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At least 19 recordsLinked to original sources
PubMed1980

Glycopyrrolate-neostigmine and atropine-neostigmine mixtures affect postanesthetic arousal times differently.

Atropine-neostigmine and glycopyrrolate-neostigmine mixtures used in 54 premedicated patients for reversal of non-depolarizing neuromuscular blockade were compared for their effects on postanesthetic arousal times. Anesthesia was induced in all patients with thiopental and was maintained with N2O-O2. Atropine-neostigmine significantly delayed arousal for the first 30 minutes following cessation of anesthesia and reversal of neuromuscular blockade. The difference between the two mixtures following reversal of neuromuscular blockade is attributed to the fact that atropine is a tertiary amine that crosses the blood-brain barrier and delays arousal, whereas glycopyrrolate is a quaternary ammonium compound that does not cross this barrier.

Adult↗
PubMed1977

Glycopyrrolate-neostigmine mixture for antagonism of neuromuscular block: comparison with atropine-neostigmine mixture.

Glycopyrrolate, a new anticholinergic agent, was evaluated and compared with atropine. Glycopyrrolate 0.2 mg to neostigmine 1.0 mg was found to be safe and effective. The heart rates remained more stable with glycopyrrolate, and the frequency of arrhythmia, which was both transient and of no consequence, was similar in the two groups. The antisialogogue action of glycopyrrolate was superior to that of atropine.

Anesthesia, General↗
PubMed1995

The effect of neostigmine on twitch tension and muscle relaxant concentration during infusion of mivacurium or vecuronium.

BACKGROUND: An investigation suggested that neostigmine may not effectively antagonize mivacurium, presumably because neostigmine impairs mivacurium's metabolism. However, the effect of neostigmine on mivacurium's metabolism in vivo has not been reported. Therefore, the effect of neostigmine on neuromuscular function and plasma mivacurium concentrations during constant mivacurium infusion was determined. METHODS: Mivacurium was infused in five patients to maintain 90% depression of adductor pollicis twitch tension, then 50 micrograms/kg intravenous neostigmine was administered without altering the mivacurium infusion. Peak twitch tension after neostigmine, plasma cholinesterase activity, and mivacurium concentrations before and after neostigmine were measured. Five additional patients were given 50 micrograms/kg neostigmine to antagonize block due to continuous infusions of vecuronium. RESULTS: Neostigmine produced less antagonism of mivacurium (39 +/- 11%) than of vecuronium (54 +/- 9%, P < 0.05). Neostigmine decreased plasma cholinesterase activity and increased plasma concentrations of the trans-trans and cis-trans stereoisomers of mivacurium (P < 0.05). CONCLUSIONS: Neostigmine is less effective at antagonizing the neuromuscular effect of mivacurium than that of vecuronium during constant infusion. Neostigmine increases plasma mivacurium concentrations, likely explaining its limited efficacy. Our results confirm that neostigmine impairs the metabolism of mivacurium in vivo and may explain the observation that neostigmine may not effectively antagonize mivacurium-induced block.

Adolescent↗
PubMed1994

[The optimal administration time for neostigmine following atracurium blockade. Kinetics of antagonists].

