Meglumine Antimoniate
1-Deoxy-1-methylamino-D-glucitol antimoniate
Also known as: Glucantime · meglumine antimonate · N-methylglucamine antimoniate · RP-2168 · antimony meglumine · Protostib · Antimoniate de meglumine
Reviewed by the VetSheet Veterinary TeamUpdated Apr 5, 2026Evidence-based veterinary reference
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Dosing by species
🌎 NA — North America🌍 EU — Europe
Dogs
| Indication | Dose | Route | Frequency | Duration | Region |
|---|---|---|---|---|---|
| Leishmaniasis (First line treatment) | 75-100 mg/kg SC once daily for 4-8 weeks, with allopurinol (10 mg/kg PO twice daily for at least 6-12 months. | SC | q24h | 4-8 weeks | 🌎 NA |
| Leishmaniasis | 100 mg/kg SC daily for 3-4 weeks; better results are obtained with longer durations (4-6 weeks) of treatment. Protocol with allopurinol may reduce relapse rates: meglumine antimoniate as above with allopurinol at 20-40 mg/kg PO daily for a minimum of 3 weeks. Followed with long-term treatment with allopurinol (alone) at 20-40 mg/kg PO daily or intermittently (one week treatment per month). | SC | q24h | 3-6 weeks | 🌎 NA |
| Leishmaniasis | 100 mg/kg/day SC until resolution; with allopurinol at 20 mg/kg PO q12h for 9 months. | SC | q24h | Until resolution | 🌎 NA |
| Leishmaniosis | 75-100 mg/kg | SC | q24h (or divided q12h) | 3-4 weeks | 🌍 EU |
- Leishmaniasis (First line treatment): Used in combination with allopurinol.
- Leishmaniasis: Longer duration (4-6 weeks) yields better results.
- Leishmaniasis: Used in combination with allopurinol.
- Leishmaniosis: Often used in combination with allopurinol (10 mg/kg PO q12h for 6-12 months).
Cats
| Indication | Dose | Route | Frequency | Duration | Region |
|---|---|---|---|---|---|
| Leishmaniosis (off-label) | 50 mg/kg | SC | q24h | 3-4 weeks | 🌍 EU |
- Leishmaniosis (off-label): Use with extreme caution; cats may be more sensitive to toxicity.
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Meglumine antimoniate is a pentavalent antimony compound primarily used for the treatment of canine leishmaniasis (caused by Leishmania infantum).
- Combination Therapy: It is frequently used in combination with allopurinol to achieve synergistic effects, improve clinical outcomes, and reduce the risk of antimonial drug resistance.
- Eradication: Complete eradication of Leishmania organisms is rarely achieved; the goal of therapy is clinical remission and reduction of parasite load.
- Availability: It is not commercially available or approved in the USA, but is widely used in Mediterranean and South American countries where leishmaniasis is endemic. In the US, it may be obtained via the CDC or legal importation for compassionate use.
Clinical Pearl: Because Leishmania amastigotes reside within host macrophages, the drug must penetrate these immune cells to exert its leishmanicidal effects. Treatment is typically prolonged and requires careful monitoring of renal function.
Mechanism of action
Meglumine antimoniate selectively inhibits leishmanial enzymes required for glycolytic and fatty acid oxidation → disruption of parasite bioenergetics → decreased ATP production → death of the organism.
- Synergy: When used with allopurinol (a leishmaniostatic agent that disrupts RNA synthesis), the combination provides synergistic efficacy and helps prevent the emergence of resistant strains.
- Mechanistic Pearl: While the exact mechanism remains partially elucidated, it is widely believed that pentavalent antimony (SbV) acts as a prodrug and is reduced to the more toxic and active trivalent antimony (SbIII) within the acidic environment of the macrophage phagolysosome, where the amastigotes reside.
