أرتزونات

أرتزونات
البيانات السريرية
النُطق	ahr-tez′ŭ-nāt
الأسماء التجارية	many
أسماء أخرى	SM-804
AHFS/Drugs.com	Micromedex Detailed Consumer Information
License data	US DailyMed: Artesunate;
مسارات; الدواء	By mouth, intravenous, intramuscular
فئة الدواء	Artemisinin
رمز ATC	P01BE03 (WHO) P01BF02 P01BF03 P01BF04 P01BF06;
الحالة القانونية
الحالة القانونية	US: ℞-only ;
المعرفات
رقم CAS	88495-63-0 ; as salt: 82864-68-4;
PubChem CID	6917864; as salt: 44410736;
DrugBank	DB09274 ; as salt: DBSALT001279;
ChemSpider	5293084 ; as salt: 23269779;
UNII	60W3249T9M; as salt: CN5E49Z611;
KEGG	D02482;
ChEBI	CHEBI:63918;
ChEMBL	CHEMBL361497 ; as salt: CHEMBL207675;
NIAID ChemDB	112081;
PDB ligand	D95 (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID3042681 ;
ECHA InfoCard	100.106.898
Chemical and physical data
التركيب	C19H28O8
الكتلة المولية	384٫43 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES [H][C@@]12CC[C@@]3(C)OO[C@@]11[C@@]([H])(CC[C@H]2C)[C@@H](C)[C@H](OC(=O)CCC(O)=O)O[C@]1([H])O3;
	InChI InChI=1S/C19H28O8/c1-10-4-5-13-11(2)16(23-15(22)7-6-14(20)21)24-17-19(13)12(10)8-9-18(3,25-17)26-27-19/h10-13,16-17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,16-,17-,18-,19-/m1/s1 ; Key:FIHJKUPKCHIPAT-AHIGJZGOSA-N ;
	(what is this?) (verify)

Artesunate آرتيزيونات (INN) جزء منآرتيميزينين مجموعة من الأدوية لعلاج الملاريا . هو مشتق شبه مخلق من آرتيميزينين , وهو يذوب في الماء, ويمكن إعطاؤه عن طريق الحقن . و يشار اليه أحيانا بالإسم المختصرAS.

. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .

الإستعمالات

آرتيزيونات يستحدم أساسا لعلاج الملاريا ولكن ظهر أخيرا قدرته على أن يكون أكثر فعالية بنسبة 90% في تقليل إنتاج البيض في عدوى Schistosoma haematobium .^[4]

الجرعات

There are no licensed forms of artesunate available in the U.S. or UK. In the UK, artesunate is available on a named patient basis only.

Intravenous dose of IV artesunate:

2.4 mg/kg loading dose over 5 minutes
1.2 mg/kg dose 12 hours later
1.2 mg/kg once daily after that

Artesunate must always be given with another antimalarial such as mefloquine^[5]^[6] or amodiaquine^[7] so as to avoid the development of resistance. The combination of artesunate/amodiaquine has been found to be of equivalence to co-artemether.^[8]

To obtain Artesunate, contact the CDC Malaria Hotline: 770-488-7788 (M-F, 8am-4:30pm, eastern time) or after hours, call 770-488-7100 and request to speak with a CDC Malaria Branch clinician.

التخليق

Artesunate is prepared from dihydroartemisinin (DHA) by reacting it with succinic acid anhydride in basic medium. Pyridine as base/solvent, sodium bicarbonate in chloroform and catalyst DMAP (N,N-dimethylaminopyridine) and triethylamine in 1,2-dichloroethane have been used, with yields of up to 100%. A large scale process involves treatment of DHA in dichloromethane with a mixture of pyridine, a catalytic amount of DMAP and succinic anhydride. The dichloromethane mixture is stirred for 6–9 h to get artesunate in quantitative yield. The product is further re-crystallized from dichloromethane. alpha-Artesunate is exclusively formed (m.p 135–137˚C).

المقاومة للدواء

Clinical evidence of drug resistance has appeared in Western Cambodia, where artemesinin monotherapy is common.^[9] There are as yet no reports of resistance emerging elsewhere.

