Antitubercular pyrazinamide

Older adults are particularly susceptible to a potentially fatal hepatitis when taking isoniazd, especially if they consume alcohol on a regular basis. Two other antitubercular drugs rifampin and pyrazinamide, can cause liver dysfunction in the older adult. Careful observation and monitoring for signs of liver impairment are necessary (eg, increased serum aspartate transaminase, increased serum alanine transferase, increased serum bilirubin, and jaundice). 

Fig. 5.17 Antitubercular compounds (see text also for details of antibiotics) A, PAS B, isoniazid C, ethionamide D, pyrazinamide E, prothionamide F, thiaeetazone G, ethambutol.

Ethambutol has replaced aminosalicylic acid as a first-line antitubercular drug. It is commonly included as a fourth drug, along with isoifiazid, pyrazinamide, and rifampin, in patients infected with MDR strains. It also is used in combination in the treatment of M. avium-intracellulare infection in AIDS patients. 

Fixed dose combination of pyrazinamide with other antitubercular drugs except combination of pyrazinamide with rifampicin and INH as per recommended daily dose given below ... 

HPI KC is a 50-year-old Mexican man who presents to the clinic with upper right quadrant pain and darkMycobacterium tuberculosis (MTB). He has no other significant PMH. Medications Rifampin, isoniazid, ethambutol, and pyrazinamide. 

Answer B. Pancreatic dysfunction, heralded by large increases in serum amylase and lipase, is associated with the use of several reverse-transcriptase inhibitors (RTIs). Didanosine appears to be the worst offender, and pancreatitis is the most characteristic adverse effect of this particular NRTI. Conditions enhancing susceptibility to drug-induced pancreatic dysfunction include hypertriglyceridemia, hypercalcemia, and history of excessive ethanol use. Liver dysfunction including hepatitis may occur with the antitubercular drugs, isonia-zid, and pyrazinamide. Cholestasis is associated with the estolate form of erythromycin. 

Pyrazinamide is an antitubercular drug which as a side effect blocks the... 

Pyrazinamide- Pyrazinamide (XIII), a drug which has been used clinically as an antitubercular agent, is now being studied for its hypoglycemic... 

Many antitubercular drugs [9] such as isoniazid, pyrazinamide, ethionamide, and ethambutol are fragment like (Figure 25.3) and this gave us an opportunity to use them as daughters. 

Figure 25.3 Antitubercular agents small fragment-like molecules used as drugs (isoniazid, pyrazinamide, ethionamide, and ethambutoi) bedaquiline is recently approved for the treatment of multidrug-resistant TB PA824 and SQ109 are in clinical trial.

The solubility of the antitubercular drug, pyrazinamide, is directly proportional to the concentration of sodium p-aminosalicylate (sodium PAS) or sodium hydroxybenzoate in aqueous solution [305]. Thermal analysis has confirmed the complex formation between the drug and sodium PAS, but the authors [305] list the alternatives of complexation and normal increase in solubility in the presence of additive as the causes of solubilization. As the antituberculars are always used clinically in combination - sodium PAS is also an effective drug-this study may have some bearing on the efficacy of the combinations. It might be of interest for an investigation to be carried out on the solution properties of isoniazid, streptomycin, and sodium PAS mixtures, especially as streptomycin is thought to have some colloidal electrolyte properties of its own. 

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