Sulfonamides類抗生素 Urinary tract infections caused by susceptible strains of E. coli, Proteus, Klebsiella, Enterobacter, H. influenzae, S. pneumoniae, Shigella spp.
藥理
Trimethoprim: Antibiotic, Miscellaneous
Trimethoprim inhibits dihydrofolic acid reduction to tetrahydrofolate resulting in sequential inhibition of enzymes of the folic acid pathway Sulfamethoxazole: Antibiotic, Sulfonamide Derivative
Sulfamethoxazole interferes with bacterial folic acid synthesis and growth via inhibition of dihydrofolic acid formation from para-aminobenzoic acid
藥動學
Absorption: Rapid; almost completely Distribution:
1. Both SMX and TMP distribute to middle ear fluid, sputum, vaginal fluid; TMP also distributes into bronchial secretions
2. Protein binding: (SMX) ~70%; (TMP) ~44% Metabolism: Hepatic, both to multiple metabolites; SMX to hydroxy (via CYP2C9) and acetyl derivatives, and also conjugated with glucuronide; TMP to oxide and hydroxy derivatives; the free forms of both SMX and TMP are therapeutically active Time to peak: 1 to 4 hours Excretion: Both are excreted in urine as metabolites and unchanged drug
禁忌症
1. Pregnancy, infants younger than 2 months, lactation
2. Hypersensitivity to sulfonamides or trimethoprim, patients with impaired renal or hepatic function
懷孕分類
C
哺乳分類
Probably safe, except in premature infant or infant with G6PD deficiency.
副作用
Agranulocytosis, aplastic and megaloblastic anemia, nausea, erythema multiforme, headache, depression
劑量和給藥方法
In urinary tract infection, MAX trimethoprin 640mg/Sulfamethoxazole 3.2g
小兒調整劑量
8 mg/kg trimethoprim and 40 mg/kg sulfamethoxazole daily, give in 2 divided dose Q12H