No

Antibiotic, Penicillin

Dental: Parenteral beta-lactamase-resistant antibiotic combination to treat more severe orofacial infections where beta-lactamase-producing staphylococci and beta-lactamase-producing Bacteroides are present

Medical: Treatment of susceptible bacterial infections involved with skin and skin structure, intra-abdominal infections, gynecological infections; spectrum is that of ampicillin plus organisms producing beta-lactamases such as S. aureus, H. influenzae, E. coli, Klebsiella, Acinetobacter, Enterobacter, and anaerobes

B

Hypersensitivity to ampicillin, sulbactam or any component, or penicillins

Dosage adjustment may be necessary in patients with renal impairment; a low incidence of cross-allergy with other beta-lactams exists; high percentage of patients with infectious mononucleosis have developed rash during therapy with ampicillin. Appearance of a rash should be carefully evaluated to differentiate a nonallergic ampicillin rash from a hypersensitivity reaction. Ampicillin rash occurs in 5% to 10% of children receiving ampicillin and is a generalized dull red, maculopapular rash, generally appearing 3-14 days after the start of therapy. It normally begins on the trunk and spreads over most of the body. It may be most intense at pressure areas, elbows, and knees.

>10%: Local: Pain at injection site (I.M.)

1% to 10%:

Dermatologic: Rash

Gastrointestinal: Diarrhea

Local: Pain at injection site (I.V.)

Miscellaneous: Allergic reaction (may include serum sickness, urticaria, bronchospasm, hypotension, etc)

<1%: Chest pain, fatigue, malaise, headache, chills, penicillin encephalopathy, seizures (with large I.V. doses or patients with renal dysfunction), itching, nausea, vomiting, enterocolitis, pseudomembranous colitis, hairy tongue, dysuria, vaginitis, leukopenia, neutropenia, thrombocytopenia, decreased hemoglobin and hematocrit, increased liver enzymes, thrombophlebitis, increased BUN/creatinine, interstitial nephritis (rare)

Symptoms of penicillin overdose include neuromuscular hypersensitivity (agitation, hallucinations, asterixis, encephalopathy, confusion, and seizures) and electrolyte imbalance with potassium or sodium salts, especially in renal failure

Hemodialysis may be helpful to aid in the removal of the drug from the blood, otherwise most treatment is supportive or symptom directed

Decreased effect: Efficacy of oral contraceptives may be reduced

Increased effect: Disulfiram, probenecid results in increased ampicillin levels

Increased toxicity: Allopurinol theoretically has an additive potential for ampicillin rash

I.M. and direct I.V. administration: Use within 1 hour after preparation; reconstitute with sterile water for injection or 0.5% or 2% lidocaine hydrochloride injection (I.M.); sodium chloride 0.9% (NS) is the diluent of choice for I.V. piggyback use, solutions made in NS are stable up to 72 hours when refrigerated whereas dextrose solutions (same concentration) are stable for only 4 hours

The addition of sulbactam, a beta-lactamase inhibitor, to ampicillin extends the spectrum of ampicillin to include some beta-lactamase producing organisms; inhibits bacterial cell wall synthesis by binding to one or more of the penicillin binding proteins (PBPs); which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

Distribution: Into bile, blister and tissue fluids; poor penetration into CSF with uninflamed meninges; higher concentrations attained with inflamed meninges

Protein binding: Ampicillin: 28%; Sulbactam: 38%

Half-life: Ampicillin and sulbactam are similar: 1-1.8 hours and 1-1.3 hours, respectively in patients with normal renal function

Elimination: ~75% to 85% of both drugs are excreted unchanged in the urine within 8 hours following administration

Unasyn® (ampicillin/sulbactam) is a combination product. Each 3 g vial contains 2 g of ampicillin and 1 g of sulbactam. Sulbactam has very little antibacterial activity by itself, but effectively extends the spectrum of ampicillin to include beta-lactamase producing strains that are resistant to ampicillin alone. Therefore, dosage recommendations for Unasyn® are based on the ampicillin component.

