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The clinical efficacy of glycopyrrolate, a synthetic anticholinergic drug, for premedication was compared in a double-blind study with that of atropine or hyoscine in patients anaesthetized with diethyl ether. The antisialogogue actions of the three drugs were similar. Glycopyrrolate produced less tachycardia, pyrexia and blurred vision than atropine, and its sedative effect was less than that of hyoscine.
Glycopyrrolate, atropine or saline were administered i.v. with oral magnesium trisilicate 1 h before induction of anaesthesia to patients about to undergo Caesarean section. Both anticholinergics greatly reduced gastric acidity. It is suggested that glycopyrrolate should be used in combination with antacid therapy before obstetric anaesthesia and puerperal tubal ligation because of its prolonged duration of action, effect on gastric secretion and failure to cross the placental barrier.
Glycopyrrolate 5 and 7.5 micrograms kg-1 and atropine 10 and 15 micrograms kg-1 were studied in 80 paediatric patients to assess more fully the dose of glycopyrrolate required for adequate prevention of the oculocardiac reflex. A dose-related improvement in protection from this reflex was seen with both drugs, but neither drug prevented reductions in heart rate in every patient. A nodal rhythm was the most common arrhythmia observed with both drugs. In the doses used, no adverse effects were noted and no further anticholinergic treatment was required during muscle traction. Higher doses may be associated with an increase in side-effects with more pronounced dryness of the mouth and tachycardia and, with atropine, a greater likelihood of the production of the "central anticholinergic syndrome".
A double-blind study of the effects of glycopyrrolate or atropine i.v. on gastric emptying was undertaken in 30 non-pregnant and 30 pregnant women. Gastric emptying, which was assessed by the uptake of orally administered paracetamol, was decreased in the patients in the first trimester of pregnancy when compared with the non-pregnant patients. Following the administration of glycopyrrolate, gastric emptying was decreased in the non-pregnant patients and decreased further in the pregnant patients.
Recovery from anaesthesia was compared, in a group of patients (n = 25) receiving a mixture of glycopyrrolate and neostigmine (to reverse non-depolarizing neuromuscular blockade), with recovery in a group of patients (n = 25) receiving an atropine-neostigmine mixture. Recovery following anaesthesia was more rapid in the patients receiving the glycopyrrolate-neostigmine mixture.
We studied 100 healthy women undergoing outpatient gynaecological laparoscopy in a randomized, double-blind and placebo-controlled study to evaluate the effect of neostigmine on postoperative nausea and vomiting (PONV). After induction of anaesthesia with propofol, anaesthesia was maintained with sevoflurane and 66% nitrous oxide in oxygen. Mivacurium was used for neuromuscular block. At the end of anaesthesia, neostigmine 2.0 mg and glycopyrrolate 0.4 mg, or saline, was given i.v. The incidence of PONV was evaluated in the postanaesthesia care unit, on the ward and at home. The severity of nausea and vomiting, worst pain, antiemetic and analgesic use, times to urinary voiding and home readiness were recorded. During the first 24 h after operation, 44% of patients in the neostigmine group and 43% in the saline group did not have PONV. We conclude that neostigmine with glycopyrrolate did not increase the occurrence of PONV in this patient group.
Memory changes are known to be associated with electroconvulsive therapy (ECT). The anticholinergic drugs used prior to the procedure have also been suspected of causing cognitive deficits. The present study was designed to assess memory and concentration in depressed patients receiving 0.6 mg atropine, 0.2 mg glycopyrrolate or placebo before anaesthesia and ECT. Glycopyrrolate is an anticholinergic agent lacking central nervous system effects. Anaesthesia and bilateral ECT resulted in significant short-term memory deficit, but this was seen equally in each of the groups of patients irrespective of which premedication was given. As no regimen was superior, as far as effect on memory is concerned, premedication for ECT should be chosen according to other criteria.
The possibility of using the longer acting antimuscarinic drug glycopyrrolate intramuscularly to prevent the bradycardia that sometimes results from successive doses of succinylcholine was examined. Atropine, in an equipotent dose, was given to another group of patients for comparison. Glycopyrrolate was as ineffective as atropine in preventing bradycardia. Later, a third group of patients who received no antimuscarinic drug was studied as controls. This last group had no more bradycardia than the other two groups.
Atropine and glycopyrrolate were compared when given in a mixture with neostigmine for the reversal of non-depolarising neuromuscular block in children. Glycopyrrolate was an effective antimuscarinic agent and could be safely used as an alternative to atropine, although the advantages in this age group were not as marked as have been observed in adults.
