Usage
- Biapenem is prescribed for severe bacterial infections, including lower respiratory tract infections (pneumonia, bronchitis), complicated urinary tract infections (pyelonephritis), intra-abdominal infections (peritonitis, abdominal abscess), gynecological infections (endometritis, pelvic inflammatory disease), septicemia, and skin and soft tissue infections. It is often used in hospital settings for nosocomial and community-acquired infections caused by multi-resistant bacterial strains.
- Pharmacological Classification: Carbapenem antibiotic.
- Mechanism of Action: Biapenem inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), specifically PBP 1 and 4, leading to bacterial cell death. It exhibits high affinity for PBP 1 and 4 in Pseudomonas aeruginosa and Bacteroides fragilis. It is considered a broad-spectrum antibiotic, effective against both Gram-positive and Gram-negative aerobic and anaerobic bacteria.
Alternate Names
- International and regional variations exist.
- Brand Names: Omegacin, Bianem, Lapenem, Bapogreat, Biapride, Zustpen, Bianem-AF.
How It Works
- Pharmacodynamics: Biapenem exerts bactericidal activity by disrupting the synthesis of bacterial cell walls. Its bactericidal activity against P. aeruginosa and B. fragilis is comparable to or superior to that of imipenem. It’s highly stable against human renal dehydropeptidase-I (DHP-I), an enzyme that can inactivate some other carbapenems.
- Pharmacokinetics:
- Absorption: Administered intravenously, ensuring rapid achievement of therapeutic levels in the bloodstream.
- Metabolism: Minimal metabolism; primarily excreted unchanged in urine. One inactive metabolite is known.
- Elimination: Primarily renal excretion (approximately 70% within 12 hours).
- Mode of Action: Biapenem irreversibly binds to and inactivates PBPs, crucial enzymes for peptidoglycan synthesis in bacterial cell walls. This disruption leads to cell wall instability and bacterial lysis.
- Elimination Pathways: Predominantly renal excretion, with minimal hepatic metabolism.
Dosage
Standard Dosage
Adults:
- 300 mg every 12 hours via intravenous infusion over 30-60 minutes.
- The dosage may be doubled for severe infections (up to 600 mg every 12 hours).
- Maximum daily dose: 1.2 g.
Children:
- Safety and efficacy not fully established in children and adolescents. Limited data available for pediatric use, and caution is advised. Dosages of 10-20 mg/kg every 8 hours have been reported for severe infections. Consult with a specialist regarding dosing adjustments.
- Pediatric safety considerations include close monitoring for adverse effects.
Special Cases:
- Elderly Patients: Close monitoring is recommended, but dose adjustments may not be necessary unless there is renal impairment. Bleeding tendency due to vitamin K deficiency may occur in elderly patients.
- Patients with Renal Impairment: Dose reduction or increased dosing interval may be necessary. For patients with severe renal impairment or on hemodialysis, once-daily administration may be recommended.
- Patients with Hepatic Dysfunction: Limited information available. Exercise caution and consider dose adjustments.
- Patients with Comorbid Conditions: Exercise caution in patients with seizures, CNS disorders, or other comorbid conditions. Close monitoring is necessary.
Clinical Use Cases
- Dosing for specific clinical situations (intubation, surgical procedures, mechanical ventilation, ICU use, emergency situations) should be adjusted based on the type and severity of the infection and the patient’s individual characteristics. Standard dosing guidelines (300 mg every 12 hours, up to 600 mg every 12 hours for severe infections) apply, but close monitoring and potential adjustments are necessary in these critical care settings.
Dosage Adjustments
- Dose modifications are required for patients with renal impairment. Monitor renal function closely during treatment.
Side Effects
Common Side Effects
- Diarrhea, nausea, vomiting, abdominal pain, skin rash, itching, headache, injection site reactions (pain, swelling, redness).
Rare but Serious Side Effects
- Allergic reactions (anaphylaxis), seizures, liver dysfunction (jaundice, elevated liver enzymes), hematologic abnormalities (thrombocytopenia, leukopenia), renal impairment, Clostridium difficile infection, superinfection with resistant bacteria or fungi.
Long-Term Effects
- Data on long-term effects are limited.
Adverse Drug Reactions (ADR)
- Anaphylaxis, severe skin reactions, seizures, severe diarrhea, colitis, pseudomembranous colitis.
Contraindications
- Hypersensitivity to biapenem or other carbapenems.
- Concurrent use with sodium valproate (increased risk of seizures).
- History of severe allergic reactions to beta-lactam antibiotics (penicillins, cephalosporins).
Drug Interactions
- Valproic acid (decreased valproic acid levels).
- Probenecid (increased biapenem levels).
- Neuromuscular blocking agents (increased neuromuscular blockade).
- Anticoagulants (increased risk of bleeding).
Pregnancy and Breastfeeding
- Safety during pregnancy and breastfeeding not established. Use only if potential benefits outweigh risks.
- Animal studies show biapenem excretion in breast milk. Discontinue breastfeeding if treatment with biapenem is necessary.
Drug Profile Summary
- Mechanism of Action: Inhibits bacterial cell wall synthesis by binding to PBPs.
- Side Effects: Diarrhea, nausea, rash, headache, injection site reactions; rarely, anaphylaxis, seizures, liver/renal dysfunction.
- Contraindications: Hypersensitivity to carbapenems, concurrent sodium valproate use.
- Drug Interactions: Valproic acid, probenecid, neuromuscular blockers.
- Pregnancy & Breastfeeding: Safety not established. Use with caution.
- Dosage: 300 mg IV q12h, up to 600 mg q12h for severe infections. Adjust for renal impairment.
- Monitoring Parameters: Renal function, liver function, complete blood count, signs of allergic reactions.
Popular Combinations
- Combinations with other antibiotics may be used in specific clinical scenarios based on identified pathogens and resistance patterns. Consult an infectious disease specialist for guidance.
Precautions
- Renal impairment, history of seizures, CNS disorders, allergy to beta-lactams, pregnancy, breastfeeding.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Biapenem?
A: 300 mg IV every 12 hours, infused over 30-60 minutes. Double the dose for severe infections (up to 600 mg every 12 hours). Maximum daily dose is 1.2 g. Adjust dosage for renal impairment.
Q2: How is Biapenem administered?
A: Intravenous infusion only.
Q3: What are the most common side effects of Biapenem?
A: Diarrhea, nausea, vomiting, rash, headache, and injection site reactions.
Q4: Is Biapenem safe to use during pregnancy?
A: Safety during pregnancy hasn’t been established. Use only if the benefits clearly outweigh the potential risks.
Q5: Can Biapenem be used in patients with renal impairment?
A: Yes, but dosage adjustments are necessary. Close monitoring of renal function is essential.
Q6: What are the contraindications for Biapenem?
A: Hypersensitivity to Biapenem or other carbapenems, concurrent use with sodium valproate.
Q7: Does Biapenem interact with other medications?
A: Yes, clinically significant interactions exist with valproic acid, probenecid, and neuromuscular blocking agents.
Q8: What is the mechanism of action of Biapenem?
A: Biapenem inhibits bacterial cell wall synthesis by binding to and inactivating PBPs, essential enzymes for cell wall construction.
Q9: What infections is Biapenem used to treat?
A: A variety of bacterial infections, including respiratory, urinary tract, intra-abdominal, gynecological, skin and soft tissue infections, and sepsis. It is often used for severe infections and infections caused by multidrug-resistant bacteria.
Q10: How should Biapenem be stored?
A: Store the unopened vials in a cool, dry place away from direct sunlight. Reconstituted solutions should be used promptly or stored according to manufacturer instructions.
