Pharmacokinetics & Dosing Regimens

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Bachelors Degree 2001 Pharmacology Flashcards on Pharmacokinetics & Dosing Regimens, created by Vicky Reese on 19/03/2015.
Vicky Reese
Flashcards by Vicky Reese, updated more than 1 year ago
Vicky Reese
Created by Vicky Reese over 9 years ago
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Question Answer
Rational Use of Drugs Assumes that a particular concentration of a drug will have the desired therapeutic effect and that adverse effects will be negligible
Therapeutic Range The range of drug concentrations having a high probability of producing the desired therapeutic effect and a low probability of producing adverse effects
Steady-State Plasma Drug Concentration Maintains the desired pharmacological response
Dosing Regimen • The size of the dose • The dosing frequency
Pharmacokinetics • Plays a major role in: - Establishing the initial dosing regimen - Adjusting the regimen to deal with a lack of response or to reduce symptoms of toxicity
Plasma Concentration-Time Profile of A Drug • This measure graphically demonstrates the relationship between the plasma drug concentration and therapeutic response or toxicity over time
BIOAVAILABILITY • The proportion of the administered dose that reaches the systemic circulation intact • Usually expressed as a % F = fg x fH
AUC (area under the plasma concentration versus time curve) Total area under the curve that describes the concentration of the drug in the systemic circulation as a function of time post dose (normally 0 - infinity)
Clearance (CL) • The ability of either an individual organ or the body to eliminate a drug
Steady state The rate of drug administration equals the rate of drug elimination & the plasma drug concentration remains constant At steady state: Elimination rate = maintenance dose rate (DR)
Volume of Distribution (V) The volume in which the amount of drug in the body would need to be uniformly distributed to produce the observed concentration in the blood V = total amount of drug in body (A)/drug concentration (C)
Clinical use of Volume of Distribution 1.) Provides an indication of accumulation of drugs in extravascular (tissue) compartments (e.g. fat, muscle) 2.) A major determinant of half-life of a drug 3.) On occasion, it is necessary to achieve a high plasma concentration quickly to produce the desired therapeutic response
Loading Dose • Administered to 'fill up' the volume of distribution • May be given to produce rapid pharmacological effect Loading dose = volume of distribution (V) x target plasma concentration (C)
Half-life (t1/2) • Time taken for the blood or plasma drug concentration to fall by one-half (50%) t1/2 = 0.693 x V/ CL
Half-life is a major determinant of the ff. • duration of action of a drug after a single dose • time taken to reach steady state with chronic dosing • dosing frequency required to avoid massive fluctuations in plasma drug concentration during the dosing interval
First order kinetics Assumes a constant proportion of the drug is eliminated per unit time (as dose and blood concentration of drug increases, the rate of elimination increase)
SATURABLE METABOLISM the situation in which the enzyme metabolizing drug reaches maximum capacity and rate of metabolism CAN'T increase further as dose increases
Zero-order Kinetics • rate of elimination does NOT increase in proportion to dose and concentration • metabolism is saturate & CL & t1/2 are not constant (CL continually decreases & t1/2 continually increase as the dose & blood concentration increase)
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