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Product name | dihydroartemisinin |
Botanical Source | Aertemiisia Annua L. |
Popular combination | dihydroartemisinin-piperaquine (DHA/PQP) |
Synonyms | DHA, Cotecxin , Artekin, dihydroqinghaosu, dihydroartemisinin injection, Duocotecxin artenimol |
CAS Number | 71939-50-9 |
Molecular formula (MF) | C15H24O5 |
Molecular Weight (MW) | 284.35 |
Appearance | White powder |
Package | 25kg/drum |
Solubility | insoluble in water, Soluble in acetone and ethanol |
Melting Point | 140oC |
Dosage | 1.6/12.8 mg/kg per dose |
Main benefits | Anti-malaria, intermediates for artesunate |
Applied industries | Pharmaceuticals, drugs, medicines |
What is Dihydroartemisinin?
Dihydroartemisinin (also known as dihydroqinghaosu, artenimol or DHA), is a drug used to treat malaria. Dihydroartemisinin is the active metabolite of all artemisinin compounds (artemisinin, artesunate,artemether, etc.). It is a semi-synthetic derivative of artemisinin and
Dihydroartemisinin (DHA), according to Wikipedia, is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin has many other names, such as dihydroqinghaosu, artenimol, DHA,etc. It is the active metabolite of all artemisinin compounds (artemisinin, artesunate,artemether, etc.) and is also available as a drug in itself. It is recommended as the first-line anti-malarial drug with low toxicity. DHA has been shown to possess promising anticancer activities and induce cancer cell death through apoptotic pathways. It is also a drug used to treat malaria. The lactone of artemisinin could selectively be reduced with mild hydride-reducing agents, such as sodium borohydride, potassium borohydride, and lithium borohydride to dihydroartemisinin (a lactol) in over 90% yield. is widely used as an intermediate in the preparation of other artemisinin-derived antimalarial drugs, such as artesunate and artemether. Dihydroartemisinin is sold commercially in combination with piperaquine and has been shown to be equivalent to artemether/lumefantrine.
Mechanism of dihydroartemisinin (How dihydroartemisinin works)
Dihydroartemisinin is a type of drug used to treat malaria. It belongs to a class of antimalarial medications that includes artemisinin and artesunate. This particular medication is often prescribed for use in combination with piperaquine. Piperaquine is a similar type of antimalarial medication that metabolizes a bit faster and offsets the delay of this particular medication.
Malaria is a parasitic disease caused by female mosquitos from tropical regions across the world. 22 countries in the Americas, Africa, and Asia have all been affected by outbreaks. The microscopic Plasmodium parasite enters the bloodstream through a bite from an infected female mosquito and travels to the liver where it uses red blood cells to multiply. The body’s immune system does not usually respond to the invasion because the parasite’s residence is in a region that is not monitored by natural defenses.
In many cases, the parasites have genetically mutated to develop a resistance to certain types of treatments such as chloroquine and sulfadoxine-pyrimethamine. Studies show that dihydroartemisinin is an effective treatment medication for resistant cases. It works by preventing the parasites from using glucose in red bloods cells, which is a necessary lifeline for the parasites.
Dihydroartemisinin has strong schizonticidal action, but has no effect on exoerythrocytic, sporogony and gametocyte forms. Dihydroartemisinin, as a drug with biological action of Artesunate and Artemether, has been used for millions of patients. Active mechanism of Dihydroartemisinin has not been known fully. Some researches suggest that the drug concentrates selectively into cells contracted by parasites and reacts with hemin (hemozoin), to kill the parasites. This reaction produces poisonous free radicals that can destroy membranes of parasites in vitro.
Piperaquine, a derivative belongs to 4-aminoquinoline group, is a biquinoline which has the same action mechanism to other quinolines. Piperaquine had been used in China to replace Chloroquine and had paid a key role in prevention and treatment of malaria and most strains of P.falciparum. (except gametocyte). LD50 of Piperaquine is 1098.578.2mg/kg (LD50 of Chloroquine is 427.9 50.4mg/kg). Using Piperaquine is safe and not poisonous.
When using Dihydroartemisinin alone, the rate of recurring after stopping therapy is high. If using Piperaquine alone in prevention chloroquine-resistant P.falciparum, drug-resistance has appeared. Many recent researches confirmed that the safety and effectiveness of the combination of 2 above drugs in treatment of most malarias, not excluding malaria caused by multi-resistant P.falciparum in Vietnam. This combination has overcome the shortcoming of using the single drug. Based on the experience of using Mefloquine, it is made known that the combination with Dihydroartemisinin can slow down the resistance against Piperaquine (the rate of failure in treatment malaria when using Mefloquine alone is 50%; while combination with an artemisinin’s derivative has good effect for 8 years (more than 95%). In clinical trial of this combination, recurrence has appeared lately.(perhaps due to Piperaquine’s long half life).
Benefits of Dihydroartemisinin
The key benefits of Dihydroartemisinin is simple-to treat malaria. It is a very effective anti-malarial drug. For more about how it works, you may read above on the mechanism of action of dihydroartemisinin.
Side effects of taking dihydroartemisinin
While most people do not experience side effects during treatment with dihydroartemisinin, some effects have been reported. Common side effects include minor headaches, nausea, and loss of appetite. Some people may also experience dizziness, loss of energy, and muscle or joint pain. These side effects are temporary and generally subside when the treatment has been completed and the medication is flushed from the body completely.
Rare side effects include an allergic reaction determined by the presence of a rash, itching, or swelling of the lips and tongue. Liver problems can also occur and are distinguished by dark colored urine and jaundice. If these side effects occur while taking dihydroartemisinin, immediate medical care is necessary, as these effects can be serious.
Dihydroartemisinin is not safe for everyone to take. Women who are pregnant or nursing should not take this antimalarial medication because the effects on a baby are unknown. People who have low potassium levels or a history of heart, kidney, or liver diseases should thoroughly weigh the benefits of this medication because it can cause complications with these conditions.
Dosage of taking dihydroartemisinin
The recommended dose for dihydroartemisinin is 120 mg initially, then 60 mg daily for a further 4 to 6 days. It is available in combination with Pipraquine. Doses are calculated as mg/Kg/day. It is given for three days. Maximun 4 tablets each containing 40mg Dihydroartemisinin are indicated for up to 100 Kg weight patient. However, there are no data on which to base a dose recommendation in patients weighing >100kg.