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PubMed1982

I.m. or i.v. atropine or glycopyrrolate for the prevention of oculocardiac reflex in children undergoing squint surgery.

The frequency and nature of the oculocardiac reflex and its prevention by atropine or glycopyrrolate (i.m. and i.v.) has been studied in 160 children undergoing surgery for the correction of squint. Ninety per cent of those given no anticholinergic premedication exhibited the reflex. This was decreased to about 50% in those receiving the drugs i.m. Glycopyrrolate 7.5 micrograms kg-1 and atropine 15 micrograms kg-1 i.v. were effective in most instances, the latter being slightly better. However, glycopyrrolate was associated with tachycardia of smaller magnitude. The reflex was observed more often following traction on the medial rectus muscle.

Adolescent↗
PubMed1984

Comparison of i.v. glycopyrrolate and atropine in the prevention of bradycardia and arrhythmias following repeated doses of suxamethonium in children.

The effectiveness of administration of glycopyrrolate 5 and 10 micrograms kg-1 and atropine 10 and 20 micrograms kg-1 i.v. immediately before the induction of anaesthesia, to prevent arrhythmia and bradycardia following repeated doses of suxamethonium in children, was studied. A control group was included for comparison with the lower dose range of glycopyrrolate and atropine. A frequency of bradycardia of 50% was noted in the control group, but this was not significantly different from the frequency with the active drugs. Bradycardia (defined as a decrease in heart rate to less than 50 beat min-1) was prevented when the larger dose of either active drug was used. It is recommended that either glycopyrrolate 10 micrograms kg-1 or atropine 20 micrograms kg-1 i.v. should immediately precede induction of anaesthesia, in children, if the repeated administration of suxamethonium is anticipated.

Arrhythmias, Cardiac↗
PubMed1985

Antagonism of the muscarinic effects of edrophonium with atropine or glycopyrrolate. A comparative study.

The efficacy of atropine or glycopyrrolate in doses of 10 or 20 micrograms kg-1 and 5 or 10 micrograms kg-1, respectively, has been compared when administered to block the muscarinic effects of edrophonium 0.5 mg kg-1 administered for the reversal of neuromuscular blockade. Both doses of atropine and the higher dose of glycopyrrolate prevented any edrophonium-induced decreases in heart rate; glycopyrrolate at this dose was associated with tachycardia. Atropine and edrophonium could be safely administered together in a mixture. The control of oropharyngeal secretions was adequate even with the lower doses of both anticholinergic agents. Atropine 10 micrograms kg-1 appears to be a better anticholinergic agent for use with edrophonium.

Adult↗
PubMed1985

Comparison between glycopyrrolate and atropine in a mixture with neostigmine for reversal of neuromuscular blockade. Studies in patients following open heart surgery.

Atropine and glycopyrrolate were compared in a mixture with neostigmine for reversal of neuromuscular blockade in patients undergoing open heart surgery. In patients not receiving beta-blocking drugs, glycopyrrolate was shown to possess advantages over atropine in terms of a lower initial increase in heart rate, better protection against the muscarinic effects of neostigmine, and smaller increases in rate-pressure product. The concomitant administration of beta-adrenergic blocking therapy significantly attenuated the effect of reversal on heart rate and the differences between atropine and glycopyrrolate were not significant. There was no difference in the incidence of arrhythmias between patients who received beta-blocking drugs and those who did not.

Adrenergic beta-Antagonists↗
PubMed1987

Comparison of the effects of atropine and glycopyrrolate on cognitive function following general anaesthesia.

Tests of orientation, concentration and short-term visual memory were used to assess 72 patients 1 day before, and 2 days after, elective major surgery. Patients were premedicated with papaveretum and either atropine or glycopyrrolate, before receiving a standard general anaesthetic. Those who had received atropine showed significant postoperative short-term memory deficit (P less than 0.01), but no change in orientation or concentration. Those who had been given glycopyrrolate showed no significant cognitive changes after surgery. As glycopyrrolate does not cross the blood-brain barrier freely, these findings support the involvement of central cholinergic mechanisms in the deterioration of cognitive function in the postoperative period.

