Identification

Name
Dicloxacillin
Accession Number
DB00485  (APRD00916)
Type
Small Molecule
Groups
Approved, Vet Approved
Description

One of the penicillins which is resistant to penicillinase. [PubChem]

Structure
Thumb
Synonyms
  • (2S,5R,6R)-6-({[3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]carbonyl}amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
  • Dicloxacilina
  • Dicloxacillin
  • Dicloxacillina
  • Dicloxacilline
  • Dicloxacillinum
External IDs
Bayer 5488 / BRL 1702 / P 1011 / R 13423
Product Ingredients
IngredientUNIICASInChI Key
Dicloxacillin sodium4CKS6MOL6Z343-55-5GXOMMGAFBINOJY-UHFFFAOYSA-M
Dicloxacillin sodium monohydrateNot AvailableNot AvailableNot applicable
Product Images
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dicloxacillin SodiumCapsule500 mg/1OralA S Medication Solutions1990-09-302017-06-20Us
Dicloxacillin SodiumCapsule500 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-19Not applicableUs
Dicloxacillin SodiumCapsule250 mg/1OralTeva1990-09-30Not applicableUs00093 3123 01 nlmimage10 eb26f597
Dicloxacillin SodiumCapsule500 mg/1OralPd Rx Pharmaceuticals, Inc.1971-04-01Not applicableUs
Dicloxacillin SodiumCapsule250 mg/1OralAvera Mc Kennan Hospital2015-10-01Not applicableUs
Dicloxacillin SodiumCapsule250 mg/1OralLiberty Pharmaceuticals, Inc.1990-09-30Not applicableUs
Dicloxacillin SodiumCapsule250 mg/1OralPd Rx Pharmaceuticals, Inc.1990-09-30Not applicableUs
Dicloxacillin SodiumCapsule250 mg/1OralA S Medication Solutions1990-09-302017-06-20Us
Dicloxacillin SodiumCapsule500 mg/1OralAvera Mc Kennan Hospital2016-01-28Not applicableUs
Dicloxacillin SodiumCapsule250 mg/1OralA S Medication Solutions1990-09-302017-06-20Us
International/Other Brands
Amcidil (MacroPhar) / Betaclox (Eskayef) / Cloxagen (Genamerica) / Dacocilin (CCPC) / Damacir (Damacir) / Dicillin (Sandoz) / Diclex (Meiji) / Diclocil (Bristol-Myers Squibb) / Dicloplus (Icofarma) / Dicloson (Unison) / Dicloxal (Magma) / Dicloxgen (General Drugs House) / Dicloxina (ECU) / Dyclobiot (Medifarma) / Dynapen / Posipen (GlaxoSmithKline) / Quimocyclar (Armofar) / Staklox (Actavis) / Terbocloxil (Terbol) / Ziefmycin (Yung Shin)
Categories
UNII
COF19H7WBK
CAS number
3116-76-5
Weight
Average: 470.326
Monoisotopic: 469.026596773
Chemical Formula
C19H17Cl2N3O5S
InChI Key
YFAGHNZHGGCZAX-JKIFEVAISA-N
InChI
InChI=1S/C19H17Cl2N3O5S/c1-7-10(12(23-29-7)11-8(20)5-4-6-9(11)21)15(25)22-13-16(26)24-14(18(27)28)19(2,3)30-17(13)24/h4-6,13-14,17H,1-3H3,(H,22,25)(H,27,28)/t13-,14+,17-/m1/s1
IUPAC Name
(2S,5R,6R)-6-[3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazole-4-amido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
SMILES
[H][[email protected]]12SC(C)(C)[[email protected]@H](N1C(=O)[[email protected]]2NC(=O)C1=C(C)ON=C1C1=C(Cl)C=CC=C1Cl)C(O)=O

Pharmacology

Indication

Used to treat infections caused by penicillinase-producing staphylococci which have demonstrated susceptibility to the drug.

Structured Indications
Pharmacodynamics

Dicloxacillin is a beta-lactamase resistant penicillin similar to oxacillin. Dicloxacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of dicloxacillin results from the inhibition of cell wall synthesis and is mediated through dicloxacillin binding to penicillin binding proteins (PBPs). Dicloxacillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.

