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.