Adult↗
PubMed1998

The use of metoprolol and glycopyrrolate to prevent hypotensive/bradycardic events during shoulder arthroscopy in the sitting position under interscalene block.

UNLABELLED: Sudden profound hypotensive and/or bradycardic events (HBE) have been reported in >20% of patients undergoing shoulder arthroscopy in the sitting position under interscalene block anesthesia. Retrospective studies suggest that the administration of beta-blockers is safe and may decrease the incidence of these episodes. We performed a randomized, prospective study to evaluate prophylaxis of these events. One hundred fifty patients were randomized to one of three groups (placebo; prophylactic metoprolol to achieve a heart rate <60 bpm or a maximal dose of 10 mg; or prophylactic glycopyrrolate to achieve a heart rate >100 bpm or a maximal dose of 6 microg/kg) immediately after the administration of the interscalene block. Blood pressure control was achieved with IV enalaprilat as needed. The incidence of HBE was 28% in the placebo group versus 5% in the metoprolol group (P = 0.004). The rate of 22% in the glycopyrrolate group was not significantly different from placebo. Preoperative heart rate and arterial blood pressure, intraoperative sedation score, IV fluids, and enalaprilat use were similar in those patients who had a HBE compared with those who did not. Many aspects of this clinical setting are similar to tilttable testing for patients with recurrent vasovagal syncope, in which beta-adrenergic blockade with metoprolol has also been shown to be effective. We conclude that the Bezold-Jarisch reflex is the most likely mechanism for these events. IMPLICATIONS: Episodes of acute hypotension and bradycardia occur during shoulder arthroscopy in the sitting position under interscalene block. In this study, we demonstrate that metoprolol, but not glycopyrrolate, markedly decreases the incidence of these episodes when given prophylactically immediately after the administration of the block.

Adrenergic beta-Antagonists↗
PubMed1999

The effects of antagonizing residual neuromuscular blockade by neostigmine and glycopyrrolate on nausea and vomiting after ambulatory surgery.

UNLABELLED: The effects of neostigmine on the incidence of postoperative nausea and vomiting (PONV) are controversial. In this study, we evaluated the effects of neostigmine and glycopyrrolate on the incidence of PONV and the need for antiemetics in patients undergoing ambulatory surgery. One hundred healthy patients undergoing outpatient surgical procedures were included in the study. A standardized anesthetic technique was used for all patients. Patients were randomized to receive either mivacurium (n = 50) or rocuronium (n = 50) to achieve muscle paralysis. Bolus doses of mivacurium 2-4 mg or rocuronium 5-10 mg were administered to maintain one or two twitches of the train-of-four stimulation of the ulnar nerve at the wrist. After surgery, residual neuromuscular blockade was reversed with neostigmine 2.5 mg i.v. and glycopyrrolate 0.5 mg i.v. only if clinically deemed necessary (i.e., fade on train-of-four stimulation, inadequate tidal volume, reduced hand grip, or inability to maintain head lift). The incidence of PONV and the need for antiemetics were recorded in the post-anesthesia care unit (PACU), in the phase II unit, and 24 h after surgery. We compared patients who received neostigmine (n = 40) for reversal of residual neuromuscular blockade with those who did not (n = 60). More patients receiving rocuronium required reversal drugs than those receiving mivacurium (68% vs 10%). There were no differences in the incidence of nausea (18% vs 15%), vomiting (8% vs 12%), and the need for antiemetics (13% in both the groups) in the PACU between patients who received neostigmine and those who did not. In addition, the duration of PACU stay and the time to home-readiness were also similar between the groups. We conclude that, compared with rocuronium, the use of mivacurium decreases the need for reversal drugs. In addition, reversal of residual neuromuscular blockade with neostigmine does not increase the incidence of PONV or the need for antiemetic medications in patients undergoing ambulatory surgery. IMPLICATIONS: In this study, we showed that the incidence of postoperative nausea and vomiting and the need for antiemetics do not increase with the use of neostigmine and glycopyrrolate for reversal of residual muscle paralysis.

