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At least 19 recordsLinked to original sources
PubMed1980

Glycopyrrolate in children. A comparison between the effects of glycopyrrolate and atropine administered before induction of anaesthesia.

The effect of intravenous administration of glycopyrrolate and atropine shortly before induction were compared in a double blind study in children. The study shows that glycopyrrolate, unlike atropine, administered before anaesthesia had little effect on heart rate. The heart rate changes at, and following, tracheal intubation were similar in both groups.

Atropine↗
PubMed2004

Iontophoresis with glycopyrrolate for the treatment of palmoplantar hyperhidrosis.

To determine the comparative efficacy of tap water iontophoresis to iontophoresis with the anticholinergic glycopyrrolate, we undertook a single-blinded right-left comparison study in 20 patients with palmoplantar hyperhidrosis. Most patients had their palms treated and one patient had the soles treated. We compared the duration of symptom relief following iontophoresis with glycopyrrolate unilaterally to iontophoresis with glycopyrrolate bilaterally. Patients filled in daily efficacy assessment cards. Each palm was rated as 'dry', 'slightly wet', 'moderately wet' or 'very wet'. Following treatment with unilateral tap water iontophoresis, unilateral glycopyrrolate and bilateral glycopyrrolate, patients reported hand dryness for a median of 3, 5 and 11 days, respectively. As the data was paired, treatment differences were analysed using a sign-rank test. Bilateral glycopyrrolate was superior to both unilateral glycopyrrolate and tap water in most patients. Unilateral glycopyrrolate was superior to tap water in most patients. All differences between groups were found to be statistically significant. We postulate that the increased efficacy of bilateral glycopyrrolate when compared with unilateral glycopyrrolate relates to its systemic absorption. We conclude that glycopyrrolate iontophoresis is more effective than tap water iontophoresis in the treatment of palmoplantar hyperhidrosis and that glycopyrrolate iontophoresis has both local and systemic effects on perspiration.

Adolescent↗
PubMed1999

Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways.

1. In this study we have evaluated the pharmacological profile of the muscarinic antagonist glycopyrrolate in guinea-pig and human airways in comparison with the commonly used antagonist ipratropium bromide. 2. Glycopyrrolate and ipratropium bromide inhibited EFS-induced contraction of guinea-pig trachea and human airways in a concentration-dependent manner. Glycopyrrolate was more potent than ipratropium bromide. 3. The onset of action (time to attainment of 50% of maximum response) of glycopyrrolate was similar to that obtained with ipratropium bromide in both preparations. In guinea-pig trachea, the offset of action (time taken for response to return to 50% recovery after wash out of the test antagonist) for glycopyrrolate (t1/2 [offset]=26.4+/-0.5 min) was less than that obtained with ipratropium bromide (81.2+/-3.7 min). In human airways, however, the duration of action of glycopyrrolate (t1/2 [offset]>96 min) was significantly more prolonged compared to ipratropium bromide (t1/2 [offset]= 59.2+/-17.8 min). 4. In competition studies, glycopyrrolate and ipratropium bromide bind human peripheral lung and human airway smooth muscle (HASM) muscarinic receptors with affinities in the nanomolar range (K1 values 0.5-3.6 nM). Similar to ipratropium bromide, glycopyrrolate showed no selectivity in its binding to the M1-M3 receptors. Kinetics studies, however, showed that glycopyrrolate dissociates slowly from HASM muscarinic receptors (60% protection against [3H]-NMS binding at 30 nM) compared to ipratropium bromide. 5. These results suggest that glycopyrrolate bind human and guinea-pig airway muscarinic receptors with high affinity. Furthermore, we suggest that the slow dissociation profile of glycopyrrolate might be the underlying mechanism by which this drug accomplishes its long duration of action.

Animals↗
PubMed1994

The parasympatholytic effects of atropine sulfate and glycopyrrolate in rats and rabbits.

