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Studies on beta‐aminopropionitrile in patients with scleroderma
Author(s) -
Keiser Harry R.,
Sjoerdsma Albert
Publication year - 1967
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt196784593
Subject(s) - hydroxyproline , scleroderma (fungus) , metabolite , drug , medicine , urinary system , pharmacology , endocrinology , pathology , inoculation
Single oral doses of β‐aminopropionitrile (BAPN) up to 3.5 Gm. and treatment for several days with doses as high as 2.0 Gm. per day were found to have no apparent pharmacologic or toxic effects in patients with scleroderma. As in the rat, cyanoacetic acid was found tobe the maior urinary metabolite of the drug. When four patients were treated with 1.0 to 3.0 Gm. of the drug per day for 22 to 67 days, distinct effects on collagen metabolism were observed, consisting of increases in urinary hydroxyproline and acid extractable dermal collagen and its a:β ratio. A reversible periosteal reaction occurred in one patient and untoward effects were observed in four other patients at a dose level which produced only moderate effects on skin collagen and no apparent therapeutic effect. Thus, future use of the drug as an inhibitor of collagen cross‐linking in man should probably be limited to short‐term trials.