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Pentamidine

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Pentamidine, Pentam, NebuPent, Nebulized Pentamidine, Aerosolized Pentamidine

  • See Also
  1. Pneumocystis Prophylaxis
  2. Pneumocystis jiroveci Pneumonia
  1. Pneumocystis Prophylaxis
  2. Pneumocystis jiroveci Pneumonia
  • 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)
  • 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
  • Efficacy
  1. Pneumocystis Prophylaxis
    1. Reduces the risk of PCP by 60 to 80% in patients with AIDS
  • 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
  • Adverse Effects
  • Nebulized Pentamidine
  1. Well tolerated
  2. Cough and bronchospasm in 50% of patients
  • Safety
  1. Pregnancy category C
  2. Avoid in Lactation
  • 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
  • Resources
  1. Pentam 300 (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cc2b635e-4840-4dc3-a177-5484371680e8
  2. Pentamidine Isethionate inhalant or NebuPent (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c484f16e-9d97-4416-84a4-8ad8deaf5e19
  • References
  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia