Usage
Sulbactam is a β-lactamase inhibitor. It is used in combination with certain beta-lactam antibiotics (like ampicillin and cefoperazone) to enhance their activity against bacteria that produce β-lactamases. These enzymes would normally break down the beta-lactam antibiotic, making it ineffective. Sulbactam itself has little antibacterial activity.
Alternate Names
Sulbactam sodium. No widely recognized international variations exist. Brand names when combined with other medications include Unasyn (with ampicillin) and various regional/international brand names for its combination with cefoperazone.
How It Works
Pharmacodynamics: Sulbactam irreversibly inhibits beta-lactamase enzymes produced by many bacteria. These enzymes typically hydrolyze the beta-lactam ring of antibiotics like ampicillin and cefoperazone, rendering them inactive. By inhibiting these enzymes, sulbactam allows the partner antibiotic to exert its antibacterial effects.
Pharmacokinetics:
- Absorption: Well-absorbed when administered intravenously or intramuscularly.
- Distribution: Widely distributed into most tissues and body fluids, including cerebrospinal fluid. Crosses the placental barrier and is present in low concentrations in breast milk.
- Metabolism: Minimal hepatic metabolism.
- Elimination: Primarily eliminated through renal excretion, with a small amount in bile and feces. The half-life can be prolonged in patients with renal impairment.
Dosage
It’s crucial to understand that sulbactam is always used in conjunction with another beta-lactam antibiotic. Therefore, dosing information here relates to the combination therapies. The specific ratio of sulbactam to the antibiotic will vary depending on the medication.
Standard Dosage
Sulbactam/Ampicillin (Unasyn)
Adults:
- 1.5 g (1 g ampicillin/0.5 g sulbactam) to 3 g (2 g ampicillin/1 g sulbactam) every 6 hours IV or IM. Maximum daily dose of sulbactam is 4 g.
Children:
-
1 month: 100-300 mg/kg/day ampicillin component divided every 6 hours, IV/IM
- Doses up to 400 mg/kg/day have been used for severe infections.
Sulbactam/Cefoperazone
Adults:
- 2-4 g/day (1-2 g cefoperazone activity) IV or IM every 12 hours. Up to 8 g/day in severe infections.
Children:
- 40-80 mg/kg/day (20-40 mg/kg/day cefoperazone activity) every 6-12 hours, IV or IM. Doses can be increased in severe infections.
Special Cases:
Sulbactam/Ampicillin (Unasyn)
- Elderly Patients: Dose adjustment based on renal function.
- Patients with Renal Impairment: Dose adjustment is required. Adjust based on creatinine clearance levels.
- Patients with Hepatic Dysfunction: Generally, no dosage adjustment is suggested, however consider not exceeding 3.0gm of ceftriaxone and sulbactam daily without close monitoring.
Sulbactam/Cefoperazone
- Elderly Patients: Dose adjustment based on renal function.
- Patients with Renal Impairment: Dose adjustment is required.
- Patients with Hepatic Dysfunction: Dose adjustment may be needed in severe cases.
Clinical Use Cases
Dosage recommendations are generally determined by the partner antibiotic and the specific infection being treated, not the clinical setting (intubation, surgical procedures, ICU, etc.). However, these settings may influence the choice of antibiotic combined with sulbactam.
Dosage Adjustments
Dose modifications are necessary based on renal function, hepatic function (in some cases), age and sometimes, other comorbid conditions.
Side Effects
Common Side Effects
- Pain at injection site
- Diarrhea
- Nausea, Vomiting
- Rash
Rare but Serious Side Effects
- Severe allergic reactions (anaphylaxis, Stevens-Johnson syndrome)
- Clostridium difficile-associated diarrhea
- Liver dysfunction
- Blood disorders
Contraindications
- Hypersensitivity to sulbactam, ampicillin, cefoperazone, or any other beta-lactam antibiotics.
- History of cholestatic jaundice/hepatic dysfunction associated with ampicillin/sulbactam
Drug Interactions
- Probenecid: Increases sulbactam and ampicillin blood levels.
- Allopurinol: May increase the risk of rash with ampicillin/sulbactam.
- Aminoglycosides: May have synergistic effects, but avoid mixing in the same IV solution.
- Anticoagulants: Sulbactam/ampicillin can enhance anticoagulant effects.
Pregnancy and Breastfeeding
Sulbactam/ampicillin is pregnancy category B. Small amounts are excreted in breast milk; use with caution while breastfeeding. The potential benefits must be weighed against possible risks.
Drug Profile Summary
- Mechanism of Action: Irreversible beta-lactamase inhibitor
- Side Effects: Injection site pain, diarrhea, nausea, rash; rare but severe reactions include allergic reactions and liver dysfunction.
- Contraindications: Hypersensitivity to beta-lactams, history of cholestatic jaundice/hepatic dysfunction with ampicillin/sulbactam
- Drug Interactions: Probenecid, allopurinol, aminoglycosides, anticoagulants.
- Pregnancy & Breastfeeding: Category B, use with caution during breastfeeding.
- Dosage: Depends on partner antibiotic and indication. Adjustments needed for renal impairment.
- Monitoring Parameters: Renal function tests, liver function tests (if indicated), complete blood count (if indicated), clinical response to therapy.
Popular Combinations
- Ampicillin/sulbactam: Used for a variety of infections, including skin and skin structure infections, intra-abdominal infections, and gynecological infections.
- Cefoperazone/sulbactam: Used for intra-abdominal infections, respiratory tract infections and skin infections.
Precautions
- Careful patient history regarding beta-lactam allergies.
- Monitor renal function, especially in patients with pre-existing renal impairment.
- Observe for signs and symptoms of allergic reactions.
- Monitor for signs and symptoms of Clostridium difficile infection.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Sulbactam?
A: Sulbactam is always used in combination with another beta-lactam antibiotic. The dosage varies depending on the partner antibiotic and the indication. Consult the specific product information.
Q2: How does Sulbactam work?
A: It acts as a beta-lactamase inhibitor, preventing bacteria from breaking down certain antibiotics.
Q3: Can Sulbactam be used in pregnant women?
A: Ampicillin/sulbactam is pregnancy category B. Caution should be exercised.
Q4: What are the common side effects of Sulbactam combinations?
A: Common side effects include pain at the injection site, diarrhea, nausea, and rash.
Q5: Are there any serious side effects of Sulbactam combinations?
A: Rare but serious side effects include severe allergic reactions and Clostridium difficile-associated diarrhea.
Q6: What are the contraindications to using Sulbactam combinations?
A: Contraindications include a history of hypersensitivity to sulbactam or other beta-lactam antibiotics.
Q7: Does Sulbactam interact with other drugs?
A: Yes, it can interact with probenecid, allopurinol, aminoglycosides, and anticoagulants.
Q8: Can Sulbactam combinations be used in patients with renal impairment?
A: Yes, but dosage adjustments are required based on creatinine clearance levels.
Q9: How is Sulbactam administered?
A: It is given intravenously or intramuscularly, usually in combination with another beta-lactam antibiotic.
Q10: What should be monitored while a patient is taking sulbactam?
A: Monitor for adverse reactions such as rash, difficulty breathing, hives, and swelling. Pay close attention to renal and liver function with regular testing, as well as signs of superinfection like persistent diarrhea or thrush.
