Pentamidine isetionate (Pentacarinat)

Pentamidine isetionate (Pentacarinat) is an approved anti-fungal and anti-protozoal drug used for the treatment and prevention of Pneumocystis pneumonia (PCP). It can be administered by either intravenous or intramuscular injection, or converted into a mist by a machine called a nebuliser then inhaled into the lungs.

Intravenous pentamidine is the standard treatment for PCP. Aerosolised pentamidine is used as a form of prophylaxis against PCP in people with CD4 counts below 200 cells/mm3 or who have had a prior episode of PCP: this usually consists of one treatment a month. However, daily use of inhaled pentamidine can also be used to treat PCP.

Aerosolised pentamidine is well tolerated, for years if necessary, but some people may experience coughs and spasm of the lungs.1 2 This is usually preventable by pre-treatment with inhaled beta-adrenergic blockers.3 If people who are taking aerosolised pentamidine do develop PCP, it can be harder to diagnose because the Pneumocystis organisms may not be detectable in samples of spit or fluid from the lungs, and chest X-rays may be unusual.4 5 Unusual forms of Pneumocystis infection may occur outside the lungs, where the inhaled drug does not provide any protection.6 In a few cases, the drug has been associated with collapsed lung.7 8

Pentamidine is equivalent to cotrimoxazole (Septrin) in preventing PCP, except among people with CD4 counts below 100 cells/mm3. In people unable to tolerate co-trimoxazole, aerosolised pentamidine has been found as effective as atovaquone (Wellvone) in preventing PCP, and is associated with fewer side-effects.9

The effectiveness of aerosolised pentamidine as prophylaxis seems to be significantly dependent on the size of the aerosol particles generated by the nebulising machine, as finer particles penetrate deeper into the lungs than large particles. The position of the patient’s body while inhaling the drug and breathing pattern also affect its effectiveness.10 11

Side-effects of intravenous or intramuscular pentamidine include kidney damage, low blood sugar, inflammation of the pancreas, blood abnormalities and alterations of the heart rhythm.12 13 Because of the elevated risk of kidney damage, the nucleotide reverse transcriptase inhibitor (NtRTI) tenofovir (Viread) should be co-administered with pentamidine with caution. There is also a risk that long-term aerosolised pentamidine can affect blood sugar and insulin levels, and may cause diabetes, although evidence is inconclusive.14

Although pentamidine inhibits Cryptococcus in the test tube, there is no evidence that aerosolised pentamidine prevents cryptococcal meningitis. However, intravenous pentamidine may be useful in treating and preventing relapses of cutaneous leishmaniasis in HIV-positive patients.15

Pentamidine does not have any significant interactions with currently available protease inhibitors or non-nucleoside reverse transcriptase inhibitors (NNRTIs).

Pentamidine for intravenous or intramuscular use is marketed under the tradename Pentam. For aerosolised use, it is marketed as NebuPent.

References

  1. Obaji J et al. The pulmonary effects of long-term exposure to aerosol pentamidine: a 5-year surveillance study in HIV-infected patients. Chest 123: 1983-1987, 2003
  2. Katzman M et al. High incidence of bronchospasm with regular administration of aerosolized pentamidine. Chest 101: 79-81, 1992
  3. Harrison KS et al. Bronchodilator pre-treatment improves aerosol deposition uniformity in HIV-positive patients who cough while inhaling aerosolized pentamidine. Chest 106: 421-426, 1994
  4. Jules-Elysee KM et al. Aerosolized pentamidine: effect on diagnosis and presentation of Pneumocystis carinii pneumonia. Ann Intern Med 112: 750-757, 1990
  5. Levine SJ et al. Effect of aerosolized pentamidine prophylaxis on the diagnosis of Pneumocystis carinii pneumonia in patients infected with the human immunodeficiency virus. Am Rev Respir Dis 144: 760-764, 1991
  6. Conces DJ et al. Atypical Pneumocystis carinii pneumonia after inhaled pentamidine prophylaxis. Am J Roentgenol 152: 1193-1194, 1989
  7. Sepkowitz KA et al. Pneumothorax in AIDS. Ann Intern Med 114: 455-459, 1991
  8. Telzak EE et al. Extrapulmonary Pneumocystis carinii infection. Rev Infect Dis 12: 380-386, 1990
  9. Chan C et al. Atovaquone suspension compared with aerosolized pentamidine for prevention of pneumocystis carinii pneumonia in human immunodeficiency virus-infected subjects intolerant of trimethoprim or sulfonamides. J Infect Dis 180: 369-376, 1999
  10. Baskin MI et al. Regional deposition of aerosolised pentamidine: effects of body position and breathing pattern. Ann Int Med 113: 677-683, 1990
  11. O'Doherty MJ et al. Does inhalation of pentamidine in the supine position increase deposition in the upper part of the lung? Chest 97: 1343-1346, 1990
  12. Girgis I et al. A prospective study of the effect of I. V. pentamidine therapy on ventricular arrhythmias and QTc prolongation in HIV-infected patients. Chest 112: 646-653, 1997
  13. Eisenhauer MD et al. Incidence of cardiac arrhythmias during intravenous pentamidine therapy in HIV-infected patients. Chest 105: 389-395, 1994
  14. Uzzan B et al. Effects of aerosolized pentamidine on glucose homeostasis and insulin secretion in HIV-positive patients: a controlled study. AIDS 9: 901-907, 1995
  15. Calza L et al. Pentamidine isethionate as treatment and secondary prophylaxis for disseminated cutaneous leishmaniasis during HIV infection: case report. J Chemother 13: 653-657, 2001

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This content was checked for accuracy at the time it was written. It may have been superseded by more recent developments. NAM recommends checking whether this is the most current information when making decisions that may affect your health.

NAM’s information is intended to support, rather than replace, consultation with a healthcare professional. Talk to your doctor or another member of your healthcare team for advice tailored to your situation.