INN monograph
Ampicillin + Cloxacillin
Beta-lactam antibiotic — penicillin · POM
Source-linked · Updated 03 Aug 2026 · Source: Local active-ingredient clinical extract; FDA drug label via OpenFDA/DailyMed; Component monographs (multi-source pipeline); Professional class pharmacology (Beta-lactam antibiotic — penicillin)
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Risk first
Contraindications
- CONTRAINDICATIONS The use of ampicillin and sulbactam for injection is contraindicated in individuals with a history of serious hypersensitivity reactions (e.g., anaphylaxis or Stevens-Johnson syndrome) to ampicillin, sulbactam or to other beta-lactam antibacterial drugs (e.g., penicillins and cephalosporins).
- Ampicillin and sulbactam for injection is contraindicated in patients with a previous history of cholestatic jaundice/hepatic dysfunction associated with ampicillin and sulbactam for injection.
Precautions
- WARNINGS Hypersensitivity Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy.
- These reactions are more apt to occur in individuals with a history of penicillin hypersensitivity and/or hypersensitivity reactions to multiple allergens.
- There have been reports of individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins.
- Before therapy with a penicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins, and other allergens.
- If an allergic reaction occurs, ampicillin and sulbactam for injection should be discontinued and the appropriate therapy instituted.
- Hepatotoxicity Hepatic dysfunction, including hepatitis and cholestatic jaundice has been associated with the use of ampicillin and sulbactam for injection.
- Hepatic toxicity is usually reversible
- however, deaths have been reported.
- Hepatic function should be monitored at regular intervals in patients with hepatic impairment.
- Severe Cutaneous Adverse Reactions Ampicillin and sulbactam for injection may cause severe skin reactions, such as toxic epidermal necrolysis (TEN), Stevens-Johnson syndrome (SJS), drug reaction with eosinophilia and systemic symptoms (DRESS), dermatitis exfoliative, erythema multiforme, and acute generalized exanthematous pustulosis (AGEP).
- If patients develop a skin rash they should be monitored closely and ampicillin and sulbactam for injection discontinued if lesions progress (see CONTRAINDICATIONS and ADVERSE REACTIONS sections).
- Clostridioides difficile -Associated Diarrhea Clostridioides difficile -associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including ampicillin and sulbactam for injection, and may range in severity from mild diarrhea to fatal colitis.
Point of care
Dosing
Adult
DOSAGE AND ADMINISTRATION Ampicillin and Sulbactam for Injection may be administered by either the IV or the IM routes. For IV administration, the dose can be given by slow intravenous injection over at least 10 to 15 minutes or can also be delivered in greater dilutions with 50 mL to 100 mL of a compatible diluent as an intravenous infusion over 15 to 30 minutes (see DIRECTION FOR USE-Preparation for Intravenous Use section). Ampicillin and Sulbactam for Injection may be administered by deep intramuscular injection (see DIRECTIONS FOR USE-Preparation for Intramuscular Injection section). The recommended adult dosage of Ampicillin and Sulbactam for Injection is 1.5 g (ampicillin 1 g and sulbactam 0.5 g) to 3 g (ampicillin 2 g and sulbactam 1 g) every six hours. This 1.5 g to 3 g range represents the total of ampicillin content plus the sulbactam content of Ampicillin and Sulbactam for Injection, and corresponds to a range of 1 g ampicillin and 0.5 g sulbactam to 2 g ampicillin and 1 g sulbactam. The total dose of sulbactam should not exceed 4 g per day. Pediatric Patients 1 Year of Age or Older: The recommended daily dose of Ampicillin and Sulbactam for Injection in pediatric patients is 300 mg per kg of body weight administered via intravenous infusion in equally divided doses every 6 hours. This 300 mg/kg/day dosage represents the total ampicillin content plus the sulbactam content of Ampicillin and Sulbactam for Injection, and corresponds to 200 mg ampicillin and 100 mg sulbactam per kg per day. The safety and efficacy of Ampicillin and Sulbactam for Injection administered via intramuscular injection in pediatric patients have not been established. Pediatric patients weighing 40 kg or more should be dosed according to adult recommendations, and the total dose of sulbactam should not exceed 4 g per day. The course of intravenous therapy should not routinely exceed 14 days. In clinical trials, most pediatric