Falcynate Group Is antimalarial Artemisinin Derivatives
The WHO accorded high priority to the development of fast acting artemisinin derivatives for the treatment of cerebral malaria as well as for the control of multi-drug resistant P. falciparum malaria.
Falcynate Kit (Artesunate + Sulfadoxine + Pyrimethamine)Tablets are a treatment for all forms of malaria due to Plasmodium falciparum, Plasmodium vivax, Plasmodium ovale and Plasmodium malariae.
A water soluble ester called artesunate (Falcynate Injection) and two oil soluble preparations called artemether and arteether (falcy) have now been developed.
Falcynate LF (Artemether and Lumefantrine) Tablets and Dry Syrup are a highly effective and well tolerated antimalarial that achieves cure rates of up to 95%, even in areas of multi-drug resistance. Both components are blood schizontocides.
Falcynate LF is indicated for the treatment of falciparum malaria, the most dangerous form of malaria. This medication is the only pre-qualified, fixed-dose ACT combining artemether, an artemisinin derivative, and lumefantrine. This fixed-dose combination is of great benefit to patients as it facilitates treatment compliance and supports optimal clinical effectiveness.
Anti malarial activity:
They act by inhibiting a P falciparum-encoded sarcoplasmic-endoplasmic reticulum calcium ATPase,.
Most clinically important artemisinins are metabolised to dihydroartemisinin (elimination half-life of about 45 min), in which form they have comparable antimalarial activity.
However, their use in monotherapy is associated with high incidences of recrudescent infection, suggesting that combination with other antimalarials might be necessary for maximum efficacy.
It is the fastest acting anti malarial available. It inhibits the development of the trophozoites and thus prevents progression of the disease.
These drugs starts acting within 12 hours.
These properties of the drug are very useful in managing complicated P. falciparum malaria. These drugs are also effective against the chloroquine resistant strains of P. falciparum.
Meta analysis of mortality in trials indicated that a patient treated with artemether had at least an equal chance of survival as a patient treated with quinine. It has also been reported that artemisinin drugs cleared parasites faster than quinine in patients with severe malaria but fever clearance was similar. Also, parenteral artemether and artesunate are easier to use than quinine and do not induce hypoglycaemia.
Absorption, fate and excretion:
Artemisinin derivatives are absorbed well after intra muscular or oral administration. The drug is fully metabolised and the major metabolite is dihydroartemisinin, which also has anti parasite effects. It is rapidly cleared, predominantly through the bile.