Nine groups of rats (n = 5 per group) received an intramuscular (IM) injection of one of the following drugs or drug combinations: saline, atropine (0.05 mg/kg), glycopyrrolate (0.5 mg/kg), ketamine:xylazine (85:15 mg/kg), ketamine:detomidine (60:10 mg/kg), atropine:ketamine:xylazine (0.05: 85:15 mg/kg), glycopyrrolate: ketamine:xylazine (0.5:85:15 mg/kg), atropine:ketamine:detomidine (0.05: 60:10 mg/kg) or glycopyrrolate: ketamine:detomidine (0.5:60:10). Similarly six groups of rabbits (n = 5) received an IM injection of either saline, atropine (0.2 mg/kg), atropine (2 mg/kg), glycopyrrolate (0.1 mg/kg), ketamine:xylazine (35:10 mg/kg) or glycopyrrolate:ketamine:xylazine (0.1:35:10 mg/kg). In rats, atropine sulfate (0.05 mg/kg) and glycopyrrolate (0.5 mg/kg) produced an increase in heart rate for 30 and 240 min, respectively. In rabbits atropine sulfate at either 0.2 or 2.0 mg/kg did not induce a significant increase in heart rate, but glycopyrrolate (0.1 mg/kg) elevated the heart rate above saline treated animals for over 50 min. Both atropine and glycopyrrolate provided protection against a decrease in heart rate in rats anesthetized with ketamine: xylazine (85:15 mg/kg) or ketamine: detomidine (60:10 mg/kg); however, glycopyrrolate was significantly more effective in maintaining the heart rate within the normal range. Glycopprrolate also prevented a decrease in heart rate in rabbits anesthetized with ketamine:xylazine (35:5 mg/kg). Neither glycopyrrolate nor atropine influenced respiration rate, core body temperature or systolic blood pressure when used alone or when combined with the injectable anesthetic. Glycopyrrolate is an effective anticholinergic agent in rabbits and rodents and more useful as a preanesthetic agent than atropine sulfate in these animals.

Animals↗
PubMed1992

A pharmacological profile of glycopyrrolate: interactions at the muscarinic acetylcholine receptor.

1. Glycopyrrolate, a synthetic quaternary ammonium compound had biphasic effects on the contraction of guinea-pig atrium. At concentrations between 0.4 and 20 microM, glycopyrrolate induced a small but consistent increase in the contraction force. 2. Further increase in the concentration of glycopyrrolate produced a concentration-dependent reduction in the force of contraction with a EC50 of 0.24 mM. 3. This negative inotropic effect was opposed by a Ca2+ channel agonist, Bay K 8644. Glycopyrrolate also antagonized potently the depressant effects of carbachol and acetylcholine in guinea-pig atrium. 4. Schild analysis showed a pA2 value of 8.16 against carbachol and 8.39 against acetylcholine. These similar pA2 values suggested that both compounds may have a common interacting site. The interactions however cannot be explained by a simple competition model as the slopes of the Schild plots were larger than unity. 5. The mutual competition between glycopyrrolate and quinuclidinyl benzilate (QNB), gallamine or methoctramine indicated that glycopyrrolate could have multiple action sites in the atrium. Interaction at an allosteric site was implicated. 6. Radioligand binding studies showed that glycopyrrolate displaced pirenzepine (PZ) and AF-DX 384 from their binding to the M1 and M2 muscarinic receptors in guinea-pig brain membranes respectively. 7. The respective binding constants (Kis) were 0.60 and 0.03 nM. The Hill coefficient value (nH) for glycopyrrolate against [3H] PZ was larger than unity, suggesting positive cooperativity at the receptor complex. In contrast, the nH of the agonist [3H] AF-DX 384 was not different from unity, indicating a simple competitive inhibition. 8. Our results confirm the antimuscarinic properties of glycopyrrolate.(ABSTRACT TRUNCATED AT 250 WORDS)

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy↗
PubMed1993

[A comparison of the two anticholinergic agents atropine and glycopyrrolate during antagonism of a muscle relaxation with pyridostigmine].

