Stibanate

Sodium Stibogluconate (0.33gm)
Price: ₹250 - ₹400 per vial
Mfr: Albert David Ltd. | Form: Injection (Powder for solution)

📋 Clinical Overview

Sodium Stibogluconate is a pentavalent antimonial compound and a first-line drug for the treatment of visceral leishmaniasis (kala-azar) and cutaneous leishmaniasis in India. It is a prodrug that is reduced to the active trivalent antimonial (SbIII) form within the macrophage, targeting the amastigote form of Leishmania parasites. It is administered parenterally, typically by slow intravenous or intramuscular injection.

💊 Dosage & Administration

Adult: 20 mg of antimony (SbV) per kg body weight per day, up to a maximum of 850 mg, administered IV/IM daily for 20-30 days. The 0.33gm vial typically contains 100 mg of antimony (Sb). Therefore, dose = (Patient weight in kg * 20) / 100 = number of vials per day. Example: 50 kg patient requires (50*20)/100 = 10 vials (3.3gm total) per day.

Note: For IV use: Dilute the calculated dose in 50-100 mL of 5% Dextrose Injection. Administer by slow IV infusion over 10-15 minutes. For IM use: Administer by deep intramuscular injection into the gluteal region. Rotate injection sites daily. IM route is more painful and can cause sterile abscesses. Patient should remain supine during and for 30-60 minutes after IV administration to monitor for anaphylaxis/cardiac events.

⚠️ Contraindications

  • Known hypersensitivity to antimonials
  • Severe myocardial disease (e.g., myocarditis, congestive heart failure)
  • Significant renal impairment (Creatinine clearance <30 mL/min) without dialysis
  • Pregnancy (first trimester - relative, but often considered absolute due to toxicity risk)
  • Concurrent administration with drugs that prolong QT interval (e.g., antiarrhythmics, certain antipsychotics, macrolides)

🔬 Mechanism of Action

Sodium stibogluconate is a prodrug. After phagocytosis by macrophages, the pentavalent antimony (SbV) is reduced to the more toxic and active trivalent antimony (SbIII) form. SbIII interferes with the parasite's trypanothione reductase system and inhibits glycolysis and fatty acid beta-oxidation by forming stable complexes with thiol groups in key enzymes, leading to disruption of energy metabolism and macromolecular synthesis in the amastigote form of Leishmania.

🤕 Side Effects

  • Pain, tenderness, and sterile abscess at IM injection site
  • Nausea, vomiting, anorexia
  • Myalgia, arthralgia
  • Headache, lethargy
  • Elevated liver enzymes (transaminitis)
  • ECG changes (T-wave flattening/inversion)

🤰 Special Populations

Pregnancy: Category D: Positive evidence of human fetal risk. Should be avoided, especially in the first trimester. Use only if the potential benefit justifies the potential risk to the fetus (e.g., life-threatening visceral leishmaniasis). Liposomal amphotericin B is the preferred agent in pregnancy.

Driving: May cause dizziness, lethargy, or syncope (due to arrhythmia). Patients should be cautioned against driving or operating heavy machinery during treatment.

🔄 Drug Interactions

Other QT-prolonging drugs (e.g., Amiodarone, Sotalol, Quinidine, Chloroquine)Additive risk of life-threatening ventricular arrhythmiasContraindicated
Macrolide antibiotics (e.g., Azithromycin, Erythromycin)Increased risk of QTc prolongation and cardiotoxicityMajor
Fluoroquinolones (e.g., Levofloxacin, Moxifloxacin)Increased risk of QTc prolongationMajor
Tricyclic Antidepressants (e.g., Amitriptyline)Increased risk of QTc prolongationMajor
Amphotericin BIncreased risk of renal toxicity and electrolyte imbalances (hypokalemia, hypomagnesemia) which can exacerbate cardiotoxicityMajor
Diuretics (especially loop and thiazide)Risk of hypokalemia and hypomagnesemia, potentiating cardiotoxicityMajor

🔁 Alternatives to Stibanate

Same composition (Sodium Stibogluconate (0.33gm)), different brands:

Sod. Stibogluconate I.P. (Generic) Pentostam (Historical/Reference Brand)