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21 Cards in this Set
- Front
- Back
Pharmacokinetics
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The study of the time course of drug absorption, distribution, metabolism and excretion
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Systemic Absorption
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process by which unchanged drug proceeds from the site of administration to the site of measurement
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First-Pass Loss
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loss of orally administered drug during its first passage through the gastrointestinal tract and liver
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Bioavailability
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describes the rate and extent of drug input into the systemic circulation
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Disposition
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all the kinetic processes that occur to a drug subsequent to its systemic absorption—distribution and elimination
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Elimination
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irreversible loss of drug from the site of measurement; occurs by excretion and metabolism
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Excretion
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irreversible loss of chemically unchanged compound
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Metabolism
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conversion of one chemical species to another
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What is Clinical Pharmacokinetics
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The application of pharmacokinetic principles to the safe and effective therapeutic management of drugs in an individual patient
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why do we need pharmacokinetics
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Optimize dosing regimens
Population pharmacokinetics Medication therapy management |
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Sites of measurement of systemic exposure of drugs (7)
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1. Plasma
2. serum 3. whole blood 4. breath 5. milk 6. saliva 7. urine |
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Unbound Drug Concentration
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Only unbound drug passes through cell membranes to reach sites of storage, metabolism, or activity
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Fraction unbound
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ratio of unbound drug to total drug (usually does not change)
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Systemic exposure of drugs-time profile
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Tmax happens at Cmax (peak of curve)
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Period of Observation
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Observations should be made within the time frame of interest
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Two principal organs of elimination
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Liver
Kidneys |
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***Pharmacokinetic Models***
What are the 7 potential uses? |
1. Predict drug levels
2. Determine optimum dosage regimen for each patient 3. Estimate possible accumulation of drugs and/or metabolites 4. Correlate drug concentrations with pharmacologic or toxicologic activity 5. Evaluate differences in the rate or extent of availability between formulations 6. Describe how changes in physiology or disease affect the absorption, distribution, or elimination of the drug 7. Explain drug interactions |
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Compartment Models
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Mammillary Model
Catenary Model |
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Physiologic Model
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Flow Model
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Zero-Order Reactions
what does it look like? |
Amount or concentration of drug decreases at a constant rate. da/dt = -ko
linear line going top left to bottom right. conc. vs. time |
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First-Order Reactions
what does it look like? |
Amount or concentration of drug decreases at a rate that is proportional to the amount of drug remaining
da/dt = -KA looks like a downward curved line (top left to bottom right conc. vs. time) |