Identification
- Summary
Imipenem is a carbapenem antibiotic normally administered with cilastatin to treat a variety of infections.
- Brand Names
- Primaxin, Recarbrio
- Generic Name
- Imipenem
- DrugBank Accession Number
- DB01598
- Background
Imipenem is a semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains.Label It is stable to many beta-lactamases. Similar compounds include meropenem, known for having greater activity against Gram negative bacteria, and the newer ertapenem which exhibits a longer half-life due to increased binding to plasma proteins.10 Imipenem is commonly used in combination with cilastatin and is now available in a triple-drug product with cilastatin and relebactam which was recently approved by the FDA. Imipenem was first approved by the FDA in November 1985 as the combination product Primaxin marketed by Merck & Co.14
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Imipenem (DB01598)
- Weight
- Average: 299.346
Monoisotopic: 299.093976737 - Chemical Formula
- C12H17N3O4S
- Synonyms
- (5R,6S)-3-((2-(Formimidoylamino)ethyl)thio)-6-((R)-1-hydroxyethyl)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid
- (5R,6S)-3-(2-Formimidoylamino-ethylsulfanyl)-6-((R)-1-hydroxy-ethyl)-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid
- (5R,6S)-6-((R)-1-Hydroxyethyl)-3-(2-(iminomethylamino)ethylthio)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carbonsaeure
- Imipenem
- Imipenem anhydrous
- Imipenemum
- N-formimidoyl thienamycin
- N-formimidoylthienamycin
Pharmacology
- Indication
Imipenem is indicated, in combination with cilastatin with or without relebactam, for the treatment of bacterial infections including respiratory, skin, bone, gynecologic, urinary tract, and intra-abdominal as well as septicemia and endocarditis.12,13
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Bacterial Septicemia
- Bone and Joint Infections
- Complicated Intra-Abdominal Infections (cIAIs) caused by Gram-negative Bacteria
- Complicated Urinary Tract Infection
- Complicated Urinary Tract Infection caused by Gram-negative Bacteria
- Endocarditis caused by staphylococcus aureus
- Gynecological Infection
- Intraabdominal Infections
- Lower respiratory tract infection bacterial
- Nosocomial Pneumonia caused by Gram-negative Bacteria
- Pyelonephritis
- Skin and Subcutaneous Tissue Bacterial Infections
- Uncomplicated Urinary Tract Infections
- Ventilator Associated Bacterial Pneumonia caused by Gram-negative Bacteria
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Imipenem is a beta-lactam antibiotic belongings to the subgroup of carbapenems.12,13 Imipenem is active against aerobic and anaerobic Gram positive as well as Gram negative bacteria including Pseudomonas aeruginosa and the Enterococcus. It exerts a bactericidal effects by disrupting cell wall synthesis.
- Mechanism of action
Imipenem acts as an antimicrobial through the inhibition of cell wall synthesis of various gram-positive and gram-negative bacteria.12,13 This inhibition of cell wall synthesis in gram-negative bateria is attained by binding to penicillin-binding proteins (PBPs). In E. coli and selected strains of P. aeruginosa, imipenem has shown to have the highest affinity to PBP-2, PBP-1a, and PBP-1b.9 This inhibition of PBPs prevents the bacterial cell from adding to the peptidoglycan polymer which forms the bacterial cell wall eventually leading to cell death.11
Target Actions Organism APenicillin-binding protein 2 inhibitorEscherichia coli (strain K12) APenicillin-binding protein 1B inhibitorEscherichia coli (strain K12) APenicillin-binding protein 1A inhibitorEscherichia coli (strain K12) UPenicillin-binding protein 3 inhibitorBacillus subtilis (strain 168) UPenicillin-binding protein 4 Not Available Staphylococcus aureus UBeta-lactamase activatorProteus vulgaris - Absorption
Imipenem is not effectively absorbed from the gastrointestinal tract and therefore must be administered parenterally. The bioavailability of the IM injection is 89%. 8
- Volume of distribution
The reported volume of distribution for imipenem ranges from 0.23-0.31 L/kg.Label,3,8
- Protein binding
- Metabolism
- Route of elimination
Approximately 70% of imipenem is excreted in the urine as the parent drug.Label,12
- Half-life
When given via IV injection imipenem has a half-life of 1 h.Label,3,8 The apparent half-life of the IM injection ranges from 1.3-5.1 h, likely due to slower absorption form the injection site.