Central, peripheral and cardiac side-effects of both anticholinergic drugs atropine and glycopyrrolate were compared during the antagonism of muscle relaxation with pyridostigmine. In a randomized, double-blind fashion 50 patients were given 10 micrograms/kg of atropine and 50 were given 5 micrograms/kg of glycopyrrolate with 125 micrograms/kg pyridostigmine intravenously. Continuous Holter ECG-monitoring over 3 hours was performed. The procedure was divided into the following phases: control (5 minutes before application of antagonists), phase I (application of antagonists and the following 5 minutes), phase II (subsequent 30 minutes), phase III (until 3 hours had passed). The first 32 minutes were subdivided into periods of 4 minutes. Analysed were: 1st: The number of patients with supraventricular, junctional and ventricular beats, 2nd: The mean heart rate per period, 3rd: The incidence of central-anticholinergic syndromes and the peripheral antimuscarinic side-effects. Supraventricular beats were found after atropine in 42 patients and after glycopyrrolate in 18 patients (p < 0.001). The differences mainly occurred during phase I (atropine 15 vs. glycopyrrolate 4 p < 0.05) and III (atropine 38 vs. glycopyrrolate 18, p < 0.01). Junctional beats were found after both drugs (atropine 7 vs. glycopyrrolate 10), above all during phase III. Ventricular beats were observed after atropine (21) and glycopyrrolate (18). Atropine as well as glycopyrrolate caused an increased heart rate within the first 4 minutes (atropine 47% vs. glycopyrrolate 27%, p < 0.01). During phase III after atropine, the heart rate decreased below the control value (p < 0.05). None of the patients showed central anticholinergic syndromes after either drug.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1987

Glycopyrrolate intensifies neuromuscular blockade produced by atracurium in the rat diaphragm preparation.

The effect of glycopyrrolate (Glycopyrronium, a muscarinic antagonist) (10 mumol.litre-1) and neostigmine (1 mumol.litre-1) on atracurium (0.1-100 mumol.litre-1) - induced neuromuscular blockade was studied in the rat isolated phrenic nerve-diaphragm preparation, to see if glycopyrrolate intensified the neuromuscular blockade produced by atracurium in this preparation. Atracurium had a rapid onset of blockade, reaching a complete block in 30-40 s. Glycopyrrolate had no significant effect on indirectly-elicited twitch (0.2 Hz) tension, whereas it significantly increased atracurium-induced depression of twitch tension and shortened the time needed to a complete block by 10 s. Combinations of glycopyrrolate+ neostigmine, only slightly reversed atracurium-induced blockade, if compared to the reversal by neostigmine alone. The mean concentrations to produce 50% depression of twitch tension were: 1.6 +/- 0.1 (atracurium), 0.3 +/- 0.1 (atracurium +glycopyrrolate), 4.8 +/- 0.2 (atracurium +neostigmine) and 2.7 +/- 0.1 mumol.litre-1 (atracurium +glycopyrrolate +neostigmine) (means +/- SEM, n = 6, P less than 0.001, with respect to control value of atracurium alone). It was concluded that glycopyrrolate enhanced atracurium-induced neuromuscular blockade in the rat diaphragm preparation, and that this effect should be noted when dosing glycopyrrolate in man.

Animals↗
PubMed2006

Synergistic effects of the anti-cholinergic R,R-glycopyrrolate with anti-inflammatory drugs.

Currently, much effort is geared towards developing therapies that impact on the inflammation in respiratory diseases such as asthma and COPD, assuming that this will improve disease pathology. R,R-Glycopyrrolate, a quaternary ammonium compound, is a muscarinic receptor antagonist with the potential to be used as a long-acting bronchodilator in patients with asthma and COPD. In this study we evaluated whether the combination of R,R-glycopyrrolate with known anti-inflammatory drugs results in synergistic effects. Human primary monocytes were used as an in vitro model system. M3, M4, M1 and M2 receptors were expressed in these cells in descending order. The combinatory effects of the drugs on the release of TNF-alpha after lipopolysaccharide stimulation were analyzed. R,R-Glycopyrrolate alone did not affect LPS induced TNF-alpha release. The PDE4 inhibitor rolipram dose dependently inhibited the TNF-alpha release. Maximum inhibition was around 70%. The IC(35) for rolipram was 68.9+/-15.2 nM. The simultaneous administration of 10 microM R,R-glycopyrrolate reduced the IC(35) to 1.70+/-1.18 nM. The anti-histamine azelastine inhibited TNF-alpha release dose dependently. The simultaneous administration of R,R-glycopyrrolate did not influence the action of azelastine. The corticosteroid budesonide inhibited the TNF-alpha release dose dependently with an IC(50) of 0.55+/-0.13 nM. The simultaneous administration of 10 microM R,R-glycopyrrolate reduced the IC(50) to 0.13+/-0.03 nM. Finally, R,R-glycopyrrolate was most effective in the triple combination with budesonide and rolipram in the reduction of TNF-alpha release. In conclusion, R,R-glycopyrrolate acts synergistically with the PDE4 inhibitor rolipram and the steroid budesonide in inhibiting inflammatory mediators.

