Pentamidine diisethionate
Definition
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Half-life
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Pharmacodynamics (Effect)
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Pentamidine is an aromatic diamine with the following effects in Leishmania: inhibition of dihydrofolate reductase, inhibition of RNA and protein synthesis.
Spectrum of action
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Indication
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Prophylaxis of Pneumocystis carinii pneumonia in HIV patients with < 200 CD4 cells/μl, African tryposomiasis (African sleeping sickness caused by Trypanosoma brucei gambiense and Trypanosoma brucei rhodiense), leishmaniasis.
Dosage and method of use
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Visceral leishmaniasis not responding 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 every 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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Interactions
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Contraindication
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Preparations
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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 ↑ |