Question:medium

Which of the following causes of non-linearity is associated with phenytoin?

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Some drugs do not show simple, proportional behaviour as the dose increases — this is called non-linear (or dose-dependent) pharmacokinetics.
Updated On: Jun 24, 2026
  • Enzyme induction
  • Saturation of metabolic enzymes
  • Saturation of plasma protein binding
  • Saturation of renal excretion
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The Correct Option is B

Solution and Explanation

Step 1: What is non-linear pharmacokinetics?
When pharmacokinetic parameters (like clearance or half-life) change with dose or concentration, the drug shows non-linear (dose-dependent) kinetics. There are several possible causes.

Step 2: Phenytoin's unique behaviour.
Phenytoin is the classic example of a drug with saturable metabolism. It is metabolised mainly by CYP2C9 enzymes. At low doses, plenty of enzyme is available and kinetics appear first-order. But as the dose increases, the enzymes become saturated and elimination shifts toward zero-order (Michaelis-Menten kinetics). A small dose increase can cause a disproportionately large rise in plasma concentration, making dosing dangerous.

Step 3: Eliminate the other causes.
Enzyme induction would increase metabolism and reduce levels, not cause non-linearity. Saturation of plasma protein binding does cause non-linearity but is not the primary reason for phenytoin's non-linearity. Saturation of renal excretion is not a significant feature of phenytoin (it is mainly hepatically metabolised).

Step 4: Clinical importance.
Because of saturable metabolism, phenytoin requires careful therapeutic drug monitoring. Even small dose increments near the therapeutic range can push levels into the toxic range.

Step 5: Conclusion.
The non-linearity of phenytoin is due to saturation of its metabolic enzymes (CYP2C9), giving it Michaelis-Menten kinetics.


Answer: Option (2) — Saturation of metabolic enzymes
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