Adult↗
PubMed1998

Pre-emptive glycopyrrolate 0.2 mg and bradycardia during gynaecological laparoscopy with mivacurium.

In a prospective, randomized, double-blind, placebo-controlled trial, the effect of pre-emptive glycopyrrolate 0.2 mg given intravenously on the incidence of bradycardia in patients undergoing elective gynaecological laparoscopy with mivacurium neuromuscular blockade was investigated. Seven out of 32 (21.6%) control patients developed bradycardia (heart rate < 50 min-1), compared with 3 of 31 (9.6%) patients receiving glycopyrrolate (P = 0.4). Glycopyrrolate 0.2 mg, given immediately before induction in gynaecological laparoscopy with mivacurium, did not significantly reduce the incidence of intraoperative bradycardia.

Adult↗
PubMedDate not supplied

Reversal of neuromuscular blockade by glycopyrrolate and neostigmine. A study of the effects on lower oesophageal sphincter tone.

The effect of intravenous glycopyrrolate and neostigmine, a drug combination routinely given to antagonize non-depolarising neuromuscular blockade, on lower oesophageal sphincter tone was studied in twenty patients undergoing Caesarean section. Glycopyrrolate 0.6 mg and neostigmine 2.5 mg i.v. increased LOS pressure insignificantly by a mean of 0.2 kPa (P less than 0.1). In contrast, glycopyrrolate 0.6 mg and neostigmine 5 mg increased LOS pressure by a mean of 1.2 kPa (P less than 0.001). The latter dosage of this drug combination thus appears preferable in patients presenting for emergency surgery, if the integrity of the lower oesophageal sphincter is to be maintained during extubation and recovery from general anaesthesia.

Anesthesia, Obstetrical↗
PubMed1981

Effects of intravenous administration of glycopyrrolate and atropine in anaesthetised patients.

The effects of glycopyrrolate in doses of 5, 10 and 15 microgram/kg and atropine 10, 20 and 30 microgram/kg on heat rate and rhythm was studied in anesthetised patients. Both drugs produced a dose-related increase in heart rate. Glycopyrrolate was approximately twice as potent as atropine in increasing heart rate. The average time taken to achieve peak effect was 2-6 and 3-7 minutes for atropine and glycopyrrolate respectively, and this was significantly different. The smallest doses of both drugs were generally associated with supraventricular dysrhythmias, whereas these were mainly ventricular following the highest dose of both drugs.

Adult↗
PubMed1983

Dose-response studies on glycopyrrolate and atropine in conscious cardiac patients.

The dose-heart rate response relationship for the two anticholinergics, atropine and glycopyrrolate, were studied in non-anaesthetised patients about to undergo coronary artery surgery. Two methods were used, the administration of increasing doses to different groups of patients, and an incremental dose technique in the same patient. Both drugs increased heart rate in a dose-related manner with glycopyrrolate being approximately twice as potent as atropine. Glycopyrrolate is as effective as atropine in correcting bradycardia prior to open heart surgery.

Atropine↗
PubMed1987

Glycopyrrolate compared with atropine in association with ketamine anaesthesia.

Atropine and glycopyrrolate given intravenously before the induction of a ketamine anaesthesia to diminish salivary secretion were compared for their effect on psychotomimetic side-effects, awakening time and heart rate. Though atropine is a tertiary amine that crosses the blood-brain barrier, which glycopyrrolate as a quaternary ammonium compound does not, it did not increase the incidence of psychotomimetic side-effects nor did it significantly prolong the awakening time after ketamine anaesthesia. During intubation the increase in heart rate was significantly higher following atropine than following glycopyrrolate.

Anesthesia↗
PubMed2006

Effect of anticholinergics (atropine, glycopyrrolate) and prokinetics (metoclopramide, cisapride) on gastric motility in beagles and labrador retrievers.

