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)

Antacids are widely used in the management of duodenal ulcer but the optimum dose of antacid required for ulcer healing has not been determined. We therefore studied 107 patients with endoscopically diagnosed duodenal ulcer who were allotted at random to one of the following treatment groups; placebo (group P) and antacid (groups A, B and C). A liquid antacid (Aludrox MH, Wyeth) with neutralising capacity of 2.3 mmol HCl/ml was administered in graded doses of 7.5 ml (Group A), 15 ml (Group B), and 30 ml (Group C), one hour and three hours after each meal, six times a day for four weeks. Patients in group P received 15 ml liquid placebo in a similar fashion. Complete symptomatic relief was obtained in 33% of patients in the placebo group, 54% in antacid group A, 89% in group B, and 92% in group C. Endoscopic assessment at the end of four weeks of treatment gave an ulcer healing rate of 29% in the placebo group, 46% in group A (103.5 mmol antacid/day), 85% in group B (207 mmol/day), and 88% in group C (414 mmol/day). There was no significant difference in the healing rates and pain relief between placebo and antacid group A, while both groups B and C had significantly higher ulcer healing rates and pain relief compared with placebo (p less than 0.001) and antacid group A (p less than 0.01). Drug related unwanted effects were recorded only in group C - 28% of patients suffered from diarrhoea. It is concluded that the optimum antacid requirements for the treatment of duodenal ulcer is 90 ml (acid neutralising capacity, 207 mmol HCl) per day.
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PMID:Controlled therapeutic trial to determine the optimum dose of antacids in duodenal ulcer. 638 73

Two local anesthetics, Duranest 1% (etidocaine HCl) and Sensorcaine 0.5% (bupivacaine HCl), were tested against each other in dose-related blocks of the fifth ray. This study was conducted under double-blind cross-over conditions using 24 healthy volunteers. It was found that 4 ml. of either agent was sufficient to anesthetize the fifth ray area in all but 4.2% of the injections and 8 ml. of etidocaine always accomplished complete fifth ray anesthesia. Also, 4 ml. of etidocaine was found to have a more rapid onset and longer duration than the same volume of bupivacaine, 6.3 vs. 8.3 min. onset, and 487 vs. 449 min. duration, respectively. Pain and burning upon injection of either bupivacaine or etidocaine was encountered in 70% of the subjects tested. Residual pain was noted in some of the subjects given etidocaine after complete resolution of sensory anesthesia. Residual pain was not noted in any of the subjects given bupivacaine. Etidocaine was found to have a more rapid onset and a longer duration than bupivacaine or a lidocaine-bupivacaine mixture, and was thus found to be a superior agent in the subjects tested.
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PMID:A double-blind crossover study comparing two doses of Duranest (etidocaine) 1% with a fixed dose of Sensorcaine (bupivacaine) 0.5% utilizing infiltration regional blocks of the fifth ray. 652 Mar 49

Methadone is a potent, long acting narcotic analgesic which can be orally administered due to its almost complete bioavailability. There is a growing interest in the rectal route of administration in the case of acute post-operative or chronic malignant pain. Since virtually no data were available on the rectal absorption profile of methadone in man, plasma concentrations of methadone were determined by means of HPLC analysis after a single dose of 10 mg methadone HCl in a cross-over pilot study in five volunteers. The rectal dosage forms included aqueous solutions and fatty suppositories. A comparison was made with an orally administered solution. Compared with oral dosing, the extent of rectal absorption from an aqueous solution was almost 80% up to 8 h after dosing. Although the mean peak concentration and the AUC0-8h was significantly lower (p less than 0.01), no marked difference in tmax was observed: 2.8 and 3.1 h respectively. Rectal absorption conditions of methadone from fatty suppositories (3 ml) were found to be less favourable. The peak plasma concentration was only reached 3-4 h after administration, whereas the relative bioavailability up to 8 h after dosing ranged from 35-58%. This rate-limiting absorption pattern may be due to the critical solubility properties of methadone HCl at physiological pH.
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PMID:Preliminary study on the absorption profile after rectal and oral administration of methadone in human volunteers. 654 62

