Nalidixate - General Information
A synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase. [PubChem]
Pharmacology of Nalidixate
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.
Nalidixate for patients
Patients should be advised NegGram may be taken with or without meals. Patients should be advised to drink fluids liberally and not take antacids.
Patients should be advised that quinolones may be associated with hypersensitivity reactions, even following a single dose, and to discontinue the drug at the first sign of a skin rash or other allergic reactions.
Quinolones may cause dizziness and lightheadedness, therefore, patients should know how they react to NegGram before they operate an automobile or machinery or engage in activities requiring mental alertness or coordination.
Patients should be advised that quinolones may increase the effects of theophylline and caffeine. There is a possibility of caffeine accumulation when products containing caffeine are consumed while taking quinolones. Patients should be advised to avoid excessive sunlight or artificial ultraviolet light while receiving nalidixic acid and to discontinue therapy if phototoxicity occurs.
Patients should be advised that convulsions have been reported in patients taking quinolones, including Nalidixic acid, and to notify their physician before taking this drug if there is a history of this condition. Patients should be advised that mineral supplements, vitamins with iron or minerals, calcium-, aluminum-, magnesium-based antacids, sucralfate or Videx®, (Didanosine), chewable/buffered tablets of the pediatric powder for oral solution should not be taken within the two-hour period before or within the two-hour period after taking nalidixic aid.
Elevated plasma levels of theophylline have been reported with concomitant quinolone use. There have been reports of theophylline-related side effects in patients on concomitant therapy with quinolones and theophylline. Therefore, monitoring of theophylline plasma levels should be considered and dosage of theophylline adjusted, as required.
Quinolones have been shown to interfere with the metabolism of caffeine. This may lead to reduced clearance of caffeine and the prolongation of its plasma half-life.
Quinolones, including nalidixic acid, may enhance the effects of the oral anticoagulant warfarin or its derivatives. When these products are administered concomitantly, prothrombin time or other suitable coagulation test should be closely monitored.
Nitrofurantoin interferes with the therapeutic action of nalidixic acid.
Antacids containing magnesium, aluminum, or calcium; sucralfate or divalent or trivalent cations such as iron; multivitamins containing zinc; and Videx®, (Didanosine), chewable/buffered tablets or the pediatric powder for oral solution may substantially interfere with the absorption of quinolones, resulting in systemic levels considerably lower than desired. These agents should not be taken within the two hour period before or within the two-hour period after nalidixic acid administration.
Elevated serum levels of cyclosporine have been reported with the concomitant use of some quinolones and cyclosporine. Therefore, cyclosporine serum levels should be monitored and appropriate cyclosporine dosage adjustments made when these drugs are used concomitantly.
NegGram is contraindicated in patients with known hypersensitivity to nalidixic acid and in patients with a history of convulsive disorders.
Additional information about Nalidixate
Nalidixate Indication: For the treatment of urinary tract infections caused by susceptible gram-negative microorganisms, including the majority of E. Coli, Enterobacter species, Klebsiella species, and Proteus species.
Mechanism Of Action: Evidence exists that the active metabolite, hydroxynalidixic acid, binds strongly, but reversibly, to DNA, interfering with synthesis of RNA and, consequently, with protein synthesis.
Drug Interactions: Anisindione The quinolone increases the anticoagulant effect
Acenocoumarol The quinolone increases the anticoagulant effect
Dicumarol The quinolone increases the anticoagulant effect
Warfarin The quinolone increases the anticoagulant effect
Food Interactions: Not Available
Generic Name: Nalidixic Acid
Synonyms: Not Available
Drug Category: Anti-Infective Agents; Enzyme Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Nalidixic Acid: Cybis; Dixiben; Dixinal; Eucistin; Innoxalon; Jicsron; Nalidic acid; Nalidixan; Nalidixate; Nalidixic acid USP27; Nalidixin; Nalidixinic acid; Nalitucsan; Nalix; Nalurin; Naxuril; NegGram; Negram; Nevigramon; Nogram; Sicmylon; Unaserus; Urisal; Uronidix; Wintomylon; Wintron; naladixic acid;
Absorption: Following oral administration, nalidixic acid is rapidly absorbed from the gastrointestinal tract. Bioavailability is approximately 96%. Absorption may be delayed if taken with antacids.
Toxicity (Overdose): ORAL (LD50): Acute: 1160 mg/kg [Rat]. 572 mg/kg [Mouse]. Toxic psychosis, convulsions, increased intracranial pressure, or metabolic acidosis may occur in patients taking more than the recommended dosage. Vomiting, nausea, and lethargy may also occur following overdosage.
Protein Binding: Nalidixic acid is 93% bound to protein in the blood, and the active metabolite, hydroxynalidixic acid is 63% bound.
Biotransformation: Hepatic. 30% of administered dose is metabolized to the active metabolite, hydroxynalidixic acid. Rapid conjugation of parent drug and active metabolite to inactive metabolites. Metabolism may vary widely among individuals. In the urine, hydroxynalidixic acid represents 80 to 85% of the antibacterial activity.
Half Life: 1.1 to 2.5 hours in healthy adult patients, and up to 21 hours in patients with impaired renal function.
Dosage Forms of Nalidixate: Tablet Oral
Chemical IUPAC Name: 1-ethyl-7-methyl-4-oxo-1,8-naphthyridine-3-carboxylic acid
Chemical Formula: C12H12N2O3
Nalidixic Acid on Wikipedia: Not Available
Organisms Affected: Enteric bacteria and other eubacteria