[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/) › Meglumine antimoniate

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

# Meglumine antimoniate

Injectable pentavalent antimonial, the mainstay for cutaneous leishmaniasis in Colombia; heart, pancreas and liver are watched.

Updated 2026-11-01

- Class: [Antileishmanials](https://durgical.com/en/pharmacology/classes/antileishmanials/)
- Enzyme: Leishmania trypanothione reductase (and the parasite's thiols)
- ATC code: P01CB01
- WHO Model List of Essential Medicines

Also called: Meglumine antimonate, N-methylglucamine antimoniate

✂**Leishmania trypanothione reductase (and the parasite's thiols)**Meglumine antimoniate

ⓘ The figure shows Leishmania infantum trypanothione reductase with trivalent antimony (Sb³⁺) bound, the active form the pentavalent antimonial turns into.

**Target in 3D:** Leishmania trypanothione reductase (and the parasite's thiols). PDB structure 2W0H (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/2W0H) · Drag to rotate · pinch to zoom

## Mechanism of action

Pentavalent antimony (Sb⁵⁺) is a prodrug: inside the macrophage and the amastigote it is reduced to the more toxic trivalent antimony (Sb³⁺). Sb³⁺ drives trypanothione and glutathione out of the parasite and inhibits trypanothione reductase, the enzyme that keeps its antioxidant defence working. Without reducing power the amastigote dies inside the phagolysosome.

- Sb⁵⁺ reaches the infected macrophage
- It is reduced to Sb³⁺, the active form
- Sb³⁺ drains thiols and inhibits trypanothione reductase
- The amastigote dies of oxidative stress

## Pharmacokinetics

**Absorption**
Not absorbed orally: given IM, IV or intralesionally

**Distribution**
Distributes quickly; antimony builds up in tissues and leaves slowly

**Elimination**
In urine

**Half-life**
Two phases: a short initial one of hours and a much longer terminal one

## Indications

- Cutaneous leishmaniasis (first-line systemic treatment in adults in Colombia) [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)
- Localised cutaneous leishmaniasis with few lesions: intralesional infiltration [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)
- Mucosal and disseminated leishmaniasis [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)
- Visceral leishmaniasis, as second line [Leishmaniasis →](https://durgical.com/en/conditions/leishmaniasis/)

## Adverse effects

### Common

- Muscle and joint pain
- Nausea, abdominal pain and other gut symptoms
- Fever, headache, weakness and malaise
- Skin rash
- Pain at the IM injection site and sterile abscesses
- Raised transaminases, amylase and lipase

### Serious (rare, important)

- Cardiotoxicity: T-wave changes, QT prolongation and dangerous arrhythmias if continued
- Chemical pancreatitis (raised pancreatic enzymes)
- Bone marrow depression
- Rare: haemolytic anaemia, severe kidney or liver damage, shock and sudden death

## Contraindications

- Pregnancy
- Electrocardiogram abnormalities
- Significant heart, kidney or liver disease (specialist assessment; local treatments or liposomal amphotericin B are preferred)
- Hypersensitivity to antimonials

## Key interactions

**Other QT-prolonging drugs**
Add to the risk of ventricular arrhythmias

**Concurrent tuberculosis treatment**
The Colombian guidance asks for close watch for adverse events from interactions

## What is monitored

- Electrocardiogram before and during treatment (over 45 years or with heart disease)
- Transaminases, amylase and lipase at mid-course and at the end
- Blood count, creatinine and urea
- Pregnancy test in women of childbearing age
- Body weight and ulcer size (measurements or photographs)

## Administration and safety

- IM or IV once daily; in Colombia it is supervised treatment.
- Intralesional infiltration is done by trained staff, like an intradermal or subcutaneous injection covering the whole ulcer.
- IM injection is painful and may leave sterile abscesses: rotate sites.
- Once the case is confirmed and treatment chosen, it is notified to SIVIGILA.

## Nursing care

- Before: ECG when indicated, baseline labs and pregnancy test.
- Ask about muscle, joint or abdominal pain (possible pancreatitis) and about palpitations or fainting.
- Weigh the patient: weight sets the dose and may change during treatment.
- Record how the ulcer evolves and the later follow-up visits (cure or failure).
- Adverse events are reported to INVIMA (pharmacovigilance).

## Pregnancy and breastfeeding

Not recommended in pregnancy; thermotherapy is used or treatment is postponed, and if urgent liposomal amphotericin B is used.

## Memory aid

Antimony = «A-P-C»: Aching joints and muscles, Pancreatic enzymes up, Cardiac long QT; ECG before the first ampoule.

## Test yourself

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

## What is the active form of meglumine antimoniate?

Trivalent antimony (Sb³⁺), formed when pentavalent antimony is reduced inside the macrophage and the amastigote.

## Which parasite enzyme does trivalent antimony inhibit?

Trypanothione reductase, which keeps Leishmania's antioxidant defence working.

## Which three organs or systems are watched during antimonial treatment?

The heart (ECG, QT), the pancreas (amylase and lipase) and the liver (transaminases), plus blood count and kidney function.

## What is done for a pregnant woman with cutaneous leishmaniasis?

Antimonials are not given: thermotherapy is used or treatment is postponed; if urgent, liposomal amphotericin B.

[Add to my cards (4)](https://durgical.app/estudiar/?add=/en/pharmacology/meglumine-antimoniate/)

## Related drugs

- [Miltefosine](https://durgical.com/en/pharmacology/miltefosine/)

## 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: [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); [Clinical Care of Leishmaniasis](https://www.cdc.gov/leishmaniasis/hcp/clinical-care/index.html) (Centers for Disease Control and Prevention (CDC), 2024); Farmacología básica y clínica (Katzung), cap. 52 (McGraw Hill, 2025); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 67 (McGraw Hill, 2023).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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