Cefixime
Identification
- Summary
Cefixime is a third generation cephalosporin used to treat susceptible Gram negative and Gram positive bacterial infections.
- Brand Names
- Suprax
- Generic Name
- Cefixime
- DrugBank Accession Number
- DB00671
- Background
Cefixime, an antibiotic, is a third-generation cephalosporin like ceftriaxone and cefotaxime. Cefixime is highly stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases, may be susceptible to cefixime. The antibacterial effect of cefixime results from inhibition of mucopeptide synthesis in the bacterial cell wall.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 453.45
Monoisotopic: 453.041289239 - Chemical Formula
- C16H15N5O7S2
- Synonyms
- (−)-cefixim
- Cefixim
- Cefixima
- Céfixime
- Cefixime
- Cefixime anhydrous
- Cefiximum
- External IDs
- FK 027
- FR 17027
Pharmacology
- Indication
For use in the treatment of the following infections when caused by susceptible strains of the designated microorganisms: (1) uncomplicated urinary tract infections caused by Escherichia coli and Proteus mirabilis, (2) otitis media caused by Haemophilus influenzae (beta-lactamase positive and negative strains), Moraxella catarrhalis (most of which are beta-lactamase positive), and S. pyogenes, (3) pharyngitis and tonsillitis caused by S. pyogenes, (4) acute bronchitis and acute exacerbations of chronic bronchitis caused by Streptococcus pneumoniae and Haemophilus influenzae (beta-lactamase positive and negative strains), and (5) uncomplicated gonorrhea (cervical/urethral) caused by Neisseria gonorrhoeae (penicillinase- and non-penicillinase-producing strains).
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
- Acute Exacerbation of Chronic Bronchitis caused by Streptococcus Pneumoniae
- Acute Exacerbations of Chronic Bronchitis caused by Haemophilus Influenzae
- Bacterial Sinusitis
- Community Acquired Pneumonia (CAP)
- Gonorrhea of anus
- Lyme Disease
- Salmonella Infections
- Shigella Infection
- Streptococcal Pharyngitis
- Tonsillitis streptococcal
- Uncomplicated Urinary Tract Infections
- Bacterial otitis media
- Bacterial rhinosinusitis
- Disease caused by Salmonella typhi
- Uncomplicated Gonorrhea
- 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
Cefixime, an antibiotic, is a third-generation cephalosporin like ceftriaxone and cefotaxime. Cefixime is highly stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases, may be susceptible to cefixime. The antibacterial effect of cefixime results from inhibition of mucopeptide synthesis in the bacterial cell wall.
- Mechanism of action
Like all beta-lactam antibiotics, cefixime binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cefixime interferes with an autolysin inhibitor.
Target Actions Organism APenicillin-binding protein 2 inhibitorHaemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) - Absorption
About 40%-50% absorbed orally whether administered with or without food, however, time to maximal absorption is increased approximately 0.8 hours when administered with food.
- Volume of distribution
Not Available
- Protein binding
65% (concentration independent)
- Metabolism
Hepatic. Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours.
- Route of elimination
Not Available
- Half-life
3-4 hours (may range up to 9 hours). In severe renal impairment (5 to 20 mL/min creatinine clearance), the half-life increased to an average of 11.5 hours.
- Clearance
Not Available
- 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
Symptoms of overdose include blood in the urine, diarrhea, nausea, upper abdominal pain, and vomiting.
- 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 softwareAbciximab The therapeutic efficacy of Abciximab can be decreased when used in combination with Cefixime. Acenocoumarol The risk or severity of bleeding can be increased when Cefixime is combined with Acenocoumarol. Alteplase The therapeutic efficacy of Alteplase can be decreased when used in combination with Cefixime. Ambroxol The risk or severity of methemoglobinemia can be increased when Cefixime is combined with Ambroxol. Ancrod The therapeutic efficacy of Ancrod can be decreased when used in combination with Cefixime. Anistreplase The therapeutic efficacy of Anistreplase can be decreased when used in combination with Cefixime. Antithrombin Alfa The therapeutic efficacy of Antithrombin Alfa can be decreased when used in combination with Cefixime. Antithrombin III human The therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Cefixime. Apixaban The therapeutic efficacy of Apixaban can be decreased when used in combination with Cefixime. Ardeparin The therapeutic efficacy of Ardeparin can be decreased when used in combination with Cefixime. 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
- Take with or without food.
