Pentamidine: Effects, Uses & Risks

Pentamidine is an active substance that is used, among other things, for the treatment of the so-called West African trypanosomiasis, which is also called sleeping sickness. Pentamidine can lead to very severe side effects, which is why the drug should always remain ultima ratio.

What is pentamidine?

The drug pentamidine is used in human medicine to treat West African trypanosomiasis (West African sleeping sickness) and certain diseases caused by Pneumocystis jirovecii. Due to its chemical and pharmacological properties, the drug is called an antiprotozoal. This refers to active substances used to fight infections when the cause of the infection can be traced to a single pathogen (protozoa). Pentamidine was deliberately and specifically developed in England in the early 1930s to combat West African trypanosomiasis. In chemistry, pentamidine is described by the molecular formula C 19 – H 24 – N 4 – O 2 , which corresponds to a moral mass of 340.422 g/mol. It is sold under the trade name pentacarinate. Strict pharmacy and prescription requirements apply.

Pharmacological effects on body and organs

Pentamidine attacks the metabolism of the targeted pathogens at various points. Efficacy exists against Pneumocystis jirovecii as well as the causative agent of West African flapping disease, which the agent was specifically developed to combat. The action of pentamidine is considered parasitic. The drug effectively and sustainably kills pathogens.

Medical application and use for treatment and prevention.

Pentamidine can be used against several pathogens of the protozoan group. Therefore, the medicinal use of pentamidine extends to the treatment of sleeping sickness as well as the control of Pneumocystis jirovecii. These fungi originate from the Pneumocystis genus and are considered to be the causative agent of particularly severe pneumonia, which occurs primarily in immunocompromised individuals (e.g., AIDS patients) or infants. There is also an indication in case of diagnosed leishmaniasis. This is a subtropical infectious disease. Pentamidine is mainly used as isethionate. For the treatment of sleeping sickness and leishmaniasis, however, the active substance is usually administered parenterally, i.e. bypassing the intestine. Injections and infusions are considered. Patients who have AIDS and consequently suffer from severe pneumonia usually receive pentamidine by inhalation. The reason for this is that the likelihood of side effects occurring, as well as their intensity, can be reduced by inhalation. Since pentamidine can have very strong and in some cases dangerous side effects, the active ingredient always represents the last available remedy in a therapy. The drug is thus considered ultima ratio. This results in a strict pharmacy and prescription requirement. The active ingredient may only be dispensed to patients after prior prescription. Medical supervision is indicated for the duration of use. This is usually ensured by infusions and injections being administered by healthcare professionals and inhalation being performed only under appropriate supervision.

Risks and side effects

Taking pentamidine can lead to very severe side effects that may cause long-term damage. For example, glucose metabolism disorders occur in approximately 10% of those treated (and are thus very common). These are accompanied by acute reductions in blood glucose levels (hypoglycemia), which can lead to diabetes mellitus. Likewise, electrolyte imbalances, some of which can be life-threatening, may develop, which are manifested primarily in a high concentration of potassium (hyperkalemia). When administered by injection, severe pain at the injection site is common. In addition, acute renal dysfunction is possible. In addition, gastrointestinal complaints, especially nausea, diarrhea, vomiting, stomach cramps and stomach pain, and constipation have been reported in the literature. Skin reactions such as itching, redness, and burning are also possible. Other side effects include headache and a general feeling of malaise.In extreme cases, a severe drop in blood pressure (hypotension) and a QT syndrome may occur after taking pentamidine. Use must be discontinued altogether if intolerance is present.