Drug reference

Sodium Stibogluconate

Antiprotozoal

Also known as Pentostam, Sodium antimony gluconate, Antimony pentavalent

Antiprotozoal

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

Manufacturer advises use only if potential benefit outweighs risk.

FDA category + note

Mechanism

Sodium stibogluconate is a pentavalent antimonial drug used as an antiprotozoal agent. It is a first-line treatment for various forms of leishmaniasis, targeting the Leishmania parasites.

Indications

Cutaneous leishmaniasisVisceral leishmaniasisMucocutaneous leishmaniasisAll species of LeishmaniaVisceral Leishmaniasis (VL) (standard first line in some parts of the world, but extensive resistance in India/Nepal)Dermal leishmaniasis (oriental sore) (local application)Visceral Leishmaniasis (VL) (most endemic regions, except Bihar, India)Cutaneous Leishmaniasis (CL) (first-line, 20 mg/kg for 20 days, also intralesional for small lesions)Diffuse Cutaneous Leishmaniasis (DCL) (repeated 20-day courses, with 10-day drug-free interval)Mucosal Leishmaniasis (ML) (regimen of choice, 20 mg/kg for 30 days)Post-kala-azar dermal leishmaniasis (PKDL) (in East Africa, 60 days of treatment for persistent lesions, previously used in India for prolonged courses)

Dosing

Adult: 20 mg/kg once daily intravenously or intramuscularly for 20 days in cutaneous leishmaniasis and 28 days in visceral and mucocutaneous disease.
Renal adjustment: Avoid in significant impairment.
Hepatic adjustment: Manufacturer advises caution (limited information available; abnormalities in hepatic function may be expected in visceral leishmaniasis).

Pharmacokinetics

Half-life

Short initial (about 2-hour) half-life and a much longer terminal (>24-hour) half-life.

Bioavailability

Rapidly absorbed and distributed after intravenous or intramuscular administration.

Metabolism

A small fraction enters tissues and remains stored for long periods. Repeated doses are cumulative. Accumulation within macrophages accounts for its prolonged inhibitory effect on leishmania.

Excretion

Eliminated in two phases.

Contraindications

Significant renal impairment

Side effects

Common

Abdominal painAppetite decreasedArthralgiaDiarrhoeaHeadacheLethargyMalaiseMyalgiaNauseaVomitingGastrointestinal symptomsFeverRashPain at intramuscular injection siteSterile abscesses at intramuscular injection siteChemical pancreatitis (nearly all patients)Elevation of serum hepatic transaminase levelsMuscle and joint painWeaknessSkin rashesReversible polyneuropathymetallic tastecoughpain abdomenpain and stiffness of injected musclesterile abscessesmental symptomselevated serum levels of aminotransferaseselectrocardiographic changes (concave ST-segment elevation, QTc prolongation >0.5s)chemical pancreatitis

Serious

Chest pain
Chills
Haemorrhage
Hyperhidrosis
Jaundice
Skin reactions
Vertigo
Arrhythmias
Cough
Pancreatitis
Pneumonia
QT interval prolongation
Thrombosis
Dangerous arrhythmias (due to ECG changes)
Hemolytic anemia
Serious liver effects
Serious renal effects
Serious cardiac effects
Severe inflammation around lesions (potentially life-threatening if pharyngeal or tracheal involvement during mucocutaneous leishmaniasis treatment)
Bone marrow suppression (decreased red cell, white cell, and platelet counts)
Hemolytic anemia (rare)
Renal damage (rare)
Shock (rare)
Sudden death (rare)
liver damage
kidney damage
myelosuppression
Q-T prolongation (may herald arrhythmias)
shock
death
ventricular arrhythmia
sudden death (with QTc prolongation >0.5s)
severe clinical pancreatitis (in immunosuppressed patients)