异烟肼 (Isonarif, Isotamine, Isotamine B +2)

概览

Isoniazid is an antibiotic used to treat mycobacterial infections; most commonly use in combination with other antimycobacterial agents for the treatment of active or latent tuberculosis.

作用机制

Isoniazid is a prodrug and must be activated by bacterial catalase. Specficially, activation is associated with reduction of the mycobacterial ferric KatG catalase-peroxidase by hydrazine and reaction with oxygen to form an oxyferrous enzyme complex. Once activated, isoniazid inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall. At therapeutic levels isoniazid is bacteriocidal against actively growing intracellular and extracellular Mycobacterium tuberculosis organisms. Specifically isoniazid inhibits InhA, the enoyl reductase from Mycobacterium tuberculosis, by forming a covalent adduct with the NAD cofactor. It is the INH-NAD adduct that acts as a slow, tight-binding competitive inhibitor of InhA.

适应症

Isoniazid is used for the treatment of all forms of tuberculosis in which organisms are susceptible. It is also used in combination with rifampin and pyrazinamide.

• Active Tuberculosis
• Mycobacterium kansasii infection
• Late phase Tuberculosis