[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Antileishmanials](https://durgical.com/en/pharmacology/classes/antileishmanials/) › Miltefosine

[Pharmacology](https://durgical.com/en/pharmacology/) · [Antileishmanials](https://durgical.com/en/pharmacology/classes/antileishmanials/)

# Miltefosine

The only oral antileishmanial: it treats cutaneous, mucosal and visceral leishmaniasis, but it is teratogenic and causes vomiting and diarrhoea.

Updated 2026-11-01

- Class: [Antileishmanials](https://durgical.com/en/pharmacology/classes/antileishmanials/)
- Target: Leishmania membrane lipids and signalling
- ATC code: P01CX04
- WHO Model List of Essential Medicines

## Mechanism of action

An alkylphosphocholine, a phospholipid analogue first developed as an anticancer drug. It enters the parasite through a phospholipid transporter (a P-type ATPase) and disturbs ether-lipid metabolism, cell signalling and the synthesis of membrane glycosylphosphatidylinositol anchors. The exact mechanism is not known; mutations in the transporter reduce drug uptake and cause resistance.

- Phospholipid analogue that enters through a parasite transporter
- Disturbs ether lipids and membrane anchors
- Amastigote cell signalling breaks down
- The parasite dies; transporter mutations give resistance

## Pharmacokinetics

**Absorption**
Well absorbed orally

**Distribution**
Wide, throughout the body

**Half-life**
Very long, weeks

## Indications

- Cutaneous leishmaniasis, including Viannia species (L. braziliensis, L. panamensis, L. guyanensis) [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)
- First line in children with cutaneous leishmaniasis above a set weight, in the Colombian guidance [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)
- Mucosal leishmaniasis [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)
- Visceral leishmaniasis and HIV coinfection (with antiretrovirals) [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)

## Adverse effects

### Common

- Vomiting and diarrhoea, very common
- Nausea, abdominal pain and loss of appetite
- Raised transaminases
- Raised creatinine

### Serious (rare, important)

- Teratogenicity and fetal death
- Dehydration from vomiting and diarrhoea
- Kidney toxicity
- Liver toxicity

## Contraindications

- Pregnancy
- Breastfeeding (during treatment and for months after)
- Hypersensitivity to miltefosine

## Key interactions

**Oral contraceptives**
Vomiting and diarrhoea can reduce their absorption; a non-hormonal method is added

## What is monitored

- Pregnancy test before starting
- Creatinine and urea
- Transaminases
- Hydration, weight and how the lesions evolve

## Administration and safety

- Oral only: it cannot be given IV because it is haemolytic.
- The course lasts several weeks and must be completed.
- Women of childbearing age use effective contraception during treatment and for months after.

## Nursing care

- Before: negative pregnancy test and a contraception plan.
- Watch for vomiting and diarrhoea, offer fluids and look for signs of dehydration.
- Check creatinine and transaminases as scheduled.
- Teaching: the teratogenic risk lasts months because of the long half-life; no breastfeeding during that time; finish the course.

## Pregnancy and breastfeeding

Contraindicated: teratogenic in animals; a negative pregnancy test and effective contraception during treatment and for months after are required.

## Memory aid

MILTefosine, the «leish pill»: Much vomiting, Interminable half-life, Lipid membranes, Teratogen.

## Test yourself

Think of the answer, then tap the question to see it.

## What advantage does miltefosine have over antimonials?

It is oral, so it avoids daily injections and lacks the cardiotoxicity of antimonials.

## Why must contraception continue for months after the last miltefosine dose?

Because its half-life is very long (weeks) and it is teratogenic.

## What are the most common adverse effects of miltefosine?

Vomiting and diarrhoea, plus nausea and raised transaminases and creatinine.

## Why is miltefosine not given IV?

Because it has haemolytic activity.

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## Related drugs

- [Meglumine antimoniate](https://durgical.com/en/pharmacology/meglumine-antimoniate/)

## Related conditions

- [Leishmaniasis](https://durgical.com/en/conditions/leishmaniasis/)

[← Back to the class: Antileishmanials](https://durgical.com/en/pharmacology/classes/antileishmanials/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Clinical Care of Leishmaniasis](https://www.cdc.gov/leishmaniasis/hcp/clinical-care/index.html) (Centers for Disease Control and Prevention (CDC), 2024); [Lineamientos de atención clínica integral para Leishmaniasis en Colombia](https://www.minsalud.gov.co/sites/rid/Lists/BibliotecaDigital/RIDE/VS/PP/PAI/Lineamientos-leishmaniasis.pdf) (Ministerio de Salud y Protección Social (Colombia), 2023); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 67 (McGraw Hill, 2023); Farmacología básica y clínica (Katzung), cap. 52 (McGraw Hill, 2025).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/miltefosine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/miltefosine/