Sodium Stibogluconate (Pentostam) Injection is an anti-protozoal drug. It is a synthetic pentavalent antimonial agent that is indicated for the treatment of leishmaniasis.
Sodium Stibogluconate (Pentostam) Uses:
-
Leishmaniasis:
- Cutaneous, mucosal & visceral leishmaniasis treatment.
Sodium Stibogluconate (Pentostam) Dose in Adults
- Dosage is expressed as mg of pentavalent antimony.
Sodium Stibogluconate (Pentostam) Dose in the treatment of Leishmaniasis:
- IM/IV:
- 20 mg/kg/day.
- For cutaneous leishmaniasis, the duration of therapy is 20 days & 28 days for mucosal & visceral leishmaniasis.
Use in Children:
- Refer to adult dosing.
Sodium Stibogluconate (Pentostam) Pregnancy Risk Category: C
- The use of sodium stibogluconate in pregnancy has been documented.
- However, spontaneous abortions may be more likely than with other agents.
- Untreated leishmaniasis can also cause spontaneous abortion.
- Also, babies who are too small to be diagnosed with congenital leishmaniasis at gestational age 7 may experience spontaneous abortion.
- Pregnancy may activate an existing maternal infection.
- Maternal infection can be transmitted to the baby during delivery.
- Lesions in cutaneous Leishmaniasis can be more severe in pregnant women.
- Other agents may be recommended for pregnant women to treat visceral Leishmaniasis.
Sodium stibogluconate use during breastfeeding:
- Breast milk contains sodium stibogluconate.
Pentostam Dose in Kidney Disease:
- Avoid use in significant impairment.
Pentostam Dose in Liver disease:
- Avoid use.
Side Effects of Sodium Stibogluconate (Pentostam):
-
Gastrointestinal:
- Diarrhea
- Nausea
- Vomiting
- Abdominal pain
- Anorexia
- Increase serum lipase levels
-
Cardiovascular:
- Flattened T Wave On ECG
- Inversion T Wave On ECG
- Prolonged Q-T Interval On ECG
-
Central Nervous System:
- Headache
- Lethargy
- Malaise
-
Endocrine & Metabolic:
- Increased Amylase
-
Hematologic & Oncologic:
- Change In Platelet Count (Decreased; Transient)
- Decreased Hemoglobin (Transient)
- Decreased White Blood Cell Count (Transient)
-
Neuromuscular & Skeletal:
- Arthralgia
- Myalgia
-
Respiratory:
- Cough (Transient)
- Pneumonia
Contraindication to Sodium Stibogluconate (Pentostam):
Hypersensitivity reactions to any drug or component of the formulations should be avoided. Advanced liver and kidney disease.
Warnings and precautions
-
Modified cardiac conduction
- ECG changes such as T-wave inversions, extended QT intervals and arrhythmia can occur. They appear to be dose and duration dependent.
- Reports of sudden death and cardiotoxicity have been rare.
- Stop immediately if a QT interval corrected >0.5 seconds is prolonged or any other signs of cardiotoxicity, such as significant arrhythmia, concave segments ST segments, or prolongation.
-
Hematologic effects
- Anemia, leukopenia and thrombocytopenia can occur during treatment.
- Monitor CBC periodically.
- If possible, iron deficiency should first be corrected before therapy can begin.
-
Hepatotoxicity:
- Elevated liver enzymes can occur.
- It is important to monitor LFTs regularly.
- If hepatotoxicity develops, discontinue use.
-
Musculoskeletal effects
- Myalgias and arthralgias can occur. Sometimes, they are severe and last for several weeks.
-
Pancreatitis
- Common symptoms are pancreatic enzyme elevations.
- Although less common, pancreatitis can occur.
- Patients with preexisting pancreatic diseases should be avoided.
-
Cardiac disease
- Patients with pre-existing heart disease should be avoided.
-
Hepatic impairment
- Patients with preexisting liver disease should be avoided.
-
Renal impairment
- Patients with severe renal impairment should not use this medication.