UNLABELLED: The aims of the study were: (1) to predict reversal time from intensive atracurium blockade; and (2) to determine the optimal time of neostigmine administration during recovery from atracurium blockade, i.e., the time at which the administration of neostigmine results in the shortest total recovery time (time from administration of last supplemental dose of atracurium to train-of-four [TOF] ratio 0.70), and at the same time results in the shortest time from administration of neostigmine to TOF ratio 0.70. METHOD: The spontaneous and neostigmine-facilitated recovery in 52 healthy women anaesthetised with thiopentone, fentanyl, droperidol, and nitrous oxide was followed. Post-tetanic count (PTC) of TOF stimulation of the ulnar nerve and mechanomyography were used for monitoring neuromuscular transmission. The neuromuscular blockade was induced with atracurium 0.6 mg/kg and supplemental doses of 0.15 mg/kg were given when the first twitch response in the TOF (TH1) had recovered to 20%. Neostigmine 0.036 mg/kg body weight was given at different levels of neuromuscular blockade to 37 of the patients. RESULTS: Multiple regression analyses including pre-reversal time (time from administration of the last atracurium dose to neostigmine administration), PTC, weight, and age of the patients suggest that pre-reversal time is the best predictor of reversal time: reversal time = 27.3 min - (0.89 x pre-reversal time [min]; (SEE = 6.0 min). If pre-reversal time is unknown, PTC can be used: reversal time = 24 min - (4.5 x ln PTC) at time of reversal); (SEE = 6.8 min). Total recovery time was 47 min (SEM = 2.0 min, n = 15) in the patients allowed to recover spontaneously, and 29 min (SEM = 1.2 min, n = 29) in the patients reversed by neostigmine; the difference of 18 min (SE diff 2.0 min) was significant (P < 0.0005). The level of blockade indicated by PTC (1-24) at the time of reversal had no influence on the total recovery time. The spontaneous recovery times from reappearance of TH1 and TH1 = 10% to TOF ratio 0.70 were 29.2 min (SEM = 1.7 min) and 24.4 min (SEM = 2.6 min), respectively. DISCUSSION: The results suggest that pre-reversal time is the strongest predictor of reversal time when neostigmine is administered during intense atracurium blockade. To achieve the optimal time-saving effect, neostigmine must be given 18 min (the time saved by giving neostigmine) plus 7 to 11 min (needed for neostigmine to reach its peak effect), giving a total of 25 to 29 min before TOF ratio 0.70. As TH1 is between 1% and 10% 25 to 29 min before TOF ratio 0.70 is reached during spontaneous recovery, the optimal level of neuromuscular blockade for neostigmine administration in atracurium blockade is when TH1 is between 1% and 10%. CONCLUSION: Reversal time can be predicted as 27.3 min - (0.89 x prereversal time (min), and the optimal time of neostigmine administration in atracurium blockade appears to be when TH1 is 1%-10%.

Adult↗
PubMed2002

Assessment of predictors of response to neostigmine for acute colonic pseudo-obstruction.

OBJECTIVE: Acute colonic pseudoobstruction (ACPO) most commonly develops after surgery, with narcotic administration, or in association with severe illness. Most cases resolve with conservative management. Colonoscopic decompression may be required in patients failing to respond to conservative treatment. Neostigmine has been proposed as an effective treatment for ACPO as an alternative to colonoscopic decompression. We sought to identify factors associated with spontaneous resolution of ACPO and to identify variables associated with a response to i.v. administration of neostigmine for the treatment of ACPO. METHODS: Retrospective analysis of Mayo Clinic's diagnostic index revealed all patients who developed ACPO between July, 1999 and September, 2001 at the Mayo Clinic Medical Center. We separately analyzed those patients who did not resolve ACPO with conservative management and to whom i.v. neostigmine was administered. Patient records were abstracted for demographic data, etiology of ACPO, management, and response to treatment. RESULTS: A total of 151 patients were identified with ACPO between July, 1999 and September, 2001; 117 patients (77%) had spontaneous resolution of symptoms. Of the 34 "nonresolvers," 18 patients received neostigmine, whereas 16 did not receive neostigmine. Of those 16 patients, 11 required colonoscopic decompression, two underwent surgery, and three died of underlying illness. "Spontaneous resolvers" were less likely to be taking narcotics (59% vs 74%, p = 0.08). Of the 16 nonresolvers who did not receive neostigmine, only one had a contraindication to neostigmine use. Of the 18 patients that who received neostigmine, 16 patients (89%) had prompt evacuation (<30 min) of flatus or stool. Sustained clinical response to neostigmine was noted in 11 of 18 (61%); the remaining seven patients (39%) required colonoscopic decompression or surgery for recurrent or persistent colonic dilation. Neostigmine-responders were more likely to be older (mean age, 76 yr vs 54 yr, p = 0.03), than nonresponders. Preneostigmine cecal diameter did not differ significantly between responders (median, 12 cm) and nonresponders (median, 13 cm), p = 0.9. Median time to resolution of ACPO in spontaneous resolvers was 4 days compared to 2 days in patients responding to neostigmine; p = 0.038. CONCLUSIONS: Most patients with ACPO respond to conservative treatment. Female gender and older age are associated with a response to neostigmine in those patients who do not respond to conservative management. Neostigmine appears to be under-used in patients with ACPO who do not have a true contraindication to its use.

