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.
小兒調整劑量
Infants, Children, and Adolescents :
Oral: 15 to 50 mg/kg/day in divided doses every 8 hours; maximum daily dose: 2,250 mg/day.
IV: 22.5 to 40 mg/kg/day in divided doses every 6 or 8 hours; maximum daily dose: 4,000 mg/day.
腎功能調整劑量
■ Altered kidney function:
IV, Oral :
CrCl 10 mL/minute: No dosage adjustment necessary.
CrCl <10 mL/minute: No dosage adjustment necessary. A dose of 500 mg every 12 hours may be adequate to achieve therapeutic plasma levels for nonsevere non-Clostridioides difficile infections.
■ Hemodialysis, intermittent (thrice weekly) :
IV, Oral : 500 mg every 8 to 12 hours
肝功能調整劑量
Initial or dose adjustment in patients with preexisting liver cirrhosis:
Note: Single-dose regimens (eg, 2 g once) do not require dose adjustment (Ref).
■ Child-Turcotte-Pugh class A and B: No dosage adjustment necessary (Ref).
■ Child-Turcotte-Pugh class C :
Oral, IV :
1. If usual recommended frequency is every 12 hours: No adjustment necessary.
2. If usual recommended frequency is every 6 to 8 hours: Maintain dose but reduce frequency to every 12 hours. For example, if usual recommended dose is 500 mg every 6 hours, then reduce to 500 mg every 12 hours.