\n\n"},"bioavailability":{"wt":""},"metabolism":{"wt":""},"excretion":{"wt":""},"CAS_number_Ref":{"wt":"{{cascite|correct|CAS}}"},"CAS_number":{"wt":"219717-42-7"},"ATC_prefix":{"wt":"P01"},"ATC_suffix":{"wt":"CB02"},"ATC_supplemental":{"wt":"{{ATCvet|P51|AB02}}"},"PubChem":{"wt":"16685683"},"DrugBank_Ref":{"wt":"{{drugbankcite|correct|drugbank}}"},"DrugBank":{"wt":"DB05630"},"ChemSpiderID_Ref":{"wt":"{{chemspidercite|correct|chemspider}}"},"ChemSpiderID":{"wt":"21106382"},"UNII_Ref":{"wt":"{{fdacite|changed|FDA}}"},"UNII":{"wt":"V083S0159D"},"KEGG_Ref":{"wt":"{{keggcite|correct|kegg}}"},"KEGG":{"wt":"D00582"},"ChEMBL_Ref":{"wt":"{{ebicite|changed|EBI}}"},"ChEMBL":{"wt":"367144"},"NIAID_ChemDB":{"wt":"007935"},"index2_label":{"wt":"nonhydrate"},"CAS_number2_Ref":{"wt":"{{cascite|correct|CAS}}"},"CAS_number2":{"wt":"16037-91-5"},"UNII2_Ref":{"wt":"{{fdacite|correct|FDA}}"},"UNII2":{"wt":"APJ6285Y89\n"},"chemical_formula":{"wt":""},"C":{"wt":"12"},"H":{"wt":"38"},"Na":{"wt":"3"},"O":{"wt":"26"},"Sb":{"wt":"2"},"smiles":{"wt":"[Na+].[Na+].[Na+].O=[Sb]2(O[Sb]1(=O)OC([C@H](O)CO)[C@H](O)[C@@H](O1)C([O-])=O)O[C@@H]([C@H](O)[C@@H](O2)C([O-])=O)[C@H](O)CO"},"StdInChI_Ref":{"wt":"{{stdinchicite|correct|chemspider}}"},"StdInChI":{"wt":"1S/2C6H10O7.3Na.3O.2Sb/c2*7-1-2(8)3(9)4(10)5(11)6(12)13;;;;;;;;/h2*2-5,7-8,10H,1H2,(H,12,13);;;;;;;;/q2*-2;3*+1;;;;2*+2/p-2/t2-,3?,4+,5-;2-,3-,4+,5-;;;;;;;;/m11......../s1"},"StdInChIKey_Ref":{"wt":"{{stdinchicite|correct|chemspider}}"},"StdInChIKey":{"wt":"RTLKTTNTVTVWPV-UQCYVGCHSA-L"}},"i":0}}]}" id="mwBA">Pharmaceutical compound
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Clinical data | |
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Trade names | Pentostam, Stiboson, others [1] |
AHFS/Drugs.com | International Drug Names |
Routes of administration | intravenous, intramusclar [2] |
ATC code | |
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CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.170.909 |
Chemical and physical data | |
Formula | C12H38Na3O26Sb2 |
Molar mass | 910.899 g·mol−1 |
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Sodium stibogluconate, sold under the brand name Pentostam among others, is a medication used to treat leishmaniasis. [3] This includes leishmaniasis of the cutaneous, visceral, and mucosal types. [4] Some combination of miltefosine, paromomycin and liposomal amphotericin B, however, may be recommended due to issues with resistance. [2] [5] It is given by injection. [6]
Side effects are common and include loss of appetite, nausea, muscle pains, headache, and feeling tired. [2] [5] Serious side effect may include an irregular heartbeat or pancreatitis. [5] Sodium stibogluconate is less safe than some other options during pregnancy. [2] It is not believed to result in any problems if used during breastfeeding. [7] Sodium stibogluconate is in the pentavalent antimonials class of medication. [5]
Sodium stibogluconate has been studied as early as 1937 and has been in medical use since the 1940s. [8] [9] It is on the World Health Organization's List of Essential Medicines. [10] In the United States, it is available from the Centers for Disease Control. [3]
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 peripherally inserted central catheter (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.[ citation needed ]
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 electrocardiograph (ECG) monitoring while the medicine is injected is advisable and changes quickly reverse after the drug is stopped or the infusion rate is decreased.[ citation needed ]
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.[ citation needed ]
Sodium stibogluconate can also cause a reduced appetite, metallic taste in mouth, nausea, vomiting, diarrhoea, headache, tiredness, joint pains, muscle aches, dizziness, and anaphylaxis.[ citation needed ]
Sodium stibogluconate is available in the United Kingdom as Pentostam, where it is manufactured by GlaxoSmithKline. It is available in the United States on a named-patient basis from the Centers for Disease Control and Prevention (CDC).[ citation needed ]
