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)

An aqueous suspension of n-butyl-p-aminobenzoate (BAB), a highly lipid-soluble congener of benzocaine, was applied epidurally in terminally ill cancer patients with intractable pain. The suspension consisted of 10% BAB and 0.025% of the nonionic surfactant polysorbate 80 in 0.9% sodium chloride. Twelve consecutive patients received epidural BAB because pain was uncontrollable either by palliative radiotherapy or oral or epidural administrations of analgesics. The catheter or injecting needle was positioned at the segmental level of the pain. Repeated epidural injections were administered. In all patients, long-lasting sensory blockade (segmental analgesia) occurred, accompanied by a marked reduction or even absence of pain. In all patients, treatment with epidural opioids, alone or combined with local anesthetics, was no longer necessary. Five of the 12 patients did not require further administration of oral opioids. Motor, bowel, and bladder function were well preserved. In 6 patients, extensive necropsy of the spinal cord and spinal nerves did not reveal pathomorphologic changes. The outer aspect of the dura showed signs of focal necrosis on microscopy, yet its collagen structure and thickness were unchanged. Epidurally, focal infiltrative reactions were seen. The epidural use of an extremely lipid-soluble--hence hydrophobic--local anesthetic, with an exceptionally low pKa (2.3), formulated in suspension of the base, is conceptually innovative and needs further investigation. The authors conclude that the epidural administration of a BAB suspension may be an effective alternative to the neurolytic agents alcohol and phenol and may replace procedures such as cordotomy. Further investigation to determine the safety of BAB in this patient group appears warranted.
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PMID:Long-lasting epidural sensory blockade by n-butyl-p-aminobenzoate in the terminally ill intractable cancer pain patient. 174 16

In a randomized double-blind study of 51 primigravida, we have examined the relative efficacies of bupivacaine, diamorphine or diamorphine with adrenaline given by the extradural route for relief of pain during labour. Group 1 (n = 18) received diamorphine 5 mg in 0.9% sodium chloride 8 ml; group 2 (n = 19) received diamorphine 5 mg in 0.9% sodium chloride 8 ml with 1:200,000 adrenaline; group 3 (n = 14) received 0.375% bupivacaine 8 ml. All patients received 0.375% bupivacaine 8 ml as a supplement after the initial analgesia had subsided. Patients in all groups had satisfactory and comparable analgesia 20 min after the initial injection. However, after 60 min and up to 8 h, analgesia was superior in group 2 as assessed by linear analogue pain scores, with statistical significance at 4, 6 and 8 h. Groups 1 and 2 required bupivacaine supplements less frequently than group 3 (P less than 0.001). There were no serious adverse effects in any group, but pruritus was a feature in the diamorphine groups. Diamorphine 5 mg may be used as an alternative to bupivacaine 0.375% 8 ml in the first stage of labour and provides a longer duration of action. The addition of adrenaline 1:200,000 appears to augment both the quality and duration of analgesia.
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PMID:Extradural diamorphine with adrenaline in labour: comparison with diamorphine and bupivacaine. 181 29

Pudendal block is a well established method of achieving analgesia during the second stage of labor. Whenever a large amount of a local anesthetic has to be injected in well vascularized tissue, local anesthetic drugs with low systemic toxicity should be used, to minimize side effects. This means that prilocaine is the drug of choice. It is well known that the metabolites of prilocaine induce methemoglobinemia, and thus the question arises as to whether the methemoglobinemia affects the fetus. PATIENTS AND METHODS. Pudendal block was achieved with 2 x 10 ml prilocaine 1% in each of 17 mothers. Plasma concentrations of the local anesthetic in the second stage of labor were determined by gas chromatography in blood samples drawn from the mother and the newborn at the moment of childbirth. In addition, the time course of methemoglobinemia was determined by capillary blood samples from the neonate up to 6 h. To evaluate methemoglobinemia in the newborn, 125 microliters heparinized capillary blood was diluted with 200 microliters 0.9% sodium chloride; methemoglobin was detected by absorbance spectrometry. RESULTS. Before the pudendal block maternal methemoglobin concentrations were about 0.2% of the total hemoglobin concentration and within the physiological range. At the moment of delivery it was increased only to a small extent, without statistical significance. In the neonates mean methemoglobin concentrations were about 1% of total hemoglobin immediately after delivery, increasing up to 1.8% in the next 2 h and then decreasing continuously in all. At the moment of childbirth maternal mean prilocaine concentrations were 0.57 micrograms/ml on an average and 0.29 micrograms/ml in the newborn. DISCUSSION. With respect to systemic toxicity, prilocaine is the drug of choice in local anesthetic procedures when a long duration of anesthesia is not required; it guarantees short latency and adequate relief of pain. Methemoglobinemia induced by its metabolites is not a contraindication for its use in humans. Formerly prilocaine was judged to be contraindicated in pregnant women during delivery because of the small redox capacity of fetal erythrocytes. Our study, however, demonstrates that 200 mg prilocaine for pudendal block does not induce methemoglobinemia in newborns to any significant extent. One explanation for this may be the increased renal elimination of local anesthetics in newborns and the low fetomaternal ratio.
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PMID:[Does the development of methemoglobin in the newborn infant affect the suitability of prilocaine for pudendal anesthesia? A clinical study in the peripartum phase]. 277 73

