Pharmacokinetics Practical 2

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Questions and Answers

How long will it take for the theophylline intravenous infusion to reach 93.75% of its final steady-state concentration?

  • 7.4 h
  • 32 h
  • 24 h
  • 48 min (correct)

In the context of the pharmacokinetics discussed, what does the term 'half-life' represent?

  • The time required for the drug concentration to decrease by half (correct)
  • The time taken for the drug to reach steady state
  • The total time for drug elimination
  • The time taken for the drug concentration to double

What would be the elimination constant (Ke) of drug X given its half-life of 3 hours?

  • 0.231 (correct)
  • 0.173
  • 0.346
  • 0.693

What is the elimination type for drug X based on the information given?

<p>First order kinetics (C)</p> Signup and view all the answers

What is the initial plasma level (C0) if the plasma level at 6 hours is 5 mg/L?

<p>20 mg/L (B)</p> Signup and view all the answers

How is the half-life of drug X calculated based on the data provided?

<p>Using two concentration values over time (C)</p> Signup and view all the answers

What is the correct formula to calculate the maintenance dose for tobramycin?

<p>Maintenance dose = Clearance x Desired concentration (D)</p> Signup and view all the answers

What is the amount of drug eliminated after 5 hours as per the provided data?

<p>32.80 mg (D)</p> Signup and view all the answers

How much tobramycin should be administered every 6 hours to maintain a plasma concentration of 8 mg/L?

<p>460.8 mg (B)</p> Signup and view all the answers

What is the concentration of drug X at 2 hours after administration?

<p>4 mcg/mL (C)</p> Signup and view all the answers

What loading dose of tobramycin is required to achieve a therapeutic plasma concentration of 8 mg/L?

<p>320 mg (B)</p> Signup and view all the answers

What is the remaining amount of drug X in the body after 4 hours as per the provided data?

<p>328.05 mg (A)</p> Signup and view all the answers

Which of the following represents the steady-state plasma concentration equation for a continuously administered drug?

<p>Css = Dosage / Clearance (D)</p> Signup and view all the answers

Given a continuously administered infusion of lidocaine at 2.9 mg/min, what is the expected steady-state plasma concentration?

<p>20 mg/L (A)</p> Signup and view all the answers

If the clearance and volume of distribution for theophylline are 48 mL/min and 35 L respectively, what pharmacokinetic property does this relate to?

<p>Maintenance dose calculation (C)</p> Signup and view all the answers

What is the relationship between half-life and plasma concentration over time?

<p>Plasma concentration decreases by half every half-life duration. (D)</p> Signup and view all the answers

What is the amount of filtered drug that must be reabsorbed in the renal tubules if the renal clearance of inulin is 120 ml/min and the clearance of the drug is 18 ml/min, given that the drug is 40% protein bound?

<p>54 ml/min (A)</p> Signup and view all the answers

If a drug is eliminated by first-order kinetics and 100 mg is eliminated from a 200 mg dose in the first two hours, how much drug remains after 6 hours?

<p>25 mg (C)</p> Signup and view all the answers

What is the loading dose required to obtain an initial plasma level of 5 mg/L in a patient weighing 70 kg?

<p>210 mg (A)</p> Signup and view all the answers

A 500 mg dose of a drug has therapeutic efficacy for 6 hours. Given the drug's half-life is 8 hours, how long would a 1-gram dose remain effective?

<p>14 hours (B)</p> Signup and view all the answers

What is the steady-state level in plasma equivalent to if the pharmacokinetic characteristics of propranolol include Vd = 300 L/70 kg and the target plasma level is 20 μg/L?

<p>300 mg (B)</p> Signup and view all the answers

How much drug is eliminated after one half-life if the total dose is 200 mg?

<p>100 mg (D)</p> Signup and view all the answers

If a drug has a clearance of 18 ml/min and is 40% protein bound, what is the free fraction of the drug available for clearance?

<p>60% (B)</p> Signup and view all the answers

What is the calculated plasma level of a drug 6 hours after an intravenous bolus dose if the plasma level at 6 hours is noted to be 5 mg/L?

<p>5 mg/L (A)</p> Signup and view all the answers

Flashcards

Renal Clearance

The volume of drug that is removed from the body per unit time. It is a measure of how quickly the body eliminates a drug.

Free Fraction (ff)

The fraction of a drug that is not bound to plasma proteins. This free fraction is the only part of the drug that can be filtered by the kidneys and eliminated from the body.

Tubular Reabsorption

The process where a drug is removed from the plasma and transported back into the bloodstream. It occurs in the renal tubules, reducing the amount of drug eliminated in urine.

Elimination Half-Life

A drug's elimination half-life is the time it takes for the concentration of the drug in the body to decrease by half. It helps determine how long a drug remains effective.

