Omegacin

Omegacin

Manufacturer:

Meiji

Distributor:

DKSH
Full Prescribing Info
Contents
Biapenem.
Description
Biapenem has a pH of 4.5-5.8 at 0.15 g (potency)/10 mL (water) and approximately 1 osmotic pressure ratio (OPR) at 300 mg (potency)/100 mL (isotonic sodium chloride solution JP).
Action
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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Click on icon to see table/diagram/image

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
Indications/Uses
Treatment of sepsis, pneumonia, lung abscess, secondary infections in chronic respiratory lesion, complicated cystitis, pyelonephritis, peritonitis, parametritis due to biapenem-susceptible strains of Staphylococcus sp, Streptococcus sp, Streptococcus pneumoniae, Enterococcus sp (excluding Enterococcus faecium), Moraxella sp, Escherichia coli, Citrobacter sp, Klebsiella sp, Enterobacter sp, Serratia sp, Proteus sp, Haemophilus influenzae, Pseudomonas aeruginosa, Acinetobacter sp, Peptostreptococcus sp, Bacteroides sp, Prevotella sp and Fusobacterium sp.
Dosage/Direction for Use
Adults: 1.2 g/day (potency) by IV drip infusion in 2 divided doses over a period of 30-60 min. The dosage may be adjusted according to the patient's age and symptoms; however, the maximum dosage should not exceed 1.2 g/day.
Administration: Omegacin should be administered only by IV drip infusion.
Contraindications
History of shock due to any of the ingredients of Omegacin. Patients under the treatment with sodium valproate. Epileptic seizures may recur (see Interactions).
Special Precautions
History of hypersensitivity to carbapenem, penicillin or cephem antibiotics. Personal or familial predisposition to allergic reactions eg, bronchial asthma, rash or urticaria. Severe renal disorder. (See Pharmacokinetics under Actions.) Poor oral food intake or who are receiving parenteral alimentation and patients in poor general health. Patients should be observed carefully because vitamin K deficiency symptoms may develop. History of epilepsy or patients with central nervous system disorder. Central nervous system disorder eg, convulsion or disturbed consciousness is likely to occur.
Important Precautions: Since no methods are available to reliably predict the potential occurrence of shock or anaphylactoid reaction due to Omegacin, the following measures should be taken: Patients should be carefully interviewed in advance to obtain any past history of such reactions to drugs. Any history of allergy to antibiotics or other agents must be ascertained.
Emergency measures must be readily available for the treatment of shock, when Omegacin is used.
Patients should be resting and kept under careful observation from the beginning until after the end of administration of Omegacin. Patients should be observed especially carefully immediately after the beginning of administration.
Effects on Laboratory Tests: Caution is required in the following: False-positive results may occur in urine glucose tests with Benedict's solution, Fehling's solution and Clinitest, but not with Tes-Tape. Positive results may occur in the direct Coombs' test.
Use in Pregnancy & Lactation: Omegacin should be used in pregnant women or women who may possibly be pregnant only if the expected therapeutic benefits outweigh the possible risks associated with treatment. The safety of Omegacin in pregnant women has not been established.
It is advisable to avoid using Omegacin in lactating mothers. If use of Omegacin is judged to be essential, breastfeeding must be discontinued during treatment. It has been reported that Omegacin is excreted in breast milk in animal studies (rats).
Use in Children: The safety of Omegacin in low birth weight infants, newborns, suckling infants, infants and children has not been established.
Use in the Elderly: Special attention should be paid to the following points when Omegacin is used in elderly patients. Omegacin should be used with care and the dose and dosing interval must be adjusted based on careful clinical observation of the patient's condition. (See Pharmacokinetics under Actions.) Adverse reactions are likely to occur in elderly patients since they often have reduced physiological function. In elderly patients, use of Omegacin may be associated with the development of a bleeding tendency due to vitamin K deficiency.
Use In Pregnancy & Lactation
Omegacin should be used in pregnant women or women who may possibly be pregnant only if the expected therapeutic benefits outweigh the possible risks associated with treatment. The safety of Omegacin in pregnant women has not been established.
It is advisable to avoid using Omegacin in lactating mothers. If use of Omegacin is judged to be essential, breastfeeding must be discontinued during treatment. It has been reported that Omegacin is excreted in breast milk in animal studies (rats).
Adverse Reactions
Adverse reactions were observed in 64 (2.7%) of 2348 cases evaluated in the clinical study. The main adverse reactions were rash (1%) and diarrhea (including loose stool) (0.7%). In a total of 2287 cases, 522 events of abnormal changes in laboratory test values were observed in 304 cases (13.3%), including increased ALT (GPT) in 144 cases, increased AST (GOT) in 93 cases and eosinophilia in 77 cases (based on the number of patients summed up at the time of the latest approval of indications).
