Pharmacokinetic evaluation of thiacetazone.
OBJECTIVE
To investigate the steady-state pharmacokinetics of thiacetazone (TB-1), which is active in vitro against Mycobacterium avium complex (MAC).


METHODS
Open-label phase I study.


METHODS
Specialized referral hospital.


METHODS
Twelve healthy men and women.


METHODS
Oral TB-1 150 mg/day was administered for 7 days, followed by blood and urine collection over 48 hours.


RESULTS
The serum concentration versus time curves of TB-1 showed sustained concentrations, with maximum values of 1.59 +/- 0.47 micrograms/ml, time to maximum 3.30 +/- 1.18 hours, and serum half-life of 15-16 hours. Less than 25% of TB-1 was recovered unchanged in the urine over 48 hours. Rashes occurred in two subjects at the end of the 7-day dosing period and resolved without progression or sequelae.


CONCLUSIONS
Based on these data, we initiated a phase II study of TB-I in patients with pulmonary MAC infection who do not have the acquired immunodeficiency syndrome.
Department of Medicine, National Jewish Center for Immunology and Respiratory Medicine, Denver, Colorado 80206, USA.
C A
CA
Peloquin
A T
AT
Nitta
S E
SE
Berning
M D
MD
Iseman
G T
GT
James
D000328:Adult; D000995:Antitubercular Agents / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D003875:Drug Eruptions; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D015269:Mycobacterium avium Complex; D015270:Mycobacterium avium-intracellulare Infection / Q000188:drug therapy*; D013828:Thioacetazone / Q000009:adverse effects / Q000493:pharmacokinetics*
D000995:Antitubercular Agents; D013828:Thioacetazone