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PubMed2001

Pharmacokinetic-pharmacodynamic model for the anticholinergic effect of glycopyrrolate.

OBJECTIVE: The purpose of this study was to develop and test a pharmacokinetic-pharmacodynamic (PK-PD) model for the anticholinergic effect of glycopyrrolate in eight healthy male volunteers. METHODS: First, arterial drug concentration (Cp) data after a single intravenous (i.v.) bolus injection (5 micrograms/kg) were individually fitted to a three-compartment PK model. Second, the effect of a 2-h glycopyrrolate i.v. infusion (5 micrograms/kg/h) on the mean R-R interval (RRI) and the Hayano index of the high frequency variability of RRI (HF CCV) was modelled using an effect-compartment, inhibitory sigmoidal Emax model, with the individual PK parameters from the first part as constants. Third, the developed model was tested using a computer-driven infusion which aimed at two ascending steady-state effect-site concentrations (Ce) at 1-h intervals, corresponding to 20% and 80% of the maximal effect (Emax) observed in the second part. RESULTS: Modeling of the HF CCV data yielded the following mean (+/- SD) estimates: concentration at 50% of Emax (EC50), 2.46 +/- 0.58 ng/ml, equilibration half-time (t1/2 ke0), 42.5 +/- 7.7 min, and sigmoidicity factor (gamma), 7.26 +/- 2.82. The corresponding values for RRI data were 2.79 +/- 0.52 ng/ml, 58.3 +/- 17.2 min, and 4.75 +/- 1.56. During the computer-controlled two-step infusion (performed using HF CCV as the effect variable), the measured Cp approached the targeted Ce in most of the subjects, while the observed effect appeared to surpass the targeted levels. CONCLUSION: Although we were able to develop individual PK-PD models for glycopyrrolate, maintaining a stable anticholinergic effect in the computer-driven infusion appeared to be difficult. This is probably due to intra-individual variability in the PK-PD parameters and the extremely steep concentration-effect relationship of glycopyrrolate.

Adult↗

PubMed1995

Effects of combined treatment with glycopyrrolate and albuterol in acute exacerbation of chronic obstructive pulmonary disease.

STUDY OBJECTIVE: To investigate whether the addition of a single aerosolized dose of glycopyrrolate leads to a greater improvement in pulmonary function than treatment with albuterol alone for patients with acute exacerbation of chronic obstructive pulmonary disease (COPD). DESIGN: Prospective, randomized, blinded, controlled study. Fifty-seven patients with acute exacerbation of COPD were entered into the study. All patients received three aerosol treatments. Patients were randomized to receive 2 mg aerosolized glycopyrrolate (combination therapy group) or aerosolized placebo in addition to their first 2.5-mg albuterol aerosol treatment. All patients received 2.5 mg of aerosolized albuterol alone for the next two treatments. SETTING: Urban teaching hospital emergency department. RESULTS: We found no difference in pretreatment 1-second fractional expired volume (FEV1) between the control and glycopyrrolate groups. There was no significant difference in the absolute value of the FEV1 at 1 hour or at 3 hours between the two groups; however, patients who received combination therapy had a greater percent increase from the pretreatment value of FEV1 (56%) as measured in milliliters than did control patients (19%; P = .008). CONCLUSION: The combination of glycopyrrolate and albuterol produces a greater improvement in FEV1 than does albuterol alone in the treatment of patients with acute exacerbation of COPD.

Acute Disease↗

PubMed1999

Oral glycopyrrolate alleviates drooling in a patient with tongue cancer.

Although sialorrhea and drooling are uncommon symptoms in cancer patients, they can cause considerable discomfort, inconvenience and social embarrassment. In this article we describe a patient with tongue cancer who was successfully treated with oral glycopyrrolate 0.4 mg 3 times daily. Glycopyrrolate is a quaternary ammonium compound. In contrast to the recommended treatment with scopolamine, glycopyrrolate is virtually without side effects to the central nervous system because it penetrates the blood-brain barrier poorly. Glycopyrrolate has a slow and erratic absorption from the gastrointestinal system, but even low plasma levels are associated with a distinct and long-lasting antisialogic effect.

Female↗

PubMed2003

The echocardiographic effects of romifidine in dogs with and without prior or concurrent administration of glycopyrrolate.

