Artemether-Lumefantrine (Coartem®)

ARTEMETHER-LUMEFANTRINE (COARTEM ®)

Pharmacology and Metabolism

Artemether and lumefantrine 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.

Coartem can cause anaphylactic reactions. The drug frequently causes headache, dizziness and anorexia, although mild forms in most cases. Other fairly common side effects (more than 3% of patients) include sleep disorder, tinnitus, tremor, palpitation, as well as unspecific reactions like vertigo, gastrointestinal disorders, itch and nasopharyngitis.

Mechanism of action

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.

Weight

Average: 298.3746

Monoisotopic: 298.178023942

Chemical Formula

C16H26O5

Synonyms

Artemetero
Artemether
Artemetherum
Artemisininelactol methyl ether
Dihydroartemisinin methyl ether
Dihydroqinghaosu methyl ether
methyl-dihydroartemisinine

Pharmacodynamics

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.

Comments

BREAST (MAMMARY GLAND)

INTRODUCTION The mammary gland (breast) is a conical shape modified sweat gland present in the superficial fascia of the pectoral region. The mammary gland is found in both sexes. However, it remains rudimentary in male but becomes well developed in female at puberty. LOCATION The breast is located in the superficial fascia of the pectoral region. A small extension from its superolateral part (axillary tail of Spence) however pierces the deep fascia and extends into the axilla. The aperture in the deep fascia through which axillary tail passes into the axilla is called foramen of Langer. The axillary tail is the site of high percentage of breast tumor. SHAPE It is hemispherical in shape LOCATION AND EXTENT Vertically, it extends from 2nd rib to 6th rib. Horizontally it extends from lateral border of the sternum to the mid-axillary area. DEEP RELATIONS The deep surface of the breast is related to the following structures in that order 1. The breast lies on t...

METRONIDAZOLE (FLAGYL)

METRONIDAZOLE INTRODUCTION AND CHEMISTRY Metronidazole, an antibiotic and antiprotozoal medication. It is used either alone or with other antibiotics to treat pelvic inflammatory disease, endocarditis, and bacterial vaginosis. It is effective for dracunculiasis, giardiasis, trichomoniasis, and amebiasis. Formula: C6H9N3O3 Molar mass: 171.16 g/mol CAS ID: 443-48-1 PubChem CID: 4173 Adult and Pediatric Dosage Forms and Strengths Capsule 375mg Tablet 250 mg 500 mg Tablet, extended-release 750 mg Infusion solution 500 mg/100mL What Are Side Effects Associated with Using Metronidazole? Common Side effects of Metronidazole include: Appetite loss Yeast infection (candidiasis) Diarrhea Dizziness Headache Nausea Vomiting Loss of control of bodily movements Dark urine Disulfiram-type reaction with ethanol Furry tongue Hypersensitivity Low white blood cell count (neutropenia) Metallic taste Neuropathy Pancreatitis Seizures Blood clot (thrombophlebitis) Dry mouth Brain disease (encepha...

Tetracycline

Pharmacology of Tetracycline Introduction Tetracycline, sold under the brand name Sumycin among others, is an oral antibiotic in the tetracyclines family of medications, used to treat a number of infections, including acne, cholera, brucellosis, plague, malaria, and syphilis. Common side effects include vomiting, diarrhea, rash, and loss of appetite. Formula : C 22 H 24 N 2 O 8 IUPAC ID : (4S,6S,12aS)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxonaphthacene-2-carboxamide Molar mass : 444.435 g/mol CAS ID : 60-54-8 Elimination half-life : 8–11 hours, 57–108 hours (kidney impairment) Metabolism : Not metabolized DOSAGES OF TETRACYCLINE Capsule / Tablet 250 mg 500 mg Syrup (extemporaneously prepared) 125mg/5mL 5 mg Dosage Considerations – Should be Given as Follows: Chronic Bronchitis , Acute Exacerbation 500 mg orally every 6 hours Acne 250-50...

MEDSCHOOL TV

Search This Blog