A new fluorinated derivative of N-propylnormetazocine, N-(3-fluoropropyl)-N-normetazocine (1) was synthesized. 1 was similar to the unfluorinated analog 3 in its ability to compete with (3H)-naltrexone for binding sites in rat brain membranes and its potency in antagonizing morphine analgesia in rats. Competition of both compounds against (3H)-naltrexone was little affected by the presence of sodium chloride, a characteristic frequently exhibited by opiate antagonists. Morphine analgesia in rats was measured by suppression of locomotion and vocalization responses to footshock. The ability of 1 to antagonize morphine analgesia in rats was similar to that of 3. Neither 1 nor 3 showed any evidence of agonist activity in rats at doses as high as 1.0 mg/kg (the highest dose tested). These results suggest that 1, labeled with 18F, may be useful for in vivo studies of the opiate receptor using positron emission tomography (PET).
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PMID:N-(3-Fluoropropyl)-N-normetazocine, a potentially useful opiate antagonist for opiate receptor studies with positron emission tomography (PET). 299 87

Arterial blood pressure, blood gas tensions (PaCO2, PaO2), and pH (pHa) were determined in 16 adult, nonpregnant Holstein cows (620 +/- 54 kg) given subarachnoid injection of a 5% procaine hydrochloride solution at the T13-L1 intervertebral space. Analgesia, as determined by response to superficial and deep muscular pinpricks at the L1 dermatome, was delayed (onset) 7 to 15 minutes, and it lasted (duration) 28 to 83 minutes. Thoracolumbar analgesia extending between spinal cord segments T9 and L4 on 1 or both sides of the spine produced significant (P less than 0.05) increases in heart rate and decreases in respiratory rate, but otherwise had no effect (P less than 0.05) on systolic, diastolic, and mean arterial blood pressures, PaCO2, PaO2, and pHa. Similarly, no significant changes (P less than 0.05) of physiologic variables were observed in a control group of 5 cows given a subarachnoidal injection of 0.9% sodium chloride solution at 1 hour before procaine hydrochloride was injected. It was concluded that the unsedated, healthy cow tolerates segmental subarachnoid analgesia between spinal segments T9 and L4 well and that this analgesia is not adversely affected by hypoxemia, respiratory acidosis, or hypotension.
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PMID:Effects of segmental subarachnoid analgesia on arterial blood pressure, gas tensions, and pH in adult conscious cows. 679 4

Hemodynamic measurements, arterial and mixed venous blood gas tensions, and pH were determined in 13 adult, nonpregnant Holstein cows (511.3 +/- 77.3 kg) after subarachnoid injection of a 5% procaine hydrochloride solution (av dosage level of 0.162 +/- 0.026 mg/kg) at the thoracolumbar (T13-L1) intervertebral space. Segmental analgesia occurred within 8 to 12 minutes after completing the procaine HCl injection and extended between spinal cord segments T7 and L3 on both sides of the spinal column. The average duration of analgesia, as determined by the cows' responses to superficial and deep muscular pinpricks, was 35.8 +/- 8.5 minutes (25 to 60 minutes, min-max). Subarachnoid injection of procaine HCl caused a significant (P less than 0.05) increase in heart rate and significant (P less than 0.05) decreases in pulse pressure and rectal temperature. Cardiac output, stroke volume, left ventricular stroke work, left ventricular minute work, total peripheral resistance, arterial blood pressure, arterial and mixed venous blood gas tensions, pH, oxygen transport, oxygen uptake, PCV, and total solids did not change significantly (P greater than 0.05) from base-line values. Similarly, no significant changes (P greater than 0.05) were observed in a group of 5 control cows after subarachnoid injection of sodium chloride solution (1.5 ml, 0.9%) at the T13-L1 intervertebral space. Segmental subarachnoid analgesia caused minimal circulatory disturbance and was well tolerated by adult, conscious, unsedated cows.
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PMID:Hemodynamic and respiratory effects of segmental subarachnoid analgesia in adult Holstein cows. 710 18

