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)

Fourteen patients with a variety of neoplasms not responsive to standard forms of therapy underwent whole body hyperthermia for a maximum 4 h at 41.8 degrees C. This was a phase-I cancer trial designed to develop whole body hyperthermia as an adjuvant to systemic chemotherapy. Intravenous analgesia was used to sedate patients, obviating the need for general endotracheal anesthesia. Hyperthermia was induced by means of a high-flow water perfusion suit. Cardiovascular performance was evaluated using a flow-directed pulmonary artery catheter. Patients developed a twofold mean increase in cardiac index without evidence of cardiac damage by ECG or creatine phosphokinase (CPK) isoenzymes. An acute fall in serum magnesium and phosphate and an acute rise in arterial pH, serum CPK values, and granulocyte count occurred in all patients. There were no clotting abnormalities. Toxicity included fatigue, diarrhea, nausea, and transient elevations in liver enzymes. Four patients were febrile for 36 h after initial defervescence. Peripheral neuropathy developed in four. These results show that with carefully monitored conditions whole body hyperthermia is feasible.
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PMID:Whole body hyperthermia: a phase-I trial of a potential adjuvant to chemotherapy. 42 99

A series of newly synthesized N-phenyl-substituted derivatives of succinimide were screened for anticonvulsant activity. Addition of a sulfonamide group in the p-position was of great consequence for the anticonvulsant effect. Substitution of a halogen in the m- or o-position improved activity against electroshock induced seizures. Pentylenetetrazole convulsions could only be prevented by few of these substances in smaller than 200 mg/kg oral doses. Activity could be further enhanced by adding more aliphatic or aromatic groups to the succinimide ring. The lethal doses of most of the active succinimides were higher than 5000 mg/kg p.o. With sublethal doses mice sometimes become drowsy and had myoclonic seizures and/or diarrhoea. At therapeutic dose levels kinetic disturbances, potentiation of pentobarbitone hypnosis or analgesia were rarely observed.
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PMID:[Anticovulsant activity of N-(p-sulfamoyl-phenyl)-succinimide derivatives (author's transl)]. 57 5

The study objective was to determine the effectiveness and safety of a single high dose (40 mg) of intraamniotically administered prostaglandin F2alpha (PGF2alpha). A total of 33 women in their 14-20th week of pregnancy were selected for the study. The outcome was considered successful if the fetus and/or placenta were expelled from the uterus within 48 hours. If the fetus and placenta were expelled completely through the cervical canal the trial was recorded as complete abortion. If the placenta was retained within the uterus, completely or partially, the trial was recorded as incomplete abortion. The patients' mean age was 22.6 years. 27 patients were under 28 years of age, and 9 patients were under age 20. 25 patients were African, 2 Caucasian, and 4 Asian. 2 others were of mixed race. The mean parity of the patients was 1.4 previous pregnancies with a standard error of +or- 1.4. 17 women were nullipara; 16 women were multipara. There was 1 case of technical failure in the series, an obese Asian patient with a 16 week pregnancy in whom difficulty was experienced in entering the amniotic sac. A bloody tap during amniocentesis was obtained in 4 patients. 28 of the 32 patients aborted within 48 hours, showing a success rate of 87.5%. At the end of the first 24 hour period, 19 patients (59.4%) had aborted and an additional 9 patients (28.1%) aborted during the following 24 hours. The mean induction abortion interval was 19.4 hours. Multiparous patients aborted more frequently and in a shorter period of time than did nulliparous patients. 92.3% of the multiparous patients aborted by 30 hours; only 84.2% of the primigravida had achieved this in 36 hours. In the successful group abortion was complete in 13 patients (46.4%). In the other 15 patients (53.6%) the placenta was partially or completely retained necessitating surgical evacuation. Minor side effects were observed in 28 patients (87.5%). None of these side effects required analgesia in the form of intramuscular pethidine. Gastrointestinal disturbances were common. Vomiting occurred in 11 patients. Diarrhea occurred in 3 patients. No instances of cervical laceration or cervicovaginal fistula were observed. Bleeding was minimal in 27 patients (84.4%). In another 5 patients the amount of bleeding was moderate. In the majority of patients bleeding ceased with 2 weeks after discharge from hospital. None of the patients needed hospital readmission. No signs of vaginal or pelvic infection or delayed uterine involution were observed.
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PMID:Induction of second-trimester abortion with a single dose (40 mg) of intra-amniotic prostaglandin F2a. 92 82