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 Cefixime trihydrate 97I1C92E55 125110-14-7 IPYWNMVPZOAFOQ-NABDTECSSA-N - Product Images
- International/Other Brands
- Cefixoral (Menarini) / Cefspan (GlaxoSmithKline) / Cephoral (Merck) / Fixam (Solas) / Fixspor (Invision) / Hifen (Hetero) / InfectoOpticef (Infectopharm) / Kuracef (Sanofi-Aventis) / Letix (Adley) / Ofex (Delta) / Omnatax-O (Abbott) / Oracef (Micro Labs) / Oroken (Sanofi Aventis) / Sancefix (Sandoz) / Secef (Novartis) / Supran (Teva) / Suprax 125 (Lupin) / Tricef (Merck) / Unixime (Firma) / Uro-Cephoral (Merck)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Suprax Powder, for suspension 100 mg / 5 mL Oral Odan Laboratories Ltd 1990-12-31 Not applicable Canada Suprax Powder, for solution 100 mg / 5 mL Oral Aventis Pharma Ltd. 1990-12-31 2005-12-07 Canada Suprax Capsule 400 mg/1 Oral LUPIN LIMITED 2013-03-15 2018-12-03 US Suprax Capsule 400 mg/1 Oral Lupin Pharmaceuticals, Inc. 2013-03-15 Not applicable US Suprax Capsule 400 mg/1 Oral PD-Rx Pharmaceuticals, Inc. 2013-03-15 Not applicable US Suprax Tablet 400 mg Oral Aventis Pharma Ltd. 1990-12-31 2006-01-16 Canada Suprax Tablet 200 mg Oral Sanofi Aventis 1990-12-31 2006-05-05 Canada Suprax Tablet 400 mg Oral Odan Laboratories Ltd 1990-12-31 Not applicable Canada Suprax Capsule 400 mg/1 Oral REMEDYREPACK INC. 2019-04-09 2020-06-02 US Suprax Capsule 400 mg/1 Oral Remedy Repack 2018-02-02 2018-02-02 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Auro-cefixime Powder, for suspension 100 mg / 5 mL Oral Auro Pharma Inc 2018-01-08 Not applicable Canada Auro-cefixime Tablet 400 mg Oral Auro Pharma Inc 2014-10-24 Not applicable Canada Cefixime Powder, for suspension 100 mg/5mL Oral Belcher Pharmaceuticals,LLC 2017-03-15 Not applicable US Cefixime Powder, for suspension 200 mg/5mL Oral Northstar RxLLC 2018-05-11 Not applicable US Cefixime Powder, for suspension 100 mg/5mL Oral Dr. Reddy’s Laboratories, Inc 2017-08-03 Not applicable US Cefixime Powder, for suspension 100 mg/5mL Oral Aurobindo Pharma Limited 2015-04-14 Not applicable US Cefixime Powder, for suspension 100 mg/5mL Oral Northstar RxLLC 2018-05-11 Not applicable US Cefixime Capsule 400 mg/1 Oral REMEDYREPACK INC. 2021-09-14 Not applicable US Cefixime Powder, for suspension 200 mg/5mL Oral Lupin Pharmaceuticals, Inc. 2015-04-24 Not applicable US Cefixime Powder, for suspension 500 mg/5mL Oral Belcher Pharmaceuticals,LLC 2017-03-15 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image INNOCEF PLUS 100/62.5 MG SASE, 20 ADET Cefixime trihydrate (111.9 mg) + Clavulanate potassium (62.5 mg) Powder Oral VİTALİS İLAÇ SAN. TİC. A.Ş. 2020-08-14 Not applicable Turkey INNOCEF PLUS 200/125 MG SAŞE, 20 ADET Cefixime trihydrate (223.8 mg) + Clavulanate potassium (125 mg) Powder Oral VİTALİS İLAÇ SAN. TİC. A.Ş. 2020-08-14 Not applicable Turkey INNOCEF PLUS 200/62.5 MG SASE, 20 ADET Cefixime trihydrate (223.8 mg) + Clavulanate potassium (62.5 mg) Powder Oral VİTALİS İLAÇ SAN. TİC. A.Ş. 2020-08-14 Not applicable Turkey INNOCEF PLUS 400/125 MG SAŞE, 10 ADET Cefixime trihydrate (447.63 mg) + Clavulanate potassium (125 mg) Powder Oral VİTALİS İLAÇ SAN. TİC. A.