Products
Miltefosine is commercially available as an oral solution (milteforan). It is approved exclusively as a veterinary drug in many countries and has been since 2010. In other countries, miltefosine is also used for human use. In Germany, for example, it is available in capsule form (Impavido) for the treatment of leishmaniasis in humans and as a solution (Miltex) for malignant skin lesions in breast cancer.
Structure and properties
Miltefosine (C21H46NO4P, Mr = 407.6 g/mol) is a synthetic alkyl phospholipid. It is an analog of phosphatidylcholine (lecithin), the major component of cell membranes.
Effects
Miltefosine (ATCvet QP51D) is antiprotozoal, antiproliferative, antitumoral, and immunostimulant. It is effective against Leishmania, for example . These are transmitted by sand fly females. After treatment, there is a rapid improvement in clinical symptoms and strong reduction in the amount of pathogens. However, the parasites are not completely eliminated by miltefosine. Miltefosine has a very long elimination half-life of 6 to 7 days. As a result, the risk of resistance development is high.
Mechanism of action
Miltefosine has direct antiparasitic activity. The effect is based on the disruption of signal transduction and phospholipid metabolism in the cell membrane of Leishmania, which has effects on cell membrane synthesis as well as membrane integrity and eventually leads to cell death. At the same time, it increases the activation of T cells and macrophages, as well as the production of microbicidal nitrogen and oxygen intermediates. In addition, miltefosine inhibits the penetration of leishmania into macrophages, thereby impairing the multiplication and dissemination of the pathogens.
Indications
For the treatment and control of leishmaniasis in dogs.
Dosage
According to the SmPC. Miltefosine is administered orally once daily for 28 days each. It should always be mixed with food and not given on an empty stomach to avoid adverse effects.
Contraindications
Miltefosine is contraindicated in hypersensitivity, during pregnancy and lactation. It should not be given to breeding animals. Care should be taken to prevent freshly treated dogs from licking people. The user is advised to wear gloves and, if necessary, protective goggles while handling miltefosine because the skin and eyes may become irritated. Pregnant women should not administer the drug. For complete precautions, see the drug label.
Interactions
No interactions with other medicines are known to date.
Adverse effects
Possible adverse effects include digestive symptoms such as vomiting, nausea, loss of appetite, diarrhea, and also fatigue, weakness, malaise, and decrease in white and red blood cells. The digestive complaints occur less frequently when miltefosine is given with feed.
