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The Effect of Food on Cysteamine Bitartrate Absorption in Healthy Participants
Author(s) -
Dohil Ranjan,
Cabrera Betty L.,
Gangoiti Jon,
Rioux Patrice
Publication year - 2012
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1177/2160763x12454423
Subject(s) - medicine , cysteamine , absorption (acoustics) , pharmacology , optics , physics
Objectives : Treatment with cysteamine reduces the rate of progression to end‐stage kidney disease in cystinosis. Although food is often taken with cysteamine to reduce associated gastrointestinal symptoms, this may alter the bioavailability of cysteamine. Methods : This is a prospective, randomized, 3‐treatment study to determine the effects of fasting and high‐fat/calorie and high‐protein meals on cysteamine absorption in healthy adult controls. On 3 separate days, serial plasma cysteamine levels were measured after cysteamine bitartrate 500 mg was ingested while fasting and also 30 minutes after high‐fat/calorie and high‐protein diets. Gastrointestinal (GI) symptoms were also monitored. Results : Eight participants (5 men) were enrolled. Cysteamine absorption, as measured by area under the cysteamine concentration‐time curve (AUC 0‐∞ ) while fasted and following high‐fat/calorie and high‐protein meals, was 3618 ± 372 min·μM, 2799 ± 405 min·μM ( P = .04 vs fasted), and 2457 ± 353 min·μM ( P = .005), respectively, and the mean C max values for participants were 26.3 ± 3.5 μM, 22.4 ± 5.6 μM ( P = .16 vs fasted), and 17.2 ± 2.6 μM ( P = .036 vs fasted), respectively. Mild GI symptoms were reported in 3 participants. Conclusions : Cysteamine absorption may be decreased by 30% when taken with food as compared with the fasting state. Food causes wide variation in t max and C max for cysteamine.