Children (3 months to 12 years): 100-200 mg ampicillin/kg/day (150-300 mg Unasyn®) divided every 6 hours; maximum dose: 8 g ampicillin/day (12 g Unasyn®)

Adults: 1-2 g ampicillin (1.5-3 g Unasyn®) every 6-8 hours; maximum dose: 8 g ampicillin/day (12 g Unasyn®)

Dosing interval in renal impairment:

Cl_cr 15-29 mL/minute: Administer every 12 hours

Cl_cr 5-14 mL/minute: Administer every 24 hours

No data reported

With prolonged therapy, monitor hematologic, renal, and hepatic function; monitor for signs of anaphylaxis during first dose

May interfere with urinary glucose tests using cupric sulfate (Benedict's solution, Clinitest®); may inactivate aminoglycosides in vitro

Large I.V. doses may rarely produce encephalopathy; penicillins have been reported to cause apprehension, illusions, agitation, insomnia, depersonalization, and encephalopathy

Rarely may cause bone marrow suppression; use caution with clozapine and carbamazepine

No information available to require special precautions

Prolonged use of penicillins may lead to development of oral candidiasis, some patients may experience hairy tongue

Take entire prescription, even if you are feeling better. Take at equal intervals around-the-clock; preferably on an empty stomach with a full glass of water (1 hour before or 2 hours after meals). Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). If diabetic, drug may cause false tests with Clinitest® urine glucose monitoring; use of glucose oxidase methods (Clinistix®) or serum glucose monitoring is preferable. This drug may interfere with oral contraceptives; an alternate form of birth control should be used. Report rash; unusual diarrhea; vaginal discharge, itching, burning, or pain; mouth sores; unresolved vomiting or constipation; fever or chills; unusual bruising or bleeding; or if condition being treated worsens or does not improve by the time prescription is completed. Breast-feeding precautions: Consult prescriber if breast-feeding.

Ampicillin and gentamicin should not be mixed in the same I.V. tubing or administered concurrently

Powder for injection: 1.5 g [ampicillin sodium 1 g and sulbactam sodium 0.5 g]; 3 g [ampicillin sodium 2 g and sulbactam sodium 1 g]

Dajani AS, "Sulbactam/Ampicillin in Pediatric Infections," Drugs, 1988, 35(Suppl 7):35-8.

Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med, 1988, 318(7):419-26 and 318(8):490-500.

Goldfarb J, Aronoff SC, Jaffé A, et al, "Sultamicillin in the Treatment of Superficial Skin and Soft Tissue Infections in Children," Antimicrob Agents Chemother, 1987, 31(4):663-4.

Itokazu GS and Danziger LH, "Ampicillin-Sulbactam and Ticarcillin-Clavulanic Acid: A Comparison of Their In Vitro Activity and Review of Their Clinical Efficacy," Pharmacotherapy, 1991, 11(5):382-414.

Kulhanjian J, Dunphy MG, Hamstra S, et al, "Randomized Comparative Study of Ampicillin/Sulbactam vs Ceftriaxone for Treatment of Soft Tissue and Skeletal Infections in Children," Pediatr Infect Dis J, 1989, 8(9):605-10.

Meyers BR, Wilkinson P, Mendelson MH, et al, "Pharmacokinetics of Ampicillin-Sulbactam in Healthy Elderly and Young Volunteers," Antimicrob Agents Chemother, 1991, 35(10):2098-101.

Rho SP, Jones A, Woo M, et al, "Single Dose Pharmacokinetics of Intravenous Ampicillin plus Sulbactam in Healthy Elderly and Young Subjects," J Antimicrob Chemother, 1989, 24(4):573-80.

Syriopoulou V, Bitsi M, Theodoridis C, et al, "Clinical Efficacy of Sulbactam/Ampicillin in Pediatric Infections Caused by Ampicillin-Resistant or Penicillin-Resistant Organisms," Rev Infect Dis, 1986, 8(Suppl 5):S630-3.

Wright AJ, "The Penicillins," Mayo Clin Proc, 1999, 74(3):290-307.

Wynn RL and Bergman SA, "Antibiotics and Their Use in the Treatment of Orofacial Infections, Part I and Part II," Gen Dent, 1994, 42(5):398-402, 498-502.