Artesunate


Thông tin thuốc gốc
Chỉ định và Liều dùng
Parenteral
Malaria
Adult: Initial treatment in severe cases: 2.4 mg/kg via slow IV bolus over 1-2 minutes or deep IM inj. Repeat after 12 hours and 24 hours then once daily thereafter. Transfer patient to an appropriate full course oral regimen after at least 24 hours of parenteral therapy and once oral medications are tolerated. Concomitant therapy with another antimalarial agent active against Plasmodium liver hypnozoites may be necessary for severe cases due to P. vivax or P. ovale. Consider local guidelines for the appropriate treatment regimen.
Child: ≥20 kg: Same as adult dose.
Hướng dẫn pha thuốc
Reconstitute vial labelled as 60 mg of artesunate with the supplied diluent. IV: Add 5 mL of 5% glucose or 0.9% NaCl inj to reconstituted solution to obtain 6 mL of artesunate solution with a concentration of 10 mg/mL. IM: Add 2 mL of 5% glucose or 0.9% NaCl inj to reconstituted solution to obtain 3 mL of artesunate solution with a concentration of 20 mg/mL. Administer within 1.5 hours after reconstitution.
Chống chỉ định
Hypersensitivity to artesunate.
Thận trọng
Patient with cardiac and gastrointestinal disease. Hepatic and renal impairment. Children. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Haemolysis, severe haemolytic anaemia, hypersensitivity (including anaphylaxis).
Ear and labyrinth disorders: Tinnitus.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, taste alteration (metallic/bitter taste).
General disorders and administration site conditions: Asthenia, pancreatitis, fever, fatigue, malaise, inj site pain.
Hepatobiliary disorders: Jaundice.
Musculoskeletal and connective tissue disorders: Muscle pain, arthralgia.
Nervous system disorders: Ataxia, balance impairment, restlessness, tremor, dizziness, headache, paresis.
Psychiatric disorders: Confusion.
Renal and urinary disorders: Haemoglobinuria, acute renal failure.
Respiratory, thoracic and mediastinal disorders: Cough, nasal symptoms.
Skin and subcutaneous tissue disorders: Pruritus, rash.
Chỉ số theo dõi
Monitor for signs and symptoms of hypersensitivity and cardiotoxicity (high doses); Hb, reticulocyte count, haptoglobin, lactate dehydrogenase and total bilirubin once weekly for up to 4 weeks after treatment initiation. Monitor for evidence of haemolytic anaemia for 4 weeks after therapy. Consider performing direct antiglobulin test to determine if therapy for immune-mediated haemolysis is needed.
Tương tác
May decrease dihydroartemisinin (DHA) plasma concentration thus reduce efficacy of artesunate with ritonavir, nevirapine or UDP-glucuronosyltransferase (UGT) inducers (e.g. rifampicin, carbamazepine, phenytoin). May increase DHA plasma concentration thereby increase the risk of side effects with UGT inhibitors (e.g. axitinib, vandetanib, imatinib, diclofenac).
Tác dụng
Description: Artesunate is a semisynthetic artemisinin derivative and a prodrug that is metabolised to the active metabolite dihydroartemisinin (DHA). Artesunate and DHA contain endoperoxide bridge that is activated by a heme iron ring binding leading to oxidative stress, protein and nucleic acid synthesis inhibition, ultrastructural changes and decrease in parasite growth and survival. They are active against the blood-stage asexual parasites and gametocytes of Plasmodium species including chloroquine-resistant strains but inactive against the hypnozoite liver stage forms of P. vivax and P. ovale.
Pharmacokinetics:
Absorption: Rapidly absorbed (IM). Time to peak plasma concentration: Within 15 minutes (DHA).
Distribution: Enters the breast milk (DHA). Volume of distribution: 68.5 L (artesunate); 59.7 L (DHA). Plasma protein binding: Approx 93%.
Metabolism: Rapidly hydrolysed by plasma esterases to DHA (active metabolite) which undergoes glucuronidation to form α-DHA-β-glucuronide metabolite.
Excretion: Via urine. Elimination half-life: 0.3 hours (artesunate); 1.3 hours (DHA).
Đặc tính

Chemical Structure Image
Artesunate

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6917864, Artesunate. https://pubchem.ncbi.nlm.nih.gov/compound/Artesunic-acid. Accessed Aug. 24, 2020.

Bảo quản
Store between 15-30°C. Protect from light.
Phân loại MIMS
Thuốc chống sốt rét
Phân loại ATC
P01BE03 - artesunate ; Belongs to the class of artemisinin and derivative antimalarials.
Tài liệu tham khảo
Anon. Artesunate. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/07/2020.

Artesunate (Guilin Pharmaceutical Co., Ltd.). MIMS Thailand. http://www.mims.com/thailand. Accessed 14/07/2020.

Artesunate For Injection (Amivas LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/07/2020.

Artesunate. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com/. Accessed 12/08/2020.

Buckingham R (ed). Artemisinin derivatives. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/07/2020.

Pharba-Arte (Pharbaco Central Pharmaceutical). MIMS Myanmar. http://www.mims.com/myanmar. Accessed 14/07/2020.

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