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Related Concept Videos

Bioequivalence: Overview01:16

Bioequivalence: Overview

Pharmaceutical equivalents, by definition, are drug products with the same active ingredient in the same quantities, encapsulated in identical dosage forms, and intended for the same administration routes. These pharmaceutical equivalents are deemed bioequivalent if the bioavailability of the active entity in the drug preparations is similar. Moreover, pharmaceutical equivalents demonstrating bioequivalence are also regarded as therapeutically equivalent. This means that when used as directed,...
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.
Pharmacokinetics: Overview01:10

Pharmacokinetics: Overview

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) administration...
Equivalence: In Vitro and In Vivo Bioequivalence01:17

Equivalence: In Vitro and In Vivo Bioequivalence

Bioequivalence studies are crucial in evaluating whether new drugs can match an approved one regarding pharmacological effects and clinical performance. These studies test if drugs, despite different dosage forms, share identical plasma concentration-time profiles. Three types of equivalence are central to these studies: chemical, pharmaceutical, and therapeutic. Chemical equivalence indicates that two or more drug products contain identical active ingredients in equal amounts. Pharmaceutical...
Pharmacokinetic–Pharmacodynamic Relationship: Dose to Pharmacological Effect01:28

Pharmacokinetic–Pharmacodynamic Relationship: Dose to Pharmacological Effect

A drug’s dosage and pharmacokinetic properties determine how quickly it acts, how intense its effects are, and how long it lasts. Higher doses increase drug concentration at receptor sites, producing a hyperbolic curve when pharmacologic response is plotted against drug dose. Converting this scale to a log-linear format results in a sigmoidal curve, better representing dose–response relationships.For drugs following a one-compartment model, the pharmacologic response is directly proportional to...
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.
Reversible agents containing quaternary amines, such as neostigmine and edrophonium, are not easily absorbed orally because they are...

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Use of Micropipette-Guided Drug Administration as an Alternative Method to Oral Gavage in Rodent Models
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Equol: pharmacokinetics and biological actions.

Kenneth D R Setchell1, Carlo Clerici

  • 1Pathology and Laboratory Medicine, Department of Pediatrics, Cincinnati Children's Hospital Medical Center, Cincinnati, OH 45229, USA. kenneth.setchell@cchmc.org

The Journal of Nutrition
|June 4, 2010
PubMed
Summary

Equol, a compound from soy isoflavones, has two forms: S-(-)equol and R-(+)equol. Research reviews their pharmacokinetics and potential biological effects, particularly S-(-)equol

Area of Science:

  • Pharmacology
  • Microbiology
  • Endocrinology

Background:

  • Equol (7-hydroxy-3-(4'-hydroxyphenyl)-chroman) is an isoflavan derived from soy isoflavones by intestinal bacteria.
  • Equol exists as S-(-)equol and R-(+)equol diastereoisomers, with intestinal bacteria producing only S-(-)equol.
  • S-(-)equol demonstrates selective affinity for the estrogen receptor (ER)-beta.

Purpose of the Study:

  • To review and summarize the plasma and urinary pharmacokinetics of S-(-)equol and R-(+)equol.
  • To consider recent evidence supporting the potential biological effects of S-(-)equol.
  • To highlight the implications of synthesizing equol diastereoisomers for future clinical trials in hormone-dependent conditions.

Main Methods:

  • Review of existing literature on equol pharmacokinetics (plasma and urinary).

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  • Analysis of recent scientific evidence regarding the biological activities of S-(-)equol.
  • Consideration of the synthetic accessibility of equol diastereoisomers.
  • Main Results:

    • Summarized pharmacokinetic data for both S-(-)equol and R-(+)equol.
    • Presented emerging evidence for the biological effects of S-(-)equol.
    • Acknowledged conflicting evidence regarding the advantage of producing S-(-)equol.

    Conclusions:

    • The synthesis of equol diastereoisomers facilitates direct clinical investigation.
    • Further research is warranted to elucidate the specific roles and therapeutic potential of S-(-)equol and R-(+)equol.
    • Understanding equol's pharmacokinetics is crucial for exploring its applications in hormone-related conditions.