Pharmacokinetics and Oral Bioavailability of Scopolamine in Normal Subjects

  title={Pharmacokinetics and Oral Bioavailability of Scopolamine in Normal Subjects},
  author={Lakshmi Putcha and Nitza M. Cintr{\'o}n and James Tsui and James M. Vanderploeg and William G. Kramer},
  journal={Pharmaceutical Research},
The pharmacokinetics and bioavailability of scopolamine were evaluated in six healthy male subjects receiving 0.4 mg of the drug by either oral or intravenous administration. Plasma and urine samples were analyzed using a radioreceptor binding assay. After iv administration, scopolamine concentrations in the plasma declined in a biexponential fashion, with a rapid distribution phase and a comparatively slow elimination phase. Mean and SE values for volume of distribution, systemic clearance… 
Dose escalation pharmacokinetics of intranasal scopolamine gel formulation
The results suggest that intranasal scopolamine gel formulation (INSCOP) offers a fast, reliable, and safe alternative for the treatment of motion sickness.
Effects of pH and Dose on Nasal Absorption of Scopolamine Hydrobromide in Human Subjects
Nasal absorption of scopolamine hydrobromide in human subjects increased substantially with increases in formulation pHand dose, and both the Cmaxand AUC values were almost doubled with doubling the dose.
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.
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.
Pharmacokinetics and Pharmacodynamics in Clinical Use of Scopolamine
Scopolamine has been shown to undergo an oxidative demethylation during incubation with CYP3A (cytochrome P-450 subfamily), and the glucuronide conjugation of scopolamine could be the relevant pathway in healthy volunteers.
A Comparison of Intranasal and Oral Scopolamine for Motion Sickness Prevention in Military Personnel
Abstract : Results from preliminary studies indicate intranasal scopolamine (IN SCOP) has faster absorption, higher bioavailability, and a more reliable therapeutic index than equivalent oral (PO
Reduced systemic exposure and brain uptake of donepezil in rats with scopolamine-induced cognitive impairment
Tmax ofDPZ and its three metabolites were prolonged and their brain uptake were decreased in scopolamine-induced rats, suggesting the potential reduced absorption of DPZ.
Efficacy of Intranasal Scopolamine Gel for Motion Sickness Treatment in Aviation Candidates
Results from preliminary studies indicate that intranasal scopolamine (INSCOP) has faster absorption, higher bioavailability and reliable therapeutic index than oral or transdermal forms and offers an excellent alternative for use in dynamic operational environments.
Clinical Pharmacokinetics of Drugs Used to Treat Urge Incontinence
  • D. Guay
  • Medicine, Biology
    Clinical pharmacokinetics
  • 2003
Only for oxybutynin and tolterodine are there adequate efficacy/tolerability data to support their use in urge incontinence, and the use of alternative formulations (controlled-release oral, transdermal) may also facilitate adherence.


Placental Transfer and Pharmacokinetics of Atropine after a Single Maternal Intravenous and Intramuscular Administration
The placental transfer and pharmacokinetics of atropine were studied in 44 healthy parturients undergoing caesarean section and there was a difference in the umbilical vein and artery concentrations after intramuscular administration.
Plasma atropine concentrations determined by radioimmunoassay after single-dose i.v. and i.m. administration.
Atropine, as a premedication, should be given not later than 30 min before induction of anaesthesia, probably because of uptake of atropine by muscarinic cholinergic receptors.
A sensitive radioreceptor assay for determining scopolamine concentrations in plasma and urine.
The applicability of the procedure for therapeutic drug monitoring of scopolamine was demonstrated by using the method to determine plasma levels in humans after transdermal administration.
Pharmacokinetics of drug permeation through human skin.
A mathematical model was developed for estimating and optimizing the temporal pattern of scopolamine delivery from a transdermal therapeutic system through human skin in vivo and experimentally measured scopolamines delivery in vivo conformed to this model.
The Pharmacological Basis of Therapeutics
On pharmacology and the rational use of drugs, 42 authors share the herculean task of reviewing the flood of recent literature under single or dual authorship and each chapter offers a complete and up-to-date review.