Imipenem/cilastatin: the first carbapenem antibiotic. 1985

J A Lyon

Imipenem/cilastatin is the first of a new class of beta-lactam antibiotics called carbapenems. The antibacterial spectrum of imipenem exceeds any antibiotic investigated to date and includes gram-positive, gram-negative, and anaerobic organisms. Only methicillin-resistant organisms, Strep. faecium, Pseudomonas cepacia, and Pseudomonas maltophilia have been shown to be resistant. Imipenem is administered in a 1:1 ratio with cilastatin, which inhibits a renal enzyme (dehydropeptidase) and improves urinary recovery of imipenem. The elimination half-life of both compounds is 1.0 hours and recommended doses are 0.25-0.5 g iv q6h. Adverse events are similar in nature and incidence to beta-lactam antibiotics, with phlebitis/thrombophlebitis, diarrhea, nausea, skin rash, and elevations of hepatic enzymes most common. Clinical studies in phase II and III trials have shown imipenem/cilastatin to be effective in soft tissue infections, endocarditis, obstetrics and gynecology, complicated urinary tract infections, mixed anaerobic-aerobic infections, osteomyelitis, bacteremias, and pneumonias. Several comparative clinical trials have shown imipenem/cilastatin to be equal in efficacy to combination therapy. Imipenem/cilastatin may prove to be an alternative to combination antibiotic therapy because of its extremely broad spectrum of activity.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D002621 Chemistry A basic science concerned with the composition, structure, and properties of matter; and the reactions that occur between substances and the associated energy exchange.
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D003521 Cyclopropanes Three-carbon cycloparaffin cyclopropane (the structural formula (CH2)3) and its derivatives.
D004150 Dipeptidases EXOPEPTIDASES that specifically act on dipeptides. EC 3.4.13.
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000900 Anti-Bacterial Agents Substances that inhibit the growth or reproduction of BACTERIA. Anti-Bacterial Agent,Anti-Bacterial Compound,Anti-Mycobacterial Agent,Antibacterial Agent,Antibiotics,Antimycobacterial Agent,Bacteriocidal Agent,Bacteriocide,Anti-Bacterial Compounds,Anti-Mycobacterial Agents,Antibacterial Agents,Antibiotic,Antimycobacterial Agents,Bacteriocidal Agents,Bacteriocides,Agent, Anti-Bacterial,Agent, Anti-Mycobacterial,Agent, Antibacterial,Agent, Antimycobacterial,Agent, Bacteriocidal,Agents, Anti-Bacterial,Agents, Anti-Mycobacterial,Agents, Antibacterial,Agents, Antimycobacterial,Agents, Bacteriocidal,Anti Bacterial Agent,Anti Bacterial Agents,Anti Bacterial Compound,Anti Bacterial Compounds,Anti Mycobacterial Agent,Anti Mycobacterial Agents,Compound, Anti-Bacterial,Compounds, Anti-Bacterial
D001419 Bacteria One of the three domains of life (the others being Eukarya and ARCHAEA), also called Eubacteria. They are unicellular prokaryotic microorganisms which generally possess rigid cell walls, multiply by cell division, and exhibit three principal forms: round or coccal, rodlike or bacillary, and spiral or spirochetal. Bacteria can be classified by their response to OXYGEN: aerobic, anaerobic, or facultatively anaerobic; by the mode by which they obtain their energy: chemotrophy (via chemical reaction) or PHOTOTROPHY (via light reaction); for chemotrophs by their source of chemical energy: CHEMOLITHOTROPHY (from inorganic compounds) or chemoorganotrophy (from organic compounds); and by their source for CARBON; NITROGEN; etc.; HETEROTROPHY (from organic sources) or AUTOTROPHY (from CARBON DIOXIDE). They can also be classified by whether or not they stain (based on the structure of their CELL WALLS) with CRYSTAL VIOLET dye: gram-negative or gram-positive. Eubacteria
D001424 Bacterial Infections Infections by bacteria, general or unspecified. Bacterial Disease,Bacterial Infection,Infection, Bacterial,Infections, Bacterial,Bacterial Diseases
D013845 Thienamycins Beta-lactam antibiotics that differ from PENICILLINS in having the thiazolidine sulfur atom replaced by carbon, the sulfur then becoming the first atom in the side chain. They are unstable chemically, but have a very broad antibacterial spectrum. Thienamycin and its more stable derivatives are proposed for use in combinations with enzyme inhibitors. Antibiotics, Thienamycin,Thienamycin Antibiotics

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