The effect of atropine, glycopyrrolate, metoclopramide and cisapride on the antral motility was investigated in eight dogs (four Beagles and four Labradors) using passive telemetry. Both anticholinergics induced a pronounced and lasting reduction of the intensity and frequency of the contractions. A definite dose-related inhibition of the antral motility was seen in Beagles, similar for both active substances. Low doses of atropine (0.02 mg/kg BW i.m.) and glycopyrrolate (0.005 mg/kg BW i.m.) completely inhibited the gastric motility for at least 30 min, whereas higher doses (0.04 or 0.01 mg/kg BW) caused a cessation of activity for more than 3 h. In Labradors, the effects of both active substances were not so dose related and the effect of glycopyrrolate lasted at least 6 h, whereas the effect of atropine gradually decreased after 3 h. A distinct breed difference regarding the effect of the two prokinetics on the antral motility was also observed. In Beagles, the prokinetics, at a low dose (metoclopramide 0.3 mg/kg BW, cisapride 0.2 mg/kg BW), resulted in a significant increase in the amplitude integral. Higher doses (metoclopramide 0.6 mg/kg BW, cisapride 0.5 mg/kg BW) also increased the integrals of the pressure profiles, but significantly less than with the lower doses. In Labradors, both medications, mainly at higher doses, resulted in an increase of the contraction amplitudes. The low dose had no (cisapride) or only a transient effect (metoclopramide). The frequency of the antral contractions was not at all influenced by cisapride, and only in Beagles metoclopramide resulted in a dose-related increase. It is not clear if the different results in Labradors and Beagles are because of breed or body weight.

Animals↗
PubMed1997

Preliminary study of glycopyrrolate in the management of drooling.

OBJECTIVE: A study was undertaken to assess the efficacy of an oral anticholinergic drug, glycopyrrolate, in the management of drooling in children and young adults with disabilities. METHODOLOGY: Glycopyrrolate was used by 24 children and young adults for up to 28 months. Parents/carers were asked to complete a questionnaire on the effects of the drug on severity and frequency of drooling and to report any side-effects. RESULTS: Twenty-two questionnaires were returned. There was a statistically significant decrease in both severity and frequency of drooling with minimal side-effects reported. CONCLUSION: In this preliminary study, glycopyrrolate was found to be an effective and well-tolerated addition to the management of drooling in children with disabilities.

Adolescent↗
PubMed1986

Atropine or glycopyrrolate with neostigmine 5 mg: a comparative dose-response study.

One hundred and fifteen patients, separated into 4 groups, received neostigmine 5 mg with either atropine 1.2 mg or 1.8 mg, or glycopyrrolate 0.6 mg or 0.9 mg. Those receiving 0.9 mg glycopyrrolate had insignificant changes in heart rate in the immediate postreversal period. It is recommended that when glycopyrrolate is used with 5 mg neostigmine, the optimum dose is 0.9 mg.

Anesthesia, General↗
PubMed1996

Comparison of nebulized glycopyrrolate and metaproterenol in chronic obstructive pulmonary disease.

We assessed the bronchodilating effect of glycopyrrolate (GP) and compared it with that of metaproterenol (MP), alone and in combination (GP+MP), in patients with chronic obstructive pulmonary disease (COPD). In a double-blind study, 11 patients (aged (mean +/- SD) 69 +/- 6 yrs; forced expiratory volume in one second (FEV1) 1.2 +/- 0.4 L) with stable COPD inhaled nebulized GP 1.0 mg, MP 15 mg, or GP 1.0 mg+MP 15 mg. Spirometry was performed before inhalation and at hourly intervals for 8 h after inhalation. It was found that GP produced a bronchodilating effect that was about equal to that of MP but lasted longer (8 vs 5 h). The combination of GP and MP produced a bronchodilating effect that was greater than that of either drug alone and was evident mostly during the effect of MP. The mean peak percentage improvement in FEV1 over baseline was 35% for GP+MP and 25% for either drug alone. These data suggest that nebulized glycopyrrolate is an effective bronchodilator in some patients with chronic obstructive pulmonary disease. Concurrent administration of glycopyrrolate and metaproterenol produces additional bronchodilation that is primarily apparent during the bronchodilator effect of metaproterenol.