Acute Disease↗
PubMed1995

Phase I safety assessment of intrathecal neostigmine methylsulfate in humans.

BACKGROUND: In dogs, sheep, and rats, spinal neostigmine produces analgesia alone and enhances analgesia from alpha 2-adrenergic agonists. This study assesses side effects and analgesia from intrathecal neostigmine in healthy volunteers. METHODS: After institutional review board approval and informed consent, 28 healthy volunteers were studied. The first 14 volunteers received neostigmine (50-750 micrograms) through a #19.5 spinal needle followed by insertion of a spinal catheter. The remaining 14 volunteers received neostigmine through a #25 or #27 spinal needle without a catheter. Safety measurements included blood pressure, heart rate, oxyhemoglobin saturation, end-tidal carbon dioxide, neurologic evaluation, and computer tests of vigilance and memory. Analgesia in response to ice water immersion was measured. RESULTS: Neostigmine (50 micrograms) through the #19.5 needle did not affect any measured variable. Neostigmine (150 micrograms) caused mild nausea, and 500-750 micrograms caused severe nausea and vomiting. Neostigmine (150-750 micrograms) produced subjective leg weakness, decreased deep tendon reflexes, and sedation. The 750-micrograms dose was associated with anxiety, increased blood pressure and heart rate, and decreased end-tidal carbon dioxide. Neostigmine (100-200 micrograms) in saline, injected through a #25 or #27 needle, caused protracted, severe nausea, and vomiting. This did not occur when dextrose was added to neostigmine. Neostigmine by either method of administration reduced visual analog pain scores to immersion of the foot in ice water. CONCLUSIONS: The incidence and severity of these adverse events from intrathecal neostigmine appears to be affected by dose, method of administration, and baricity of solution. These effects in humans are consistent with studies in animals. Because no unexpected or dangerous side effects occurred, cautious examination of intrathecal neostigmine alone and in combination with other agents for analgesia is warranted.

Adult↗
PubMed1998

A multi-center study of intrathecal neostigmine for analgesia following vaginal hysterectomy.

BACKGROUND: Intrathecal neostigmine injection produces analgesia in volunteers and reduces hypotension from intrathecal bupivacaine in animals. Initial clinical trials with neostigmine studied doses of more than 100 microg, but animal studies suggest that smaller doses may be effective. In addition, all controlled clinical trials of neostigmine have come from one Brazilian university. This multicenter, placebo-controlled trial investigated the effects of 25-75 microg intrathecal neostigmine on analgesia and blood pressure in women undergoing vaginal hysterectomy. METHODS: After institutional review board approval was obtained at the three university centers, and after patients gave informed consent, 92 women scheduled for vaginal hysterectomy were randomized to receive an intrathecal injection of 2 ml bupivacaine, 0.75%, in dextrose plus either 1 ml saline or 25, 50, or 75 microg neostigmine. Blood pressure, heart rate, pain and nausea (both assessed by visual analog scale), and intravenous morphine use were recorded during surgery and at specified intervals afterward. RESULTS: Morphine use was reduced similarly by all doses of neostigmine. Only the 75-microg dose of neostigmine increased the nausea score in the recovery room. The incidence of treatment for nausea was greater in patients receiving neostigmine (61%) than in those receiving saline placebo (29%) and was unaffected by neostigmine dose. Neostigmine did not reduce the incidence of hypotension from bupivacaine. CONCLUSION: These data in patients after vaginal hysterectomy suggest that analgesia from intrathecal neostigmine may occur at doses less than 50 microg. In these doses, neostigmine does not reduce spinal bupivacaine-induced hypotension but may increase the need for treatment of nausea.

