Adult: 100-500 mg (as pentavalent antimony), every 3-7 days for 1-5 sessions.
Parenteral Visceral leishmaniasis
Adult: 20 mg/kg (as pentavalent antimony) daily for 30 days (28 days for L. infantum) via IM or slow IV injection over at least 5 minutes. Evaluate for evidence of relapse after 2 and 6 months (and after 12 months in Africa). Child: <10 kg: ≥200 mg daily.
Parenteral Cutaneous leishmaniasis
Adult: For lesions requiring systemic therapy: 20 mg/kg (as pentavalent antimony) daily for 10-20 days via IM or slow IV injection over at least 5 minutes. Child: Same as adult dose.
Parenteral Mucocutaneous infection caused by Leishmania
Adult: 20 mg/kg (as pentavalent antimony) for 30 days via IM or slow IV injection over at least 5 minutes. Child: Same as adult dose.
Renal Impairment
Significant impairment: Contraindicated.
Hepatic Impairment
Contraindicated.
Contraindications
Hepatic and significant renal impairment. Concomitant use of amphotericin B and other drugs that prolong QT interval.
Special Precautions
Patient with CV disease, history of ventricular arrhythmias, risk factors for QT prolongation (e.g. congenital QTc prolongation). Children. Pregnancy and lactation.
Adverse Reactions
Significant: Prolonged QT interval, anaemia, leucopenia, thrombocytopenia, cough, vomiting, substernal pain, arthralgia, myalgia, pancreatitis, elevated hepatic and pancreatic enzymes. Blood and lymphatic system disorders: Jaundice. Cardiac disorders: ECG changes (e.g. reduced T-wave amplitude, t-wave inversion). Gastrointestinal disorders: Abdominal pain, diarrhoea, nausea. General disorders and administration site conditions: Malaise, lethargy, fever; transient pain on injection site, venous thrombosis (IV). Metabolism and nutrition disorders: Anorexia. Musculoskeletal and connective tissue disorders: Rigor. Nervous system disorders: Headache, vertigo. Respiratory, thoracic and mediastinal disorders: Nasal or gum bleeding. Skin and subcutaneous tissue disorders: Rash, worsening of lesions on the cheek. Vascular disorders: Facial flushing. Potentially Fatal: Severe inflammation with pharyngeal or tracheal involvement, cardiac arrhythmia. Rarely, pneumonia, anaphylactic shock.
Monitoring Parameters
Monitor ECG before and during therapy; CBC and LFT periodically, serum creatinine, serum amylase.
Overdosage
Symptoms: Nausea, vomiting, diarrhoea, hepatitis, haemorrhagic nephritis. Management: Administer IM dimercaprol 200 mg 6 hourly until complete recovery. 2,3-dimercaptosuccinic acid (DMSA) may also be used.
Drug Interactions
Potentially Fatal: Increased risk of cardiac arrhythmia with amphotericin B; allow a 14-day resting period between sodium stibogluconate treatment and amphotericin B therapy initiation. Concurrent use with drugs that prolong QT interval (e.g. cisapride, astemizole, terfenadine) may increase the risk of torsade de pointes which may lead to ventricular arrhythmia.
Action
Description: Mechanism of Action: Sodium stibogluconate is a pentavalent antimony compound. Its mechanism of action is unknown. However, it has been suggested that the reduction in ATP and GTP (guanosine triphosphate) synthesis contributes to decreased macromolecular synthesis.
Synonym: sodium antimony gluconate. Pharmacokinetics: Absorption: Rapidly absorbed via IV and IM route. Excretion: Via urine (80%, as unchanged drug). Elimination half-life: Initial phase: Approx 2 hours. Terminal phase: Approx 33-76 hours.
Chemical Structure
Storage
Store at or below 25°C. Do not freeze. Protect from light.