Safety & warnings
Contraindications
- Previous hypersensitivity to meglumine antimoniate
- Severe renal, hepatic, or cardiac failure (relative contraindication; weigh risks vs. benefits)
- Severe renal impairment
- Hepatic failure
- Cardiac disease
Adverse effects
- Injection site reactions (cutaneous abscesses, cellulitis, pain)
- Lethargy
- Gastrointestinal effects (inappetence, vomiting)
- Transient increases in liver enzymes
- Nephrotoxicity (tubular damage, proximal tubule cell vacuolization, coagulative necrosis)
- Pain and swelling at the injection site
- Nephrotoxicity (proteinuria, elevated BUN/creatinine)
- Anorexia
- Hepatotoxicity (rare)
- Myalgia/arthralgia
Precautions
Extreme caution is advised in patients with pre-existing renal, hepatic, or cardiac insufficiency.
- Renal Impairment: Decreased renal function can lead to significant drug accumulation and an increased risk of severe toxicity. In dogs with severe renal failure (IRIS stages III-IV), correction of fluid and acid-base imbalances prior to treatment with allopurinol alone is recommended before considering antimonials.
- Hypersensitivity: Hypersensitivity reactions have been reported in humans; avoid in patients with known allergies to the drug.
- Pregnancy: Teratogenic effects (fetal resorptions, bone abnormalities) have been noted in animal models. Weigh risks versus benefits carefully.
Drug interactions
Meglumine antimoniate may prolong QT interval further with increased risk for arrhythmias
Increased risk of nephrotoxicity
Increased risk of nephrotoxicity
Monitoring
- Efficacy (PCR preferred)
- CBC (baseline and periodic)
- Liver enzymes (baseline and periodic)
- Renal function tests (serum creatinine, BUN) (baseline and periodic)
- Serum lipase and amylase (baseline and periodic)
- Urinalysis (baseline and periodic)
- Urinalysis (specifically for proteinuria/UPC ratio)
- BUN and Creatinine
- Liver enzymes (ALT, AST, ALP)
- Complete Blood Count (CBC)
- Clinical signs of injection site reactions
Pharmacokinetics
Half-life
Absorption
Systemic bioavailability is approximately 92% after subcutaneous or intramuscular injections in dogs.
Distribution
Highest tissue concentrations are found in the liver, spleen, and skin.
Metabolism
Pentavalent antimony is believed to undergo in vivo reduction to trivalent antimony, which is the more active leishmanicidal form.
Elimination
Rapidly excreted primarily via the kidneys; within 9 hours of dosing, 80% of the antimony is excreted in the urine.
Overdose
No specific overdose information is available. Depending on the dosage, a single massive overdose could potentially cause renal, hepatic, pancreatic, and hematologic toxicity.
Clinically, gastrointestinal effects (severe vomiting) and profound lethargy would be the most likely immediate outcomes.
Management: Observe the patient closely, provide supportive care (IV fluids to protect renal function), and contact an animal poison control center for further guidance.
Available products
Formulations
- Injection solution (1.5 g meglumine antimoniate / 5 mL, equivalent to 425 mg pentavalent antimony)
- Injectable: 300 mg/ml solution
Veterinary
- None approved in the USA. May be available via the CDC.
- Glucantime 300 mg/ml solution for injection
Human-labeled
- Glucantime® / Glucantim® solution containing 1.5 grams of meglumine antimoniate (425 mg pentavalent antimony) per 5 mL (Available in Europe, Brazil, Venezuela; None in the USA)
- Glucantime 1.5 g/5 ml solution for injection
Regulatory status
Approved in several EU countries (e.g., France, Spain, Italy) for canine leishmaniosis.
Available as POM-V.
No regulatory data for: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Storage & stability
Unless otherwise specified by the manufacturer, commercially available ampules should be stored below 40°C, preferably between 15°-30°C; protect from freezing.
Client information
Treatment for leishmaniasis requires a strong commitment. Here is what you need to know:
- Long and Costly Treatment: The treatment protocol is prolonged (often lasting months when combined with other oral medications) and the medication can be expensive.
- Management, Not a Cure: It is highly unlikely that this drug will completely eradicate the parasite from your dog's body. The goal is to put the disease into remission and give your dog a good quality of life. Relapses can occur.
- Injection Site Reactions: Because this medication is given by injection, your dog may develop soreness, swelling, or small abscesses at the injection sites.
- Watch for Side Effects: Monitor your dog closely for loss of appetite, vomiting, or extreme tiredness. If you notice these signs, contact your veterinarian immediately, as the drug can occasionally affect the kidneys or liver.
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.