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Sodium stibogluconate

Brand and Other Names: Pentostam
Mechanism of Action:
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Description:

Not FDA‑approved; used via CDC for visceral leishmaniasis. 

GOOGLE OVERVIEW

Sodium stibogluconate, also known by the brand name Pentostam, is a synthetic, pentavalent antimonial agent used primarily to treat leishmaniasis, a parasitic disease caused by sandfly bites. This includes cutaneous, visceral, and mucosal forms of leishmaniasis. It's considered the drug of choice in the United States, available through the Centers for Disease Control (CDC). However, combination therapy with other drugs like miltefosine, paromomycin, and liposomal amphotericin B may be considered due to increasing resistance. 
 
Mechanism of action
 
While the exact mechanism of action is not fully understood, it's believed that sodium stibogluconate may work by binding to thiol groups within the parasite and inhibiting the formation of high-energy phosphates like ATP and GTP. This potentially leads to decreased synthesis of essential macromolecules and ultimately reduces parasite viability. 
 
Administration and dosage
 
Sodium stibogluconate is administered parenterally, meaning not through the digestive system. This can be done either through intramuscular injection or slow intravenous infusion. Typical dosage regimens for treating leishmaniasis involve 20 mg/kg/day of pentavalent antimony. For cutaneous leishmaniasis, treatment may last 20 days, while visceral and mucosal leishmaniasis may require 28 days of treatment. 
 
Side effects
 
Sodium stibogluconate can cause a range of side effects, some of which are common and others more serious. 
 
Common side effects
  • Gastrointestinal issues, such as nausea, vomiting, diarrhea, and abdominal pain.
  • Muscle and joint pain.
  • Fatigue, lethargy.
  • Headache.
  • Pain and irritation at the injection site. 
Serious side effects
  • Pancreatitis.
  • Liver and kidney damage.
  • Cardiac issues, including irregular heartbeat, ECG changes, and arrhythmias.
  • Severe allergic reactions like anaphylaxis (rare). 
Contraindications
 
Sodium stibogluconate is contraindicated in individuals with known hypersensitivity to the drug. It should be used with caution in patients with pre-existing heart disease (especially arrhythmias), renal failure, severe liver disease, severe malnutrition, or advanced HIV infection. Pregnancy is also a contraindication unless the potential benefits outweigh the risks. 
 
Drug interactions
 
Sodium stibogluconate can interact with other medications, particularly those affecting cardiac rhythm (like beta-blockers or other antiarrhythmics) or those with hepatotoxic potential. Inform your healthcare provider about all medications you are currently taking, including over-the-counter drugs and supplements, to avoid harmful interactions. 
See package insert for full prescribing information.