Description: Biapenem is white to yellowish crystalline powder. Biapenem is a carbopenems antibiotic which suppresses bacterial growth by inhibiting the enzymes responsible for bacterial cell wall synthesis, and shows broad-spectrum antibacterial activity both against gram-positive bacteria and gram-negative bacteria.
Pharmacological effects: Biapenem is a carbopenems antibiotic which suppresses bacterial growth by inhibiting the enzymes responsible for bacterial cell wall synthesis, and shows broad-spectrum antibacterial activity both against gram-positive bacteria and gram-negative bacteria. Biapenem is stable to dehaloperoxidase-I（DHP-I）and can not be administered together with DHP-I inhibitor.
Pharmacokinetics: The pharmacokinetics of biapenem were studied in healthy elderly volunteers aged 65 to 74 years (71.6 ± 2.7 years [mean ± standard deviation], n = 5; group B) and ≥75 years (77.8 ± 1.9 years, n = 5; group C), following single intravenous doses (300 and 600 mg), and compared with those of healthy young male volunteers aged 20 to 29 years (23.0 ± 3.5 years, n = 5; group A). The agent was well tolerated in all three age groups. Serial blood and urine samples were analyzed for biapenem to obtain key pharmacokinetic parameters by both two-compartment model-dependent and -independent methods. The maximum plasma concentration and area under plasma concentration-versus-time curve (AUC) increased in proportion to the dose in all three groups. Statistically significant age-related effects for AUC, total body clearance, and renal clearance (CLR) were found, while elimination half-life (t1/2β) and percent cumulative recovery from urine of unchanged drug (% UR) remained unaltered (t1/2β, 1.51 ± 0.42 [300 mg] and 2.19 ± 0.64 [600 mg] h [group A], 1.82 ± 1.14 and 1.45 ± 0.36 h [group B], and 1.75 ± 0.23 and 1.59 ± 0.18 h [group C]; %UR, 52.6% ± 3.0% [300 mg] and 53.1% ± 5.1% [600 mg] [group A], 46.7% ± 7.4% and 53.0% ± 4.8% [group B], and 50.1% ± 5.2% and 47.1% ± 7.6% [group C]). A significant linear correlation was observed between the CLR of biapenem and creatinine clearance at the dose of 300 mg but not at 600 mg. The steady-state volume of distribution tended to be decreased with age, although not significantly. Therefore, the age-related changes in parameters of biapenem described above were attributable to the combination of decreased lean body mass and lowered renal function of the elderly subjects. However, the magnitude of those changes does not necessitate dosage adjustment in elderly patients with normal renal function for their age.
Indications: Strains sensitive to this product include: staphylococcus, streptococcus, pneumococcus, enterococcus (enterococcus faecium is not included), moraxella, coliform bacilli,
citrobacter, klebsiella, enterobacter, serratia, proteus, haemophilus influenzae, pseudomonas aeruginosa, actinomyces, peptostreptococcus, bacteroides, prevotella, fusiformis. This product is applicable to the treatment of a variety of infections caused by sensitive bacteria: septicemia, pneumonia, lung abscess, secondary infections resulting from Chronic respiratory disease, cystitis, pyelonephritis, peritonitis, appendagitis.
Precautions: This product should be used with caution by patients who are allergic to carbopenems, penicillins and cephalosporins; This product should be used with caution by patients who or whose direct relatives are susceptible to induced hypersensitivities including bronchial asthma, rash, urticaria and so on; Patients with severe renal inadequacy take precautions before using this product; Senile patients should use this product with cautions (see “Medication for senile patients”); When this product is used by the patients with eating difficulty and poor body condition, symptoms of Vitamin k Deficiency may occur; Patients with history of epilepsy and illness of central nervous system shall use this product with caution; False positive findings may occur during clinical Urine Glucose Test, Benedict's test and Fehling’s test for reducing sugar; Positive findings may occur in Kveim test.
Adverse reaction: A clinically significant reduction in serum valproic acid concentration has been reported in patients receiving carbapenem antibiotics and may result in loss of seizure control. Patients concurrently taking valproic acid concentrations should be monitored frequently after initiating carbapenem therapy. Alternative antibacterial or anticonvulsant therapy should be considered if serum valproic acid concentrations drop below the therapeutic range or a seizure occurs.