Ş. 2020-08-14 Not applicable Turkey INNOCEF PLUS 400/125 MG SAŞE, 20 ADET Cefixime trihydrate (447.63 mg) + Clavulanate potassium (125 mg) Powder Oral VİTALİS İLAÇ SAN. TİC. A.Ş. 2020-08-14 Not applicable Turkey MOLCEF PLUS 100/62.5 MG FILM KAPLI TABLET, 20 ADET Cefixime (100 mg) + Clavulanic acid (62.5 mg) Tablet, coated Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2020-08-14 2021-08-05 Turkey MOLCEF PLUS 100/62.5/5 ML ORAL SUSPANSIYON HAZIRLAMAK ICIN KURU TOZ, 100 ML Cefixime (100 mg/5ml) + Clavulanic acid (62.5 mg/5ml) Suspension Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2020-08-14 2021-08-05 Turkey MOLCEF PLUS 200 MG+62.5/5 ML ORAL SÜSPANSİYON HAZIRLAMAK İÇİN KURU TOZ, 100 ML Cefixime (200 mg/5ml) + Clavulanic acid (62.5 mg/5ml) Suspension Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2020-08-14 2021-08-05 Turkey MOLCEF PLUS 200/125 MG FILM KAPLI TABLET, 20 ADET Cefixime (200 mg) + Clavulanic acid (125 mg) Tablet, coated Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2020-08-14 2021-08-05 Turkey MOLCEF PLUS 400/125 MG FILM KAPLI TABLET, 10 ADET Cefixime (400 mg) + Clavulanic acid (125 mg) Tablet, coated Oral NEUTEC İLAÇ SAN. TİC. A.Ş. 2020-08-14 2021-08-05 Turkey
Categories
- ATC Codes
- J01DD08 — Cefixime
- J01DD — Third-generation cephalosporins
- J01D — OTHER BETA-LACTAM ANTIBACTERIALS
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- J01RA — Combinations of antibacterials
- J01R — COMBINATIONS OF ANTIBACTERIALS
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cephalosporins. These are compounds containing a 1,2-thiazine fused to a 2-azetidinone to for a oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid moiety or a derivative thereof.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Lactams
- Sub Class
- Beta lactams
- Direct Parent
- Cephalosporins
- Alternative Parents
- N-acyl-alpha amino acids and derivatives / 2,4-disubstituted thiazoles / 1,3-thiazines / 2-amino-1,3-thiazoles / Dicarboxylic acids and derivatives / Tertiary carboxylic acid amides / Heteroaromatic compounds / Secondary carboxylic acid amides / Amino acids / Azetidines show 9 more
- Substituents
- 1,3-thiazol-2-amine / 2,4-disubstituted 1,3-thiazole / Alpha-amino acid or derivatives / Amine / Amino acid / Amino acid or derivatives / Aromatic heteropolycyclic compound / Azacycle / Azetidine / Azole show 23 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- cephalosporin (CHEBI:472657)
- Affected organisms
- Enteric bacteria and other eubacteria
Chemical Identifiers
- UNII
- XZ7BG04GJX
- CAS number
- 79350-37-1
- InChI Key
- OKBVVJOGVLARMR-QSWIMTSFSA-N
- InChI
- InChI=1S/C16H15N5O7S2/c1-2-6-4-29-14-10(13(25)21(14)11(6)15(26)27)19-12(24)9(20-28-3-8(22)23)7-5-30-16(17)18-7/h2,5,10,14H,1,3-4H2,(H2,17,18)(H,19,24)(H,22,23)(H,26,27)/b20-9-/t10-,14-/m1/s1
- IUPAC Name
- (6R,7R)-7-[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(carboxymethoxy)imino]acetamido]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
- SMILES
- [H][C@]12SCC(C=C)=C(N1C(=O)[C@H]2NC(=O)C(=N/OCC(O)=O)\C1=CSC(N)=N1)C(O)=O
References
- Synthesis Reference
Pandurang Deshpande, "Process for the preparation of cefixime." U.S. Patent US20040082560, issued April 29, 2004.
