Severe infections caused by susceptible anaerobic bacteria or infections caused by Bacteroides fragilis that are resistant to clindamycin, chloramphenicol, and penicillin.
藥理
Amebicide; Antibiotic; Antiprotozoal, Nitroimidazole
After diffusing into the organism, interacts with DNA to cause a loss of helical DNA structure and strand breakage resulting in inhibition of protein synthesis and cell death in susceptible organisms.
藥動學
1.Distribution: To bile, seminal fluid, bone, liver, and liver abscesses, lung and vaginal secretions; crosses blood-brain barrier; saliva and CSF concentrations similar to those in plasma.
2.Protein binding: <20%.
3.Metabolism: Hepatic (30% to 60%) to several metabolites including an active hydroxyl metabolite which maintains activity ~30% to 65% of the parent compound.
4.Half-life elimination:Adults: ~8 hours.
5.Excretion: Urine (unchanged drug and metabolites: 60% to 80%; ~20% of total as unchanged drug); feces (6% to 15%).
禁忌症
1.Hypersensitivity to metronidazole, nitroimidazole derivatives, or any component of the formulation.
2.During the first trimester of pregnancy in patients with trichomoniasis.
3.Use of disulfiram within the past 2 weeks; use of alcohol or propylene glycol-containing products during therapy or within 3 days of therapy discontinuation.
懷孕分類
Cleft lip with or without cleft palate has been reported following first trimester exposure to metronidazole.
哺乳分類
Infant risk cannot be ruled out.
副作用
Nausea, vomiting, abdominal abnormalities, diarrhea, and an unpleasant metallic taste, reversible neutropenia, peripheral neuropathy, dizziness, confusion, allergy, depression, weakness and insomnia.
劑量和給藥方法
For anaerobic infection: IV, initial dose 15mg/kg, followed by maintenance dose 7.5 mg/kg/Q6H, MAX dose 4 g/day.