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- Pharmacology For Artemether + Lumefantrine
Artemether + Lumefantrine Pharmacology
Artemether + LumefantrineAbout Artemether + LumefantrineN/AMechanism of Action of Artemether + LumefantrineN/APharmacokinets of Artemether + LumefantrineN/AOnset of Action for Artemether + LumefantrineN/ADuration of Action for Artemether + LumefantrineN/AHalf Life of Artemether + LumefantrineN/ASide Effects of Artemether + Lumefantrine1.Fever
14.Potentially fatal:Anaphylactic reactions.
Contra-indications of Artemether + Lumefantrine1.Severe malaria according to the World Health Organisation (WHO) definition, eg malaria affecting the brain, or causing pulmonary oedema or kidney failure.
2.History of an abnormal heart rhythm, present from birth, seen on a heart monitoring trace (ECG) as a 'prolonged QT interval'.
3.History of irregular arrhythmias
6.Disturbances in the levels electrolytes in the blood, eg: hypokalaemia or hypomagnesaemia
Special Precautions while taking Artemether + Lumefantrine1.Severely decreased kidney function.
2.Severely decreased liver function.
4.Should be taken with or after food
5.Avoid drinking grapefruit juice while taking this medicine
6.This medicine may cause fatigue and dizziness. Care to be taken performing potentially hazardous activites
Pregnancy Related InformationContraindicated in first trimestes,
Use with caution in late trimesters
Old Age Related InformationN/ABreast Feeding Related InformationContraindicatedChildren Related InformationN/AIndications for Artemether + LumefantrineTreatment of uncomplicated Plasmodium falciparum malaria in adults, children and infants weighing 5kg and above.Interactions for Artemether + Lumefantrine1.It is recommended that artemether-lumefantrine not be administered concurrently with other antimalarials.
2.Mefloquine administration may reduce bile production, resulting in a reduction in the absorption of lumefantrine by 30 to 40%.
3.Artemether-lumefantrine should not be used concurrently with other drugs known to prolong the QTc interval.
4.It should be used with caution in patients taking drugs metabolized by CYP2D6 or drugs that act as a substrate, inhibitor, or inducer of CYP3A4.
Typical Dosage for Artemether + Lumefantrine(Tablet containing 20 mg artemether and 120 mg lumefantrine)
Treatment with artemether-lumefantrine consists of a six-dose regimen given over 3 days, with doses based on patient age and weight (described below)
1.Adults and children > 35 kg or 12 Years
Four tablets are given as a single dose at the time of diagnosis, followed by four tablets 8 hours later, and then four tablets twice daily for 2 days (a total of 24 tablets over 3 days).
2.Infants and Children < 35 kg or 12 Years
5?14 kg One tablet is given at diagnosis, another tablet 8 hours later, and then 1 tablet twice daily for 2 days (a total of 6 tablets over 3 days).
15?24 kg Two tablets are given at diagnosis, another two tablets 8 hours later, and then two tablets twice daily for 2 days (a total of 12 tablets over 3 days).
25?34 kg Three tablets are given at diagnosis, another three tablets 8 hours later, and then three tablets twice daily for 2 days (a total of 18 tablets over 3 days).
Schedule of Artemether + LumefantrineN/AStorage Requirements for Artemether + LumefantrineKeep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture.
Effects of Missed Dosage of Artemether + LumefantrineTake the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.Effects of Overdose of Artemether + LumefantrineN/A
ArtemetherAbout ArtemetherIt is a derivative of artemesinin. Methylether of dihydroartemisinin, a novel sesquiterpene lactone very rapid schizontocidal, used to treat fever and malaria.Mechanism of Action of ArtemetherIt is a schizonticidal drug. The endoperoxide bridges in Artemether are cleaved by the binding of haeme and liberate highly active free radicals. These radicals bind to membrane proteins and cause lipid peroxidation and damages endoplasmic reticulum. It also inhibits protein synthesis and lysis of the parasite.Pharmacokinets of ArtemetherAbsorption: Artemether is orally well absorbed. Distribution: It is distributed in plasma protein bound form. Metabolism: It is metabolised in the liver to active dihydro artemisninOnset of Action for ArtemetherN/ADuration of Action for ArtemetherN/AHalf Life of Artemether45 minutesSide Effects of Artemether1.Nausea
6.Reduction in reticulocyte and leucocytes count
9.Pain at the site of injection
Contra-indications of Artemether1.Hypersensitivity to Artemether and other Artemisnin derivativesSpecial Precautions while taking Artemether1.Renal impairment
4.Monitor patients on concomitant use of drugs which cause prolongation of QT intervalsPregnancy Related InformationUse with caution
First trimester: contraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationN/AIndications for Artemether1.Multi drug resistant Malaria
3.Chloroquine resistant Malaria
Interactions for ArtemetherErythromycin, terfenadine, astemizole, quinidine, amiodarone, disopyramide, bretylium, bearidil, sotalol, TCAs should be avoided.
Typical Dosage for ArtemetherAdult(IM)80 mg twice daily for 1 day followed by 80 mg once daily for 4 days
Maximum dose: 480 mg for 5 days
Children (IM): 3.2 mg/kg body weight /day in 2 divided dose followed by 1.6 mg / kg body weight / day once daily for 4 days
Maximum dose: 9.6 mg / kg for 5 days
Schedule of ArtemetherHStorage Requirements for ArtemetherStore at 15-30 degree C in a tightly closed container. Protect from heat and moisture.Effects of Missed Dosage of ArtemetherTake the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.Effects of Overdose of ArtemetherGive supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or by inducing emesis. Absorption of the drug can be reduced by administration of activated charcoal. Excretion of the drug can be enhanced by administration of sodium bicarbonate. Haemodialysis can be done in emergency conditions.
LumefantrineAbout LumefantrineLumefantrine is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with artemether for improved efficacy. Lumefantrine is a racemic mixture of a synthetic fluorine derivative and is structurally related to quinine, mefloquine, and halofantrine.Mechanism of Action of LumefantrineIt interferes with the conversion of heme, the toxic intermediate step produced during hemoglobin break-down, to non-toxic hemozoin. Accumulation of heme and free radicals results in parasite death.Pharmacokinets of Lumefantrine1.Absorption:Food increases absorption
2.Distribution: Protein binding 99.7% bound
3.Metabolism:Extensively metabolized in the liver primarily by cytochrome P450 3A4. The major metabolite found in plasma is desbutyl-lumefantrine.
Onset of Action for LumefantrineN/ADuration of Action for LumefantrineN/AHalf Life of Lumefantrine~4.5 daysSide Effects of LumefantrineN/AContra-indications of LumefantrineN/ASpecial Precautions while taking LumefantrineN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Lumefantrine1.Lumefantrine and artemether combination therapy is indicated for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum, including malaria acquired in chloroquine-resistant areas.
2.May also be used to treat uncomplicated malaria when the Plasmodium species has not been identified. Indicated for use in adults and children greater than 5 kg.
Interactions for LumefantrineN/ATypical Dosage for LumefantrineN/ASchedule of LumefantrineN/AStorage Requirements for LumefantrineN/AEffects of Missed Dosage of LumefantrineN/AEffects of Overdose of LumefantrineN/A
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