Glycopyrrolate is frequently administered in combination with neostigmine to reverse a neuromus- cular blockade. The dosage was well established at 1/5 of neostigmine. But the authers have often observed a delayed manifestation of relative bradycardia after such a recommended dosage. This is not mentioned in the literature, but this may be due to an insufficient observation period. The authors monitored the change of pulse rate for 1 hour after the administration of the recom. mended dose. Further, the data wIns compared with that obtained after studies of lower and higher doses. The doses were 0.004, 0.008 and 0.012mg/kg of glycopyrrolate with 0.04mg/kg of neostigmine. 1) At all doses, bradycardia relative to the pre-reversal pulse rate was progressive until 30 minutes after injection. 2) As the glycopyrrate dose was increased the degree of bradycardia decreased (-24.7, -20.5, - 15.0 at 30 min.). 3) There was no difference in the immediate change in the pulse rate between the dcsages of 0.008 and 0.012 mg/kg. Change occured at 9 mins. 4) At dosages of 0.004 and 0.008 mg/kg, the pulse rates at 60 min were comparable to their ward pulses, but at a dosage of 0.012 mg/kg, the pulse rate was 8.5 beats/min higher.
Bradycardia ; Glycopyrrolate* ; Heart Rate* ; Neostigmine*

The hypothesis that administration of neostigmine in divided doses might accelerate the antagonism of nuromuscular blockade was investigated. Neostigmine 0.05mg/kg was adminsitered either in a single bolus dose (Group I, n=10) or in an initial dose of 0.01 mg/kg 1 minute later (Group II, n=10), 2 minutes later (Group III, n=10) and 3 minutes later (Group IV, n=10) for antagonism of vecuronium- induced blockade. Reversal was attepted at 10 percent spontaneous recovery of twitch height. The mean time (+/-SE) from the first injection of the drug until the train-of-four(TOF) ratio value had reached 0. 75 was signifincantly longer in Group II and IV (594.8+/-63.9 seconds and 555.6+/-22.2 seconds respectively) than Group I and III (380.6+36.0 seconds and 357.8+/-44.2 seconds respectively). It is concluded that adminstration of neostigmine in divided doses with 0. 01 mg/kg and 0.04 mg/kg did not produce a significantly faster reversal of residual vecuronium-induced neuromuscular blockade as compared to a single bolus administration.
Neostigmine* ; Neuromuscular Blockade ; Vecuronium Bromide*

BACKGROUND: A question was whether it was preferable to give the reversal agent when profound block was present or wait for some spontaneous recovery before antagonizing the block. This study has been conducted to evaluate the reversal effects of neostigmine with divided doses in the rabbits after pancuronium when profound relaxation(PTC=O) or the first twitch of TOF stimulation was appeared (TOF,T1) was confirmed. METHODS: Rabbits(n=60) were randomly allocated to 5 groups. After pancuronium 0.2 mg/kg intravenously, spontaneous recovery was evaluated in group 1. When the profound relaxation(PTC=O) was confirmed at 5 min. after pancuronium, neostigmine 50 ug/kg with atropine 20 ug/kg were injected in group 2. At that time, neostigmine 10 ug/kg with atropine 4 ug/kg were injected and after 3 min. neostigmine 40 ug/kg with atropine 16 ug/kg were injected in group 3. When TOF, Tl was confirmed, neostigmine 50 ug/kg with atropine 20 ug/kg were injected in group 4. At that time, neostigmine and atropine were injected in group 5 as the same way of group 3. RESULTS: The mean time from injection of pancuronium to 95% recovery was 98.9 min. in group 1, 60.3 min. in group 2, 50.9 min. in group 3, 71.0 min. in group 4 and 67.1 min. in group 5. The recovery index was significantly reduced when neostigmine was injected at TOF,T1(p<0.05). The recovery time after neostigmine with divided doses was reduced, but there was no significant difference. CONCLUSIONS: The results of present study suggested that total recovery time was reduced when neostigmine was injected earlier with divided doses than single dose unrelated to profound relaxation.
Atropine ; Muscle Relaxation* ; Neostigmine* ; Pancuronium ; Rabbits* ; Relaxation

