Sodium stibogluconate

What is sodium stibogluconate?

Sodium stibogluconate is a medication used to treat cutaneous, visceral, and mucosal leishmaniasis, a parasitic infection transmitted by sand-fly bites. It is also known by its chemical name antimony D-gluconic acid, and the brand name Pentostam^®.

Sodium stibogluconate is also occasionally used to treat acute myeloid leukaemia.

Sodium stibogluconate is not approved by the US Food and Drugs Administration and is not available in New Zealand. It is most used in tropical countries.

How does sodium stibogluconate work?

Sodium stibogluconate belongs to the class of medicines known as the pentavalent antimonials. Its mechanism is unclear; it may act by binding to thiol groups (–SH) in the parasite and inhibiting the formation of adenosine triphosphate (ATP) and guanosine triphosphate [GTP].

Sodium stibogluconate is eliminated by the kidneys and has a half-life of 6 hours.

How is sodium stibogluconate used?

Sodium stibogluconate is usually administered by intravenous or intramuscular injection daily at a dose of 20 mg/kg/day (maximum 850 mg) for 21–28 days.

Intralesional injections may be used for a single lesion or a few small lesions of cutaneous leishmaniasis. Intralesional injections are not suitable for lesions on the nose, ears, fingers, eyelids, lips, or genitalia. The intradermal injections are preceded by local anaesthetic or cryotherapy. The dose is 0.1 mL/cm2 (ie, 0.2–5 mL in up to 4–5 sites) repeated every 3–7 days until healing occurs.

What are the side effects of sodium stibogluconate?

Side effects and risks from sodium stibogluconate can be significant and are more likely to occur in older patients. They include:

• Gastrointestinal tract symptoms (nausea and diarrhoea)
• Musculoskeletal complaints (myalgia and arthralgia)
• Fatigue
• Pancreatitis
• Liver damage
• Rarely, damage to the kidney or heart
• Bone marrow suppression.

Elevated serum amylase levels are seen very commonly with sodium stibogluconate administration and rapidly recover with cessation of treatment. Although symptoms are common, clinical pancreatitis is rarely severe, and fatal pancreatitis is extremely rare.

Acute hepatocellular damage and a loss of functional metabolic capacity of the liver is rapidly reversible on stopping treatment with sodium stibogluconate.

What monitoring should be done on the use of sodium stibogluconate?

The following tests should be undertaken before treatment and weekly during treatment with sodium stibogluconate.

• Complete blood cell count — use of sodium stibogluconate can cause transient thrombocytopenia and leucopenia.
• Liver function tests — check serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST); cease treatment if either ALT or AST is greater than 3–4 times the upper normal limit.
• Serum amylase and lipase — cease treatment if amylase is more than 5 times the upper limit or lipase is more than 12 times the normal upper limit.
• Renal function tests for serum urea and creatinine.
• Electrocardiogram — cease treatment if a T-wave inversion or prolonged QT interval occurs.

Adverse effects of intralesional injection of stibogluconate can include:

• Pain
• Local allergic reaction
• Pruritus
• Transient erythema
• Oedema.

What are the contraindications with sodium stibogluconate?

Contraindications to the use of sodium stibogluconate include:

• Cardiac disease, especially an arrhythmia
• Renal failure or severe liver disease
• Severe malnutrition
• Advanced human immunodeficiency virus (HIV) infection
• Previous allergic reaction to sodium stibogluconate
• Pregnancy.