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1.
Am J Emerg Med ; 46: 797.e1-797.e2, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-33583621

RESUMO

We describe a case of a young female who presented to the emergency department with 4 days of progressive myopia, dry mouth, anhidrosis and urinary hesitancy due to overuse of a new topical anticholinergic wipes, glycopyrronium tosylate (GT). In the United States medication misuse accounts for nearly 10% of pediatric emergency visits with 65% of these visits considered to be preventable [1]. Being familiar with new medications and their side effect profiles can prevent unnecessary or harmful interventions.


Assuntos
Antagonistas Colinérgicos/toxicidade , Glicopirrolato/toxicidade , Administração Tópica , Adolescente , Axila , Antagonistas Colinérgicos/administração & dosagem , Serviço Hospitalar de Emergência , Feminino , Glicopirrolato/administração & dosagem , Rouquidão/induzido quimicamente , Humanos , Hiperidrose/tratamento farmacológico , Midríase/induzido quimicamente , Incontinência Urinária/induzido quimicamente
2.
Toxicol Appl Pharmacol ; 287(1): 9-16, 2015 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-26026369

RESUMO

Long acting inhaled muscarinic receptor antagonists, such as tiotropium, are widely used as bronchodilator therapy for chronic obstructive pulmonary disease (COPD). Although this class of compounds is generally considered to be safe and well tolerated in COPD patients the cardiovascular safety of tiotropium has recently been questioned. We describe a rat in vivo model that allows the concurrent assessment of muscarinic antagonist potency, bronchodilator efficacy and a potential for side effects, and we use this model to compare tiotropium with NVA237 (glycopyrronium bromide), a recently approved inhaled muscarinic antagonist for COPD. Anaesthetized Brown Norway rats were dosed intratracheally at 1 or 6h prior to receiving increasing doses of intravenous methacholine. Changes in airway resistance and cardiovascular function were recorded and therapeutic indices were calculated against the ED50 values for the inhibition of methacholine-induced bronchoconstriction. At both time points studied, greater therapeutic indices for hypotension and bradycardia were observed with glycopyrronium (19.5 and 28.5 fold at 1h; >200 fold at 6h) than with tiotropium (1.5 and 4.2 fold at 1h; 4.6 and 5.5 fold at 6h). Pharmacokinetic, protein plasma binding and rat muscarinic receptor binding properties for both compounds were determined and used to generate an integrated model of systemic M2 muscarinic receptor occupancy, which predicted significantly higher M2 receptor blockade at ED50 doses with tiotropium than with glycopyrronium. In our preclinical model there was an improved safety profile for glycopyrronium when compared with tiotropium.


Assuntos
Broncoconstrição/efeitos dos fármacos , Broncodilatadores/farmacocinética , Sistema Cardiovascular/efeitos dos fármacos , Glicopirrolato/farmacocinética , Antagonistas Muscarínicos/farmacocinética , Derivados da Escopolamina/farmacocinética , Resistência das Vias Respiratórias/efeitos dos fármacos , Animais , Pressão Sanguínea/efeitos dos fármacos , Bradicardia/induzido quimicamente , Bradicardia/fisiopatologia , Testes de Provocação Brônquica , Broncodilatadores/administração & dosagem , Broncodilatadores/sangue , Broncodilatadores/toxicidade , Sistema Cardiovascular/fisiopatologia , Glicopirrolato/administração & dosagem , Glicopirrolato/sangue , Glicopirrolato/toxicidade , Frequência Cardíaca/efeitos dos fármacos , Hipotensão/induzido quimicamente , Hipotensão/fisiopatologia , Masculino , Modelos Biológicos , Antagonistas Muscarínicos/administração & dosagem , Antagonistas Muscarínicos/sangue , Antagonistas Muscarínicos/toxicidade , Ligação Proteica , Ensaio Radioligante , Ratos Endogâmicos BN , Receptor Muscarínico M2/efeitos dos fármacos , Receptor Muscarínico M2/metabolismo , Medição de Risco , Derivados da Escopolamina/administração & dosagem , Derivados da Escopolamina/sangue , Derivados da Escopolamina/toxicidade , Brometo de Tiotrópio
3.
Acta Anaesthesiol Scand ; 28(1): 112-5, 1984 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-6711256

RESUMO

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.


Assuntos
Atropina/toxicidade , Glicopirrolato/toxicidade , Medicação Pré-Anestésica , Pirrolidinas/toxicidade , Transtornos Urinários/induzido quimicamente , Adulto , Método Duplo-Cego , Feminino , Frequência Cardíaca/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Náusea/induzido quimicamente , Cateterismo Urinário , Vômito/induzido quimicamente
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