Background: Sildenafil citrate (Viagra), a drug used to treat erectile dysfunctions, causes adverse reactions such as headache, flushing or nasal congestion. Sildanefil’s potency as inhibitor of diamine oxidase was investigated, as side effects may also be induced by histamine itself due to an impaired histamine metabolism. Methods: Placental diamine oxidase inhibition experiments were performed with consecutive dilutions of sildenafil citrate (10–5 to 10–9 mol/l). In 9 male volunteers in vivo diamine oxidase inhibition was investigated after taking 100 mg sildenafil (Viagra). Results: Sildenafil citrate did not inhibit placental diamine oxidase either in vitro or in vivo. However, infusion of 300 mg of cimetidine inhibited diamine oxidase activity by 27 ± 7% 15 min after infusion, demonstrating that drugs may inhibit diamine oxidase in vivo. Conclusion: As side effects of sildenafil are not caused due to inhibition of diamine oxidase, sildenafil citrate seems to be harmless for patients suffering from histamine intolerance.

Keywords:
Sildenafil citrate, Diamine oxidase, Inhibition, diamine oxidase in vitro and in vivo, Histamine intolerance
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© 2001 S. Karger AG, Basel
2001
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