Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0011570 (depression)
 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The perfect analgesic regimen is constantly sought, no matter how labor is conducted. The quest for an effective drug that will afford maximum relaxation and pain relief with minimum interruption of any natural homeostatic mechanism is a foremost subject in present obstetric analgesics research. Synthetic alternatives are being offered, promising perfect compatibility with the clinician's demands. Nalbuphine, a semisynthetic narcotic agonist-antagonist analgesic of the penanthren series, is supposed not to be liable to cause respiratory depression and is expected to have fewer side effects. A double-blind, randomised prospective study of 137 patients who received 10 mg nalbuphine or 50 mg pethidine i.v. during the active phase of labor in term was carried out. Maternal cardiovascular variables, pain intensity, progress of labor and fetal heart rate during labor were related to side effect and neonatal outcome (1- and 5-min Apgar scores and umbilical venous pH). Neither regimen showed an advantage over the other. Data analysis points to a possible transient depressive effect induced by nalbuphine on the fetal or neonatal central nervous system.
 ...
PMID:Intravenous pethidine and nalbuphine during labor: a prospective double-blind comparative study. 176 17

The analgesic profile of epidural nalbuphine for postoperative pain relief and the impact of local anaesthetic choice upon this profile was investigated in 58 patients undergoing elective Caesarean delivery under epidural anaesthesia. Patients were randomized to receive either lidocaine 2% with 1:200,000 epinephrine or 2-chloroprocaine 3% for perioperative anaesthesia, followed by either 10, 20, or 30 mg of epidural nalbuphine administered at the first complaint of postoperative discomfort. Postoperative analgesia was quantitated on a visual analogue (VAS) scale, and by the time from the epidural opioid injection until the first request for supplemental pain medication. The duration of analgesia after lidocaine anaesthesia followed by 10, 20 or 30 mg nalbuphine was 77 (53-127) min, 205 (110-269) min, and 185 (116-241), respectively (median, 95% confidence interval, P less than 0.01, 20 and 30 mg vs 10 mg). Following 2-chloroprocaine anaesthesia, VAS remained consistently elevated: the median duration of analgesia was only 30-40 min and did not differ among the three doses of nalbuphine. Side-effects consisted only of somnolence, and were noted only following lidocaine anaesthesia. Somnolence was observed in 0, 20% and 50% of those receiving 10 mg, 20 mg and 30 mg of nalbuphine respectively (NS). No evidence of respiratory depression was noted in any patient. It is concluded that 20 or 30 mg of epidural nalbuphine provides analgesia for only two to four hours following Caesarean delivery with lidocaine anaesthesia, but anaesthesia with 2-chloroprocaine resulted in minimal or no analgesia from this opioid. Nalbuphine appears to be a disappointing agent for epidural use after Caesarean delivery.
 ...
PMID:Epidural nalbuphine for analgesia following caesarean delivery: dose-response and effect of local anaesthetic choice. 191 55

As most patients undergoing pulmonary surgery by postero-lateral thoracotomy have decreased preoperative pulmonary function, efficient postoperative analgesia is mandatory. Nalbuphine, a new agonist-antagonist opioid analgesic, and nefopam were compared in a double blind trial involving 60 patients. Intravenous injections of 0.3 mg.kg-1 of either drug were started when the patient evaluated his pain as being above 60 mm on a visual scale graduated from 0 to 100 mm. Repeated injections were carried out at the same dose, at the patient's request, after a minimal interval of 3 h for nalbuphine, and 6 h for nefopam. Analgesia was assessed by the visual scale, and by the patient's verbal appraisal. The respiratory and cardiovascular repercussions were evaluated clinically, and by monitoring breathing rate, blood gases, systolic and diastolic blood pressures, heart rate, and consciousness. Nalbuphine provided a convenient analgesia to all patients whereas analgesia with nefopam was insufficient in 15 out of 30 patients. No significant respiratory depression with either drug occurred. Nefopam led to a 30% increase in heart rate for one hour (p less than 0.01). Whereas patients given nalbuphine were more drowsy, although easily aroused, (p less than 0.001), nefopam was responsible for adverse effects (sweating, nausea, tachycardia with pallor, vertigo, malaise) requiring the exclusion of 7 patients from the study. Nalbuphine, although not ideal, would therefore seem to be a better analgesic than nefopam in thoracotomy patients.
 ...
PMID:[Analgesic and respiratory effects of nalbuphine during the immediate postoperative period in thoracotomy]. 218 3

