| 词条 | Sulfadoxine/pyrimethamine | |||||||||||||||||||||
| 释义 |
| verifiedrevid = 447624347 | type = combo | drug_name = | component1 = Sulfadoxine | class1 = Sulfonamide | component2 = Pyrimethamine | class2 = Antiparasitic | tradename = Fansidar, Fanlar, others | pronounce = peer-i-METH-a-meen/sul-fa-DOX-een[1] | Drugs.com = {{drugs.com|cdi|pyrimethamine-sulfadoxine}} | MedlinePlus = | licence_EU = | licence_US = Fansidar | DailyMedID = | pregnancy_AU = C | pregnancy_US = C | pregnancy_category= | legal_AU = S4 | legal_CA = | legal_UK = POM | legal_US = Rx-only | legal_status = | dependency_liability = | routes_of_administration = by mouth | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = | CAS_supplemental = | ATCvet = | ATC_prefix = P01 | ATC_suffix = BD51 | ATC_supplemental = | PubChem = | PubChemSubstance = | IUPHAR_ligand = | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = | UNII_Ref = {{fdacite|correct|FDA}} | UNII = | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = }}Sulfadoxine/pyrimethamine, sold under the brandname Fansidar, is a combination medication used to treat malaria.[1][1] It contains sulfadoxine (a sulfonamide) and pyrimethamine (an antiprotozoal).[4] For the treatment of malaria it is typically used along with other antimalarial medication such as artesunate.[4] Side effects include diarrhea, rash, itchiness, headache, and hair loss.[4][1] Rarely a severe allergic reaction or rash such as toxic epidermal necrolysis, may occur.[1] It is not generally recommended in people with a sulfonamide allergy or significant liver or kidney disease.[2] It is unclear if use during pregnancy is safe for the baby.[3] It works by blocking malaria's ability to use folinic acid.[1] Sulfadoxine/pyrimethamine was initially approved for medical use in the United States in 1981.[1] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[4] The wholesale cost in the developing world is about US$0.08–0.36 per day.[5] It is not currently commercially available in the United States.[6] Medical usesMalariaIt is approved by the United States' Food and Drug Administration for use as a treatment and preventive measure against malaria.[16] The combination is considered to be more effective in treating malaria caused by Plasmodium falciparum than that caused by P. vivax, for which chloroquine is considered more effective, though in the absence of a species-specific diagnosis, the sulfadoxine-pyrimethamine combination may be indicated.[7] Due to side effects, however, it is no longer recommended as a routine preventive,[8] but only to treat serious malaria infections or to prevent them in areas where other drugs may not work.[9] OtherIt has also be used as a treatment and prophylactic measure for toxoplasmosis and Pneumocystis jiroveci pneumonia.[20][10][11][12][13][14] Adverse effectsAdverse effects by incidence include:[15][16][17][18] Common (>1% frequency):
ContraindicationsUse of this drug is contraindicated in:[15][17]
PharmacologySulfadoxine is a sulfonamide antibiotic that competes with p-aminobenzoic acid in the biosynthesis of folate.[15] Pyrimethamine serves as a selective inhibitor of protozoal dihydrofolate reductase, hence preventing the synthesis of tetrahydrofolate — the active form of folate.[15] A great degree of synergy occurs between the two drugs due to their inhibition of two different steps in the biosynthesis of tetrahydrofolate.[15]
