Metroshin Infusion
Metronidazole B.P 5 mg/mL
(Sterile, Pyrogen Free, Isotonic, Single Dose)
Indication
Metronidazole intravenous infusion is used in the treatment of anaerobic infections in patients for whom oral administration is not possible. It is indicated for,
-Treatment of skin and skin structure infections caused by Bacteroides species and anaerobic cocci.
-Bone and joint infections, as adjunctive therapy, caused by Bacteroides species including the B. fragilis.
-Intra-abdominal infections: appendicitis, cholecystitis, peritonitis, liver abscess and post-operative wound infection.
-Gynaecological and obstetrical appendicitis, pelvic cellulitis, pelvic peritonitis.
-Respiratory tract infection that include pneumonia, empyema and lung abscess.
-Central nervous system (CNS) infections including meningitis and brain abscess caused by B. fragilis and Clostridium species.
-Endocarditis caused by Bacteroides species including B. fragilis.
-Amoebic abscess of the liver and in moribund or toxic cases of fulminating intestinal amoebiasis.
-Prevention of pre-operative and post-operative infection due to anaerobic bacteria.
In a mixed aerobic and anaerobic infection, appropriate antibiotic for the treatment of aerobic infection should be used in addition to metronidazole infusion.
Dosage and Administration
Inject 500 mg (100 mL) slowly by intravenous route over a period of 20-30 minutes at intervals of 8 hours.
A maximum of 4 g should not be exceeded during 24-hour period.
Composition
Each 100 mL contains:
Metronidazole B.P ... 500 mg
Water for Injection B.P ... q.s.
Description
Metronidazole Infusion is an sterile solution containing metronidazole as a ready-to-use solution. It is 2-(2-methyl -5-nitro-1H-imidazol-1-yl)ethanol. The molecular formula is C6H9N3O3 and molecular weight is 171.2.
Clinical Pharmacology
Mechanism of Action
Metronidazole is a nitroimidazole anti-infective agent which affects the nucleic acid metabolism of the bacteria. The nitro group of metronidazole is able to serve as electron receptor, forming reduced cytotoxic compounds that bind to proteins and DNA, resulting in cell death.
Pharmacological Action
Metronidazole has a specific activity against a number of obligate anaerobic organism and protozoa. A chemically reactive, reduced form of metronidazole, is thought to be responsible for the drug’s activity.
Antimicrobial Spectrum
Metronidazole attains the bactericidal action and is active against Trichomonas vaginalis, Entamoeba histolytica, Giardia lamblia, Bacteroides fragilis, B. melaninogenicus, Campylobacter fetus, C. perfrigens, Eubacterium, Peptococcus, Fusobacterium, Pepostreptococcus and Veilonella species.
Pharmacokinetics
Metronidazole is widely distributed in body tissues and fluids. Less than 20% of the circulating metronidazole is bound to plasma proteins. It readily penetrates tissues and has a large apparent volume of distribution equivalent to distribution over 70 to 95% body weight. The metabolites of metronid...
Contraindication
In patient with evidence if a history of blood dyscrasias (Occasionally a mild leukopenia has been observed during administration: however no persistent hematological abnormalities have been observed in animals or clinical studies.);
In the presence of active organic disease of central nervous system;
In patient who are hypersensitive to metronidazole or other nitroimidazoles.
Warning and Precaution
Metronidazole should be used with caution in patients with hepatic impairment or hepatic encephalopathy. As metronidazole is excreted in relatively high concentration in human breast milk, its use should be avoided in nursing mothers. Metronidazole can cross the placenta barrier. Therefore, it shoul...
Adverse Effects
Central Nervous System: headache, syncope, dizziness, peripheral neuropathy, vertigo, incoordination, ataxia, confusion, dysarthria, irritability, depression, weakness and insomnia.
Gastrointestinal: Particularly nausea, anorexia and occasionally vomiting, diarrhoea, epigastric distress, abdominal cramping and constipation.
Dermatologic: Erythematous rash and pruritus. Hematopoietic: Reversible neutropenia (leukopenia): rarely reversible thrombocytopenia.
Local reactions: Thrombophlebitis after intravenous infusion. This reaction can be minimized or avoided by avoiding prolonged use of indwelling intravenous catheters. Hypersensitivity: Urticaria, erythematous rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, flushing, nasal congestion, d...
Overdose
Overdose with metronidazole appears to be associated with very few abnormal signs or symptoms. Disorientation and vomiting may occur, especially after ingestion of large amounts.
Drug Interaction
Alcohol: Metronidazole inhibits the alcohol dehydrogenase and other oxidizing enzymes and may lead to mild disulfiram-like reaction.
Busulfan: Metronidazole increases the plasma concentration of busulfan during concomitant treatment which can result in serious busulfan toxicity.
Cimetidine: Since Cimetidine can decrease microsomal liver enzyme activity, it may prolong the half-life and decrease the plasma clearance of metronidazole.
Coumarins Anticoagulants: Metronidazole enhances the anticoagulant effect of coumarin resulting in prolongation of prothrombin time.
Disulfiram: Psychotic reaction reported when metronidazole given with disulfiram.
Fluorouracil: Increases toxicity of metronidazole by reducing drug removal from the body.
Lithium: Metronidazole increase the risk of toxicity of lithium.
Mycophenolate: Metronidazole possibly reduced the bioavailability of mycophenolate.
Phenobarbital and Phenytoin: Phenobarbital and phenytoin may accelerate the elimination of metronidazole resulting in reduced plasma concentration.
Corticosteroids: Care should be taken when administering metronidazole infusion to patients receiving corticosteroid therapy or to patients predisposed to oedema since administration of solutions containing sodium ions may result in sodium retention.
Storage
Should be stored between 15°C and 30°C. Do not remove inner container from carton box until ready for use.