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document
Pharmacokinetics and pharmacodynamics of the monoamine oxidase B inhibitor mofegiline assessed during a phase I dose tolerance trial . The safety , pharmacokinetics , and pharmacodynamics of single oral doses of up to 48 mg and daily ( for 28 days ) doses of up 24 mg mofegiline were investigated in healthy male volunteers . Plasma pharmacokinetics indicated rapid absorption and elimination : time to reach maximum concentration occurred at about 1 hour ; half-life ranged from 1 to 3 hours . Maximal plasma concentration and area under the plasma concentration-time curve increased and oral clearance decreased disproportionately with dose . Mofegiline rapidly and markedly inhibited platelet monoamine oxidase B ( MAOB ) activity , which returned to baseline within 14 days . Urinary excretion of phenylethylamine increased proportionately with doses up to 24 mg. No changes in urinary elimination of catecholamines , blood pressure , heart rate , or ECG were observed . A classic maximum tolerated dose was not achieved in these studies . However , the 48 mg single dose and the 24 mg multiple daily dose far exceeded the dose ( 1 mg ) that was associated with > 90 % platelet MAOB inhibition .
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Intervention_Pharmacological
monoamine oxidase B inhibitor mofegiline
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Intervention_Pharmacological
mofegiline
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Intervention_Pharmacological
Mofegiline
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Outcome_Other
Maximal plasma concentration and area under the plasma concentration-time curve
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Outcome_Physical
Mofegiline rapidly and markedly inhibited platelet monoamine oxidase B ( MAOB ) activity
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Outcome_Physical
Urinary excretion of phenylethylamine
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Outcome_Physical
urinary elimination of catecholamines
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Outcome_Physical
blood pressure
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Outcome_Physical
heart rate
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Outcome_Physical
ECG
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Outcome_Other
maximum tolerated dose