A drug is dosed orally with F = 0.5; to achieve a target Css,inf with Vd = 40 L and Cl = 5 L/h, calculate the required continuous oral dose rate. If Css,inf is 4 mg/L, what is the rate?

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Multiple Choice

A drug is dosed orally with F = 0.5; to achieve a target Css,inf with Vd = 40 L and Cl = 5 L/h, calculate the required continuous oral dose rate. If Css,inf is 4 mg/L, what is the rate?

Explanation:
At steady state, the amount entering the system equals the amount being eliminated. For an oral dose with bioavailability F, the input rate is F times the dose rate, while the elimination rate is Cl times the steady-state concentration (Css,inf). Setting these equal gives F × Dose_rate = Cl × Css,inf, so Dose_rate = (Css,inf × Cl) / F. Plugging in the numbers: Css,inf = 4 mg/L, Cl = 5 L/h, F = 0.5. Dose_rate = (4 × 5) / 0.5 = 40 mg/h. The distribution volume (Vd) doesn’t affect the steady-state input rate; it influences how long it takes to reach Css,inf, not the rate needed to maintain it.

At steady state, the amount entering the system equals the amount being eliminated. For an oral dose with bioavailability F, the input rate is F times the dose rate, while the elimination rate is Cl times the steady-state concentration (Css,inf). Setting these equal gives F × Dose_rate = Cl × Css,inf, so Dose_rate = (Css,inf × Cl) / F.

Plugging in the numbers: Css,inf = 4 mg/L, Cl = 5 L/h, F = 0.5. Dose_rate = (4 × 5) / 0.5 = 40 mg/h.

The distribution volume (Vd) doesn’t affect the steady-state input rate; it influences how long it takes to reach Css,inf, not the rate needed to maintain it.

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