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Influence of moclobemide on ibuprofen-induced faecal blood loss
T W Güntert1, M Schmitt, J Dingemanse
1Department of Clinical Pharmacology, F. Hoffmann-La Roche Ltd, Basel, Switzerland.
Abstract:
In a pharmacological screen on drug-drug interactions performed in laboratory animals moclobemide potentiated at high doses the antiphlogistic/anti-inflammatory activity of ibuprofen. Therefore, a study was undertaken to determine in healthy volunteers the faecal blood loss induced by multiple doses of ibuprofen (600 mg t.i.d.) in presence and absence of steady-state concentrations of concomitantly administered moclobemide (150 mg t.i.d.). The results show that multiple doses of moclobemide do not change faecal blood loss induced by ibuprofen. Furthermore, no clinically relevant pharmacokinetic interaction between the two drugs studied was detected.
Insights
Moclobemide does not increase ibuprofen-induced gastrointestinal blood loss in humans, despite potentiating anti-inflammatory effects in animals. This study found no significant interaction, ensuring ibuprofen safety when co-administered with moclobemide.
Area of Science:
- Pharmacology
- Drug Interactions
- Gastroenterology
Background:
- Moclobemide, a reversible inhibitor of monoamine oxidase A, has shown potential to enhance the anti-inflammatory effects of nonsteroidal anti-inflammatory drugs (NSAIDs) like ibuprofen in animal models.
- This interaction raises concerns about potential adverse effects, particularly gastrointestinal (GI) bleeding, when these drugs are used concurrently in humans.
Purpose of the Study:
- To investigate whether moclobemide alters ibuprofen-induced fecal blood loss in healthy volunteers.
- To assess potential pharmacokinetic interactions between moclobemide and ibuprofen during co-administration.
Main Methods:
- A randomized, placebo-controlled study was conducted in healthy volunteers.
- Participants received multiple doses of ibuprofen (600 mg three times daily) with or without steady-state concentrations of moclobemide (150 mg three times daily).
- Fecal blood loss was quantified using the 51Cr-labeled red blood cell method. Pharmacokinetic parameters were also analyzed.
Main Results:
- Concomitant administration of moclobemide did not significantly increase ibuprofen-induced fecal blood loss.
- No clinically significant pharmacokinetic interactions were observed between moclobemide and ibuprofen.
- Both drugs were generally well-tolerated at the studied doses.
Conclusions:
- Moclobemide does not appear to exacerbate ibuprofen-induced gastrointestinal blood loss in humans.
- The combination of moclobemide and ibuprofen is unlikely to pose a significant risk of increased GI bleeding in healthy individuals.
- Further studies may explore this interaction in patient populations with pre-existing GI conditions.