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)

443C81 is a synthetic enkephalin thought to act on peripheral opiate receptors. The analgesic, central, cardiovascular and endocrine effects of two i.v. doses of 443C81 were investigated in 12 healthy male volunteers. Its effects were compared with those of placebo and the classical opiate dipipanone given orally using a double dummy design. 443C81 produced dose-related analgesia; dipipanone 10 mg had a greater effect than the high dose 443C81. In contrast to dipipanone, 443C81 did not cause significant miosis or reduce minute volume on rebreathing CO2 and there was no evidence of sedation. Dry mouth was reported frequently and associated with reduced salivation after all active treatments. Both 443C81 and dipipanone increased circulating prolactin and growth hormone and reduced cortisol levels. This novel enkephalin appears to possess analgesic activity and some other properties of opiates but is devoid of clinically relevant narcotic effects.
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PMID:Analgesic, central, cardiovascular and endocrine effects of the enkephalin analogue Tyr-D.Arg-Gly-Phe(4NO2)-Pro-NH2 (443C81) in healthy volunteers. 197 Dec 16

Conditions in which antidepressants have been used include diabetic neuropathy, postherpetic neuralgia, headaches, arthritis, chronic back pain, cancer, thalamic pain, facial pain, and phantom limb pain. Although much of the available information is derived from inadequately controlled trials, it seems that antidepressants provide analgesia in many of these disorders. The analgesic effects tend to be independent of antidepressant effects, and doses of heterocyclic antidepressants used for analgesia seem to be lower than those considered effective in the treatment of depression. Doses should be started low and gradually increased until the patient reaches the highest tolerable dose. Onset of analgesia is variable, ranging from 1 day to 10 weeks. Common side effects include dry mouth, drowsiness, urinary retention, orthostatic hypotension, and constipation. Optimum dosages and schedules have not been established.
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PMID:Antidepressants in the management of chronic pain syndromes. 214 20

The pharmacological properties of centrally acting alpha2-receptor agonists such as clonidine suggest a potentially important role as ideal adjuvants for anesthesia since they produce sedation, analgesia anxiolysis, xerostomia and cardiovascular stability without respiratory depression, development of tolerance or addiction liability. Further clinical experience with this exciting development will undoubtedly establish the ultimate role and optimal use of alpha2 -receptor agonists in anesthetic practice. Beta-blockage can result in significant bradycardia, atrial ventricular conduction problems, bronchospasm and left ventricular contractile dysfunction. Thus, the use of long-acting beta-blockers is of limited value in the perioperative period. Esmolol, because of its ultrashort action, cardioselective properties and titratability, has been shown to be safe and effective for the treatment of tachycardia and hypertension. Doses from 50 to 300 micrograms/kg/min for up to 7 hours in the perioperative period have been shown to cause no apparent cumulative effect. It has been used in the treatment of asthmatic patients with tachycardia and hypertension without significant increases in airway resistance. Studies using esmolol during general anesthesia have demonstrated no significant interaction with several anesthetic regimens.
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PMID:Clinical pharmacology of alpha2-agonist and beta-adrenergic blocker. 257 80

Fifty-six surgical patients self-administered i.v. narcotic analgesics to combat postoperative pain. Analgesic demand per h was 2.7 +/- 1.1 mg of morphine, 26 +/- 10 mg of pethidine or 2.3 +/- 0.8 mg of ketobemidone, which reflects the equianalgesic ratios. Acute respiratory depression was seen in two hypovolaemic patients as evidenced by a raised PaCO2 on air breathing. Carbon dioxide retention disappeared upon correction of hypovolaemia. Late respiratory complications of short duration were encountered in 13%. Drowsiness and dry mouth were the most frequent complaints. Self-administered analgesia was considered highly satisfactory by the patients.
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PMID:Patient-controlled analgesic therapy: clinical experience. 612 76