US20040082560- General References
- McMillan A, Young H: The treatment of pharyngeal gonorrhoea with a single oral dose of cefixime. Int J STD AIDS. 2007 Apr;18(4):253-4. [Article]
- Adam D, Hostalek U, Troster K: 5-day cefixime therapy for bacterial pharyngitis and/or tonsillitis: comparison with 10-day penicillin V therapy. Cefixime Study Group. Infection. 1995;23 Suppl 2:S83-6. [Article]
- External Links
- Human Metabolome Database
- HMDB0014809
- KEGG Drug
- D00258
- KEGG Compound
- C06881
- PubChem Compound
- 5362065
- PubChem Substance
- 46508684
- ChemSpider
- 4514923
- BindingDB
- 84007
- 25033
- ChEBI
- 472657
- ChEMBL
- CHEMBL1541
- ZINC
- ZINC000004468778
- Therapeutic Targets Database
- DAP000439
- PharmGKB
- PA164768821
- PDBe Ligand
- C04
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Cefixime
- PDB Entries
- 4kou
- FDA label
- Download (3.07 MB)
- MSDS
- Download (43.7 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Health Services Research Antibiotic Resistant Infection / Uncomplicated Urinary Tract Infections 1 4 Recruiting Treatment Disease caused by Salmonella typhi 1 4 Unknown Status Treatment Disease caused by Salmonella typhi 1 3 Active Not Recruiting Prevention Chronic Kidney Disease (CKD) / Renal Hypodysplasia, Nonsyndromic, 1 / Vesicoureteral Reflux (VUR) 1 3 Recruiting Treatment Human Immunodeficiency Virus (HIV) Infections / Syphilis 1 3 Terminated Treatment Bacterial Vaginitis / Cervicitis 1 3 Unknown Status Treatment Hepatic abscess 1 2 Completed Treatment Chlamydia Trachomatis Infection / Neisseria Gonorrhoeae Infection 1 2 Completed Treatment Early Syphilis / Syphilis 1 2 Completed Treatment Urinary Tract Infection 1
Pharmacoeconomics
- Manufacturers
- Lederle laboratories div american cyanamid co
- Lupin pharmaceuticals inc
- Lupin ltd
- Packagers
- A-S Medication Solutions LLC
- Dept Health Central Pharmacy
- Dispensing Solutions
- Lupin Pharmaceuticals Inc.
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmedix
- Physicians Total Care Inc.
