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Clinical pharmacokinetics of dapsone
Clinical Pharmacokinetics
|July 1, 1986
Summary
Dapsone (DDS) is a key leprosy treatment with predictable pharmacokinetics and a new long-acting injection available. Understanding its absorption, metabolism, and therapeutic range is crucial for effective patient management.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Drug Metabolism
Background:
- Dapsone (DDS) has been the primary antileprosy drug for decades.
- Accurate determination of DDS and its metabolite MADDS is possible using high-performance liquid chromatography.
- Understanding DDS pharmacokinetics is vital for optimizing treatment regimens.
Purpose of the Study:
- To review the pharmacokinetics of dapsone (DDS) after oral and parenteral administration.
- To highlight the clinical significance of a new long-acting injectable DDS formulation.
- To discuss factors influencing DDS absorption, distribution, metabolism, and excretion.
Main Methods:
- Pharmacokinetic analysis of dapsone (DDS) and its metabolite MADDS.
- Review of concentration-time profiles after oral and parenteral administration.
- Assessment of protein binding, volume of distribution, and elimination half-life.
Main Results:
- DDS exhibits slow oral absorption (t½ ≈ 1.1 hours) with peak plasma concentrations around 4 hours.
- The elimination half-life of DDS is approximately 30 hours, fitting a 2-compartment model.
- A new long-acting injectable formulation allows monthly supervised administration, ensuring sustained absorption.
Conclusions:
- Dapsone (DDS) demonstrates linear pharmacokinetics within the therapeutic range (0.5-5 mg/L).
- Genetic variations in acetylation affect DDS metabolism, defining 'slow' and 'rapid' acetylators.
- Factors like liver disease, celiac disease, and severe leprosy can influence DDS pharmacokinetics, necessitating careful monitoring.