Bactalev-750/Bactalev-1.5

Bactalev-750: White crystalline powder filled in USP Type I Clear Glass Vial.
Each vial contains: Sterile Ampicillin Sodium eq. to Anhydrous Ampicillin 500 mg, Sterile Sulbactam Sodium eq. to Anhydrous Sulbactam 250 mg.
Bactalev-1.5: Ampicillin Sodium and Sulbactam Sodium 1 g/500 mg Powder for Injection: White crystalline powder filled in USP Type I Clear Glass Vial.
Each vial contains: Sterile Ampicillin Sodium eq. to Anhydrous Ampicillin USP 1 g, Sterile Sulbactam Sodium eq. to Anhydrous Sulbactam 500 mg.

Pharmacology: Pharmacokinetics: Ampicillin is relatively resistant to inactivation by gastric acid and is moderately well absorbed from the gastrointestinal tract after oral doses. Food can interfere with the absorption of Ampicillin so doses should preferably be taken at least 30 minutes before meals. Peak concentrations in plasma are attained in about 1 to 2 hours and after a 500 mg oral dose be reported to range from 3 to 6 micrograms/mL. Peak plasma concentrations of Ampicillin after a 500 mg intramuscular dose given as the sodium salt occur within 1 hour and are reported to range from 7 to 14 micrograms/mL.
Ampicillin is widely distributed and therapeutic concentrations can be achieved in ascitic, pleural, and joint fluids. It crosses the placenta and small amounts are distributed into breastmilk. There is little diffusion into the CSF except when the meninges are inflamed. About 20% is bound to plasma proteins and the plasma half-life is about 1 to 1.5 hours, but this may be increased in neonates, the elderly, and patients with renal impairment; in severe renal impairment half-lives of 7 to 20 hours have been reported.
Ampicillin is metabolized to some extent to penicilloic acid which is excreted in the urine. Renal clearance of Ampicillin occurs partly by glomerular filtration and partly by tubular secretion; it is reduced by probenecid. About 20 to 40% of an oral dose may be excreted unchanged in the urine in 6 hours; urinary concentrations have ranged from 0.25 to 1 mg/mL following dose of 500 mg. After parenteral use about 60 to 80% is excreted in the urine within 6 hours. Ampicillin is removed by hemodialysis. High concentrations are reached in bile; it undergoes enterohepatic recycling and some is excreted in the faeces, Ampicillin with Sulbactam. The pharmacokinetics of Ampicillin and Sulbactam are broadly similar and neither appears to affect the other or to any great extent.

For the treatment of infections due to beta-lactamase producing organisms.

Doses are expressed in terms of the equivalent amounts of ampicillin and sulbactam; available injections contain ampicillin and sulbactam in the ratio 2:1, respectively. The usual dose is ampicillin 1 g with sulbactam 500 mg every 6 hours; doses may be doubled in severe infections. Or as prescribed by the physician.

Neurological adverse reactions, including convulsions, may occur with the attainment of high CSF levels of beta-lactams. Ampicillin may be removed from circulation by hemodialysis. The molecular weight, degree of protein binding and pharmacokinetics profile of sulbactam suggest that this compound may also be removed by hemodialysis.

The use of Ampicillin + Sulbactam 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 + Sulbactam is contraindicated in patients with a previous history of cholestatic jaundice/hepatic dysfunction associated with Ampicillin + Sulbactam.

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 + Sulbactam should be discontinued and the appropriate therapy instituted.
Hepatotoxicity: Hepatic dysfunction, including hepatitis and cholestatic jaundice has been associated with the use of Ampicillin + Sulbactam. 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 + Sulbactam may cause severe skin reactions, such as toxic epidermal necrolysis (TEN), Stevens-Johnson syndrome (SJS), dermatitis exfoliative, erythema multiforme, and Acute generalized exanthematous pustulosis (AGEP). If patients develop a skin rash they should be monitored closely and Ampicillin + Sulbactam discontinued if lesion progress.
Clostridium difficile-Associated Diarrhea: Clostridium difficile-Associated Diarrhea (CDAD) has been reported with use of nearly all antibacterial agents including Ampicillin + Sulbactam, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.
C. difficile produces toxins A and B which contribute tot he development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibacterial drug use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.
If CDAD is suspected or confirmed, ongoing antibacterial drug use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibacterial treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.

A high percentage of patients with mononucleosis who receive ampicillin develop a skin rash. Thus, ampicillin class antibacterials should not be administered to patients with mononucleosis. In patients treated with Ampicillin + Sulbactam the possibility of superinfections with mycotic or bacterial pathogens should be kept in mind during therapy. If superinfections occur (usually involving Pseudomonas or Candida), the drug should be discontinued and/or appropriate therapy instituted.
Prescribing Ampicillin + Sulbactam in the absence of proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.

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 + Sulbactam. 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.
Lactation: Low concentrations of ampicillin and sulbactam are excreted in the milk; therefore, caution should be exercised when it is administered to a nursing woman.

Skin rashes among the most common adverse effects and generally either urticarial or maculopapular; the urticarial reactions are typical of penicillin hypersensitivity, while the erythematous maculopapular eruptions are characteristic of ampicillin and amoxicillin and often appear more than 7 days after commencing treatment. Such rashes may be due to hypersensitivity to the beta-lactam moiety or to the amino group in the side-chain, or to a toxic reaction. The occurrence of a maculopapular rash during ampicillin use does not necessarily preclude the subsequent use of other penicillins. However, since it may be difficult in practice to distinguish between hypersensitive and toxic responses, skin testing for hypersensitivity may be advisable before another penicillin is used in patients who have had ampicillin rashes. Most patients with infectious mononucleosis develop a maculo-papular rash when treated with ampicillin, and patients with other lymphoid disorders such as lymphatic leukemia, and possibly those with HIV infection, also appear to be at higher risk. More serious skin reactions may occur and erythema multiforme associated with ampicillin has occasionally been reported.

Probenecid decreases the renal tubular secretion of ampicillin and sulbactam. Concurrent use of probenecid with it 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 + Sulbactam and allopurinol administered concurrently. Ampicillin + Sulbactam and aminoglycosides should not be reconstituted together due to the in vitro inactivation of aminoglycosides by the ampicillin component of Ampicillin + Sulbactam.

Direction for reconstitution: Ampicillin Sodium and Sulbactam Sodium 500 mg/250 mg injection should be reconstituted with 1.6 mL Sterile Water for Injection and should be used within 1 hour of reconstitution.
Ampicillin Sodium and Sulbactam Sodium 1 g/500 mg injection should be reconstituted with 3.2 mL Sterile Water for Injection and should be used within 1 hour of reconstitution.

Store at temperatures not exceeding 30°C.

Penicillins

J01CR01 - ampicillin and beta-lactamase inhibitor ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.

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