- Clearance
The total clearance of imipenem is 0.2 L/h/kg.8 When used alone, the renal clearance is 0.05 L/h/kg. In combination with cilastatin the renal clearance of imipenem is 0.15 L/h/kg, likely due to the increased concentration of the parent drug.
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
In case of overdose with the combination product, including relebactam and cilastatin, it is recommended to provide supportive care.13 Imipenem, cilastatin, and relebactam may be removed via hemodialysis.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcenocoumarol The risk or severity of bleeding can be increased when Imipenem is combined with Acenocoumarol. Acetazolamide The therapeutic efficacy of Acetazolamide can be decreased when used in combination with Imipenem. Acetophenazine Acetophenazine may increase the neurotoxic activities of Imipenem. Alimemazine Alimemazine may increase the neurotoxic activities of Imipenem. Amifampridine The risk or severity of seizure can be increased when Imipenem is combined with Amifampridine. Amisulpride Imipenem may increase the neurotoxic activities of Amisulpride. Amitriptyline Amitriptyline may increase the neurotoxic activities of Imipenem. Amitriptylinoxide Imipenem may increase the neurotoxic activities of Amitriptylinoxide. Amobarbital The therapeutic efficacy of Amobarbital can be decreased when used in combination with Imipenem. Amoxapine Amoxapine may increase the neurotoxic activities of Imipenem. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Imipenem monohydrate 71OTZ9ZE0A 74431-23-5 GSOSVVULSKVSLQ-JJVRHELESA-N - International/Other Brands
- Tienamycin
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BACQURE 500 MG Imipenem monohydrate (500 MG/1VIAL) + Cilastatin (500 MG/1VIAL) Injection, powder, for solution บริษัท แรนแบ็กซี่ (ประเทศไทย) จำกัด 2016-11-22 Not applicable Thailand 
CILAPEM 500 MG/500 MG IV ENJEKSİYONLUK ÇÖZELTİ HAZIRLAMAK İÇİN TOZ, 1 ADET Imipenem (500 mg) + Cilastatin (500 mg) Injection, solution Intravenous TÜM-EKİP İLAÇ A.Ş. 2020-08-14 Not applicable Turkey 
CILAPEM 500 MG/500 MG IV ENJEKSİYONLUK ÇÖZELTİ HAZIRLAMAK İÇİN TOZ, 25 ADET Imipenem (500 mg) + Cilastatin (500 mg) Injection, solution Intravenous TÜM-EKİP İLAÇ A.Ş. 2020-08-14 Not applicable Turkey IMEPEN 500 MG Imipenem monohydrate (500 MG/1VIAL) + Cilastatin (500 MG/1VIAL) Powder บริษัท ฐิติรัตน์สานนท์ จำกัด 2013-07-03 2019-10-21 Thailand IMICILA ALVOGEN Imipenem monohydrate (500 MG/1VIAL) + Cilastatin (500 MG/1VIAL) Injection, powder, for solution บริษัท อัลโวเจน (ประเทศไทย) จำกัด 2016-12-27 2020-08-20 Thailand IMIPENEM /CILASTATIN Kabi 500 mg/ 500 mg, Powder for solution for infusion Imipenem (500 mg) + Cilastatin (500 mg) Injection, powder, for solution FRESENIUS KABI MALAYSIA SDN. BHD 2020-09-08 Not applicable Malaysia 
IMIPENEM /CILASTATIN KABI POWDER FOR SOLUTION FOR INFUSION 500MG/500MG Imipenem (500 mg) + Cilastatin (500 mg) Injection, powder, for solution Intravenous FRESENIUS KABI (SINGAPORE) PTE LTD 2015-03-26 Not applicable Singapore Imipenem + Cilastatin Mevon Powder for solution for Injection 500 mg + 500 mg Imipenem (500 mg) + Cilastatin (500 mg) Injection, powder, for solution Intravenous NOVEM PHARMA PRIVATE LIMITED 2013-03-20 Not applicable Singapore IMIPENEM 0.5G + CILASTATINA0.5G Imipenem monohydrate (0.5 g) + Cilastatin sodium (0.5 g) Injection, powder, for solution Intravenous FARMALOGICA S.A 2007-02-20 2017-03-27 Colombia 