Adult↗
PubMed2000

Transdermal nitroglycerine enhances spinal neostigmine postoperative analgesia following gynecological surgery.

BACKGROUND: Intrathecal neostigmine causes analgesia by inhibiting the breakdown of acetylcholine. Experimental data suggest that the production of endogenous nitric oxide is necessary for tonic cholinergic inhibition of spinal pain transmission. The purpose of this study was to determine whether association of transdermal nitroglycerine would enhance analgesia from a low dose of intrathecal neostigmine in patients undergoing gynecologic surgery during spinal anesthesia. METHODS: Forty-eight patients were randomized to one of four groups. Patients were premedicated with use of 0.05-0.1 mg/kg intravenous midazolam and received 15 mg bupivacaine plus 1 ml test drug intrathecally (saline or neostigmine, 5 microgram). Twenty to 30 min after the spinal puncture, a transdermal patch of either 5 mg nitroglycerin or placebo was applied. The control (Con) group received spinal saline and transdermal placebo. The neostigmine group received spinal neostigmine and transdermal placebo. The nitroglycerin group received spinal saline and a transdermal nitroglycerine patch. Finally, the neostigmine-nitroglycerin group received spinal neostigmine and transdermal nitroglycerine. Pain and adverse effects were evaluated using a 10-cm visual analog scale. RESULTS: Patients in the groups were similar regarding age, weight, height, and American Society of Anesthesiologists status. Sensory level to pin prick at 10 min, surgical duration, anesthetic duration, and visual analog scale score for pain at the time of administration of first rescue medication were statistically the same for all groups. The time to administration of first rescue analgesic (min) was longer in the neostigmine-nitroglycerin group (550 min; range, 458-1,440 min; median, 25-75th percentile) compared with the other groups (P < 0.001). The neostigmine-nitroglycerin group required fewer rescue analgesics in 24 h than did the control group (P < 0.0005), whereas the neostigmine group required less analgesics compared with the control group (P < 0.02). The incidence of perioperative adverse effects (nausea, vomiting, headache, back pain) was similar among groups (P > 0.05). CONCLUSION: Although neither intrathecal 5 microgram neostigmine alone nor transdermal nitroglycerine alone (5 mg/day) delayed the time to administration of first rescue analgesics, the combination of both provided an average of 14 h of effective postoperative analgesia after vaginoplasty, suggesting that transdermal nitroglycerin and the central cholinergic agent neostigmine may enhance each other's antinociceptive effects at the dose studied.

Administration, Cutaneous↗
PubMed2003

Antinociceptive effect of low-dose intrathecal neostigmine combined with intrathecal morphine following gynecologic surgery.

BACKGROUND: The purpose of this study was to determine whether combination of 1-5 microg intrathecal neostigmine would enhance analgesia from a fixed intrathecal dose of morphine. METHODS: A total of 60 patients undergoing gynecologic surgery were randomized to one of five groups. Patients received 15 mg bupivacaine plus 2 ml of the test drug intrathecally (saline, 100 microg morphine, or 1-5 microg neostigmine). The control group received spinal saline as the test drug. The morphine group received spinal morphine as test drug. The morphine + 1 microg neostigmine group received spinal morphine and 1 microg neostigmine. The morphine + 2.5 microg neostigmine group received spinal morphine and 2.5 microg neostigmine. Finally, the morphine + 5 microg neostigmine group received spinal morphine and 5 microg neostigmine. RESULTS: The groups were demographically similar. The time to first rescue analgesic (minutes) was longer for all patients who received intrathecal morphine combined with 1-5 microg neostigmine (median, 6 h) compared with the control group (median, 3 h) (P < 0.02). The morphine group (P < 0.05) and the groups that received the combination of 100 microg intrathecal morphine combined with neostigmine (P < 0.005) required less rescue analgesics in 24 h compared with the control group. The incidence of perioperative adverse effects was similar among groups (P > 0.05). CONCLUSIONS: The addition of 1-5 microg spinal neostigmine to 100 microg morphine doubled the duration to first rescue analgesic in the population studied and decreased the analgesic consumption in 24 h, without increasing the incidence of adverse effects. The data suggest that low-dose spinal neostigmine may improve morphine analgesia.

