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)

Vaginal suppositories containing 9-deoxo-16,16-dimethyl-9-methylene prostaglandin E2 were administered to 40 subjects in an attempt to induce an early abortion. All subjects were 49 days or less from their last menstrual period. Ten subjects (Group A) received the 75-mg suppository followed in 6 hours by a 30-mg suppository, ten subjects (Group B) received the 30-mg suppository followed in 2 hours by the 75-mg suppository and twenty subjects (Group C) received a 30-mg suppository followed in 3 hours by a second 30-mg suppository and in three more hours, at the discretion of the principal investigator, they could receive a third 30-mg suppository. Twenty-seven subjects (68%) had a successful termination of their pregnancy using the multiple vaginal prostaglandin suppository regimens. Seven subjects from Group A, 6 subjects from Group B, and 14 subjects from Group C successfully aborted. One subject in Group B and one subject in Group C were lost to follow-up and the remaining 11 subjects (28%) failed to abort. Twenty-six subjects reported side effects which included nausea, emesis, diarrhea, and uterine cramping requiring analgesia. Thirty-four subjects experienced hyperpyrexia of 99.6 degrees or greater and 12 subjects had their body temperature reach 101 degrees or higher. The use of vaginal suppositories containing 9-deoxo-16,16-dimethyl-9-methylene prostaglandin E2 did not significantly increase the overall abortifacient efficacy of this method from the 60% rate we previously observed with (15S)-15-methyl-prostaglandin F2 alpha methyl ester suppositories.
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PMID:Termination of early gestation with 9-deoxo-16,16-dimethyl-9-methylene prostaglandin E2. 618 97

The prostaglandins F2alpha (PGF2alpha) and E2 (PGE2) used for abortion during the 2nd trimester of pregnancy were compared and are presented along with a method of management that minimizes patient discomfort. The study included 23 consecutive patients who wanted to undergo elective 2nd trimester abortion at the Unviersity of California, Davis Medical Center, during the January 1981-May 1981 period. Gestational age was determined by menstrual history, fundal size, and, when necessary, ultrasonography. Patients between 14-20 weeks of estimated gestational age were assigned to either PGF2alpha or PGE2 therapy using a set of random numbers. Patients were excluded from the study if a history of significant renal, cardiac, or pulmonary disease was obtained, if a uterine or cervical anomaly was suspected, or if abortion was desired because of a known fetal anomaly, abnormal karyotype, or fetal demise. 13 patients were in the PGF2alpha group and 12 were in the PGE2 group. 4 patients in the PGF2alpha group and 5 in the PGE2 group were nulliparas. The mean induction to abortion interval was 9.19 +or- 6.18 hours, 3-22 hours, for those in the PGF2alpha group and 9.19 +or- 2.59 hours, 5.75-12.78 hours, for those in the PGE2 group. The difference was not statistically significant. The cumulative abortions rates of the 2 methods were similar. Except for 2 patients who received PGF2alpha, all of the patients studied aborted within 14 hours. There was a 31% incidence of emesis in those patients in the PGF2alpha group, but none of these patients had more than a single episode. A 20% incidence of emesis was noted for the PGE2 group, with each of these patients having 2 episodes. No patient had diarrhea or hyperthermia develop, and none required antidiarrheal or antipyretic medication after the intial prophylactic dosages. Of the patients in the PGF2alpha group, 61.5% required supplementary analgesia as compared with 60% for those in the PGE2 group. Of those patients requiring additional analgesia, those in the PGF2alpha group, on an average, had more medication given orally and intramuscularly. Curettage was considered to be an integral part of the abortion procedure. Products of conception were obtained from all of the patients at the time of curettage. No patient returned after discharge from the hospital because of hemorrhage or infection as a result of retained products of conception. With the use of laminaria tents for cervical priming, prophylaxis of minor side effects, oxytocin supplementation and postabortal curettage, PGF2alpha and PGE2 are equivalent midtrimester abortifacients when rapidity, safety, and patient comfort are considered.
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PMID:A comparative study of two types of prostaglandins for abortion during the second trimester. 657 7

