Sulfadoxine/pyrimethamine explained

Sulfadoxine/pyrimethamine, sold under the brand name Fansidar, is a combination medication used to treat malaria.[1] It contains sulfadoxine (a sulfonamide) and pyrimethamine (an antiprotozoal). For the treatment of malaria it is typically used along with other antimalarial medication such as artesunate. In areas of Africa with moderate to high rates of malaria, three doses are recommended during the second and third trimester of pregnancy.[2]

Side effects include diarrhea, rash, itchiness, headache, and hair loss. Rarely a severe allergic reaction or rash such as toxic epidermal necrolysis, may occur. It is not generally recommended in people with a sulfonamide allergy or significant liver or kidney disease.[3] It works by blocking malaria's ability to use folinic acid.

Sulfadoxine/pyrimethamine was initially approved for medical use in the United States in 1981. It is on the World Health Organization's List of Essential Medicines.[4] It is not commercially available in the United States.[5]

Medical uses

Malaria

It is approved in the United States as a treatment and preventive measure against malaria. 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.[6] Due to side effects, however, it is no longer recommended as a routine preventive,[7] but only to treat serious malaria infections or to prevent them in areas where other drugs may not work.[8] However, it is recommended by the World Health Organization (WHO) for seasonal preventative use in children when combined with amodiaquine.[9]

Other

It has also be used as a treatment and prophylactic measure for toxoplasmosis and Pneumocystis jiroveci pneumonia.[10] [11] [12] [13] [14]

Adverse effects

Adverse effects by incidence include:[15] [16] [17] [18]

Common (>1% frequency):

Rare (<1% frequency):

Unknown frequency:

Contraindications

Use of this drug is contraindicated in:[15] [17]

Pharmacology

Sulfadoxine 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]

Pharmacokinetics! Pharmacokinetic parameter !! Pyrimethamine !! Sulfadoxine
Half-life 111 hours 169 hours
Cmax 0.2 mg/L 60 mg/L
Tmax 4 hours 4 hours
Protein bound 87% 90%
Excretion Renal (16-30%) Renal (30%)
Metabolism Hepatic Hepatic

Notes and References

  1. Book: ((World Health Organization)) . 2015 . 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) . World Health Organization . Geneva . World Health Organization . 10665/189763 . WHO technical report series;994 . free . 9789241209946 . 0512-3054 .
  2. Web site: Intermittent preventive treatment in pregnancy (IPTp) . https://web.archive.org/web/20140305032600/http://www.who.int/malaria/areas/preventive_therapies/pregnancy/en/ . dead . 5 March 2014 . WHO . 22 May 2020.
  3. Book: WHO Model Formulary 2008 . 2009 . 9789241547659 . ((World Health Organization)) . Stuart MC, Kouimtzi M, Hill SR . 10665/44053 . World Health Organization . World Health Organization . 187–91, 198–200 . free .
  4. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 21st list 2019 . 2019 . 10665/325771 . World Health Organization . World Health Organization . Geneva . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO . free .
  5. Web site: Pyrimethamine/sulfadoxine: Indications, Side Effects, Warnings - Drugs.com. www.drugs.com. 11 December 2016. live. https://web.archive.org/web/20161220233445/https://www.drugs.com/cdi/pyrimethamine-sulfadoxine.html. 20 December 2016.
  6. http://jama.ama-assn.org/cgi/content/abstract/297/20/2201 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
  7. Web site: Medical Treatment - Sulphadoxine and Pyrimethamine . 31 August 2011 . 28 December 2007 . https://web.archive.org/web/20071228220926/http://www.malaria-ipca.com/sulphadoxine_pyrimethamine.html . dead .
  8. http://www.mayoclinic.com/health/drug-information/DR600357 Pyrimethamine and Sulfadoxine (Oral Route) - MayoClinic.com
  9. Book: ((World Health Organization)) . Seasonal malaria chemoprevention with sulfadoxine–pyrimethamine plus amodiaquine in children: a field guide . Geneva . World Health Organization (WHO) . August 2013 . 978-92-4-150473-7 . 10665/85726 . free.
  10. Bath PM, Lillicrap DA, Winter M . Fansidar--a treatment for AIDS-related pneumocystis? . Postgraduate Medical Journal . 63 . 740 . 509–510 . June 1987 . 3501583 . 2428336 . 10.1136/pgmj.63.740.509-a .
  11. Foot AB, Garin YJ, Ribaud P, Devergie A, Derouin F, Gluckman E . Prophylaxis of toxoplasmosis infection with pyrimethamine/sulfadoxine (Fansidar) in bone marrow transplant recipients . Bone Marrow Transplantation . 14 . 2 . 241–245 . August 1994 . 7994239 .
  12. Bessesen MT, Miller LA, Cohn DL, Bartlett S, Ellison RT . Administration of pyrimethamine/sulfadoxine for prevention of Pneumocystis carinii pneumonia in patients with AIDS . Clinical Infectious Diseases . 20 . 3 . 730–731 . March 1995 . 7756514 . 10.1093/clinids/20.3.730 .
  13. Michalová K, Ríhová E, Havlíková M . [Fansidar in the treatment of toxoplasmosis] . cs . Ceska a Slovenska Oftalmologie . 52 . 3 . 173–178 . July 1996 . 8768475 .
  14. Schürmann D, Bergmann F, Albrecht H, Padberg J, Grünewald T, Behnsch M, Grobusch M, Vallée M, Wünsche T, Ruf B, Suttorp N . Twice-weekly pyrimethamine-sulfadoxine effectively prevents Pneumocystis carinii pneumonia relapse and toxoplasmic encephalitis in patients with AIDS . The Journal of Infection . 42 . 1 . 8–15 . January 2001 . 11243747 . 10.1053/jinf.2000.0772 .
  15. Web site: Pyrimethamine, Sulfadoxine and Pyrimethamine Monograph for Professionals. Drugs.com. American Society of Health-System Pharmacists. 9 January 2014. live. https://web.archive.org/web/20140109145912/http://www.drugs.com/monograph/pyrimethamine-sulfadoxine-and-pyrimethamine.html. 9 January 2014.
  16. Web site: Fansidar, Pyrimethamine-sulfadoxine (pyrimethamine/sulfadoxine) dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. 9 January 2014. live. https://web.archive.org/web/20140109135919/http://reference.medscape.com/drug/fansidar-pyrimethamine-sulfadoxine-342694#showall. 9 January 2014.
  17. Book: 978-0-85711-084-8 . British National Formulary (BNF) . Joint Formulary Committee . 2013 . Pharmaceutical Press . London, UK . 65 . 429 .
  18. Web site: Fansidar (sulfadoxine and pyrimethamine). medicines.org.au. Roche Products Pty Limited. 17 April 2008. 9 January 2014. live. https://web.archive.org/web/20140109142735/http://www.medicines.org.au/files/ropfansi.pdf. 9 January 2014.

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