See also
References1. ^{{cite book|title=The selection and use of essential medicines: Twentieth report of the WHO Expert Committee 2015 (including 19th WHO Model List of Essential Medicines and 5th WHO Model List of Essential Medicines for Children).|date=2015|publisher=WHO|isbn=9789240694941|pages=435|url=http://apps.who.int/iris/bitstream/10665/189763/1/9789241209946_eng.pdf?ua=1|accessdate=8 December 2016|deadurl=no|archiveurl=https://web.archive.org/web/20161220085929/http://apps.who.int/iris/bitstream/10665/189763/1/9789241209946_eng.pdf?ua=1|archivedate=20 December 2016|df=}} {{Antimalarials}}{{DEFAULTSORT:Sulfadoxine pyrimethamine}}{{portal bar|Pharmacy and pharmacology|Medicine}}2. ^1 2 3 {{cite book|title=WHO Model Formulary 2008|date=2009|publisher=World Health Organization|isbn=9789241547659|pages=187, 198-1999|url=http://apps.who.int/medicinedocs/documents/s16879e/s16879e.pdf|accessdate=8 December 2016|deadurl=no|archiveurl=https://web.archive.org/web/20161213060118/http://apps.who.int/medicinedocs/documents/s16879e/s16879e.pdf|archivedate=13 December 2016|df=}} 3. ^{{cite web|title=Pyrimethamine / sulfadoxine (Fansidar) Use During Pregnancy|url=https://www.drugs.com/pregnancy/pyrimethamine-sulfadoxine.html|website=www.drugs.com|accessdate=11 December 2016|deadurl=no|archiveurl=https://web.archive.org/web/20161220233515/https://www.drugs.com/pregnancy/pyrimethamine-sulfadoxine.html|archivedate=20 December 2016|df=}} 4. ^{{cite web|title=WHO Model List of Essential Medicines (19th List)|url=http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|work=World Health Organization|accessdate=8 December 2016|date=April 2015|deadurl=no|archiveurl=https://web.archive.org/web/20161213052708/http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|archivedate=13 December 2016|df=}} 5. ^{{cite web|title=Sulfadoxine + Pyrimethamine |url=http://mshpriceguide.org/en/single-drug-information/?DMFId=742&searchYear=2014|website=International Drug Price Indicator Guide|accessdate=8 December 2016}} 6. ^1 2 3 4 5 6 {{cite web|title=Pyrimethamine/sulfadoxine: Indications, Side Effects, Warnings - Drugs.com|url=https://www.drugs.com/cdi/pyrimethamine-sulfadoxine.html|website=www.drugs.com|accessdate=11 December 2016|deadurl=no|archiveurl=https://web.archive.org/web/20161220233445/https://www.drugs.com/cdi/pyrimethamine-sulfadoxine.html|archivedate=20 December 2016|df=}} 7. ^JAMA -Abstract: Sulfadoxine-Pyrimethamine, Chlorproguanil-Dapsone, or Chloroquine for the Treatment of Plasmodium vivax Malaria in Afghanistan and Pakistan: A Randomized Controlled Trial, May 23/30, 2007, Leslie et al. 297 (20): 2201 {{webarchive|url=https://web.archive.org/web/20080709084005/http://jama.ama-assn.org/cgi/content/abstract/297/20/2201 |date=2008-07-09 }}. 8. ^Medical Treatment - Sulphadoxine and Pyrimethamine {{webarchive|url=https://web.archive.org/web/20071228220926/http://www.malaria-ipca.com/sulphadoxine_pyrimethamine.html |date=2007-12-28 }}. 9. ^Pyrimethamine and Sulfadoxine (Oral Route) - MayoClinic.com {{webarchive|url=https://web.archive.org/web/20110612153023/http://www.mayoclinic.com/health/drug-information/DR600357 |date=2011-06-12 }}. 10. ^{{cite journal|title=Fansidar - a treatment for AIDS-related pneumocystis?