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Oral sumatriptan and almotriptan--delimiting the MAOI effect
Florian Oberhardt1, Anthony W Fox
1EBD Consulting, 2032 Corte del Nogal #120, Carlsbad, CA 92011, USA.
Headache
|March 23, 2012
Summary
A pharmacokinetic model for oral sumatriptan was developed and validated. This model accurately predicted sumatriptan and almotriptan concentrations, even with monoamine oxidase A inhibitors (MAOI-A).
Area of Science:
- Pharmacokinetics
- Pharmacology
- Mathematical Modeling
Background:
- Sumatriptan's pharmacokinetic model for subcutaneous administration exists.
- US product labeling contains statements regarding oral sumatriptan and its interactions.
Purpose of the Study:
- To adapt a parsimonious pharmacokinetic model for oral sumatriptan.
- To assess the impact of monoamine oxidase A inhibitors (MAOI-A) on this model.
- To determine the generalizability of the model to oral almotriptan.
Main Methods:
- Extended a prior subcutaneous sumatriptan pharmacokinetic model.
- Employed numerical solutions for three concurrent differential equations.
- Utilized prospective criteria for model validation against clinical data.
Main Results:
- Successfully adapted the model by incorporating a time factor in the absorption phase.
- The extended model accurately reflected clinical data for oral sumatriptan across three doses, with and without MAOI-A.
- The model demonstrated robustness and generalizability to oral almotriptan.
Conclusions:
- A differential calculus-based pharmacokinetic model for oral sumatriptan is feasible and generalizable to almotriptan.
- MAOI-A appears to influence elimination kinetics more than first-pass metabolism.
- The interaction between MAOI-A and sumatriptan may be overstated in current product labeling.
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