Long acting local anesthetics have been used successfully during third molar extractions and endodontic procedures. They were shown to provide longer duration of anesthesia and contribute to less postoperative pain. This study evaluated the effectiveness of one long acting local anesthetic agent (etidocaine) for periodontal flap procedures. A double-blind, split mouth design treated 17 matched contralateral pairs of posterior sextants. One region was treated following administration of 1.5% etidocaine HCl with 1:200,000 epinephrine. The matched control region was treated following administration of 2% lidocaine with 1:100,000 epinephrine. The results indicate that, while etidocaine provided a longer duration of anesthesia (P less than 0.005), no difference was noted in the number of pain pills patients took or the period of time over which they took them. Inadequate hemostasis was a recurrent problem with etidocaine anesthesia. The use of 1.5% etidocaine HCl with 1:200,000, epinephrine offers no significant advantages over traditional anesthetic solutions.
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PMID:Etidocaine HCl local anesthetic for periodontal flap surgery. 658 93

The cyanide antidote 4-dimethylaminophenol . HCl (DMAP) was administered orally, i.v., or i.m. to man and dog. Ferrihemoglobin formation and changes of several parameters in human blood were investigated to obtain information on damage to liver, kidney, muscle, and red blood cells; in addition, the metabolism of DMAP was studied. In dogs, the initial rate of ferrihemoglobin production (DMAP, 3.25 mg/kg i.v. or i.m., 15 mg/kg orally) amounted to 28%, 3.5%, and 2% of the total hemoglobin per min; the corresponding values for man were 9%, 2%, and 2% per min. The dogs behaved normally while CPK increased after i.m. injection. In man, only i.m. injection of DMAP (3.25 mg/kg) was followed by increases in LDH, GOT, and CPK of 110, 260, and 490%, resp.; while total bilirubin, conjugated bilirubin, and iron concentration rose by 270, 120, and 50%, respectively. Bilirubin and iron concentration increased also after DMAP i.v. (3.25 mg/kg) or when it was taken orally (600 or 900 mg). The lactate concentration was not influenced while the pyruvate concentration increased by 50%. DMAP produced hemolysis in vitro. Generally, the values determined in vivo approached the starting level within 1 week. Intramuscular injection of DMAP induced reversible subjective and objective symptoms, e.g., local pain, swollen buttock, fever reaction. The urine showed no pathological changes. About 54% of DMAP taken orally was excreted as metabolites in the urine, 41% as glucuronide, 7% as sulfate, and 6% as thioethers. After i.v. administration the total of metabolites was somewhat higher, and the thioether proportion was 15%. The results indicate that DMAP is readily absorbed after oral administration but undergoes significant first pass effect in the liver. Therefore, the 4-fold i.v. dose must be administered orally to achieve the same ferrihemoglobin formation.
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PMID:Effects and biotransformation of 4-dimethylaminophenol in man and dog. 663 49

To study the effects of acute myocardial infarction on its pharmacokinetics a single oral dose of 400 mg mexiletine HCl was administered to seven patients. The study was performed within 24 h of the onset of pain (Study I) and was repeated 10-14 days later, during the recovery phase (Study II). Mexiletine in plasma and urine was quantified by a GLC method. The peak plasma concentrations of mexiletine were 0.65 +/- 0.05 (SEM) microgram ml and 1.08 +/- 0.11 micrograms/ml (p less than 0.05) in Studies I and II, respectively. The corresponding peak times were 4.68 +/- 2.04 h and 1.46 +/- 0.17 h (N.S.). The lag time averaged 0.48 +/- 0.08 h in Study I and 0.39 +/- 0.05 h in Study II (N.S.). The area under the plasma concentration-time curve remained unchanged. The elimination half-life was 15.03 +/- 0.61 h and 11.75 +/- 0.80 h (p less than 0.01) in Studies I and II, respectively. The recovery of unchanged mexiletine in urine and its renal clearance was also the same in both studies. The plasma protein binding of mexiletine was similar in Studies I and II (61 +/- 2% and 63 +/- 3%; N.S.). Thus, the rate of gastrointestinal absorption of mexiletine was definitely slowed in the acute phase of myocardial infarction, whereas the extent of absorption was not altered. The prolongation of the elimination half-life of mexiletine in the acute phase of myocardial infarction is probably related to an increase in its volume of distribution.
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PMID:Pharmacokinetics of oral mexiletine in patients with acute myocardial infarction. 666 76