Nalbuphine hydrochloride, an agonist-antagonist opioid, is reported to reverse the respiratory depression of moderate doses of fentanyl (20 micrograms.kg-1) and still provide good analgesia. We report four patients having abdominal aortic aneurysm repair in which we attempted to reverse the respiratory depression of large doses of fentanyl (50-75 micrograms.kg-1) with nalbuphine (0.3 mg.kg-1, 0.1 mg.kg-1 or 0.05 mg.kg-1). Nalbuphine reversed respiratory depression in all four patients and the respiratory rate increased from 10 to 23 breaths per minute, end-tidal CO2 decreased from 7.0 +/- 0.3 per cent to 5.6 +/- 0.7 per cent, and peak inspiratory pressure after 0.1 seconds increased from 4 +/- 1.4 to 13 +/- 2.6 mmHg. However, hypertension, increased heart rate, and significant increase in analogue pain scores accompanied reversal of respiratory depression. Agitation, nausea, vomiting, and cardiac dysrhythmias also were observed frequently. We do not recommend the use of nalbuphine to facilitate early extubation of the trachea after large doses of fentanyl for abdominal aortic surgery.
 ...
PMID:Side effects of nalbuphine while reversing opioid-induced respiratory depression: report of four cases. 165

We studied the effect of nalbuphine on the ventilatory and occlusion pressure responses to carbon dioxide rebreathing in six healthy male volunteers (mean age 25.5 yr) in a single-blind laboratory study. On four separate days volunteers were assigned randomly to receive either placebo (0.9% sodium chloride) or three i.v. doses of nalbuphine (15, 30 and 60 mg 70 kg-1), followed 90 min later by naloxone 0.4 mg 70 kg-1. Duplicate rebreathing tests were performed and the mean intercept at PE'CO2 7 kPa and the slopes of the linear relationship between inspiratory minute ventilation (Vl) or occlusion pressure (P0.1) with PE'CO2 were measured. Nalbuphine significantly decreased the mean intercept of the Vl (P less than 0.01) and P0.1 (P less than 0.05) responses, but caused no changes in the slopes. No significant difference between the doses was noted, suggesting that an Effect maximum (E'max) for respiratory depression was reached with a dose of approximately 15 mg 70 kg-1. Naloxone was less effective in antagonizing the depression in Vl at the higher dose of nalbuphine. Similar P0.1 values were associated with the same inspiratory flow rate (1 litre s-1) before and after drug treatment, suggesting that nalbuphine acts centrally to depress ventilation. Sedation increased significantly following each dose of nalbuphine (P less than 0.001). No demonstrable difference between the doses was shown, suggesting an Effect maximum (E'max) for sedation was reached at about 15 mg 70 kg-1. Administration of nalbuphine was associated with pain at the injection site, dizziness, dreaming, nausea and vomiting. Cardiovascular stability was maintained in all subjects.
 ...
PMID:Effect of nalbuphine hydrochloride on the ventilatory and occlusion pressure responses to carbon dioxide in volunteers. 250 65