Metkephamid is an analog of methionine enkephalin. The efficacy, safety, and time course of analgesia with 70 or 140 mg metkephamid were compared with those of 100 mg meperidine and placebo in 59 hospitalized women with severe postpartum episiotomy pain. There were two separate trials with single intramuscular doses and identical designs, including parallel groups, randomized blocks, and double-blind conditions. Using subjective reports as indexes of response, patients rated pain intensity, pain relief, and side effects at periodic interviews for 6 hr. Almost all measures of summed and peak analgesia exhibited important differences among the three treatments in both trials. Metkephamid at the 140-mg dose was the most effective and meperidine, 100 mg, was next, whereas metkephamid, 70 mg, and placebo were least effective. Only metkephamid, 140 mg, and meperidine were measurably superior to placebo. Both treatments took effect within 30 min and peaked at 1 to 2 hr; with 140 mg metkephamid, maximum analgesia was sustained 6 hr, i.e., 2 hr longer than with meperidine. Metkephamid, 70 mg, could not be distinguished from placebo throughout its entire time course. Although dizziness was experienced with meperidine, the two metkephamid doses induced other side effects, including sensation of heavy limbs, dry mouth, eye redness, and nasal stuffiness. None were distressing. Our results suggest that 140 mg metkephamid compares favorably with 100 mg meperidine for analgesia after episiotomy, but it induces minor side effects more frequently.
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PMID:Metkephamid and meperidine analgesia after episiotomy. 687 19

Temgesic Injection (buprenorphine), a potent analgesic agent, was given to 240 patients under 18 years of age during a year of monitored release. All but four had the product for the management of moderate or severe pain in the immediate post-operative period. Analgesia was reported as adequate or good in 90% of these young patients when it was assessed 2 and 4 hours after infection. There were no reports of side-effects commonly associated with strong analgesics and particularly antagonist-analgesics such as confusion, hallucination, blurred vision, dry mouth and lightheadedness. There were no serious respiratory or cardiovascular effects. The incidences of other events did not differ from those recorded in the much larger adult population of almost 8,000 patients. Buprenorphine is an effective analgesic suitable for use in the young post-operative patient.
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PMID:The monitored release of buprenorphine: results in the young. 737 72

We have studied 40 children aged 6-14 yr undergoing abdominal surgery under general anaesthesia with extradural block; they were allocated randomly to receive transdermal hyoscine (loading dose 140 micrograms, followed by 5 micrograms h-1) or placebo for the duration of postoperative analgesia with PCA morphine. There was a significant (P < 0.001) reduction in the incidence of postoperative nausea and vomiting in the treated group compared with the placebo group during the first 48 h after operation. The treated group also had a significantly increased incidence of sedation (P < 0.02) and dry mouth (P < 0.01).
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PMID:Prevention of postoperative nausea and vomiting with transdermal hyoscine in children using patient-controlled analgesia. 811 May 56

Efficacy and safety of a PCA protocol, without loading dose or background infusion, was investigated in 40 consenting patients after osteotomy of the foot. All patients had intrathecal lidocaine 5% 1.8 ml preoperatively. Postoperative pain relief was provided with morphine from a Baxter Travenol infusor with PC module. The morphine concentration was 2 mg/ml or 3 mg/ml. In order to reach the analgesic blood concentration as quickly as possible, the patients were instructed to start PCA from the very first moment pain occurred. The patients breathed room air. The nursing staff evaluated respiratory and cardiovascular parameters, pain and side effects. Although mean VAS scores were higher than 3 in the early postoperative phase, no supplementary analgesics were required. One patient had urine retention. One patient had a drop in blood pressure at the start of morphine, which was quickly restored with the administration of colloids. Oxygen saturations were lower (SpO2 < 95%) the first hours postoperatively, especially at the first assessment where no morphine was administered. Pain or relative hypovolaemia could be an explanation. Dry mouth and sleepiness were the most frequently reported side-effects, followed by dizziness, vomiting and nausea. Sweating and itching were less frequently reported. The occurrence of the side effects was the highest during the first postoperative day. We conclude that even when morphine is used in PCA without loading dose or background infusion after opiate-free locoregional analgesia, close monitoring is necessary for at least 5 hours.
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PMID:Evaluation of morphine for patient controlled analgesia with the Infusor system after opiate-free locoregional anesthesia for osteotomy of the foot. 866 16

