Sulfadoxine/pyrimethamine

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Sulfadoxine/pyrimethamine
Combination of
SulfadoxineSulfonamide
PyrimethamineAntiparasitic
Clinical data
Pronunciationpeer-i-METH-a-meen/sul-fa-DOX-een[1]
Trade namesFansidar, Fanlar, others
AHFS/Drugs.comConsumer Drug Information
License data
Pregnancy
category
  • AU: C
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Identifiers
CAS Number
KEGG
  (verify)

Sulfadoxine/pyrimethamine, sold under the brand name Fansidar, is a combination medication used to treat malaria.[1][2] It contains sulfadoxine (a sulfonamide) and pyrimethamine (an antiprotozoal).[3] For the treatment of malaria it is typically used along with other antimalarial medication such as artesunate.[3] In areas of Africa with moderate to high rates of malaria, three doses are recommended during the second and third trimester of pregnancy.[4]

Side effects include

sulfonamide allergy or significant liver or kidney disease.[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.[5] It is not commercially available in the United States.[1]

Medical uses

Malaria

It is approved in the United States as a treatment and preventive measure against malaria.[6] 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] However, it is recommended by the World Health Organization (WHO) for seasonal preventative use in children when combined with amodiaquine.[10]

Other

It has also be used as a treatment and prophylactic measure for

Pneumocystis jiroveci pneumonia.[11][12][13][14][15][16]

Adverse effects

Adverse effects by incidence include:[6][11][17][18]

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:

  • Weight loss
  • Abdominal cramps
  • Hair loss
  • Photosensitivity
  • Fatigue
  • Fever
  • Polyneuritis
  • Atrophic glossitis
  • Gastritis
  • Abnormal liver function test results (e.g. elevated serum ALT, AST, alkaline phosphatase, and bilirubin concentrations)

Contraindications

Use of this drug is contraindicated in:[6][17]

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

Pharmacology

Sulfadoxine is a

tetrahydrofolate — the active form of folate.[6] A great degree of synergy occurs between the two drugs due to their inhibition of two different steps in the biosynthesis of tetrahydrofolate.[6]

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

References

  1. ^ a b c d e f g "Pyrimethamine/sulfadoxine: Indications, Side Effects, Warnings - Drugs.com". www.drugs.com. Archived from the original on 20 December 2016. Retrieved 11 December 2016.
  2. ISSN 0512-3054
    . WHO technical report series;994.
  3. ^ .
  4. ^ "Intermittent preventive treatment in pregnancy (IPTp)". WHO. Archived from the original on 5 March 2014. Retrieved 22 May 2020.
  5. . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  6. ^ a b c d e f "Pyrimethamine, Sulfadoxine and Pyrimethamine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 9 January 2014. Retrieved 9 January 2014.
  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 Archived 9 July 2008 at the Wayback Machine.
  8. ^ "Medical Treatment - Sulphadoxine and Pyrimethamine". Archived from the original on 28 December 2007. Retrieved 31 August 2011.
  9. ^ Pyrimethamine and Sulfadoxine (Oral Route) - MayoClinic.com Archived 12 June 2011 at the Wayback Machine.
  10. .
  11. ^ a b "Fansidar, Pyrimethamine-sulfadoxine (pyrimethamine/sulfadoxine) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 9 January 2014. Retrieved 9 January 2014.
  12. PMID 3501583
    .
  13. .
  14. .
  15. .
  16. .
  17. ^ .
  18. ^ "Fansidar (sulfadoxine and pyrimethamine)" (PDF). medicines.org.au. Roche Products Pty Limited. 17 April 2008. Archived (PDF) from the original on 9 January 2014. Retrieved 9 January 2014.