Nalbuphine reverses opioid-induced respiratory depression, but the effect on analgesia is unclear. The analgesic interaction between subcutaneous (sc) nalbuphine and intrathecal morphine in conscious, male, Sprague-Dawley rats implanted with chronic intrathecal catheters was investigated. Nalbuphine (10 mg/kg) injected 30 min after intrathecal morphine (4 micrograms) significantly antagonized the effect of morphine in the tail flick test. The antagonism was rapid in onset and persisted beyond the experimental period of 240 min. The magnitude and the duration of the effect were comparable to that observed with sc naloxone (1 mg/kg). In contrast to the results in the tail flick test, nalbuphine enhanced the effect of intrathecal morphine in the noninflamed paw pressure test. Nalbuphine (10 mg/kg) alone had no effect on the time course of tail flick latency but significantly increased paw pressure threshold during the 15-90 min interval after sc injection. Nalbuphine (0.5 mg/kg, sc) alone had no antinociceptive effect in either pain test and did not antagonize the antinociceptive effect of intrathecal morphine (4 micrograms) in the tail flick test. However, sc nalbuphine (0.5 mg/kg), injected 30 min after intrathecal morphine (1.5 micrograms), significantly enhanced the effect of morphine in the paw pressure test compared with intrathecal morphine + sc saline-treated rats. The results indicate a complex analgesic interaction between intrathecal morphine and sc nalbuphine. The net analgesic effect during the interaction was determined by the following: 1) the doses of morphine and nalbuphine; 2) the time after nalbuphine administration; and 3) the nature of the nociceptive stimulus. At lower doses, sc nalbuphine appeared to potentiate the effect of intrathecal morphine in the noninflamed paw pressure test.
 ...
PMID:A study of the analgesic interaction between intrathecal morphine and subcutaneous nalbuphine in the rat. 281 64

Nalbuphine is a potent analgesic with a low side effect and dependence profile in animals and man. Nalbuphine is distinguished from other agonist/antagonist analgesics in having greater antagonist activity and fewer behavioral effects at analgesic doses than pentazocine, butorphanol or buprenorphine. At equi-analgesic doses, nalbuphine is quantitatively similar to nalorphine in regard to its large ratio of antagonist to analgetic activity. Clinical studies have confirmed this balance of strong antagonist to analgesic activity. Nalbuphine has been shown to effectively antagonize the respiratory depressant activity of narcotic analgesics while concomitantly adding to their analgetic responses. Unlike nalorphine or pentazocine, nalbuphine produces few overt behavioral or autonomic effects in animals at doses over 300 times its analgesic range. These findings are confirmed by clinical results which show that nalbuphine produces few psychotomimetic effects, even at elevated dose levels, in contrast to nalorphine or pentazocine. Nalbuphine produces limited respiratory depression in animals and in man. Significant cardiovascular effects have not been found. Nalbuphine was found to produce significantly less inhibition of gastrointestinal activity than any of the clinically useful narcotic or agonist/antagonist analgesics tested in animals. Nalbuphine's analgetic effects are reversed by naloxone doses similar to those which reverse nalorphine's agonist effects. Results in this and other tests suggest that nalbuphine is primarily a kappa-agonist/mu-antagonist analgesic. Unlike pentazocine or buprenorphine, nalbuphine does not suppress the narcotic abstinence syndrome in partly-withdrawn morphine-dependent animals or man. Rather, due to nalbuphine's strong antagonist activity, analgesic-range doses of nalbuphine severely exacerbate the withdrawal syndrome in partly-withdrawn mice, monkeys and humans. Nalbuphine also precipitates a strong abstinence response in non-withdrawn morphine-dependent animals and man. In post-addict humans, analgesic-range doses of nalbuphine are perceived as minimally morphine-like, but higher doses are judged to be progressively more nalorphine-like (i.e. dysphoric), which further limits nalbuphine's abuse potential in drug-seeking individuals. Primary dependence studies have demonstrated that physical dependence is possible at high dose levels that produce marked side effects. Other studies show that dependence is unlikely to be of significance within nalbuphine's usual analgesic range. Six-month studies in patients with chronic pain have confirmed that analgesic tolerance or physical dependence is uncommon.(ABSTRACT TRUNCATED AT 400 WORDS)
 ...
PMID:Nalbuphine. 298 29