|journal=Postgraduate Medical Journal|volume=63|issue=740|date=June 1987|pages=509–510|doi=10.1136/pgmj.63.740.509-a|pmid=3501583|pmc=2428336|url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2428336/pdf/postmedj00198-0080b.pdf|format=PDF|author1=Bath, PM|author2=Lillicrap, DA|author3=Winter, M|deadurl=no|archiveurl=https://web.archive.org/web/20170910173601/https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2428336/pdf/postmedj00198-0080b.pdf|archivedate=2017-09-10|df=}} 11. ^{{cite journal|title=Prophylaxis of toxoplasmosis infection with pyrimethamine/sulfadoxine (Fansidar) in bone marrow transplant recipients|journal=Bone Marrow Transplantation|date=August 1994|volume=14|issue=2|pages=241–245|pmid=7994239|author1=Foot, AB |author2=Garin, YJ |author3=Ribaud, P |author4=Devergie, A |author5=Derouin, F |author6=Gluckman, E }} 12. ^{{cite journal|title=Administration of pyrimethamine/sulfadoxine for prevention of Pneumocystis carinii pneumonia in patients with AIDS|journal=Clinical Infectious Diseases|volume=20|issue=3|pages=730–731|doi=10.1093/clinids/20.3.730|pmid=7756514|date=March 1995|author=Bessesen, MT; Miller, LA; Cohn, DL; Bartlett, S; Ellison, RT 3rd}} 13. ^{{cite journal|title=[Fansidar in the treatment of toxoplasmosis]|journal=Cesk Slov Oftalmol.|date=July 1996|volume=52|issue=3|pages=173–178|language=Czech|author1=Michalová, K |author2=Ríhová, E |author3=Havlíková, M |pmid=8768475}} 14. ^{{cite journal|title=Twice-weekly pyrimethamine-sulfadoxine effectively prevents Pneumocystis carinii pneumonia relapse and toxoplasmic encephalitis in patients with AIDS|journal=The Journal of Infection|volume=42|issue=1|pages=8–15|date=January 2001|doi=10.1053/jinf.2000.0772|pmid=11243747|author1=Schürmann, D |author2=Bergmann, F |author3=Albrecht, H |author4=Padberg, J |author5=Grünewald, T |author6=Behnsch, M |author7=Grobusch, M |author8=Vallée, M |author9=Wünsche, T |author10=Ruf, B |author11=Suttorp, N }} 15. ^1 2 3 4 5 {{cite web|title=Pyrimethamine, Sulfadoxine and Pyrimethamine Monograph for Professionals|work=Drugs.com|accessdate=9 January 2014|url=https://www.drugs.com/monograph/pyrimethamine-sulfadoxine-and-pyrimethamine.html|deadurl=no|archiveurl=https://web.archive.org/web/20140109145912/http://www.drugs.com/monograph/pyrimethamine-sulfadoxine-and-pyrimethamine.html|archivedate=9 January 2014|df=}} 16. ^1 {{cite web|title=Fansidar, Pyrimethamine-sulfadoxine (pyrimethamine/sulfadoxine) dosing, indications, interactions, adverse effects, and more|work=Medscape Reference|publisher=WebMD|accessdate=9 January 2014|url=http://reference.medscape.com/drug/fansidar-pyrimethamine-sulfadoxine-342694#showall|deadurl=no|archiveurl=https://web.archive.org/web/20140109135919/http://reference.medscape.com/drug/fansidar-pyrimethamine-sulfadoxine-342694#showall|archivedate=9 January 2014|df=}} 17. ^1 {{cite book | isbn = 978-0-85711-084-8 | title = British National Formulary (BNF) | last1 = Joint Formulary Committee | year = 2013 | publisher = Pharmaceutical Press | location = London, UK | edition = 65 | page = 429 }} 18. ^{{cite web|title=FANSIDAR® (sulfadoxine and pyrimethamine)|work=medicines.org.au|publisher=Roche Products Pty Limited|date=17 April 2008|accessdate=9 January 2014|url=http://www.medicines.org.au/files/ropfansi.pdf|format=PDF|deadurl=no|archiveurl=https://web.archive.org/web/20140109142735/http://www.medicines.org.au/files/ropfansi.pdf|archivedate=9 January 2014|df=}} 3 : Antimalarial agents|World Health Organization essential medicines|RTT |
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