Adult↗
PubMed2004

Epidural neostigmine produces analgesia but also sedation in women after cesarean delivery.

BACKGROUND: Intrathecal neostigmine produces analgesia but also nausea, limiting its utility. In contrast, epidural administration of neostigmine has been suggested to produce postoperative analgesia without nausea in nonpregnant patients. The purpose of this study was to examine the dose range for efficacy and side effects of epidural neostigmine in women at cesarean delivery receiving combined spinal-epidural anesthesia. METHODS: After institutional approval and informed consent, 80 patients for elective cesarean delivery were given combined spinal-epidural anesthesia with 8 mg hyperbaric bupivacaine plus 10 microg fentanyl. Patients were randomized to receive either saline or 75, 150, or 300 microg neostigmine (n = 20 per group) in 10 ml saline after cord clamping. Pain, morphine consumption, and side effects were monitored for 24 h. RESULTS: Global pain assessment for the first 24 h was reduced from 5.4 +/- 0.2 in the saline group to 3.0-3.5 +/- 0.3 in the neostigmine groups, dose independently. Correspondingly, global satisfaction with neostigmine was also improved (P < 0.05). Nausea and morphine consumption were similar among groups. Intraoperative shivering and sedation were increased in the 300-microg neostigmine group only (P < 0.05), and postoperative sedation was increased by neostigmine in a dose-independent fashion (P < 0.05). CONCLUSIONS: Epidural neostigmine produced modest analgesia in women after cesarean delivery. In contrast with previous reports, which focused primarily on nausea, these data suggest that epidural neostigmine can also produce mild sedation for several hours. These data suggest a limited role for single bolus-administration epidural neostigmine for analgesia after cesarean delivery. They also support future study of epidural neostigmine for obstetric analgesia.

Adult↗
PubMed1995

Postoperative analgesia from intrathecal neostigmine in sheep.

Spinal neostigmine produces analgesia in chronically prepared rats, but not in sheep. However, since pain itself activates bulbospinal inhibitory pathways, neostigmine may be more effective in the postoperative period. We examined in sheep the antinociceptive effect of intrathecal neostigmine in the acute postoperative period and determined the muscarinic receptor subtype activated by neostigmine. A cervical intrathecal catheter was inserted via a laminotomy in 14 sheep that then received, in random order 1 mg of spinal neostigmine or saline on postoperative Day 1 and the other injection on postoperative Day 2. Three additional sheep received, on separate days, intrathecal neostigmine alone or with the muscarinic receptor subtype-specific antagonists pirenzepine (M1) 2 mg or AFDX-116 (M2) 2 mg. Antinociception was tested using a mechanical stimulus after each injection. Baseline withdrawal threshold did not change postoperatively. Intrathecal neostigmine, but not saline caused antinociception on both of the first two postoperative days. In contrast, intrathecal neostigmine caused no antinociception in another similar study performed at least 5 days after surgery. Pirenzepine, but not AFDX-116, abolished antinociception from neostigmine, suggesting an action on M1 subtype muscarinic receptors. Intrathecal neostigmine is antinociceptive in sheep during the acute postoperative period, and these data suggest that spinal cholinergic tone, and hence intrathecal neostigmine's analgesic effect, may be enhanced during the acute postoperative period.

Analgesia, Epidural↗
PubMed1995

Reversal of residual neuromuscular block with neostigmine at one to four hours after a single intubating dose of vecuronium.

