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31 Cards in this Set
- Front
- Back
What is the measure of the bodies ability to eliminate the drug?
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clearance
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What is volume of distribution?
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the measure of the apparent space in the body available to contain the drug
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What is the equation for volume of distribution?
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Vd= amount of drug in the body/C
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What is the equation for clearance?
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clearance=rate of elimination/C
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What are the two major sites of drug elimination?
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kidneys and liver
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When a drug's clearance is first-order, how can it be estimated?
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by calculating the area under the curve of the time-concentration profile after a dose
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What type of elimination is dependent on the concentration of the drug that is achieved?
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capacity-limited elimination
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What is the rate of elimination equation for capacity-limited elimination?
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(Vmax x C)/ (Km + C)
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What three drugs is the capacity-limited elimination pattern important?
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ethanol, phenytoin, and aspirin
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What type of elimination is dependent on the rate of delivery to the organ of elimination?
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flow-dependent elimination
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What is a drugs half-life?
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the time required to change the amount of drug in the body by one-half during elimination
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What is the equation for half-life?
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t1/2 = (.7 x Vd)/CL
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What is the "rule of thumb" of half-life effects?
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four half-lives must elapse after starting a drug-dosing regimen before full effects will be seen
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If the dosing interval is shorter than ___ half-lives, the accumulation is detectable.
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4
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What is the equation for accumulation factor?
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1/fraction lost in one dosing interval
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What is the fraction of unchanged drug reaching the systemic circulation following administration by any route?
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bioavailability
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When does bioavailablility equal unity?
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intravenous dose of the drug
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What is the function of P-glycoprotein?
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reverse transporter of drugs in the gut
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What is the first-pass extraction ratio in the liver?
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ER = CL/Q
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What is the equation for systemic bioavailability of the drug?
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F = f x (1-ER) f is the extent of absorption and ER si the extraction ratio
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What determines the rate of absorption?
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the site of administration and the drug formulation
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When is the mechanism of drug absorption zero-order?
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when the rate is independent of the amount of drug remaining in the gut
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What is the equation for maintenance dose?
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maintenance dose = dosing rate x dosing interval
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What is the equation for the loading dose to match the peak steady-state concentration?
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loading dose = maintenance dose x accumulation factor
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What 2 factors determine the amount of drug that enters the body?
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patient's compliance and rate/extent of transfer from the site of administration to the blood
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What is drug sensitivity?
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the concentration required to produce 50% of the maximum affect
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What are the three factors that influence clearance?
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dose, organ blood flow, and intrinsic function of the liver or kidneys
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What drugs are exculsively bound to albumin?
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phenytoin, salicyclates, and disopyramide
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What drugs are exculsively bound to alpha1-acid glycoprotein?
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quinidine, lidocaine, and propranolol
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What increases alpha1-acid glycoprotein levels?
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acute inflammatory disorders
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What determines unbound drug concentrations?
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dosing rate and clearance
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