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)

The choline analog, N-amino-N,N-dimethylaminoethanol (NADe), was fed ad libitum (chloride salt; 0.5%) to weanling rats in a low choline, low methionine synthetic diet. Control rats were fed choline chloride (0.5%) in place of NADe. Initial observation and behavioral screen tests of grasp strength, startle reflex, righting reflex, analgesia (hot plate test) and body temperature did not reveal any toxic effects caused by NADe, although both experimental and control groups gained weight more slowly than rats fed standard lab chow. After 25 days on the diet, the performance of rats fed NADe in a one-trial passive avoidance test was significantly impaired compared to control rats. There was no difference between experimental and control rats in sensitivity to foot shock or in activity monitored in a closed field. A subjective, 6-component behavioral rating scale indicated rats fed NADe were resistant to handling but not aggressive. These behavioral results were similar in two separate feeding experiments using deuterium-labeled and unlabeled NADe. The twitch response of isolated rat phrenic nerve-diaphragms during stimulation did not show any impairment of neuromuscular function in rats fed NADe. Receptor binding experiments indicated there were no differences between experimental and control rats in tritiated quinuclidinyl benzilate [( 3H]QNB) binding capacity in cortex, heart and ileum. Competitive [3H]QNB binding with carbachol indicated there was no difference in the IC50's measured in cortex homogenates. Acetylcholinesterase (AChE) and choline acetyltransferase (ChAT) activities in cortex were similar in experimental and control groups.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Effects of chronic dietary administration of the cholinergic false precursor N-amino-N,N-dimethylaminoethanol on behavior and cholinergic parameters in rats. 301 61

Bromfenac sodium (2-amino-3-(4-bromobenzoyl)benzeneacetic acid sodium salt sesquihydrate, AHR-10282B) is a potent long-acting, peripheral, analgesic compound possessing antiinflammatory, antipyretic, and prostaglandin synthetase-inhibiting properties. In the acetylcholine abdominal constriction assay in mice, bromfenac (bromfenac sodium) by the oral route at pretreatment times of 10, 20 and 300 min was respectively 3.7, 6.5 and 2.9 times more potent than zomepirac and 3.4, 6.6., and 44.2 times more potent than suprofen. In dogs bromfenac when given orally was 5.8 times more potent than zomepirac in blocking the nociceptive response to bradykinin. Naloxone did not alter the analgesic properties of bromfenac in mice; and after repeated administration, tolerance to analgesia did not develop. Bromfenac, given orally, was more potent than indometacin in suppressing acute (7.5-20 times) and chronic (3.8 times) inflammation. The gastric and intestinal toxicity potencies of bromfenac, given orally, were comparable with and 1.8 times more potent than indometacin, respectively. Bromfenac was 6.1 to 32.8 times more potent than indometacin in inhibiting the formation of prostaglandin E2 and F2 alpha from microsomes of bovine seminal vesicles, rabbit uteri, and rabbit renal medullae; but it did not block the direct action of prostaglandin E1 (abdominal constriction) and prostaglandin F2 alpha (contraction of the uterus). Bromfenac produced no unwanted central nervous system, cardiovascular, or autonomic effects.
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PMID:The analgesic and antiinflammatory activity and pharmacologic properties of bromfenac. 349 37

In the double-blind study reported here the authors were able to confirm the time- and dose-related effect of dilatation of the cervix by means of the new prostaglandin-E2 derivative (9-deoxo-16, 16-dimethyl-9-methylene-PG-E2-potassium salt) as compared to placebo. In spite of the short preoperative duration of action of three hours it was observed that half of the patients treated with the prostaglandin derivative vomited once or several times. The authors therefore consider that administration of the prostaglandin vaginal suppository is only justified in cases with a high risk of cervical injury, and in primiparae undergoing termination under local anesthesia. In 38 patients termination was performed by means of direct cervicomyometrial analgesia. With one exception they approved of chemical dilatation of the cervix in spite of the side-effects, assuming that it would result in less intraoperative pain.
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PMID:[Preoperative cervix dilatation in 1st trimester pregnancy interruption using 9-deoxy-16, 16-dimethyl-9-methylene prostaglandin E2. A randomized double-blind study]. 404 11