OBJECTIVE: To determine the cardiopulmonary response to romifidine (RO) in the dog with or without prior or concurrent administration of glycopyrrolate. STUDY DESIGN: Randomized, cross-over experimental study. ANIMALS: Six (three male, three female) cross-bred dogs weighing 23 +/- 2.4 kg. METHODS: Two-dimensional guided M-mode echocardiography was performed in conscious dogs simultaneously with measurement of systolic arterial blood pressure (SBP) and heart rate (HR). Dimensions of the left ventricle (LVID), interventricular septum (IVS), and left ventricular free wall (LVFW) were obtained in systole (S) and diastole (D). Amplitude of motion (Amp) of the IVS and LVFW were also measured. From these, measures of wall stress (WS) and fractional shortening (FS) of the left ventricle were derived. Baseline echocardiographic measurements were recorded, following which one of the five treatments was administered. Glycopyrrolate (G) 0.01 mg kg-1, or saline (S) 0.5 mL, was administered IM as pre-medication (Gp or Sp), or G was administered concurrently (Gc) with romifidine (RO). Treatments were: T1, Sp + RO (40 micro g kg-1); T2, Gp + RO (40 micro g kg-1); T3, Sp + RO (120 micro g kg-1); T4, Gp + RO (120 micro g kg-1); and T5, Sp + Gc +RO (120 micro g kg-1). Romifidine or RO + Gc was administered SC 20 minutes after pre-medication (time 0), and further measurements were taken 10, 20, 30, 60, and 90 minutes after RO. RESULTS: Echocardiographic indices of cardiac systolic function (LVID-S, FS, Amp-LVFW) and HR were decreased in RO-sedated dogs (p < 0.0001). The magnitude of change in cardiac indices was least with low-dose RO. At most sampling times, high-dose RO produced significantly more alteration in cardiac indices. Systolic blood pressure increased in all treatment groups, with the greatest increases in those groups receiving G. Glycopyrrolate significantly increased HR; however, cardiac indices were further reduced. Wall stress significantly increased, with a more dramatic increase in groups receiving G. CONCLUSIONS: Indices of LV systolic function were reduced in RO-sedated dogs in a dose-related manner. Glycopyrrolate further reduced these indices and dramatically increased measurements of wall stress in dogs sedated with RO. CLINICAL RELEVANCE: Use of low-dose RO minimizes cardiac dysfunction; however, it should still be used cautiously in dogs with cardiomyopathy or heart failure. The routine use of G is not recommended to alleviate the bradycardia associated with RO in conscious dogs.

Adrenergic alpha-Agonists↗

PubMed1977

Glycopyrrolate-neostigmine mixture for antagonism of neuromuscular block: comparison with atropine-neostigmine mixture.

Glycopyrrolate, a new anticholinergic agent, was evaluated and compared with atropine. Glycopyrrolate 0.2 mg to neostigmine 1.0 mg was found to be safe and effective. The heart rates remained more stable with glycopyrrolate, and the frequency of arrhythmia, which was both transient and of no consequence, was similar in the two groups. The antisialogogue action of glycopyrrolate was superior to that of atropine.

Anesthesia, General↗

PubMed1985

Comparison of the ocular effects of atropine or glycopyrrolate with two I.V. induction agents.

Atropine and glycopyrrolate combined with either methohexitone or thiopentone were compared with the induction agent alone in patients undergoing electroconvulsive therapy. Patients acted as their own controls in each sub-group defined by induction agent. Pupil size, muscle twitches, presence of hiccups and the extent of oropharyngeal secretions were noted. Methohexitone produced a greater and more prolonged increase in pupil size than did thiopentone. The subsequent pupil size following the atropine-methohexitone mixture was significantly greater than that following the glycopyrrolate-methohexitone mixture. The combination of atropine with thiopentone produced a greater "secondary" mydriasis than thiopentone alone, or thiopentone combined with glycopyrrolate. The effect of the glycopyrrolate-thiopentone combination did not differ significantly from that of thiopentone alone. Methohexitone was associated with a greater incidence of hiccups, muscle twitching and excessive salivation.

Adult↗

PubMed1999

Glycopyrrolate reduces nausea during spinal anaesthesia for caesarean section without affecting neonatal outcome.

