Malasaf
Malasaf 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.
Lumefantrine is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with artemether for improved efficacy. This combination therapy exerts its effects against the erythrocytic stages of Plasmodium spp. and may be used to treat infections caused by P. falciparum and unidentified Plasmodium species, including infections acquired in chloroquine-resistant areas.
Lumefantrine is a blood schizonticide active against erythrocytic stages of Plasmodium falciparum. It is thought that administration of lumefantrine with artemether results in cooperate antimalarial clearing effects. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thus thought to provide 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 | Malasaf |
| Generic | Artemether + Artemether + Lumefantrine |
| Weight | 15mg/5ml, 90mg/5ml, 40mg, 240mg, 20mg, 120mg |
| Type | Suspension, Tablet |
| Therapeutic Class | |
| Manufacturer | Saaaf Pharmaceuticals |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Artemether is used for Malaria, Schistosomiasis.
Lumefantrine is an antimalarial agent used in combination with artemether for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum.
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. 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.
Malasaf is also used to associated treatment for these conditions: Plasmodium Infections, Acute, uncomplicated Malaria caused by plasmodium falciparumUncomplicated Malaria caused by Plasmodium falciparum
How Malasaf 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.
The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, available data suggest that lumefantrine inhibits the formation of β-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.
Dosage
Malasaf 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.
Common side effects of combination artemether/lumefantrine therapy in adults include headache, anorexia, dizziness, and asthenia. Common side effects in children include pyrexia, cough, vomiting, anorexia, and headache. Possible serious adverse effects include QT prolongation, bullous eruption, urticaria, splenomegaly (9%), hepatomegaly (adults, 9%; children, 6%), hypersensitivty reaction, and angioedema.
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.
Elimination Route
Food increases absorption.
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
~ 4.5 days
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.
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