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45 Cards in this Set
- Front
- Back
Passage of drug through cell layers into the general circulation
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Absorption
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Passage of drug from blood through capillary tubes into extracellular fluid, cells and tissue
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Distribution
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Passage of drugs into heptatic tissues
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Metabolism
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Passage of drug through nephron units in kidney for removal from the body
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Excretion
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determines kinetic properties of drug
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polarity
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Passage of drug driven by concentration gradient (high to low) Spontaneous and bidirectional. Not saturable and cannot by inhibited
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Aqueous (Passive) Diffusion
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Passage of drug that requires carrier protein. Can be saturated; Driven by conc. gradient (high to Low) Can be inihibited
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Facilitated Diffusion
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Passage of drug by specific carrier protein. Can be saturated. move drugs against conc. gradient; requires ATP
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Active Transport
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Substance is engulfed by the cell membrane and carried into the cell or out of the cell; energy dependent and saturable
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Endocytosis/ Exocytosis
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most absorption in the gut occurs in the
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proximal duodenum
(200 m2) |
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Prevents dissolution in the acidic gastric contents
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enteric coating
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product that contain the same active ingredients are identical in strength or concentration, dosage form and route of administration
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pharmaceutical equivalents
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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
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Bioquivalents
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Albumin
vs alpha1-acid glycoprotein |
acid drugs bind to it
basic drugs bind to it |
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increased amount of alpha 1 acidic glycoprotein
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Crohn's Disease
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Patterns of Distribution
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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 |
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Fetal plasma is ________ than the mother's
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more acidic
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foreign substance that enters the body
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xenobiotics
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Routes with no 1st pass effect
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sublingual or buccal route or parenterally
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Phase I
Phase II |
oxidative, reductive, hydrolytic
glucuronic, sulfonate, glycine conj. methylation |
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P450 responsible for metabolizing more than 50% of clinically prescribed drugs metabolized in the liver
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CYP3A4
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activity increased in smokers
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CYP1A2
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absent in 12-20% of Asians and 2-5% whites
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CYP2C19
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absent in 7% of whites
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CYP2d6
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Activity increased by alcohol
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CYP2E1
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inhibits CYP3A4
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grapefruit juice (narangenin)
ketoconazole diltiazem erythromycin |
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Induces CYP3A4
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carbamazepine and rifampicin
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normal glomerular filtration rate
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110-130 ml/min (180 L/day)
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responsible for resorption of water and secretion of weak electrolytes
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proximal tubule
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responsible for reabsorption of lipid soluble drugs
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distal tubule
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acidic urine
alkaline urine |
weak acids reabsorbed
weak bases reabsorbed |
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Enteric circulation
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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
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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
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First order kinetics
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rate is constant and fixed; rate of drug entering body is independent of dose or amount of drug present
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Zero order kinetics
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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
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mixed order kinetics
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absolute amount of drug eliminated is constant; half life is not constant
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zero order kinetics
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fraction of drug eliminated is constant; half life is constant
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first order kinetics
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relates amount of drug in body to the concentration of the drug in the blood or plasma
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volume of distribution
high if highly lipid soluble low if lipid insoluble |
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amount of drug in body/ C of drug in plasma
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Vd
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ratio of the rate of elimination of a drug by all routes to the concentration of the drug in a biological fluid
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Clearance
rate of elimination/ concentration of drug in plasma |
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0.693 (Vd)/CL
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Half life
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half lives required to reach steady state or eliminate drug that follows first order kinetics
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4-5 half lives
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variable half life indicates
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saturation of first order elimination mechanisms
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dose equal to the rate of elimination at steady state
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maintenance dose
Dosing rate= CL * desired plasma C |
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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
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loading dose
= VdX desired plasma C |