Artemether + Lumefantrine
Therapeutic Class: Anti-malarial drugs
Pharmacology:
This formulation contains a hard and fast ratio of 1:6 parts of Artemether and Lumefantrine. the location of the antiparasitic action of both components is that the food vacuole of the malarial parasite, where they're thought to interfere with the conversion of haem, a toxic intermediate produced during hemoglobin breakdown, to the non-toxic hemozoin (malaria pigment). Lumefantrine is assumed to interfere with the polymerization process, while Artemether generates reactive metabolites as a result of the interaction between its peroxide bridge and haem iron. Both Artemether and Lumefantrine have a secondary action involving inhibition of macromolecule and protein synthesis within the malarial parasite.
Indications:
Artemether & Lumefantrine may be a fixed combination, which acts as a blood schizontocide. this is often indicated for Treatment and stand by emergency treatment of adults, children, and infants with acute, uncomplicated infection thanks to Plasmodium falciparum or mixed infections including P. falciparum. Because Artemether and Lumefantrine are effective against both drug-sensitive and drug resistance P. falciparum. Artemether & Lumefantrine is additionally recommended for malaria infections acquired in areas where the parasites could also be immune to other antimalarials.
Stand by emergency treatment: Most tourists and business travelers, considered to be non-immune, are going to be ready to obtain prompt medical attention if malaria is suspected. However, a minority in danger of infection could also be unable to get such care within 24 hours of the onset of symptoms, particularly if they're in an isolated location far away from medical services. In such a case, prescribers are advised to issue Artemether & Lumefantrine to be carried by the traveler for self-administration (stand by emergency treatment). Consideration should tend to official guidance regarding the acceptable use of anti-malarial agents.
Dosage & Administration:
Patients with acute malaria are frequently averse to food. The dose should be crazy high fat food or drinks like milk. within the event of vomiting within 1 hour of administration, a repeat dose should be taken.
A standard 3 days treatment schedule with a complete of 6 doses is suggested Dosage in adults and youngsters weighing-
- 35 kg and above: 4 tablets as a single dose at the time of initial diagnosis, again 4 tablets after eight hours, and then 4 tablets twice daily (morning and evening) on each of the following two days (Total course comprises 24 tablets).
- 5 to <15 kg body weight: 1 tablet at the time of initial diagnosis, 1 tablet again after 8 hours, and then 1 tablet twice daily (morning and evening) on each of the following two days (Total course comprises of 6 tablets).
- 15 to <25 kg body weight: 2 tablets as a single dose at the time of initial diagnosis, 2 tablets again after 8 hours, and then 2 tablets twice daily (morning and evening) on each of the following two days (Total course comprises 12 tablets).
- 25 to <35 kg body weight: 3 tablets as a single dose at the time of initial diagnosis, 3 tablets again after 8 hours, and then 3 tablets twice daily (morning and evening) on each of the following two days (Total courses comprises 18 tablets).
Interaction:
Dose adjustment of this mix is taken into account unnecessary when administered in association with ketoconazole. The likelihood of interactions with other drugs is the minimal insight of its short duration of administration and wide therapeutic index. From the study, it had been found that the danger of QTc-prolongation related to IV quinine was enhanced by prior administration of this mix.
Contraindications:
Hypersensitivity to any of the ingredients or excipients; Patients with severe malaria consistent with WHO definition; trimester of pregnancy; Patients with a case history of congenital prolongation of the QTc interval or overtime or with the other clinical condition known to prolong the QTc interval like patients with a history of symptomatic cardiac arrhythmias with clinically relevant bradycardia or with severe cardiac disease; Patients with known disturbance of balance e.g. hypokalaemia or hypomagnesemia; Patients taking any drug which is metabolized by the cytochrome enzyme CYP2D6 (e.g. flecainide, metoprolol, imipramine, amitriptyline, clomipramine).
Side Effects:
It is generally alright tolerated by children and adults, with most adverse effects are of mild to moderate severity and duration. Hypersensitivity, headache, dizziness, disorder, somnolence, smooth muscle contractions, paraesthesia, hypoesthesia, abnormal gait, ataxia, palpitation, cough, abdominal pain, anorexia, diarrhea, vomiting, nausea, pruritus, rash, arthralgia, myalgia, asthenia, fatigue.
Pregnancy & Lactation:
Contraindicated; especially within the trimester of pregnancy. nursing women shouldn't take this preparation. thanks to the long elimination half-life of Lumefantrine (4-6 days), it's recommended that nursing shouldn't resume before day 28 unless the potential benefits to the mother and child outweigh the danger of treatment.
Precautions & Warnings:
If a patient deteriorates whilst taking this mix, alternative treatment for malaria should be started at once. The long elimination half-life of Lumefantrine must be taken under consideration when administering quinine in patients previously treated with this mix. this mix has not been evaluated for: prophylaxis; treatment of cerebral malaria; treatment of severe malaria including pulmonary edema or renal failure; treatment of malaria thanks to P. vivax, P. malariae or P. ovale.
Overdose:
In cases of suspected overdosage, symptomatic and supportive therapy should tend as appropriate. ECG and electrolytes (e.g. potassium) should be monitored.
Storage:
Keep out of the reach of youngsters. Store during a cool and dry place shielded from light.