The degree of generalization to the effects of DFP, an organophosphate anticholinesterase, was studied in two lines of Sprague-Dawley derived rats selectively bred for varying sensitivities to DFP. In the S13, S14, S15, and S16 generations the Flinders S-line of rats were still more sensitive to the effects of DFP on the criterion variables upon which selection was based: core body temperature, body weight and a simple operant response for water reward. The flinders S-line were also more sensitive to the effects of DFP on locomotor activity, FR5 responding for a water reward, and analgesia, indicating some degree of generalization. However, diarrhea, a symptom of peripheral effects of DFP, occurred at a similar incidence in the two lines, although males of both lines had higher incidences than the females. Neither of the two lines was affected by DFP for variables in which aversive (i.e. shock) motivation was used: The number of discriminative escape responses and the escape times were similar. These findings indicate that while the effects of DFP do generalize beyond the criterion variables upon which selection was based, the generalization is relatively specific. The data are consistent with the hypothesis that the changes in sensitivity have arisen because of changes in the functioning of a central cholinergic system(s).
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PMID:Selective breeding for sensitivity to DFP: generalization of effects beyond criterion variables. 689 Oct 70

In this multicentre, double-blind clinical study, the pain-relieving effects of single doses of pirprofen (200 and 400 mg) and pentazocin (100 mg) were compared with those of a placebo in 210 patients after oral surgery. Pirprofen and pentazocin were significantly more effective than the placebo. At either of the two dosage levels, pirprofen proved more active than pentazocin. A dose-activity ratio could be established with pirprofen and showed that the 400 mg dose was distinctly more effective than the 200 mg dose (p less than 0.05). The analgesia procured by the drug was perceptible after about 15 minutes. One of the 51 patients who received the 400 mg dose developed diarrhoea, this being the only side effect observed.
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PMID:[A study of the analgesic effects of pirprofen after oral surgery]. 713 74

Intramuscular injections of 15-methyl-prostaglandin F2alpha (PGF2alpha) were used to induce 48 terminations of pregnancy in the 2nd trimester as well as to deliver 8 cases of fetal death in utero and 1 hydatidiform mole. It is an effective method of treatment with a failure rate of 1.9%. As compared to the administration of pain-relieving drugs intravenously, continuous epidural analgesia has shown itself to be the only method which will allow the best possible conditions for the maintenance and control of PG induction to be carried out, suppressing effectively even the pains which are associated with uterine contractions brought on by PGs. Although the method of systemic administration of PGs does avoid any intervention through the cervicovaginal route, it does not completely do away with rare infections which are found to complicate matters when PGF2alpha gel is administered by the extraamniotic route. Nevertheless, the acceptability and use of this method as a routine method must be limited by the high incidence of episodes of diarrhea which are made worse by the paralysis of sphincters which is inseparable from epidural analgesia. (author's)
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PMID:[Induction for termination of pregnancy in the second trimester and for delivery of babies dead in utero using intramuscular injections of 15-methyl-PGF2 alpha (author's transl)]. 729 1

Prostaglandin (PG) D2 was studied to determine the pharmacological effects of this PG on the central nervous system. PGD2 (0.45-4.05 mg/kg) decreased spontaneous locomotor activity in rats by as much as 66% of control, however, the neuromuscular coordination of mice, treated at the same doses of PGD2, was not impaired. PGD2 (0.05-4.05 mg/kg) also increased pentobarbital sleeping time in mice from 42% to 238% of control, in a dose-related manner. PGD2 did not prevent convulsions induced in response to electroshock or pentylenetetrazol. Cats monitored for EEG responses to PGD2 infusion displayed variable sensitivity to different doses (16-3000 microgram) of drug, however, the characteristic response to PGD2 was the conversion from a uniform low voltage, fast wave pattern to high voltage, slow waves. Cats administered PGD2 were sedated and sometimes catatonic, and displayed brief periods of hypotension, bradycardia, diarrhea, analgesia and hyperthermia at higher doses of the drug. Thus, PGD2 possesses sedative properties in rodents and cats and may have a role in the central nervous system.
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PMID:PGD2 effects on rodent behavior and EEG patterns in cats. 739 69

