The pharmacokinetics of ampicillin and sulbactam in pediatric patients receiving ampicillin and sulbactam are similar to those observed in adults. Mean half-life values were approximately 1 hour. It acts through the inhibition of cell wall mucopeptide biosynthesis. Ampicillin has a broad spectrum of bactericidal activity against many gram-positive and gram-negative aerobic and anaerobic bacteria. Ampicillin is, however, degraded by beta-lactamases and therefore the spectrum of activity does not normally include organisms which produce these enzymes.
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The pharmacokinetics of ampicillin and sulbactam in pediatric patients receiving ampicillin and sulbactam are similar to those observed in adults.
Mean half-life values were approximately 1 hour. It acts through the inhibition of cell wall mucopeptide biosynthesis. Ampicillin has a broad spectrum of bactericidal activity against many gram-positive and gram-negative aerobic and anaerobic bacteria. Ampicillin is, however, degraded by beta-lactamases and therefore the spectrum of activity does not normally include organisms which produce these enzymes. A wide range of beta-lactamases found in microorganisms resistant to penicillins and cephalosporins have been shown in biochemical studies with cell free bacterial systems to be irreversibly inhibited by sulbactam.
Although sulbactam alone possesses little useful antibacterial activity except against the Neisseriaceae, whole organism studies have shown that sulbactam restores ampicillin activity against beta-lactamase producing strains. In particular, sulbactam has good inhibitory activity against the clinically important plasmid mediated beta-lactamases most frequently responsible for transferred drug resistance.
Sulbactam has no effect on the activity of ampicillin against ampicillin susceptible strains. The presence of sulbactam in the ampicillin and sulbactam for injection formulation effectively extends the antibacterial spectrum of ampicillin to include many bacteria normally resistant to it and to other beta-lactam antibacterials.
Thus, ampicillin and sulbactam for injection possesses the properties of a broad-spectrum antibacterial and a beta-lactamase inhibitor.
Gram-Negative Bacteria Hemophilus influenzae beta-lactamase and non-beta-lactamase producing , Moraxella Branhamella catarrhalis beta-lactamase and non-beta-lactamase producing , Escherichia coli beta-lactamase and non-beta-lactamase producing , Klebsiella species all known strains are beta-lactamase producing , Proteus mirabilis beta-lactamase and non-beta-lactamase producing , Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Morganella morganii, and Neisseria gonorrhoeae beta-lactamase and non-beta-lactamase producing.
Intra-Abdominal Infections caused by beta-lactamase producing strains of Escherichia coli, Klebsiella spp. While ampicillin and sulbactam for injection, USP 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, USP 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, USP 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, USP. 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, USP and other antibacterial drugs, ampicillin and sulbactam for injection, USP should be used only to treat infections that are proven or strongly suspected to be caused by susceptible bacteria.
When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. 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.
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. Clostridium difficile-Associated Diarrhea Clostridium 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.
Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. Hypertoxin producing strains of C. 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. Appropriate fluid and electrolyte management, protein supplementation, antibacterial treatment of C.
Thus, ampicillin class antibacterials should not be administered to patients with mononucleosis. In patients treated with ampicillin and sulbactam the possibility of superinfections with mycotic or bacterial pathogens should be kept in mind during therapy.
Prescribing ampicillin and sulbactam for injection 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. Information for Patients Patients should be counseled that antibacterial drugs including ampicillin and sulbactam for injection should only be used to treat bacterial infections. They do not treat viral infections e.
When ampicillin and sulbactam for injection is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may 1 decrease the effectiveness of the immediate treatment and 2 increase the likelihood that bacteria will develop resistance and will not be treatable by ampicillin and sulbactam for injection or other antibacterial drugs in the future.
Diarrhea is a common problem caused by antibacterials which usually ends when the antibacterial is discontinued. Sometimes after starting treatment with antibacterials, patients can develop watery and bloody stools with or without stomach cramps and fever even as late as two or more months after having taken the last dose of the antibacterial. If this occurs, patients should contact their physician as soon as possible. Drug Interactions Probenecid decreases the renal tubular secretion of ampicillin and sulbactam.
Concurrent use of probenecid with ampicillin and sulbactam 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 and allopurinol administered concurrently. Ampicillin and sulbactam and aminoglycosides should not be reconstituted together due to the in vitro inactivation of aminoglycosides by the ampicillin component of ampicillin and sulbactam.
Following administration of ampicillin to pregnant women, a transient decrease in plasma concentration of total conjugated estriol, estriol-glucuronide, conjugated estrone and estradiol has been noted. This effect may also occur with ampicillin and sulbactam. Carcinogenesis, Mutagenesis, Impairment of Fertility Long-term studies in animals have not been performed to evaluate carcinogenic or mutagenic potential.
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.
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. Labor and Delivery Studies in guinea pigs have shown that intravenous administration of ampicillin decreased the uterine tone, frequency of contractions, height of contractions, and duration of contractions.
However, it is not known whether the use of ampicillin and sulbactam in humans during labor or delivery has immediate or delayed adverse effects on the fetus, prolongs the duration of labor, or increases the likelihood that forceps delivery or other obstetrical intervention or resuscitation of the newborn will be necessary.
Nursing Mothers Low concentrations of ampicillin and sulbactam are excreted in the milk; therefore, caution should be exercised when ampicillin and sulbactam is administered to a nursing woman.
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.
The safety and effectiveness of ampicillin and sulbactam for injection have not been established for pediatric patients for intra-abdominal infections. The following adverse reactions have been reported in clinical trials.
Pediatric Patients Available safety data for pediatric patients treated with ampicillin and sulbactam 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. 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. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made.
Blood and Lymphatic System Disorders: Hemolytic anemia, thrombocytopenic purpura, and agranulocytosis have been reported. These reactions are usually reversible on discontinuation of therapy and are believed to be hypersensitivity phenomena. Some individuals have developed positive direct Coombs Tests during treatment with ampicillin and sulbactam for injection, as with other beta-lactam antibacterials. 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.
Of 99 pediatric patients evaluable for clinical efficacy, 60 patients received a regimen containing intravenous ampicillin and sulbactam, and 39 patients received a regimen containing intravenous cefuroxime.
This trial demonstrated similar outcomes assessed at an appropriate interval after discontinuation of all antimicrobial therapy for ampicillin and sulbactam- and cefuroxime-treated patients: TABLE 2.
Ampicilina + Sulbactam
Los reportes de casos de efectividad anticonceptiva oral reducida en mujeres que toman ampicilina, amoxicilina y penicilina V, lo que resulta en un embarazo no planificado. La ampicilina puede haber alterado la flora gastrointestinal y, en consecuencia, el metabolismo de la sulfasalazina. La ampicilina mezclada con gentamicina, por periodos prolongados causa perdida de actividad antimicrobiana de la gentamicina. La penicilina V y la amoxicilina no se ven afectadas por los alimentos y pueden administrarse independientemente de las comidas. Los autoanticuerpos son poco comunes.
Ampicilina: Qué es, para qué sirve, nombre comercial y más