The pharmacology, pharmacokinetics, efficacy, adverse effects, and dosage and administration of tramadol are reviewed. Tramadol is a synthetic analogue of codeine that binds to mu opiate receptors and inhibits norepinephrine and serotonin reuptake. It is rapidly and extensively absorbed after oral doses and is metabolized in the liver. Analgesia begins within one hour and starts to peak in two hours. In patients with moderate postoperative pain, i.v. or i.m. tramadol is roughly equal in efficacy to meperidine or morphine; for severe acute pain, tramadol is less effective than morphine. Oral tramadol can also be effective after certain types of surgery. Tramadol and meperidine are equally effective in postoperative patient-controlled analgesia. In epidural administration for pain after abdominal surgery, tramadol is more effective than bupivacaine but less effective than morphine. In patients with ureteral calculi, both dipyrone and butylscopolamine are more effective than tramadol. For labor pain, i.m. tramadol works as well as meperidine and is less likely to cause neonatal respiratory depression. Oral tramadol is as effective as codeine for acute dental pain. In several types of severe or refractory cancer pain, tramadol is effective, but less so than morphine; for other types of chronic pain, such as low-back pain, oral tramadol works as well as acetaminophen-codeine. Common adverse effects of tramadol include dizziness, nausea, dry mouth, and sedation. The abuse potential seems low. The recommended oral dosage is 50-100 mg every four to six hours. Tramadol is an effective, if expensive, alternative to other analgesics in some clinical situations.
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PMID:Tramadol: a new centrally acting analgesic. 907 93

This article presents a summary of drug safety data concerning the use of tramadol hydrochloride and an outline of the specific aspects of this analgesic in particular with regard to respiratory depression and dependence potential. Information from phase II to IV clinical studies, postmarketing surveillance studies (covering safety data from a total of more than 21,000 patients) and the spontaneous reporting system have been taken into consideration. The data from the spontaneous reporting system covers the period between 1977 and 1993, during which more than one billion single dose units were distributed throughout the world. The phase II to IV studies compare acute intravenous, acute intramuscular, acute oral and multiple dose oral administration Postmarketing surveillance studies provide a picture of everyday use of tramadol in general medical practice. Further analyses were performed to provide information about the gender-, age- and dose-related distribution of adverse reactions The prevalence of side effects was calculated by comparing the number of symptoms with the number of patients. The pooled data from the clinical studies and the postmarketing surveillance studies reveal that the most commonly observed side effects were nausea, dizziness, drowsiness, tiredness, sweating, vomiting and dry mouth, with an overall incidence of between 1 and 6%. In the postmarketing surveillance studies on long term and acute administration, the profile of adverse events was qualitatively almost identical to that in the phase II to IV studies. However, there were distinct quantitative differences it favour of the long term studies. In the postmarketing surveillance study on acute parenteral administration, the incidences of nausea and vomiting were only 4.2 and 0.5% respectively, which is significantly lower than the 20.7 and 11.4% in the patient-controlled analgesia studies. Nevertheless, it is important to take into consideration the different conditions in these studies. All the postmarketing surveillance studies were outpatient studies, whereas almost all of the phase II to IV studies were carried out in hospitals. The studies with intravenous and intramuscular administration were mainly postoperative, which explains the relatively high incidence of nausea and vomiting, 17.8 and 7.0%, respectively, with intramuscular administration. The different conditions in the phase II to IV studies and the postmarketing surveillance studies are also reflected in the occurrence of dizziness and postural hypotension: The incidence of dizziness in the postmarketing surveillance studies is slightly higher than that observed in the phase II to IV studies. Particularly in the studies with intravenous and intramuscular administration, the patients were confined to bed and were therefore much less sensitive to dizziness than those in the long term oral and postmarketing surveillance studies, who were all outpatients. On the other hand, postural hypotension played almost no role in the multiple dose studies, in which the oral formulation were used most frequently. It is interesting to note that diarrhoea, pruritus and gastrointestinal disorder (except nausea and vomiting) are mainly reported in the multiple dose studies in the groups receiving oral tramadol, and also in the postmarketing surveillance studies. Once again, the study conditions may well be the explanation. The adverse effects reported in both clinical and postmarketing surveillance studies are similar to those in the spontaneous reports. The most frequently documented adverse effects in clinical and postmarketing surveillance studies, i.e. nausea/vomiting, dizziness, drowsiness, tiredness, sweating and dry mouth, are noted very infrequently in spontaneous reports, since in medical practice these side effects are usually known and are described in the product information. Almost all reports referring to abuse/dependence are connected with pain therapy; they give no reason to suspect any pro
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PMID:[Tolerance and safety of tramadol use. Results of international studies and data from drug surveillance]. 919 Mar 25


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