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45 Cards in this Set

  • Front
  • Back
Passage of drug through cell layers into the general circulation
Absorption
Passage of drug from blood through capillary tubes into extracellular fluid, cells and tissue
Distribution
Passage of drugs into heptatic tissues
Metabolism
Passage of drug through nephron units in kidney for removal from the body
Excretion
determines kinetic properties of drug
polarity
Passage of drug driven by concentration gradient (high to low) Spontaneous and bidirectional. Not saturable and cannot by inhibited
Aqueous (Passive) Diffusion
Passage of drug that requires carrier protein. Can be saturated; Driven by conc. gradient (high to Low) Can be inihibited
Facilitated Diffusion
Passage of drug by specific carrier protein. Can be saturated. move drugs against conc. gradient; requires ATP
Active Transport
Substance is engulfed by the cell membrane and carried into the cell or out of the cell; energy dependent and saturable
Endocytosis/ Exocytosis
most absorption in the gut occurs in the
proximal duodenum
(200 m2)
Prevents dissolution in the acidic gastric contents
enteric coating
product that contain the same active ingredients are identical in strength or concentration, dosage form and route of administration
pharmaceutical equivalents
products that are pharmaceutical equivalents when the rate and extent of bioavailability of the active ingredient in the two products are not significantly different under suitable test conditions
Bioquivalents
Albumin
vs
alpha1-acid glycoprotein
acid drugs bind to it

basic drugs bind to it
increased amount of alpha 1 acidic glycoprotein
Crohn's Disease
Patterns of Distribution
1. drugs largely within the vascular system
2. Drug uniformly distributeed throughout the body water
3. Drug concentration in one or more tissues
4. combination of 1, 2, 3
Fetal plasma is ________ than the mother's
more acidic
foreign substance that enters the body
xenobiotics
Routes with no 1st pass effect
sublingual or buccal route or parenterally
Phase I

Phase II
oxidative, reductive, hydrolytic

glucuronic, sulfonate, glycine conj. methylation
P450 responsible for metabolizing more than 50% of clinically prescribed drugs metabolized in the liver
CYP3A4
activity increased in smokers
CYP1A2
absent in 12-20% of Asians and 2-5% whites
CYP2C19
absent in 7% of whites
CYP2d6
Activity increased by alcohol
CYP2E1
inhibits CYP3A4
grapefruit juice (narangenin)
ketoconazole
diltiazem
erythromycin
Induces CYP3A4
carbamazepine and rifampicin
normal glomerular filtration rate
110-130 ml/min (180 L/day)
responsible for resorption of water and secretion of weak electrolytes
proximal tubule
responsible for reabsorption of lipid soluble drugs
distal tubule
acidic urine

alkaline urine
weak acids reabsorbed

weak bases reabsorbed
Enteric circulation
high molecular weight conjugates are subject to enzymatic cleavage of the conjugate bond by intestinal flora... returns to parent drug form and effect is prolonged
rate is proportionate to amount of drugs present in the body; a constance fraction of drug int he body is eliminated per unit of time
First order kinetics
rate is constant and fixed; rate of drug entering body is independent of dose or amount of drug present
Zero order kinetics
Rate is proportionate to the amount present at low therapeutic concentrations, then shifts to constant rate independent of dose at higher therapeutic concentrations as degradative enzymes are saturated
mixed order kinetics
absolute amount of drug eliminated is constant; half life is not constant
zero order kinetics
fraction of drug eliminated is constant; half life is constant
first order kinetics
relates amount of drug in body to the concentration of the drug in the blood or plasma
volume of distribution

high if highly lipid soluble
low if lipid insoluble
amount of drug in body/ C of drug in plasma
Vd
ratio of the rate of elimination of a drug by all routes to the concentration of the drug in a biological fluid
Clearance

rate of elimination/ concentration of drug in plasma
0.693 (Vd)/CL
Half life
half lives required to reach steady state or eliminate drug that follows first order kinetics
4-5 half lives
variable half life indicates
saturation of first order elimination mechanisms
dose equal to the rate of elimination at steady state
maintenance dose

Dosing rate= CL * desired plasma C
dose of drug sufficient to produce a plasma concentration of drug that would fall within the therapeutic window after only one or very few doeses over a very short interval
loading dose

= VdX desired plasma C