patients received a course of oral antimicrobials following initial treatment with intravenous Ampicillin and Sulbactam for Injection (see CLINICAL STUDIES section.) Impaired Renal Function In patients with impairment of renal function the elimination kinetics of ampicillin and sulbactam are similarly affected, hence the ratio of one to the other will remain constant whatever the renal function. The dose of Ampicillin and Sulbactam for Injection in such patients should be administered less frequently in accordance with the usual practice for ampicillin and according to the following recommendations: TABLE 3: Ampicillin And Sulbactam For Injection Dosage Guide for Patients with Renal Impairment Creatinine Clearance (mL/min/1.73m 2 ) Ampicillin and Sulbactam Half-Life (Hours) Recommended Ampicillin And Sulbactam For Injection Dosage ≥ 30 1 1.5 g to 3 g every 6 to 8 hours 15 to 29 5 1.5 g to 3 g every 12 hours 5 to 14 9 1.5 g to 3 g every 24 hours When only serum creatinine is available, the following formula (based on sex, weight, and age of the patient) may be used to convert this value into creatinine clearance. The serum creatinine should represent a steady state of renal function. Males Weight (kg) x (140 - age) 72 x serum creatinine Females 0.85 x above value
Paediatric
Pediatric Use: The safety and effectiveness of ampicillin and sulbactam for injection have been established for pediatric patients one year of age and older for skin and skin structure infections as approved in adults. Use of ampicillin and sulbactam for injection in pediatric patients is supported by evidence from adequate and well-controlled studies in adults with additional data from pediatric pharmacokinetic studies, a controlled clinical trial conducted in pediatric patients and post-marketing adverse events surveillance (see CLINICAL PHARMACOLOGY , INDICATIONS AND USAGE , ADVERSE REACTIONS , DOSAGE AND ADMINISTRATION , and CLINICAL STUDIES sections). The safety and effectiveness of ampicillin and sulbactam for injection have not been established for pediatric patients for intra-abdominal infections.
Renal
Renal excretion dominant — reduce dose or extend interval in significant renal impairment; risk of accumulation and seizures at high levels.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Hepatic
Low intrinsic hepatotoxicity; cholestatic hepatitis rare (notably flucloxacillin/co-amoxiclav patterns for related agents).
Safety
Drug interactions
- Cloxacillin has protective effect on enzymatic degradation of ampicillin by penicillinase, in addition to having its own activities.
- It may not be given to patients with infectious mononucleosis, lymphatic leukaemia and patients receiving allopurinol treatment because of an increased risk of developing skin rashes
- Fixed-dose/multi-ingredient product.
- Clinical details partially inherited from component monographs: Ampicillin, Cloxacillin.
- Confirm combination SmPC for exact dosing.
Safety
Adverse effects
- ADVERSE REACTIONS Adult Patients: Ampicillin and sulbactam for injection is generally well tolerated.
- The following adverse reactions have been reported in clinical trials.
- Local Adverse Reactions Pain at IM injection site – 16% Pain at IV injection site – 3% Thrombophlebitis – 3% Phlebitis – 1.2% Systemic Adverse Reactions The most frequently reported adverse reactions were diarrhea in 3% of the patients and rash in less than 2% of the patients.
- Additional systemic reactions reported in less than 1% of the patients were: itching, nausea, vomiting, candidiasis, fatigue, malaise, headache, chest pain, flatulence, abdominal distension, glossitis, urine retention, dysuria, edema, facial swelling, erythema, chills, tightness in throat, substernal pain, epistaxis and mucosal bleeding.
- Pediatric Patients: Available safety data for pediatric patients treated with ampicillin and sulbactam for injection demonstrate a similar adverse events profile to those observed in adult patients.
- Additionally, atypical lymphocytosis has been observed in one pediatric patient receiving ampicillin and sulbactam for injection.
- Adverse Laboratory Changes Adverse laboratory changes without regard to drug relationship that were reported during clinical trials were: Hepatic : Increased AST (SGOT), ALT (SGPT), alkaline phosphatase, and LDH.
- Hematologic : Decreased hemoglobin, hematocrit, RBC, WBC, neutrophils, lymphocytes, platelets and increased lymphocytes, monocytes, basophils, eosinophils, and platelets.
- Blood Chemistry : Decreased serum albumin and total proteins.
- Renal : Increased BUN and creatinine.
