أرتزونات
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أرتزونات {{{English
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| الاسم النظامي (أيوپاك) | |
| الاسم النظامي (أيوپاك) | |
| ? | |
| المعينات Identifiers | |
| رقم CAS |
80155-81-3 (sodium salt) |
| كود ATC | P01 |
| PubChem | |
| بيانات كيميائية | |
| الصيغة | 19288 |
| كتلة جزيئية | 384.421 g/mol |
| بيانات الحركية الدوائية Pharmacokinetic | |
| التوافر الحيوي | ? |
| الأيض | ? |
| عمر النصف | ? |
| اخراج | ? |
| اعتبارات علاجية | |
| فئة السلامة أثناء الحمل |
? |
| الوضع القانوني |
Not licensed in UK or US |
| المسارات | oral, IV, IM |
Artesunate آرتيزيونات (INN) جزء منآرتيميزينين مجموعة من الأدوية لعلاج الملاريا . هومشتق شبه مخلق من آرتيميزينين , وهويذوب في الماء, ويمكن إعطاؤه عن طريق الحقن . ويشار اليه أحيانا بالإسم المختصرAS.
الإستعمالات
آرتيزيونات يستحدم أساسا لعلاج الملاريا ولكن ظهر أخيرا قدرته على حتىقد يكون أكثر فعالية بنسبة 90% في تقليل إنتاج البيض في عدوى Schistosoma haematobium .
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 overخمسة 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 or amodiaquine so as to avoid the development of resistance. The combination of artesunate/amodiaquine has been found to be of equivalence to co-artemether.
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. There are as yet no reports of resistance emerging elsewhere.
المراجع
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^ Boulangier D, Dieng Y, Cisse B; et al. "Antischistosomal إذا فعالية هجريبات آرتيزيونات العلاجية المستخدمة كعلاج شافى لإصابات". Trans R Soc Trop Med Hyg. 101 (2): 113–16. doi:10.1016/j.trstmh.2006.03.003. Unknown parameter
|الملاريا year=ignored (help); Explicit use of et al. in:|author=(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. 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. 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. 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. Explicit use of et al. in:
|author=(help)CS1 maint: multiple names: authors list (link) - ^ White NJ (2008). "Qinghaosu (Artemisinin): The price of success". Science. 320 (5874): 330–334. PMID 18420924.
