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)

Butorphanol, a new, totally synthetic morphinan, which is chemically related to naloxone, has been demonstrated to have both analgesic and narcotic antagonist properties. In rodent antiwrithing analgesic tests, butorphanol was 4 to 30 times more potent than morphine and dl-pentazocine, respectively. As an antagonist, butorphanol was about equivalent to nalorphine and 30 times more potent than dl-pentazocine. On the basis of the naloxone-induced mouse jumping test and the lack of substitution in withdrawn morphine-dependent mice, it is estimated that the potential for physical dependence of butorphanol will be less than that of dl-pentazocine but greater than that of nalorphine and dl-cyclazocine. Animal data also show that agonistic actions of butorphanol, such as respiratory depression and miosis, reach ceiling effects which are lower than those seen with morphine with an increase in dosage. Thus, butorphanol differed from morphine which exhibited agonist effects in a dose-related manner. Butorphanol showed weak to moderate central depressant properties at doses which were considerably higher (greater than 100 X) than those producing analgesia. Minimal cardiovascular and respiratory effects were seen with butorphanol in conscious dogs.
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PMID:The pharmacology of butorphanol, a 3,14-dihydroxymorphinan narcotic antagonist analgesic. 6 89

Enhancing effect of an opiate agonist-antagonist butorphanol (0.2 mg/kg) on sedation induced by medetomidine (80 micrograms/kg) was evaluated in pigs. Butorphanol significantly enhanced the depth of medetomidine-induced sedation and prolonged the duration of that assessed by posture score and spontaneous movement of pigs. The combination of medetomidine and butorphanol produced excellent muscle relaxation and moderate surface analgesia which was enough for procedures with mild pain in pigs.
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PMID:Enhancing effect of butorphanol on medetomidine-induced sedation in pigs. 147 68

Butorphanol (0.025, 0.05, 0.1, 0.2, 0.4, and 0.8 mg/kg of body weight, and placebo) was given SC to 8 healthy unmedicated dogs to determine its efficacy for visceral analgesia, using a colonic balloon for minimal threshold nociceptor stimulation. Degree of sedation; systolic, diastolic, and mean arterial pressure; and pulse rate were recorded. The highest 3 dosages, 0.2, 0.4, and 0.8 mg/kg, were found to be most effective, with 0.8 mg/kg the only dosage that was significantly different from control responses at the 45-minute interval. Duration of analgesia ranged from 23 to 53 minutes for all 6 dosages and dosing durations were not significantly different from one another. Blood pressures did not change, but pulse rate was significantly decreased by 0.8 mg of butorphanol/kg. We concluded that butorphanol is an effective visceral analgesic of relatively short duration in the dog.
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PMID:Dose response to butorphanol administered subcutaneously to increase visceral nociceptive threshold in dogs. 178 25

Butorphanol tartrate (Stadol; Anaquest, Madison, WI/Bristol-Meyers Squibb, Evansville, IN) is an analgesic possessing mixed agonist-antagonist activity at opiate receptors. Receptor specificity has been used to limit respiratory depression, gastrointestinal side effects, and reduce the risk of dependency. Theoretically it offers an advantage over traditional opiates such as morphine and meperidine in the treatment of moderate pain. Butorphanol has been used as a preoperative sedative and analgesic, as a supplement to balanced anesthesia, and for suppression of postanesthesia shaking. Other recognized uses include obstetric analgesia during labor and relief of moderate postpartum pain. In addition, butorphanol has been used effectively for conscious sedation. Its lack of euphoric effects may be useful in emergency medicine for clinical populations prone to drug-seeking behavior. Butorphanol has been used more recently for epidural analgesia or for intravenous patient-controlled analgesia when allergies to opiates exist. Since butorphanol is not a controlled substance, its use can reduce administrative liability for abuse and can lower the number of distribution records associated with Schedule II narcotics.
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PMID:Butorphanol tartrate (stadol): a review. 184 91

To determine the efficacy and the safety of epidural morphine or butorphanol combined with bupivacaine, 40 healthy parturients were studied during labor and delivery. All patients received an epidural test dose of 2 ml of 0.5% bupivacaine. Patients were then randomly assigned to receive one of four epidural regimens in a double-blind fashion: 0.25% bupivacaine + 1 mg butorphanol (Group I), 0.25% bupivacaine + 2 mg butorphanol (Group II), 0.25% bupivacaine + 2 mg morphine (Group III), or 0.25% bupivacaine alone (Group IV). Each group consisted of ten patients. All subsequent epidural injections were with plain 0.25% bupivacaine. Duration of analgesia was significantly longer for groups I, II, and III when compared to group IV (p less than or equal to .01); 139 +/- 111, 141 +/- 14, 199 +/- 29, and 96 +/- 6 minutes, X +/- SEM respectively. Quality of analgesia was significantly better in groups I, II, and III when compared with group IV. There were no differences between groups in duration of first and second stages of labor, uterine activity, or method of delivery. Thirty percent of patients in the morphine group (group III) developed mild pruritus that did not require any treatment. All neonates were vigorous at 5 minutes and had good Apgar Scores, umbilical cord acid base status, and Neurological Adaptive Capacity Scores. The authors conclude that adding small doses of either morphine or butorphanol to epidural bupivacaine during labor is effective and safe. Butorphanol may be preferable since none of the patients experienced pruritus.
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PMID:Epidural morphine or butorphanol augments bupivacaine analgesia during labor. 248 90

This study attempts to determine the analgesic properties of nalbuphine, pentazocine and butorphanol during labor and their potential effects on maternal and fetal blood gases and pH. Butorphanol analgesia was superior to either nalbuphine or pentazocine in relieving labor pain. The studied analgesics caused significant maternal respiratory acidosis and fetal metabolic acidosis. These acidotic changes were most marked with pentazocine, moderate with nalbuphine and minimal with butorphanol.
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PMID:Effect of some recent analgesics on labor pain and maternal and fetal blood gases and pH. 289 42

Premedication that provides sedation and analgesia is commonly used for patients undergoing endoscopic procedures. We studied the efficacy and safety of butorphanol and diazepam as preprocedure medications for patients having upper gastrointestinal endoscopy. To achieve an adequate level of sedation, patients receiving diazepam required a mean (+/- SEM) dose of 12.0 +/- 1.0 mg, whereas those receiving butorphanol required a mean dose of 4.8 +/- 0.4 mg. There were no differences between treatment groups in the overall assessment of sedation, the ease of performance of the endoscopic procedure, or vital signs during or following the procedure. Fifty-four percent of butorphanol patients and 48% of diazepam patients experienced at least one minor adverse event. Butorphanol in small doses can produce satisfactory sedation and analgesia for patients undergoing gastrointestinal endoscopic procedures.
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PMID:Randomized, prospective, double-blind clinical trial of butorphanol and diazepam in patients undergoing upper gastrointestinal endoscopy. 327 94

Butorphanol and meperidine, each combined with titrated diazepam, 10 to 20 mg, were compared in a randomized, double-blind trial for their sedative-analgesic effects. The fifty patients underwent multiple dental extractions under local anesthesia and sedation in an outpatient clinic. Butorphanol was significantly superior to meperidine with respect to the diazepam dose required to achieve the target level of sedation, the total diazepam dose administered, the clinical level of sedation, the surgeon's overall evaluations of effectiveness and of sedation level, and several patient evaluation parameters measured at discharge from the recovery room and at follow-up interview. All study drugs were well tolerated. Butorphanol offers clinical advantages over meperidine when combined with diazepam for sedation analgesia in outpatient oral surgery.
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PMID:Butorphanol/diazepam compared to meperidine/diazepam for sedation in oral maxillofacial surgery: a double-blind evaluation. 330 81

Patient-controlled analgesia (PCA) has been studied extensively for the treatment of postoperative pain using narcotic analgesics. Butorphanol, a nonnarcotic injectable analgesic, has not previously been investigated using this drug delivery mechanism. Twenty-five patients undergoing general abdominal surgery and general anesthesia used a PCA device with butorphanol as the analgesic agent. Most patients (84%) were able to obtain excellent postoperative pain relief. The role of butorphanol in the management of postoperative pain should be expanded to include patient-controlled drug delivery.
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PMID:Patient-controlled analgesia using butorphanol for postoperative pain relief: an open-label study. 334 98

The cardiopulmonary, sedative and analgesic effects of butorphanol tartrate and nalbuphine hydrochloride were evaluated in six adult crossbred Dorset sheep (Ovis aries). The animals were divided randomly into two groups of three. The first group received butorphanol tartrate (0.5mg/Kg s.c.) followed in 3 days by nalbuphine hydrochloride (1 mg/Kg, s.c.). The second group received nalbuphine followed in 3 days by butorphanol. Cardiopulmonary parameters were evaluated at baseline (once the animal had accommodated to restraint); immediately following analgesic administration; and at 15, 30, 60, 90 and 120 minutes after analgesic administration. No significant changes (alpha greater than .05) from baseline were seen in any of the measured cardiopulmonary parameters from either the butorphanol or nalbuphine groups. Butorphanol produced the most dramatic analgesic and sedative effects with onset of both within 15 minutes of administration and peak effects occurring 30 minutes post injection. The degree of analgesia was diminished at 120 minutes while the sedative effect returned to near baseline by 90 minutes. The nalbuphine group also showed an onset of analgesia 15 minutes post injection reaching a peak effect after 30 minutes. However, onset of sedation occurred 30 minutes post injection achieving a peak effect at 60 minutes which was markedly less than that of butorphanol. As in the butorphanol group, analgesia was diminished at 120 minutes.
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PMID:Cardiopulmonary effects of nalbuphine hydrochloride and butorphanol tartrate in sheep. 336 23


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