Initial examination and therapy, and the avoidance of maltreatment are emphasized. Gastric decompression is of prime importance, after which no compound should be administered via stomach tube. Where large amounts of high starch grains are fed, primary acute gastric dilatation must be differentiated from that secondary to small bowel dilatation, by immediate gastric intubation and irrigation of the cardia with lidocaine. If cessation of pain and improvement of peristalsis and general attitude follow, the former state may be assumed. If pain persists and peristalsis does not improve markedly, one should assume small bowel displacement. Rectal examination is helpful in initial evaluation: impactions, inguinal herniation and ileocaecal intussusception may be diagnosed and small bowel displacement suspected. Palpation of one or more distended loops of bowel in the ventral middle third of the abdomen indicates small bowel displacement or ileus and flaccid distension. Distinction by rectal palpation alone is difficult. Palpation of the gas-distended apex of the caecum in the middle third of the abdomen is virtually pathognomonic for 180 degrees rotation of the large bowel. Abdominal paracentesis yielding true sanguineous effusion indicates a necrotizing segment of the bowel. If negative, such a segment is absent, or there is an infarcted segment, not yet damaged to the point of leaching whole blood, or the necrotizing segment is outside the peritoneal cavity, i.e., in the thorax, intussuscepted into the caecum, or herniated into the inguinal canal. Recurrent colics frequently may be due to verminous arteritis but the relationship to diet should be investigated. Recurrent colics after grain ingestion with occult blood in the faeces may be due to ulcers; such cases respond well to grain withdrawal. The advantages and disadvantages of phenothiazine-derived tranquillizers are discussed. They are contra-indicated if there is any evidence of circulating volume insufficiency but are benefical in many instances through improved peripheral perfusion of organs provided circulating volume is adequate, i.e., early in acute abdominal disease prior to development of circulatory insufficiency. They should not be administered if immediate surgery is contemplated because of hypotensive effects. The administration of oral antibiotics (Neomycin) early in the course of the disease is encouraged. This is contra-indicated if the horse is already toxic, when it should receive parenteral antibiotics, preferably chloromycetin. Tetracyclines may predispose to the later development of salmonella diarrhoea. Absolute analgesia should be provided; our preference is the magnesium sulphate-chloral hydrate solutions. Administration of mineral oil is desirable in initiation of peristalsis, depression of Gram-negative overgrowth and softening of impactioning obstructions but nothing should be administered per os if the stomach has required decompression.
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PMID:Monitoring and evaluating the physiological changes in the horse with acute abdominal disease. 117 34

Swaziland is a kingdom with 800,000 inhabitants bordering on Mozambique and South Africa with about 50% of the population under 15 years of age. The experience of a nurse in a small clinic in the course of several years is recounted. Swaziland ranks 3rd in the world in alcohol abuse which often leads to wounds requiring suturing. Penicillin is given prophylactically with a paracetamol preparation for analgesia. As a rule, every injured person will get a .5 ml tetanus injection for prophylaxis. The most serious conditions of polyclinic patients are hepatitis, bilharzia, diarrhea, pellagra, pneumonia, and malnutrition. A great number of patients have sexually transmitted diseases, and the rate of AIDS infection is not known. According to 1 study 60-80% of the population in reproductive age will die of AIDS in the course of a 5-year period. The majority of people are impervious to counseling about their sexual behavior in spite of educational programs on the radio, in schools, and in work places. Condoms are not popular, since they are not considered manly. Pregnant women receive iron and multivitamin tablets in the course of pregnancy. Many pregnant women are anemic, and 70% give birth at home, the rest in a hospital or clinic. During delivery they get no analgesia, and there are few complications. The average weight of the newborn is 3.5 kg, although none of the women are under 150 cm. A little after birth all children are vaccinated with bacillus Calmette-Guerin (BCG) and polio, later with diphtheria-pertussis-tetanus (DPT) and measles.
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PMID:[Nursing under a different sky. Swaziland]. 146 29

