artemotil

Action and Spectrum

Actions and Spectrum: 

Action: 

Antimalarial Activity: artemotil is classified as an artemisinin derivative, which is a group of drugs known for their potent antimalarial properties. It is used to treat uncomplicated and severe forms of malaria, including both Plasmodium falciparum and Plasmodium vivax strains. artemotil is highly effective against multidrug-resistant strains of Plasmodium falciparum, making it a valuable tool in malaria control and treatment. 

Spectrum: 

Plasmodium falciparum: This is the deadliest species of malaria parasite and is responsible for most malaria-related deaths. artemotil is highly effective against Plasmodium falciparum, including drug-resistant strains. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Stomach discomfort and pain 

Pain at the injection site 

Body pain 

Dizziness 

Persistent cough 

Nausea/Vomiting 

Headache 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: Do not use artemotil if you have a known hypersensitivity or allergy to the active ingredient or any of the other components in the medication.  

G6PD Deficiency: Individuals with glucose-6-phosphate dehydrogenase (G6PD) deficiency may be at risk of developing hemolysis (destruction of red blood cells) when taking artemotil. artemotil should only be used under strict medical care in these patients, and it should be avoided until the possible advantages outweigh the dangers. 

Severe Hepatic Impairment: artemotil is metabolized by the liver, and its use is not recommended in individuals with severe hepatic impairment due to the potential for drug accumulation and adverse effects. It should be used with caution and at reduced doses in individuals with mild to moderate liver impairment. 

Pregnancy and Breastfeeding: The safety of artemotil in pregnant and breastfeeding women has not been well-established. It is generally avoided during pregnancy, especially during the first trimester, unless the benefits significantly outweigh the risks. It is important to consult a healthcare professional to weigh the potential risks and benefits. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: artemotil is an antimalarial drug. 

Pharmacodynamics:  

artemotil is part of the artemisinin class of antimalarial drugs, which are known for their rapid and potent activity against the malaria parasite. 

It exerts its antimalarial effects by interacting with the heme molecules within the parasites, causing harmful free radicals to be produced and the disruption of the parasite’s membrane structures. 

This results in the destruction of the malaria parasite, making it an effective treatment for uncomplicated falciparum malaria.   

Pharmacokinetics: 

Absorption 

artemotil is typically administered by intramuscular injection, which allows for rapid and complete absorption into the bloodstream. 

Due to its poor oral bioavailability, intramuscular or intravenous administration is preferred to ensure therapeutic drug levels in the body. 

Distribution 

Following its absorption, artemotil disperses throughout the body and has the capability to traverse the blood-brain barrier, which is essential for treating cerebral malaria. 

It is highly lipophilic, which helps it distribute into various tissues, including the liver, spleen, and adipose tissue. 

Plasma protein binding of artemotil is relatively low. 

Metabolism 

artemotil undergoes hepatic metabolism, mainly within the liver, leading to the conversion of the drug into its active metabolite, dihydroartemisinin (DHA). DHA is responsible for the antimalarial activity. 

The metabolism of artemotil involves cytochrome P450 enzymes, particularly CYP3A4. 

Excretion and Elimination 

The primary route of excretion for artemotil and its metabolites is through the urine, with a small fraction excreted in feces. 

The elimination half-life of artemotil is relatively short, typically around 3 to 6 hours, and it is rapidly cleared from the body. 

Adminstartion

Administration:  

artemotil is typically administered by intramuscular injection. The healthcare provider will administer the drug directly into a muscle. The injection site should be chosen carefully. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: artemotil 

Why do we use artemotil?  

artemotil is effective in treating various forms of malaria, including plasmodium falciparum and plasmodium vivax. It is often used in combination with other antimalarial drugs, such as lumefantrine, to enhance its effectiveness and reduce the risk of resistance. 

It is used in cases of severe malaria, including cerebral malaria, where the infection has affected the central nervous system. In such cases, intravenous administration of artemotil may be required for a more rapid response.