- Urinalysis : Presence of RBC's and hyaline casts in urine.
- Post-marketing Experience In addition to adverse reactions reported from clinical trials, the following have been identified during post-marketing use of ampicillin sodium and sulbactam sodium or other products containing ampicillin.
- Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made.
- These events have been chosen for inclusion due to a combination of their seriousness, frequency, or potential causal connection to ampicillin sodium and sulbactam sodium.
Use
Indications
- INDICATIONS AND USAGE Ampicillin and Sulbactam for Injection is indicated for the treatment of infections due to susceptible strains of the designated microorganisms in the conditions listed below.
- Skin and Skin Structure Infections caused by beta-lactamase producing strains of Staphylococcus aureus , Escherichia coli *, Klebsiella spp.* (including K. pneumoniae *), Proteus mirabilis *, Bacteroides fragilis *, Enterobacter spp.*, and Acinetobacter calcoaceticus * .
- NOTE: For information on use in pediatric patients see PRECAUTIONS-Pediatric Use and CLINICAL STUDIES sections.
- Intra-Abdominal Infections caused by beta-lactamase producing strains of Escherichia coli , Klebsiella spp.
- (including K. pneumoniae * ) , Bacteroides spp.
- (including B. fragilis ), and Enterobacter spp.* Gynecological Infections caused by beta-lactamase producing strains of Escherichia coli*, and Bacteroides spp.* (including B. fragilis * ) . *Efficacy for this organism in this organ system was studied in fewer than 10 infections.
- While ampicillin and sulbactam for injection is indicated only for the conditions listed above, infections caused by ampicillin-susceptible organisms are also amenable to treatment with ampicillin and sulbactam for injection due to its ampicillin content.
- Therefore, mixed infections caused by ampicillin-susceptible organisms and beta-lactamase producing organisms susceptible to ampicillin and sulbactam for injection should not require the addition of another antibacterial.
- Appropriate culture and susceptibility tests should be performed before treatment in order to isolate and identify the organisms causing infection and to determine their susceptibility to ampicillin and sulbactam for injection.
- Therapy may be instituted prior to obtaining the results from bacteriological and susceptibility studies when there is reason to believe the infection may involve any of the beta-lactamase producing organisms listed above in the indicated organ systems.
- Once the results are known, therapy should be adjusted if appropriate.
- To reduce the development of drug-resistant bacteria and maintain effectiveness of ampicillin and sulbactam for injection and other antibacterial drugs, ampicillin and sulbactam for injection should be used only to treat infections that are proven or strongly suspected to be caused by susceptible bacteria.
Pharmacology
Mode of action
Inhibits synthesis of bacterial cell wall, causing cell death, hence bactericidal.
Full mechanism text
Inhibits synthesis of bacterial cell wall, causing cell death, hence bactericidal. Penicillins bind penicillin-binding proteins (PBPs) and inhibit the final transpeptidation step of peptidoglycan synthesis, weakening the bacterial cell wall. Osmotic lysis follows; activity is bactericidal against susceptible organisms in the growth phase. Spectrum and beta-lactamase stability vary by agent (narrow natural penicillins vs aminopenicillins vs antipseudomonal/anti-staphylococcal agents).