Misoprostol is a stable, orally active synthetic analogue of prostaglandin E, which is used for the prophylaxis and treatment of peptic ulcer. It is cheap, effective, and associated with fewer gastrointestinal side effects. Misoprostol has an uterotonic effect and it is contraindicated for women in early pregnancy. Preliminary reports suggest that misoprostol in combination with mifepristone at a dose of 200 mg or 600 mg may be as effective as gemeprost or sulprostone for inducing early abortion but with fewer side effects. The authors report their experience using misoprostol together with mifepristone to induce abortion in 100 women in early pregnancy. 100 women requesting medical termination of pregnancy at the Medical Termination Unit of Simpson Memorial Maternity Pavilion, Edinburgh, with amenorrhea of or less than 56 days were given 200 mg mifepristone; 48 hours later they were given 600 ug misoprostol orally. The study found the combination of misoprostol with mifepristone to be inexpensive, simple, effective, noninvasive, and an acceptable alternative to current regimens for medical termination. One woman had an incomplete abortion prior to the administration of misoprostol, 93% of 99 women had complete abortion following administration of misoprostol, there were three ongoing pregnancies and four incomplete abortions, 24% of the women vomited and 7% had diarrhea following administration of misoprostol, and 62% did not require analgesia.
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PMID:Induction of abortion with mifepristone and misoprostol in early pregnancy. 147 3

Mifepristone (an antiprogesterone) and misoprostol (a synthetic analogue of prostaglandin E1) were administered to 60 women diagnosed with missed abortion or anembryonic pregnancy (gestation sac present but no developing embryo) equivalent to 13 weeks' gestation or less who were recruited after counselling. The median age was 227 (range 15-44), and the median duration of amenorrhoea was 71 (42-110) days. 25 of the women had been referred for ultrasound scanning because of bleeding in early pregnancy, while the rest were diagnosed by routine scanning. 29 patients had anembryonic pregnancies, and 31 had a missed abortion. Each patient received a 600 mg single oral dose of mifepristone, and 36-48 hours later misoprostol 600 mcg was given orally (400 mcg and, 2 hours later, 200 mcg). If the products of conception were not expelled within 4 hours, vaginal ultrasonography was performed. 8 patients aborted with mifepristone alone, 43 aborted after taking 600 mcg of misoprostol, and 5 more aborted after receiving a 2nd divided dose of 600 mcg misoprostol. In 3 patients the treatment failed, and they underwent evacuation of the uterus under general anaesthesia. Exploratory curettage was performed in 2 other patients at 14 and 22 days after treatment with misoprostol, but no products of conception were obtained. The median time from administration of misoprostol to abortion was 4 (1-11) hours. The median duration of bleeding after abortion was 10 (2-22) days. Side effects included nausea, vomiting (5 patients received antiemetic drugs), and diarrhoea (7 patients) from misoprostol treatment. 39 women did not want any pain relief, 13 asked for oral analgesia, and 7 obtained parenteral analgesia.
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PMID:Medical management of missed abortion and anembryonic pregnancy. 148 4

MK-329 is a nonpeptidal, highly specific cholecystokinin (CCK) receptor antagonist, with affinity for pancreatic and gallbladder CCK receptors similar to CCK itself. MK-329 and its progenitor, asperlicin, can inhibit the growth of CCK receptor-positive human pancreatic cancer in athymic mice. Based on these activities and the ability of MK-329 to transiently increase food intake and enhance morphine analgesia in murine models, we conducted an open trial of MK-329 in 18 patients with advanced pancreatic cancer in whom the CCK receptor status of the tumors was unknown. Tumor response, pain control, and nutritional parameters (hunger rating, caloric intake, body weight, and anthropometrics) were serially assessed. The results of the study failed to demonstrate any impact of MK-329 on tumor progression, pain, or nutrition. Toxicity was mild and limited to nausea, vomiting, diarrhea, and abdominal cramps, with 17 of 18 patients able to tolerate treatment. While a role for MK-329 in the management of patients with advanced pancreatic cancer cannot be supported by the results of this trial, additional studies of this agent in patients with known CCK receptor-positive tumors, at escalated doses, and possibly in conjunction with other growth antagonists, appear warranted.
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PMID:A pilot clinical trial of the cholecystokinin receptor antagonist MK-329 in patients with advanced pancreatic cancer. 155 66

