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Nalidixic acid | CAS No: 389-08-2 | GMP-certified suppliers
A medication that treats urinary tract infections caused by susceptible gram-negative bacteria, including Escherichia coli, Enterobacter, Klebsiella, and Proteus species.
Therapeutic categories
Primary indications
- For the treatment of urinary tract infections caused by susceptible gram-negative microorganisms, including the majority of <i>E
- Coli</i>, <i>Enterobacter</i> species, <i>Klebsiella</i> species, and <i>Proteus</i> species
Product Snapshot
- Nalidixic acid is available as oral tablets, suspensions, syrups, granules, and effervescent formulations
- It is primarily indicated for the treatment of urinary tract infections caused by susceptible gram-negative bacteria including E
- Coli, Enterobacter, Klebsiella, and Proteus species
Clinical Overview
Pharmacologically, nalidixic acid acts as a bactericidal quinolone. Its antibacterial activity is particularly notable against gram-negative organisms such as Enterobacter, Escherichia coli, Morganella morganii, Proteus mirabilis, Proteus vulgaris, and Providencia rettgeri. Pseudomonas species generally exhibit resistance. The drug maintains efficacy across the urinary pH spectrum, which is relevant to its clinical use in urinary tract infections.
The mechanism of action involves inhibition of bacterial DNA gyrase, specifically binding to the A subunit, thereby interfering with DNA synthesis. Its active metabolite, hydroxynalidixic acid, reversibly binds to DNA, disrupting RNA synthesis and subsequent protein synthesis, contributing to bacterial cell death. Resistance emerging during therapy is reported in 2 to 14 percent of patients but is chromosomal in nature and not transferable via plasmid-mediated R factors.
Key safety considerations include its classification as a moderate risk QTc-prolonging agent and photosensitizing potential, necessitating monitoring for cardiac effects and minimizing UV exposure during treatment. Nalidixic acid can reduce seizure threshold and interacts with cytochrome P450 enzymes, particularly CYP1A2, warranting caution in patients with predisposing conditions or concomitant medications.
Approved for systemic use, nalidixic acid is categorized as a 4-quinolone antibacterial and topoisomerase II inhibitor. It is utilized mainly in oral formulations for urinary indications.
For sourcing or procurement, attention should be given to API purity, adherence to pharmacopeial specifications specific to quinolone antibacterials, and control of potential impurities that may affect safety or efficacy. Stability under recommended storage conditions and compliance with regulatory standards are critical to ensure consistent therapeutic performance.
Identification & chemistry
| Generic name | Nalidixic acid |
|---|---|
| Molecule type | Small molecule |
| CAS | 389-08-2 |
| UNII | 3B91HWA56M |
| DrugBank ID | DB00779 |
Pharmacology
| Summary | Nalidixic acid is a quinolone antibacterial agent targeting bacterial DNA, primarily used to treat urinary tract infections caused by susceptible gram-negative bacteria. Its active metabolite binds reversibly to DNA, inhibiting RNA synthesis and subsequent protein production, resulting in bactericidal effects. Resistance development occurs chromosomally but is not transferable via plasmids. |
|---|---|
| Mechanism of action | Evidence exists for Nalidixic acid that its active metabolite, hydroxynalidixic acid, binds strongly, but reversibly, to DNA, interfering with synthesis of RNA and, consequently, with protein synthesis. |
| Pharmacodynamics | Nalidixic acid is a quinolone antibacterial agent for oral administration. Nalidixic acid has marked antibacterial activity against gram-negative bacteria including <i>Enterobacter</i> species, <i>Escherichia coli</i>, <i>Morganella Morganii</i>; <i>Proteus Mirabilis</i>, <i>Proteus vulgaris</i>, and <i>Providencia rettgeri</i>. <i>Pseudomonas</i> 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | other |
ADME / PK
| 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. |
|---|---|
| Half-life | 1.1 to 2.5 hours in healthy adult patients, and up to 21 hours in patients with impaired renal function. |
| Protein binding | Nalidixic acid is 93% bound to protein in the blood, and the active metabolite, hydroxynalidixic acid is 63% bound. |
| Metabolism | 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. |
| Route of elimination | Following oral administration, NegGram is rapidly absorbed from the gastrointestinal tract, partially metabolized in the liver, and rapidly excreted through the kidneys. Approximately four percent of NegGram is excreted in the feces. |
Formulation & handling
- Nalidixic acid is a small molecule antibiotic formulated exclusively for oral administration, including tablets, suspensions, and effervescent granules.