Clinically Significant Adverse Reactions: Shock (<1%) or anaphylactoid reactions (incidence unknown) may occur. Patients should be carefully monitored and if any abnormalities eg, feeling unwell, oral cavity discomfort, stridor, vertigo, defecation desire, tinnitus or diaphoresis are observed, administration should be discontinued and appropriate measures should be taken.
Interstitial pneumonia (0.1 to <5%) may occur. Patients should be carefully monitored and if any abnormalities eg, fever, cough, exertional breathlessness and dyspnea are observed, a chest X-ray should be obtained immediately. When interstitial pneumonia is suspected, administration should be discontinued and appropriate measures eg, administration of adrenocortical hormones should be taken.
Serious colitis with diarrhea or bloody stool eg, pseudomembranous colitis (incidence unknown) may occur. Patients should be carefully monitored and if any abnormality is observed, administration should be discontinued immediately and appropriate measures should be taken.
Central nervous system disorder eg, convulsion or disturbed consciousness (incidence unknown) may occur. Patients should be carefully monitored and if such symptoms occur, administration should be discontinued immediately and appropriate measures should be taken. Since convulsion or disturbed consciousness is more likely to occur in patients with renal disorder or central nervous system disorder, special attention should be given when Omegacin is administered to such patients.
Hepatic function disorder with markedly increased AST (GOT), ALT (GPT), γ-GTP or AL-P or jaundice (incidence unknown) may occur. Patients should be carefully monitored, and periodic laboratory tests should be performed. If any abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Serious renal disorder eg, acute renal failure (incidence unknown) may occur. Patients should be carefully monitored, and periodic laboratory tests should be performed. If any abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Agranulocytosis, pancytopenia, leucopenia or thrombocytopenia (incidence unknown) may occur. Patients should be carefully monitored, and periodic blood tests should be performed. If any abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Clinically Significant Adverse Reactions (Similar Drugs): Muco-cutaneo-ocular syndrome (Stevens-Johnson syndrome) or toxic epidermal necrolysis (Lyell syndrome) may occur when other carbapenem antibiotics are used. Patients should be carefully monitored, and if any abnormalities eg, fever, erythema, itching, ocular hyperemia or stomatitis are observed, administration should be discontinued and appropriate measures should be taken.
Hemolytic anemia may occur when other carbapenem antibiotics are used. Patients should be carefully monitored, and periodic blood tests should be performed. If any abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Thrombophlebitis may occur when other carbapenem antibiotics are used. Patients should be carefully monitored, and if any abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Pulmonary infiltrates with eosinophilia (PIE) syndrome may occur when other carbapenem antibiotics are used. Patients should be carefully monitored, and if any abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Fulminant hepatitis may occur when other carbapenem antibiotics are used. Patients should be carefully monitored, and if any abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Other Adverse Reactions: When the following adverse reactions occur, appropriate measures should be taken to treat the symptoms. (See Table 4).

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Drug Interactions
Omegacin should not be co-administered with the following drugs: Sodium valproate, depakene, valerin, hyserenin. Blood levels of valproate may be decreased and epileptic seizures may recur. The mechanism is unknown.
Caution For Usage
After Dissolution: After Omegacin is dissolved, the solution should be used promptly. Even if Omegacin has to be stored for unavoidable reasons, it must be stored at room temperature (<25°C) and IV drip infusion must be completed within 6 hrs. If Omegacin is dissolved in isotonic sodium chloride solution (JP) and stored under refrigeration (≤8°C), IV drip infusion must be completed within 24 hrs. Preparation of the Solution for Injection: Water for injection must not be used as a solvent, because the solution would then not be isotonic. Omegacin should be dissolved in isotonic sodium chloride solution or glucose injection, etc. Omegacin must not be mixed with an amino-acid preparation containing L-cysteine or L-cystine because mixing with such a preparation reduces the potency of biapenem.
Storage
Store below 30°C.
MIMS Class
ATC Classification
J01DH05 - biapenem ; Belongs to the class of carbapenems. Used in the systemic treatment of infections.
Presentation/Packing
Powd for inj (vial) 300 mg (crystalline, white to pale yellowish white) x 10's.
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