This study determines the efficacy and incidence of side effects associated with intravaginal prostaglandin F2alpha (PGF2alpha). 20 healthy patients (16 to 30 years of age; 9-16 weeks gestational age) with no history of threatened abortion in the current pregnancy were studied. Baseline hematologic, metabolic, urinary, and hormonal studies were conducted. Transabdominal amniocentesis was performed in 7 patients. The uterus was observed for spontaneous contractility. Lactose tablets with 50 mg PGF2alpha (THAM salt) were administered vaginally. The intensity and frequency of uterine contractions in the 7 monitored patients determined the treatment regimen. Prostaglandin tablets were inserted at hourly intervals to maintain frequency of contractions at 5 per 10 minute time interval and/or intensity of contractions greater than an average of 40 mm Hg over a 10 minute-period. 13 patients whose uterine activity during the abortion process was assessed by clinical observation were given a similar time schedule. Blood studies were peformed 6 hours after the onset of therapy and immediately following abortion. Analgesia were used intramuscularly as antiemetic agents where necessary. Prepared questionnaires and personal interviews were completed at the 4-week clinic visit to determine patient acceptability of the method. 19 of 20 patients aborted, with 7 classified as complete and the remaining 12 requiring a uterine exploration and curettage for removal of retained placental fragments. Average induction-complete abortion interval was 17 hours and 50 minutes. There was no difference between multiparous and primiparous patients. In 1 patient who failed to abort with the prostaglandin tablet, administration of 900 mg PGF2alpha and hypertonic saline were used to facilitate abortion which occurred 24 hours later. Emesis occurred in 18 patients, diarrhea in 13, and fever in 11. Of 15 patients who agreed to an interview during the clinic visit, 14 stated they would choose the method again. Vaginal administration of PGs appears to exert effects by systemic, rather than by local mechanism. Although this method is effective, it has a high incidence of side effects and is associated with increased utilization of professional time.
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PMID:Abortifacient efficacy of intravaginal prostaglandin F2 . 468 31

Carbonated lidocaine is believed to penetrate membranes more rapidly than its hydrochloride salt and could possibly cause higher serum levels. To compare serum levels, arterial blood samples drawn at intervals were analyzed in a group of 18 patients under epidural anaesthesia with equivalent doses of lidocaine hydrochloride and lidocaine hydrocarbonate, with and without epinephrine. Results show that serum levels were significantly higher when lidocaine hydrocarbonate was used for epidural analgesia.
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PMID:Effects of carbon dioxide and epinephrine on serum levels of lidocaine after epidural anaesthesia. 678 11

Epidural analgesia was administered to one hundred patients undergoing various types of surgical procedures. They were divided at random into four equal groups who received lidocaine hydrocarbonate or lidocaine hydrochloride, both with or without epinephrine. A double blind method was used. The study was designed first to test the validity of claims that lidocaine hydrocarbonate produces a shorter period of onset for effective analgesia, a more profound sensory and motor block, and a higher spread of analgesia than the hydrochloride salt and secondly, to identify the respective roles of carbon dioxide and epinephrine in obtaining this alleged superior effectiveness. The results of the study showed that carbon dioxide improved the quality of sensory block, but we could not find any significant difference between lidocaine hydrocarbonate and lidocaine hydrochloride salt, with and without epinephrine, with regard to rapidity of onset, upward spread of analgesia and quality of motor block. As was already known, duration of analgesia was prolonged by the addition of epinephrine but not by the addition of carbon dioxide. They study also showed that the compliance of the epidural space was decreased in the lidocaine hydrocarbonate groups compared to those with lidocaine hydrochloride. There is a positive correlation between the duration of sensory block or the upper level of analgesia and compliance in the hundred patients studied. It is concluded that the hydrocarbonate base, because of its more profound sensory block in the L5-S1 segment, can be useful for operations on the lower extremities, especially in the L5-S1 segmental distribution. However, knowing that the hydrocarbonate base is more expensive, one must use his own judgment in appraising the cost-benefit of its use.
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PMID:Comparison of the clinical effectiveness of lidocaine hydrocarbonate and lidocaine hydrochloride with and without epinephrine in epidural anaesthesia. 701 64

