Definition:
Anti-tubercular drugs are medications used in the treatment of tuberculosis (TB), a bacterial infection caused by Mycobacterium tuberculosis. These drugs work by inhibiting the growth and replication of the bacteria, thus helping to eliminate the infection from the body. Treatment typically involves a combination of several anti-tubercular drugs to prevent the development of drug resistance.
Classification of Anti-tubercular drugs
Anti-tubercular drugs can be classified into several categories based on their mechanism of action and effectiveness against different forms of tuberculosis:
1. First-Line Drugs:
First-line drugs are the primary agents used in the treatment of tuberculosis (TB) and are usually the first choice for drug-sensitive TB. These drugs are highly effective and form the backbone of TB treatment regimens. Here are examples of first-line drugs:
Isoniazid (INH):
– Isoniazid is one of the most important anti-tubercular drugs and is commonly used in TB treatment.
– It works by inhibiting the synthesis of mycolic acids, essential components of the bacterial cell wall.
– Isoniazid is often included in combination therapy for both active TB and latent TB infection.
– Common side effects include hepatotoxicity (liver damage), peripheral neuropathy, and drug-induced lupus.
Rifampin (RIF):
– Rifampin is a potent bactericidal drug that is highly effective against Mycobacterium tuberculosis.
– It works by inhibiting bacterial RNA synthesis.
– Rifampin is a key component of first-line TB treatment regimens and is often used in combination with other drugs.
– Side effects may include hepatotoxicity, gastrointestinal disturbances, and drug interactions.
Pyrazinamide (PZA):
– Pyrazinamide is an important first-line drug with potent activity against intracellular mycobacteria.
– It works by disrupting bacterial metabolism and is particularly effective against dormant bacilli.
– Pyrazinamide is used in the initial phase of TB treatment to shorten the duration of therapy.
– Common side effects include hepatotoxicity, hyperuricemia (elevated uric acid levels), and gastrointestinal upset.
Ethambutol (EMB):
– Ethambutol is a bacteriostatic drug that inhibits the synthesis of mycobacterial cell wall components.
– It is often included in first-line TB treatment regimens to prevent the emergence of drug resistance.
– Ethambutol is generally well-tolerated, but it can cause optic neuritis, leading to visual disturbances.
– Regular monitoring of visual acuity is recommended during treatment with ethambutol.
Streptomycin:
– Streptomycin is an aminoglycoside antibiotic that was one of the first drugs used to treat TB.
– It works by inhibiting bacterial protein synthesis.
– Streptomycin is less commonly used today due to the availability of more effective and less toxic drugs.
– Side effects may include ototoxicity (hearing loss), nephrotoxicity (kidney damage), and neuromuscular blockade.
2. Second-Line Drugs:
Second-line drugs are used in the treatment of drug-resistant tuberculosis (TB) when first-line drugs are ineffective or intolerable. These drugs are often less effective and more toxic than first-line agents and are reserved for specific situations. Here are examples of second-line drugs:
Fluoroquinolones:
– Fluoroquinolones are a class of antibiotics that inhibit bacterial DNA synthesis.
– Examples include ofloxacin, levofloxacin, moxifloxacin, and ciprofloxacin.
– Fluoroquinolones are used in the treatment of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB).
– Side effects may include gastrointestinal upset, tendonitis, and QT interval prolongation.
Other Oral Drugs:
– Ethionamide, prothionamide, cycloserine, terizidone, para-aminosalicylic acid (PAS), rifabutin, and rifapentine are among the other oral drugs used in the treatment of drug-resistant TB.
– These drugs have varying mechanisms of action and may be used in combination therapy to improve treatment outcomes.
– Side effects vary depending on the specific drug but may include hepatotoxicity, neurotoxicity, and gastrointestinal disturbances.
Injectable Drugs:
– Injectable drugs such as kanamycin, amikacin, and capreomycin are used in the treatment of MDR-TB and XDR-TB.
– These drugs are administered by injection and are often included in multidrug regimens for the treatment of drug-resistant TB.
– Side effects may include ototoxicity, nephrotoxicity, and injection site reactions.
Dose:
The dosage of anti-tubercular drugs varies depending on factors such as the patient’s weight, age, and the severity of the infection. It is essential to follow the dosage regimen prescribed by a healthcare professional. Here are some typical dosages for first-line anti-tubercular drugs:
1. Isoniazid (INH):
– Adult dose: 5 mg/kg (up to 300 mg) once daily or 15 mg/kg (up to 900 mg) three times weekly.
– Pediatric dose: 10-15 mg/kg (up to 300 mg) once daily or three times weekly.
2. Rifampicin (RIF):
– Adult dose: 10 mg/kg (up to 600 mg) once daily or twice weekly.
– Pediatric dose: 10-20 mg/kg (up to 600 mg) once daily or twice weekly.
3. Pyrazinamide (PZA):
– Adult dose: 25-30 mg/kg (up to 2 g) once daily.
– Pediatric dose: 15-30 mg/kg (up to 2 g) once daily.
4. Ethambutol (EMB):
– Adult dose: 15-25 mg/kg (up to 2.5 g) once daily.
– Pediatric dose: 15-25 mg/kg (up to 2.5 g) once daily.
Indications of Anti-tubercular drugs
Anti-tubercular drugs are indicated for the treatment of tuberculosis in various forms, including pulmonary and extrapulmonary TB. They are used in the following situations:
1. Active Tuberculosis:
– Anti-tubercular drugs are the primary treatment for active TB infection, aiming to eradicate the bacteria and prevent disease progression.
2. Latent Tuberculosis Infection (LTBI):
– In some cases, individuals with latent TB infection may be prescribed isoniazid or other medications to prevent the development of active TB disease.
3. Drug-Resistant Tuberculosis:
– Second-line anti-tubercular drugs are used to treat drug-resistant strains of tuberculosis, including multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB).
Contraindications of Anti-tubercular drugs
While anti-tubercular drugs are generally safe and effective, there are certain situations where their use may be contraindicated. Contraindications may include:
1. Drug Allergies:
– Individuals with a known allergy or hypersensitivity to any anti-tubercular drug should avoid using that specific medication.
2. Liver Disease:
– Some anti-tubercular drugs, such as isoniazid and rifampicin, can cause hepatotoxicity (liver damage). These drugs may be contraindicated or require close monitoring in patients with pre-existing liver disease or elevated liver enzymes.
3. Pregnancy and Breastfeeding:
– Certain anti-tubercular drugs may pose risks to pregnant or breastfeeding women and their infants. The decision to use these medications during pregnancy or breastfeeding should be carefully weighed against the risks of untreated tuberculosis.
4. Drug Interactions:
– Anti-tubercular drugs can interact with other medications, potentially reducing their effectiveness or increasing the risk of adverse effects. Healthcare professionals should review the patient’s medication list for potential drug interactions before prescribing anti-tubercular therapy.
5. Neurological Disorders:
– Some anti-tubercular drugs, such as ethambutol, can cause optic neuritis and other neurological side effects. These drugs may be contraindicated or require cautious use in patients with pre-existing neurological disorders.
It’s crucial for healthcare professionals to carefully assess each patient’s medical history and individual risk factors before initiating anti-tubercular therapy. Additionally, patients should be educated about the importance of adherence to treatment and monitored regularly for drug efficacy and potential adverse effects.
