Pharmacokinetics and Pharmacodynamics in Clinical Use of Scopolamine
@article{Renner2005PharmacokineticsAP, title={Pharmacokinetics and Pharmacodynamics in Clinical Use of Scopolamine}, author={Ulf D Renner and Reinhard Oertel and Wilhelm Kirch}, journal={Therapeutic Drug Monitoring}, year={2005}, volume={27}, pages={655-665} }
The alkaloid L-(−)-scopolamine [L-(−)-hyoscine] competitively inhibits muscarinic receptors for acetylcholine and acts as a nonselective muscarinic antagonist, producing both peripheral antimuscarinic properties and central sedative, antiemetic, and amnestic effects. The parasympatholytic scopolamine, structurally very similar to atropine (racemate of hyoscyamine), is used in conditions requiring decreased parasympathetic activity, primarily for its effect on the eye, gastrointestinal tract…
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References
SHOWING 1-10 OF 97 REFERENCES
Development and application of a radioreceptor assay for scopolamine.
- Biology, MedicineArzneimittel-Forschung
- 1988
A highly sensitive radioreceptor assay with an absolute detection limit of 15 pg scopolamine was developed and moderate anticholinergic effects were observed in patients, although in general the patches were well tolerated.
Pharmacokinetics and related pharmacodynamics of anticholinergic drugs
- Biology, MedicineActa anaesthesiologica Scandinavica
- 1993
The pharmacokinetics and some pharmacodynamic properties of atropine, glycopyrrolate and scopolamine are reviewed and the differences in clinical effects are not very prominent in healthy patients.
Pharmacokinetic implications for the clinical use of atropine, scopolamine and glycopyrrolate
- Medicine, BiologyActa anaesthesiologica Scandinavica
- 1988
Age, but not sex, appears to have a clear effect on its kinetics, explaining at least partly the higher sensitivity of very young and very old patients to this anticholinergic agent.
Transdermal hyoscine (Scopolamine). A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
- Medicine, BiologyDrugs
- 1985
Transdermal hyoscine may offer an effective and conveniently administered alternative for the prevention of motion-induced nausea and vomiting in certain situations, but the duration of its clinical effectiveness, and its relative efficacy and tolerability compared with other agents needs to be confirmed.
Pharmacokinetic‐Pharmacodynamic Modeling of the Electroencephalogram Effects of Scopolamine in Healthy Volunteers
- Medicine, BiologyJournal of clinical pharmacology
- 2001
The results provide the first demonstration of a direct correlation between serum concentrations of scopolamine and changes in total power in alpha frequency band in healthy volunteers using PK‐PD modeling techniques and indicate a rapid equilibration between serum and effect site.
Comparison of radioreceptor assay and radioimmunoassay for atropine: Pharmacokinetic application
- Biology, MedicineEuropean Journal of Clinical Pharmacology
- 2004
The RRA measures only the active component of atropine, 1-hyscyamine and in this respect it differs from the RIA and the pharmacokinetics according to the 2 methods are presumably due to preferential tissue uptake of the l-form.
Pharmacokinetics of scopolamine during caesarean section: relationship between serum concentration and effect
- Medicine, BiologyActa anaesthesiologica Scandinavica
- 1989
There appears to be a surprisingly great difference between the pharmacokinetic parameters and the clinical effects of scopolamine, which appeared to be delayed, but long‐lasting in contrast to the rapid absorption and quick disappearance from the serum.
A comparison of plasma levels of hyoscine after oral and transdermal administration.
- Medicine, BiologyJournal of pharmaceutical and biomedical analysis
- 1983
Glycopyrrolate: pharmacokinetics and some pharmacodynamic findings
- Biology, MedicineActa anaesthesiologica Scandinavica
- 1989
The RRA method proved to be quite useful in evaluating the kinetics of glycopyrrolate and its relationship to various clinical effects, indicating that the oral route of drug administration is of no value as a routine premedication.
Pharmacokinetic Considerations in the Use of Newer Transdermal Formulations
- Biology, MedicineClinical pharmacokinetics
- 1988
Overall, while the enthusiasm for attraction and benefits of transdermal delivery remain evident, it is clear that future successes will demand a heightened level of commitment and skill from the pharmaceutical scientist.