Nitrofurans:
- These are group of synthetic antibacterial compounds which contain 5-nitrofuran ring.
- These agents include furazolidine, furaltadone, nifuraldezone and nifurprazine
Mechanism of action:
These are types of pro drug which diffuses into susceptible bacteria
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Bacterial enzymes reduce these drug into reactive metabolites
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These metabolites blocks oxidative decarboxylation of pyruvate to acetyl coA
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Deprivation of energy in bacteria
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Antibacterial action of nitrofurans
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Antimicrobial spectrum:
- These have broad spectrum of activity against both gram -ve and gram +ve bacteria
- It is also active against coccidia, trichomonads, amoebae and giardia
- It is primarily bacteriostatic but may become bactericidal at high concentration
- Presence of pus, blood, plasma and milk may reduce antibacterial activity.
Bacterial resistance:
- Bacterial resistance develops slowly
- Resistance is mainly by chromosomal mutation
- It may show complete cross-resistance but no cross-resistance with any other antibacterial agent.
Pharmacokinetics:
- They are either absorbed or after absorption they are rapidly eliminated that no systemic inhibitory concentration is achieved in body varies with individual drugs.
- Administration along with feed promotes absorption
- Acidic urine promotes passive reabsorption of nitrofurans in renal tubule and also decreases their overall urine concentration.
Side effects/Adverse effects:
- GI disturbances (nausea, vomiting, diarrhoea)
- CNS signs (excitement, tremors, convulsion and peripheral neuritis)
- Depression of spermatogenesis, disturbances of eye and poor weight gain
- Hypersensitivity
Contraindications and precautions:
- In patients who are hypersensitive to nitrofurans
- It is not recommended in food producing animal
- It should not be used by parenteral route due to systemic toxicity
Clinical uses:
- It is used topically for cutaneous infection and wound dressing in all species
- It is used as urinary antiseptics in dogs and cats
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Nitrofurantoin:
- It is synthetic nitrofuran used mainly for prevention and treatment of urinary tract infections
Antimicrobial spectrum:
- It has wide range of antimicrobial activity including Staphylococcus aureus, Escherichia coli, Aerobacter aerogenes and species of Salmonella, Shigella, Klebsiella, Enterobacter and Corneybacterium.
- Pseudomonas aeruginosa & proteus, Serratia and Actinobacter species show little or no susceptibility to nitrofurantoin
- Antibacterial activity of nitrofurantoin is high in acidic urine
Pharmacokinetics:
- It is rapidly and almost completely absorbed from G.I tract
- They are rapidly excreted in urine via glomerular filtration
- Peak urine levels occur within 30 minutes of oral dosing
- Food enhances the oral absorption of nitrofurantoin
- Plasma half-lives is almost 20 minutes.
Side effects/Adverse effects:
- Nausea, vomiting, diarrhoea
- CNS disorders
Contraindications and precautions:
- It is contraindicated in patients with glucose-6-phosphate dehydrogenase deficiency because of risk of extravascular hemolysis resulting in anemia.
Uses:
- It is used exclusively for treatment of lower UTI in small animals
Dose:
Dogs & cats: 4 mg/kg, PO, 3 times daily
Horses: 2.5-4.5 mg/kg, PO, 3 times daily
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Furazolidone:
- It is synthetic nitrofuran used for enteric infection
Antimicrobial spectrum:
- It has wide spectrum of activity that includes Clostridium, Salmonella, Shigella, Staphylococcus & Streptococcus species and E.coli
- It is also active against Giardia, Trichomonas, Coccidia and Histomonas
Pharmacokinetics:
- They are poorly absorbed from G.I tract after oral administration
- After absorption, they are rapidly metabolized and excreted in urine
- Distributed into CSF.
Side effects/Adverse effects:
- Inappetence, nausea, vomiting, abdominal cramps and diarrhoea
- Tremors, ataxia, convulsions and visual impairment
Contraindications and precautions:
- It should not be administered with SSRI antidepressant, tricyclic antidepressant and triptans.
Indications:
- In treatment of enteric infections
- In bacterial enteritis, food poisoning, diarrhoea, bacillary dysentery and giardiasis
- It is used topically for subcutaneous infection
Dose:
For enteric infections
Dogs: 2.2 mg/kg, PO, 3 times daily for 7 days
Cats: 4 mg/kg, PO, 2 times daily for 7-10 days
Horses: 4mg/kg, PO, 3 times daily
Birds: 100-200 mg/L in drinking water
For coccidiosis
Dogs and cats: 8-20mg/kg, PO, 3 times daily for 7 days
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