Grindar 80 and 480 Artemether and Lumefantrine Tablets

Artemether and Lumefantrine Tablets



Each Uncoated tablet contains

Artemether 80 mg

Lumefantrine 480 mg




GRINDAR comprises a fixed combination of 1 part of Artemether and 6 parts of Lumefantrine. Artemether has quick onset of action while Lumefantrine has longer duration of action. Both exerts their anti-parasitic action at the blood stage of malarial parasite, where they convert the haem (a toxic metabolite produced during haemoglobin breakdown) to nontoxic haemozoin (malaria pigment). Lumefantrine interfaces with the polymerization process, while Artemether generates reactive metabolites as a result of interaction between its peroxide bridge and haem iron. Both components also have a secondary action involving inhibition of nucleic acid and protein synthesis within the malarial parasite. There is a synergism of independent actions of both Artemether and Lumefantrine, which has been shown to potentiate the blood schizontocidal effects. It is also effective against drug resistant strains of P.falciparum malaria. Comprehensive in vitro studies using laboratory maintained and fresh field parasite isolates from different malaria endemic areas have shown marked synergic effect of these two components. Results of comparative clinical trials indicate that this Artemether and Lumefantrine combination also clears gametocytes more rapidly than other conventional antimalarials.




Artemether is absorbed quickly with peak plasma concentrations reaching in about 2 hours after dosing, while absorption of Lumefantrine is started after a lag-time of up to 2 hours, with peak plasma concentration in about 6-8 hours after dosing. Food enhances the absorption of Artemether and Lumefantrine. In healthy volunteers the relative bioavailability of Lumefantnne increases sixteen fold compared with intake on empty stomach. High fat content is conducive for absorption. Food has also been shown to increase the absorption of Lumefantrine in patients with malaria. Usually in acutely ill patients there is a tendency of consuming low fat diet. Absorption of Lumefantrine under fasted conditions is very poor. Patients should therefore be encouraged to take the medication with a normal diet as soon as food can be tolerated.



Artemether and Lumefantrine are both highly bound to human serum proteins in vitro (95.4% and 99.9%, respectively). Artemether is well distributed throughout the body with some affinity for the brown fat and adrenal glands, while Lumefantrine has an affinity for adipose and glandular tissue and to some extent for the lungs, spleen (due to slow elimination from lymphoid tissue) and bone marrow.



Artemether is rapidly and extensively metabolized in human liver microsomes to the biologically active main metabolite dihydroartemisinin (demethylation), predominantly through the enzyme system CYP3A4. Lumefantrine is also metabolized by CYP3A4 in human liver microsomes, where glucuronidation of Lumenfantrine takes place directly, after the oxidative biotransformation. However, Lumafantrine inhibits the cytochrome enzyme CYP2D6.



Artemether is rapidly cleared from plasma with an elimination half-life of about 2 – 3 hours. Lumefantrine is eliminated very slowly with an elimination half-life of 4-6 days in patients with falciparum malaria. Demographic characteristics such as sex and weight appear to have no clinically relevant effects on the pharmacokinetics of Artemether/Lumefantrine unchanged.

Artemether has not been detected in faeces and urine due to its rapid and high-first-pass metabolism, but several metabolites (unidentified) have been detected in both faeces and urine. Lumefantrine is eliminated via the bile in animals with excretion primarily in the faeces. After oral dosing in animals qualitative and quantitative recovery of metabolites in bile and faeces was relatively low, most of the dose being recovered as parent drug.



Artemether/Lumefantrine is indicated for the treatment of uncomplicated P. falciparum malaria including multi-drug resistant strains of P. falciparum. GRINDAR is also effective against the blood stage of P. vivax but not active against hypnozoites.

Artemether/Lumefantrine must be used for the malaria infections acquired in areas where the parasites may be resistant to other anti-malarial drugs.

World Health Organization recommends Artemether/Lumefantrine as a first line treatment for the acute uncomplicated P. falciparum malaria for both multi-drug resistant areas and drug sensitive areas.



Patients with acute malaria are frequently averse to food. The dose may be encouraged to resume normal eating as soon as food can be tolerated since this improves absorption of Artemether and Lumefantrine. In the event of vomiting within 1 hour of administration a repeat dose should be taken. 6-dose regimen should be given over 3 days. First dose at the time of initial diagnosis and then at 8, 24, 36, 48 and 60 hours.



Second dose to be taken after 8 hours of first dose.

Better taken with food especially fatty meal.

Body Weight Total Tablets Doses in Number of Tablets
  Initial Dose Initial Dose After 8 hours Day 2 Morning Day 2 Evening Day 3 Morning Day 3 Evening
35kg and above 6 1 1 1 1 1 1



Artemether/Lumefantrine is well tolerated and there is no drug induced serious unwanted side effects. The most common adverse experiences (> 1%) in patients treated with Artemether/Lumefantrine combination are abdominal pain, diarrhoea, vomiting, nausea, palpitation, headeache, dizziness, arthralgia, cough, myalgia, pruritis, rash, asthenia and fatigue. The preclinical investigations and the clinical trial programms revealed no cardiotoxicity with Artemether/Lumefantrine combination, and to date there have been no reports of adverse clinical cardiac events. Recent studies comparing Artemether/Lumefantrine with Halofantrine in human showed a clear distinction between the two substances and confirmed no sign of cardiotoxicity with Artemether/Lumefantrine combination.



In case of suspected over-dosage, symptomic and supportive therapy should be given as appropriate.



Artemether/Lumefantrine is contra-indicated to those patients which have a history of hypersensitivity to Artemether/Lumefantrine.



Pregnancy: There are no adequate data from the use of Artemether/Lumefantrine in pregnant women. Artemether/Lumefantrine treatment should only be considered if the expected benefit to the mother outweighs the risk to the fetus.

Lactation: Artemether/Lumefantrine excretes into breast milk. It should not be taken by breast-feeding women.



Patients who are taking any drug which inhibits the cytochrome enzyme CYP3A4 (e.g. erythromycin, ketoconazole, itraconazole, cimetidine, HIV protease inhibitor, etc.).
Patients who are taking any drug which is metabolized by the cytochrome enzyme CYP2D6 (e.g. flecainide, metoprolol, imiprarnine, amitryptyline, clomipramine etc.).



Yellow color, round shape, biconvex, uncoated tablets.



GRINDAR tablets are available in Alu Alu blister packs of 6 tablets. Such one blister pack in one carton.



Storage: Store below 30oC, Protect From light.

Keep well closed.

Keep out of reach of children.



36 months


Mfg. Lic. No.: G/25/1749



Manufactured by

Globela Pharma Pvt. Ltd.

357, GIDC, Sachin, Surat -394230

Gujarat, India.


Product of

Grandies Healthcare and Services Ltd.

1 Scotland Crescent Aba,

Abia State, Nigeria.

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