Metronidazole
Also known as: 5-Nitroimidazole
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.
Primary Characteristics
Metronidazole is also known as 5-Nitroimidazole.
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.
Molecular Weight: 171.15 · pKa: 2.62 · Solubility in Water: 1 in 100 · Solubility in Alcohol: 1 in 200 · Non-proprietary name: Metronidazole.
Pharmacokinetics
Absorption: Metronidazole has an oral bioavailability is 97.5% (±2.5%).
Distribution: Metronidazole has a volume of distribution is 0.76 - 1.02 l/kg. plasma protein binding is 10 %.
Elimination: it is metabolised via Hepatic, plasma half-life is 7.9 - 9.8 hr, renal excretion is 80 %. also excreted in feces.
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Indications
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.
Metronidazole is also indicated for secondary conditions like Amoebic liver abscess, Bacterial vaginosis, Cancer, Clostridium difficile colitis, Crohn's disease, Dental infections, Helicobacter pylori infection.
Contraindications
Metronidazole is contraindicated in conditions like Alcohol dependence, Blood dyscrasias, Neurosis, Seizures, Hypersensitivity, Liver damage.
Dosage
Metronidazole's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 30 mg/kg | 30 mg/kg | — | IV | |
| 32.5 mg/kg | 32.5 mg/kg | — | Oral | Dose very according to condition. |
| 400 mg | 400 mg | — | PO | For 5 to 10 days , frequency could be 2 or 3 times a day. |
| Paediatric Dosage (20kg) | ||||
| 7.5 mg/kg | 7.5 mg/kg | Every 8h | Intra Venous | - |
| 15 mg/kg | 15 mg/kg | — | IV Infusion | Over 60 mins.Initial then 7.5 mg/kg every 24 hour is given starting 48 hours after initial dose. |
| 7.5 mg/kg | 7.5 mg/kg | Every 8h | Oral | - |
| Neonatal Dosage (3kg) | ||||
| 7.5 mg/kg | 7.5 mg/kg | Every 8h | Iv Infusion | |
| 7.5 mg/kg | 7.5 mg/kg | Every 8h | Oral | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Metronidazole in overdosage may give rise to further complications which include Encephalopathy , Convulsions , Ataxia , Peripheral neuropathy , Neutropenia , Seizures , Depression , Headache , Dysarthria, Aseptic meningitis.
The signs and symptoms that are produced after acute overdosage of Metronidazole are Disorientation , Vomiting, Ataxia.
Metronidazole is known to cause more or less tolerable side effects which are usually transient. These include Acute pancreatitis, Anorexia , Chest pain, Darkening of urine, Diarrhea, Dizziness, Dry mouth, Dysuria, Flushing, GI upset, Gynecomastia, Headache, Insomnia, Maculopapular rash, Metallic taste, Nausea and vomiting, Palpitation, Paresthesias, Phlebitis , Pruritus , Rashes , Stomatitis, Thrush, Urticaria, Vertigo, Weakness.
Warnings / Precautions
Interference in Pathology
Metronidazole may interfere in the diagnosis of Aspartate Aminotransferase Assay .
Available Brands
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Single Ingredient
Multi-Ingredient Combinations
Storage Conditions
Drug Classification
- 1.6.2.2.6 — Metronidazole
- 2.6.4.1 — Antiamebic & antigiardiasis drugs
Manufacturers
Manufacturers of Metronidazole in Pakistan: