Metronidazole + Furazolidone Pharmacology

Metronidazole + Furazolidone

About Metronidazole + Furazolidone
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Mechanism of Action of Metronidazole + Furazolidone
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Pharmacokinets of Metronidazole + Furazolidone
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Onset of Action for Metronidazole + Furazolidone
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Duration of Action for Metronidazole + Furazolidone
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Half Life of Metronidazole + Furazolidone
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Side Effects of Metronidazole + Furazolidone
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Contra-indications of Metronidazole + Furazolidone
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Special Precautions while taking Metronidazole + Furazolidone
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Metronidazole + Furazolidone
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Interactions for Metronidazole + Furazolidone
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Typical Dosage for Metronidazole + Furazolidone
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Schedule of Metronidazole + Furazolidone
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Storage Requirements for Metronidazole + Furazolidone
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Effects of Missed Dosage of Metronidazole + Furazolidone
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Effects of Overdose of Metronidazole + Furazolidone
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Metronidazole

About Metronidazole
A nitroimidazole antibiotic, Anti-infective, Antiprotozoal,amebicide.
Mechanism of Action of Metronidazole
Metronidazole is nitro imidazoles which have broad spectrum cidal activity against Protozoa and some anaerobic bacteria. Its selective toxicity to anaerobic microbes involves 1. Drug enters the cell by diffusion, 2. Nitro group of drug is reduced by redox proteins present only in anaerobic organisms to reactive nitro radical which exerts cytotoxic action by damaging DNA and other critical biomolecules. 3. DNA helix destabilization & strand breakage has been observed.
Pharmacokinets of Metronidazole
Absorption: Well absorbed orally, Distribution: Widely distributed,
Metabolism: Metabolized in liver by oxidation & glucuronide conjugation, Excretion: Excreted in urine.
Onset of Action for Metronidazole
1 to 2 days
Duration of Action for Metronidazole
8hours.
Half Life of Metronidazole
8 hours.
Side Effects of Metronidazole
1.Anorexia.
2.Metallic taste
3.Nausea
4.Vomiting
5.Diarrhoea
6.Headache
7.Looseness of stool.
8.Peripheral neuropathy &CNS effects.
9.Mutagenesis.
10.Radiosensitisation.
11.Transient leucopenia
12.Dry mouth
13.Abdominal distress
14.Dizziness
15.Vertigo
16.Thrombophlebitis at site of injection
17.Ototoxicity
Contra-indications of Metronidazole
1.Hypersensitivity to the drug
2.Blood dyscrasias
3.CNS disorders
Special Precautions while taking Metronidazole
1.Renal impairment
2.Hepatic impairment
3.Alcoholic cirrhosis
4.Use cautiously along with other hepatotoxic drugs & In visual field changes
Pregnancy Related Information
Use with caution
First trimester:contra indicated
Old Age Related Information
May be used.
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Neonates: Contraindicated
Indications for Metronidazole
1.Amoebiasis
2.Giardiasis
3.Trichomonas vaginitis
4.Pseudo membranous enterocolitis
5.Anaerobic bacterial infections after surgery, Brain abscess, & Endocarditis
6.Helicobacter pylori infections
7.Ulcerative gingivitis
Interactions for Metronidazole
Warfarin & other coumarin anticoagulants: Potentiates the anticoagulant effect resulting in increased prothrombin time.
Alcohol: A disulfiram-like reaction. Abdominal cramps, nausea, vomiting, headache & flushing.
Disulfiram: Acute psychotic reaction or confusional state.
Phenobarbital & Phenytoin: Increased metabolism of metronidazole resulting in decreased efficacy.
Lithium: Increased lithium levels and toxicity.
Flurouracil: Increased toxicity of flurouracil.
Lab tests: May interfere with chemical analysis for AST,SGOT, ALT, SGPT, LDH, triglycerides and hexokinase glucose. Zero values may occur.
Typical Dosage for Metronidazole
Adult
Amoebiasis:400 to 800 mg 8hourly for 5 to 10days depending up on the severity of infection
In severe infections and liver abscess: 1gm as slow I.V. infusion followed by 0.5 gm twice daily till oral therapy is started
Giardiasis:200mg 8hourly for 1week or 2gm/day for 3days or I.V.500mg thrice daily
Trichomonas vaginitis: 400mg 8 hourly for a week or 2gm once daily for a week.
Male partner should be concurrently treated with the drug
Pseudo membranous enterocolitis:800 mg 8hourly
Anaerobic bacterial infections after surgery, Brain abscess, & Endocarditis:400 to 800 mg 8hourly
In severe cases: 15mg/kg I.V. infusion for 1hour followed by 7.5mg/kg 4 times daily till oral therapy is substituted
Helicobacter pylori infections:400mg 8hourly along with amoxicillin/clarithromycin and a proton pump inhibitor
Ulcerative gingivitis:200 to 800mg 8hourly
Children
Amoebiasis: 30 to 50mg/kg/day for 5to10 days.
Giardiasis:10 to 15mg/kg/day thrice daily
Children (below 12years): 7.5mg/kg I.V.
Schedule of Metronidazole
H
Storage Requirements for Metronidazole
Store in a well closed container in a cool dark place. Keep out of the reach of children.
Effects of Missed Dosage of Metronidazole
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Metronidazole
Treatment is supportive & symptomatic. Drug is removed by induced emesis, gastric lavage, and administration of activated charcoal & use of cathartics. For controlling seizures diazepam & phenytoin may be used.

Furazolidone

About Furazolidone
A nitro furan derivative, Antibacterial,Antiprotozoal.
Mechanism of Action of Furazolidone
Furazolidone is a nitro furan which is employed as a broad spectrum bactericidal agent the actual mechanism of action is not clear. But it is known that it interfere with several bacterial enzyme systems. They have effects on DNA and bring about various changes in bacteria & also have radiomimetic & mutagenic properties
Pharmacokinets of Furazolidone
Absorption: It is partially absorbed orally
Excretion: It is excreted in urine
Onset of Action for Furazolidone
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Duration of Action for Furazolidone
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Half Life of Furazolidone
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Side Effects of Furazolidone
1. Dizziness
2. Headache
3. Nausea
4. Vomiting
5. Decreased B.P
6. Deafness with tinnitus
7. Urticaria
8. Fever
9. Arthralgia
10. Disulfiram like reactions with alcohol.
Contra-indications of Furazolidone
1. Hypersensitivity
2. Along with alcohol
Special Precautions while taking Furazolidone
1. Use cautiously in G6PD deficiency
2. Urine colour turns orange which has no clinical significance
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Neonates : Contraindicated
Indications for Furazolidone
1. Bacterial diarrhoea
2. Protozoal diarrhoea
3. Enteritis
4. Giardiasis
5. Trichomoniasis
6. Food poisoning
7. Infections caused by salmonella shigella etc.
8. Bacterial and monilial vaginitis
Interactions for Furazolidone
Alcohol: Disulfiram like reaction-facial flushing,light headedness, weakness, lacrimation.
Anorexiants: Increased pressor response of anorexiants due to MAO inhibition.
Levodopa: Both efficacy and adverse effects of levodopa increased especially hypertensive crisis. Effect lasts for several weeks after stopping furazolidone.
Sympathomimetics (indirect & mixed): Increased pressor sensitivity to these agents due to MAO inhibition.
TCAs: Hypertension, hyperpyrexia, seizures, tachycardia, acute psychosis.
Hypnotics & Sedatives: Dose of hypnotics and sedatives should be reduced.
Hypoglycaemics: Potentiates them.
Food: Hypertensive crisis with tyramine containing foods.

Typical Dosage for Furazolidone
Adults: 100mg 6 hourly 2 to 7 days depending up on the severity of infections
Children: 1.25 mg 6 hourly for 2 to 5 days & up to 10days for Giardiasis
Schedule of Furazolidone
H
Storage Requirements for Furazolidone
Store at controlled room temperature at a range of 15 to 30 degree C. in a well closed container and protects from light.
Effects of Missed Dosage of Furazolidone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Furazolidone
Treatment is supportive and symptomatic.

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