Ninety adult patients about to undergo strabismus surgery received glycopyrrolate or atropine intramuscularly. Three doses of each anticholinergic were studied. Cardiac rate and rhythm were recorded during halothane anaesthesia. The oculocardiac reflex, defined as a fall of 20% in heart rate during traction of the extraocular muscle was inhibited in a dose-dependent manner by the drugs studied. The potency ratio of glycopyrrolate to atropine according to the oculocardiac reflex was established as 1:2.
Atropine, glycopyrrolate, or saline solution was administered before anesthesia in a blinded, controlled study of 40 dogs scheduled to undergo surgery. Effects of treatment on esophageal, gastric, and tracheal pH were measured with an intraluminal pH meter. Preanesthetic administration of atropine and glycopyrrolate had no effect on esophageal, gastric, or tracheal pH but did result in increased heart rate. Thoracotomy procedures resulted in decreased intraluminal esophageal pH and increased heart rate. Esophageal pH at the level of the thoracic inlet decreased over the duration of surgery.
Based on plasma levels determined with a radioreceptor assay and following a single oral (50 micrograms/kg) and intravenous (5 micrograms/kg) administration of glycopyrrolate in six healthy children operated twice during a several weeks period, a negligible and variable oral bioavailability was found (3.3; 1.3-13.3%) (median;range). No significant changes in heart rate after oral or intravenous administration of the drug could be seen. Oral glycopyrrolate appears to have no place in paediatric premedication.
Fifty-four parents/caretakers of children with cerebral palsy were surveyed regarding their use of antisialorrheic medication for excessive drooling. Glycopyrrolate was used by 37 of 41 respondents, with significant improvement in drooling noted in the vast majority (95%) of cases as indicated by a five-point rating scale. Side effects (dry mouth, thick secretions, urinary retention, or flushing) surfaced in almost half (44%) of the patients but necessitated discontinuation of pharmacologic treatment in less than a third. While larger clinical studies are needed, our preliminary data indicate a trial of glycopyrrolate should be considered in children with cerebral palsy where drooling is a significant problem.
Heart rate and rhythm were studied in conscious children and children under nitrous oxide and halothane anaesthesia following intravenous administration of atropine or glycopyrrolate. Both drugs produced a similar increase in heart rate when the potency of glycopyrrolate is considered twice that of atropine. There is no difference in the response of anaesthetised and awake children. Junctional rhythm is the main dysrhythmia observed which appears to occur more frequently in anaesthetised children. The administration of both drugs is safe in paediatric patients.
Two cases of organophosphorus poisoning are reported. Both were treated with a combination of atropine and glycopyrrolate as well as benzodiazepine and pralidoxime. The advantages of glycopyrrolate over atropine are discussed.
Glycopyrrolate and atropine were compared as to their effects on heart rate, arrhythmias, blood pressure, and volume of oropharyngeal secretions. Glycopyrrolate protects against neostigmine-induced bradycardia, produces less initial tachycardia, causes a lower incidence of cardiac arrhythmias, and is a superior oropharyngeal drying agent. Use of this drug instead of atropine should be considered during reversal of nondepolarizing neuromuscular block.
The incidence of cardiac dysrhythmias was investigated in 60 patients undergoing dental operations under halothane anaesthesia following either hyoscine, glycopyrrolate or placebo as a supplement to nalbuphine for premedication. Forty-five percent of the patients given 6 micrograms/kg hyoscine exhibited cardiac dysrhythmias compared to 25 percent of the group given 4 micrograms/kg glycopyrrolate and to 5 percent in the placebo group. The difference between the first two groups was not significant. But there was a significant difference between these two groups and the placebo group in which only 5 percent of the patients had cardiac dysrhythmias. There was neither a connection between the frequency of cardiac dysrhythmias and the demographic characteristics of the patients nor with their PaCO2. The author recommends to avoid premedication with anticholinergic combined with halothane anaesthesia with spontaneous respiration during dental operations.
The effects of atropine and glycopyrrolate on forced vital capacity (FVC), forced expired volume in one second (FEV1), the FEV1/FVC ratio, and peak expiratory flow (PFL) were compared in 44 patients undergoing fiberoptic bronchoscopy under general anesthesia. Both anticholinergic agents improved pulmonary function equally before general anesthesia, but in both groups there was a small and again equal deterioration in pulmonary function after the procedure. The protective effects of the two drugs were not significantly different. Because of the lower incidence of undesirable side effects, glycopyrrolate is recommended as the anticholinergic agent of choice for bronchoscopy.