Name: | Daptomycin |
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PubChem Substance ID: | 12013658 |
Description: | A cyclic lipopeptide antibiotic that inhibits GRAM-POSITIVE BACTERIA. |
Synonyms: |
Cubicin; Dapcin; Daptomycin; LY-146032; Cidecin
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Name: | Daptomycin |
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Name (isomeric): | DB00080 |
Drug Type: | biotech |
Description: | A cyclic lipopeptide antibiotic that inhibits GRAM-POSITIVE BACTERIA. |
Synonyms: |
LY 146032
|
Brand: | Cubicin |
Category: | Anti-Bacterial Agents |
CAS number: | 103060-53-3 |
Indication: | For the treatment of complicated skin and skin structure infections caused by susceptible strains of Gram-positive microorganisms. |
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Pharmacology: |
Daptomycin is a 13 member amino acid cyclic lipopeptide antibiotic active against Gram-positive bacteria only. It has proven in vitro activity against enterococci (including glycopeptide-resistant Enterococci (GRE)), staphylococci (including methicillin-resistant Staphylococcus aureus), streptococci and corynebacteria. Daptomycin is derived ...
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Mechanism of Action: |
Daptomycin appears to bind or insert into the outer membrane of gram positive bacteria. The binding and integration of daptomycin into the cell membrane is calcium dependent. Calcium ions cause a conformational change in daptomycin, augmenting its amphipathicity (hydrophilic head group and hydrophobic tail group), leading to incorporation into the ...
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Protein binding: | Daptomycin is reversibly bound to human plasma proteins, primarily to serum albumin, in a concentration-independent manner. The overall mean binding ranged from 90 to 93%. |
Biotransformation: | Minor amounts of three oxidative metabolites and one unidentified compound have been detected in urine. The site of metabolism has not been identified. |
Route of elimination: | Daptomycin is excreted primarily by the kidney. In a mass balance study of 5 healthy subjects using radiolabeled daptomycin, approximately 78% of the administered dose was recovered from urine based on total radioactivity (approximately 52% of the dose based on microbiologically active concentrations) and 5.7% of the dose was recovered from feces (collected for up to 9 days) based on total radioactivity. Because renal excretion is the primary route of elimination, dosage adjustment is necessary in patients with severe renal insufficiency (CLCR <30 mL/min) |
Half Life: | 7 days |
Affected organisms: | Enteric bacteria and other eubacteria |