Pentamidine diisethionate

Authors: Prof. Dr. med. Peter Altmeyer, Prof. Dr. med. Martina Bacharach-Buhles

All authors of this article

Last updated on: 29.10.2020

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Definition
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Chemotherapeutic agent, antiprotozoal.

Half-life
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Four days.

Pharmacodynamics (Effect)
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Inhibition of dihydrofolate reductase, inhibition of RNA and protein synthesis.

Spectrum of action
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Leishmania spp., Trypanosoma brucei gambiense (except cerebral stage), Pneumocystis carinii.

Indication
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Prophylaxis of Pneumocystis carinii pneumonia in HIV patients with < 200 CD4 cells/μl, African tryposomiasis, leishmaniasis .

Dosage and method of use
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  • Visceral leishmaniasis that does not respond to antimony compounds: 4 mg/kg bw/day for 2 weeks or 4 mg/kg bw 3 times/week (until parasites are no longer detected in 2 spleen biopsies 2 weeks apart).
  • Cutaneous leishmaniasis (L. aethiopica, L. guyanensis): 3-4 mg/kg bw 1-2 times/week until the ulcers have healed
  • Mucocutaneous leishmaniasis (L. brasiliensis, L. aethiopica): 4 mg/kg bw 3 times/week until the ulcers have healed, possibly for several months.
  • Diffuse cutaneous leishmaniasis (L. aethiopica): 3-4 mg/kg bw/day for months, at least another 4 months until the smears have become negative.
  • Trypanosoma brucei spp.: 5 mg/kg bw/day for the 2nd day, 10 cycles in total.
  • Pneumocystis carinii pneumonia:
    • Prophylaxis: 200 mg/day for 4 days by inhalation, then 300 mg every 28 days.
    • Therapy: 4 mg/kg bw/day i.v. (over 60 min.) for 14 days, then 300-600 mg/day.

Undesirable effects
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hypotension, hypertension, vomiting, kidney failure, hypo- and hyperglycaemia, pancreatic necrosis, BB changes, liver damage, shock, rarely Herxheimer's reaction, allergic reactions, contact eczema, erythroderma

Interactions
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See Table 2.

Contraindication
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Pregnancy, kidney dysfunction.

Preparations
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Pentacarinate

Tables
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Essential interactions of pentamidine diisethionate

amphotericin B

Nephrotoxicity ↑

Erythromycin

Cardiac arrhythmia

Foscarnet

Hypocalcemia, nephrotoxicity ↑

Ganciclovir

Haematotoxicity ↑

Zalcitabine

Pancreatitis ↑

Zidovudine

Haematotoxicity ↑