pharmacokinetics Flashcards
renal excretion terminates actions of what drugs?
small hydrophilic
fully/nearly fully ionized at physiological ph
not protein bound
most pharmacologically active drugs are..
lipophilic
unionized / partially ionized
bound to plasma proteins
what is the primary determinant of duration and intensity of drug action?
rate of drug metabolism
drug metabolism mainly occurs where?
liver in er
what other organs can also metabolize substances?
gi mucosa = lower bowel kidneys lungs nasal mucosa skin
first pass effect
drugs are extensively metabolized during initial pass though the liver
what enzymes are involved in phase I ?
CYP450
oxidases
what is the most common phase ii rxn?
glucuronidation
conjugation using what?
glucorunic acid
sulphate
glutathione
what are examples of phase ii rxns?
glucuronidation
methylation
sulfation
n-acetylation
codeine, a prodrug, is demethylated to produce
morphine
inducers of metabolism
increase synthesis of p450 and reduce degradation
inhibitors of metabolism
bind to cytochrome oxidase and inhibit metabolism of other drugs
CYP2D6 affects
beta blockers –> alter effect
CYP2C9
warfarin –> change dose
CYP2C19
omeprazole –> variable response in peptic ulcers
what are the most imp routes of drug elimination?
urine and feces
what drugs follow zero order kinetics?
ethanol and aspirin
ethanol is excreted in …
sweat
what’s penicillin?
an acidic antibiotic
how are penicillin and aspirin excreted?
via proximal tubular secretion (renal excretion)
what is used in the excretion of penicillin and aspirin?
anion transport system
what may prolong effects of penicillin?
competition for secretion with probenecid