أرتزونات

أرتزونات
Artesunate.svg
Artesunate 3D balls.png
البيانات السريرية
النُطقahr-tez′ŭ-nāt[1]
الأسماء التجاريةmany[2]
أسماء أخرىSM-804
AHFS/Drugs.comMicromedex Detailed Consumer Information
License data
مسارات
الدواء
By mouth, intravenous, intramuscular
فئة الدواءArtemisinin
رمز ATC
الحالة القانونية
الحالة القانونية
المعرفات
رقم CAS
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
NIAID ChemDB
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.106.898 Edit this at Wikidata
Chemical and physical data
التركيبC19H28O8
الكتلة المولية384٫43 g·mol−1
3D model (JSmol)
 ☒NYesY (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

  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.
  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.