May cause gi irritation, renal impairment, leukopenia, and rash. Cilastatin sodium, an inhibitor of this enzyme, effectively prevents renal metabolism of imipenem so that when imipenem and cilastatin sodium are given concomitantly, adequate antibacterial levels of imipenem are achieved in the urine. Imipenemresiststheactionsofmanyenzymesthatdegrademostotherpenicillinsandpenicillinlikeantiinfectives. Cilastatin inhibits the human enzyme dehydropeptidase uses. Removal of imipenem and cilastatin by hemodialysis in. Cilastatin sodium, an inhibitor of this enzyme, effectively prevents renal metabolism of imipenem so that when imipenem and cilastatin sodium are given concomitantly, increased levels of imipenem are achieved in the urine. Each 125 mg, 250 mg, or 500 mg dose should be given by intravenous administration over 20 to 30 minutes. Imipenem and cilastatin combination is used in the treatment of infections caused by bacteria. The pharmacokinetics of imipenem were studied in 11 adult patients with severe burns who were receiving a therapeutic regimen of imipenemcilastatin 500 mg intravenously every 6 hours.
Imipenem is the first available semisynthetic thienamycin and is administered intravenously in combination with cilastatin,1 a renal dipeptidase inhibitor that increases urinary excretion of active drug. The binding of imipenem to human serum proteins is approximately 20% and that of cilastatin is approximately 40%. Following intravenous infusion of imipenem and cilastatin at a combined concentration of 10 mgkg of body weight, drug levels in plasma were determined serially during off and onhemodialysis periods, which were 2 and 4 h, respectively. Medscape indicationspecific dosing for primaxin imipenemcilastatin. Dailymed primaxin iv imipenem and cilastatin sodium. Antiinfective pregnancy risk category c action acts against many grampositive and gramnegative organisms by binding to bacterial cell wall, causing cell death. Imipenemcilastatin side effects, dosage, interactions.
Renal dosing adult if usual dose 500mg q6h crcl 6089. The coadministration of imipenum with the renal dehydropeptidase inhibitor cilastatin results in an increase of the urinary recovery of the antibiotic, both in animals and humans. Imipenem with cilastatin drug bnfc content published. Cilastatin plus imipenem an overview sciencedirect topics. Imipenem and cilastatin intravenous route, intramuscular. The pharmacokinetics of imipenem thienamycinformamidine. Severe diarrhea may be a sign of a serious side effect. Because imipenem is rapidly inactivated by renal dehydropeptidase i. The recommended dosage is 250 mg to 1 gram given intravenously. Key points imipenemcilastatin primaxin is includes a carbapenem antibiotic imipenem plus a dehydropeptidasei dhpi inhibitor cilastatin that prevents inactivation of imipenem by renal dhpi it kills bacteria in a timedependent fashion by interfering with the bacterial cell wall in susceptible organisms coverage is broad, including multidrug resistant pseudomonas sp.
It is made from a combination of imipenem and cilastatin. The patient should receive a dose after hemodialysis and at 12 hour intervals timed from the end of that hemodialysis session. Imipenem and cilastatin dosage in renal impairment reduced i. Imipenem with cilastatin medicinal forms bnfc content. Imipenemcilastatin je organsko jedinjenje, koje sadrzi 28 atoma ugljenika i ima molekulsku masu od 675,814 da. Imipenemcilastatinrelebactam imirel is a broadspectrum antibiotic that combines three active ingredients. Primaxin imipenemcilastatin dosing, indications, interactions.
It works by killing bacteria or preventing their growth. Imipenem and cilastatin professional patient advice. Elimination studies performed during haemodialysis indicated efficient removal of both imipenem and cilastatin during a 4 h session. For adult patients with normal renal function creatinine clearance of greater than or equal to 90 mlmin, the recommended dosage regimens are. Imipenemcilastatin is a topic covered in the johns hopkins abx guide to view the entire topic, please sign in or purchase a subscription official website of the johns hopkins antibiotic abx, hiv, diabetes, and psychiatry guides, powered by unbound medicine. Pricing, sizing, legal catgories and other medicinal forms information for imipenem with cilastatin. Imipenem and cilastatin is used to treat severe infections of the lower respiratory tract, skin, stomach, female reproductive organs. Imipenem and cilastatin for injection is a sterile formulation of imipenem a thienamycin antibiotic and cilastatin sodium the inhibitor of the renal dipeptidase, dehydropeptidase l, with sodium bicarbonate added as a buffer. Injection vial 500mg imipenem and 500mg cilastatin powder add 10ml of. Imipenem is active in vitro against a wide range of grampositive and gramnegative aerobic and anaerobic bacteria, including most strains which are betalactamase producing. An equivalent amount of cilastatin is also present in. Using imipenem and cilastatin during continuous renal replacement therapy article pdf available in international journal of clinical pharmacy 275.