IMIPENEM 500 MG + CILASTATINA 500 MG Imipenem (500 mg) + Cilastatin (500 mg) Injection, powder, for solution Intravenous AUROBINDO PHARMA COLOMBIA S.A.S. 2017-07-11 Not applicable Colombia
Categories
- ATC Codes
- J01DH51 — Imipenem and cilastatin
- J01DH — Carbapenems
- J01D — OTHER BETA-LACTAM ANTIBACTERIALS
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Agents that reduce seizure threshold
- Amides
- Anti-Bacterial Agents
- Anti-Infective Agents
- Antibacterials for Systemic Use
- Antiinfectives for Systemic Use
- Beta-Lactam Antibacterials
- beta-Lactams
- Carbapenems
- Heterocyclic Compounds, Fused-Ring
- Lactams
- Neurotoxic agents
- Penem Antibacterial
- Sulfur Compounds
- Thienamycins
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as thienamycins. These are 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.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Lactams
- Sub Class
- Beta lactams
- Direct Parent
- Thienamycins
- Alternative Parents
- Alpha amino acids and derivatives / Pyrroline carboxylic acids / Azepines / Vinylogous thioesters / Tertiary carboxylic acid amides / Thioenol ethers / Secondary alcohols / Azetidines / Sulfenyl compounds / Azacyclic compounds show 10 more
- Substituents
- Alcohol / Aliphatic heteropolycyclic compound / Alpha-amino acid or derivatives / Amidine / Azacycle / Azepine / Azetidine / Carbonyl group / Carboxamide group / Carboximidamide show 23 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- carbapenems (CHEBI:471744) / carbapenems (C06665)
- Affected organisms
- Pseudomonas aeruginosa
- Streptococcus agalactiae
- Haemophilus influenzae
- Escherichia coli
- Staphylococcus aureus
- Enterococcus faecalis
- Staphylococcus epidermidis
- Serratia marcescens
- Proteus vulgaris
- Providencia rettgeri
- Morganella morganii
- Enterobacter cloacae
- Klebsiella pneumoniae
- Haemophilus parainfluenzae
- Citrobacter freundii
- Bacteroides thetaiotaomicron
- Klebsiella aerogenes
- Bacteroides caccae
- Bacteroides ovatus
- Bacteroides stercoris
- Bacteroides uniformis
- Bacteroides vulgatus
- Fusobacterium nucleatum
- Parabacteroides distasonis
- Acinetobacter spp.
- Enterobacter spp.
- Klebsiella spp.
- Citrobacter spp.
- Proteus spp.
- Bifidobacterium spp.
- Clostridium spp.
- Eubacterium spp.
- Peptococcus spp.
- Peptostreptococcus spp.
- Propionibacterium spp.
- Bacteroides spp.
- Fusobacterium spp.
- Serratia spp.
- Gardnerella vaginalis
Chemical Identifiers
- UNII
- Q20IM7HE75
- CAS number
- 64221-86-9
- InChI Key
- ZSKVGTPCRGIANV-ZXFLCMHBSA-N
- InChI
- InChI=1S/C12H17N3O4S/c1-6(16)9-7-4-8(20-3-2-14-5-13)10(12(18)19)15(7)11(9)17/h5-7,9,16H,2-4H2,1H3,(H2,13,14)(H,18,19)/t6-,7-,9-/m1/s1
- IUPAC Name
- (5R,6S)-3-({2-[(E)-(aminomethylidene)amino]ethyl}sulfanyl)-6-[(1R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
- SMILES
- [H][C@]12CC(SCC\N=C\N)=C(N1C(=O)[C@]2([H])[C@@H](C)O)C(O)=O
References
- Synthesis Reference
Maurizio Zenoni, "Imipenem production process." U.S. Patent US20020095034, issued July 18, 2002.
