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The effect of intravenously administered glycopyrrolate and orally given analgetic-spasmolytic combination preparation on the contraction of the human gallbladder.

The effects of intravenously administered glycopyrrolate 0.2 mg (n = 10, Group I) or one orally given analgesic-spasmolytic combination preparation tablet (n = 10, Group II) on the contraction of human gallbladder during control oral cholecystography were compared with patients without any medication (n = 10, Group III). Neither drug had any effect on the gallbladder contraction and, hence, their usefulness in a patient with pain caused by gallstones is questionable. Heart rates and blood pressures were constant in Groups II and III but in Group I glycopyrrolate occasionally caused slight tachycardia and elevated blood pressure. Only in Group I 2 patients had mild side-effects (anticholinergic).

Administration, Oral↗

Effect of intramuscular atropine and glycopyrrolate on the cardiovascular response to tracheal intubation.

The effect of premedication with intramuscular atropine and glycopyrrolate on the cardiovascular changes resulting from the performance of laryngoscopy and tracheal intubation has been evaluated in two groups of 25 patients undergoing surgery. Neither atropine nor glycopyrrolate attenuated the hypertensive and tachycardic response to laryngoscopy and intubation; both significantly enhanced it (P less than 0,05).

Adolescent↗

Fetal and maternal cardiovascular effects of atropine and glycopyrrolate.

This study compared the effects of intravenous atropine and glycopyrrolate on maternal and fetal heart rates and variability, maternal blood pressure, and uterine activity in 20 normal full-term parturients in labor. Group 1 (N = 10) received 0.005 mg/kg of glycopyrrolate, and group 2 (N = 10) received 0.01 mg/kg of atropine. There were no statistically significant changes in fetal heart rates or variability in either group. Uterine activity increased in a normal manner as labor progressed. Maternal heart rate increased significantly and essentially equally in all patients in both groups ranging from 15 to 78 beats/min and a mean (+/- SD) of 36 +/- 16 in group 1 and from 15 to 65 beats/min with a mean of 35 +/- 17 in group 2. There were no statistically significant changes in maternal blood pressure in either group.

Adult↗

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↗

Effects of atropine, glycopyrrolate, and cimetidine on gastric secretions in morbidly obese patients.

Gastric volume and pH were studied immediately after induction of anesthesia and endotracheal intubation in 40 morbidly obese patients undergoing gastric bypass procedures. Of 14 patients receiving intramuscular atropine (0.6 mg) preoperatively, 67% had gastric pH values < 2.5; 33% of these patients had both a gastric pH < 2.5 and a volume > 20 ml. When the drug administered was intramuscular glycopyrrolate (0.3 mg), 62% of the patients had gastric pH values > 2.5; 30% had both gastric pH values < 2.5 and volumes > 20 ml. Differences between the two drugs were not significant. Thirteen patients received cimetidine orally at midnight preoperatively and again 2 to 4 hours before the induction of anesthesia. Patients in this group had gastric pH values that were significantly higher than those observed in patients given anticholinergic drugs. Only 15% had gastric pH values < 2.5. Gastric volumes observed in patients receiving cimetidine were not significantly different from those receiving anticholinergic drugs. Whereas only 7.9% of patients receiving cimetidine had both low pH values and gastric volumes > 20 ml, this was not statistically different from the observations made in patients receiving atropine or glycopyrrolate. Despite this, it is concluded that cimetidine administered before the induction of anesthesia in morbidly obese patients may reduce the high risk of aspiration pneumonitis in such patients.

Adult↗

Comparison of the effects of atropine and glycopyrrolate on various end-organs.

Atropine and glycopyrrolate (glycopyrronium bromide), a quaternary ammonium drug, were evaluated in volunteers following intramuscular administration with respect to effects on various end-organs with cholinergic innervation. Glycopyrrolate appears to be five to six times more potent than atropine in its antisialogogue effect and also exhibits a selective, though prolonged, effect on salivary secretion and sweat gland activity. It has minimal cardiovascular, ocular and central nervous system effects.

Adult↗

Cardiorespiratory effects of glycopyrrolate-butorphanol-xylazine combination, with and without nasal administration of oxygen in dogs.

