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)

A new analgesic, nefopam, is chemically distinct and pharmacologically unrelated to any presently known analgesic. A comparison was made of morphine and nefopam in 74 patients who required parenteral analgesia for moderate to severe postoperative and somatic pain, using a single administration, 2-dose level, double-blind design. A significant dose-response curve was obtained with nefopam and with morphine, and there was no significant deviation from parallelism. The time-effect curves for the 2 drugs were similar. The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine SO4. There were no adverse effects with nefopam and one adverse reaction to morphine.
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PMID:Nefopam and morphine in man. 110 31

The results of a controlled, double-blind clinical trial are reported demonstrating the potency of analgesia produced by orally and parenterally administered nefopam HCl in hospitalized patients with pain principally of skeletal and neuromuscular origin. The drug is an analogue of orphenadrine, consisting of a cyclization of the diphenhydramine molecule. A double-blind, crossover study was made of the analgesic effects of intramuscular doses of 20 mg nefopam HCl, 50 mg pethidine, and saline placebo in 20 patients. Nefopam and pethidine were found to be equally effective and statistically superior to placebo. A double-blind, randomized study was made of orally administered nefopam HCl, 60 mg t.i.d., for three days and of placebo t.i.d. for three days in 80 patients. Nefopam was distinctly superior to placebo in analgesic effectiveness, both in the initial single dose and in maintaining therapeutic benefit for the duration of the three-day trial. It was concluded that nefopam is a potent analgesic of novel structure and unique physiologic properties.
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PMID:Controlled clinical trial of oral and parenteral nefopam hydrochloride. A novel and potent analgesic drug. 110 59

Seven drugs administered im were evaluated to determine their efficacy in immobilizing captive agoutis. Ketamine HCl (63-83 mg/kg) and phencyclidine HCl (16.5-22.0 mg/kg) produced immobilization and analgesia. Phencyclidine administration was accompanied by numerous side effects and prolonged recovery. Xylazine HCl (3-70 mg/kg) and fentanyl-droperidol (0.28-1.11 ml/kg( produced varying degrees of ataxia and intermittent recumbency. Acetylpromazine, chlorpromazine, and promazine HCl were ineffective. Surgical anesthesia was successfully induced and maintained with halothane.
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PMID:An evaluation of sedatives and anesthetics in the agouti (Dasyprocta sp). 127 34

Four groups of mink were immobilized with medetomidine-HCl (MED) 0.1 mg/kg + ketamine (KET) 5 or 7.5 mg/kg at different ambient temperatures. The induction time, degree of immobilization and analgesia, rectal temperature, heart and respiration rates were recorded at intervals throughout the immobilization period. The animals were then given atipamezole-HCl (ATI) 0.5 mg/kg for reversal at different times after injection of MED/KET and the effects of the antagonist were evaluated. Subcutaneous administration of MED/KET induced complete immobilization in all 20 animals, and the highest dose was considered suitable for major surgery. Prolonged immobilization at low ambient temperatures (-10 to +5 degrees C) caused severe hypothermia in all animals. The mean rectal temperature had dropped to 37.8 degrees C and 32.1 degrees C at 15 and 85 min, respectively, after injection of MED/KET, significantly lower than the corresponding values for animals immobilized at room temperature. Intramuscular administration of ATI 20 or 40 min after injection of MED/KET rapidly remobilized the animals without apparent side-effects. Administration of ATI to animals recovering spontaneously 90 min after injection of MED/KET induced thermogenesis (shivering) in animals immobilized at a low ambient temperature, while no such effect was seen in animals immobilized at room temperature. One hour after injection of ATI, the rectal temperatures of all treated animals had returned to normal and there were no signs of abnormal behaviour.
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PMID:Immobilization of mink (Mustela vison) with medetomidine-ketamine and remobilization with atipamezole. 136 Dec 73