US20020095034- General References
- Kattan JN, Villegas MV, Quinn JP: New developments in carbapenems. Clin Microbiol Infect. 2008 Dec;14(12):1102-11. doi: 10.1111/j.1469-0691.2008.02101.x. [Article]
- Pastel DA: Imipenem-cilastatin sodium, a broad-spectrum carbapenem antibiotic combination. Clin Pharm. 1986 Sep;5(9):719-36. [Article]
- Buckley MM, Brogden RN, Barradell LB, Goa KL: Imipenem/cilastatin. A reappraisal of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1992 Sep;44(3):408-44. [Article]
- Richerson MA, Ambrose PG, Quintiliani R, Nightingale CH: Formulary review of the carbapenems: comparison of imipenem/cilastatin and meropenem. Conn Med. 1998 Mar;62(3):165-9. [Article]
- Birnbaum J, Kahan FM, Kropp H, MacDonald JS: Carbapenems, a new class of beta-lactam antibiotics. Discovery and development of imipenem/cilastatin. Am J Med. 1985 Jun 7;78(6A):3-21. [Article]
- Hellinger WC, Brewer NS: Imipenem. Mayo Clin Proc. 1991 Oct;66(10):1074-81. [Article]
- Kahan FM, Kropp H, Sundelof JG, Birnbaum J: Thienamycin: development of imipenen-cilastatin. J Antimicrob Chemother. 1983 Dec;12 Suppl D:1-35. [Article]
- Balfour JA, Bryson HM, Brogden RN: Imipenem/cilastatin: an update of its antibacterial activity, pharmacokinetics and therapeutic efficacy in the treatment of serious infections. Drugs. 1996 Jan;51(1):99-136. doi: 10.2165/00003495-199651010-00008. [Article]
- Nicolau DP: Carbapenems: a potent class of antibiotics. Expert Opin Pharmacother. 2008 Jan;9(1):23-37. [Article]
- Zhanel GG, Wiebe R, Dilay L, Thomson K, Rubinstein E, Hoban DJ, Noreddin AM, Karlowsky JA: Comparative review of the carbapenems. Drugs. 2007;67(7):1027-52. [Article]
- Brunton LL, Hilal-Dandan R, Knollmann BC. eds (2018). Goodman & Gilman's: The Pharmacological Basis of Therapeutics (13th ed.). McGraw-Hill Education. [ISBN:978-1-25-958473-2]
- FDA: Primaxin Label [Link]
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Drugs@FDA: Primaxin [Link]
- External Links
- FDA label
- Download (616 KB)
- MSDS
- Download (45 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Not Available Ventilator Associated Bacterial Pneumonia (VABP) 1 4 Completed Prevention Acute Pancreatitis 1 4 Completed Treatment Febrile Neutropenia 1 4 Completed Treatment Febrile Neutropenia / Hematological Malignancy 1 4 Completed Treatment Infection 1 4 Completed Treatment Infection / Pneumonia 1 4 Completed Treatment Infective Endocarditis (IE) 1 4 Completed Treatment Intraabdominal Infections 1 4 Completed Treatment Ventilator Associated Bacterial Pneumonia (VABP) 2 4 Enrolling by Invitation Other Critically Ill Patients / Obesity 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Cardinal Health
- Merck & Co.
