II. Indications

  1. Active Tuberculosis
  2. Latent Tuberculosis (no longer recommended due to hepatotoxicity risk)
    1. Previously used in combination with Rifampin for Latent Tb

III. Mechanism

  1. Pyrazinamide is a prodrug that is metabolized into the active pyrazinoic acid via Bacterial pyrazinamidase enzyme
  2. Synthetic pyrazinoic acid amide derivative that is bactericidal against intracellular bacilli

IV. Dosing: Active Tuberculosis

  1. Used as part of multi-drug Active Tuberculosis Treatment regimen
  2. Child: 15 to 30 mg/kg (up to 2000 mg) orally daily
  3. Adult: 20 to 25 mg/kg orally daily based on estimated Lean Body Mass
    1. Weight 40 to 55 kg: Give 1000 mg orally daily
    2. Weight 56 to 75 kg: Give 1500 mg orally daily
    3. Weight 76 to 90 kg: Give 2000 mg orally daily
    4. Weight >90 kg: Give 2000 mg orally daily and consider monitoring serum drug levels for adequate dosing
    5. Maximum Dose: 2000 mg

V. Adverse Effects

  1. Drug-Induced Hepatitis or Hepatotoxicity
  2. Gastrointestinal upset
  3. Transient Morbiliform Rash
  4. Arthralgias (unrelated to gout)
  5. Hyperuricemia (or Acute Gout)

VI. Safety

  1. Pregnancy Category C
  2. Considered safe in Lactation

VII. Monitoring

  1. Baseline
    1. Liver Function Tests (LFT)
    2. Serum Creatinine
      1. Consider reducing dose in renal dysfunction
  2. Periodic LFT testing
    1. Liver Function Tests repeated 1-2 times monthly if risks for hepatotoxicity
      1. Stop if LFTs >3x baseline if sympomatic (>5x baseline if asymptomatic)
    2. Indications for Liver Function Test monitoring
      1. Abnormal baseline Liver Function Test
      2. History suggestive of Possible liver disorder
      3. Human Immunodeficiency Virus (HIV)
      4. Pregnancy
      5. Postpartum (within 3 months)
      6. Chronic Liver Disease
        1. Viral Hepatitis (Hepatitis B or Hepatitis C)
        2. Alcoholic Hepatitis
        3. Cirrhosis
  3. Other testing
    1. Serum Uric Acid if symptoms related to gout

IX. References

  1. (2019) Presc Lett, Resource #350309, Tuberculosis Treatment in Adults: FAQ
  2. (2012) Med Lett Drugs Ther 10(116): 29-36

Images: Related links to external sites (from Bing)

Related Studies

Cost: Medications

pyrazinamide (on 10/19/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
PYRAZINAMIDE 500 MG TABLET Generic $2.83 each

Ontology: Pyrazinamide (C0034239)

Definition (NCI) A synthetic pyrazinoic acid amide derivative with bactericidal property. Pyrazinamide is particularly active against slowly multiplying intracellular bacilli (unaffected by other drugs) by an unknown mechanism of action. Its bactericidal action is dependent upon the presence of bacterial pyrazinamidase, which removes the amide group to produce active pyrazinoic acid. Pyrazinamide is an important component of multidrug therapy for tuberculosis. (NCI04)
Definition (MSH) A pyrazine that is used therapeutically as an antitubercular agent.
Definition (CSP) antibacterial derived from nicotinic acid, used as a tuberculostatic.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D011718
SnomedCT 13592004, 387076005
LNC LP15007-5, MTHU001493
English Pyrazinamide, Pyrazinecarboxamide, pyrazinamide, pyrazinamide (medication), Pyrazinamide [Chemical/Ingredient], PYRAZINAMIDE, Pyrazinoic acid amide, Pyrazinamide (product), Pyrazinamide (substance)
Swedish Pyrazinamid
Czech pyrazinamid
Finnish Pyratsiiniamidi
Russian PIRAZINAMID, ПИРАЗИНАМИД
Japanese ピラジナミド
Spanish Pirazinamida, Piracinamida, amida de ácido pirazinoico, pirazinamida (producto), pirazinamida (sustancia), pirazinamida
Polish Pirazynamid
French Pyrazinamide
German Pyrazinamid
Italian Pirazinamide
Portuguese Pirazinamida