Anti-Inflammatory Agents↗
PubMed2006

Pharmacological assessment of the duration of action of glycopyrrolate vs tiotropium and ipratropium in guinea-pig and human airways.

1. Our study was aimed at investigating the duration of the bronchodilator action of the antimuscarinc drug glycopyrrolate compared to tiotropium and ipratropium. In the guinea-pig isolated trachea, the time (t1/2) necessary for a contractile response to carbachol (0.3 microM) to return to 50% recovery after washout of the antagonist was studied. The offset of the antagonist effect of glycopyrrolate, tiotropium and ipratropium (10 nM each) was t1/2 = 4.0 +/- 0.5, > 4.5 and 0.5 +/- 0.1 h, respectively. At 4.5 h from the washout of the antagonist, the recovery of the response to carbachol was 50 +/- 8, 10 +/- 4 and 70 +/- 7%, respectively. 2. In the human isolated bronchus, the offset of the bronchodilator effects of glycopyrrolate (3 nM), tiotropium (1 nM) and ipratropium (10 nM) was t1/2 = 3.7 +/- 0.2; > 6 and 3.0 +/- 0.2 h, respectively. At 6.0 h from the washout of the antagonist, the recovery of the response to carbachol (1 microM) was 101 +/- 10, 27 +/- 3 and 110 +/- 10%, respectively. 4. In anaesthetized guinea-pigs, acetylcholine-induced bronchoconstriction was markedly reduced by intratracheal instillation of glycopyrrolate (3 nmol kg(-1); 88.1 +/- 4% inhibition), tiotropium (1.3 nmol kg(-1); 86.2 +/- 5% inhibition) or ipratropium (1.45 nmol kg(-1); 88.1 +/- 10% inhibition). These inhibitory effects assessed 3 or 24 h after antagonist administration were reduced to 69.9 +/- 5 and 29.7 +/- 6%; 28.3 +/- 5 and 14.2 +/- 5% for glycopyrrolate and ipratropium, respectively, whereas they remained stable (83.5 +/- 4; 70.6 +/- 6) for tiotropium. The residual inhibitory effect of glycopyrrolate was also assessed at 16 h from administration, and proved to be as low as that found at 24 h (31.2 +/- 10 vs 29.7 +/- 6%, respectively). 5. In conclusion, glycopyrrolate-induced bronchodilation has a longer duration than that of ipratropium, but less than that of tiotropium. The efficacy of a possible glycopyrrolate-based therapy for asthma or chronic obstructive pulmonary disease given once-a-day is not guaranteed by the present investigation.

Acetylcholine↗
PubMed2005

Glycopyrrolate during sevoflurane-remifentanil-based anaesthesia for cardiac catheterization of children with congenital heart disease.

BACKGROUND: Remifentanil is recommended for use in procedures with painful intraoperative stimuli but minimal postoperative pain. However, bradycardia and hypotension are known side-effects. We evaluated haemodynamic effects of i.v. glycopyrrolate during remifentanil-sevoflurane anaesthesia for cardiac catheterization of children with congenital heart disease. METHODS: Forty-five children undergoing general anaesthesia with remifentanil and sevoflurane were randomly allocated to receive either saline, glycopyrrolate 6 microg kg(-1) or glycopyrrolate 12 microg kg(-1). After induction of anaesthesia with sevoflurane, i.v. placebo or glycopyrrolate was administered. An infusion of remifentanil at the rate of 0.15 microg kg(-1) min(-1) was started, sevoflurane continued at 0.6 MAC and cisatracurium 0.2 mg kg(-1) was given. Heart rate (HR) and non-invasive arterial pressures were monitored and noted every minute for the first 10 min and then every 2.5 min for subsequent maximum of 45 min. RESULTS: Baseline HR [mean (SD)] of 117 (20) beats min(-1) decreased significantly from 12.5 min onwards after starting the remifentanil infusion in the control group [106 (18) at 12.5 min and 99 (16) beats min(-1) at 45 min]. In the groups receiving glycopyrrolate, no significant decrease in HR was noticed. Glycopyrrolate at 12 microg kg(-1) induced tachycardia between 5 and 9 min after administration. Systolic and diastolic arterial pressures decreased gradually, but there were no significant differences in the pressures between groups. CONCLUSION: I.V. glycopyrrolate 6 microg kg(-1) prevents bradycardia during general anaesthesia with remifentanil and sevoflurane for cardiac catheterization in children with congenital heart disease. Administering 12 microg kg(-1) of glycopyrrolate temporarily induces tachycardia and offers no additional advantage.

