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経口投与で完全に吸収され、食品は生物学的利用能に影響を与えない。活性型であるヒドロキシフルタミドの血中濃度は2-4日の投与で定常状態に達し、フルタミドの濃度の約50倍になる。血漿タンパク結合率は高く、フルタミド94-96%、ヒドロキシフルタミド92-94%である。フルタミドは肝臓のCYP1A2(α-水酸化反応)による初回通過代謝において、主代謝物であるヒドロキシフルタミド(投与1時間後に投与量の23%が変換される)、および少なくとも5種類の微量代謝物に代謝される。4-ニトロ-3-フルオロメチルアニリンを含む少なくとも10種類の不活性代謝物が存在する。さまざまな形で尿中に排泄されるが、主な代謝物は2-アミノ-5-ニトロ-4-(トリフルオロメチル)フェノールである。
排泄半減期は、成人でフルタミド4.7時間、ヒドロキシフルタミド6時間である。ヒドロキシフルタミドの半減期は、高齢者では単回投与で8時間、定常状態で9.6時間に延長される。半減期の短さから、8時間間隔で1日3回の投与が必要となる。一方、新しいNSAAであるニルタミド、ビカルタミド、エンザルタミドは半減期が非常に長く、1日1回の投与で十分である。