Pharmacokinetics and Pharmacodynamics in Clinical Use of Scopolamine

  title={Pharmacokinetics and Pharmacodynamics in Clinical Use of Scopolamine},
  author={Ulf D Renner and Reinhard Oertel and Wilhelm Kirch},
  journal={Therapeutic Drug Monitoring},
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… 
Liquid Chromatography-Mass Spectrometric Analysis of Tropane Alkaloids in Mammalian Samples: Techniques and Applications
TA are used as antiemetic to treat vomiting and nausea and being used to improve blood flow for the treatment of septic shock, and ingestion of plants containing natural TA such as hyoscyamine and scopolamine may cause fatal intoxications.
Pharmacokinetic-pharmacodynamic relationships of central nervous system effects of scopolamine in healthy subjects.
Scopolamine affected different CNS functions in a concentration-dependent manner, which based on their distinct PK-PD characteristics seemed to reflect multiple distinct functional pathways of the cholinergic system.
Scopolamine: a journey from the field to clinics
The aim of this review is to give a comprehensive overview regarding the current knowledge on botanical origin, pharmacology, biosynthesis as well as agricultural and biotechnological production of scopolamine.
Scopolamine Sublingual Spray: An Alternative Route of Delivery for the Treatment of Motion Sickness
Considering the limitations of delivering scopolamine orally or transdermally to patients who experience motion sickness, the sublingual route of administration using a spray delivery dosage form, is a potential alternative modality for the prevention of nausea and vomiting associated with motion sickness.
Comparative effects of scopolamine and phencynonate on organophosphorus nerve agent-induced seizure activity, neuropathology and lethality
The differing efficacies of phencynonate and scopolamine when given at the early or late phase of seizure progression are demonstrated and warrant further investigation into the timing and mechanisms of the seizure maintenance phase in different animal models.
A Selective M1 and M3 Receptor Antagonist, Penehyclidine Hydrochloride, Exerts Antidepressant-Like Effect in Mice
The findings suggest that PHC, an anti-muscarinic drug in clinical use, elicits rapid onset antidepressant-like effect, shedding light on the development of new antidepressants.
The Pharmacokinetics and Efficacy of a Low-dose, Aqueous, Intranasal Scopolamine Spray
INSCOPs positive efficacy and safety profile having been identified, future studies can address multi-dose schedules and operational field trials.
Anticholinergic syndrome following an unintentional overdose of scopolamine
The need to consider nonprescription products, ie, over the counter medications, herbal/nutritional supplements as causes of anticholinergic syndrome when a patient presents with symptoms suggestive of this diagnosis is highlighted.


Development and application of a radioreceptor assay for scopolamine.
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
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
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.
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
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
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
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.
  • C. Muir, R. Metcalfe
  • Medicine, Biology
    Journal of pharmaceutical and biomedical analysis
  • 1983
Glycopyrrolate: pharmacokinetics and some pharmacodynamic findings
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
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.