- The compound exhibits moderate water solubility and low lipophilicity (LogP 0.79), supporting oral bioavailability and formulation flexibility.
- Food intake is recommended to reduce gastrointestinal irritation, and formulation should consider ease of ingestion with fluids.
Regulatory status
| Lifecycle | The API's primary patent protection expired recently in the US and Canada, allowing for increased generic competition. Consequently, the product is entering a mature market phase with established availability across both regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Nalidixic acid is manufactured by multiple companies, including originator and generic suppliers, indicating an established supply base. Branded products such as NegGram are available primarily in the US and Canadian markets. Given the presence of multiple manufacturers, patent expiration has likely resulted in existing generic competition. |
|---|
Safety
| Toxicity | ORAL (LD<sub>50</sub>): 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. |
|---|
- Handle with appropriate protective equipment to avoid ingestion and minimize exposure risk due to potential central nervous system toxicity
- Avoid inhalation and skin contact, as overdose toxicity includes convulsions and metabolic disturbances observed in animal studies
- Store under controlled conditions to prevent degradation and maintain compound integrity given its acute toxicity profile
Nalidixic Acid is a type of Quinolones
Quinolones belong to a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs). They are a group of synthetic antibiotics that possess a broad-spectrum activity against various bacterial infections. This technical description will shed light on the key characteristics and applications of quinolones.
Quinolones exhibit potent bactericidal activity by targeting DNA gyrase and topoisomerase IV, which are essential enzymes for bacterial DNA replication and repair. This mechanism of action distinguishes quinolones from other classes of antibiotics, making them effective against both Gram-positive and Gram-negative bacteria.
The versatility of quinolones enables their application in the treatment of a wide range of infections, including respiratory tract infections, urinary tract infections, gastrointestinal infections, skin and soft tissue infections, and sexually transmitted diseases. Furthermore, they have proven efficacy against bacteria resistant to other antibiotics, making them indispensable in clinical practice.
Pharmaceutical companies utilize advanced manufacturing processes to synthesize quinolones with high purity and quality. Stringent quality control measures ensure the safety and efficacy of these APIs, complying with regulatory standards.
Quinolones have revolutionized the field of antibacterial therapy, providing healthcare professionals with potent tools to combat bacterial infections. However, it is crucial to utilize them judiciously to prevent the emergence of antibiotic resistance.
In conclusion, quinolones, as a subcategory of pharmaceutical APIs, possess remarkable antibacterial properties, making them invaluable in the treatment of various infections. Their broad-spectrum activity, mechanism of action, and effectiveness against resistant bacteria make quinolones a crucial component of modern healthcare.
Nalidixic Acid (Quinolones), classified under Anti-infective Agents
Anti-infective agents are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various infectious diseases. These agents play a crucial role in combating bacterial, viral, fungal, and parasitic infections. The demand for effective anti-infective APIs has grown significantly due to the increasing prevalence of drug-resistant microorganisms.
Anti-infective APIs encompass a wide range of substances, including antibiotics, antivirals, antifungals, and antiparasitics. Antibiotics are particularly important in fighting bacterial infections and are further categorized into different classes based on their mode of action and target bacteria. Antivirals are designed to inhibit viral replication and are essential in the treatment of viral infections such as influenza and HIV. Antifungals combat fungal infections, while antiparasitics are used to eliminate parasites that cause diseases like malaria and helminthiasis.
The development and production of high-quality anti-infective APIs require stringent manufacturing processes and adherence to regulatory standards. Pharmaceutical companies invest heavily in research and development to discover new and more effective anti-infective agents. Additionally, ensuring the safety, efficacy, and stability of these APIs is of utmost importance.
The global market for anti-infective APIs is driven by factors such as the rising incidence of infectious diseases, the emergence of new and drug-resistant pathogens, and the growing demand for improved healthcare infrastructure. Continuous advancements in pharmaceutical technology and the development of innovative drug delivery systems further contribute to the expansion of this market.
In conclusion, anti-infective agents are a critical category of pharmaceutical APIs that play a pivotal role in treating infectious diseases. Their effectiveness in combating various types of infections makes them essential components in the arsenal of modern medicine.
Nalidixic Acid API manufacturers & distributors
Compare qualified Nalidixic Acid API suppliers worldwide. We currently have 1 companies offering Nalidixic Acid API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| ABC Farmaceutici | Producer | Italy | Italy | CEP, CoA, GMP | 4 products |
When sending a request, specify which Nalidixic Acid API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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