On the example of the surface anaesthetic homologous series of 4-alkoxybenzoic-diethylaminoethylester-HCl (parethoxycaine) the so-called "cut off"-effect was studied. The "cut off"-effect is the phenomenon, that a weaker efficiency or an inefficiency is observed on the higher homologues of therapeutic substances. It is demonstrated that the "cut off"-effect is referred to the micellisation and aggregation of the higher homologues of the local anaesthetics in aqueous solution. This has the consequence, that the higher homologues cannot diffuse on the pain receptors and so the efficiency is reduced. By the addition of urea the aggregation will be reduced and the chain length-efficiency curve will take a different course.
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PMID:[Micelle formation as the origin of the cut-off phenomenon in a homologous series of local anesthetics]. 668 75

Fifty patients in a double-blind study received in randomized fashion either etidocaine HCl (Duranest) 1% or lidocaine HCl (Xylocaine) 2% with epinephrine 1:200,000 in a retrobulbar block for cataract surgery. Two parallel groups of 25 patients each were studied comparing the clinical properties of the drugs. The onset time for sensory and motor blocks of both drugs was essentially the same (3 minutes). The duration of action of etidocaine was considerably longer than lidocaine and less postoperative pain medication was required by patients blocked with etidocaine.
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PMID:Etidocaine used for retrobulbar block: a comparison with lidocaine. 699 10

The report deals with the clinical use and effects of tramadol-HCl (Tramal) as an adjuvant in regional anaesthesia. As distinguished from triflupromazine, diazepam, flunitrazepam, droperidol, piritramide and pentazocine this drug can be applied safely, reliably and without secondary effects in patients of all ages for sedation and analgesia without loss of cooperation (no sleep, no pain from body-positioning, no psychic distress) and for the prevention of centralisation in the unblocked region (no trembling- and freezing-reaction, no alteration of the blood-gas-analysis.
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PMID:[The use of tramadol-HCl (Tramal) as adjuvant in regional anaesthesia. Clinical report (author's transl)]. 707 94

In 80 patients with duodenal ulcer, the effects of various factors--symptoms, endoscopic findings, and peak acid output (PAO)--on the healing rate were studied during eight weeks of outpatient therapy with low-dose antacid (neutralising capacity less than 50 mmol HCl/d). Fifty-six per cent of the ulcers healed. The following unfavourable factors were found to cause a significant delay in ulcer healing: a long duration of pain in the last ulcer relapse and the present period of ulcer pain, smoking, stenosis of the duodenal bulb, and a high PAO. Multiple regression analysis showed that three factors (duration of the present ulcer pain, smoking, and stenosis of the duodenum) had a significant influence on healing rate. According to the results obtained with this method, the patients with no or only one unfavourable factor (n = 35) had the best healing rate: 80%, compared with patients who had two (n = 31) or three (n = 14) unfavourable factors. The healing rate of the latter two groups was 41% and 28%, respectively (p less than 0.001). A prognostic score based on these three factors represents the severity of duodenal-ulcer disease with regard to the healing process under placebo-like doses of antacid.
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PMID:Factors affecting the healing rate of duodenal and pyloric ulcers with low-dose antacid treatment. 721 49


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