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Chemical Compound Review

GLYCOPYRROLATE     (1,1-dimethyl-2,3,4,5- tetrahydropyrrol-3...

Synonyms: Robanul, Robinal, zlchem 10, AGN-PC-00YUUG, SureCN133002, ...
 
 
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Disease relevance of GLYCOPYRROLATE

  • CONCLUSION: For moderate to severe symptoms of diabetic gustatory sweating, topical application of glycopyrrolate is safe, effective, well tolerated, and convenient [1].
  • METHODS: Daily topical application of glycopyrrolate roll-on lotion was offered as an alternative to oral anticholinergic agents to an 87-year-old woman with long-standing type 2 diabetes mellitus who complained of profuse sweating after eating [1].
  • In this group, the combination of a 60-minute erythromycin infusion and glycopyrrolate pretreatment decreased clinically important toxicity by 79% from 47% to 10%, a statistically and clinically significant 37% (95% CI, 14% to 60%) difference (p = 0.007) [2].
  • When neuromuscular blockade is antagonized with anticholinesterases, atropine or glycopyrrolate is used commonly to prevent bradycardia and excessive oral secretions [3].
  • The decrease in SBP after cuff deflation (-9.2 +/- 1.2 mmHg) was significantly greater after atropine (-15 +/- 1 mmHg) or glycopyrrolate (-14 +/- 1 mmHg), with abolished reflex tachycardia [4].
 

Psychiatry related information on GLYCOPYRROLATE

 

High impact information on GLYCOPYRROLATE

  • With glycopyrrolate administration and heart rate control by pacing, lumen area decreased by 26% (P = .011) [10].
  • Vasodilation was prevented by prior muscarinic blockade with glycopyrrolate [10].
  • We recorded cortical auditory responses with a magnetometer from 13 healthy subjects after intravenous injection of scopolamine, centrally acting cholinergic antagonist, or glycopyrrolate, a drug with a peripheral anticholinergic properties without penetrating the blood-brain barrier, using a double-blind protocol [11].
  • We found that the sheep model can differentiate between doses of GTA and that the anticholinergic, glycopyrrolate, enhanced transgene expression [12].
  • Further, in vivo application of either Nacystelyn or the anticholinergic glycopyrrolate, both clinically used agents, resulted in increased reporter gene expression in the mouse lung, but no significant correction of the bioelectric defect in CF null mice [13].
 

Chemical compound and disease context of GLYCOPYRROLATE

 

Biological context of GLYCOPYRROLATE

 

Anatomical context of GLYCOPYRROLATE

  • Glycopyrrolate is a quaternary ammonium anticholinergic compound that is poorly absorbed from mucus membranes, thus reducing anticholinergic side effects [22].
  • Glycopyrrolate, a synthetic anticholinergic agent, was administered parenterally to two groups of patients referred for 99mTc-pertechnetate brain imaging to assess its ability to suppress pertechnetate uptake by the choroid plexus, oral mucosa, and salivary (parotid) glands [23].
  • The reduction of gastric juice volume and acidity produced by glycopyrrolate would have important clinical implications in case of accidental aspiration [24].
  • 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 [21].
  • 5. It is concluded that because of its selective inhibitory effect on gastric acid secretions, glycopyrrolate appears superior to other anticholinergic drugs [24].
 

Associations of GLYCOPYRROLATE with other chemical compounds

 

Gene context of GLYCOPYRROLATE

  • 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 [29].
  • 2. Glycopyrrolate and ipratropium bromide inhibited EFS-induced contraction of guinea-pig trachea and human airways in a concentration-dependent manner [30].
  • 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 [31].
  • Racemic glycopyrrolate is an anticholinergic drug that has been used orally to control gastric acidity, parenterally as an antisialogogue and to reverse neuromuscular blockade, and has been studied by inhalation for asthma and COPD [14].
  • At the conclusion of surgery, at a TOF count of 2, neostigmine 0.05 mg/kg plus glycopyrrolate 10 micro g/kg was administered [32].
 