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

A series of 1-arylsulfonylpyrrolidin-2-ones (and 2-thiones), 1-aryl sulfonylpiperidin-2-ones (and 2-thiones) and 1-arylsulfonyl hexahydro-2H-azepin-2-one were synthesized and submitted to a battery of binding assays. The compounds showed little or no affinity for the receptors tested other than muscarinic receptors labelled either with [3H]pirenzepine or with [3H]quinuclidinyl benzilate. When tested in the isolated guinea pig ileum, they antagonized the contractions induced by acetylcholine and behaved as competitive muscarinic antagonists. After parenteral administration in mice, most compounds inhibited carbachol-induced diarrhoea but were less effective in counteracting salivation and lacrimation and showed little or no mydriatic action, thus displaying selectivity at the intestinal level. The reference drugs tested, atropine, butyl scopolamine and cimetropium bromide were far less selective. maximal in vivo activity was obtained by introducing diethylamino or 1-piperidino or 1-hexahydroazepinyl groups in the 4-position of the phenyl ring while the enlargement of a 5- to a 6-membered lactam ring or its conversion into a thiolactam had a less marked effect. The most interesting compounds were further evaluated for their ability to antagonize carbachol-induced colonic hypermotility in the rat and arecoline-induced analgesia in mice. The effect on gastric acid secretion in the rat was also investigated. The overall in vivo data showed that compounds 14, 15, 26 and 27, i.e. those bearing a 1-hexahydroazepinyl group in the 4-position of the phenyl ring, were the most potent and selective compounds.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:New classes of antimuscarinic agents endowed with selective antispasmodic properties. 1-Arylsulfonyl pyrrolidin-2-ones and 2-thiones, 1-arylsulfonyl piperidin-2-ones and 2-thiones and 1-arylsulfonyl hexahydro-2H-azepin-2-one. 801 Oct 4

At the Los Angeles County--University of Southern California Medical Center, physicians compared data on 27 women who received 20 mg prostaglandin E2 (PGE2) intravaginally every 3 hours to induce a 2nd trimester abortion with data on 28 similar women who received 200 mcg misoprostol intravaginally every 12 hours. The women underwent termination of pregnancy for intrauterine fetal death or medical or genetic reasons. The successful abortion rate within 24 hours was similar for both groups (81% for PGE2 and 89% for misoprostol; p = 0.47). For both groups, the mean intervals between treatment and abortion among women who successfully delivered the conceptus within 24 hours were not statistically different (10.6 hours for PGE2 and 12 hours for misoprostol; p = 0.33). Every woman in the misoprostol group successfully aborted within 38 hours. Passage of the fetus and the placenta simultaneously occurred in 32% of PGE2 cases and in 43% of misoprostol cases (p = 0.56). Women receiving PGE2 were more likely to suffer from a fever (= or 38 degrees Celsius) (63% vs. 11%; p .001), severe pain requiring analgesia medication more than once (26% vs. 4%; p = .025), vomiting (33% vs. 4%; p = .005), and diarrhea (30% vs. 4%; p = 0.012) than women receiving misoprostol. The average number of doses and the average cost per treatment were much higher for PGE2 than for misoprostol (3.7 vs. 1.4 and $315.30 vs. $0.97, respectively). 57% of misoprostol patients had a successful abortion with just 1 dose of 200 mg misoprostol. These findings demonstrate that intravaginal administration of misoprostol is a safe and effective method of terminating 2nd trimester pregnancy, easier to administer and less costly than PGE2.
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PMID:A comparison of intravaginal misoprostol with prostaglandin E2 for termination of second-trimester pregnancy. 802 46

Colonic dilatation has been reported as an occasional complication of infectious colitis in single case reports and short series, but no large series has been published. We analysed 19 cases of self-limited colitis complicated by colonic dilatation, with infective agents identified in 14, admitted to a Regional Infectious Diseases Unit. Colonic dilatation, defined as a minimum transverse colonic diameter of 7 cm on plain abdominal X-ray, was associated with approximately 1% of cases of notifiable diarrhoea requiring hospital admission. The clinical course was associated with pyrexia (in 90%), tachycardia (in 90%), hypoalbuminaemia (in 100%), anaemia (in 84%) and reactive thrombocytosis (in 63%). There was a history of antidiarrhoeal agents or opiate analgesia in eighteen patients (95%). Intensive medical management, consisting of intravenous antibiotics, steroids, supplementary nutrition and withdrawal of anti-motility agents, resulted in resolution in 17 patients. Two patients required subtotal colectomy for perforation of the transverse colon, but neither developed severe peritonitis, and both subsequently underwent reversal of ileostomy. With early recognition and close observation of colonic dilatation in patients with acute diarrhoea, most cases can be successfully managed conservatively with preservation of the colon. Surgical intervention should be considered in patients with progressive colonic dilatation despite intensive medical management. There were no clinically useful parameters distinguishing self-limited colitis from inflammatory bowel disease acutely, so initial management should cover both possibilities.
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PMID:Dilatation of the colon complicating acute self-limited colitis. 814 Feb 18


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