Noradrenergic neuronal hyperactivity following chronic morphine administration has been postulated to cause withdrawal signs and symptoms. Suppression of this hyperactivity, for example, by clonidine attenuates withdrawal. It might follow, therefore, that the prevention of suppression of noradrenergic systems during chronic morphine administration might diminish hyperactivity and prevent withdrawal. If the normalization of noradrenergic activity during opioid administration did not also suppress analgesia, it might be of medical and theoretical interest. To test this hypothesis, we gave the alpha-2-antagonist yohimbine to rats in order to increase noradrenergic activity during morphine treatment and then subsequently precipitated morphine withdrawal with naloxone. Six groups were examined: saline controls (N = 11), morphine (N = 11), morphine + 2.0 mg/kg/day yohimbine (N = 15), morphine + 3.0 mg/kg/day yohimbine (N = 5), 2.0 mg/kg/day yohimbine (N = 11) and 3.0 mg/kg/day yohimbine (N = 5). Subjects received 75 mg morphine pellets implanted on day 1,4 and 6 of the treatment or sham implantation. Yohimbine was delivered throughout the morphine treatment by subcutaneously implanted osmotic pumps. On day 7, all subjects were given 1.0 mg/kg naloxone and rated for behavioral signs of withdrawal. Analgesia was measured by observing tail flick latencies (TFL) before and after chronic drug treatments. Naloxone-precipitated withdrawal was characterized by irritability, ptosis, penile erection, diarrhea, rhinorrhea, abnormal posture, wet-dog shakes, jumping, and teeth chattering, none of which were observed in groups receiving only saline or yohimbine. Withdrawal behavior was attenuated in a dose-dependent manner when yohimbine was administered during morphine treatment but analgesia was not attenuated.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Yohimbine co-treatment during chronic morphine administration attenuates naloxone-precipitated withdrawal without diminishing tail-flick analgesia in rats. 205 41

The aim of the present study was to investigate if a physical dependence could be induced by chronic activation of the endogenous enkephalinergic system. We have therefore evaluated naloxone-induced withdrawal syndrome in rats after central infusion during 7 days of comparable antinociceptive doses of RB 38 A ((R,S)HONH-CO-CH2-CH(CH2C6H5)-CONH-CH(CH2C6H5)-COOH), a mixed enkephalin catabolism blocker and of the selective mu, DAGO (Tyr-D-Ala-Gly-(Me)Phe-Gly-ol) and delta, DSTBULET (Tyr-D-Ser(OtBu)-Gly-Phe-Leu-Thr), opioid agonists. The responses were compared to those induced by RB 38 B ((S,S)HONH-CO-CH2-CH(CH2C6H5)-CONH-CH(CH2C6H5)-COOH), a selective inhibitor of the 24.11 neutral endopeptidase (NEP) 'enkephalinase'. DAGO induced a severe withdrawal syndrome evidenced by a large weight loss, hypothermia, jumping, mastication, teeth chattering, diarrhoea, lacrimation and salivation. In contrast, DSTBULET and RB 38 A produced only a moderate physical dependence. Only two signs were statistically different in these two groups: wet dog shakes and temperature. Chronic i.c.v. administration of DAGO, DSTBULET and RB 38 A produced a time-dependent reduction in analgesia, but 120 h after continuous infusion only RB 38 A was able to still induce a significative antinociceptive effect. The present data suggest that even in the drastic conditions used here long-term complete inhibition of enkephalin catabolism induces a weak tolerance and a moderate physical dependence, similar to that produced by delta opioid agonists. This effect was not observed after chronic selective inhibition of NEP by RB 38 B.
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PMID:Differences in physical dependence induced by selective mu or delta opioid agonists and by endogenous enkephalins protected by peptidase inhibitors. 216 53


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