II. Indications: Human Immunodeficiency Virus (HIV)

III. Mechanism

  1. Synthetic derivative of amidine
    1. Binds AT-rich regions of duplex DNA (as well as minor groove of DNA)
    2. Inhibits DNA Replication
  2. Activity
    1. Antiprotozoal (e.g. trypanosomiasis, Leishmaniasis)
    2. Antifungal (Pneumocystis jirovecii)

IV. Dosing

  1. Pneumocystis Prophylaxis (adults, and off label use in age >5 years)
    1. Nebulized Pentamidine (NebuPent) 300 mg every 4 weeks
  2. Pneumocystis jiroveci Pneumonia (adults and children)
    1. Give 4 mg/kg IM or IV infused over 60 to 90 minutes daily for 21 days
    2. Risk of serious, life-threatening adverse effects, especially with IV use

V. Efficacy

  1. Pneumocystis Prophylaxis
    1. Reduces the risk of PCP by 60 to 80% in patients with AIDS

VI. Adverse Effects: IV or IM

  1. Severe Hypotension
  2. Cardiac Arrhythmias (including Torsades de Pointes)
  3. Neutropenia (15%)
  4. Thrombocytopenia
  5. Hypocalcemia
  6. Nephrotoxicity and Renal Insufficiency
  7. Hepatitis
  8. Pancreatitis
  9. Dysglycemia (20% treated for 3 weeks)
    1. Pentamidine causes pancreatic islet cell toxicity
    2. Hypoglycemia
    3. Hyperglycemia
  10. Gastrointestinal Upset (Nausea or Vomiting)
  11. Rash

VII. Adverse Effects: Nebulized Pentamidine

  1. Well tolerated
  2. Cough and bronchospasm in 50% of patients

VIII. Safety

  1. Pregnancy category C
  2. Avoid in Lactation

IX. Monitoring

  1. Electrocardiogram (EKG)
    1. Telemetry during infusion
  2. Comprehensive metabolic panel
    1. Liver Function Tests
    2. Renal Function tests
    3. Serum Calcium
    4. Blood Glucose

XI. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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