Why chloroquine has high volume of distribution

Discussion in 'Plaquenil Generic' started by pimc, 11-Mar-2020.

  1. Surok97 Guest

    Why chloroquine has high volume of distribution


    In rough terms, drugs with a high lipid solubility (non-polar drugs), low rates of ionization, or low plasma protein binding capabilities have higher volumes of distribution than drugs which are more polar, more highly ionized or exhibit high plasma protein binding in the body's environment. Volume of distribution may be increased by kidney failure (due to fluid retention) and liver failure (due to altered body fluid and plasma protein binding). The initial volume of distribution describes blood concentrations prior to attaining the apparent volume of distribution and uses the same formula.

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    If the drug distributes into all body water the volume of distribution would increase to approximately = 0.57 l/kg If the drug readily diffuses into the body fat the volume of distribution may increase dramatically, an example is chloroquine which has a = 250-302 l/kg Bioavailability is 89% for tablets. Peak plasma concentration is reached 1.5 to 3 hours after ingestion. Distribution by route of exposure Protein binding 5O to 65%. Chloroquine accumulates in high concentrations in kidney, liver, lung and spleen, and is strongly bound in melanin-containing cells eye and skin. Red cell concentration is five to ten times the plasma concentration. The volume of distribution at steady state will also be influenced by protein binding and consequently the terminal half-life. Drugs can compete for the same binding site and thus there is the potential for drug-drug interactions, this would be a particular concern for highly protein bound drugs that have a low therapeutic index such as warfarin.

    As body composition changes with age, V But this is generally not what happens. Is not a physiologic value; it is more a reflection of how a drug will distribute throughout the body depending on several physicochemical properties, e.g. The unit for Volume of Distribution is typically reported in liters.

    Why chloroquine has high volume of distribution

    Disposition of chloroquine in man after single intravenous and oral doses., Chloroquine phosphate C18H32ClN3O8P2 - PubChem

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  4. Basic Concepts in Pharmacokinetics. Objectives 1. Define pharmacokinetics 2. Describe absorption 3. Describe distribution. Volume of Distribution V d = Apparent and hypothetical volume in which the drug is dispersed. Very high molecular weight drugs,

    • Basic Concepts in Pharmacokinetics.
    • Distribution and plasma protein binding Cambridge MedChem..
    • Clinical Pharmacokinetics and Metabolism of Chloroquine..

    Chloroquine was selected as the agent of choice for further studies, as this drug displayed the highest potency as an uptake inhibitor and was previously shown to have a high volume of. Volume of distribution is a pharmacokinetic concept which is used to describe the distribution of drugs in the body as relative to the measured concentration. In brief, it is the apparent volume into which the drug appears to be distributed when only the sample concentration is considered. It is a purely theoretical volume, which can substantially exceed the total body volume, or potentially. In contrast to quinine which has a relatively limited apparent volume of distribution approximately 2.51/kg in healthy adults and short elimination half-life 11 hours in healthy subjects, 16 hours in cerebral malaria, chloroquine has an enormous total apparent volume of distribution 100–10001/kg and a terminal elimination half-life of.

     
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