The purpose of this study was to measure the degree of residual neuromuscular block at different times after a single dose of vecuronium, and to evaluate the effectiveness of two different doses of neostigmine in antagonizing this residual block. Train-of-four (TOF) ratios were examined for up to 4 h after a single dose of vecuronium, 0.1 mg/kg, in 60 patients during nitrous oxide/isoflurane/fentanyl anesthesia. The effect of neostigmine, 40 micrograms/kg, was studied at 1,2,3, or 4 h. The effect of neostigmine, 20 micrograms/kg, was studied at 2 or 4 h after the vecuronium. Before neostigmine administration, the TOF ratio was less than 0.75 in 17 patients (including one patient at 4 h). Neostigmine produced an increase in TOF ratio in 52 patients and a decrease in 8. The TOF ratio decreased after neostigmine only, at 2,3, or 4 h after vecuronium, when the TOF ratio was > or = 0.9 and when neostigmine 40 micrograms/kg was administered. One patient, at 1 h, had a TOF ratio of 0.00 and this did not reach 0.75 until 57 min after neostigmine, 40 micrograms/kg. There was a high incidence (50%) of adverse cardiovascular effects after both doses of neostigmine. In making the decision as to whether neostigmine should be administered, the risk to the patient of residual neuromuscular block must be balanced against the adverse cardiovascular effects of the neostigmine.

Adult↗
PubMed1996

Intravenous ketamine or fentanyl prolongs postoperative analgesia after intrathecal neostigmine.

The purpose of this study was to determine whether intravenous (i.v.) ketamine would enhance analgesia from intrathecal (IT) neostigmine compared with combining i.v. fentanyl with IT neostigmine. Sixty patients undergoing vaginoplasty under spinal anesthesia were assigned to one of six groups (n = 10). Patients were premedicated with midazolam plus the i.v. test drug. The IT drugs were 20 mg bupivacaine plus saline or 50 micrograms neostigmine. The control group (CG) received saline i.v. and IT. The neostigmine control group (NCG) received saline i.v. and neostigmine IT. The ketamine group (KG) received ketamine 0.2 mg/kg i.v. and saline IT, and the ketamine neostigmine group (KNG), ketamine i.v. and neostigmine IT. The fentanyl group (FG) received fentanyl 1 microgram/kg i.v. and saline IT, and the fentanyl neostigmine group (FNG), fentanyl i.v. and neostigmine IT. The time to first rescue analgesic was longer for the FNG and KNG compared with the CG, with less rescue analgesic consumption (P < 0.02 and P < 0.01, respectively). Only the FNG had significantly intraoperative nausea/vomiting (P < 0.02). In conclusion, the combination of i.v. ketamine and IT neostigmine results in prolonged postoperative analgesia and less intraoperative nausea and vomiting than the combination of i.v. fentanyl and IT neostigmine.

Analgesia↗
PubMed1993

Neostigmine counteracts spinal clonidine-induced hypotension in sheep.

BACKGROUND: Intraspinal clonidine injection produces analgesia free of respiratory depression, but also decreases blood pressure and causes sedation. Spinal neostigmine injection alone increases blood pressure in animals and enhances clonidine-induced analgesia. METHODS: To test whether neostigmine would alter clonidine-induced hypotension, nine chronically prepared sheep received intrathecal injections of saline or neostigmine (150, 300, 1,000 micrograms) followed in 15 min by 200 micrograms clonidine. RESULTS: Clonidine plus saline decreased mean arterial pressure by 12 +/- 3% associated with small, statistically nonsignificant decreases in heart rate, cardiac output, and systemic vascular resistance. Prior injection of neostigmine diminished hypotension 60 min after clonidine injection in a dose-dependent manner. To further define the time course and pharmacology of this interaction, seven other sheep received intrathecal saline, neostigmine (1,000 micrograms), or neostigmine plus methylatropine (1,000 micrograms) 75 min prior to 200 micrograms clonidine. With this longer interval between injections, neostigmine abolished clonidine-induced hypotension, and this protective effect was inhibited by methylatropine. To test whether rostral spread of neostigmine in cerebrospinal fluid would alter its hemodynamic effects, we injected intrathecal neostigmine into the upper cervical site. Intrathecal neostigmine increased mean arterial pressure and heart rate at this site to a degree similar to that in the thoracic area, with no effect on behavioral or arterial blood gas tensions. CONCLUSIONS: These data are consistent with neostigmine's counteraction of clonidine-induced hypotension by a spinal muscarinic mechanism and support investigation of spinal alpha 2-adrenergic-cholinergic combinations for pain therapy.

Animals↗