Artemether

Artemether Uses, Dosage, Side Effects, Food Interaction and all others data.

Artemether is a potent and rapidly acting blood schizontocide, which is highly efficacious in treating chloroquine-resistant falciparum malaria, and complicated falciparum malaria including cerebral malaria. Its quick onset of effect and high efficacy in bringing down the parasite load are the properties which make this drug a suitable therapeutic option against falciparum infection.

In the body, artemether is metabolized into the active metabolite metabolite dihydroartemisinin. The drug works against the erythrocytic stages of P. falciparum by inhibiting nucleic acid and protein synthesis. Artemether is administered in combination with lumefantrine for improved efficacy. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thought that artemether provides rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.

Trade Name Artemether
Generic Artemether
Artemether Other Names Artemetero, Artemether, Artemetherum, Artemisininelactol methyl ether, Dihydroartemisinin methyl ether, Dihydroqinghaosu methyl ether, methyl-dihydroartemisinine
Weight 80mg/ml
Type Injection
Formula C16H26O5
Weight Average: 298.3746
Monoisotopic: 298.178023942
Protein binding

Artemether and lumefantrine are both highly bound to human serum proteins in vitro (95.4% and 99.7%, respectively). Dihydroartemisinin is also bound to human serum proteins (47% to 76%).

Groups Approved
Therapeutic Class Anti-malarial drugs
Manufacturer Ciron Drugs & Pharma Pvt Ltd
Available Country India, Nigeria
Last Updated: September 19, 2023 at 7:00 am
Artemether
Artemether

Uses

Artemether is used for Malaria, Schistosomiasis.

Artemether is also used to associated treatment for these conditions: Plasmodium Infections, Acute, uncomplicated Malaria caused by plasmodium falciparum

How Artemether works

Involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species.

The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals.

Dosage

Artemether dosage

Adult: 80 mg twice daily for 1 day followed by 80 mg once daily for 4 days. Maximum dose: 480 mg for 5 days.

Children: 3.2 mg/kg/day in 2 divided doses followed by 1.6 mg/kg/day once daily for 4 days. Maximum dose: 9.6 mg/kg for 5 days.

Side Effects

Mild Gl disturbance, dizziness, tinnitus, reduction in reticulocyte and leucocyte counts, nausea, vomiting, abdominal pain, bradycardia, first degree heart block, transient increase in serum transaminases.

Toxicity

Animal studies on acute toxicity show that the LD50 of Artemether in mice is a single i.g. administration of 895mg/kg and a single i.m. injection of 296mg/kg dose; in rats, the LD50 is a single i.m. injection of 597mg/kg dose.

Precaution

Avoid concomitant use of drugs known to prolong QT interval or monitor such patients.

Interaction

Artemether causes QT prolongation in some patients. Thus concomitant use of erythromycin, terfenadine, procainamide, quinidine, disopyramide, amiodarone, bretylium, bepridil, sotalol, astemizole, probucol, tricyclic antidepressants, phenothiazines may be avoided.

Food Interaction

  • Avoid grapefruit products.
  • Take with food. Food increases absorption.

Elimination Route

Food increases absorption.

Half Life

Artemether, 1.6 +/- 0.7 and 2.2 +/- 1.9 hr; Dihydroartemisinin, 1.6 +/- 0.6 and 2.2 +/- 1.5 hr

Pregnancy & Breastfeeding use

Pregnancy Category-C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks

Contraindication

Contraindicated in patients with hpersensitivity to Artemether.

Innovators Monograph

You find simplified version here Artemether

FAQ

What is Artemether used for?

Artemether is a medication used for the treatment of malaria. The injectable form is specifically used for severe malaria rather than quinine. In adults, it may not be as effective as artesunate. Artemether is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.

How safe is Artemether?

Strong evidence now demonstrates that artemether-lumefantrine (AL) is effective and safe in the treatment of malaria in pregnancy.

How does Artemether work?

Artemether works by killing the organisms that cause malaria.

What are the common side effects of Artemether?

Common side effects of Artemether may include:

  • headache, dizziness;
  • fever, cough, feeling weak or tired;
  • muscle pain, tenderness, or weakness;
  • joint pain;
  • vomiting; or.
  • loss of appetite.

Is Artemether safe during pregnancy?

Artemether is effective and safe in the treatment of pregnancy.

Is Artemether safe during breastfeeding?

Yes, mothers who are taking Artemether may continue to breastfeed, provided they are healthy enough to do so.

Can I drink alcohol with Artemether?

Artemether is safe to drink while taking your malaria tablets. However, as always, it is best to consume alcohol within the recommended guidelines to stay safe and look after your health.

Can I drive after taking Artemether?

Do not drive or operate heavy machinery until you know how this medication affects you.

When should be taken of Artemether?

This Artemether is usually taken twice a day with a meal for 3 days (6 doses).

How often can I take Artemether?

Take your first dose with food, followed by your second dose 8 hours later. Then each day for the next 2 days, take one dose in the morning and one dose in the evening.

How long does it take for Artemether to work?

Artemether is absorbed rapidly, reaching a peak concentration at approximately two hours after dosing. It is quickly hydrolysed to its main active metabolite, dihydroartemisinin (DHA), which also shows a maximum concentration within two to three hours after dosing.

What is the half-life of Artemether?

Artemether is rapidly eliminated from plasma with a half-life of two to three hours, whereas lumefantrine is eliminated more slowly with a half-life of three to six days and provides a high long-term cure rate after a short treatment course.

How long do I have to take Artemether?

You should start the tablets 2 days before you travel and take them each day you're in a risk area, and for 4 weeks after you return.

Who should not take Artemether?

Artemether should not be given to a child younger than 2 months or who weighs less than 11 pounds. Serious drug interactions can occur when certain medicines are used together. Tell your doctor about all your current medicines and any you start or stop using, especially carbamazepine, phenytoin, rifampin, or St. John's wort.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happen if I take too much Artemether?

If you take too much Artemether call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

What happen If I stop taking Artemether?

It is common for travellers to follow different antimalarial medication regimes, but you should not discontinue or change the regime you were prescribed without the advice of a doctor.

Can Artemether affect my kidneys?

Artemether has biological effects by targeting mitochondria and exhibits potential therapeutic value for kidney disease. However, the underlying molecular mechanisms have not been fully elucidated.

Can Artemether affects my liver?

Liver injury associated with the use of artemisinin is extraordinarily rare.

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0000012
http://classyfire.wishartlab.com/tax_nodes/C0000259
http://classyfire.wishartlab.com/tax_nodes/C0001550
http://classyfire.wishartlab.com/tax_nodes/C0002440
http://classyfire.wishartlab.com/tax_nodes/C0001729
http://classyfire.wishartlab.com/tax_nodes/C0001853
http://classyfire.wishartlab.com/tax_nodes/C0002012
http://classyfire.wishartlab.com/tax_nodes/C0003951
http://classyfire.wishartlab.com/tax_nodes/C0004140
http://classyfire.wishartlab.com/tax_nodes/C0001656
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:195280
http://www.hmdb.ca/metabolites/HMDB0015643
http://www.genome.jp/dbget-bin/www_bget?drug:D02483
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=68911
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443251
https://www.chemspider.com/Chemical-Structure.62138.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50022886
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=18343
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=195280
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL566534
https://zinc.docking.org/substances/ZINC000014263142
http://www.pharmgkb.org/drug/PA165111698
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/D8Z
http://www.rxlist.com/coartem-drug.htm
https://www.drugs.com/pro/coartem.html
https://en.wikipedia.org/wiki/Artemether
*** Taking medicines without doctor's advice can cause long-term problems.
Share