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Instructions and solutions for homework 1 of a pharmacokinetics course. It includes calculations for the area under the curve (auc0∞) of a drug based on its concentration-time profile, identification of the elimination order, and discussion on the distribution of drugs into different organs and tissues.
Typology: Assignments
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Homework # (Total: 10 points) #1) Calculate AUC (^0) Æ ∞ from the given concentration-time profile. (3 points)
Time (h) Plasma concentration (mg/L) 1 94. 4 80. 6 70. 8 59. 12 40.
We first need to determine whether the drug is eliminated in a first or a zero-order elimination process. An easy way to approach this question is to graph the data.
y = -4.9831x + 99. R^2 = 0.
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0 2 4 6 8 10 12 14 Time (h)
Plasma concentration (mg/L)
Plasma concentration and time show a linear relationship on a normal scale. Therefore, drug is eliminated in a zero-order process. (First-order process would show a linear relationship on a semi-log scale!) Æ Equal amounts of drug are eliminated per hour. In order to determine AUC (^0) Æ∞ we need to calculate t(0 hours) and the time when the plasma concentration reaches zero. Looking at the data set, we see that the plasma concentration decreases by approximately 5mg/L per hour. Thus, the plasma concentration will be about 100mg/L at time zero and approach zero after about 20 hours. Now let’s calculate the areas of the individual trapezoids according to:
C (^) 2 + C (^1) • t − t
Time (h) Plasma concentration (mg/L) AUCs (mg*h)/L 0 100 1 94.8 97. 4 80.1 262. 6 70.3 150. 8 59.9 130. 12 40.1 200 20 0 160. SUM 1000.
Homework # (Total: 10 points) The AUC (^0) Æ∞ can be determined by summing up the individual areas which results in a value of about 1000mgh/L. (Alternatively, you could calculate the area of the triangle formed by the data: 100mg/L20h/2 = 1000mg*h/L)
#2) Fractions and amounts of drugs eliminated through zero- and first-order kinetics (2 points)
#2a) How do fraction and amount of a drug eliminated through first-order kinetics change? Please, mark the right answer. (1 point)
#2b). How do fraction and amount of a drug eliminated through zero-order kinetics change? Please, mark the right answer. (1 point)
#3) Please derive the half-life equation for a first-order elimination process. (3 points)
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