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Loading Dose

The amount of drug needed to achieve a specific therapeutic effect immediately. It is used when a rapid effect is needed and is often calculated based on the volume of distribution.

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Volume of Distribution (Vd)

The total volume of fluid in which a drug is distributed after administration. It reflects how widely the drug is distributed throughout the body.

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Oral Bioavailability (f)

A measure of a drug's ability to be absorbed from the gastrointestinal tract and reach the bloodstream. It is expressed as a percentage.

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Steady-State Level

The state where the rate of drug elimination is equal to the rate of drug administration. It occurs after repeated dosing and results in a consistent plasma concentration.

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Maintenance Dose

The amount of drug required to maintain a steady-state plasma concentration, calculated using the drug's clearance, desired concentration, and bioavailability.

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Steady-State Plasma Concentration (Css) Continuous Infusion Equation

The steady-state plasma concentration (Css) of a drug during continuous intravenous infusion is calculated by dividing the dosage rate by the drug's clearance.

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Drug Clearance

The rate at which a drug is eliminated from the body, measured in units of volume per time.

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Bioavailability

The proportion of an administered drug that reaches the systemic circulation.

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Initial Plasma Concentration (Co)

The concentration of a drug in the plasma at time zero, meaning immediately after administration.

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Half-life

The time it takes for the concentration of a drug in the body to decrease by half.

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Drug Elimination

The process by which a drug is removed from the body.

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Elimination Rate Constant (Ke)

The rate at which a drug is eliminated from the body.

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First Order Kinetics

The pattern of drug elimination where a constant fraction of the drug is removed per unit of time.

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Initial Redistribution Phase

A rapid decrease in drug concentration shortly after administration.

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Steady State Concentration

The concentration of a drug in the body after repeated doses, where the rate of drug elimination equals the rate of drug administration.

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Time to Reach Steady State

The time it takes for a drug to reach a certain percentage of its steady-state concentration.

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Study Notes

Practical 2 - Pharmacokinetic Problems

  • Renal Clearance: A subject with a renal clearance of inulin at 120 ml/min is given a drug. The drug's clearance is measured at 18 ml/min. If the drug is 40% plasma protein bound, the amount of filtered drug reabsorbed in the renal tubules is 54 ml/min.

First-Order Elimination Kinetics

  • Drug Dose and Elimination: A patient receives a 200 mg IV dose of a drug. 100 mg is eliminated in the first two hours. Assuming first-order elimination kinetics, 25 mg of the drug will remain after 6 hours.
  • Half-Life: The elimination half-life is two hours. Each half-life reduces the amount in the body by 50%. At 6 hours, three half-lives have passed (200 mg to 100 mg, then 100 mg to 50 mg, and finally 50 mg to 25 mg).

Volume of Distribution and Loading Dose

  • Total Body Water: If a drug distributes into total body water, and a patient weighs 70 kg (and 60% of body weight is water), the volume of distribution is 42 liters. A loading dose of 210 mg is needed to achieve an initial plasma level of 5 mg/L.
  • Loading Dose Formula: Loading dose (LD) = Volume of Distribution (Vd) x plasma concentration (CP).

Therapeutic Efficacy and Half-Life

  • Drug Efficacy Duration: A 500 mg dose of a drug has therapeutic efficacy for 6 hours. The drug's half-life is 8 hours. A 1 gram dose will be effective for 14 hours (8 hours + 6 hours). Duration of effectiveness is not directly related to half-life. it's about drug concentration remaining above the minimum effective concentration in the body.

Propranolol Pharmacokinetics

  • Pharmacokinetic Parameters: Propranolol has a volume of distribution (Vd) of 300 L/70 kg, a clearance (Cl) of 700 ml/min, and an oral bioavailability (f) of 0.25.
  • Loading Dose Calculation: A loading dose of 24 mg is needed to achieve a steady-state plasma level of 20 µg/L. (Using the formula: LD = Vd x CP / f)

Bolus Dose and Half-Life

  • Initial Plasma Level: A drug is administered as a bolus dose IV. At 6 hours post-injection, the plasma level is 5 mg/L. The volume of distribution (Vd) is 10 L, and the elimination half-life is 3 hours. The dose administered was 200 mg..

Tobramycin Maintenance Dose

  • Pharmacokinetic Data: The patient's tobramycin clearance is 0.16 L/min and the volume of distribution (Vd) is 40 L.
  • Calculating the Maintenance Dose: A maintenance dose of 460.8 mg is delivered intravenously every six hours to achieve a steady-state plasma concentration of 8 mg/L. (using formula: Maintenance dose = Clearance X Desired concentration / Bioavailability)

Aminoglycoside Pharmacokinetics

  • Half-Life: A single intravenous bolus of an aminoglycoside administered to a 70 kg man. The elimination half-life of the drug can be calculated from the graph/data displayed.
  • Elimination Constant: The elimination constant (Ke) of drug X is 0.231.

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