Analytical, diagnostic and therapeutic context of GLYCOPYRROLATE

References

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  2. Gastrointestinal side effects of intravenous erythromycin: incidence and reduction with prolonged infusion time and glycopyrrolate pretreatment. Bowler, W.A., Hostettler, C., Samuelson, D., Lavin, B.S., Oldfield, E.C. Am. J. Med. (1992) [Pubmed]
  3. Effects of anticholinergics on postoperative vomiting, recovery, and hospital stay in children undergoing tonsillectomy with or without adenoidectomy. Chhibber, A.K., Lustik, S.J., Thakur, R., Francisco, D.R., Fickling, K.B. Anesthesiology (1999) [Pubmed]
  4. Vagal cardiac function and arterial blood pressure stability. Wray, D.W., Formes, K.J., Weiss, M.S., O-Yurvati, A.H., Raven, P.B., Zhang, R., Shi, X. Am. J. Physiol. Heart Circ. Physiol. (2001) [Pubmed]
  5. No response to high-dose muscarinic agonist therapy in Alzheimer's disease. Mouradian, M.M., Mohr, E., Williams, J.A., Chase, T.N. Neurology (1988) [Pubmed]
  6. Comparison of the ocular effects of atropine or glycopyrrolate with two I.V. induction agents. Greenan, J., Prasad, J. British journal of anaesthesia. (1985) [Pubmed]
  7. Effects of combined treatment with glycopyrrolate and albuterol in acute exacerbation of chronic obstructive pulmonary disease. Cydulka, R.K., Emerman, C.L. Annals of emergency medicine. (1995) [Pubmed]
  8. Treatment of sialorrhea with glycopyrrolate: A double-blind, dose-ranging study. Mier, R.J., Bachrach, S.J., Lakin, R.C., Barker, T., Childs, J., Moran, M. Archives of pediatrics & adolescent medicine. (2000) [Pubmed]
  9. Glycopyrrolate versus atropine in post-ECT amnesia in the elderly. Sommer, B.R., Satlin, A., Friedman, L., Cole, J.O. Journal of geriatric psychiatry and neurology. (1989) [Pubmed]
  10. Vagal modulation of epicardial coronary artery size in dogs. A two-dimensional intravascular ultrasound study. Kovach, J.A., Gottdiener, J.S., Verrier, R.L. Circulation (1995) [Pubmed]
  11. Auditory sensory memory and the cholinergic system: implications for Alzheimer's disease. Pekkonen, E., Hirvonen, J., Jääskeläinen, I.P., Kaakkola, S., Huttunen, J. Neuroimage (2001) [Pubmed]
  12. Optimizing aerosol gene delivery and expression in the ovine lung. McLachlan, G., Baker, A., Tennant, P., Gordon, C., Vrettou, C., Renwick, L., Blundell, R., Cheng, S.H., Scheule, R.K., Davies, L., Painter, H., Coles, R.L., Lawton, A.E., Marriott, C., Gill, D.R., Hyde, S.C., Griesenbach, U., Alton, E.W., Boyd, A.C., Porteous, D.J., Collie, D.D. Mol. Ther. (2007) [Pubmed]
  13. Mucus altering agents as adjuncts for nonviral gene transfer to airway epithelium. Ferrari, S., Kitson, C., Farley, R., Steel, R., Marriott, C., Parkins, D.A., Scarpa, M., Wainwright, B., Evans, M.J., Colledge, W.H., Geddes, D.M., Alton, E.W. Gene Ther. (2001) [Pubmed]
  14. Glycopyrrolate causes prolonged bronchoprotection and bronchodilatation in patients with asthma. Hansel, T.T., Neighbour, H., Erin, E.M., Tan, A.J., Tennant, R.C., Maus, J.G., Barnes, P.J. Chest (2005) [Pubmed]
  15. Comparative study of atropine and glycopyrrolate on suxamethonium-induced changes in cardiac rate and rhythm. Cozanitis, D.A., Dundee, J.W., Khan, M.M. British journal of anaesthesia. (1980) [Pubmed]
  16. Thiopental-nitrous oxide- halothane anesthesia and repeated succinylcholine: comparison of preoperative glycopyrrolate and atropine administration. Sørensen, O., Eriksen, S., Hommelgaard, P., Viby-Mogensen, J. Anesth. Analg. (1980) [Pubmed]
  17. Mucosal irritant potential of a potassium-sparing diuretic and of wax-matrix potassium chloride. Ryan, J.R., McMahon, F.G., Akdamar, K., Ertan, A., Agrawal, N. Clin. Pharmacol. Ther. (1984) [Pubmed]
  18. Cardiac and vasomotor components of the carotid baroreflex control of arterial blood pressure during isometric exercise in humans. Fisher, J.P., Ogoh, S., Dawson, E.A., Fadel, P.J., Secher, N.H., Raven, P.B., White, M.J. J. Physiol. (Lond.) (2006) [Pubmed]