- Dosage Forms
Form Route Strength Injection, solution Intravenous Powder Powder Not applicable 1 kg/1kg Injection, powder, for solution Intravenous 500 mg Injection, powder, for solution Intravenous 250 mg Powder, for solution Intravenous Injection, powder, for solution Parenteral Injection, powder, for suspension Intramuscular Injection, powder, for solution Intravenous Injection, powder, for solution Injection, powder, for suspension Intravenous Injection Intravenous - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8487093 No 2013-07-16 2029-11-19 US 
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 1E+004 mg/L MERCK INDEX (1996) pKa 3.2 MERCK INDEX (1996) - Predicted Properties
Property Value Source Water Solubility 0.776 mg/mL ALOGPS logP -0.19 ALOGPS logP -3.9 Chemaxon logS -2.6 ALOGPS pKa (Strongest Acidic) 3.44 Chemaxon pKa (Strongest Basic) 10.88 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 116.22 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 75.84 m3·mol-1 Chemaxon Polarizability 31.1 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.8406 Blood Brain Barrier - 0.9711 Caco-2 permeable - 0.6608 P-glycoprotein substrate Substrate 0.7111 P-glycoprotein inhibitor I Non-inhibitor 0.9011 P-glycoprotein inhibitor II Non-inhibitor 0.8328 Renal organic cation transporter Non-inhibitor 0.5947 CYP450 2C9 substrate Non-substrate 0.7648 CYP450 2D6 substrate Non-substrate 0.7854 CYP450 3A4 substrate Non-substrate 0.5309 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.923 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.9125 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9583 Ames test Non AMES toxic 0.648 Carcinogenicity Non-carcinogens 0.9203 Biodegradation Not ready biodegradable 0.9309 Rat acute toxicity 1.8089 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9852 hERG inhibition (predictor II) Non-inhibitor 0.8603
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. It synthesizes cross-linked peptidoglycan from lipid intermediates.
- Gene Name
- mrdA
- Uniprot ID
- P0AD65
- Uniprot Name
- Penicillin-binding protein 2
- Molecular Weight
- 70856.1 Da
References
- Nicolau DP: Carbapenems: a potent class of antibiotics. Expert Opin Pharmacother. 2008 Jan;9(1):23-37. [Article]
- Zhanel GG, Wiebe R, Dilay L, Thomson K, Rubinstein E, Hoban DJ, Noreddin AM, Karlowsky JA: Comparative review of the carbapenems. Drugs. 2007;67(7):1027-52. [Article]
- Neu HC: Carbapenems: special properties contributing to their activity. Am J Med. 1985 Jun 7;78(6A):33-40. [Article]
- Luchi M, Morrison DC, Opal S, Yoneda K, Slotman G, Chambers H, Wiesenfeld H, Lemke J, Ryan JL, Horn D: A comparative trial of imipenem versus ceftazidime in the release of endotoxin and cytokine generation in patients with gram-negative urosepsis. Urosepsis Study Group. J Endotoxin Res. 2000;6(1):25-31. [Article]
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation. Synthesis of cross-linked peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcB
- Uniprot ID
- P02919
- Uniprot Name
- Penicillin-binding protein 1B
- Molecular Weight
- 94291.875 Da
References
- Nicolau DP: Carbapenems: a potent class of antibiotics. Expert Opin Pharmacother. 2008 Jan;9(1):23-37. [Article]
- Zhanel GG, Wiebe R, Dilay L, Thomson K, Rubinstein E, Hoban DJ, Noreddin AM, Karlowsky JA: Comparative review of the carbapenems. Drugs. 2007;67(7):1027-52. [Article]
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serine-type d-ala-d-ala carboxypeptidase activity
- Specific Function
- Cell wall formation. Synthesis of cross-linked peptidoglycan from the lipid intermediates. The enzyme has a penicillin-insensitive transglycosylase N-terminal domain (formation of linear glycan str...
