Sulfadoxine/pyrimethamine

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Sulfadoxine/pyrimethamine
Combination of
Sulfadoxine Sulfonamide
Pyrimethamine Antiparasitic
Clinical data
Trade names Fansidar
Licence data US FDA:link
Pregnancy cat.
Legal status
Routes Oral
Identifiers
CAS number  YesY
ATC code P01BD51
 YesY (what is this?)  (verify)

Sulfadoxine/pyrimethamine (Fansidar) is a combination antimalarial drug containing the sulfonamide antibiotic sulfadoxine and the antiprotozoal pyrimethamine.

Medical uses[edit]

Malaria[edit]

It is FDA approved for use as a treatment and preventive measure against malaria.[1] 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.[2] Due to side effects, however, it is no longer recommended as a routine preventive,[3] but only to treat serious malaria infections or to prevent them in areas where other drugs may not work.[4]

Other[edit]

It has also be used as a treatment and prophylactic measure for toxoplasmosis and Pneumocystis jiroveci pneumonia.[5][6][7][8][9][10]

Adverse effects[edit]

Adverse effects by incidence include:[1][5][11][12]

Common (>1% frequency):

  • Hypersensitivity reactions (e.g. itchiness, contact dermatitis, and hives)
  • Myelosuppression
  • Gastrointestinal effects (e.g. nausea, vomiting, and diarrhoea)
  • Headache

Rare (<1% frequency):

Unknown frequency:

  • Abnormal liver function test results (e.g. elevated serum ALT, AST, alkaline phosphatase, and bilirubin concentrations)

Contraindications[edit]

Use of this drug is contraindicated in:[1][11]

  • Megaloblastic anaemia caused by folate deficiency
  • Hypersensitivity to pyrimethamine, sulfonamides, or any ingredient in the formulation
  • Repeated prophylactic (prolonged) use in patients with renal or hepatic failure or blood dyscrasias
  • Infants <2 months of age
  • Prophylaxis in pregnancy at term
  • Prophylaxis in nursing women
  • Acute porphyria

Pharmacology[edit]

Sulfadoxine is a sulfonamide antibiotic that competes with p-aminobenzoic acid in the biosynthesis of folate.[1] Pyrimethamine serves as a selective inhibitor of protozoal dihydrofolate reductase, hence preventing the synthesis of tetrahydrofolate — the active form of folate.[1] A great degree of synergy occurs between the two drugs due to their inhibition of two different steps in the biosynthesis of tetrahydrofolate.[1]

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

See also[edit]

References[edit]

  1. ^ a b c d e f "Pyrimethamine, Sulfadoxine and Pyrimethamine Monograph for Professionals". Drugs.com. Retrieved 9 January 2014. 
  2. ^ 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.
  3. ^ Medical Treatment - Sulphadoxine and Pyrimethamine.
  4. ^ Pyrimethamine and Sulfadoxine (Oral Route) - MayoClinic.com.
  5. ^ a b "Fansidar, Pyrimethamine-sulfadoxine (pyrimethamine/sulfadoxine) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 January 2014. 
  6. ^ Bath, PM; Lillicrap, DA; Winter, M (June 1987). "Fansidar - a treatment for AIDS-related pneumocystis?" (PDF). Postgraduate Medical Journal 63 (740): 509–510. doi:10.1136/pgmj.63.740.509-a. PMC 2428336. PMID 3501583. 
  7. ^ Foot, AB; Garin, YJ; Ribaud, P; Devergie, A; Derouin, F; Gluckman, E (August 1994). "Prophylaxis of toxoplasmosis infection with pyrimethamine/sulfadoxine (Fansidar) in bone marrow transplant recipients". Bone Marrow Transplantation 14 (2): 241–245. PMID 7994239. 
  8. ^ Bessesen, MT; Miller, LA; Cohn, DL; Bartlett, S; Ellison, RT 3rd (March 1995). "Administration of pyrimethamine/sulfadoxine for prevention of Pneumocystis carinii pneumonia in patients with AIDS". Clinical Infectious Diseases 20 (3): 730–731. doi:10.1093/clinids/20.3.730. PMID 7756514. 
  9. ^ Michalová, K; Ríhová, E; Havlíková, M (July 1996). "[Fansidar in the treatment of toxoplasmosis]". Cesk Slov Oftalmol. (in Czech) 52 (3): 173–178. PMID 8768475. 
  10. ^ Schürmann, D; Bergmann, F; Albrecht, H; Padberg, J; Grünewald, T; Behnsch, M; Grobusch, M; Vallée, M; Wünsche, T; Ruf, B; Suttorp, N (January 2001). "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. doi:10.1053/jinf.2000.0772. PMID 11243747. 
  11. ^ a b Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. p. 429. ISBN 978-0-85711-084-8.  edit
  12. ^ "FANSIDAR® (sulfadoxine and pyrimethamine)" (PDF). medicines.org.au. Roche Products Pty Limited. 17 April 2008. Retrieved 9 January 2014.