- Redpharm Drug
- Remedy Repack
- Dosage Forms
Form Route Strength Capsule Oral 400.000 mg Tablet Oral 400.00 mg Capsule Oral 200.000 mg Suspension Oral 2.000 g Capsule Oral 400 mg Suspension Oral 2.000 g Capsule, coated Oral 400 mg Powder Parenteral 100 MG/5ML Granule, for suspension Oral Tablet Oral 400 mg Tablet Oral 200 mg Syrup Oral 2 g Tablet, film coated Oral 400 MG Powder, for suspension Oral Powder, for suspension Oral 2 g Powder, for suspension Oral 100 mg/5mL Powder, for suspension Oral 200 mg/5mL Capsule Oral Powder, for suspension Oral 1 g Suspension Oral Granule Oral 100 mg Syrup Oral 100 MG/5ML Solution / drops; suspension / drops Tablet, orally disintegrating Oral 400 mg Granule Oral Tablet, film coated Oral Granule Oral 100 MG/5ML Powder Oral Tablet, orally disintegrating Oral Powder Oral Tablet, coated Oral Suspension Oral Capsule Oral 100 MG Capsule Oral 200 MG Tablet, effervescent Syrup Oral Capsule Oral 111.19 MG Capsule Oral 223.8 MG Syrup Oral 100 mg Powder, for suspension Oral Granule, for suspension Oral 100 MG/5ML Suspension Oral 100 MG/5ML Tablet, coated Oral 400 MG Tablet, for suspension Oral 400 MG Capsule Oral 400 mg/1 Granule, for suspension Oral 2 g/100ml Powder, for solution Oral 100 mg / 5 mL Powder, for suspension Oral 100 mg / 5 mL Powder, for suspension Oral 500 mg/5mL Tablet Oral 400 mg/1 Tablet, chewable Oral 100 mg/1 Tablet, chewable Oral 200 mg/1 Tablet, coated Oral 200 MG Tablet Oral 200 mg / tab Capsule, coated Oral 52.5 mg Capsule Oral 112 MG Tablet, film coated Oral 224 MG Powder, for solution Oral 100 mg/5ml Tablet, film coated Oral 200 mg Tablet, effervescent 100 mg Tablet, effervescent 200 mg Tablet, effervescent 400 mg Tablet Oral Syrup Oral 50 mg/5ml - Prices
Unit description Cost Unit Suprax 400 mg Tablet 3.86USD tablet Suprax 100 mg/5ml Suspension 2.8USD ml Suprax 20 mg/ml Suspension 0.45USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9233112 No 2016-01-12 2028-12-14 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 218-225 °C Not Available water solubility 55.11 mg/L Not Available logP -0.4 Not Available - Predicted Properties
Property Value Source Water Solubility 0.104 mg/mL ALOGPS logP 0.25 ALOGPS logP -1.3 Chemaxon logS -3.6 ALOGPS pKa (Strongest Acidic) 2.54 Chemaxon pKa (Strongest Basic) 4.07 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 10 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 184.51 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 104.91 m3·mol-1 Chemaxon Polarizability 41.93 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.7776 Blood Brain Barrier - 0.9704 Caco-2 permeable - 0.7432 P-glycoprotein substrate Substrate 0.6934 P-glycoprotein inhibitor I Non-inhibitor 0.8863 P-glycoprotein inhibitor II Non-inhibitor 0.8724 Renal organic cation transporter Non-inhibitor 0.8301 CYP450 2C9 substrate Non-substrate 0.9002 CYP450 2D6 substrate Non-substrate 0.8161 CYP450 3A4 substrate Non-substrate 0.5 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9029 Ames test Non AMES toxic 0.7495 Carcinogenicity Non-carcinogens 0.8549 Biodegradation Not ready biodegradable 0.9911 Rat acute toxicity 1.6878 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9897 hERG inhibition (predictor II) Non-inhibitor 0.895
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 LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-004i-3920000000-3269e737530417831893
Targets

- Kind
- Protein
- Organism
- Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Penicillin binding
- Specific Function
- Cell wall formation; PBP-2 is responsible for the determination of the rod shape of the cell. Its synthesize cross-linked peptidoglycan from the lipid intermediates (By similarity).
