Metronidazole is a synthetic antibacterial and antiprotozoal agent that belongs to the nitroimidazole class. Metronidazole is effective therapy against protozoa such as Trichomonas vaginalis, amebiasis, and giardiasis. In addition, Metronidazole is one of the most effective drugs available against anaerobic bacterial infections. Metronidazole is also useful in treating Crohn's disease, antibiotic-associated diarrhea, and rosacea. It initially was approved by the FDA in 1963 and is available in oral, parenteral, and topical formulations.Metronidazole is amebicidal, bactericidal, and trichomonicidal. Unionized Metronidazole is readily taken up by anaerobic organisms and cells. It acts selectively aganist anaerobic bacterias as only these bacteria are capabale to reduce it to its active form intracellularly. Reduced it then disrupts DNA's helical structure, thereby inhibiting bacterial nucleic acid synthesis. This eventually results in bacterial cell death.
Metronidazole Benzoate is the derivative of Metronidazole. It is of Synthetic origin and belongs to Nitroimidazole. It belongs to Antibiotic (Prokaryote DNA) pharmacological group on the basis of mechanism of action and also classified in Amebicides pharmacological group.The Molecular Weight of Metronidazole is 171.15. Its pKa is 2.62.
Oral absorption of Metronidazole is found to be 97.5% ±2.5. Volume of distribution is found to be 0.76 - 1.02 l/kg and plasma protien binding is 10 %. and metabolism is reported Hepatic. Renal Excretion accounts for 80 %. also excreted in feces and plasma half life is 7.9 - 9.8 hr.
Metronidazole is primarily indicated in conditions like
Acute dental infections, Acute ulcerative gingivitis, Amoebiasis, Anaerobic bacterial infection, Anaerobic infections, Dysentery, Giardiasis, Lung cancer and pancreatic cancer, Pelvic inflammatory disease, Protozoa infection, Schizophrenia and other psychoses, Surgical prophylaxis, Treatment of locally advanced or metastatic pancreatic cancer, Trichomoniasis, Urogenital trichomoniasis, and can also be given in adjunctive therapy as an alternative drug of choice in Bacterial vaginosis, Cancer, Clostridium difficile colitis, Crohn's disease, Dental infections, Helicobacter pylori infection.
Metronidazole is known to interact with other drugs, the details of drug interactions is as follows:
Drug Details Severity Onset Management Alprazolam Carbamazepine Metronidazole enhances the serum concentration of carbamazepine. Moderate During coadministration carbamazepine serum kevel and clinical effects should be closely monitored. Cimetidine (HCl) Cimetidine increases the serum concentration of metronidazole by inhibiting its hepatic metabolism. Minor Disulfiram Coadministration results in confusion and acute psychoses. Moderate Metronidazole should not be administered when using disulfiram. Disulfiram Fluorouracil Lithium Lithium toxicity occurs when lithium is used with metronidazole. Nicoumalone Phenindione Phenytoin (Na) Metronidazole increases the serum concentration of phenytoin by inhibiting its metabolism. Also phentytoin increases elimination of metronidazole. Moderate Serum level of phenytoin should be closely monitor and dose of phenytoin should be adjusted accordingly. Podophyllum The risk of peripheral neuropathy may be increased during concurrent use of two or more agents that are associated with this adverse effect. In some cases, the neuropathy may progress or become irreversible despite discontinuation of the medications. Moderate Caution is advised during concomitant use of agents with neurotoxic effects. Patients should be monitored closely for symptoms of neuropathy such as burning, tingling, pain, or numbness in the hands and feet. Since the development of peripheral neuropathy may be dose-related for many drugs, the recommended dosages should generally not be exceeded. Ritonavir Stavudine Warfarin (Na) Metronidazole increases the plasma concentration and thus hypoprothrombinemic effect of warfarin by inhibiting is metabolism, and hence increase prothrombin time of patients taking metronidazole. Major Frequently checked INR and dose of warfarin should be adjusted accordingly. Patient should report any sign of bleeding to physician. Zalcitabine
These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interference in Pathology
Aspartate Aminotransferase Assay
The severe or irreversible adverse effects of Metronidazole, which give rise to further complications include Encephalopathy, Ataxia, Peripheral neuropathy, Neutropenia, Seizures, Headache.
The signs and symptoms that are produced after the acute overdosage of Metronidazole include Disorientation.
The symptomatic adverse reactions produced by Metronidazole are more or less tolerable and if they become severe, they can be treated symptomatically, these include Weakness, Dizziness, Vertigo, Headache, Anorexia, Diarrhea, Palpitation, Insomnia, Dry mouth, Maculopapular rash, Rashes, Stomatitis, Urticaria, Pruritus, Dysuria, GI upset, Flushing, Phlebitis, Nausea and vomiting, Gynecomastia, Chest pain, Metallic taste, Paresthesias, Acute pancreatitis, Darkening of urine, Thrush.
Click on the appropriate strength of the dosage form to view its available brands.
Single Ingredient Inj: 500 mg, 5 mg/ml, Inf: 500 mg, 5 mg/ml, 500 mg/100ml, Syrup: 75 mg/5ml, Susp: 200 mg, 75 mg/5ml, 200 mg/5ml, Cream: 0.75 %w/w, Gel: 0.75 %, 0.75 %w/w, Tabs: 200 mg, 250 mg, 400 mg, 500 mg, Tabs DS: 400 mg, Vag Tabs: 500 mg, Multi ingredient
Syrup: 200 mg/5ml, Susp: 200 mg, 75 mg/5ml, 100 mg/5ml, 200 mg/5ml, 250 mg/5ml, 400 mg/5ml, 200 mg/10ml, 321.6 mg/5ml, Gel: 1 % w/w, 0.75 % w/w, Tabs: 100 mg, 200 mg, 250 mg, 300 mg, 400 mg, 500 mg,
Metronidazole's dosage details are as follows:
30 mg/kg 30 (30) As recommended. IV
500 to 2000 mg 1200 (1250) 8 hourly PO For 5 to 10 days
Paedriatic Dosage ( 20 Kg. )
7.5 mg/kg 7.5 (7.5) 8 hourly Intra Venous - 7.5 mg/kg 7.5 (7.5) 8 hourly IV Infusion -
7.5 mg/kg 7.5 (7.5) 8 hourly Oral -
Neonatal Dosage ( 3 Kg. )
7.5 mg/kg 7.5 (7.5) 8 hourly Iv Infusion
7.5 mg/kg 7.5 (7.5) 8 hourly Oral
High Risk Groups
Drug should not be given to Pregnant Mothers, and patients suffering from Liver Malfunction.
If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Warning / Precautions
Metronidazole should be used with caution in patients with any allergy. Avoid use during pregnancy or lactation. Avoid alcoholic beverages while taking this medication as severe stomach upset, nausea, vomiting, headache and flushing can occur.
Tab, Susp, Inj
Store Below 40°C. Protect from Sunlight.
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