an NK-1 (substance P) receptor antagonist, implicating an endogenous neurokinin. When electrical stimulation preceded the vibrational stimulus, the inhibitory effect of vibration was potentiated. Thus, we suggest that endogenous substance P may potentiate the inhibitory response to endogenous adenosine. The results have important implications for integration of inputs from different sensory modalities, especially as they relate to nociception and pain.
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PMID:Substance P released endogenously by high-intensity sensory stimulation potentiates purinergic inhibition of nociceptive dorsal horn neurons induced by peripheral vibration. 752 99

It has been reported that the lipid soluble, anti-inflammatory drug triclosan, which is currently used in toothpastes and mouthrinses, may reduce pain. This may be an aspect of the anti-inflammatory effect of triclosan, which probably reduces the production of prostaglandin PGE2. However, triclosan may also exhibit a direct analgesic effect through an effect on excitable membranes. The aim of the present study was to examine the possible effect of triclosan on the nerve action potential, on the neuromuscular transmission and on the excitation-contraction coupling of skeletal muscle. Phrenic nerve-hemidiaphragm preparations, as well as isolated phrenic nerves, were dissected from Wistar albino rats and mounted by standard methods in Tyrode solution. Both during indirect and direct stimulation, the preparations were irreversibly inhibited by triclosan at concentrations higher than 5.0 x 10(-6)M. At low concentrations, the inhibition of the twitches during indirect stimulation and of the compound action potential was probably caused by a threshold increase for excitation of the phrenic nerve. At high concentrations, an additional inhibitory effect at the neuromuscular junction was disclosed. The directly stimulated preparation was also probably inhibited by an increase of the threshold for initiation of the muscle action potentials. In addition, a reduced KCl contracture and an acceleration of the caffeine contracture indicated an interaction with the sarcolemma. These results suggest that the analgesic effect of triclosan may be due to a direct interaction with excitable membranes.
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PMID:Effects of triclosan on the rat phrenic nerve-diaphragm preparation. 756 Feb 30

The present study examined antinociception produced by systemic administration of caffeine in the rat hot-plate (HP) and formalin tests and addressed several aspects of the mechanism of action of caffeine. Locomotor activity was monitored throughout. Caffeine produced a dose-related antinociception the HP (50-100 mg/kg) and formalin tests (12.5-75 mg/kg). When observed during the formalin test, caffeine stimulated locomotor activity between 12.5 and 50 mg/kg; this was followed by a depression in activity at 75 mg/kg. Caffeine did not produce an anti-inflammatory effect as determined by hindpaw plethysmometry, suggesting that antinociception was not secondary to an anti-inflammatory action. Peripheral co-administration of caffeine with the formalin did not produce antinociception, suggesting a predominant central rather than peripheral site of action for caffeine. Naloxone (10 mg/kg) did not reduce the antinociceptive or locomotor stimulant effects of caffeine, suggesting a lack of involvement of endogenous opioids in these actions. Phentolamine (5 mg/kg) enhanced antinociception by caffeine in both the HP and formalin tests, but inhibited locomotor stimulation. Prazosin (0.15 mg/kg) mimicked the action of phentolamine on locomotor stimulation, but idazoxan (0.5 mg/kg) mimicked the action of phentolamine on antinociception in the formalin test. These observations suggest an involvement of different alpha-adrenergic receptors in the two actions of phentolamine. Microinjection of 6-hydroxydopamine (6-OHDA) into the locus coeruleus, which depleted noradrenaline (NA) in the spinal cord and forebrain, inhibited the action of caffeine in the HP test. This was mimicked by intrathecal 6-OHDA which depleted NA in the spinal cord, but not by microinjection of 6-OHDA into the dorsal bundle which depleted NA in the forebrain. These results suggest an integral involvement of noradrenergic mechanisms in the antinociceptive action of caffeine in the HP and formalin tests and in locomotor stimulation, but the nature of this involvement differs for the 3 end points.
Pain 1995 May
PMID:Caffeine antinociception in the rat hot-plate and formalin tests and locomotor stimulation: involvement of noradrenergic mechanisms. 765 30


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