- Gene Name
- mrdA
- Uniprot ID
- P44469
- Uniprot Name
- Penicillin-binding protein 2
- Molecular Weight
- 73812.47 Da
References
- Takahata S, Senju N, Osaki Y, Yoshida T, Ida T: Amino acid substitutions in mosaic penicillin-binding protein 2 associated with reduced susceptibility to cefixime in clinical isolates of Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2006 Nov;50(11):3638-45. Epub 2006 Aug 28. [Article]
- Zhao S, Duncan M, Tomberg J, Davies C, Unemo M, Nicholas RA: Genetics of chromosomally mediated intermediate resistance to ceftriaxone and cefixime in Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2009 Sep;53(9):3744-51. doi: 10.1128/AAC.00304-09. Epub 2009 Jun 15. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Symporter activity
- Specific Function
- Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
- Gene Name
- SLC22A5
- Uniprot ID
- O76082
- Uniprot Name
- Solute carrier family 22 member 5
- Molecular Weight
- 62751.08 Da
References
- Ganapathy ME, Huang W, Rajan DP, Carter AL, Sugawara M, Iseki K, Leibach FH, Ganapathy V: beta-lactam antibiotics as substrates for OCTN2, an organic cation/carnitine transporter. J Biol Chem. 2000 Jan 21;275(3):1699-707. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Proton-dependent oligopeptide secondary active transmembrane transporter activity
- Specific Function
- Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
- Gene Name
- SLC15A1
- Uniprot ID
- P46059
- Uniprot Name
- Solute carrier family 15 member 1
- Molecular Weight
- 78805.265 Da
References
- Wenzel U, Gebert I, Weintraut H, Weber WM, Clauss W, Daniel H: Transport characteristics of differently charged cephalosporin antibiotics in oocytes expressing the cloned intestinal peptide transporter PepT1 and in human intestinal Caco-2 cells. J Pharmacol Exp Ther. 1996 May;277(2):831-9. [Article]
- Ganapathy ME, Prasad PD, Mackenzie B, Ganapathy V, Leibach FH: Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2. Biochim Biophys Acta. 1997 Mar 13;1324(2):296-308. [Article]
- Luckner P, Brandsch M: Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1. Eur J Pharm Biopharm. 2005 Jan;59(1):17-24. [Article]
- Terada T, Saito H, Mukai M, Inui K: Characterization of stably transfected kidney epithelial cell line expressing rat H+/peptide cotransporter PEPT1: localization of PEPT1 and transport of beta-lactam antibiotics. J Pharmacol Exp Ther. 1997 Jun;281(3):1415-21. [Article]
- Terada T, Saito H, Mukai M, Inui K: Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells. Am J Physiol. 1997 Nov;273(5 Pt 2):F706-11. [Article]
- Tsuji A: Transporter-mediated Drug Interactions. Drug Metab Pharmacokinet. 2002;17(4):253-74. [Article]
- Tamai I, Nakanishi T, Hayashi K, Terao T, Sai Y, Shiraga T, Miyamoto K, Takeda E, Higashida H, Tsuji A: The predominant contribution of oligopeptide transporter PepT1 to intestinal absorption of beta-lactam antibiotics in the rat small intestine. J Pharm Pharmacol. 1997 Aug;49(8):796-801. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Peptide:proton symporter activity
- Specific Function
- Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides.
- Gene Name
- SLC15A2
- Uniprot ID
- Q16348
- Uniprot Name
- Solute carrier family 15 member 2
- Molecular Weight
- 81782.77 Da
References
- Ganapathy ME, Prasad PD, Mackenzie B, Ganapathy V, Leibach FH: Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2. Biochim Biophys Acta. 1997 Mar 13;1324(2):296-308. [Article]
- Terada T, Saito H, Mukai M, Inui K: Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells. Am J Physiol. 1997 Nov;273(5 Pt 2):F706-11. [Article]
- Luckner P, Brandsch M: Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1. Eur J Pharm Biopharm. 2005 Jan;59(1):17-24. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 28, 2023 01:14