The effects of epidural morphine for pain relief after orthopaedic surgery of the lower extremity were examined in 60 patients. Intraoperative analgesia was achieved with epidural administration of 2% mepivacaine. The patients were divided in a double-blind, random fashion into 3 groups. Group I received 2 mg morphine base (2.63 mg morphine hydrochloride) in 10 ml 0.9% sodium chloride, Group II received 2 mg morphine base in 10 ml 5% glucose, and Group III, 10 ml 5% glucose as placebo. The quality of analgesia was judged by 1) the amount of i.m. pentazocine (0.5-1 mg/kg) required during the first 24 h, and 2) the analysis of a visual analog scale. The duration of epidural morphine analgesia was 13 +/- 9.4 h. For supplementary postoperative analgesia, the patients in Group I required a mean dose of 24 mg, Group II 18 mg, and Group III 48 mg of pentazocine (P less than 0.001 and 0.05 respectively) within the first 12 h. The solution (glucose or normal saline) had no influence on morphine effectiveness. The side effects were urinary retention in 8 patients (20%) and pruritus in one (3%). It is concluded that 2 mg of morphine base administered epidurally is an effective method of postoperative pain relief in orthopaedic patients.
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PMID:[Investigations on epidural morphine. Efficacy, solvent, analgesic supplementation]. 712 77

In this study we aimed to investigate clinically whether morphine acts on the peripheral nervous system directly. Twenty adult patients, who were scheduled for upper extremity surgery under tourniquet, had intravenous regional anesthesia. They were divided into two groups: one group was given 30 ml of 1% prilocaine plus 10 ml of 0.9% sodium chloride (P group) and the other group was given 30 ml of 1% prilocaine plus 6 mg morphine sulfate in 10 ml of 0.9% sodium chloride (P/M group). The onset of analgesia and anesthesia and recovery from anesthesia and analgesia were investigated in both groups. In the P/M group, the onset of analgesia and anesthesia was statistically faster and the recovery from anesthesia and analgesia was statistically slower than in the P group (P < 0.05). We conclude that morphine is clinically effective in the peripheral nervous system at this dosage range.
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PMID:Morphine/prilocaine combination for intravenous regional anesthesia. 748 46

This prospective, double-blind study examined the antiemetic effectiveness of the addition of droperidol to a morphine solution for use in patient-controlled analgesia in a group of 50 patients undergoing elective lumbar laminectomy. The addition of 20 mg droperidol to 120 mg morphine in 60 ml saline given by a Baxter 'Infusor' patient-controlled analgesia device reduced the incidence of vomiting as compared to the addition of sodium chloride from 42.8% to 12.5% (p = 0.028) and of nausea from 71.4% to 29.2% (p = 0.005). The proportion of patients requiring rescue antiemetic therapy was reduced from 47.6% to 16.7% (p = 0.025) and the time interval to the first use of rescue antiemetic agent was significantly prolonged (p = 0.029). The use of droperidol was associated with an increased degree of sedation during the first 12 h after operation.
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PMID:The antiemetic effectiveness of droperidol during morphine patient-controlled analgesia. 761 77

We have studied the analgesic effects of somatostatin during surgery and its influence on the plasma glucose levels and the liver enzyme profile in 40 ASA 1 or 2 patients undergoing surgery for carcinoma of the gastrointestinal tract. Each patient received either somatostatin bolus 3.5 micrograms.kg-1 intravenously plus an infusion of somatostatin 3.5 micrograms.kg-1.h-1, or sodium chloride 0.9% as a placebo in a double-blind manner. Anaesthesia was induced with propofol 1 mg.kg-1 followed by a continuous infusion of propofol in a stepwise declining regimen. Vecuronium was used for muscular relaxation. Fentanyl 100 micrograms was administered intravenously in bolus doses for analgesia during surgery as required. Blood samples were taken at 10 min pre-induction, 5 min postintubation, 5, 30, 60, 120 min postincision and 30 min post-recovery for plasma glucose levels. Blood samples were also taken at 10 min pre-induction, 120 min postincision and 24 h postoperatively for liver enzymes. The total requirement for fentanyl in the control group was significantly higher (p < 0.001) than in the group that received somatostatin. Eight out of 20 patients in the study group required no additional analgesia intra-operatively. The changes in blood glucose values followed the same pattern in both groups. There was a tendency for liver enzymes to increase in both groups. Although this increase was less in the study group, this change was not statistically significant.
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PMID:Somatostatin and total intravenous anaesthesia. Assessment of analgesic requirements during surgery and the effects on liver enzymes. 765 56


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