المراجع

^ "Artesunate definition". Drugs.com. Archived from the original on 20 December 2016. Retrieved 7 December 2016.
^ "Artesunate". Drugs.com. Archived from the original on 20 December 2016. Retrieved 7 December 2016.
^ "Artesunate for injection safely and effectively. See full prescribing information for Artesunate for injection. Artesunate for injection, for intravenous use Initial U.S. Approval: 2020". DailyMed. 5 November 2021. Retrieved 11 March 2022.
^ Boulangier D, Dieng Y, Cisse B; et al. "Antischistosomal إن فعالية تركيبات آرتيزيونات العلاجية المستخدمة كعلاج شافى لإصابات". Trans R Soc Trop Med Hyg. 101 (2): 113–16. doi:10.1016/j.trstmh.2006.03.003. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |الملاريا year= ignored (help)CS1 maint: multiple names: authors list (link)
^ Looareesuwan S, Viravan C, Vanijanonta S; et al. (1992). "Randomised trial of artesunate and mefloquine alone and in sequence for acute uncomplicated falciparum malaria". Lancet. 339 (8797): 821–4. doi:10.1016/0140-6736(92)90276-9. PMID 1347854. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
^ Nosten F, van Vugt M, Price R; et al. (2000). "Effects of artesunate-mefloquine combination on incidence of Plasmodium falciparum malaria and mefloquine resistance in western Thailand: a prospective study". Lancet. 356 (9226): 297–302. doi:10.1016/S0140-6736(00)02505-8. PMID 11071185. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
^ Adjuik M, Agnamey P, Babiker A; et al. (2002). "Amodiaquine-artesunate versus amodiaquine for uncomplicated Plasmodium falciparum malaria in African children: a randomised, multicentre trial". Lancet. 359 (9315): 1365–72. doi:10.1016/S0140-6736(02)08348-4. PMID 11978332. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
^ Meremikwu M, Alaribe A, Ejemot R; et al. (2006). "Artemether-lumefantrine versus artesunate plus amodiaquine for treating uncomplicated childhood malaria in Nigeria: randomized controlled trial". Malar J. 5: 43. doi:10.1186/1475-2875-5-43. PMID 16704735. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link) CS1 maint: unflagged free DOI (link)
^ White NJ (2008). "Qinghaosu (Artemisinin): The price of success". Science. 320 (5874): 330–334. PMID 18420924.

[1] "Artesunate definition". Drugs.com. Archived from the original on 20 December 2016. Retrieved 7 December 2016.

[2] "Artesunate". Drugs.com. Archived from the original on 20 December 2016. Retrieved 7 December 2016.

[FDA_label-3] "Artesunate for injection safely and effectively. See full prescribing information for Artesunate for injection. Artesunate for injection, for intravenous use Initial U.S. Approval: 2020". DailyMed. 5 November 2021. Retrieved 11 March 2022.

[4] Boulangier D, Dieng Y, Cisse B; et al. "Antischistosomal إن فعالية تركيبات آرتيزيونات العلاجية المستخدمة كعلاج شافى لإصابات". Trans R Soc Trop Med Hyg. 101 (2): 113–16. doi:10.1016/j.trstmh.2006.03.003. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |الملاريا year= ignored (help)CS1 maint: multiple names: authors list (link)

[5] Looareesuwan S, Viravan C, Vanijanonta S; et al. (1992). "Randomised trial of artesunate and mefloquine alone and in sequence for acute uncomplicated falciparum malaria". Lancet. 339 (8797): 821–4. doi:10.1016/0140-6736(92)90276-9. PMID 1347854. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)

[6] Nosten F, van Vugt M, Price R; et al. (2000). "Effects of artesunate-mefloquine combination on incidence of Plasmodium falciparum malaria and mefloquine resistance in western Thailand: a prospective study". Lancet. 356 (9226): 297–302. doi:10.1016/S0140-6736(00)02505-8. PMID 11071185. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)

[7] Adjuik M, Agnamey P, Babiker A; et al. (2002). "Amodiaquine-artesunate versus amodiaquine for uncomplicated Plasmodium falciparum malaria in African children: a randomised, multicentre trial". Lancet. 359 (9315): 1365–72. doi:10.1016/S0140-6736(02)08348-4. PMID 11978332. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)

[8] Meremikwu M, Alaribe A, Ejemot R; et al. (2006). "Artemether-lumefantrine versus artesunate plus amodiaquine for treating uncomplicated childhood malaria in Nigeria: randomized controlled trial". Malar J. 5: 43. doi:10.1186/1475-2875-5-43. PMID 16704735. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link) CS1 maint: unflagged free DOI (link)

[9] White NJ (2008). "Qinghaosu (Artemisinin): The price of success". Science. 320 (5874): 330–334. PMID 18420924.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]