Cardiopulmonary consequences of IV administered glycopyrrolate (0.01 mg/kg of body weight), followed in 11 +/- 2 minutes by butorphanol (0.2 mg/kg) and xylazine (0.5 mg/kg), were evaluated in 6 dogs, with and without nasal administration of oxygen (100 ml/kg/min). Glycopyrrolate caused significant (P < 0.05) increases in heart rate and cardiac index and significant (P < 0.05) decreases in stroke index. Subsequent administration of butorphanol and xylazine was associated with significant (P < 0.05) increases in systemic vascular resistance, mean arterial blood pressure, mean pulmonary artery pressure, central venous pressure, pulmonary capillary wedge pressure, PaCO2, venous admixture, oxygen extraction ratio, and hemoglobin concentration. It caused significant (P < 0.05) decreases in cardiac index, stroke index, breathing rate, minute volume index, oxygen delivery, and oxygen consumption. Mean arterial blood pressure, pulmonary vascular resistance, tidal volume index, and minute volume index were significantly (P < 0.05) higher when dogs were breathing room air. The arterial and venous PO2 and PCO2, and venous oxygen content were significantly (P < 0.05) higher, and the arterial and venous pH, and oxygen consumption were significantly (P < 0.05) lower when oxygen was administered. Pulsus alternans and S-T segment depression were observed in dogs of both groups. Ventricular premature contractions were observed in 1 dog breathing room air. All dogs were intubated briefly 15 minutes after administration of butorphanol and xylazine. Time to first spontaneous movement was 45 minutes. All dogs remained in lateral recumbency without physical restraint for 60 minutes.

Animals↗

The effect of prophylactic glycopyrrolate on maternal haemodynamics following spinal anaesthesia for elective caesarean section.

We conducted a randomised controlled trial to compare the severity of hypotension and ephedrine requirements following spinal anaesthesia for elective caesarean section in women pretreated with either i.v. glycopyrrolate 4.0 microg/kg (group G) or saline (group S). Data were analysed using sequential analysis which allowed us to terminate the study after data from 40 patients had been analysed (20 in each group). There were no differences between the two groups in the severity of hypotension (mean +/- SD decrease from baseline 35 +/- 14% in group G and 29 +/- 15% in group S) or ephedrine requirements (15 +/- 11 mg in group G and 18 +/- 12 mg in group S). Intra-operative heart rate increased by a greater amount in group G than in group S (58 +/- 26% vs 35 +/- 21% mean +/- SD;P = 0.002) and there was a greater incidence of dry mouth (75% vs 15%;P = 0.0006) but no difference in the incidence of nausea and vomiting (30% vs 50%;P = 0.33). Pretreatment with glycopyrrolate did not confer an advantage in this study.

Clinical Trial↗

Comparison of Atropine with Glycopyrrolate for Use in ECT.

The occurrence of undesirable events during the postictal electroconvulsive therapy (ECT) period was retrospectively compared between 29 patients who had received glycopyrrolate premedication 0.002 mg/lb i.v. and 25 patients who had received atropine 1.0 mg i.m. A separate comparison was made for 14 patients who had received ECTs with each of these premedications. A total of 952 ECTs were reviewed. In both comparisons supraventricular tachycardia was more common with atropine (p <.0001 with each), after approximately 13% of ECTs. Otherwise, postictal events with the two agents were indistinguishable; specifically, bradycardia and nausea were not more frequent with glycopyrrolate.

Journal Article↗

Protective Effects of Intramuscular Glycopyrrolate on Cardiac Conduction During ECT.

The immediate effects of electroconvulsive therapy (ECT) on cardiac conduction, with or without anticholinergic (glycopyrrolate) premedication, were systematically assessed in 19 patients. The resumption of cardiac rhythm after ECT was significantly delayed in treatments without glycopyrrolate. There was no apparent clinical impact of this phenomenon, even though some patients showed asystole of up to 6 s during nonglycopyrrolate treatments.

Journal Article↗

The effects of five potassium chloride preparations on the upper gastrointestinal mucosa in healthy subjects receiving glycopyrrolate.

The effects on the upper gastrointestinal tract of five different preparations of KCl were compared in 90 healthy subjects treated with glycopyrrolate. The KCl preparations studied were wax-matrix KCl, microencapsulated KCl, liquid KCl, experimental extended-release capsules, experimental extended-release tablets,and placebo. The subjects were endoscoped prior to and after seven days of dosing. Upper gastrointestinal mucosal pathology was seen with all of the potassium preparations as well as with placebo. No statistically significant differences between the various KCl groups or between KCl groups and placebo were seen. All of the lesions were superficial, except for one ulcer seen with the microencapsulated KCl. None of the subjects developed occult gastrointestinal bleeding. There were no differences in the incidence of abdominal symptoms.