Adjuvants, Anesthesia↗
PubMed2000

The effects of glycopyrrolate on oral mucous host defenses in healthy volunteers.

UNLABELLED: We studied the effects of glycopyrrolate on oral mucous host defenses. Single IV doses of glycopyrrolate (4 microg/kg) or placebo were administered to 12 healthy volunteers in a randomized, double-blinded, cross-over study. Salivary flow rates and the concentrations/activities of total protein, amylase, and nonimmunologic (lysozyme, lactoferrin, myeloperoxidase, total salivary peroxidase, and thiocyanate) and immunologic (total immunoglobulin A, immunoglobulin G, and immunoglobulin M) mucous host defense factors were determined for paraffin-stimulated whole saliva before and 1, 3, 6, 12, 24, and 48 h after drug administration. Glycopyrrolate serum concentrations were determined before and 2, 4, 6, 10, 15, and 30 min and 1, 2, 3, 6, 12, and 24 h after IV drug injection. Salivary flow rates were decreased significantly for 12 h after glycopyrrolate injection, compared with saline injection. The concentrations of immunologic and nonimmunologic defense factors were increased in the glycopyrrolate group, and differences between the groups were found for all factors (P < 0.05-0.001) except lysozyme and total salivary peroxidase. In contrast, because of the reduced flow rate, the output of all defense factors into the saliva was decreased after glycopyrrolate injection, compared with saline injection. Glycopyrrolate thus decreases the output of salivary host defense factors into the oral cavity. IMPLICATIONS: Glycopyrrolate induces long-lasting hyposalivation and decreases the secretion of salivary immunologic and nonimmunologic defense factors in healthy volunteers.

Adjuvants, Anesthesia↗
PubMedDate not supplied

The effects of atropine and glycopyrrolate on heart rates in conscious mature goats.

The effects of intravenously administered atropine (0.2 mg/kg) and glycopyrrolate (0.01 mg/kg) on heart rate were studied in 10 conscious mature goats. In a drug cross-over fashion, either atropine, glycopyrrolate, or 0.9% saline solution was administered using the same volume (0.05 mL/kg). Atropine and glycopyrrolate caused a significant increase in heart rate (P < .05), whereas saline solution (0.09%) did not. The mean percent changes in heart rate from baseline were similar for atropine and glycopyrrolate up to 14 minutes after administration. Thereafter, glycopyrrolate had a significantly greater mean change in heart rate than atropine, ie, up to 29 minutes (P < .05). Within the atropine group, the mean percentage changes in heart rate became significantly lower compared with the initial increase (1 minute) starting at 11 minutes. For the glycopyrrolate group, the mean percent changes became significantly lower starting at 27 minutes. Glycopyrrolate and atropine had a mean percentage change in heart rate of greater than 1.0%, up to 31 and 22 minutes, respectively. At the doses used, glycopyrrolate had longer duration of action than atropine but the magnitude of increase was similar.

Animals↗
PubMed2004

Effects of glycopyrrolate on cardiorespiratory function in horses anesthetized with halothane and xylazine.