A combination of tiletamine HCl and zolazepam HCl is frequently used as an anesthetic, but little is known about the antinociceptive properties of tiletamine-zolazepam. The antinociceptive properties of tiletamine-zolazepam alone or combined with xylazine or butorphanol were determined in the adult male rate using the tail-flick test. Changes in tail-flick latency were determined at 15, 45, and 75 min after IP drug administration of sterile water, sodium pentobarbital, morphine, tiletamine-zolazepam, xylazine, butorphanol, and tiletamine-zolazepam plus xylazine or butorphanol. Tail-flick latency approximated 100% maximum possible effect (MPE) at 15-75 min postinjection in morphine-treated rats. Tiletamine-zolazepam, xylazine, and butorphanol alone, at any dose utilized, produced less than 50% MPE. However, the combination of tiletamine-zolazepam with butorphanol or xylazine increased tail-flick latency approximately three times greater than tiletamine-zolazepam alone. These results demonstrate that: a) consonant with earlier findings, analgesia and anesthesia are independent states; b) tiletamine-zolazepam is not an effective combination with respect to analgesia; but c) in concert with appropriate drugs, it can exhibit potent antinociceptive properties.
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PMID:Antinociceptive properties of tiletamine-zolazepam improved by addition of xylazine or butorphanol. 147 95

Iontophoresis is a method of transdermal administration of ionized drugs in which electrically charged molecules are propelled through the skin by an external electrical field. This was a prospective, randomized, single-blind study to determine the effectiveness of iontophoretically delivered morphine HCl for the control of postoperative pain. Thirty-eight patients who underwent total knee or hip replacement completed this clinical trial. Informed consent was obtained before surgery and patients were instructed on the use of a patient-controlled analgesia (PCA) device. Postoperatively, pain in the recovery room was initially controlled with IV meperidine, and thereafter with PCA therapy using meperidine, 2 mg/cc, with a dose of 10 mg IV and a lock-out period of 15 min. The dose was adjusted as necessary and the lock-out period remained the same. The number of patient requests and the dose (mg) administered was recorded hourly. On the morning following surgery, iontophoresis devices were attached for 6 hr to patients who received either morphine HCl or lactated ringers solution. During this period and for 12 hr following completion of iontophoresis, PCA analgesia remained available to patients. Venous blood samples for determination of morphine levels were obtained every 30 min during iontophoresis, then every 60 min for 2 hr following iontophoresis. Of the 38 patients, 17 received iontophoresed morphine, and 21 received iontophoresed lactated ringers. The morphine group utilized the PCA device more than the control group during the baseline period. However, following the institution of iontophoresis and continuing up to 12 hr following completion of iontophoresis, the morphine group used significantly less PCA meperidine to maintain analgesia than the control group (p = 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Iontophoretic delivery of morphine for postoperative analgesia. 153 78

Repeated postnatal treatment of rats with the dopamine receptor agonist, quinpirole results in exaggeration of selected behaviors that are induced by quinpirole in adulthood. To determine whether the antinociceptive response to quinpirole could be similarly enhanced, rats were treated daily from birth with quinpirole HCl (3.0 mg/kg per day i.p. x 28 days) and their response time in the hot plate analgesia test was determined at 4 months. An acute dose of quinpirole HCl (100 or 1000 micrograms/kg i.p.) produced an analgesic response in the neonatally primed rats and in the vehicle controls. More significantly, the effect was substantially greater in the quinpirole-primed group at each of these two doses of quinpirole. This effect of quinpirole was fully attenuated in both groups by treatment with the dopamine receptor antagonist, spiperone HCl (0.30 mg/kg i.p., 1 h before quinpirole). The analgesic effect of morphine sulfate (6.0 mg/kg i.p.) was not greater in the quinpirole-primed group. These findings demonstrate that the ontogenetic sensitization of quinpirole receptors results in enhanced antinociceptive responses to quinpirole in adulthood. This animal model may be useful for studying the involvement of dopamine systems in algesia and analgesia.
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PMID:Ontogenetic homologous sensitization to the antinociceptive action of quinpirole in rats. 168 67

The local anaesthetic bupivacaine could be very useful for analgesia in pediatric neurosurgery. Since systemic toxic reactions to bupivacaine are correlated with high plasma levels it was important, as an adjunct to clinical evaluation, to measure plasma bupivacaine. This report describes a high-performance liquid chromatography (HPLC) method for the quantitation of plasma bupivacaine. Sample preparation involves extraction into ether followed by back-extraction into HCl. After evaporation, the acid extract is redissolved and separated by reversed-phase chromatography. The assay is linear to 5 mg bupivacaine/L and shows excellent recovery and precision. With samples from children undergoing brain surgery following scalp infiltration with either 0.125% or 0.25% bupivacaine, plasma levels peak within 10 min, then fall rapidly to a plateau by 30 min. This plateau is maintained for at least 120 min. In no case did we find supposed toxic levels of bupivacaine.
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PMID:Determination of bupivacaine in plasma by high-performance liquid chromatography. Levels after scalp infiltration in children. 177 85