We have tested the hypotheses that glycopyrrolate, administered immediately before induction of subarachnoid anaesthesia for elective Caesarean section, reduces the incidence and severity of nausea, with no adverse effects on neonatal Apgar scores, in a double-blind, randomized, controlled study. Fifty women received either glycopyrrolate 200 micrograms or saline (placebo) i.v. during fluid preload, before induction of spinal anaesthesia with 2.5 ml of 0.5% isobaric bupivacaine. Patients were questioned directly regarding nausea at 3-min intervals throughout operation and asked to report symptoms as they arose. The severity of nausea was assessed using a verbal scoring system and was treated with increments of i.v. ephedrine and fluids. Patients in the group pretreated with glycopyrrolate reported a reduction in the frequency (P = 0.02) and severity (P = 0.03) of nausea. Glycopyrrolate also reduced the severity of hypotension, as evidenced by reduced ephedrine requirements (P = 0.02). There were no differences in neonatal Apgar scores between groups.

Anesthesia, Obstetrical↗

PubMed1984

The effects of atropine and glycopyrrolate on intra-ocular pressure in anaesthetised elderly patients.

The effects of glycopyrrolate 0.2 mg and atropine 0.6 mg, given intravenously, were studied in 40 elderly patients undergoing intra-ocular surgery. Twenty patients had normal intra-ocular pressure (IOP) and 20 had raised IOP. The effects of each of the drugs on IOP, heart rate, prevention of the oculocardiac reflex and incidence of dysrhythmias were assessed. Anaesthesia with thiopentone, suxamethonium, nitrous oxide/oxygen, and halothane, using a semiclosed circle system resulted in a decrease in mean IOP in both the atropine and glycopyrrolate groups. Patients who had pre-existing raised IOP showed a significantly greater decrease in IOP than those with normal IOP. Patients with raised IOP who had received atropine experienced a greater decrease in IOP than those who had received glycopyrrolate. Both atropine and glycopyrrolate were effective in preventing the oculocardiac reflex. The increase in heart rate was greater in those patients who had received atropine. The incidence of dysrhythmias was low.

Aged↗

PubMed1996

The effect of glycopyrrolate on postoperative pain and analgesic requirements following laparoscopic sterilisation.

In order to evaluate the contribution of tubal spasm to pelvic pain following laparoscopic sterilisation, we have studied the effect of glycopyrrolate, an anticholinergic agent with antispasmodic properties, on 60 ASA 1 and 2 patients presenting as day-cases for laparoscopic sterilisation using Filshie clips. In a randomised, double-blind, controlled trial, patients received either glycopyrrolate 0.3 mg or saline intravenously prior to induction of anaesthesia. Compared with the control group, patients receiving glycopyrrolate had significantly reduced immediate postoperative pain scores (p < 0.02) and required significantly less postoperative morphine (p < 0.01). Nausea, vomiting and anti-emetic requirements were also reduced though not significantly. We conclude that glycopyrrolate 0.3 mg at induction of anaesthesia is an effective method of improving the quality of recovery after day-case laparoscopic sterilisation using clips.

Adult↗

PubMed1980

Comparison of Glycopyrrolate, atropine and hyoscine in mixture with neostigmine for reversal of neuromuscular block following closed mitral valvotomy.

Atropine, glycopyrrolate and hyoscine were compared in a mixture with neostigmine for the reversal of neuromuscular block in patients undergoing closed mitral valvotomy. Both atropine and glycopyrrolate were effective in counteracting the muscarinic effects of neostigmine. Glycopyrrolate was, associated with less initial increase in heart rate, a factor of importance in patients with mitral stenosis. The incidence of significant dysrhythmias was low in this small series. The control of secretions was better with glycopyrrolate. Administration of hyoscine was associated with unacceptable falls in heart rate and is not recommended.

Adult↗

PubMed1984

Comparison of some postanaesthetic effects of atropine and glycopyrrolate with particular emphasis on urinary problems.

Two hundred and two patients undergoing elective surgery were given either atropine (98 patients) or glycopyrrolate (104 patients) for intravenous premedication and as an adjunct to reversal of neuromuscular block by neostigmine in a double-blind study. The dose ratio of atropine and glycopyrrolate was 2.5:1. After reversal, both drugs induced an initial increase and a subsequent decrease in heart rate. The mean values in % heart rate were statistically significantly higher in the glycopyrrolate group than in the atropine group. Semiquantitative measurement of salivation showed glycopyrrolate to be more potent as an antisialogogue drug. Nausea and vomiting were equally common after both drugs. There were no differences between the drugs in the occurrence of postoperative micturition difficulties, the total rate of this complication being 18%. It is concluded that factors other than the choice of anticholinergic drug may be blamed for postoperative micturition difficulties.