OBJECTIVE: To evaluate cardiopulmonary effects of glycopyrrolate in horses anesthetized with halothane and xylazine. ANIMALS: 6 horses. PROCEDURE: Horses were allocated to 2 treatment groups in a randomized complete block design. Anesthesia was maintained in mechanically ventilated horses by administration of halothane (1% end-tidal concentration) combined with a constant-rate infusion of xylazine hydrochloride (1 mg/kg/h, i.v.). Hemodynamic variables were monitored after induction of anesthesia and for 120 minutes after administration of glycopyrrolate or saline (0.9% NaCl) solution. Glycopyrrolate (2.5 microg/kg, i.v.) was administered at 10-minute intervals until heart rate (HR) increased at least 30% above baseline or a maximum cumulative dose of 7.5 microg/kg had been injected. Recovery characteristics and intestinal auscultation scores were evaluated for 24 hours after the end of anesthesia. RESULTS: Cumulative dose of glycopyrrolate administered to 5 horses was 5 microg/kg, whereas 1 horse received 7.5 microg/kg. The positive chronotropic effects of glycopyrrolate were accompanied by an increase in cardiac output, arterial blood pressure, and tissue oxygen delivery. Whereas HR increased by 53% above baseline values at 20 minutes after the last glycopyrrolate injection, cardiac output and mean arterial pressure increased by 38% and 31%, respectively. Glycopyrrolate administration was associated with impaction of the large colon in 1 horse and low intestinal auscultation scores lasting 24 hours in 3 horses. CONCLUSIONS AND CLINICAL RELEVANCE: The positive chronotropic effects of glycopyrrolate resulted in improvement of hemodynamic function in horses anesthetized with halothane and xylazine. However, prolonged intestinal stasis and colic may limit its use during anesthesia.

Adjuvants, Anesthesia↗
PubMed1996

The mydriatic effect of topical glycopyrrolate.

BACKGROUND: Glycopyrrolate, an anticholinergic agent that does not cross the blood-brain barrier, has several indications, but its mydriatic effect has never been tested. This study was carried out in order to compare the mydriatic effect of glycopyrrolate 0.5% to that of atropine sulfate 1%. METHODS: Glycopyrrolate 0.5% and atropine 1.0% were instilled separately in the eyes of albino rabbits. Pupil diameter and intra-ocular pressure were monitored. RESULTS: Mydriasis was noted within 5 min of glycopyrrolate instillation, reached near-maximal level at 15 min and persisted for 1 week. Glycopyrrolate 0.5% showed a faster, stronger and more persistent mydriatic effect than atropine 1.0%. Administration of glycopyrrolate 0.5% solution b.i.d. for 1 week did not affect intra-ocular pressure or produce any adverse reaction. CONCLUSION: Glycopyrrolate solution has the potential to deliver an ocular anticholinergic effect without causing associated central anticholinergic hazards.

Administration, Topical↗
PubMed2005

Treatment of suspected symptomatic cholelithiasis with glycopyrrolate: a prospective, randomized clinical trial.

STUDY OBJECTIVE: Glycopyrrolate is advocated for the treatment of acute pain from suspected symptomatic cholelithiasis. However, there is no clinical evidence to substantiate its use. This study is designed to evaluate the efficacy of glycopyrrolate in relieving acute abdominal pain of suspected biliary tract origin. METHODS: Between July 2002 and April 2003, a convenience sample of patients presenting to the emergency department with upper abdominal pain of suspected biliary tract origin was randomized to receive either intravenous glycopyrrolate or placebo (normal saline solution). Pain level was assessed at baseline using a visual analog scale, with a repeat assessment 20 minutes after intervention. Patients and clinicians were blinded to the study drug. RESULTS: Because of difficulty with patient enrollment, the trial was terminated before achievement of the initial goal of 54 patients. On analysis of the 38 patients completing the study protocol, glycopyrrolate and placebo groups had similar demographic and baseline characteristics. There was no significant difference in pain relief between patients receiving glycopyrrolate and those receiving placebo (median decrease in visual analog pain scale pain 3 mm [95% confidence interval -2 to 17 mm] versus 8 mm [95% confidence interval -2 to 20 mm], respectively). CONCLUSION: Although limited by small size and convenience sampling, these results fail to demonstrate any improvement in pain of suspected biliary tract origin with the administration of glycopyrrolate. Further study is needed to determine whether intravenous glycopyrrolate has any significant analgesic effect for patients with this condition.

Adult↗
PubMedDate not supplied

A double-blind trial of glycopyrrolate for transesophageal echocardiography.

