Pharmacology Lecture 6: Serum Concentration-Time Curves

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Questions and Answers

What is the main difference in the absorption rate of the two formulations discussed?

Formulation A has a slower rate of release.

Both formulations have the same rate of release.

Formulation A has a faster rate of release, but only for a short time.

Formulation B has a slower rate of release. (correct)

What is the primary factor in determining the peak concentration and time to reach the MEC?

Duration of action.

Formulation of the drug.

Rate of absorption. (correct)

Dose of the drug.

What is the minimum effective concentration (MEC) in the context of pharmacokinetics?

The lowest concentration at which the drug is effective. (correct)

The highest concentration at which the drug is effective.

The concentration at which the drug is first absorbed.

The concentration at which the drug is fully absorbed.

What does the area under the serum concentration-time curve (AUC) represent?

The total amount of drug absorbed into the circulation. Signup and view all the answers

What is the main difference in the duration of action between formulations A and B?

Formulation B has a longer duration of action. Signup and view all the answers

What is the primary factor in determining the bioavailability of a drug?

Rate of absorption. Signup and view all the answers

What parameter represents the maximum concentration of the drug in the blood?

Cmax Signup and view all the answers

What is the relationship between the peak concentration and the rate of absorption?

A faster rate of absorption results in a higher peak concentration. Signup and view all the answers

What does a difference in AUC values between formulations indicate?

A difference in the extent of absorption. Signup and view all the answers

What is the primary difference between formulations A and B?

Formulation B has a slower rate of release. Signup and view all the answers

What is the AUC for formulation A?

34.4 µg/mL X hours. Signup and view all the answers

What represents the total amount of the drug absorbed by the body?

AUC Signup and view all the answers

What is the time it takes to reach the peak concentration of the drug in the blood?

Tmax Signup and view all the answers

What does the Time of Peak (Tmax) reflect?

The rate of absorption of the drug from the formulation Signup and view all the answers

What is the process of comparing the amount of the drug absorbed by the body from different formulations?

Bioavailability Signup and view all the answers

What is the graph that shows the concentration of the drug in the blood over time?

Concentration-time curve Signup and view all the answers

What is the primary goal of individual dosing of a patient?

To achieve the MEC but not the MTC Signup and view all the answers

What is the minimum concentration of the drug required to produce a therapeutic effect?

Minimum Effective Concentration Signup and view all the answers

What is the effect of increasing the dose size on the blood drug concentration-time curve?

The Cmax is proportionately higher and the AUC is proportionately greater Signup and view all the answers

What is the difference between the two formulations A and B in terms of achieving the desired pharmacologic effect?

Formulation A achieves the MEC but formulation B does not Signup and view all the answers

What is the relationship between the dose size and the Area Under the Curve (AUC)?

The AUC is directly proportional to the dose size Signup and view all the answers

What is the effect of increasing the dose size on the Tmax?

The Tmax is unchanged Signup and view all the answers

What is the role of bioavailability in achieving the desired pharmacologic effect?

It affects the rate of absorption of the drug from the formulation Signup and view all the answers

What is the minimum concentration of the drug required to produce the desired pharmacologic effect?

Minimum Effective Concentration (MEC) Signup and view all the answers

Study Notes

Serum Concentration-Time Curve

Shows peak height concentrations, peak height times, times to reach Minimum Effective Concentration (MEC), and areas under the curves for equal amounts of drug from two different formulations following oral administration.

Formulations A and B

Formulation A achieves the required blood levels of drug to produce the desired pharmacologic effect, whereas formulation B does not.
If the MEC for the drug is 2.0 µg/mL and the Minimum Toxic Concentration (MTC) is 4.0 µg/mL, equal doses of the two formulations result in toxic effects produced by formulation A but only desired effects by formulation B.

Individual Dosing

The objective is to achieve the MEC but not the MTC.

Effect of Dose Size on Blood Drug Concentration-Time Curves

As the dose increases, the Cmax (peak height concentration) is proportionately higher and the AUC (area under the curve) proportionately greater.
Tmax (time to reach Cmax) is the same for each dose.

Rate of Absorption

Reflects the rate of absorption from a formulation, which determines the time needed to reach the MEC and thus initiate the desired effect.
Influences the period over which the drug enters the bloodstream and affects the duration of the drug's presence in the blood.

Time of Peak

Formulation A allows the drug to reach the MEC within 30 minutes following administration and a peak concentration in 1 hour.
Formulation B has a slower rate of release, reaching the MEC 2 hours after administration and its peak concentration 4 hours after administration.

Comparative Evaluation of Bioavailability

Important parameters to consider:
- Peak height concentration (Cmax)
- Time of the peak concentration (Tmax)
- Area under the blood concentration-time curve (AUC)

Peak Height

Concentration-time curves showing different peak height concentrations for equal amounts of drug from two different formulations following oral administration.

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Description

Compare the serum concentration-time curves of two drug formulations, Formulation A and Formulation B, to determine their effectiveness in achieving desired blood levels and pharmacologic effects.