As dosage regimens for treating leishmaniasis have evolved, the daily dose of antimony and the duration of therapy have been progressively increased to combat unresponsiveness to therapy. In the 1980s, the use of 20 mg/kg/day (instead of 10 mg/kg/day) of antimony was recommended, but only to a maximum daily dose of 850 mg. Recent research has suggested on the basis of recent efficacy and toxicity data that this 850-mg restriction should be removed. The evidence to date, which is in their research, suggests that a regimen of 20 mg/kg/day of pentavalent antimony, without an upper limit on the daily dose, is more efficacious and is not substantially more toxic than regimens with lower daily doses. It is recommend treating all forms of leishmaniasis with a full 20 mg/kg/day of pentavalent antimony. Treatment of cutaneous leishmaniasis usually lasts for 20 days and visceral and mucosal leishmaniasis for 28 days. [11]
The dose of sodium stibogluconate is by slow intravenous infusion (at least five minutes with cardiac monitoring). The injection are stopped if there is coughing or central chest pain. The chemotherapeutic index was established by Leonard Goodwin during the Second World War when a treatment was urgently required for Allied troops during the invasion of Sicily. [12]
The duration of treatment is usually 10 to 21 days and depends on the species of Leishmania and the type of infection (cutaneous or visceral).[ citation needed ]
The chemical structure of sodium stibogluconate is somewhat ambiguous, and the structure shown above is idealized. Its solutions may contain multiple antimony compounds, although this heterogeneity may be unimportant. It has been speculated that the active species contains only a single antimony centre. [13]
Pentavalent antimony does not appear to accumulate in the body and is excreted by the kidneys. [14]
The mechanism of sodium stibogluconate is poorly understood, but is thought to stem from the inhibition of macromolecular synthesis via a reduction in available ATP and GTP, likely secondary to inhibition of the citric acid cycle and glycolysis. Bermann et al. studied the effects of stibogluconate on Leishmania mexicana and demonstrated a 56–65% reduction in incorporation of a label into purine nucleoside triphosphates (ATP and GTP) as well as between a 34–60% increase of label incorporation into purine nucleoside mono- and diphosphates (AMP, GMP, ADP, and GDP) following 4 hour exposure to stibogluconate. [15]
Pentamidine is an antimicrobial medication used to treat African trypanosomiasis, leishmaniasis, Balamuthia infections, babesiosis, and to prevent and treat pneumocystis pneumonia (PCP) in people with poor immune function. In African trypanosomiasis it is used for early disease before central nervous system involvement, as a second line option to suramin. It is an option for both visceral leishmaniasis and cutaneous leishmaniasis. Pentamidine can be given by injection into a vein or muscle or by inhalation.
Leishmaniasis is a wide array of clinical manifestations caused by protozoal parasites of the Trypanosomatida genus Leishmania. It is generally spread through the bite of phlebotomine sandflies, Phlebotomus and Lutzomyia, and occurs most frequently in the tropics and sub-tropics of Africa, Asia, the Americas, and southern Europe. The disease can present in three main ways: cutaneous, mucocutaneous, or visceral. The cutaneous form presents with skin ulcers, while the mucocutaneous form presents with ulcers of the skin, mouth, and nose. The visceral form starts with skin ulcers and later presents with fever, low red blood cell count, and enlarged spleen and liver.
Suramin is a medication used to treat African sleeping sickness and river blindness. It is the treatment of choice for sleeping sickness without central nervous system involvement. It is given by injection into a vein.
Amoxicillin/clavulanic acid, also known as co-amoxiclav or amox-clav, sold under the brand name Augmentin, among others, is an antibiotic medication used for the treatment of a number of bacterial infections. It is a combination consisting of amoxicillin, a β-lactam antibiotic, and potassium clavulanate, a β-lactamase inhibitor. It is specifically used for otitis media, streptococcal pharyngitis, pneumonia, cellulitis, urinary tract infections, and animal bites. It is taken by mouth or by injection into a vein.
Ivermectin is an antiparasitic drug. After its discovery in 1975, its first uses were in veterinary medicine to prevent and treat heartworm and acariasis. Approved for human use in 1987, it is used to treat infestations including head lice, scabies, river blindness (onchocerciasis), strongyloidiasis, trichuriasis, ascariasis and lymphatic filariasis. It works through many mechanisms to kill the targeted parasites, and can be taken by mouth, or applied to the skin for external infestations. It belongs to the avermectin family of medications.
