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Equations

This document defines key terms related to drug binding, kinetics, pharmacokinetics, toxicology, and molecular recognition. It defines terms such as KD, rate constants, bioavailability, volume of distribution, clearance, therapeutic index, lethal dose, effective dose, partition coefficient, and eudismic ratio.

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林雪莉
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22 views26 pages

Equations

This document defines key terms related to drug binding, kinetics, pharmacokinetics, toxicology, and molecular recognition. It defines terms such as KD, rate constants, bioavailability, volume of distribution, clearance, therapeutic index, lethal dose, effective dose, partition coefficient, and eudismic ratio.

Uploaded by

林雪莉
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd

Affinity,

efficacy and
potency of
drug binding
• P = fractional receptor occupancy
• DR = drug receptor complex's
• RT = occupied receptors (DR) + unoccupied receptors (R)
• D = drug
• KD = equilibrium dissociation constant
=
• k+1 = rate constant of association
• k-1 = rate constant of dissociation
• Ki = equilibrium dissociation
constant of the ligand displacer (M).
• L = radioligand
Introduction
to ADEM
• F = oral bioavailability (no unit)
• AUC = area under curve (sq unit)
• Vd = apparent volume of distribution (L) or (L/kg)
• Cp = plasma concentration (M)
• t0.5 = half life (time)
• Ct = plasma concentration at time t (M)
• C0 = plasma concentration at time 0 (M)
• t = time (time)
• k = rate constant (min-1)
• Cl = clearance (volume/time)
• Css = steady state concentration (M)
• CssAV = average Css in oral dosing (M)
• Dose of drug (mol)
• T = time interval of dosing (time)
Toxicology
Therapeutic Index (TI) =

• Therapeutic index: reflects the selectivity of a drug to elicit a desired effect


rather than toxicity. (no unit)
• LD50: The dose required to kill 50% of animals (dose).
• ED50: The dose required to produce a particular therapeutic effect in 50% of
animals.
• TD50: The dose required to produce a particular toxic effect in 50% of animals
Therapeutic range (therapeutic
window) = MTD – MED

• Therapeutic range: range of the dosing


level (dose)
• MTD = minimum toxic dose (dose)
• MED = minimum therapeutic dose (dose)
Therapeutic ratio =
Standard Safety Margin (SSM) =

𝑳𝑫𝟏
𝑬𝑫𝟗𝟗

• LD1 = dose required to kill 1% tested animals


• ED99 = dose required to produce a particular
therapeutic effect in 99% tested animals
• ADI = acceptable daily intake (dose)
• NOAEL = no-observed-adverse-effect level
Molecular
Recognition
𝑏𝑖𝑜𝑙𝑜𝑔𝑖𝑐𝑎𝑙 𝑎𝑐𝑡𝑖𝑣𝑖𝑡𝑦 𝑜𝑓 𝑒𝑢𝑡𝑜𝑚𝑒𝑟
𝐸𝑢𝑑𝑖𝑠𝑚𝑖𝑐 𝑅𝑎𝑡𝑖𝑜 𝐸𝑅 =
𝑏𝑖𝑜𝑙𝑜𝑔𝑖𝑐𝑎𝑙 𝑎𝑐𝑡𝑖𝑣𝑖𝑡𝑦 𝑜𝑓 𝑑𝑖𝑠𝑡𝑜𝑚𝑒𝑟
• P = partition coefficient (a parameter that measures the lipophilicity
of a substance.
• [solution]oil = concentration of substance that preferentially
dissolves in the oil layer in the separating funnel containing a layer of
oil and water.
• [solution]water = concentration of substance that preferentially
dissolves in the aqueous layer in the separating funnel containing a
layer of oil and water.

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