Nalidixic Acid

Nalidixic Acid is an quinoline antibiotic used to treat urinary tract infections.

Nalidixic Acid is Rapidly and almost completely absorbed from the GI tract. (oral); peak plasma concentrations after 1-2 hr (oral) and Crosses the placenta; enters the breast milk. Protein-binding: 93% (nalidixic acid); 63% (hydroxynalidixic acid).It is Partially converted in the liver to hydroxynalidixic acid and get excreted Via urine (80-90% as inactive metabolites); faeces (4%); 1-2.5 hr (elimination half-life).

Nalidixic Acid shows common side effects like Hives, Difficulty breathing, Swelling of your face, lips, tongue, or throat, Increased difficulty breathing, Chest pain, and Fever

Nalidixic Acid is available in the form of tablet.

Nalidixic Acid is available in India, Germany, Canada, Italy.

Nalidixic acid is a quinolone antibacterial agent for oral administration. Nalidixic acid has marked antibacterial activity against gram-negative bacteria including Enterobacter species, Escherichia coli, Morganella Morganii; Proteus Mirabilis, Proteus vulgaris, and Providencia rettgeri. Pseudomonas species are generally resistant to the drug.

Nalidixic Acid is available in the form of tablet.

Nalidixic Acid is an quinoline antibiotic used to treat urinary tract infections.

Nalidixic acid is a 4-quinolone antibacterial. It interferes with the replication of bacterial DNA by inhibiting DNA gyrase activity. It acts against gram-negative bacteria including E. coli, Proteus, Klebsiella, Enterobacter, Salmonella and Shigella spp.

Nalidixic Acid is approved for use in the following clinical indications

To treat Urinary tract Infection.

Oral

Uncomplicated lower urinary tract infections

Adult: 1 g 4 times daily for 1-2 wk. Long-term therapy: Reduce daily dose to 2 g.

Child: >3 mth: 50 mg/kg daily in 4 equally divided doses. Long-term therapy: Reduce dose to 30 mg/kg daily. Prophylaxis: 15 mg/kg bid.

Nalidixic Acid is available in various strengths: 500 mg

Nalidixic Acid is available in the form of tablet and suspension.

Hypersensitivity. History of convulsive disorders or porphyria. Infants <3 month. Severe renal impairment.

Blood counts and renal and liver function tests should be performed periodically if treatment is continued for more than two weeks. Nalidixic Acid should be used with caution in patients with liver disease, epilepsy, or severe cerebral arteriosclerosis. While caution should be used in patients with severe renal failure, therapeutic concentrations of Nalidixic Acid in the urine, without increased toxicity due to drug accumulation in the blood, have been observed in patients on full dosage with creatinine clearances as low as 2 mL/minute to 8 mL/minute.

Moderate to severe phototoxicity reactions have been observed in patients who are exposed to direct sunlight while receiving Nalidixic Acid or other members of this drug class. Excessive sunlight should be avoided. Therapy should be discontinued if phototoxicity occurs.

If bacterial resistance to Nalidixic Acid emerges during treatment, it usually does so within 48 hours, permitting rapid change to another antimicrobial. Therefore, if the clinical response is unsatisfactory or if relapse occurs, cultures and sensitivity tests should be repeated. Underdosage with Nalidixic Acid during initial treatment (with less than 4 g per day for adults) may predispose to emergence of bacterial resistance.

Pregnancy Category C

Nalidixic Acid has been shown to be teratogenic and embryocidal in rats when given in oral doses six times the human dose. Nalidixic Acid also prolonged the duration of pregnancy especially at four times the clinical dose. There are no adequate and well-controlled studies in pregnant women. Since nalidixic acid, like other drugs in this class, causes arthropathy in immature animals, Nalidixic Acid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

• Common Adverse effects

Nausea, vomiting, diarrhoea, abdominal pain; photosensitivity reactions, allergic rash, urticaria, pruritus; visual disturbances, headache, dizziness or vertigo, drowsiness, confusion, depression, excitement, hallucinations, toxic psychoses or convulsions (especially after large doses), intracranial hypertension

• Less Common Adverse effects

Metabolic acidosis; peripheral neuropathies, muscular weakness, myalgia

• Rare Adverse effects

Arthralgia, tendon damage; cholestatic jaundice, thrombocytopenia, leucopenia.

Absorption reduced by sucralfate, and divalent and trivalent cations e.g. aluminium, calcium, iron, magnesium, zinc. Excretion reduced and plasma concentrations increased with probenecid. Reduced effects with chloramphenicol, nitrofurantoin, tetracycline.

Potentially Fatal: Fatal haemorrhagic enterocolitis may occur when used with high-dose melphalan in children. Increased risk of nephrotoxicity with ciclosporin. May increase effects of oral anticoagulants e.g. warfarin.

The common side effects of Nalidixic Acid include the following Nausea, vomiting, diarrhoea, abdominal pain; photosensitivity reactions, allergic rash, urticaria, pruritus; visual disturbances, headache, dizziness or vertigo, drowsiness, confusion, depression, excitement, hallucinations, toxic psychoses or convulsions (especially after large doses), intracranial hypertension.

Symptoms: Toxic psychosis, convulsions, increased intracranial pressure, metabolic acidosis, vomiting, nausea, lethargy.

Management: Increase fluid admin; supportive measures. Anticonvulsants may be used in severe cases.

Pharmacodynamics

Nalidixic acid is a quinolone antibacterial agent for oral administration. Nalidixic acid has marked antibacterial activity against gram-negative bacteria including Enterobacter species, Escherichia coli, Morganella Morganii; Proteus Mirabilis, Proteus vulgaris, and Providencia rettgeri. Pseudomonas species are generally resistant to the drug. Nalidixic acid is bactericidal and is effective over the entire urinary pH range. Conventional chromosomal resistance to nalidixic acid taken in full dosage has been reported to emerge in approximately 2 to 14 percent of patients during treatment; however, bacterial resistance to nalidixic acid has not been shown to be transferable via R factor.

Pharmacokinetics

• Absorption: Rapidly and almost completely absorbed from the GI tract. (oral); peak plasma concentrations after 1-2 hr (oral).
• Distribution: Crosses the placenta; enters the breast milk. Protein-binding: 93% (nalidixic acid); 63% (hydroxynalidixic acid).
• Metabolism: Partially converted in the liver to hydroxynalidixic acid.
• Excretion: Via urine (80-90% as inactive metabolites); faeces (4%); 1-2.5 hr (elimination half-life).

• https://www.uptodate.com/contents/topical-agents-and-dressings-for-local-burn-wound-care
• https://www.mims.com/india/drug/info/silver Nalidixic Acid ?type=full
• https://go.drugbank.com/drugs/DB00359