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  • Pentostam
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    Active Ingredient
    Sodium Stibogluconate 10 g / 100 ml

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Vial

    100 ml

    full basket chart 26839 16127

    Dosage

    Except where otherwise stated, all doses should be given by the intravenous or intramuscular route.
    Due to the presence of particulates (size range 20 to 300 microns) sodium stibogluconate solution should be drawn up through a sterile filter immediately prior to administration. These particulates are insoluble complexes formed by an interaction between product preservative and the antioxidant in the rubber stopper. Filters of pore size 5 microns or less and membrane types polyvinylidene difluoride, polyethersulphone, polysulphone, nylon, surfactant-free cellulose acetate and mixed cellulose esters have been shown to be suitable. Where sterile filters are not available the risks and benefits of administering unfiltered sodium stibogluconate therapy should be assessed by the clinician on an individual basis.
    All dosage recommendations are based on the findings of the WHO Expert Committee on leishmaniasis, which met in 1984. There are no special recommendations for different age groups.
    Visceral Leishmaniasis
    10 to 20mg pentavalent antimony (0.1-0.2ml Sodium stibogluconate injection) per kg bodyweight to a maximum of 850mg (8.5ml Sodium stibogluconate injection ) daily for a minimum period of 20 days.
    Patients should be examined for evidence of relapse after 2 and 6 months, and in Africa after twelve months.
    Cutaneous Leishmaniasis not caused by L. aethiopica
    The dosage regimen outlined for visceral leishmaniasis is recommended.
    Alternatively, single, non-inflamed nodular lesions known not to be due to L. braziliensis may be treated with intralesional injections of 100 to 300mg pentavalent antimony (1-3ml Sodium stibogluconate injection) repeated once or twice if necessary at intervals of 1 to 2 days. Infiltration must be thorough and produce complete blanching of the base of the lesion.
    Individuals with cutaneous leishmaniasis due to L. braziliensis should be treated systemically for several days after the lesion is healed.
    Note:-After successful treatment of L. braziliensis, anti-leishmania antibody titres decline steadily over 424 months.
    Muco – cutaneous leishmaniasis
    Patients with parasitologically confirmed leishmaniasis should be treated with 20mg pentavalent antimony (0.2ml Sodium stibogluconate injection) ) per kg bodyweight to a maximum of 850mg (8.5ml Sodium stibogluconate injection) daily, continuing this dosage for several days longer than it takes to achieve parasitological and clinical cure.
    In the event of relapse, a further course should be given for at least twice the previous duration.
    Diffuse cutaneous leishmaniasis in the new world and leishmaniasis recidivans.
    Owing to the rarity of these conditions, precise data on dosage are not available. A dose of 10 to 20mg pentavalent antimony (0.1-0.2ml Sodium stibogluconate injection) per kg bodyweight to a maximum of 850mg (8.5ml Sodium stibogluconate injection) may be given daily for 2-3 weeks. If there is a response then treatment should be maintained until several days after clinical cure of leishmaniasis recidivans and for several months after clinical and parasitological cure of diffuse cutaneous leishmaniasis.
    Populations
    Elderly: There is little information on the effects of Sodium stibogluconate on elderly individuals. If treatment of cutaneous leishmaniasis is necessary then local infiltration is preferred. The normal precautions should be strictly adhered to when treating older patients for visceral leishmaniasis.
    For full details see prescribing information.


    Indications

    Sodium stibogluconate is indicated for the following diseases:
    Visceral leishmaniasis (Kala Azar);
    Cutaneous leishmaniasis;
    South American mucocutaneous leishmaniasis.
    Sodium stibogluconate may also be of value in the treatment of leishmaniasis recidivans and diffuse cutaneous leishmaniasis in the New World.
    Note: Cutaneous and diffuse cutaneous leishmaniasis caused by Leishmania aethiopica infections are unresponsive to treatment with pentavalent antimony compounds, including Sodium stibogluconate injection, at conventional dosage, but may respond slowly at higher dosage.


    Contra-Indications

    – Sodium stibogluconate injection should not be given to any patient with significantly impaired renal function.
    – Sodium stibogluconate injection should not be given to any patient who has experienced a serious adverse reaction to a previous dose.


