Pharmacotherapeutics: treatment effect of the drug
Pharmacodynamics: action of the drug on the body
- Receptor interactions
- Dose-response phenomena
- Mechanisms of therapeutic and toxic reactions
Pharmacokinetics: what the body does to the drug
- Absorption
o Oral: convenient, takes longer to reach bloodstream, may be destroyed by
stomach acid, must be broken down in stomach acid to work, need enough liquid
o Parenteral: IV, fast, inconvenient
o Sublingual: faster than oral, more readily absorbed, avoid 1st pass metabolism o
Rectal: faster than oral, absorb directly through mucus membranes and into
bloodstream
o IV is the fastest route of absorption; inhalation is fast, but can be unreliable
- Distribution o Drugs CANNOT create action if they are not distributed in adequate
concentrations o Passive Diffusion: creates equal amounts of un-ionized drug on both
sides of the membrane, works best for small, unbound, uncharged drugs
o Plasma Protein Binding: drugs may compete for protein binding sites
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o Ex: Coumadin and Bactrim – they compete for the same binding sites, one
monopolizes the binding sites leading to less transport of the other drug
o Hypoalbuminemia: more free (unbound drug) in the bloodstream, risk for toxic
effect because drug is just hanging in the bloodstream and not doing anything
productive, less drug available to work in the target tissues
- Metabolism (Biotransformation) o First Pass Effect: takes place in the liver after oral
administration, the liver metabolizes a certain amount of the drug before it gets to its
target site, higher dosing may be needed
o Drugs with high 1st pass effect will not be given orally o CYP 450: an oxidative
reaction that can vary with genetics o CYP34A: responsible for metabolism of
many drugs
drugs may compete for this enzyme, meaning one will not be metabolized,
so they will need to be given at different times
there are inducers and inhibitors (ex: grapefruit juice inhibits CYP34A)
Inducer: drug is metabolized too fast, make enzymes work better
Inhibitor: drug can’t be metabolized by enzymes properly o Half Life: the
time it takes for a drug’s concentration to be reduced by half, important
when determining how often to give a medication
Ex: Zithromax – long half life (once a day); penicillin VK – short half life
(q6h) o Prodrug: inactive until metabolized
- Excretion
o Process in which drugs are transferred from inside the body to outside the body
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