  19. Increased baroreceptor response in mice deficient in monoamine oxidase A and B. Holschneider, D.P., Scremin, O.U., Roos, K.P., Chialvo, D.R., Chen, K., Shih, J.C. Am. J. Physiol. Heart Circ. Physiol. (2002) [Pubmed]
  20. Infusion of neostigmine-glycopyrrolate for bowel evacuation in persons with spinal cord injury. Korsten, M.A., Rosman, A.S., Ng, A., Cavusoglu, E., Spungen, A.M., Radulovic, M., Wecht, J., Bauman, W.A. Am. J. Gastroenterol. (2005) [Pubmed]
  21. Pharmacological assessment of the duration of action of glycopyrrolate vs tiotropium and ipratropium in guinea-pig and human airways. Villetti, G., Bergamaschi, M., Bassani, F., Bolzoni, P.T., Harrison, S., Gigli, P.M., Janni, A., Geppetti, P., Civelli, M., Patacchini, R. Br. J. Pharmacol. (2006) [Pubmed]
  22. Twelve-hour bronchodilation in asthma with a single aerosol dose of the anticholinergic compound glycopyrrolate. Schroeckenstein, D.C., Bush, R.K., Chervinsky, P., Busse, W.W. J. Allergy Clin. Immunol. (1988) [Pubmed]
  23. Glycopyrrolate in 99mTc-pertechnetate brain imaging. Holmes, R.A., Luth, C.N. J. Nucl. Med. (1975) [Pubmed]
  24. Premedicant drugs and gastric juice pH and volume in pediatric patients. Salem, M.R., Wong, A.Y., Mani, M., Bennett, E.J., Toyama, T. Anesthesiology (1976) [Pubmed]
  25. Analysis of the specificity of physostigmine stimulation of adrenocorticotropin in man. Lewis, D.A., Sherman, B.M., kathol, R.G. J. Clin. Endocrinol. Metab. (1984) [Pubmed]
  26. Analyses of quaternary ammonium drugs in horse urine by capillary electrophoresis-mass spectrometry. Tang, F.P., Leung, G.N., Wan, T.S. Electrophoresis (2001) [Pubmed]
  27. {beta}-Adrenergic receptor desensitization in man: insight into post-exercise attenuation of cardiac function. Hart, E., Dawson, E., Rasmussen, P., George, K., Secher, N.H., Whyte, G., Shave, R. J. Physiol. (Lond.) (2006) [Pubmed]
  28. The cardioacceleratory response to arecoline infusion during sleep in narcoleptic subjects and controls. Baruch, H.L., Kelwala, S., Kapen, S. Sleep. (1987) [Pubmed]
  29. The effects of glycopyrrolate on oral mucous host defenses in healthy volunteers. Lähteenmäki, M.T., Salo, M.S., Tenovuo, J.O., Helminen, A.V., Vilja, P.J., Huupponen, R.K. Anesth. Analg. (2000) [Pubmed]
  30. Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways. Haddad, E.B., Patel, H., Keeling, J.E., Yacoub, M.H., Barnes, P.J., Belvisi, M.G. Br. J. Pharmacol. (1999) [Pubmed]
  31. The effect of glycopyrrolate on postoperative pain and analgesic requirements following laparoscopic sterilisation. Guard, B.C., Wiltshire, S.J. Anaesthesia. (1996) [Pubmed]
  32. Antagonism of cisatracurium and rocuronium block at a tactile train-of-four count of 2: should quantitative assessment of neuromuscular function be mandatory? Kopman, A.F., Zank, L.M., Ng, J., Neuman, G.G. Anesth. Analg. (2004) [Pubmed]
  33. Cholinergic modulation of preattentive auditory processing in aging. Pekkonen, E., Jääskeläinen, I.P., Kaakkola, S., Ahveninen, J. Neuroimage (2005) [Pubmed]
  34. A randomised controlled trial of topical glycopyrrolate, the first specific treatment for diabetic gustatory sweating. Shaw, J.E., Abbott, C.A., Tindle, K., Hollis, S., Boulton, A.J. Diabetologia (1997) [Pubmed]
  35. Endoscopic evaluation of slow-release potassium chloride preparations. Kendall, C., Krantz, K.D., Berger, A., Sharp, T. Clin. Pharmacol. Ther. (1985) [Pubmed]
  36. Effects of prophylactic nalmefene on the incidence of morphine-related side effects in patients receiving intravenous patient-controlled analgesia. Joshi, G.P., Duffy, L., Chehade, J., Wesevich, J., Gajraj, N., Johnson, E.R. Anesthesiology (1999) [Pubmed]
  37. Emesis and defecations induced by the 5-hydroxytryptamine (5-HT3) receptor antagonist zacopride in the ferret. King, G.L. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
 
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