Pharmacokinetics and related pharmacodynamics of anticholinergic drugs

  title={Pharmacokinetics and related pharmacodynamics of anticholinergic drugs},
  author={Timo Ali‐Melkkil{\"a} and Jussi H. Kanto and E. U. M. Iisalo},
  journal={Acta Anaesthesiologica Scandinavica},
The pharmacokinetics and some pharmacodynamic properties of atropine, glycopyrrolate and scopolamine are reviewed. With the development of new analytical methods for drug determination, it is now possible to measure relatively low concentrations of these drugs in biological fluids and, consequently, some new kinetic data have been collected. Following intravenous administration, a fast disappearance from the circulation is observed and due to a high total clearance value their elimination phase… 

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.

Pharmacokinetics and pharmacodynamics of glycopyrrolate following a continuous-rate infusion in the horse.

The relationship between plasma GLY concentration and heart rate exhibited counterclockwise hysteresis that was adequately described using an effect compartment and an improved understanding of the plasma concentration-effect relationship in racehorses is warranted.

Pharmacology, toxicology and clinical safety of glycopyrrolate

Pharmacokinetic and Pharmacodynamic Evaluations of the Zwitterionic Metabolite of a New Series of N-Substituted Soft Anticholinergics

N-Substituted zwitterionic metabolites retain some, but only considerably reduced activity of their parent quaternary ammonium ester soft anticholinergic drugs, and they are very rapidly eliminated from the systemic circulation.

Pharmacological effects of some newly developed soft anticholinergics and a receptor-binding QSAR study.

Receptor-binding studies using cloned human muscarinic receptors were performed on newly synthesized soft anticholinergics that are isosteric/ isoelectronic analogs of glycopyrrolate, confirming the known stereospecificity of these receptors, pure 2R isomers were found more active than the corresponding isomeric mixtures.

Synthesis and pharmacological effects of new, N‐substituted soft anticholinergics based on glycopyrrolate

  • F. JiW. Wu N. Bodor
  • Chemistry, Biology
    The Journal of pharmacy and pharmacology
  • 2005
Two new N‐substituted glycopyrrolate analogues designed using soft drug design approaches have been synthesized and evaluated in vitro and in vivo, indicating that, in agreement with their soft nature, they are locally active, but safe and with a low potential to cause systemic side‐effects.

Anticholinergics in Palliative Medicine

  • E. Prommer
  • Biology, Medicine
    The American journal of hospice & palliative care
  • 2013
The purpose of this review is to highlight anticholinergic agents, their pharmacology, and an evidence-based assessment of their role in palliative care.

Antidote for organophosphate insecticide poisoning: atropine and pralidoxime

Pralidoxime is a biochemical antidote that reactivates acetylcholinesterase by removing OP from it, and is effective in treating both muscarinic and nicotinic symptoms.

Oral glycopyrrolate after the failure of oral oxybutynin in the treatment of primary hyperhidrosis

GLY was prescribed to patients diagnosed with primary hyperhidrosis between January 2012 and October 2014, for whom previous treatment with oral oxybutynin had failed, and the response was excellent for 15 patients (65%) and partial for four patients (17%).

Pharmacokinetics and Pharmacodynamics of Glycopyrrolate in the Horse

Pharmacokinetics studies are important for determining drug plasma and urine concentrations following a typical often clinically relevant dosage in horseracing.



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.

Intramuscular atropine in elderly people: pharmacokinetic studies using the radioreceptor assay and some pharmacodynamic responses.

The pharmacokinetics (radioreceptor assay, RRA) and some clinical effects of atropine were studied in 7 elderly gynaecological surgery patients and the sedative effect of the drug is clear and long lasting in elderly people.

Integrated pharmacokinetics and pharmacodynamics of atropine in healthy humans. I: Pharmacokinetics.

There was evidence that the kinetics of distribution of the drug was dose dependent and the renal clearance of atropine depended on urine flow, implying extensive tissue binding and/or partitioning.

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.

Integrated pharmacokinetics and pharmacodynamics of atropine in healthy humans. II: Pharmacodynamics.

The kinetics of the effects of atropine on heart rate and saliva flow in three healthy male volunteers after intravenous administration of 1.35 and 2.15 mg of the drug were determined simultaneously.

Pharmacokinetics of atropine in children.

RIA appeared to be useful in the clinical kinetic studies of this alkaloid, but RRA determined the whole antimuscarinic activity produced by atropine plus glycopyrrolate when the latter agent was used as an anticurarizing component together with neostigmine at the end of anesthesia.

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.

Intramuscular atropine in healthy volunteers: a pharmacokinetic and pharmacodynamic study.

The plasma concentrations of l-hyoscyamine and the change in heart rate expressed as percentages showed a linear correlation: concentrations under 0.5 micrograms/l caused slowing of rate, higher concentrations caused acceleration and the antisialagogue effect correlated with plasma concentrations.

Anticholinergic drugs in anaesthesia.

  • R. Mirakhur
  • Medicine
    British journal of hospital medicine
  • 1991
Before assessing the value of these drugs critically, it was considered worthwhile to conduct a countrywide survey amongst practising anaesthetists regarding their use in premedication and anaesthesia to see if the general concepts about anticholinergic drugs inPremedication had changed.

Radioreceptor assay of anticholinergic drugs.

Results with RRA have been shown to correlate with anticholinergic effects, both desired and side effects, and a careful familiarization with the method used for each individual drug analysis allows its useful clinical application.