Adult↗

PubMed1984

Atropine vs glycopyrrolate during reversal of pancuronium block in patients anaesthetized with halothane.

Atropine 0.015 mg kg-1 and glycopyrrolate 0.0075 mg kg-1 were compared as antimuscarinic agents during reversal of pancuronium block with neostigmine 0.03 mg kg-1 in 30 patients anaesthetized with thiopental-N2O-halothane and undergoing minor surgery. In patients treated with atropine-neostigmine, the frequencies of bradycardia and junctional rhythm were relatively high and about the same as those reported by us previously in patients anaesthetized with thiopental-N2O-fentanyl. As in our previous study, glycopyrrolate seemed to have advantages over atropine during reversal of pancuronium block: the incidences of bradycardia and junctional rhythm were significantly less in patients treated with glycopyrrolate. Recovery from anaesthesia, as assessed by the awakening after discontinuation of N2O and halothane administration, and the incidence of postoperative nausea and vomiting, were not significantly different between the atropine and glycopyrrolate groups.

Adult↗

PubMed1989

Glycopyrrolate: pharmacokinetics and some pharmacodynamic findings.

In the present study, a sensitive and reproducible radioreceptor assay (RRA) was used to evaluate the basic pharmacokinetic properties of glycopyrrolate, a quaternary amine with peripheral antimuscarinic activity. Based on the plasma levels after a single intravenous injection, 6 micrograms/kg (n = 6), the distribution phase half-life (2.22 +/- 1.26 s.d. min) and the elimination phase half-life (0.83 +/- 0.29 h) of glycopyrrolate were short due to the low distribution volume during the elimination phase (0.64 +/- 0.29 l/kg) and to the respectively high total plasma clearance value (0.54 +/- 0.14 l/kg/h). An intramuscular injection, 8 micrograms/kg (n = 6), was followed by a fast and predictable systemic drug absorption and clinical effects (heart rate increase, dry mouth). In this group the time to maximum plasma concentration (tmax) was 27.48 +/- 6.12 min and the maximum plasma concentration (Cmax) was 3.47 +/- 1.48 micrograms/l. After oral drug intake, 4 mg (n = 6), an apparently low and variable gastrointestinal absorption was found (tmax = 300.0 +/- 197.2 min, Cmax = 0.76 +/- 0.35 microgram/l), thus indicating that the oral route of drug administration is of no value as a routine premedication. The correlation between the plasma concentration of glycopyrrolate and the drug effects appears to be variable. Because of its sensitivity, the RRA method proved to be quite useful in evaluating the kinetics of glycopyrrolate and its relationship to various clinical effects.

Absorption↗

PubMed1991

Split-dose atropine versus glycopyrrolate with neostigmine for reversal of gallamine-induced neuromuscular blockade.

The effects of a split-dose of atropine sulphate versus a single dose of glycopyrrolate given with neostigmine for the reversal of gallamine-induced neuromuscular blockade were studied in 55 patients undergoing gynaecological surgery. The patients were randomized to receive either a single dose of glycopyrrolate (7 micrograms.kg-1) or two doses of atropine (8 micrograms.kg-1 each), given with an interval of 1 min. There were no differences between the two methods with respect to percentage heart rate changes, salivation or arousal time. Four patients demonstrated cardiac arhythmias in the atropine group, whereas none occurred in the glycopyrrolate group (P less than 0.05). It is concluded that a split-dose of atropine has similar chronotropic effects to a single dose of glycopyrrolate for the reversal of gallamine-induced neuromuscular blockade. However, the finding of a higher incidence of cardiac arrhythmias in the atropine group suggests that this reversal regime should be reserved for patients without cardiac disease.

Adult↗

PubMed1991

Effects of glycopyrrolate and atropine on heart rate variability.