Adolescent↗

A glycopyrrolate-ritodrine drug-drug interaction.

This is a case report of a 39-year-old patient who developed supraventricular tachycardia secondary to a ritodrine-glycopyrrolate interaction. The cardiovascular effects of ritodrine as well as the possible mechanism for this interaction are discussed. Suggested treatment for ritodrine-induced tachycardia in the parturient are presented.

Adult↗

Intramuscular ketamine, midazolam, and glycopyrrolate for pediatric sedation in the emergency department.

PURPOSE: The safety and efficacy of a new sedation technique for children with facial injuries in the emergency department were prospectively evaluated. MATERIALS AND METHODS: Thirty-seven children between the ages of 12 months and 7 years old who required sedation for minor surgical procedures were administered an intramuscular injection of ketamine (3 mg/kg), midazolam (0.05 mg/kg), and glycopyrrolate (0.005 mg/kg). A second 1-mg/kg intramuscular injection of ketamine alone was given if needed. Pulse rate, cardiac rhythm, respiratory rate, oxygen saturation, side effects, and behavior were recorded. RESULTS: Satisfactory sedation was achieved after a single injection in 32 children; five others required a second ketamine injection (1 mg/kg). Onset of anesthesia occurred within 6 minutes in 73% of the children who received one injection, and there were generally adequate working conditions for 30 minutes. The average time from initial injection to discharge was 76 minutes. Results of physiologic monitoring, behavioral ratings, and side effects are reported. Emergence delirium and hallucinations were not observed. Ketamine reliably produced dissociative anesthesia without loss of respiratory drive or protective airway tone. Midazolam reduced the incidence of ketamine-induced dysphoric reactions and muscular hypertonicity. CONCLUSION: The use of intramuscular ketamine, midazolam, and glycoyrrolate is a safe, effective, and practical approach to managing selected pediatric injuries in the emergency department. Advanced airway management proficiency is recommended for use of this technique.

Anesthesia Recovery Period↗

The effect of ammonium glycopyrrolate (Robinul)-induced xerostomia on oral mucosal wetness and flow of gingival crevicular fluid in humans.

The antisialogogue, ammonium glycopyrrolate (Robinul), was used to reduce the salivary flow rate in healthy individuals with normal salivary function to determine whether the dry-mouth symptoms and reduced amounts and patterns of oral mucosal wetness found previously in hyposalivators could be induced by this means. After baseline measurements, the drug was given to 10 healthy volunteers and their resting whole-saliva flow rate was measured at 0, 15, 60, 105 and 150 min thereafter. At the same times, the thickness of the layer of residual mucosal saliva (a measure of residual mucosal wetness) at each of 22 intraoral sites was also determined. The saliva flow rate fell from a mean of 0.45 +/- 0.07 ml/min to a mean of 0.05 +/- 0.02 ml/mm by 1 h and slowly thereafter to a mean of 0.02 +/- 0.01 to 0.03 +/- 0.01 ml/min for the remainder of the experiment. Onset of dryness symptoms was observed approx. 30 min after giving the drug. Simultaneously, the residual saliva at each of the 22 sites teted decreased to a thickness level previously found in patients with hyposalivation and who exhibited an intense feeling of dry mouth. Despite these decreases in thickness, the pattern of residual mucosal wetness throughout the mouth remained more or less unchanged. As in earlier studies, wetness was least on the hard palate and highest on the posterior dorsum of the tongue. An altered taste of the residual saliva in the mouth and an increased feeling of roughness as the tongue was passed over labial and buccal mucosal surfaces were noted. The amount of gingival crevicular fluid (GCF) in 12 gingival sites in each of the participants was also measured. Unlike the reduction in salivary flow, changes in GCF over the 150 min of the study were negligible. From this it was concluded that GCF could contribute much more to the oral fluids in dry-mouth than in normal individuals, especially when there is greater gingival inflammation.

Adult↗

Stability of buprenorphine, haloperidol and glycopyrrolate mixture in a 0.9% sodium chloride solution.