ADME
Pharmacokinetics & PD
| Onset | Within 1 hour (oral); faster IV |
|---|---|
| Duration | 4–8 hours typical (agent/formulation dependent) |
| Route | INTRAMUSCULAR, INTRAVENOUS |
| Elimination | kinetics of ampicillin and sulbactam are similarly affected, hence the ratio of one to the other will remain constant whatever the renal function. The dose of ampicillin and sulbactam for injection in such patients should be administered less frequently in accordance with the usu... |
| Half-life | of both drugs is approximately 1 hour in healthy volunteers. Approximately 75 to 85% of both ampicillin and sulbactam are excreted unchanged in the urine during the first 8 hours after administration of ampicillin and sulbactam for injection to individuals with normal renal funct... |
Full PK/PD text
CLINICAL PHARMACOLOGY General: Immediately after completion of a 15-minute intravenous infusion of ampicillin and sulbactam for injection, peak serum concentrations of ampicillin and sulbactam are attained. Ampicillin serum levels are similar to those produced by the administration of equivalent amounts of ampicillin alone. Peak ampicillin serum levels ranging from 109 to 150 mcg/mL are attained after administration of 2000 mg of ampicillin plus 1000 mg sulbactam and 40 to 71 mcg/mL after administration of 1000 mg ampicillin plus 500 mg sulbactam. The corresponding mean peak serum levels for sulbactam range from 48 to 88 mcg/mL and 21 to 40 mcg/mL, respectively. After an intramuscular injection of 1000 mg ampicillin plus 500 mg sulbactam, peak ampicillin serum levels ranging from 8 to 37 mcg/mL and peak sulbactam serum levels ranging from 6 to 24 mcg/mL are attained. The mean serum half-life of both drugs is approximately 1 hour in healthy volunteers. Approximately 75 to 85% of both ampicillin and sulbactam are excreted unchanged in the urine during the first 8 hours after administration of ampicillin and sulbactam for injection to individuals with normal renal function. Somewhat higher and more prolonged serum levels of ampicillin and sulbactam can be achieved with the concurrent administration of probenecid. In patients with impaired renal function the elimination kinetics of ampicillin and sulbactam are similarly affected, hence the ratio of one to the other will remain constant whatever the renal function. The dose of ampicillin and sulbactam for injection in such patients should be administered less frequently in accordance with the usual practice for ampicillin (see DOSAGE AND ADMINISTRATION section). Ampicillin has been found to be approximately 28% reversibly bound to human serum protein and sulbactam approximately 38% reversibly bound. The following average levels of ampicillin and sulbactam were measured in the tissues and fluids listed: TABLE 1: Concentration of Ampicillin and Sulbactam for Injection in Various Body Tissues and Fluids Fluid or Tissue Dose (grams) Ampicillin/Sulbactam Concentration (mcg/mL or mcg/g) Ampicillin/Sulbactam Peritoneal Fluid 0.5/0.5 IV 7/14 Blister Fluid (Cantharides) 0.5/0.5 IV 8/20 Tissue Fluid 1/0.5 IV 8/4 Intestinal Mucosa 0.5/0.5 IV 11/18 Appendix 2/1 IV 3/40 Penetration of both ampicillin and sulbactam into cerebrospinal fluid in the presence of inflamed meninges has been demonstrated after IV administration of ampicillin and sulbactam for injection. The pharmacokinetics of ampicillin and sulbactam in pediatric patients receiving ampicillin and sulbactam for injection are similar to those observed in adults. Immediately after a 15-minute infusion of 50 to 75 mg ampicillin and sulbactam for injection/kg body weight, peak serum and plasma concentrations of 82 to 446 mcg ampicillin/mL and 44 to 203 mcg sulbactam/mL were obtained. Mean half-life values were approximately 1 hour.
Kenya
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Special populations
Pregnancy & lactation
Pregnancy
Pregnancy: Reproduction studies have been performed in mice, rats, and rabbits at doses up to ten (10) times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to ampicillin and sulbactam for injection. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed (see PRECAUTIONS-Drug/ Laboratory Test Interactions section).
Lactation
Nursing Mothers: Low concentrations of ampicillin and sulbactam are excreted in the milk; therefore, caution should be exercised when ampicillin and sulbactam for injection is administered to a nursing woman.
Diet
Food & alcohol
- Drug & food interactions (label) Drug Interactions: Probenecid decreases the renal tubular secretion of ampicillin and sulbactam. Concurrent use of probenecid with ampicillin and sulbactam for injection may result in increased and prolonged blood levels of ampicillin and sulbactam. The concurrent administration of allopurinol and ampicillin increases substantially the incidence of rashes in patients receiving both drugs as compared to patients receiving ampicillin alone. It is not known whether this potentiation of ampicillin rashes is due to allopurinol or the hyperuricemia present in these patients. There are no data with ampicillin and sulbactam for injection and allopurinol administered concurrently. Ampicillin and sulbactam for injection and aminoglycosides should not be reconstituted together due to the in vitro inactivation of aminoglycosides by the ampicillin component of ampicillin and sulbactam for injection.
Trust
Sources & disclaimer
Source: Local active-ingredient clinical extract; FDA drug label via OpenFDA/DailyMed; Component monographs (multi-source pipeline); Professional class pharmacology (Beta-lactam antibiotic — penicillin)
Clinical review date not recorded.
Decision support only — not a substitute for clinical judgment, product SmPC, or Kenya STG/EML.