Analysis of heart rate variability, combined with physiological tests (deep breathing and tilt tests) was used to characterise the effects of atropine and glycopyrrolate on the parasympathetic nervous tone of the heart in healthy male volunteers. The low dose of atropine (120 micrograms) administered as a continuous infusion in 15 min was associated with parasympatomimetic effects estimated by the slowing of the heart rate and an increase of the mean and beat-to-beat heart rate variability. The bradycardia and increase of heart rate variability following infusion of glycopyrrolate (50 micrograms) was less marked and did not differ significantly from that of placebo. The higher doses of atropine (720 micrograms) and glycopyrrolate (300 micrograms) administered as a continuous infusion in 15 min produced an equal vagal cardiac blockade characterised by significant tachycardia and a decrease in overall and beat-to-beat heart rate variability. It is concluded that at low doses the parasympatomimetic action of glycopyrrolate is less marked than that of atropine; and at higher doses only small differences exist between these two muscarinic antagonists in their effects on cardiac vagal outflow, assessed by heart rate and heart rate variability.

Adult↗

PubMed2005

Infusion of neostigmine-glycopyrrolate for bowel evacuation in persons with spinal cord injury.

Defecatory complications are common after spinal cord injury (SCI) and have been attributed, in part, to an imbalance of the autonomic nervous system between parasympathetic and sympathetic effects on the colon. Because parasympathetic (i.e., cholinergic) input to the bowel may be downregulated after SCI, it was hypothesized that neostigmine, a medication that increases cholinergic tone by blocking the metabolism of acetylcholine, might promote bowel evacuation in these persons. Since neostigmine is known to cause bradycardia and bronchoconstriction, we also assessed whether these side-effects could be prevented by coadministration of neostigmine with glycopyrrolate, an anticholinergic agent that has limited activity on the muscarinic receptors of the colon. The hypothesis was tested in 13 persons with SCI in whom videofluoroscopy was carried out after instillation of a barium oatmeal paste into the rectum and descending colon. On separate days, subjects received, in a randomized, blinded design, one of three intravenous infusates (normal saline, 2 mg neostigmine, or 2 mg neostigmine + 0.4 mg glycopyrrolate). The effect of these infusates on bowel evacuation of the barium paste, heart rate, and airway resistance was determined. Both neostigmine and neostigmine + glycopyrrolate resulted in prompt bowel evacuation. The nadir heart rate was lower after neostigmine alone than with the combination. Neostigmine administration increased both total and central airway resistance, an effect that was not observed with the coadministration of glycopyrrolate. Other side-effects of neostigmine and the combination of drugs included muscle fasciculations and dry mouth, both of which were mild and short-lived. Abdominal cramping was noted in subjects with spinal cord lesions below thoracic level 10. These results indicated that neostigmine/glycopyrrolate administration is safe and well tolerated in persons with chronic SCI.

Adult↗

PubMed1984

Glycopyrrolate and atropine inhalation: comparative effects on normal airway function.

Bronchodilation was produced in normal subjects by inhalation of high doses of a quaternary parasympatholytic agent (glycopyrrolate), and responses were compared with those of atropine and a placebo. Both drugs induced significant increases in specific airway conductance (SGaw) and forced expiratory flows, but the effects of glycopyrrolate were sustained significantly longer (greater than 6 h). Whereas atropine produced an increased heart rate (26%) and severe dry mouth in all subjects, these symptoms were absent with glycopyrrolate and placebo. Therefore, glycopyrrolate produces significant bronchodilation of long duration but free of the side effects of muscarinic blockade that characterize atropine inhalation.

Adult↗

PubMedDate not supplied

Glycopyrrolate versus atropine in post-ECT amnesia in the elderly.

The neurotransmitter acetylcholine is important in memory function, and low brain concentrations may be associated with cognitive impairment. Our hypothesis was that atropine, a centrally acting anticholinergic drug known to cause amnesia, confusion, and delirium, may further exacerbate the amnesia and/or confusion resulting from electroconvulsive therapy (ECT) when used as a preanesthetic, and that the peripherally acting glycopyrrolate would by comparison decrease these side effects. We randomly administered glycopyrrolate versus atropine in equivalent doses as the preanesthetic agent to 20 consecutively admitted geriatric patients with major depression, for whom ECT was the clinical treatment of choice. Patients were matched for age, Hamilton Scale for Depression, and baseline performance on the Buschke Selective Reminding Task (BSRT). We found no significant difference in outcome between patients treated prior to ECT with atropine versus glycopyrrolate, as assessed by the above measures. We conclude from this study that atropine is no more deleterious to memory than is glycopyrrolate when given before ECT.

Aged↗