Glycopyrrolate is an anticholinergic agent used to dry oral secretions and has been advocated for routine use with transesophageal echocardiography (TEE). To evaluate the safety and efficacy of glycopyrrolate for this unique application, a prospective double-blind placebo-controlled study of glycopyrrolate was performed in 61 patients who were awake while undergoing TEE. Thirty patients were randomized to the standard dose of glycopyrrolate (0.2 mg intravenously), and 31 patients received 1 ml of saline solution as placebo. Intravenous midazolam was used for sedation in all but one patient. Heart rate, electrocardiogram, blood pressure, and oxygen saturation were continuously monitored before, during, and after TEE. The patients scored their comfort immediately after TEE and were interviewed at 24 hours for side effects. The operator scored the ease of performing the TEE. No complications occurred in either group. Changes in vital signs and oxygen saturation were similar in both groups. The operator ease and patient comfort was similar in both groups. A significantly higher incidence of the following side effects was observed at 24 hours in patients who received glycopyrrolate versus those who received placebo: sore throat, 63% versus 19%; dry mouth, 43% versus 6%; and urinary retention, 16% versus 0% (p < 0.05 for all). No benefit from glycopyrrolate was noted in operator ease or patient comfort. In conclusion, glycopyrrolate is not recommended for routine use when performing TEE on patients who are awake.

Adult↗
PubMed1982

A comparison of atropine and glycopyrrolate in anaesthetic practice.

The two anticholinergics, atropine and glycopyrrolate, were used for premedication and as an adjunct to reversal of residual neuromuscular block in a double-blind study. Glycopyrrolate, being about twice as potent as atropine in the clinical situation, was used in half the dosage of atropine. When used for premedication, no difference was found between the drugs concerning patients complaining of dry mouth, but more patients in the glycopyrrolate group had a gastric juice pH greater than 2.5 compared to the atropine group (not statistically different). The reversal mixture consisted of necostigmine 2.5 mg with either atropine 1 mg or glycopyrrolate 0.5 mg. The heart rate response between 2 and 10 min after injecting the reversal mixture was statistically significant (P ranged from 0.0001 to 0.05), the atropine group showing the most marked decrease: 18% in the atropine group had sinus bradycardia compared to 5% in the glycopyrrolate group: 34% in the atropine group exhibited arrhythmias compared to 10% in the glycopyrrolate group, the most common form being a nodal rhythm in both groups. More patients in the atropine group had "excessive" oropharyngeal secretions (more than 2 ml) when extubated (P less than 0.05). The postoperative assessment showed little difference in the two groups, apart from a lower incidence of nausea and vomiting in the atropine group (not statistically different). The study shows that the use of glycopyrrolate was associated with a more stable cardiovascular system, fewer arrhythmias and superior control of oropharyngeal secretions at the time of reversal.

Adolescent↗
PubMed2001

A study comparing hyoscine hydrobromide and glycopyrrolate in the treatment of death rattle.

This study looked at the efficacy of drug treatment in managing death rattle in a 30-bedded specialist palliative care unit. The study was conducted in two phases. In the first, patients received hyoscine hydrobromide as the antimuscarinic; glycopyrrolate was used in the second phase. The patients in the two phases were well matched for diagnosis, age, sex and duration of death rattle. A noise score scale of 0-3 was used, which was separately validated using a verbal rating scale and noise-meter readings. Noise scores were taken at the start; 30 min after an antimuscarinic drug was administered; an hour after the initial injection if a repeat dose was given at 30 min; and 4-hourly thereafter. Drug charts of all patients with death rattle were analysed to ascertain the amount of each drug given and the cost. The incidence of death rattle was 44% in phase I, and 36% in phase II. The percentage of patients with reduced noise scores 30 min after one injection of hyoscine was significantly greater than after one dose of glycopyrrolate (56% vs 27%, P = 0.002). The need for a second injection after 30 min was less using hyoscine (33% vs 50%, P = 0.03). There was no statistically significant difference in improvement at 1 h, or at the last recorded score before death. A comparison of the cost of drug treatment using hyoscine or glycopyrrolate was made, and the potential reduction in cost per patient in the glycopyrrolate group was largely offset by increased expenditure on other drugs, especially diamorphine, midazolam and levomepromazine. The results of this study suggest that: (1) glycopyrrolate 0.2 mg is less effective at reducing death rattle than hyoscine hydrobromide 0.4 mg when assessed at 30 min, (2) the use of glycopyrrolate may lead to an increased need for other sedative or anti-emetic medication such as diamorphine, midazolam or levomepromazine, and (3) the cost benefit of using glycopyrrolate over hyoscine hydrobromide is a small part of the total drug budget, and may be less than anticipated due to the increased need of these other drugs.

Adult↗