Omegacin

Omegacin Mechanism of Action

Manufacturer:

Meiji

Distributor:

DKSH
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Full Prescribing Info
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Pharmacology: Mechanism of Action: Biapenem inhibits bacterial cell wall synthesis (by blocking the murein crosslink formation). In particular, biapenem exhibits high affinity for penicillin-binding protein (PBP) 1 and 4 in MSSA and PBP 2 and 4 in E. coli and P. aeruginosa.
Antibacterial Activity (In vitro): Biapenem has a broad antibacterial spectrum against aerobic gram-positive/gram-negative bacteria and anaerobic bacteria, and shows strong antibacterial activity. It also shows strong antibacterial activity against P. aeruginosa resistant to imipenem, meropenem, ceftazidime, ofloxacin and gentamicin. Biapenem exerts bactericidal activity and its bactericidal activity against P. aeruginosa and B. fragilis is equivalent to or better than that of imipenem in particular. In addition, biapenem is more stable than meropenem against human renal dehydropeptidase-I (DHP-I).
Therapeutic Effect on Experimental Infection in Mice: The therapeutic efficacy of biapenem against intraperitoneal infection caused by various bacteria, mixed intraperitoneal infection caused by E. coli and P. aeruginosa, P. aeruginosa infection in leucopenic mice, respiratory infections caused by K. pneumoniae, P. aeruginosa and penicillin-resistant S. pneumoniae and urinary tract infections (UTI) caused by E. coli and P. aeruginosa in mice was equivalent to or better than that of imipenem.
Pharmacokinetics: Plasma Concentration: The plasma concentrations in healthy adults (n=5) after a single administration of 150 mg, 300 mg and 600 mg of biapenem by IV drip infusion over 60 min are shown in Figure 1, and a dose dependency was observed. When biapenem was administered by repeated IV drip infusion, the pharmacokinetics were almost similar to those obtained after a single IV drip infusion and no accumulation of biapenem was observed. (See Table 1 and Figure 1.)

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Body Fluid and Tissue Distribution: When biapenem 300 mg was administered once by IV drip infusion over 30 or 60 min, the maximum concentration in the dead space fluid in the pelvis was 9.6 mcg/mL. The concentrations in the sputum within 6 hrs after administration ranged from 0.1-2.5 mcg/mL.
Metabolism: No metabolites were detected in the plasma following a single IV drip infusion of biapenem 150, 300 and 600 mg or repeated IV drip infusion of 300 and 600 mg in healthy adults (n=5). When biapenem was administered once by IV drip infusion or administered by repeated IV drip infusion, 9.7-23.4% of its total metabolites were excreted in the urine. These metabolites showed no antibacterial activity.
Excretion: When biapenem 150, 300 and 600 mg were administered once by IV drip infusion over 60 min to healthy adults (n=5), the average urinary concentrations of biapenem were, 325.5, 584.8 and 1105.1 mcg/mL, respectively at 0-2 hrs after administration, and 2.4, 4.7 and 21.4 mcg/mL, respectively at 8-12 hrs after administration. The cumulative urinary excretion rates were 62.1%, 63.4% and 64%, respectively at 0-12 hrs after administration.
Plasma Concentrations in Patients with Renal Function Impairment: When biapenem 300 mg was administered once by IV drip infusion over 60 min to patients with renal function impairment (n=3), biapenem disappearance from the plasma was confirmed to be delayed as renal function decreased. (See Table 2 and Figure 2.)

Click on icon to see table/diagram/image


Click on icon to see table/diagram/image

When biapenem was administered twice daily for 7 days, 14 times in total by repeated IV drip infusion over 30 min to patients with moderate renal function impairment with a creatinine clearance (CrCl) of about 50 mL/min, no accumulation of biapenem was observed in the plasma or urine.
Biapenem disappearance from the plasma was confirmed to be delayed when hemodialysis was not performed, following administration of biapenem 300 mg by IV drip infusion over 60 min to patients with renal function impairment requiring hemodialysis (n=5). (See Table 3 and Figure 3.)

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Click on icon to see table/diagram/image
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