Introductionwwwwwwwwwwwlwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwll
● Pharmacology = PK + PD
○ Pharmacokinetics: What the body does to the drug → Describe these changes
■ Amount of drug in the body at a certain time point → Calculate how much
the amount changes
■ Fate of drug in the body as a function of the time (Described by ADME)
○ Pharmacodynamics: What does the drug do to the body
■ Together find the therapeutic effect of the drug
● Effect of a drug
○ Binding to receptor → Receptor activation → Therapeutic effect
○ Medicine needs to achieve sufficient concentration at the right place (Hard to get
in brain through BBB e.g.)
■ Target concentration: Sufficient concentration at the right place (=target)
● Most commonly plasma concentration is used as a proximation for
the target concentration, because it’s very hard to measure
○ Relation of drug exposure and cplasma = (drug) plasma concentration
○ Relation of plasma concentration and dose
■ What happens with this size dose and how does it change over time?
● PK in practice
○ Drug development
■ Calculate the time it reaches a muscle etc.
○ Determination of dosing regimen
■ Also for individual patients
○ Dose adjustments
■ Certain increase in plasma concentration → Why and how to bring it back
to TW
○ Toxicology
○ Used in community and hospital pharmacies and in drug development
○ Preclinical testing: Asses safety of drug in 4 phases
■ Bioequivalence study: Study on generic compound → Plasma
concentration curve comparisons
● Don’t have to go through all phases → Only prove that it’s the
same as the originator (Same active ingredient + therapeutic
effect)
● Dosing equal, so everything else should also be the same
● Main parameters read from the curve:
○ tmax: at which time point the Cmax is reached
○ Cmax
● Therapeutic and adverse effects are already correlated to the
plasma concentration
● Therapeutic window: Concentration range where the therapeutic response is adequate
and adverse effects are tolerable
● ADME
○ Absorption: Amount of drug entering the systemic circulation
● Pharmacology = PK + PD
○ Pharmacokinetics: What the body does to the drug → Describe these changes
■ Amount of drug in the body at a certain time point → Calculate how much
the amount changes
■ Fate of drug in the body as a function of the time (Described by ADME)
○ Pharmacodynamics: What does the drug do to the body
■ Together find the therapeutic effect of the drug
● Effect of a drug
○ Binding to receptor → Receptor activation → Therapeutic effect
○ Medicine needs to achieve sufficient concentration at the right place (Hard to get
in brain through BBB e.g.)
■ Target concentration: Sufficient concentration at the right place (=target)
● Most commonly plasma concentration is used as a proximation for
the target concentration, because it’s very hard to measure
○ Relation of drug exposure and cplasma = (drug) plasma concentration
○ Relation of plasma concentration and dose
■ What happens with this size dose and how does it change over time?
● PK in practice
○ Drug development
■ Calculate the time it reaches a muscle etc.
○ Determination of dosing regimen
■ Also for individual patients
○ Dose adjustments
■ Certain increase in plasma concentration → Why and how to bring it back
to TW
○ Toxicology
○ Used in community and hospital pharmacies and in drug development
○ Preclinical testing: Asses safety of drug in 4 phases
■ Bioequivalence study: Study on generic compound → Plasma
concentration curve comparisons
● Don’t have to go through all phases → Only prove that it’s the
same as the originator (Same active ingredient + therapeutic
effect)
● Dosing equal, so everything else should also be the same
● Main parameters read from the curve:
○ tmax: at which time point the Cmax is reached
○ Cmax
● Therapeutic and adverse effects are already correlated to the
plasma concentration
● Therapeutic window: Concentration range where the therapeutic response is adequate
and adverse effects are tolerable
● ADME
○ Absorption: Amount of drug entering the systemic circulation
