Cơ chế tác động của Nalidixic Acid trong điều trị nhiễm khuẩn đường tiết niệu

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Nalidixic acid is a synthetic antibacterial drug that has been used to treat urinary tract infections (UTIs) for decades. It is a member of the quinolone class of antibiotics, which are known for their effectiveness against a wide range of bacteria. Nalidixic acid works by inhibiting the activity of an enzyme called DNA gyrase, which is essential for bacterial DNA replication. By blocking DNA gyrase, nalidixic acid prevents bacteria from multiplying and ultimately leads to their death.

Mechanism of Action

Nalidixic acid is a selective inhibitor of bacterial DNA gyrase, an enzyme that plays a crucial role in DNA replication. DNA gyrase is a type of topoisomerase that helps to relieve the torsional stress that builds up during DNA replication. This stress can cause the DNA molecule to become tangled and knotted, making it difficult for the replication machinery to function properly. Nalidixic acid binds to the DNA gyrase enzyme and prevents it from performing its normal function. This inhibition of DNA gyrase leads to the accumulation of torsional stress in the bacterial DNA, which ultimately results in the inhibition of DNA replication and bacterial cell death.

Pharmacokinetics

Nalidixic acid is rapidly absorbed from the gastrointestinal tract after oral administration. It is widely distributed throughout the body, including the urinary tract. The drug is primarily excreted in the urine, with a half-life of approximately 1 to 2 hours.

Clinical Applications

Nalidixic acid is primarily used to treat UTIs caused by susceptible strains of bacteria. It is effective against a wide range of gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis. However, it is not effective against gram-positive bacteria or anaerobic bacteria.

Resistance

Resistance to nalidixic acid can develop in bacteria, which can limit its effectiveness in treating UTIs. Resistance is often due to mutations in the DNA gyrase gene, which can alter the enzyme's structure and prevent nalidixic acid from binding to it.

Side Effects

Nalidixic acid can cause a variety of side effects, including nausea, vomiting, diarrhea, and abdominal pain. It can also cause allergic reactions, such as skin rash and itching. In rare cases, nalidixic acid can cause more serious side effects, such as seizures, liver damage, and blood disorders.

Conclusion

Nalidixic acid is a synthetic antibacterial drug that is effective against a wide range of gram-negative bacteria. It works by inhibiting the activity of DNA gyrase, an enzyme essential for bacterial DNA replication. Nalidixic acid is primarily used to treat UTIs, but resistance to the drug can develop, limiting its effectiveness. The drug can also cause a variety of side effects, ranging from mild to severe. Despite these limitations, nalidixic acid remains a valuable tool for treating UTIs in appropriate patients.