BACKGROUND: Sugammadex is a novel neuromuscular reversal agent, but its associated hypersensitivity reaction and high cost have been obstacles to its widespread use. In the interest of reducing the necessary dosage of sugammadex, the reversal time of the combined use of sugammadex and neostigmine from moderate neuromuscular blockade were investigated. METHODS: The patients enrolled ranged in age from 18 to 65 years old with American Society of Anesthesiologists class 1 or 2. The subjects were randomly assigned into one of the four groups (Group S2, S1, SN, and N; n = 30 per group). The reversal agents of each groups were as follows: S2 - sugammadex 2 mg/kg, S1 - sugammadex 1 mg/kg, SN - sugammadex 1 mg/kg + neostigmine 50 microg/kg + glycopyrrolate 10 microg/kg, N - neostigmine 50 microg/kg + glycopyrrolate 10 microg/kg. The time to recovery of the train-of-four (TOF) ratio was checked in each group. RESULTS: The time to 90% recovery of TOF ratio was 182.6 +/- 88.9, 371.1 +/- 210.4, 204.3 +/- 103.2, 953.2 +/- 379.7 sec in group S2, S1, SN and N, respectively. Group SN showed a significantly shorter recovery time than did group S1 and N (P < 0.001). However, statistically significant differences between the S2 and SN groups were not be observed (P = 0.291). No hypersensitivity reactions occurred in all groups. CONCLUSIONS: For the reversal from rocuronium-induced moderate neuromuscular blockade, the combined use of sugammadex and neostigmine may be helpful to decrease the recovery time and can also reduce the required dosage of sugammadex. However, the increased incidence of systemic muscarinic side effects must be considered.
Glycopyrrolate ; Humans ; Hypersensitivity ; Incidence ; Neostigmine* ; Neuromuscular Blockade*

The authors have experience of a case of prolonged paresis following administration of galamine triethiodide to a patient undergoing reoperation. The muscular weakness continued for 20 hours, necessitating artificial ventilation intermittently. It was reversed by neostigmine.
Humans ; Muscle Weakness ; Neostigmine ; Paresis* ; Reoperation* ; Ventilation

The purpose of this study is to investigate the effects of doxapram on the rates of spontaneous and neostigmine-induced recovery from neuromuscular block with vecuronium and atracurium. Following intravenous injection of either vecuronium (40 patients) or atracurium (40 patients), recovery index (RI) was measured without administering either doxapram or neostigmine (Group 1), or after administration of a combination of neostigmine 40 ug/kg and doxapram 1 mg/kg (Group 2), neostigmine 40 ug/kg (Group 3) or doxapram 1 mg/kg (Group 4) when twitch tension returned to 25% block of train of four response, each of the four group had 10 patients. The results were such that RI was significantly prolonged after vecuronium in the presence of doxapram compared with Group 1 (13.5 min vs 8.2 min). There was no significant difference in the RI after atracurium in the presence of doxapram compared with Group 1 (7.0 min vs 7.1 min). There was rapid recovery which was significant when neostigmine was administered with or without doxapram (2.4 min vs 2.3 min respectively after vecuronium; 2.3 min vs 2.4 min respectively after atracurium). The authors conclude that administration of doxapram in situation where neuromuscular block with vecuronium is not adequately antagonized does not contribute to rapid recovery from neuromuscular block.
Atracurium* ; Doxapram* ; Humans ; Injections, Intravenous ; Neostigmine ; Neuromuscular Blockade ; Vecuronium Bromide*

BACKGROUND: Rapid and complete reversal of neuromuscular blockade (NMB) is desirable at the end of surgery. Sugammadex reverses rocuronium-induced NMB by encapsulation. It is well tolerated in Caucasian patients, providing rapid reversal of moderate (reappearance of T2) rocuronium-induced NMB. We investigated the efficacy and safety of sugammadex versus neostigmine in Korean patients. METHODS: This randomized, safety assessor-blinded trial (NCT01050543) included Korean patients undergoing general anesthesia. Rocuronium 0.6 mg/kg was given prior to intubation with maintenance doses of 0.1-0.2 mg/kg as required. Patients received sugammadex 2.0 mg/kg or neostigmine 50 microg/kg with glycopyrrolate 10 microg/kg to reverse the NMB at the reappearance of T2, after the last rocuronium dose. The primary efficacy endpoint was the time from sugammadex or neostigmine administration to recovery of the train-of-four (TOF) ratio to 0.9. The safety of these medications was also assessed. RESULTS: Of 128 randomized patients, 118 had evaluable data (n = 59 in each group). The geometric mean (95% confidence interval) time to recovery of the TOF ratio to 0.9 was 1.8 (1.6, 2.0) minutes in the sugammadex group and 14.8 (12.4, 17.6) minutes in the neostigmine group (P < 0.0001). Sugammadex was generally well tolerated, with no evidence of residual or recurrence of NMB; four patients in the neostigmine group reported adverse events possibly indicative of inadequate NMB reversal. CONCLUSIONS: Sugammadex was well tolerated and provided rapid reversal of moderate rocuronium-induced NMB in Korean patients, with a recovery time 8.1 times faster than neostigmine. These results are consistent with those reported for Caucasian patients.
Anesthesia, General ; Glycopyrrolate ; Humans ; Intubation ; Neostigmine* ; Neuromuscular Blockade* ; Recurrence