Mechanism of action

Dicloxacillin exerts a bactericidal action against penicillin-susceptible microorganisms during the state of active multiplication. All penicillins inhibit the biosynthesis of the bacterial cell wall. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, dicloxacillin inhibits 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 dicloxacillin interferes with an autolysin inhibitor.

TargetActionsOrganism
APenicillin-binding protein 3
inhibitor
Listeria monocytogenes serotype 4b str. LL195
APenicillin-binding protein 1b
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
APenicillin-binding protein 2a
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
APenicillin-binding protein 3
inhibitor
Streptococcus pneumoniae
APenicillin-binding protein 1A
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
APenicillin-binding protein 2B
inhibitor
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Absorption

Absorption of the isoxazolyl penicillins after oral administration is rapid but incomplete: peak blood levels are achieved in 1-1.5 hours. Oral absorption of cloxacillin, dicloxacillin, oxacillin and nafcillin is delayed when the drugs are administered after meals.

Volume of distribution
Not Available
Protein binding

Binds to serum protein, mainly albumin.

Metabolism
Not Available
Route of elimination

Dicloxacillin sodium is rapidly excreted as unchanged drug in the urine by glomerular filtration and active tubular secretion.

Half life

The elimination half-life for dicloxacillin is about 0.7 hour.

Clearance
Not Available
Toxicity

Oral LD50 in rat is 3579 mg/kg. Symptoms of overexposure include irritation, rash, labored breathing, hives, itching, wheezing, nausea, chills, and fever.

Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcenocoumarolDicloxacillin may decrease the anticoagulant activities of Acenocoumarol.Approved
AclarubicinThe serum concentration of Aclarubicin can be decreased when it is combined with Dicloxacillin.Investigational
AmikacinThe serum concentration of Amikacin can be decreased when it is combined with Dicloxacillin.Approved, Vet Approved
AmrubicinThe serum concentration of Amrubicin can be decreased when it is combined with Dicloxacillin.Approved, Investigational
annamycinThe serum concentration of annamycin can be decreased when it is combined with Dicloxacillin.Investigational
ApramycinThe serum concentration of Apramycin can be decreased when it is combined with Dicloxacillin.Experimental, Vet Approved
ArbekacinThe serum concentration of Arbekacin can be decreased when it is combined with Dicloxacillin.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Dicloxacillin.Approved, Investigational
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Dicloxacillin.Investigational
BekanamycinThe serum concentration of Bekanamycin can be decreased when it is combined with Dicloxacillin.Experimental
ChlortetracyclineThe therapeutic efficacy of Dicloxacillin can be decreased when used in combination with Chlortetracycline.Approved, Investigational, Vet Approved
ClorindioneDicloxacillin may decrease the anticoagulant activities of Clorindione.Experimental
DaunorubicinThe serum concentration of Daunorubicin can be decreased when it is combined with Dicloxacillin.Approved
DemeclocyclineThe therapeutic efficacy of Dicloxacillin can be decreased when used in combination with Demeclocycline.Approved
DibekacinThe serum concentration of Dibekacin can be decreased when it is combined with Dicloxacillin.Experimental
DicoumarolDicloxacillin may decrease the anticoagulant activities of Dicoumarol.Approved
DihydrostreptomycinThe serum concentration of Dihydrostreptomycin can be decreased when it is combined with Dicloxacillin.Investigational, Vet Approved
DiphenadioneDicloxacillin may decrease the anticoagulant activities of Diphenadione.Experimental
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Dicloxacillin.Approved, Investigational
DoxycyclineThe therapeutic efficacy of Dicloxacillin can be decreased when used in combination with Doxycycline.Approved, Investigational, Vet Approved
EpirubicinThe serum concentration of Epirubicin can be decreased when it is combined with Dicloxacillin.Approved
Ethyl biscoumacetateDicloxacillin may decrease the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
FluindioneDicloxacillin may decrease the anticoagulant activities of Fluindione.Investigational
FramycetinThe serum concentration of Framycetin can be decreased when it is combined with Dicloxacillin.Approved
GeneticinThe serum concentration of Geneticin can be decreased when it is combined with Dicloxacillin.Experimental
GentamicinThe serum concentration of Gentamicin can be decreased when it is combined with Dicloxacillin.Approved, Vet Approved
GENTAMICIN C1AThe serum concentration of GENTAMICIN C1A can be decreased when it is combined with Dicloxacillin.Experimental
GPX-150The serum concentration of GPX-150 can be decreased when it is combined with Dicloxacillin.Investigational
Hygromycin BThe serum concentration of Hygromycin B can be decreased when it is combined with Dicloxacillin.Vet Approved
IdarubicinThe serum concentration of Idarubicin can be decreased when it is combined with Dicloxacillin.Approved
INNO-206The serum concentration of INNO-206 can be decreased when it is combined with Dicloxacillin.Investigational
IsepamicinThe serum concentration of Isepamicin can be decreased when it is combined with Dicloxacillin.Experimental
KanamycinThe serum concentration of Kanamycin can be decreased when it is combined with Dicloxacillin.Approved, Investigational, Vet Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Dicloxacillin.Approved
MetrizamideThe serum concentration of Metrizamide can be decreased when it is combined with Dicloxacillin.Approved
MicronomicinThe serum concentration of Micronomicin can be decreased when it is combined with Dicloxacillin.Experimental
MinocyclineThe therapeutic efficacy of Dicloxacillin can be decreased when used in combination with Minocycline.Approved, Investigational
Mycophenolic acidThe serum concentration of the active metabolites of Mycophenolic acid can be reduced when Mycophenolic acid is used in combination with Dicloxacillin resulting in a loss in efficacy.Approved
NeamineThe serum concentration of Neamine can be decreased when it is combined with Dicloxacillin.Experimental
NeomycinThe serum concentration of Neomycin can be decreased when it is combined with Dicloxacillin.Approved, Vet Approved
NetilmicinThe serum concentration of Netilmicin can be decreased when it is combined with Dicloxacillin.Approved, Investigational
ParomomycinThe serum concentration of Paromomycin can be decreased when it is combined with Dicloxacillin.Approved, Investigational
PhenindioneDicloxacillin may decrease the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonDicloxacillin may decrease the anticoagulant activities of Phenprocoumon.Approved, Investigational
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Dicloxacillin.Approved
PirarubicinThe serum concentration of Pirarubicin can be decreased when it is combined with Dicloxacillin.Investigational
PlazomicinThe serum concentration of Plazomicin can be decreased when it is combined with Dicloxacillin.Investigational
PlicamycinThe serum concentration of Plicamycin can be decreased when it is combined with Dicloxacillin.Approved, Investigational, Withdrawn
ProbenecidThe serum concentration of Dicloxacillin can be increased when it is combined with Probenecid.Approved
PuromycinThe serum concentration of Puromycin can be decreased when it is combined with Dicloxacillin.Experimental
RibostamycinThe serum concentration of Ribostamycin can be decreased when it is combined with Dicloxacillin.Approved, Investigational
SabarubicinThe serum concentration of Sabarubicin can be decreased when it is combined with Dicloxacillin.Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Dicloxacillin.Approved
SisomicinThe serum concentration of Sisomicin can be decreased when it is combined with Dicloxacillin.Investigational
SP1049CThe serum concentration of SP1049C can be decreased when it is combined with Dicloxacillin.Investigational
SpectinomycinThe serum concentration of Spectinomycin can be decreased when it is combined with Dicloxacillin.Approved, Investigational, Vet Approved
StreptomycinThe serum concentration of Streptomycin can be decreased when it is combined with Dicloxacillin.Approved, Vet Approved
StreptozocinThe serum concentration of Streptozocin can be decreased when it is combined with Dicloxacillin.Approved
TioclomarolDicloxacillin may decrease the anticoagulant activities of Tioclomarol.Experimental
TobramycinThe serum concentration of Tobramycin can be decreased when it is combined with Dicloxacillin.Approved, Investigational
ValrubicinThe serum concentration of Valrubicin can be decreased when it is combined with Dicloxacillin.Approved
WarfarinDicloxacillin may decrease the anticoagulant activities of Warfarin.Approved
Zoptarelin doxorubicinThe serum concentration of Zoptarelin doxorubicin can be decreased when it is combined with Dicloxacillin.Investigational
ZorubicinThe serum concentration of Zorubicin can be decreased when it is combined with Dicloxacillin.Experimental
Food Interactions
  • Take on an empty stomach, food decreases the availability.

