Pharmakinetics Flashcards
Pharmacokinetics
what the body does to a drug
Enteral
GI tract
Parenteral
injection
Absorption (Adme)
getting drug to systemic circulation: impacted by:
size of molecule, concentration across membranes, charge (unionized pass), solubility (hydrophobic cross membrane)
A: transporters
Influx transporter: move drug into cell: OCT, OAT
efflux transporter: drug out of cell: p-gpolp
A: bioavailability (F)
unaltered fraction of administered dose that reaches circulation: reduced by metabolism
A: stomach and small intestine
first pass effect: metabolism of drug prior to entering circulation gastric emptying GI blood flow stomach acid interactions with food or drugs
Distribution (aDme)
getting drug to tissues
drug binds to protein )albumin) to make complex, inactive
plasma protein binding is variable, unbound drug is therapeutic
D: influenced by
size of organ, blood flow, disease sate , solubility, pH
Metabolism (adMe)
biotransformation: drug is converted to metabolite in liver, may inactivate or activate drug
M: phase 1
smooth ER: CYP450 enzymes
adds functional group to prep for excretion or phase 2
M: Phase 2
conjugation reaction: react with functional group to make drug more water soluble for excretion
pharmacogenetics
slow metabolism: no benefit and toxicity
ultra rapid: no benefit no toxicity
Concentration (mass/volume)
C = Co(e^-kt)
Apparent volume (Vd)
Vd = drug adminitered / drug concentration