Preliminary research on twostep dosing of imipenemcilastatin protdoi the safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Imipenem is an antibiotic that fights serious infections caused by bacteria. The dosage recommendations for primaxin represent the quantity of imipenem to be administered. Detailed cilastatin imipenem dosage information for adults and children. Impact of renal impairment and human organic anion transporter inhibition on. The mean serum halflife of imipenem is about 2 hours, whereas that of cilastatin is 5 to 6. Dehydropeptidase is an enzyme found in the kidney and is responsible for degrading the antibiotic imipenem. Pubmed journal articles for imipenem cilastatin were found in prime pubmed.
Imipenem, when administered alone, is metabolized in the kidneys by dehydropeptidase i resulting in relatively low levels in urine. Cilastatin can therefore be combined intravenously with imipenem in order to protect it from degradation, prolonging its antibacterial effect imipenem alone is an effective antibiotic and can be given without cilastatin. Specifically it is used for pneumonia, sepsis, endocarditis, joint infections, intraabdominal infections, and urinary tract infections. In vitro studies have demonstrated that imipenem has an extremely wide spectrum of antibacterial activity against gramnegative and grampositive aerobic and anaerobic bacteria, even. The combination of imipenem and cilastatin is available generically and under the brand name primaxin as 250 mg or 500 mg infusion bottles for iv use or 500 mg or 750 mg vials of lyophilized powder for im injection. In view of the important increase in halflife of cilastatin as a function of increasing renal failure, a dosage reduction is proposed in patients with severe renal failure. Preliminary research on twostep dosing of imipenem.
Combination with cilastatin prevents renal inactivation of imipenem, resulting in high urinary concentrations. An equivalent amount of cilastatin is also present in the solution. In some patients, imipenem and cilastatin combination may cause diarrhea. Listing a study does not mean it has been evaluated by the u. Imipenemcilastatin, sold under the brand name primaxin among others, is an antibiotic useful for the treatment of a number of bacterial infections. Do not take any diarrhea medicine without first checking with your doctor. Cilastatin prevents renal metabolism of imipenem by competitive.
The dosage of primaxin in adult patients should be based on suspected or confirmed pathogen susceptibility as shown in table 1 below. The most common side effects of imipenem are diarrhea, nausea, vomiting, skin rash, pruritus and injection site reactions. Imipenem and cilastatin for injection usp page 3 of 43 and of the patients clinical condition. Imipenem and cilastatin drug monograph pediatric care online. Frequency of convulsions during treatment with imipenem cilastatin is dose dependent. Physiological modifications related to pregnancy increased volume of distribution and glomerular filtration rate, especially with hydrophilic antibiotics lead to adapting doses of imipenemcilastatin, especially as nonrenal elimination is suspected during pregnancy. Both imipenem and cilastatin are cleared from the circulation during hemodialysis. Pediatric drugs analgesics antihypertensive and cardiovascular agents antimicrobial agents miscellaneous agents sedatives, hypnotics, and other drugs used in psychiatry. Diarrhea medicines may make your diarrhea worse or make it last longer. Imipenem imi is a carbapenem antibiotic that inhibits bacterial cell wall synthesis through binding penicillin binding proteins, cilastatin sodium is a renal dehydropeptidase inhibitor that prevents inactivation if imipenem by renal. Imipenem and cilastatin for injection primaxin is a sterile formulation of imipenem a thienamycin antibiotic and cilastatin sodium the inhibitor of the renal dipeptidase, dehydropeptidase l, with sodium bicarbonate added as a buffer.
For intravenous infusion dilute to a concentration of 5 mg as imipenemml in sodium chloride 0. Prime pubmed imipenem cilastatin journal articles from pubmed. Imipenem and cilastatin is a powder medicine that must be mixed with a liquid diluent before using it. Pdf imipenem pharmacokinetics in patients with burns. Cilastatin sodium, an inhibitor of this enzyme, effectively prevents renal metabolism of imipenem so that when imipenem and cilastatin. Includes dosages for urinary tract infection, pyelonephritis and intraabdominal infection. Cilastatin inhibits renal dihydropeptidase i, preventing imipenem metabolism. The removal of imipenem and cilastatin by hemodialysis was studied in 14 for imipenem and 6 for cilastatin subjects. After 3 to 4 days of treatment with 20mgkg intravenous doses of imipenemcilastatin every 12 hours, peak serum concentrations are 35 and 86. Imipenemcilastatin definition of imipenemcilastatin by. Imipenem and cilastatin is a potent broad spectrum antibacterial agent for intravenous administration. If you are using the injections at home, be sure you understand how to properly mix and. Cilastatin definition of cilastatin by medical dictionary. Detailed cilastatin imipenem relebactam dosage information for adults.
Imipenem and cilastatin injection drug information. Cilastatin helps imipenem work more effectively by preventing the breakdown of the antibiotic in the kidneys. Includes dosages for bacterial infection, urinary tract infection, bronchitis and more. Dosage regimen based on creatinine clearance mlminute1. Imipenem binds to the bacterial cell wall, resulting in cell death. Using imipenem and cilastatin during continuous renal. Risk factors for this complication are renal failure and an underlying neurological disease. Addition of cilastatin prevents renal inactivation of imipenem, resulting in increased urinary concentration.
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