Artesun (Artesunate 60mg) Inj


UGX8,500

Artesunate

Artesunate (AS) is a medication used to treat malaria.[3][4] The intravenous form is preferred to quinidine for severe malaria.[3] Often it is used as part of combination therapy, such as artesunate plus mefloquine.[4] It is not used for the prevention of malaria.[4] Artesunate can be given by injection into a vein, injection into a muscle, by mouth, and by rectum.[4][5][6]

Artesunate is generally well tolerated.[5] Side effects may include a slow heartbeat, allergic reaction, dizziness, and low white blood cell levels.[4] During pregnancy, it appears to be a safer option, even though animal studies have found harm to the baby.[7] Use is likely okay during breastfeeding.[8] It is in the artemisinin class of medication.[3]

Artesunate was developed by Liu Xu in 1977.[9] It is on the World Health Organization’s List of Essential Medicines, the safest and most effective medicines needed in a health system.[10] The wholesale cost in the developing world is US$2.09 to US$2.57 a dose.[11] It is not commercially available in the United States; however, it can be obtained via the Centers for Disease Control.[3][12] It was originally made from the sweet wormwood plant.[3]

Medical uses

Artesunate is the first-line treatment for children or adults with severe malaria,[13][12] usually in combination with another antimalarial drug. There is moderate-quality evidence that treatment with artesunate plus mefloquine is superior to treatment with artesunate plus amodiaquine or artesunate plus sulfadoxine-pyrimethamine.[14] Artemisinin-based combination therapy may be used by mouth in persons that can tolerate it after 24 hours by injection. In facilities where long-term care is not appropriate, initial treatment with artesunate may be given as a single intramuscular injection or by rectal route (children < 6 years) prior to transferring care to a higher-level facility.

Artesunate is preferred over parenteral quinine for severe malaria treatment.[3] Artesunate was shown to prevent more deaths from severe malaria than quinine in two large multicentre randomized controlled trials from Africa[15] and Asia.[16] A subsequent systematic review of seven randomized controlled trials found this improvement in survival rates to be consistent across all trials.[17]

Artesunate is also used to treat less severe forms of malaria when it can be given orally.[13] It has activity against P. ovaleP. malariae, and severe P. knowlesi.[13]

Artesunate + sulfadoxine/pyrimethamine for the treatment of P. vivax is not recommended due to high rates of resistance.[citation needed]

While artesunate is used primarily as a treatment for malaria, there is some evidence that it may also have some beneficial effects in Schistosoma haematobium infection,[18] but has not been evaluated in large randomized trials.

Although not FDA-approved for use in the United States, artesunate is used as the treatment of choice for severe malaria by the World Health Organization (WHO) over quinidine.[3]

Pregnancy

When given in the second or third trimesters of pregnancy, no artesunate-related adverse pregnancy outcomes have been reported.[19] However, there is insufficient evidence regarding the safety of artesunate use in the first trimester of pregnancy. The WHO recommends that artesunate use for severe malaria in the first trimester should be based on individual risks versus benefits. In the absence of other viable treatment options, the artesunate may be used.[medical citation needed]

Children

Artesunate is safe for use in children. Artesunate + sulfadoxine/pyrimethamine should be avoided in the newborns due to sulfadoxine/pyrmethamine effects on bilirubin.[13] Parenteral artesunate dosing for treatment of severe malaria in children less than 20 kg should be higher than that of adults in order to increase exposure.[13] When artesunate cannot be given orally or intramuscularly due to an individual’s weakness or inability to swallow, rectal administration may be given as pre-referral treatment as long as parenteral administration is initiated after transfer to a more advanced facility

Adverse effects

Artesunate is generally safe and well-tolerated. Artesunate-based regimens are less likely to cause vomiting and tinnitus than quinine plus anti-malarial antibiotic therapy.[20] The best recognized adverse effect of the artemisinins is that they lower reticulocyte counts.[21] This is not usually of clinical relevance.[medical citation needed]

With the increased use of I.V. artesunate, there have been reports of post-artesunate delayed hemolysis (PADH).[22] Delayed hemolysis (occurring around two weeks after treatment) has been observed in patients treated with artesunate for severe malaria.[23]

Contraindications

Artesunate is typically a well-tolerated medicine. Known contraindications include a previous severe allergic reaction to the artesunate.[24]

Drugs that should be avoided while on artesunate are the drugs that inhibit the liver enzyme CYP2A6. These drugs include amiodarone, desipramine, isoniazid, ketoconazole, letrozole, methoxsalen, tranylcypromine.[25]

Mechanisms of action

The mechanisms of action of artesunate remain unclear and debatable. Artesunate is a prodrug that is rapidly converted to its active form dihydroartemisinin (DHA). This process involves the hydrolysis of the 4-carbon ester group via plasma esterase enzyme.[26] It is hypothesized that the cleavage of the endoperoxide bridge in the pharmacophore of DHA generates reactive oxygen species (ROS), which increases oxidative stress and causes malarial protein damage via alkylation.[26] In addition, Artesunate potently inhibits the essential Plasmodium falciparum exported protein 1 (EXP1), a membrane glutathione S-transferase.[27] As a result, the amount of glutathione in the parasite is reduced.[medical citation needed]

In 2016, artemisinin has been shown to bind to a large number of targets, suggesting that it acts in a promiscuous manner.[28] There is evidence suggesting DHA inhibition of calcium-dependent ATPase on endoplasmic membrane, which disrupts protein folding of parasites.[26]

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