II. Indications: Human Immunodeficiency Virus (HIV)
III. Mechanism
- Synthetic derivative of amidine
- Binds AT-rich regions of duplex DNA (as well as minor groove of DNA)
- Inhibits DNA Replication
- Activity
- Antiprotozoal (e.g. trypanosomiasis, Leishmaniasis)
- Antifungal (Pneumocystis jirovecii)
IV. Dosing
-
Pneumocystis Prophylaxis (adults, and off label use in age >5 years)
- Nebulized Pentamidine (NebuPent) 300 mg every 4 weeks
-
Pneumocystis jiroveci Pneumonia (adults and children)
- Give 4 mg/kg IM or IV infused over 60 to 90 minutes daily for 21 days
- Risk of serious, life-threatening adverse effects, especially with IV use
V. Efficacy
-
Pneumocystis Prophylaxis
- Reduces the risk of PCP by 60 to 80% in patients with AIDS
VI. Adverse Effects: IV or IM
- Severe Hypotension
- Cardiac Arrhythmias (including Torsades de Pointes)
- Neutropenia (15%)
- Thrombocytopenia
- Hypocalcemia
- Nephrotoxicity and Renal Insufficiency
- Hepatitis
- Pancreatitis
- Dysglycemia (20% treated for 3 weeks)
- Pentamidine causes pancreatic islet cell toxicity
- Hypoglycemia
- Hyperglycemia
- Gastrointestinal Upset (Nausea or Vomiting)
- Rash
VII. Adverse Effects: Nebulized Pentamidine
- Well tolerated
- Cough and bronchospasm in 50% of patients
VIII. Safety
- Pregnancy category C
- Avoid in Lactation
IX. Monitoring
-
Electrocardiogram (EKG)
- Telemetry during infusion
- Comprehensive metabolic panel
X. Resources
- Pentam 300 (DailyMed)
- Pentamidine Isethionate inhalant or NebuPent (DailyMed)
XI. References
- Hamilton (2020) Tarascon Pocket Pharmacopoeia