pentamidine; 4,4' diamidinophenoxy pentane (Pentam 300, Nebupent)
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Introduction
Tradename: Pentam-300. 4,4' diamidinophenoxy pentane. Pentamidine isethionate (Pentam 300, Nebupent)
Indications
- treatment of early African trypanosomiasis (ineffective if CNS involved)
- leishmaniasis, cutaneous & visceral.
- treatment of Pneumocystis pneumonia
- prophylaxis for Pneumocystis carinii
Dosage
Nebulized: Tradename NebuPent.
Injection: 300 mg vial
Dosage adjustment in renal failure
Table
| creatinine clearance | dosage |
|---|---|
| > 50-90 mL/min | every 24 hours |
| 10-50 mL/min | every 24 hours |
| < 10 mL/min | every 24-36 hours |
Pharmacokinetics
Caution: Although < 5% of pentamidine is renally excreted, the 1/2life is prolonged in dialysis patients, with a terminal 1/2life after multiple doses as long as 10-15 days.
elimination via liver
elimination via kidney
1/2life = 6.4-9.4 hours
1/2life = 26-32 hours
1/2life = 10-15 days renal failure
Monitor
- liver function tests (serum AST, serum ALT, serum bilirubin, serum alkaline phosphatase) before, during, & after treatment[9]
Adverse effects
- common (> 10%)
- chest pain, rash, wheezing, dyspnea, coughing, pharyngitis, hyperkalemia, local reaction at site of injection, acute renal failure[2]
- less common (1-10%)
- bitter or metallic taste
- uncommon (< 1%)
- extrapulmonary pneumocystis, pancreatitis, pneumothorax, hyperglycemia, hypoglycemia, renal insufficiency, hypotension, tachycardia, dizziness, fever, Jarisch-Herxheimer-like reaction, hypocalcemia, vomiting, megaloblastic anemia, granulocytopenia, leukopenia, thrombocytopenia, mild renal or hepatic injury, airway irritation, fatigue
- other[2]
- directly toxic to pancreatic islet cells
- hyperkalemia - inhibits tubular excretion of K+
- nebulized pentamidine
- chest pain
- bronchospasm
- cough
- bitter taste
Drug interactions
- foscarnet in combination increases risk of hypoglycemia & nephrotoxicity
Laboratory
- specimen:
- serum, plasma; stable at -20 degrees C for 6 days
- whole blood, urine
- methods:
Mechanism of action
- inhibits dihydrofolate reductase
- interferes with DNA/RNA, phospholipid & protein synthesis
- complete mechanism of action is unclear
More general terms
References
- ↑ Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1990, pg 1011-3
- ↑ 2.0 2.1 2.2 The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, 1190
- ↑ Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 625
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ 9.0 9.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com