The authors studied the respiratory and analgesic effects of nalbuphine (0.21 mg/kg, intravenous), naloxone (0.014 mg/kg, intravenous), and placebo (normal saline) when given after morphine (0.21 mg/kg, intravenous) in a double-blind, randomized fashion. Resting end-tidal CO2 (PETCO2), ventilatory and occlusion pressure responses to CO2 rebreathing, and pain threshold were measured in 12 healthy adult volunteers before, 5 min, and 30 min after morphine. Nalbuphine, naloxone, or saline were administered 55 min after morphine, and the above measurements were repeated 5 min later (60 min after morphine) as well as 90, 120, 180, and 240 min after morphine. Whereas naloxone reversed respiratory depression as measured by all three respiratory parameters, nalbuphine either further depressed (resting PETCO2) or did not affect (ventilatory and occlusion pressure responses to CO2 rebreathing) respiratory drive. Morphine produced a significant elevation of the pain threshold. Significant decreases in the pain threshold were seen only after naloxone. Saline and nalbuphine did not significantly alter the pain threshold. The data indicate that nalbuphine may not reliably antagonize moderate doses of morphine.
 ...
PMID:Failure of nalbuphine to antagonize morphine: a double-blind comparison with naloxone. 308 51

The postoperative treatment of pain in children is often inadequate: Periphal acting analgetics are not sufficient, opioids are believed to be dangerous because of their respiratory depression. Nalbuphine and tramadol are two narcotics with only a few side effects. The aim of this trial was to investigate the efficacy and safety of these drugs in postoperative pain therapy in children aged 1-9 years. 30 children in each group received in a double-blind and randomized manner either 0.15-0.2 mg/kg nalbuphine or 0.75-1.0 mg/kg tramadol im. Pain intensity and sleep-awake behaviour were documented by a visual analogue scale for 24 h. After 1 h 70% of the patients in both groups had no pain and were sleeping. There was no change in heart rate and systolic blood pressure. Only the diastolic blood pressure decreased as did the respiratory rate, while the tcpCO2 estimated in some patients remained constant. Narcotic reinjections were necessary three times in the nalbuphine group and four times in the tramadol group. Typical opioid side effects were found to be equal in both groups.
 ...
PMID:[Nalbuphine and tramadol for the control of postoperative pain in children]. 309 99

The authors anesthetized 18 patients with good pulmonary and ventricular function for coronary artery bypass grafting with high doses of fentanyl. When the patients were arousable and their vital signs stable in the intensive care unit, the authors administered nalbuphine or placebo (randomly and double-blinded) until extubation criteria were met, and subsequently gave nalbuphine for analgesia. In one of ten placebo patients, tracheal extubation was accomplished without nalbuphine. This patient then retained CO2 and required nalbuphine; the other nine placebo patients could not be extubated after placebo trials and were given nalbuphine. In all other patients in both groups, tracheal extubation was successful following nalbuphine (median dose 60 micrograms/kg, range 30-180 micrograms/kg). One patient became renarcotized 4 h after tracheal extubation without an increase in plasma fentanyl concentration; he received an additional dose of nalbuphine and recovered without further incident. Nine patients required treatment with vasoactive agents or beta-blockers for hypertension or tachycardia associated with the administration of nalbuphine. Eight of 18 patients were not satisfied with nalbuphine analgesia, and required morphine for relief of their pain. Recurrent elevations of fentanyl concentrations in plasma were observed and appeared to be related to increasing motor activity. Nalbuphine is an effective opioid antagonist after fentanyl anesthesia, but its use is associated with side effects, and analgesia for the post-sternotomy patient may be unsatisfactory unless the dose is carefully titrated to the minimum required to antagonize respiratory depression.
 ...
PMID:Nalbuphine antagonism of fentanyl-induced ventilatory depression: a randomized trial. 327 86


1 2 3 4 Next >>