In two multicentric randomized, double-blind, parallel design trials the more appropriate dose of ketoprofen lysine salt suppositories, by considering benefit-risk ratio, was determined in children affected by acute inflammatory disease of respiratory or urinary tract with fever and pain. Fifty-three children ranging 6-36 months (infants) randomly assigned to 20, 30, 40 mg dose levels, and 54 children ranging 3-13 years (children) randomly assigned to 40, 60, 80 mg dose levels were included in the studies. Efficacy variables considered were hyperthermia and pain; body temperature was measured rectally, at fixed intervals and pain was evaluated by Maunuskela scale at the same interval times. Standard laboratory test were obtained at the beginning and end of treatment, and blood arterial pressure and heart rate were recorded regularly. Systemic and local tolerability were also determined. In infants all doses were associated with analgesia and temperature reduction; antipyretic effect was statistically significant starting from the first hour (p = 0.007). The dose of 30 mg resulted different from 20 mg dose from third hour (p < 0.05). The appropriate dose that better relate antipyretic and analgesic efficacy with a good tolerability was 30 mg. In children the analgesic and antipyretic efficacy was well established at all doses tested, however the effects were more marked and prolonged at 60 and 80 mg doses, with a better tolerability for 60 mg dose. The tolerability of all doses studied was good. Doses of 30 mg in infants and 60 mg in children correspond to a range of 2.0-3.5 mg of ketoprofen lysine salt for kg body weight, for each administration.
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PMID:[Effects of various dosage of ketoprofen salt suppositories in acute inflammatory disease in infants (3-36 month old) and children (3-13 year old)]. 764 21

Epidurally administered fentanyl is commonly used in postoperative pain management. The onset of action is rapid, but the duration of analgesia is short. In this study we examined the hypothesis that a poorly soluble salt of fentanyl (fentanyl pamoate) would create a depot of the drug in the epidural space and thus provide prolonged analgesia. The dose-response relationship and duration of analgesic action of epidural fentanyl citrate (FC) and fentanyl pamoate (FP) were studied in white male Sprague-Dawley rats. Somatic and visceral nociceptive stimulation (tail flick and colorectal distension, respectively) were used to test the analgesic effects of the drugs. The calculated dose producing 100% of the maximum possible effect (100% MPE) for FP was 31 micrograms toward somatic and 33 micrograms toward visceral noxious stimulation, and for FC it was 3 micrograms toward both stimulations. The antinociceptive effects were similar, with 31 micrograms of FP and 3 micrograms of FC. The areas under the time-response curves (AUC) were significantly higher with FP than with FC when high doses (5 micrograms of FC or 50 micrograms of FP) were used, but with doses expected to produce 100% MPE, differences between the study drugs were not observed in the duration of analgesia. We conclude that the duration of antinociceptive effect of fentanyl can be prolonged when administered as a poorly soluble salt.
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PMID:Prolonged analgesia after epidural injection of a poorly soluble salt of fentanyl. 797 8

Porulaca pilosa has been used in Brazil as a traditional remedy to cause diuresis, antipyresis and analgesia. Achyrocline satureioides has been used in folk medicine as antiinflammatory, hypoglycemic, sedative and to treat gastrointestinal disorders such as diarrhea and dysentery suggesting that it may affect salt and water reabsorption by the gastrointestinal tract. In the current study, hydroalcoholic extracts of both plants were investigated in order to examine their renal effects. The results support the claim that extracts of P. pilosa present renal effects but not the popular belief that it affects diuresis. It has also been provided that, in rats, it causes an increase in K excretion without a concomitant change in water diuresis or Na excretion. Our findings also support the popular belief that A. satureioides does not apparently have renal effects and it might change renal ion transport based on observations that it affects gastrointestinal reabsorption.
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PMID:Effects of hydroalcoholic extracts of Portulaca pilosa and Achyrocline satureioides on urinary sodium and potassium excretion. 799 Apr 91

Topical formulations of tetracaine in vehicles of propylene glycol and saline are tested on human volunteers with standard occlusive, adhesive, transdermal patches. The effects of formulation composition, dose, and onset time are investigated. Dose-response studies indicate that the optimum formulation for the diffusion of tetracaine in vivo is 60% free base and 40% acid salt (w/w) in 40% propylene glycol and 60% saline (v/v). A concentration of 0.3 M [8.3% (w/v)] tetracaine is sufficient to reach the dose plateau. Time-response studies indicate that high concentrations of tetracaine in the optimum formulation [1.1 and 1.8 M, 30 and 50% (w/v), respectively] can produce statistically significant analgesia relative to a placebo after 45 min. Comparison of these in vivo data with earlier in vitro data indicate that the optimum formulation with regard to clinical studies is identical to that for in vitro diffusion through hairless mouse skin [60% free base and 40% acid salt (w/w) in 40% propylene glycol and 60% saline].
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PMID:Evaluation of local anesthesia provided by transdermal patches containing different formulations of tetracaine. 828 25


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