PENTOSTAM INJECTION

Indications

• Visceral leishmaniasis
• Cutaneous leishmaniasis
• Mucosal leishmaniasis

Dosage

Children: Refer to the BNF for Children

Adults: The usual adult dose for visceral leishmaniasis is 20 mg/kg per day, administered intravenously for 28 days. For cutaneous leishmaniasis, the dosage may vary and should be determined based on specific clinical guidelines.

Mechanism of action

Stibogluconate is believed to exert its antileishmanial effects through the inhibition of glycolysis and fatty acid oxidation in Leishmania species. The active form of the drug interacts with thiol groups in the parasite, disrupting its metabolic processes and leading to cell death. This mechanism of action is crucial for its effectiveness against the pathogenic forms of Leishmania.

Pharmacodynamics

The pharmacodynamic properties of stibogluconate involve its ability to cause apoptosis in Leishmania parasites. The drug alters the redox state of the intracellular environment of the parasites, contributing to their death. Additionally, stibogluconate can induce immunomodulatory effects, enhancing the host's immune response against the infection. The therapeutic window of stibogluconate is relatively narrow, necessitating careful monitoring of patients during treatment.

Pharmacokinetics

Stibogluconate is administered intravenously and exhibits variable pharmacokinetics, with peak plasma concentrations occurring shortly after administration. The drug is distributed throughout the body, including to the liver and spleen, where it exerts its effects. It has a half-life of approximately 3 to 4 hours and is primarily excreted through the kidneys. Due to its complex pharmacokinetic profile, dosing may need to be adjusted based on individual patient factors.

Contra-indications

• Hypersensitivity to stibogluconate or any of its components
• Severe renal impairment

Adverse effects

• Nausea
• Vomiting
• Abdominal pain
• Diarrhea
• Headache
• Fatigue
• Transient electrocardiogram changes
• Pancreatitis

Interactions

• May enhance the toxic effects of other antimonials
• Caution with agents that affect renal function

Precautions

• Careful monitoring in patients with pre-existing cardiac conditions
• Monitor renal function regularly during therapy
• Use with caution in patients with a history of pancreatitis

Pregnancy

Stibogluconate should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus, as there are no adequate and well-controlled studies in pregnant women.

Breast-feeding

It is unknown whether stibogluconate is excreted in human milk. Caution is advised when administering to breastfeeding women.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Injection: 100 mg/ml solution for injection