III - Pharmacokinetics Flashcards
Concentration of a drug at the receptor site
Effective Drug Concentrationh
The concentration at the receptor site is usually proportional to the drug’s concentration in the plasma or whole blood at equilibrium except for
topical drugs
Volume at which the drug would need to be uniformly distributed to produce an observed blood concentration
Apparent Volume of Distribution
Apparent Volume of Distribution =
Vd = amount of drug in the body/plasma drug concentration
Apparent Volume of Distribution can be altered by
liver or kidney disease
Distribution: Low Vd
blood
Distribution: Medium Vd
extracellular space, body water
Distribution: High Vd
tissues
Relates the rate of elimination of the plasma concentration
Clearance
Clearance =
Cl = rate of elimination/plasma drug concentration
Clearance depends on
drug, condition of organs of elimination
Clearance is a constant proportion
First-Order Kinetics
Clearance is a constant amount
Zero-Order Kinetics
Most important pharmacokinetic parameter to be considered in defining a rational steady state during dosage regimen
Clearance
Condition in which the average total amount of drug in the body does not change over multiple dosing intervals
Steady State
Rate of drug input equals the rate of elimination
Steady State
Steady State is reached after _____ half-lives of the drug.
4-5
Constant for drugs following first order kinetics
Half-Life
Half-Life =
t1/2 = (0.693 x volume of distrubution)/clearance
Fraction of the administered dose that reaches the systemic circulation
Bioavailability
Drugs administered via _____ have 100% bioavailability.
IV
Bioavailability is reduced by
incomplete absorption, first-pass metabolism, pre-systemic redistribution
Bioavailability is determined by
computing the area under the plasma concentration curve (AUC)
Plan for a drug administration over a time period
Dosage Regimen
Dosage Regimen results in the achievement of _____ levels of the drug without exceeding _____.
therapeutic levels, minimum toxic concentration
Equal to the rate of elimination at steady state
Maintenance Dose
Maintenance Dose =
(clearance x desired plasma concentration)/bioavailability
Important to maintain concentration above minimum therapeutic level
Maintenance Dose
Not involved in calculating maintenance dose
Volume of Distribtion
If the therapeutic concentration must be achieved rapidly and the volume of distribution is large
Loading Dose
Not involved in calculating loading dose
Clearance
Safe range between the minimum therapeutic concentration and the minimum toxic concentration of a drug
Therapeutic Window
Adjustment of Dosage in Renal Impairment
Average Dose x Crea Clearance / 100mL/min
Used to calculate the patient’s creatinine clearance
Cockroft-Gault Equation
Cockroft-Gault Equation
[(140-age) x weight (kg)] / [72xcrea mg/dl] (x 0.85 in females)