The interaction between succinylcholine(SCC) and non-depolarizer; atracurium or vecuronium, was investigated in 36 cats of either sex using the sciatic nerve-anterior tibialis muscle preparation. And also, its relation to the pseudocholinesterase activity was examined. The duration of action of vecuronium(6.5+/-1.3 to 7.3+/-2.2 minutes) in cats pretreated with SCC was greater than those(2.0+/-0.6 minutes) in non-pretreated cats. However, SCC had no influence on the duration of atracurium. The serum pseudocholinesterase activity was decreased after the injection of atracurium or neostigmine in contrast to vecuronium. The authors conclude that the prior administration of SCC prolongs the duration of vecuronium but not that of atracurium, and pseudocholinesterase activity is not related to the prolonging effect of SCC.
Animals ; Atracurium* ; Cats* ; Neostigmine ; Pseudocholinesterase ; Succinylcholine* ; Vecuronium Bromide*

When antagonism to neuromuscular block is needed, glycopyrrolate is the new anticholinergic drug emplyed to counteract the muscarinic action of neostigmine. To know the effect on heart rate after an injection of glycopyrrolate and neostigmine mixture, we observed the changes in heart rate after injection of the mixtures and changing the ratio of glycopyrrolate(0.2mg/vial) to neostigmine(0.5mg/smpul) using 2 to 1, 2 to 1.5, 1 to 1, 1.5 to 2 and 1 to 2 during halothane anesthesia. The result of this study showed that the heart rates were more stable in the group given the ratio of glycopyrrolate 1 vial(0.2mg) to neostigmine 1 ampule(0.5mg) than any other gorups.
Anesthesia ; Glycopyrrolate* ; Halothane ; Heart Rate* ; Heart* ; Neostigmine* ; Neuromuscular Blockade

BACKGROUND: The reversal of neuromuscular blocker might be accelerated if the anticholinesterase was administered in divided doses. This study has been conducted to evaluate the correct ratio of divided doses of neostigmine for the rapid recovery in the rabbits after pancuronium when the profound relaxation(PTC=0) was confirmed. METHODS: Rabbits(n=60) were randomly allocated to 6 groups. After pancuronium 0.2 mg/kg intravenously, spontaneous recovery was evaluated in group 1. When the profound relaxation(PTC=O) was confirmed at 5 min. after pancuronium, neostigmine 50 ug/kg was injected as a bolus in group 2. At that time, neostigmine was given at 10 ug/kg followed by 40 ug/kg 3 min. later in group 3. At that time, neostigmine was given at 20 ug/kg followed by 30 ug/kg 3 min. later in group 4. At that time, neostigmine was given at 30 ug/kg followed by 20 ug/kg 3 min. later in group 5. At that time, neostigmine was given at 40 ug/kg followed by 10 ug/kg 3 min. later in group 6. RESULTS: The mean time from injection of pancuronium to 95% recovery was 99.3 min. in group 1, 59.8 min. in group 2, 53.2 min. in group 3, 51.5 min. in group 4, 50.8 min. in group 5 and 41.1 min. in group 6. The recovery index was significantly reduced in group 6(p<0.05). CONCLUSIONS: We conclude that the recovery time is reduced when neostigmine is administered in divided doses: a larger priming dose followed by a smaller bolus at profound relaxation.
Muscle Relaxation* ; Neostigmine* ; Neuromuscular Blockade ; Pancuronium* ; Pharmacokinetics ; Rabbits* ; Relaxation