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Sodium stibogluconate

Author: Dr Heba Fawal, Department of Dermatology, Lattakia National Hospital, Lattakia, Syria. DermNet NZ Editor in Chief: Adjunct A/Prof Amanda Oakley, Dermatologist, Hamilton, New Zealand. Copy edited by Gus Mitchell. June 2020.


Sodium stibogluconate — codes and concepts
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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.

Leishmaniasis

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:

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.

New Zealand approved datasheets are the official source of information for prescription medicines, including approved uses and risk information. Check the individual New Zealand datasheet on the Medsafe website.

If you are not based in New Zealand, we suggest you refer to your national drug approval agency for further information about medicines (eg, the Australian Therapeutic Goods Administration and the US Food and Drug Administration) or a national or state-approved formulary (eg, the New Zealand Formulary and New Zealand Formulary for Children and the British National Formulary and British National Formulary for Children).

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References

  • Waller DG, Sampson AP. Medical Pharmacology and Therapeutics, 5th edn, London: Elsevier Health Sciences, 2018.
  • Aronson N, Herwaldt BL, Libman M, et al. Diagnosis and treatment of leishmaniasis: clinical practice guidelines by the Infectious Diseases Society of America (IDSA) and the American Society of Tropical Medicine and Hygiene (ASTMH). Am J Trop Med Hyg. 2017;96(1):24-45. doi: 10.4269/ajtmh.16-84256. PubMed
  • World Health Organization.‎ Draft Manual for case management of cutaneous leishmaniasis in the WHO Eastern Mediterranean Region. July 2012. Available at: www.who.int/iris/handle/10665/120002 [accessed 26 June 2020]
  • Brito NC, Rabello A, Cota GF. Efficacy of pentavalent antimoniate intralesional infiltration therapy for cutaneous leishmaniasis: A systematic review. PLoS One. 2017;12(9):e0184777. doi: 10.1371/journal.pone.0184777. PubMed
  • Blum J, Buffet P, Visser L, et al. LeishMan recommendations for treatment of cutaneous and mucosal leishmaniasis in travelers, 2014. J Travel Med. 2014;21(2):116-29. doi:10.1111/jtm.12089. PubMed
  • Gasser RA Jr, Magill AJ, Oster CN, Franke ED, Grögl M, Berman JD. Pancreatitis induced by pentavalent antimonial agents during treatment of leishmaniasis. Clin Infect Dis. 1994 Jan;18(1):83-90. doi: 10.1093/clinids/18.1.83. PubMed
  • Wise ES, Armstrong MS, Watson J, Lockwood DN. Monitoring toxicity associated with parenteral sodium stibogluconate in the day-case management of returned travellers with New World cutaneous leishmaniasis [corrected]. PLoS Negl Trop Dis. 2012;6(6):e1688. doi: 10.1371/journal.pntd.0001688. Epub 2012 Jun 26. Erratum in: PLoS Negl Trop Dis. 2012 Sep;6(9). doi:10.1371/annotation/15ab4f39-31e7-40bc-9b15-6e90a612b49a. PMID: 22745840; PMCID: PMC3383730. PubMed
  • Hepburn NC, Siddique I, Howie AF, Beckett GJ, Hayes PC. Hepatotoxicity of sodium stibogluconate in leishmaniasis. Lancet. 1993;342(8865):238-9. doi: 10.1016/0140-6736(93)92327-p. PubMed
  • Hepburn NC. Thrombocytopenia complicating sodium stibogluconate therapy for cutaneous leishmaniasis. Trans R Soc Trop Med Hyg. 1993;87(6):691. doi: 10.1016/0035-9203(93)90298-5. PubMed
  • Wortmann GW, Aronson NE, Byrd JC, Grever MR, Oster CN. Herpes zoster and lymphopenia associated with sodium stibogluconate therapy for cutaneous leishmaniasis. Clin Infect Dis. 1998;27(3):509-12. doi:10.1086/514689. PubMed

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