Administration, Inhalation↗
PubMedDate not supplied

A comparative study of the haemodynamic effects of atropine and glycopyrrolate at induction of anaesthesia in children.

BACKGROUND: Bradycardia following administration of halothane and suxamethonium in children leads to reduced cardiac output, which can be prevented with prophylactic anticholinergics. Anticholinergics may result in tachycardia and arrhythmias. This study was designed to compare haemodynamic changes and incidence of cardiac arrhythmias following intravenous atropine and glycopyrrolate. STUDY DESIGN: Ninety ASA I and II children between one month and twelve years were studied. Premedication was with oral promethazine 1mg/kg. Anaesthesia was achieved with 3 % halothane in 33 % oxygen and nitrous oxide. Patients were randomly allocated to receive atropine 0.01mg/kg (Group I) or glycopyrrolate 0.005mg/kg (Group II). Tracheal intubation was facilitated with suxamethonium 1.5mg/kg. RESULTS: Patients in Group I had a 35.7% rise in heart rate from baseline, compared to 22.5 % in Group II two minutes after anticholinergic administration (p=0.001). Following intubation, heart rate rose by 9.7 % and 13.2 % (p<0.05) in Groups I and II respectively. MAP rose similarly in both groups. Arrhythmia occurred in 44.4 % of patients in Group I and 11.1% in Group II (p=0.001) and were mainly sinus tachycardia. 2.2% of patients in Group I exhibited bigemini. No patient experienced bradycardia. Hypoxia occurred in 2.2 %, hypotension in 13.3% and mild laryngeal spasm in 0% of Group I and 11.1%, 4.4% and 4.4% of Group II respectively. CONCLUSION: The use of glycopyrrolate compared to atropine, offered better cardiovascular stability in Nigerian children. Arrhythmias occurred more in patients who had atropine and occurred most frequently after tracheal intubation.

Anesthesia, Inhalation↗
PubMed2000

Design, synthesis, and pharmacological evaluation of soft glycopyrrolate and its analog.

Glycopyrrolate is a quaternary anticholinergic drug. Like for other anticholinergics, the usefulness of this agent is limited by its side effects. In this study, based on the structure of glycopyrrolate, we designed a soft drug, methoxycarbonylphenyl-cyclopentylacetoxy-N,N-dimethyl-3-p yrrolidinium methyl sulfate (SG), and its analog, methoxycarbonylphenylcyclopentyl-acetoxyethyl-N,N,N-trimethylammon ium methyl sulfate (SGA). These soft drugs are expected to be locally active, but systemically inactive in order to increase therapeutic index. SG and SGA were synthesized by (i) carboxylation of methyl phenylcyclopentylacetate, (ii) esterification with N-methyl-3-pyrrolidinol (for SG) or 2-chloro-N,N-dimethylaminoethane (for SGA), and (iii) quarternization with dimethyl sulfate. Receptor binding studies demonstrate that SG has muscarinic subtype selectivity (m3/m2). Guinea pig ileum pA2 assay indicates that activity of SG is moderate, and SG is about ten times more potent than SGA. The in vivo characterization of SG and SGA, both in mydriasis tests and in prevention of carbachol induced bradycardia, supported its soft nature. Applying SG or SGA into rabbit eyes, the dilation of the contralateral (water-treated) pupils was not observed. Glycopyrrolate application, however, caused dilation of the contralateral pupil, indicating a systemic effect of this drug. Cardiac studies were carried out by evaluating the protective effect of soft anticholinergics against carbachol induced bradycardia. The results indicate that SG and SGA were as potent as atropine-MeBr in preventing carbachol induced bradycardia in the rat; however, their durations of action were significantly shorter. In conclusion, the newly synthesized SG and SGA showed soft nature in the body. They are anticholinergics with subtype selectivity and moderate potency, and can be used as topical antiperspirants.

Administration, Topical↗