    Special Precautions

    Intravenous injection should be filtered immediately prior to use (see Dosage and Administration). Administer very slowly over 5 min to reduce the risk of local thrombosis. In the unlikely event of coughing, vomiting or substernal pain occurring, administration should be discontinued immediately. In such cases, extreme care should be taken if Sodium stibogluconate is re-administered by this route.
    Successful treatment of mucocutaneous leishmaniasis may induce severe inflammation around the lesion. In cases of pharyngeal or tracheal involvement, this may be life threatening. Under such circumstances, corticosteroids may be used. Very rarely, anaphylactic shock may develop during treatment, for which adrenalin injection and appropriate supportive measures should be given immediately.
    Prolongation of the QTc interval has been observed in some patients taking sodium stibogluconate and appears to be dose-related. There have also been reports of fatal cardiac arrhythmias in patients receiving higher dose antimonial therapy for visceral leishmaniasis. Therefore, ECG monitoring is recommended before and during therapy with sodium stibogluconate. Where ECG monitoring is not available, the risks and benefits of sodium stibogluconate therapy should be assessed on an individual basis. If clinically significant prolongation of QTc interval occurs, sodium stibogluconate should be discontinued. Electrocardiographic changes, notably alterations in T wave amplitude may be expected in the majority of patients given sodium stibogluconate. These appear to be reversible on cessation of therapy and are not of serious significance. Sodium stibogluconate should be used cautiously in patients with cardiovascular disease, a history of ventricular arrhythmias or other risk factors known to predispose towards QT prolongation: for example, those with congenital QTc prolongation or taking concomitant drugs known to significantly prolong the QT interval (e.g. class III anti-arrhythmics such as sotalol and amiodarone). As there appears to be a dose relationship in the development of ECG abnormalities, prior exposure to antimonial therapy should be considered when assessing a patient’s suitability for initiating or continuing therapy with sodium stibogluconate. Patients who have recently received other antimonial drugs should be monitored closely for signs of antimony intoxication such as bradycardia and cardiac arrhythmias during administration of Sodium stibogluconate. There have been some reports of cardiac arrhythmias and sudden death when amphotericin B deoxycholate is administered soon after sodium stibogluconate for retreatment of visceral leishmaniasis. Electrolyte imbalances should be corrected prior to administration of amphotericin B deoxycholate, and patients appropriately monitored. Intercurrent infections, such as pneumonia, should be sought and treated concurrently. High concentrations of antimony are found in the livers of animals after repeated dosage with pentavalent antimony. Sodium stibogluconate should therefore be used with caution in patients with hepatic disease. However, some abnormalities of liver function may be expected in cases of visceral leishmaniasis. In such patients the benefit of pentavalent antimony treatment outweighs the risk. Sodium stibogluconate may induce mild elevation of hepatic enzymes in serum which later return to normal.


    Side Effects

    Approximately 1 to 2% of patients complain of nausea, vomiting and/or diarrhoea and a slightly higher number of abdominal pain.
    Other common side effects include anorexia, malaise, myalgia, arthralgia, headache and lethargy.
    ECG changes, including reduction in T-wave amplitude, T-wave inversion and QT prolongation have been observed.
    Transient coughing immediately following injection was reported with varying frequency during several trials.
    Intravenous injection of Sodium stibogluconate may cause transient pain along the course of the vein and eventually thrombosis of that vein.
    Transient rises in serum lipase and amylase may occur during treatment with sodium stibogluconate. Symptomatic pancreatitis has also been reported. During some early trials of sodium stibogluconate, pneumonia occurred in a small number of patients treated for visceral leishmaniasis and this occasionally proved fatal. Pneumonia is a feature of the visceral leishmaniasis disease process; however it has been associated with the toxicity profile of trivalent antimony. It is, therefore, not possible to determine whether these cases were due to the disease or to Sodium stibogluconate. Other (rarely reported) side effects include fever, rigor, sweating, vertigo, facial flushing, worsening of lesions on the cheek, bleeding from the nose or gum, substernal pain, jaundice and rash. Transient reductions in platelets, white blood cells and haemoglobin have been reported.


    Drug interactions

    No interactions with Sodium stibogluconate have been reported.
    There is no information on whether sodium stibogluconate interferes with the accuracy of routine biochemical tests.


    Pregnancy and Lactation

    Pregnancy: Although no effects on the foetus have been reported, Sodium stibogluconate should be withheld during pregnancy unless the potential benefits to the patient outweigh the possible risk to the foetus.
    Lactation: Children should not be breast-fed by mothers receiving Sodium stibogluconate.


    Overdose

    Symptoms and Signs: The main symptoms of antimony overdose are gastro-intestinal disturbances (nausea, vomiting and severe diarrhoea). Haemorrhagic nephritis and hepatitis may also occur.
    Treatment: There is only limited information on the use of chelating agents in the treatment of intoxication by antimony compounds.
    Dimercaprol has been reported to be effective; a dose of 200 mg by i.m. injection every six hours until recovery is complete has been suggested.
    2,3-Dimercaptosuccinic acid (DMSA) may also be effective treatment.


    Manufacturer
    Glaxo Operations UK Ltd
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