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Related Concept Videos

Ophthalmic Drug Delivery Systems01:23

Ophthalmic Drug Delivery Systems

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Ophthalmic drug delivery faces major limitations due to poor absorption across the corneal membrane. This process is primarily driven by diffusion and is influenced by two main factors: the physicochemical properties of the drug and tear drainage. Most ophthalmic drugs, such as pilocarpine, epinephrine, atropine, and local anesthetics, are weak bases. They are typically formulated at an acidic pH to enhance chemical stability. However, this leads to high ionization, reducing their ability to...
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Indirect-Acting Cholinergic Agonists: Pharmacokinetics01:22

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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.
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As individuals age, their body's physiology evolves, affecting drug pharmacokinetics. The most apparent changes occur in the gastrointestinal tract, where an increase in gastric pH, a delay in gastric emptying, and a reduction in gastrointestinal motility are observed. Remarkably, these changes do not substantially modify the absorption of orally administered drugs, particularly those absorbed via passive diffusion.Transdermal drug delivery emerges as a highly viable method for older adults due...
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Cholinergic Antagonists: Pharmacokinetics01:24

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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...
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Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

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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...
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Pharmacokinetics: Overview01:10

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Pharmacokinetics is a scientific discipline that focuses on the journey of a drug within the body, encompassing four key stages: absorption, distribution, metabolism, and elimination. The first stage, absorption, involves the drug's transfer into the bloodstream. Several factors dictate the extent and speed of this process. For example, the liver often metabolizes oral drugs before they reach systemic circulation, leading to only partial absorption. In contrast, intravenous (IV)...
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Use of Rabbit Eyes in Pharmacokinetic Studies of Intraocular Drugs
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A comprehensive insight on ocular pharmacokinetics.

Vibhuti Agrahari1, Abhirup Mandal1, Vivek Agrahari1,2

  • 1Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 2464 Charlotte Street, Kansas City, MO, 64108, USA.

Drug Delivery and Translational Research
|November 6, 2016
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Summary

Understanding ocular drug delivery pharmacokinetics is crucial for effective eye treatments. This review details compartment models, influencing factors, and challenges in ocular drug absorption, distribution, and elimination.

Keywords:
Animal modelsAnterior chamberCompartment modelsOcular pharmacokineticsPosterior chamberSimulation studyTransporter

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Area of Science:

  • Ocular pharmacology
  • Drug delivery systems
  • Pharmacokinetics

Background:

  • The eye presents unique anatomical and physiological barriers to drug delivery.
  • Ocular drug delivery requires specialized pharmacokinetic models to understand drug disposition.
  • Determining pharmacokinetics parameters in ocular tissues is complex due to the eye's dynamic nature.

Purpose of the Study:

  • To review pharmacokinetic compartment models for ocular drug delivery.
  • To explore factors influencing intraocular drug bioavailability.
  • To summarize ocular transporters and relevant animal models.

Main Methods:

  • Literature review of ocular pharmacokinetics.
  • Analysis of various drug delivery systems and administration routes.
  • Discussion of factors affecting ocular drug absorption, distribution, and elimination.

Main Results:

  • Several pharmacokinetic compartment models for ocular drug delivery are discussed.
  • Factors like precorneal drainage, protein binding, and corneal penetration significantly impact bioavailability.
  • Ocular transporters and animal models play a key role in studying ocular pharmacokinetics.

Conclusions:

  • Ocular drug delivery is challenging due to multiple physiological barriers and factors.
  • Compartment models and understanding transporters are essential for optimizing ocular drug therapies.
  • Further research using animal models aids in developing effective ocular formulations.