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Artemether injection

Function and Efficacy

1 Pharmacology Artemether is a derivative of artemisinin, which has a strong and rapid killing effect on the erythrocytic stage of malarial parasites and can quickly control clinical attacks and symptoms. The mechanism of action of artemisinin is not very clear, but it mainly interferes with the function of mitochondria, the surface membrane of malarial parasites. Artemisinin changes the membrane structure of malarial parasites by affecting the ultrastructure of the erythrocytic stage. 2 Due to the effect on the food vesicle membrane, the nutritional intake of malarial parasites is blocked. When malarial parasites lose a large amount of cytoplasm and nutrients and cannot be replenished, they die quickly. Its mode of action is through its peroxide (dioxygen) bridge, mediated by the free iron produced after the decomposition of hemoglobin, to produce unstable organic free radicals and/or other electrophilic mediators, and then form covalent adducts with malarial parasite proteins, causing the death of malarial parasites. The antimalarial activity of artemether is 6 times greater than that of artemisinin. 3 Toxicology The LD50 of oral artemether in mice is 895-977 mg/kg, and the LD50 of intramuscular injection of artemether oil in rats is 597 mg/kg. Subacute toxicity tests show that rats were intramuscularly injected with artemether oil at 18 mg/kg per day for 14 days, and there were no other adverse reactions except for a decrease in the number of reticulocytes. This drug has a certain embryotoxicity, which is manifested as embryo absorption.

Ingredients

Main ingredients: Its chemical name is: (3R, 5aS, 6R, 8aS, 9R, 10S, 12R, 12aR)-decahydro-10-methoxy-3,6,9-trimethyl-3,12-oxo-12H-pyrano[4,3-j]-1,2-benzodiphenylamine. Molecular formula: C16H26O5 Molecular weight: 298.4

Name Description Content CAS NO. Manufacturer
ArtemetherIngredients

Artemether is a derivative of artemisinin, which has a strong and rapid killing effect on the erythrocytic stage of malarial parasites and can quickly control clinical attacks and symptoms. It mainly interferes with the function of the mitochondria of the surface membrane of malarial parasites, changes the membrane structure of the erythrocytic stage of malarial parasites by affecting their ultrastructure, blocks the nutritional intake of malarial parasites, and generates unstable organic free radicals and/or other electrophilic mediators mediated by the free iron produced after the decomposition of hemoglobin, which form covalent adducts with malarial parasite proteins and kill malarial parasites. The antimalarial activity of artemether is 6 times greater than that of artemisinin.

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71963-77-4 14

Appearance

Colorless or light yellow clear oily solution.

Indication

It is suitable for the treatment of various types of malaria, including the treatment of chloroquine-resistant falciparum malaria, such as falciparum malaria and vivax malaria.

Usage and Dosage

1 Common adult dose, intramuscular injection, first dose 160 mg, 80 mg once a day from the second day onwards, for 5 consecutive days. 2 Common pediatric dose, intramuscular injection, first dose 3.2 mg/kg body weight; from the second to the fifth day, 1.6 mg/kg body weight once a day.

Adverse Reactions

This product has a mild reaction. Some patients may have a slight increase in aspartate aminotransferase and alanine aminotransferase, and a transient decrease in reticulocytes.

Precautions

Not yet clear.

Drug Interactions

Not yet clear.

Storage

Protect from light, seal tightly and store in a cool place.

Packaging Specification

0.5ml:40mg

Manufacturer

KPC Pharmaceuticals, Inc.

  • Founded in:

    1995-12-14
  • Address:

    No. 166, Keyi Road, High-tech Industrial Development Zone, Kunming, Yunnan Province
  • Tax NO.:

    91530000216562280W
  • Registered Funds:

    757.986969 yuan
  • Website:

  • Email:

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