国家: 加拿大
语言: 英文
来源: Health Canada
TRIMETHOPRIM
AA PHARMA INC
J01EA01
TRIMETHOPRIM
200MG
TABLET
TRIMETHOPRIM 200MG
ORAL
100
Prescription
URINARY ANTI-INFECTIVES
Active ingredient group (AIG) number: 0114346002; AHFS:
APPROVED
2010-06-17
PRODUCT MONOGRAPH TRIMETHOPRIM TRIMETHOPRIM TABLETS USP 100 MG AND 200 MG ANTIBACTERIAL AGENT AA PHARMA INC. DATE OF REVISION: 1165 CREDITSTONE ROAD, UNIT #1 MAY 14, 2014 VAUGHAN, ON L4K 4N7 CONTROL #: 172985 - 1 - PRODUCT MONOGRAPH TRIMETHOPRIM Trimethoprim Tablets USP 100 mg and 200 mg THERAPEUTIC CLASSIFICATION Antibacterial agent ACTIONS AND CLINICAL PHARMACOLOGY Trimethoprim blocks the production of tetrahydrofolic acid from dihydrofolic acid by binding to and reversibly inhibiting the enzyme dihydrofolate reductase. This binding is very much stronger for the bacterial enzyme than for the corresponding mammalian enzyme; thus, trimethoprim selectively interferes with bacterial biosynthesis of nucleic acids and proteins by causing a deficiency of endogenously produced thymine. The effect is usually bactericidal in the absence of an adequate external supply by thymine or thymidine (see MICROBIOLOGY). Trimethoprim is rapidly absorbed following oral administration. It exists in the blood as unbound, protein-bound and metabolized forms. Ten to 20% of trimethoprim is metabolized, primarily in the liver; the remainder is excreted unchanged in the urine. The principal metabolites of trimethoprim are the 1- and 3-oxides and the 3 - and 4 -hydroxy derivatives. The free form is considered to be the therapeutically active form. Approximately 44% of trimethoprim is bound to plasma proteins. Mean peak serum concentrations of approximately 1.0 µg/mL occur 1 to 4 hours after oral administration of a single 100 mg dose. A single 200 mg dose will result in serum levels approximately twice as high. The half-life of trimethoprim ranges from 8 to 10 hours. However, patients with severely impaired renal function exhibit an increase in the half-life of trimethoprim, which requires either dosage regimen adjustment or not using the drug in such patients (see DOSAGE AND ADMINISTRATION). During a 13-week study of trimethoprim administered at a daily dosage of 200 mg (50 mg q.i.d.), the mean minimum steady-state concentration of the dr 阅读完整的文件