Sandfly or sand fly is a colloquial name for any species or genus of flying, biting, blood-sucking dipteran (fly) encountered in sandy areas. In the United States, sandfly may refer to certain horse flies that are also known as "greenheads", or to members of the family Ceratopogonidae. The bites usually result in a small, intensely itchy bump or welt, the strength of which intensifies over a period of 5-7 days before dissipating. Sandfly bites can be distinguished from mosquito bites as sandfly bite are usually found in clusters as they attack animals in groups. Moderate relief is achieved with varying success through the application of over-the-counter products such as Benadryl (ingested) or an analgesic cream such as After Bite. Outside the United States, sandfly may refer to members of the subfamily Phlebotominae within the Psychodidae. Biting midges (Ceratopogonidae) are sometimes called sandflies or no-see-ums. New Zealand sandflies are in the genus of sand fly Austrosimulium, a type of black fly.
Paromomycin is an antimicrobial used to treat a number of parasitic infections including amebiasis, giardiasis, leishmaniasis, and tapeworm infection. It is a first-line treatment for amebiasis or giardiasis during pregnancy. Otherwise, it is generally a second line treatment option. It is taken by mouth, applied to the skin, or by injection into a muscle.
Cutaneous leishmaniasis is the most common form of leishmaniasis affecting humans. It is a skin infection caused by a single-celled parasite that is transmitted by the bite of a phlebotomine sand fly. There are about thirty species of Leishmania that may cause cutaneous leishmaniasis.
Visceral leishmaniasis (VL), also known as kala-azar or "black fever", is the most severe form of leishmaniasis and, without proper diagnosis and treatment, is associated with high fatality. Leishmaniasis is a disease caused by protozoan parasites of the genus Leishmania.
Antimonials, in pre-modern medicine, were remedies principally containing antimony, used chiefly for emetic purposes. They might also have qualified for cathartic, diaphoretic, or simply alternative uses. Such treatments were considered unparalleled in their strength.
Pentavalent antimonials are a group of compounds used for the treatment of leishmaniasis. They are also called pentavalent antimony compounds.
Meglumine antimoniate is a medicine used to treat leishmaniasis. This includes visceral, mucocutaneous, and cutaneous leishmaniasis. It is given by injection into a muscle or into the area infected.
The Drugs for Neglected Diseases initiative (DNDi) is a collaborative, patients' needs-driven, non-profit drug research and development (R&D) organization that is developing new treatments for neglected diseases, notably leishmaniasis, sleeping sickness, Chagas disease, malaria, filarial diseases, mycetoma, paediatric HIV, cryptococcal meningitis, hepatitis C, and dengue. DNDi's malaria activities were transferred to Medicines for Malaria Venture (MMV) in 2015.
Miltefosine, sold under the trade name Impavido among others, is a medication mainly used to treat leishmaniasis and free-living amoeba infections such as Naegleria fowleri and Balamuthia mandrillaris. This includes the three forms of leishmaniasis: cutaneous, visceral and mucosal. It may be used with liposomal amphotericin B or paromomycin. It is taken by mouth.
Alan Hutchinson Fairlamb, CBE, FRSE, FLS, FMedSci, FRSB is a Wellcome Trust Principal Research Fellow and Professor of Biochemistry in the Division of Biological Chemistry and Drug Discovery at the School of Life Sciences, University of Dundee, Scotland. From 2006-2011 he was a member of the Scientific and Technical Advisory Committee of the Special Programme for Research and Training in Tropical Diseases (TDR) -- an independent global programme of scientific collaboration co-sponsored by UNICEF, UNDP, the World Bank and WHO. Currently he is a member of the governing board of the Tres Cantos Open Lab Foundation, whose aim is to accelerate the discovery and development of medicines to tackle diseases of the developing world in an open collaborative manner.
Diloxanide is a medication used to treat amoeba infections. In places where infections are not common, it is a second line treatment after paromomycin when a person has no symptoms. For people who are symptomatic, it is used after treatment with metronidazole or tinidazole. It is taken by mouth.
Leishmania tropica is a flagellate parasite and the cause of anthroponotic cutaneous leishmaniasis in humans. This parasite is restricted to Afro-Eurasia and is a common cause of infection in Afghanistan, Iran, Syria, Yemen, Algeria, Morocco, and northern India.
Post-kala-azar dermal leishmaniasis (PKDL) is a complication of visceral leishmaniasis (VL); it is characterised by a macular, maculopapular, and nodular rash in a patient who has recovered from VL and who is otherwise well. The rash usually starts around the mouth from where it spreads to other parts of the body depending on severity.
Antimony potassium tartrate, also known as potassium antimonyl tartrate, potassium antimontarterate, or tartar emetic, has the formula K2Sb2(C4H2O6)2. The compound has long been known as a powerful emetic, and was used in the treatment of schistosomiasis and leishmaniasis. It is used as a resolving agent. It typically is obtained as a hydrate.
Shyam Sundar is an Indian academic and professor at Banaras Hindu University. He works on Infectious Diseases - Leishmaniasis & HIV/AIDS.