Abstract
Pentamidine has a long history in the treatment of human African trypanosomiasis (HAT) and leishmaniasis. Early guidelines on the dosage of pentamidine were based on the base-moiety of the two different formulations available. Confusion on the dosage of pentamidine arose from a different labelling of the two available products, either based on the salt or base moiety available in the preparation. We provide an overview of the various guidelines concerning HAT and leishmaniasis over the past decades and show the confusion in the calculation of the dosage of pentamidine in these guidelines and the subsequent published reports on clinical trials and reviews. At present, only pentamidine isethionate is available, but the advised dosage for HAT and leishmaniasis is (historically) based on the amount of pentamidine base. In the treatment of leishmaniasis this is probably resulting in a subtherapeutic treatment. There is thus a need for a new, more transparent and concise guideline concerning the dosage of pentamidine, at least in the treatment of HAT and leishmaniasis.
Highlights
Pentamidine has a long history in the treatment of human African trypanosomiasis (HAT) and leishmaniasis
Pentamidine (Figure 1) proved to be the most useful, and since the early 1940s it has been used in the treatment and prophylaxis of human African trypanosomiasis (HAT, known as sleeping sickness) and to some extent in the treatment of visceral leishmaniasis in India
Pentamidine is mainly used for prophylaxis and treatment of Pneumocystis jirovecii pneumonia (PCP), and in the treatment of first-stage HAT and of several forms of American cutaneous leishmaniasis
Summary
The finding of the antiprotozoal activity of the diamidine family of drugs was largely a matter of serendipity They were discovered during a search for hypoglycaemic compounds that could affect trypanosomes. Two galenic formulations, both lyophilized salts of pentamidine (see Box 1), were available, one the 2-hydroxyethanesulfonic acid salt, called pentamidine isethionate (Pentacarinat or Pentam), the other the methanesulfonic acid salt, called pentamidine methanesulfonate or mesylate (Lomidine). These two preparations were used interchangeably, depending on local availability and preference, until the early 1990s when production of pentamidine methanesulfonate was stopped and only pentamidine isethionate remained
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