Loading dose

Calculate the dose needed to reach a target plasma concentration immediately, rather than waiting the five half-lives that maintenance dosing alone would require.

High-consequence calculationA loading dose delivers a large amount of drug at once and is a recognised source of serious dosing errors. Verify the volume of distribution, the target concentration, and the bioavailability independently before administration.

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What is this for?

A loading dose fills the volume of distribution to the desired concentration in one step. It depends only on the volume of distribution and the target concentration, corrected for bioavailability — it does not depend on clearance, which is what distinguishes it from the maintenance dose.

How to use it

  1. Enter the target plasma concentration. Confirm it against a current reference — therapeutic ranges are revised.
  2. Enter the volume of distribution, choosing whether your source gives it in absolute litres or per kilogram. If per kilogram, add the weight.
  3. Enter the bioavailability as a fraction — 1 for intravenous.

Worked example

A drug has a volume of distribution of 0.7 L/kg. A 70 kg patient needs a plasma concentration of 20 mg/L. Calculate the intravenous loading dose.

Answer: Vd = 0.7 × 70 = 49 L. LD = (20 × 49) ÷ 1 = 980 mg.

Clinical pearls & pitfalls

  • The loading dose does not depend on clearance. This is why it is unchanged in renal impairment even though the maintenance dose must be reduced — a point that is frequently missed.
  • mg/L and mcg/mL are numerically identical. Therapeutic ranges are quoted in both, and mixing them up is not an error, but confusing either with mg/dL is.
  • For drugs with a slow distribution phase, giving the whole loading dose as one rapid bolus produces a transient toxic peak before distribution completes. Digoxin is loaded in divided doses for exactly this reason.
  • If a patient has already received some drug, subtract the amount already in the body — the loading dose is only the gap between the current and target concentrations.

Assumptions & limitations

  • Assumes a one-compartment model with instantaneous distribution. For multi-compartment drugs the initial concentration after a bolus is far higher than the calculated steady-state value.
  • Uses a population volume of distribution, which varies substantially between individuals and is altered by obesity, oedema, ascites, and critical illness.
  • Does not account for drug already present. Recalculate against the measured concentration if the patient has had recent doses.
  • Says nothing about infusion rate. Several loading doses must be given slowly to avoid rate-related toxicity — phenytoin and vancomycin are examples.

References

  • Rowland M, Tozer TN. Clinical Pharmacokinetics and Pharmacodynamics. 4th ed. Lippincott Williams & Wilkins.
  • Bauer LA. Applied Clinical Pharmacokinetics. 3rd ed. McGraw-Hill.
  • Institute for Safe Medication Practices. ISMP List of High-Alert Medications in Acute Care Settings.

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