Sodium stibogluconate (United States: Available via CDC drug service investigational drug [IND] protocol only)s: Drug Interaction
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Chloroquine |
Chloroquine's QTcprolonging impact may be enhanced by QT-prolonging Other Agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Clofazimine |
The QTcprolonging effect of Clofazimine may be enhanced by QT-prolonging Other Agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Gadobenate Dimeglumine |
Gadobenate Dimeglumine's ability to prolong QTc may be enhanced by QT-prolonging Other Agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Halofantrine |
Halofantrine's ability to prolong QTc may be strengthened by other QT-prolonging substances (moderate risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Haloperidol |
The QTcprolonging effect of haloperidol may be enhanced by QT-prolonging Other Agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
Lofexidine |
QT-prolonging Miscellaneous Agents (Moderate Risk) may enhance the QTcprolonging effect of Lofexidine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
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Midostaurin |
Midostaurin's ability to prolong QTc may be strengthened by other QT-prolonging substances (moderate risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Ondansetron |
Ondansetron's ability to prolong QTc may be enhanced by other QT-prolonging substances (moderate risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Pentamidine (Systemic) |
Pentamidine's ability to prolong QTc may be enhanced by other QT-prolonging substances (moderate risk) (Systemic). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Piperaquine |
The QTcprolonging effect of piperaquine may be enhanced by QT-prolonging Other Agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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Probucol |
The QTcprolonging effect of Probucol may be enhanced by QT-prolonging Miscellaneous Agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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QT-prolonging Antidepressants (Moderate Risk) |
May increase the QTc-prolonging action of other QT-prolonging agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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QT-prolonging Antipsychotics (Moderate Risk) |
The QTc-prolonging impact of QT-prolonging antipsychotics may be enhanced by QT-prolonging Miscellaneous Agents (Moderate Risk) (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. Examples include pimozide. |
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QT-prolonging Class IC Antiarrhythmics (Moderate Risk) |
The QTc-prolonging impact of QT-prolonging Class IC Antiarrhythmics may be enhanced by QT-prolonging Miscellaneous Agents (Moderate Risk) (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
QT-prolonging Kinase Inhibitors (Moderate Risk) |
May increase the QTc-prolonging action of other QT-prolonging agents (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
QT-prolonging Miscellaneous Agents (Moderate Risk) |
May increase the sodium stibogluconate's ability to extend QTc. When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) |
Potentially amplifies the QTc-prolonging effects of other QT-prolonging agents (Moderate Risk). QT-prolonging Miscellaneous Agents' serum concentration may be increased by QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
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QT-prolonging Quinolone Antibiotics (Moderate Risk) |
The action of QT-prolonging Quinolone Antibiotics may be enhanced by QT-prolonging Miscellaneous Agents (Moderate Risk) (Moderate Risk). When using these medications together, watch out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
Amphotericin B |
Sodium Stibogluconate's cardiotoxic effects can be amplified. |
|
Amphotericin B (Conventional) |
Sodium Stibogluconate's cardiotoxic effects can be amplified. Particularly, chances for arrhythmia and abrupt cardiac death could rise. |
|
Domperidone |
The QTc-prolonging action of Domperidone may be strengthened by QT-prolonging Agents (Moderate Risk). Management: Take into account different pharmacological combinations. If combined, keep an eye out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
QT-prolonging Agents (Highest Risk) |
May increase the sodium stibogluconate's ability to extend QTc. Management: Take into account alternatives to this fusion. If combined, keep an eye out for cardiac arrhythmias and a prolonged QTc interval. Patients may be considerably more at risk for QTc prolongation if they have additional risk factors. |
|
Pimozide |
Could make QT-prolonging agents' effect on QTc longer (Moderate Risk). |
|
QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk) |
Potentially amplifies the QTc-prolonging effects of other QT-prolonging agents (Moderate Risk). The serum concentration of QT-prolonging Miscellaneous Agents may rise in response to QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk) (Moderate Risk). |
Monitoring parameters:
- Baseline & weekly EKG, serum creatinine, liver function tests, serum amylase & CBC.
- During week 3 of therapy, patients requiring >20 days of treatment should begin twice-weekly EKG monitoring.
- In certain patients, twice-weekly or more frequent EKG monitoring may be indicated (eg, elderly, underlying cardiac, renal, or hepatic disease).
How to administer Sodium Stibogluconate (Pentostam)?
- IM/IV:
- Administer IM or IV (preferred) over 5-10 mins.
- IM injection may be painful because volume per dose may be large.
Mechanism of action of Sodium Stibogluconate (Pentostam):
- It is not known what the exact mechanism of action is.
- The proposed mechanisms include the conversion to a trivalent antimony form that affects glucose metabolism, fatty acids beta-oxidation, and adenosine triphosphate formation.
- It can cause the formation of a complex containing adenine nucleotides that acts as an inhibitor for Leishmania purine transporters, or interfere with purine salvage pathway.
- Activation and stimulation of the host immune system.
Absorption:
- IM:
- Well absorbed.
Half-life elimination:
- ~10 hours.
Excretion:
- Urine (80% as an unchanged drug over 6 hours)
International Brands of Sodium Stibogluconate:
- Pentostam
- Stibovita
Sodium Stibogluconate Brand Names in Pakistan:
Sodium Stibogluconate Injection 333 mg |
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| Stibotim | Star Laboratories (Pvt) Ltd. |