Continuous epidural anesthesia (CEA) is generally accepted as a routine method of regional anesthesia while there has been only limited application of continuous spinal anesthesia (CSA), due mainly to a lack of adequate spinal catheters. With the introduction of a new, ultra-thin spinal catheter (32 G) inserted via a thin puncture needle, some of the complications reported after CSA can be eliminated. We studied CSA versus CEA in lower-extremity operations. METHODS. We evaluated 33 patients in a prospective, randomized study. All were comparable with respect to age, anesthetic risk (ASA II-III), and pre-existing diseases. The only exclusion criterium was the presence of a coagulation disturbance. The CSA group consisted of 17 patients (mean age 75.5 +/- 0.1 year); 26 G puncture needle and 32 G catheter were used. The CEA group consisted of 16 patients (mean age 73.8 +/- 11.0 years); an 18 G puncture needle and 22 G epidural catheter with a stylet were inserted with the loss-of-resistance technique. Both catheters were placed with the patient in a sitting position and left in place for 24 h in order to administer local anesthetics (LA) for postoperative analgesia as required. Hemodynamic parameters-mean arterial pressure (MAP) and heart rate (HR)-were compared in each group at 5-min intervals for 30 min after administration of local anesthetic and at 10-min intervals during the operation. Additionally, the ECG, pulse oximetry, respiratory rate, diuresis, and blood gases were monitored. After placement of the catheter, patients in the CSA group received 1.9 ml (+/- 0.2) bupivacaine HCl 0.5%. Patients in the CEA group received 12.6 ml (+/- 2.5) bupivacaine HCl 0.5%. For statistical evaluation of the data we used mean values, standard deviation (+/-), the Kruscal-Wallis procedure, and Student's t-test for unpaired data. P less than 0.05 was considered significant. RESULTS. The mAPs in the CSA group generally remained lower than those of the CEA group. However, over the course of the operation as well as after repeated injections, the difference between the two groups decreased. Only at 5 min after administration of the initial dose was a statistically significant difference in blood pressures between the two groups observed. A clinically relevant, rapid decrease in blood pressure due to relatively high doses of LA was seen in 1 case in each group. The first reinjection of LA after the initial dose was after 1.9 h in the CSA group (bupivacaine HCl 0.5% 1 +/- 0.3 ml) and after 1.8 h in the CEA group (bupivacaine HCl 0.5% 4.5 +/- 1 ml). The total dose of bupivacaine in the CSA group was 0.18 ml/kg per hour versus 0.8 ml/kg in the CEA group. No post-dural puncture headache was observed in the CSA group. DISCUSSION. The catheter designed for CSA is easy to use, although because of its small diameter a certain manual dexterity is required. In addition, CSA resulted in a more rapid onset of action and more pronounced sensorimotor blockade than did CEA. Hemodynamic alterations and side effects were comparably low in both groups.
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PMID:[Continuous spinal anesthesia versus continuous epidural anesthesia in surgery of the lower extremities. A prospective randomized study]. 182 99

The disposition of bupivacaine and degree of analgesia following a 72 h interpleural infusion was investigated in 12 adult patients undergoing elective cholecystectomy. The infusion regimen of an initial interpleural bolus dose of 20 ml of 0.5% bupivacaine HCl with adrenaline (1:200,000) followed by continuous infusion at a rate of 8 ml h-1 of 0.25% plain bupivacaine HCl was designed to achieve continuous post-operative pain relief for 72 h. In practice an additional bolus dose (identical to the first) administered 5 h after infusion commencement was required to achieve adequate pain relief on the first postoperative day. The mean measured steady-state plasma bupivacaine concentration was 2.1 mg l-1 (s.d. +/- 0.54, range 1.3-3.2 mg l-1). Disposition parameters for bupivacaine measured for the infusion were calculated by non-compartmental methods and compared with previous values obtained after single and multiple interpleural bolus dose administration. No statistically significant differences were noted and, in particular, the systemic clearance of bupivacaine (mean 10.2 l h-1 s.d +/- 3.0; range 6.3-16.0 1 h-1) remained unchanged following the long-term interpleural infusion. Analgesia was deemed satisfactory throughout the entire post-operative period.
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PMID:The disposition of bupivacaine following a 72 h interpleural infusion in cholecystectomy patients. 193 77


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