- Gene Name
- mrcA
- Uniprot ID
- P02918
- Uniprot Name
- Penicillin-binding protein 1A
- Molecular Weight
- 93635.545 Da
References
- Nicolau DP: Carbapenems: a potent class of antibiotics. Expert Opin Pharmacother. 2008 Jan;9(1):23-37. [Article]
- Zhanel GG, Wiebe R, Dilay L, Thomson K, Rubinstein E, Hoban DJ, Noreddin AM, Karlowsky JA: Comparative review of the carbapenems. Drugs. 2007;67(7):1027-52. [Article]
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Kind
- Protein
- Organism
- Bacillus subtilis (strain 168)
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Penicillin binding
- Specific Function
- Not Available
- Gene Name
- pbpC
- Uniprot ID
- P42971
- Uniprot Name
- Penicillin-binding protein 3
- Molecular Weight
- 74405.915 Da
References
- Kind
- Protein
- Organism
- Proteus vulgaris
- Pharmacological action
- Unknown
- Actions
- Activator
- General Function
- Beta-lactamase activity
- Specific Function
- Hydrolyzes broad-spectrum beta-lactam antibiotics. Active against cephalosporins such as cefuroxime and cefotaxime.
- Gene Name
- blaB
- Uniprot ID
- P52664
- Uniprot Name
- Beta-lactamase
- Molecular Weight
- 32991.385 Da
References
- Chen HY, Livermore DM: Comparative in-vitro activity of biapenem against enterobacteria with beta-lactamase-mediated antibiotic resistance. J Antimicrob Chemother. 1994 Mar;33(3):453-64. doi: 10.1093/jac/33.3.453. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Zinc ion binding
- Specific Function
- Hydrolyzes a wide range of dipeptides. Implicated in the renal metabolism of glutathione and its conjugates. Converts leukotriene D4 to leukotriene E4; it may play an important role in the regulati...
- Gene Name
- DPEP1
- Uniprot ID
- P16444
- Uniprot Name
- Dipeptidase 1
- Molecular Weight
- 45673.48 Da
References
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Kind
- Protein
- Organism
- Escherichia coli
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Beta-lactamase activity
- Specific Function
- Not Available
- Gene Name
- bla
- Uniprot ID
- P0AD63
- Uniprot Name
- Beta-lactamase SHV-1
- Molecular Weight
- 31223.635 Da
References
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Kind
- Protein
- Organism
- Escherichia coli
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- TEM-type are the most prevalent beta-lactamases in enterobacteria; they hydrolyze the beta-lactam bond in susceptible beta-lactam antibiotics, thus conferring resistance to penicillins and cephalosporins. TEM-3 and TEM-4 are capable of hydrolyzing cefotaxime and ceftazidime. TEM-5 is capable of hydrolyzing ceftazidime. TEM-6 is capable of hydrolyzing ceftazidime and aztreonam. TEM-8/CAZ-2, TEM-16/CAZ-7 and TEM-24/CAZ-6 are markedly active against ceftazidime. IRT-4 shows resistance to beta-lactamase inhibitors.
- Specific Function
- Beta-lactamase activity
- Gene Name
- bla
- Uniprot ID
- P62593
- Uniprot Name
- Beta-lactamase TEM
- Molecular Weight
- 31514.865 Da
References
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Kind
- Protein group
- Organism
- Escherichia coli
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Not Available
- Specific Function
- Beta-lactamase activity
Components:
References
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
- Kind
- Protein
- Organism
- Klebsiella pneumoniae
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Not Available
- Specific Function
- Beta-lactamase activity
- Gene Name
- KPC-2
- Uniprot ID
- Q93LQ9
- Uniprot Name
- Beta-lactamase
- Molecular Weight
- 31114.99 Da
References
- Bradford PA, Bratu S, Urban C, Visalli M, Mariano N, Landman D, Rahal JJ, Brooks S, Cebular S, Quale J: Emergence of carbapenem-resistant Klebsiella species possessing the class A carbapenem-hydrolyzing KPC-2 and inhibitor-resistant TEM-30 beta-lactamases in New York City. Clin Infect Dis. 2004 Jul 1;39(1):55-60. doi: 10.1086/421495. Epub 2004 Jun 14. [Article]
- FDA Approved Drug Products: Recarbrio (imipenem, cilastatin, and relebactam) for intravenous injection [Link]
Drug created at August 29, 2007 18:42 / Updated at March 17, 2022 22:24