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Related Concept Videos

Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and the conjunctiva.
Indirect-Acting Cholinergic Agonists: Pharmacokinetics01:22

Indirect-Acting Cholinergic Agonists: Pharmacokinetics

Indirect-acting cholinergic agonists, or anticholinesterases, enhance the body's cholinergic activity by inhibiting acetylcholine's breakdown. They are categorized as reversible or irreversible agents based on their mechanism of action. They are further classified into short-acting, intermediate-acting, and long-acting agents based on their duration of action.
Reversible agents containing quaternary amines, such as neostigmine and edrophonium, are not easily absorbed orally because they are...
Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics01:11

Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

All neuromuscular blocking agents are injected intravenously because they are poorly absorbed from the GI tract. Rapid onset is achieved with intravenous administration, although absorption is also adequate from an intramuscular injection. Since these agents are highly ionized, they do not readily penetrate cell membranes or cross the blood-brain barrier.
Instead, they are transported by the blood to different tissues. Muscles with a greater blood supply (arteries) and blood flow receive more...
Dosage Regimens: Partial Pharmacokinetic Parameters01:01

Dosage Regimens: Partial Pharmacokinetic Parameters

It is not uncommon for complete drug pharmacokinetic profiles to remain elusive in pharmacokinetics. This necessitates certain educated assumptions by pharmacokineticists to determine appropriate dosage regimens without comprehensive pharmacokinetic data from animal or human studies. One prevalent assumption is setting the bioavailability factor, denoted as F, to 1 or 100%. This assumption caters to the scenario where a drug doesn't achieve full systemic absorption, resulting in the patient...
Depolarizing Blockers: Pharmocokinetics01:19

Depolarizing Blockers: Pharmocokinetics

Depolarizing blockers are administered through intravenous injection. Succinylcholine is the most common choice of depolarizing blockers in emergency clinical practices. Although they have a rapid onset, they readily diffuse away from the motor end plate into the extracellular fluid. They are metabolized by enzymes such as liver butyrylcholinesterase and plasma pseudocholinesterases. This produces a short duration of action, typically 5-10 minutes long, unlike nondepolarizing blockers, which...

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Related Experiment Video

Updated: Jul 13, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

Pharmacokinetic rationale for the rivastigmine patch.

Jeffrey Cummings1, Gilbert Lefèvre, Gary Small

  • 1UCLA Alzheimer's Center, Los Angeles, CA 90095-7226, USA. jcummings@mednet.ucla.edu

Neurology
|July 31, 2007
PubMed
Summary

The new rivastigmine patch offers a potential alternative to oral capsules for Alzheimer disease (AD) and Parkinson disease (PD) dementia treatment. It may reduce gastrointestinal side effects while maintaining therapeutic drug exposure.

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Using Enzyme-based Biosensors to Measure Tonic and Phasic Glutamate in Alzheimer's Mouse Models
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Using Enzyme-based Biosensors to Measure Tonic and Phasic Glutamate in Alzheimer's Mouse Models

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Related Experiment Videos

Last Updated: Jul 13, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

Using Enzyme-based Biosensors to Measure Tonic and Phasic Glutamate in Alzheimer's Mouse Models
10:46

Using Enzyme-based Biosensors to Measure Tonic and Phasic Glutamate in Alzheimer's Mouse Models

Published on: May 3, 2017

Area of Science:

  • Pharmacology
  • Neurology
  • Drug Delivery Systems

Background:

  • Rivastigmine, a dual cholinesterase inhibitor, treats dementia in Alzheimer disease (AD) and Parkinson disease (PD).
  • Oral formulations are linked to central cholinergic gastrointestinal side effects, especially during dose titration.
  • These side effects are attributed to rapid increases in brain acetylcholine levels.

Purpose of the Study:

  • To evaluate the potential of a newly developed rivastigmine transdermal patch.
  • To assess if the patch can mitigate gastrointestinal side effects associated with oral rivastigmine.
  • To compare pharmacokinetic profiles and therapeutic exposure between the patch and oral capsules.

Main Methods:

  • Pharmacokinetic studies were conducted to analyze rivastigmine absorption and distribution.
  • Plasma concentrations, time to maximum concentration (tmax), and maximum concentration (Cmax) were measured.
  • Area under the curve (AUC) was calculated to assess overall drug exposure.

Main Results:

  • Transdermal rivastigmine administration resulted in prolonged tmax, lower Cmax, and reduced plasma concentration fluctuations.
  • A 10-cm(2) rivastigmine patch demonstrated comparable AUC to the highest oral capsule dose (6-mg BID).
  • The patch may provide optimal therapeutic exposure for maintenance dosing.

Conclusions:

  • The rivastigmine transdermal patch shows potential for improved tolerability compared to oral capsules.
  • Similar drug exposure achieved with the patch could lead to enhanced efficacy and patient compliance.
  • This formulation may offer a viable option for managing AD and PD dementia with fewer side effects.