Combinations of opioids and adjuvant drug solutions are often used in clinical practice while little information is available on their microbiological or chemical stability. Currently there are no commercially available, prepacked, ready-to-use epidural or subcutaneous mixtures. Thus, epidural and subcutaneous analgesic mixtures must be prepared in the pharmacy on an as-needed basis. Such mixtures are typically used for the treatment of severe pain in cancer patients. The aim of this study was to investigate the microbiological and chemical stability of a buprenorphine, haloperidol and glycopyrrolate mixture in a 0.9% sodium chloride solution. A high performance liquid chromatographic (HPLC) method and pH-meter were used to conduct the analyses. Antimicrobial activity of each component was studied by an agar dilution method. According to the results from the chemical and microbiological stability studies, this mixture can be stored in polypropylene (PP) syringes and polyvinyl chloride (PVC) medication cassettes for at least 30 days at either 21 degrees C or 4 degrees C, and for 16 days in PP syringes at 36 degrees C, and for 9 days in PVC medication cassettes at 36 degrees C.

Analgesics, Opioid↗

Neostigmine 50 microg kg(-1) with glycopyrrolate increases postoperative nausea in women after laparoscopic gynaecological surgery.

BACKGROUND: Neostigmine, used for reversal of neuromuscular block, has been implicated in the development of postoperative nausea and vomiting (PONV). The use of mivacurium, which does not require neostigmine reversal due to its metabolism by plasma cholinesterase, has made it possible to study the effect of neostigmine on PONV in a randomised, double-blind, placebo-controlled manner. METHODS: Ninety healthy women scheduled for laparoscopic gynaecological surgery were randomly allocated to two groups in a double-blind manner. One group was given neostigmine (50 microg kg(-1)) and glycopyrrolate (10 microg kg(-1)) (group NG), the other NaCl i.v. as placebo (group P) at the end of surgery when all the patients were spontaneously reversed to at least 75% of full muscle power. The risk of PONV was reduced by using low doses of opioids and ondansetron prophylaxis. All the patients were monitored and assessed for 24 h with regard to pain, nausea, vomiting and overall satisfaction. RESULTS: There was a statistically significant difference (P=0.03) in the occurrence of nausea during the first 6 h postoperatively between NG group (30%) and P group (11%), resulting in the more extensive use of antiemetic drugs in the NG group (28%) than in P group (7%) (P=0.01) in this period. There was no difference between the groups in the frequency of vomiting; seven nauseated patients had vomiting, four in group NG, three in group P. Total number of patients with PONV during the observation period of 24 h, usage of antiemetic rescue medication and overall patient satisfaction did not differ significantly between the groups. CONCLUSION: The results suggest that antagonism of neuromuscular block with a high dose of neostigmine increases postoperative nausea and the use of antiemetic drugs during the first 6 h after administration.

Adjuvants, Anesthesia↗

Comparison of the effects of atropine and glycopyrrolate on lower oesophageal sphincter pressure.

Lower oesophageal sphincter pressure (LOSP) has been measured on three separate occasions in nine healthy volunteers using oesophageal pressure transducers. Atropine 0.6 mg decreased LOSP significantly at 5 min after i.v. injection (P less than 0.025) and this change was sustained for 40 min. Glycopyrrolate 0.3 mg or 0.2 mg decreased LOSP significantly at 3 min after i.v. injection (P less than 0.0025). This change was sustained for 60 min and was similar for both doses and also similar in magnitude to the change produced by atropine.

Adult↗

Pattern of change of bronchomotor tone following reversal of neuromuscular blockade. Comparison between atropine and glycopyrrolate.

Specific airways conductance (s.Gaw) was measured using the forced airflow oscillation method, to study the effect of two regimens, commonly used for the reversal of neuromuscular blockade, on bronchomotor tone. Patients who had received neuromuscular blockers and had undergone elective surgery were randomly allocated to receive neostigmine 50 microgram kg-1 given concurrently with either atropine 20 microgram kg-1 (10 patients) or glycopyrrolate 10 microgram kg-1 (10 patients). Before administration, five baseline measurements of s.Gaw were obtained and measurements were then made at intervals of 1 min for the next 10 min. At 3 min there was a significant difference in s.Gaw between the two groups, higher values being found in the atropine group. At 10 min, no significant difference was seen between the groups, although both showed a significant decrease in s.Gaw compared with baseline values (P less than 0.05).

Atropine↗