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31 Cards in this Set

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