pentostam
pentostam Uses, Dosage, Side Effects, Food Interaction and all others data.
Sodium stibogluconate directly inhibits DNA topoisomerase 1 leading to inhibition of both DNA replication and transcription.
The mode of action of sodium stibogluconate is not clearly understood. In vitro exposure of amastigotes to 500 mg pentavalent antimony/ml results in a greater than 50% decrease in parasite DNA, RNA protein and purine nucleoside triphosphate levels. It has been postulated that the reduction in ATP (adenosine triphosphate) and GTP (guanosine triphosphate) synthesis contributes to decreased macromolecular synthesis.
| Trade Name | pentostam |
| Generic | Sodium Stibogluconate |
| Sodium Stibogluconate Other Names | Antimony sodium gluconate, Estibogluconato sodico, Myostibin, Natrii stibogluconas, Sodium stibogluconate, Stibanate, Stibanose, Stibatin, Stibinol, Stibogluconate de sodium |
| Weight | 100mg/ml, |
| Type | Solution |
| Formula | C12H35Na3O26Sb2 |
| Weight | Average: 907.88 Monoisotopic: 905.918601405 |
| Groups | Approved, Investigational |
| Therapeutic Class | Leishmaniacides |
| Manufacturer | Glaxowellcome |
| Available Country | Saudi Arabia, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Leishmaniasis, Visceral leishmaniasis
pentostam is also used to associated treatment for these conditions: Leishmaniasis, Mucocutaneous Leishmaniasis, Visceral Leishmaniasis
How pentostam works
Sodium stibogluconate directly inhibits DNA topoisomerase I leading to inhibition of both DNA replication and transcription.
Dosage
pentostam dosage
Leishmaniasis:20 mg/kg/day (maximum 850 mg) intramuscularly or intravenously for 20 to 28 days.
Side Effects
Sodium stibogluconate is exceedingly toxic to veins. One of the practical problems is that after a few doses it can become exceedingly difficult to find a vein in which to inject the drug. The insertion of a PICC does not prevent the problem and can instead exacerbate it: the entire vein along the course of the PICC line can become inflamed and thrombose. Large doses of sodium stibogluconate are often administered as dilute solutions.
Pancreatitis is a common deleterious effect of the drug, and the serum amylase or lipase should be monitored twice weekly; there is no need to stop treatment if the amylase remains less than four times the upper limit of normal; if the amylase rises above the cut-off, then treatment should be interrupted until the amylase falls to less than twice the upper limit of normal, whereupon treatment can be resumed. Cardiac conduction disturbances are less common, but ECG monitoring while the medicine is injected is advisable and changes quickly reverse after the drug is stopped or the infusion rate is decreased.
The drug can be given intramuscularly but is exceedingly painful when given by this route. It can also be given intralesionally when treating cutaneous leishmaniasis (i.e., injected directly into the area of infected skin) and again, this is exceedingly painful and does not give results superior to intravenous administration.
Sodium stibogluconate can also cause a reduced appetite, metallic taste in mouth, nausea, vomiting, diarrhoea, headache, tiredness, joint pains, muscle aches, dizziness, and anaphylaxis.
Toxicity
The main symptoms of antimony overdosage are gastro-intestinal disturbances (nausea, vomiting and severe diarrhoea). Haemorrhagic nephritis and hepatitis may also occur.
Pregnancy & Breastfeeding use
Pregnancy category is not classified.
Contraindication
Hypersensitivity, significant renal impairment, breast feeding
Innovators Monograph
You find simplified version here pentostam
FAQ
What is pentostam used for?
pentostam used to treat cutaneous, visceral, and mucosal leishmaniasis, a parasitic infection transmitted by sand-fly bites.
How safe is pentostam?
pentostam is as safe and effective as pentostamed meglumine antimoniate.
How does pentostam work?
pentostam may act by binding to thiol groups in the parasite and inhibiting the formation of adenosine triphosphate and guanosine triphosphate.
Is pentostam safe in pregnancy?
pentostam for pregnant women is difficult to treat because for them the two commonly used drugs, sodium stibogluconate and pentamidine, are not considered safe.
Is pentostam safe during breastfeeding?
Limited information indicates that maternal doses of pentostam up to 1.4 grams daily produce low levels in milk and would not be expected to cause any adverse effects in breastfed infants,especially if the infant is older than 2 months.
What are the common side effects of pentostam?
Common side effects of pentostam include:
- Loss of appetite
- Nausea
- Vomiting
- Abdominal pain
- ECG changes
- Headache
- Lethargy
- Muscle pain
- Raised liver enzymes
- Coughing and substernal pain
- Fever
- Sweating
- Flushing
- Spinning sensation (vertigo)
- Bleeding from nose or gum
- Yellowing skin and eyes (jaundice)
- Rash
- Pain and thrombosis on intravenous administration, intramuscular injection also painful
- Anaphylaxis (rare)
How long does it take for pentostam to work?
The duration of treatment is usually 10 to 21 days and depends on the species of pentostam and the type of infection.
How do I administer pentostam?
pentostam usually administered by intravenous or intramuscular injection daily at a dose of 20 mg/kg/day .
Does pentostam affect the heart?
This regimen of pentostam does not measurably impair left ventricular systolic or diastolic function.In most young fit patients, this regimen has no cardiac side-effects.
Who should not take pentostam?
Do not take pentostam if you are allergic to pentostam or any ingredients contained in this drug.
What is the effect of pentostam on the Kidneys?
pentostam has very mild side effects on the kidneys.
What is the effect of pentostam on the Liver?
There are no any side effects of pentostam on the liver.
Can I drive after taking pentostam?
pentostam does not cause dizziness or sleep, so you can drive a vehicle or operate machinery also.
Can I take alcohol with pentostam?
Due to lack of research, there is no information about the side effects of taking Sodium Stibogluconate with alcohol.
Is pentostam able to treat mental disorders?
No, pentostam is not used to treat mental disorders.
