PBL workshop (1st) Flashcards
what defines the relationship between the administration of a drug, the time-course of its distribution, and the concentration attained in different regions of the body (effects of body on drug)
pharmacokinetics
what is the quantitative description of the biochemical and physiological effects of drugs and the mechanisms underlying these effects (effects of drug on body)
pharmacodynamics
what is the threshold PC (enough drug enters tissues to interact with receptors and produce effect)
minimal effect concentration (MEC)
what is the driving force for lipid diffusion
concentration gradient
what is the driving force for aqueous diffusion
concentration gradient
what is the rate of diffusion equation
(available surface area X concentration gradient) / (resistance of membrane X thickness of membrane)
what environment do acids readily denote proteins and become deprotonated
aqueous solutions
what happens to a base when put in an aqueous solution
becomes ionized when protonated (accepts protons)
are weak acids excreted faster in alkaline or acidic environment
alkaline
are weak bases excrete faster in acidic or alkaline environment
acidic
what does sodium bicarbonate increase the excretion of
weak acids
what does ammonium chloride increase in the excretion of
weak bases
what is the bioavailability for drugs applied IV route
100%
what is the bioavailability for drugs applied subcutaneously
75-100%
what is the bioavailability for drugs applied orally
5-100%
what is the bioavailability for drugs applied rectally
30-100%
what is the bioavailability for drugs applied through inhalation
5-100%
what is the bioavailability for drugs applied transdermally
80-100%
what must be true for bioequivalence
same active ingredients, identical strength/concentration, dosage form and route of administration must be the same
what drugs may cross the BBB
low MW (200-300 Da) and lipid soluble drugs
what is the most important plasma protein
albumin
what drugs (in general) bind primarily to albumin
acidic drugs and some neutral compounds
what drugs bind more primarily to alpha-acid glycoprotein (AAG)
more basic drugs (lidocaine, quinidine, propranolol)
common places of drug loss (areas where drug is not used or has no effect)
fat, GI tract, others
what is the equation for volume of distribution
dose/plasma drug concentration
what are some factors that influence volume of distribution
plasma protein binding, lipid solubility, organ/tissue specific accumulation
what type of reactions occur with phase 1 reactions
oxidation/reduction reactions
what type of reactions occur with phase 2 reactions
conjugation/hydrolysis reactions
what is the principle organ of drug metabolism
liver
what is the location of cytochrome P-450 enzymes
smooth ER of hepatocytes and intestinal epithelia
what is the number one role of P450 system
metabolism and detoxification of substances
what are some inducing agents for the 3A4 cyp-450 isozyme
carbamazepine and phenobarbitol
what are some substrates that correlate with the inducing agents of 3A4 isozyme
alprazolam and erythromycin
what are some inhibiting agents of the 3A4 isozyme of CYP-450
cimetidine and grapefruit juice
what are some substrates that go along with the inhibiting agents of 3A4 isozyme
midazolam and atorvastatin
what happens to bioavailability when an inhibiting substrate is used
increased bioavailability
what is rate of elimination dependent on
rate of biotransformation and rate of excretion by one or more routes
what happen to rate of elimination if drug concentration is high
rate of elimination is rapid
what happens to rate of elimination if drug concentration is low
rate of elimination is slow
what is the equation to determine half-life (1st order)
(0.7 X Vd) / CL
what are some zero-order kinetic drugs
ETOH, aspirin and phenytoin
where in the kidney does filtration of drugs occur
glomerulus
where in the kidney does tubular secretion of drugs occur
proximal tubule
where in the kidney does reabsorption of drugs occur
into renal capillaries
what is the equation for Css
infusion rate / clearance
when is 94% of the steady state of Css reached
4 half lives
what is the equation for loading dose
(Vd X Ct) / F