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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/06 13:41:00」(JST)

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

It is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.^[1]

Medical uses

Malaria

It is approved by the United States' Food and Drug Administration for use as a treatment and preventive measure against malaria.^[2] 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.^[3] Due to side effects, however, it is no longer recommended as a routine preventive,^[4] but only to treat serious malaria infections or to prevent them in areas where other drugs may not work.^[5]

Other

It has also be used as a treatment and prophylactic measure for toxoplasmosis and Pneumocystis jiroveci pneumonia.^[6]^[7]^[8]^[9]^[10]^[11]

Adverse effects

Adverse effects by incidence include:^[2]^[6]^[12]^[13]

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):

Stevens-Johnson syndrome
Toxic epidermal necrolysis
Agranulocytosis
Aplastic anaemia
Disorder of haematopoietic structure
Drug-induced eosinophilia
Thrombocytopaenia
Liver necrosis
Hepatitis
Jaundice
Hepatomegaly
Nephrotoxicity

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:^[2]^[12]

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 sulfonamide antibiotic that competes with p-aminobenzoic acid in the biosynthesis of folate.^[2] Pyrimethamine serves as a selective inhibitor of protozoal dihydrofolate reductase, hence preventing the synthesis of tetrahydrofolate — the active form of folate.^[2] A great degree of synergy occurs between the two drugs due to their inhibition of two different steps in the biosynthesis of tetrahydrofolate.^[2]

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

References

^ "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.
^ ^a ^b ^c ^d ^e ^f "Pyrimethamine, Sulfadoxine and Pyrimethamine Monograph for Professionals". Drugs.com. Retrieved 9 January 2014.
^ 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.
^ Medical Treatment - Sulphadoxine and Pyrimethamine.
^ Pyrimethamine and Sulfadoxine (Oral Route) - MayoClinic.com.
^ ^a ^b "Fansidar, Pyrimethamine-sulfadoxine (pyrimethamine/sulfadoxine) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 January 2014.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ ^a ^b Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. p. 429. ISBN 978-0-85711-084-8.
^ "FANSIDAR® (sulfadoxine and pyrimethamine)" (PDF). medicines.org.au. Roche Products Pty Limited. 17 April 2008. Retrieved 9 January 2014.

UpToDate Contents

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1. 抗マラリア剤：概要 antimalarial drugs an overview
2. 合併症のない熱帯熱マラリアの治療 treatment of uncomplicated falciparum malaria
3. 妊娠中のマラリアの予防および治療 prevention and treatment of malaria in pregnant women
4. HIVとマラリア hiv and malaria
5. HIV感染患者における肺寄生虫感染症 parasitic pulmonary infections in hiv infected patients

English Journal

Host candidate gene polymorphisms and associated clearance of P. falciparum amodiaquine and fansidar resistance mutants in children less than 5 years in Cameroon.

Ali IM, Evehe MS, Netongo PM, Atogho-Tiedeu B, Akindeh-Nji M, Ngora H, Domkam IK, Diakite M, Baldip K, Ranford-Cartwright L, Mimche PN, Lamb T, Mbacham WF.
Pathogens and global health.Pathog Glob Health.2014 Oct;108(7):323-33. doi: 10.1179/2047773214Y.0000000159. Epub 2014 Nov 12.
BACKGROUND: In this post-hoc analysis, we determined the influence of single nucleotide polymorphisms in host candidate immune genes on the outcome of drug resistant malaria in Cameroon.METHODS: Human DNA from 760 patients from a previous clinical trial was subjected to mass spectrometry-based singl
PMID 25388906

Cotrimoxazole prophylactic treatment prevents malaria in children in sub-Saharan Africa: systematic review and meta-analysis.

Mbeye NM1, ter Kuile FO, Davies MA, Phiri KS, Egger M, Wandeler G; IeDEA-Southern Africa.
Tropical medicine & international health : TM & IH.Trop Med Int Health.2014 Sep;19(9):1057-67. doi: 10.1111/tmi.12352. Epub 2014 Jul 8.
OBJECTIVES: Cotrimoxazole prophylactic treatment (CPT) prevents opportunistic infections in HIV-infected or HIV-exposed children, but estimates of the effectiveness in preventing malaria vary. We reviewed studies that examined the effect of CPT on incidence of malaria in children in sub-Saharan Afri
PMID 25039469

Effectiveness of intermittent preventive treatment with sulfadoxine-pyrimethamine during pregnancy on placental malaria, maternal anaemia and birthweight in areas with high and low malaria transmission intensity in Tanzania.

Mosha D1, Chilongola J, Ndeserua R, Mwingira F, Genton B.
Tropical medicine & international health : TM & IH.Trop Med Int Health.2014 Sep;19(9):1048-56. doi: 10.1111/tmi.12349. Epub 2014 Jun 26.
OBJECTIVE: To assess the effectiveness of IPTp in two areas with different malaria transmission intensities.METHODS: Prospective observational study recruiting pregnant women in two health facilities in areas with high and low malaria transmission intensities. A structured questionnaire was used for
PMID 24965022

Japanese Journal

抗マラリア薬(Fansidar^<【encircled R】>)による発症した薬剤過敏症肝障害の1例

岡崎有博,渡辺勲史,内山順三,中野敦史,西崎泰弘,加川建弘,松崎松平
日本消化器病學會雜誌 = The Japanese journal of gastro-enterology 94(2), 129-132, 1997-02-05
NAID 10005018657

Liver damage associated with Fansidar

WEJISTAL R.
Lancet I, 854-855, 1986
NAID 30005717588

「ファンシダール」

Sulfadoxine/pyrimethamine
Combination of
Sulfadoxine	Sulfonamide
Pyrimethamine	Antiparasitic
Clinical data
Trade names	Fansidar
License data	US FDA: Fansidar;
Pregnancy; category	AU: C; US: C (Risk not ruled out); ;
Routes of; administration	Oral
Legal status
Legal status	AU: S4 (Prescription only); UK: POM (Prescription only); US: ℞-only;
Identifiers
ATC code	P01BD51 (WHO)
(verify)

　　[★]

英: Fansidar
商: FANSIDAR
関: pyrimethamine-sulfadoxine、スルファドキシン・ピリメタミン

「FANSIDAR」

　　[★] ファンシダール pyrimethamine-sulfadoxine

[WHO2015E-1] "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.

[Drugs-2] ^ ^a ^b ^c ^d ^e ^f "Pyrimethamine, Sulfadoxine and Pyrimethamine Monograph for Professionals". Drugs.com. Retrieved 9 January 2014.

[3] 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.

[autogenerated1-4] Medical Treatment - Sulphadoxine and Pyrimethamine.

[5] Pyrimethamine and Sulfadoxine (Oral Route) - MayoClinic.com.

[MSR-6] "Fansidar, Pyrimethamine-sulfadoxine (pyrimethamine/sulfadoxine) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 January 2014.

[7] 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.

[8] 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.

[9] 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.

[10] 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.

[11] 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.

[BNF-12] Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. p. 429. ISBN 978-0-85711-084-8.

[TGA-13] "FANSIDAR® (sulfadoxine and pyrimethamine)" (PDF). medicines.org.au. Roche Products Pty Limited. 17 April 2008. Retrieved 9 January 2014.

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案内

Fansidar