References

Synthesis Reference

Sallmann, A. and Pfister, R.; U.S.Patent 3,558,690; January 26,1971; assigned to Geigy Chemical Corporation. Sallmann, A. and Pfister, R.; US. Patent 3,652,762; March 28,1972; assigned to Ciba Geigy Corporation.

General References
Not Available
External Links
Human Metabolome Database
HMDB14628
KEGG Drug
D02348
KEGG Compound
C06950
PubChem Compound
18381
PubChem Substance
46508182
ChemSpider
17358
BindingDB
50350476
ChEBI
4511
ChEMBL
CHEMBL893
Therapeutic Targets Database
DAP000435
PharmGKB
PA164749649
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Dicloxacillin
ATC Codes
J01CR50 — Combinations of penicillinsJ01CF01 — Dicloxacillin
MSDS
Download (51.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentOsteomyelitis1
1RecruitingTreatmentHealthy Volunteers1
3CompletedTreatmentBacteremia / Bacterial Infections / Infections, Gram-Positive Bacterial1

Pharmacoeconomics

Manufacturers
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Glaxosmithkline
  • Wyeth ayerst laboratories
  • Apothecon inc div bristol myers squibb
Packagers
Dosage forms
FormRouteStrength
CapsuleOral250 mg/1
CapsuleOral500 mg/1
Prices
Unit descriptionCostUnit
Dicloxacillin Sodium 500 mg capsule1.25USD capsule
Dicloxacillin 500 mg capsule1.2USD capsule
Dicloxacillin Sodium 250 mg capsule0.69USD capsule
Dicloxacillin 250 mg capsule0.66USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility3.63 mg/LNot Available
logP2.91HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.0296 mg/mLALOGPS
logP3.19ALOGPS
logP2.91ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)3.75ChemAxon
pKa (Strongest Basic)-0.71ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area112.74 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity111.44 m3·mol-1ChemAxon
Polarizability42.86 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8368
Blood Brain Barrier-0.9903
Caco-2 permeable-0.8957
P-glycoprotein substrateNon-substrate0.6204
P-glycoprotein inhibitor INon-inhibitor0.8951
P-glycoprotein inhibitor IINon-inhibitor0.9204
Renal organic cation transporterNon-inhibitor0.9629
CYP450 2C9 substrateNon-substrate0.8262
CYP450 2D6 substrateNon-substrate0.905
CYP450 3A4 substrateSubstrate0.5977
CYP450 1A2 substrateInhibitor0.8592
CYP450 2C9 inhibitorNon-inhibitor0.891
CYP450 2D6 inhibitorNon-inhibitor0.918
CYP450 2C19 inhibitorNon-inhibitor0.8832
CYP450 3A4 inhibitorNon-inhibitor0.819
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9186
Ames testNon AMES toxic0.6979
CarcinogenicityCarcinogens 0.5672
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9946 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9996
hERG inhibition (predictor II)Non-inhibitor0.8486
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as n-acyl-alpha amino acids and derivatives. These are compounds containing an alpha amino acid (or a derivative thereof) which bears an acyl group at its terminal nitrogen atom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
N-acyl-alpha amino acids and derivatives
Alternative Parents
Penams / Dichlorobenzenes / Aryl chlorides / Thiazolidines / Tertiary carboxylic acid amides / Heteroaromatic compounds / Isoxazoles / Azetidines / Thiohemiaminal derivatives / Azacyclic compounds
show 12 more
Substituents
N-acyl-alpha amino acid or derivatives / Penam / 1,3-dichlorobenzene / Halobenzene / Chlorobenzene / Aryl chloride / Aryl halide / Benzenoid / Monocyclic benzene moiety / Azole
show 31 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
dichlorobenzene, penicillin (CHEBI:4511)

Targets

Kind
Protein
Organism
Listeria monocytogenes serotype 4b str. LL195
Pharmacological action
Yes
Actions
Inhibitor
General Function
Not Available
Specific Function
Penicillin binding
Gene Name
pbpC
Uniprot ID
A0A0E1R3H3
Uniprot Name
Penicillin-binding protein 3
Molecular Weight
75015.58 Da
References
  1. Gutkind GO, Ogueta SB, de Urtiaga AC, Mollerach ME, de Torres RA: Participation of PBP 3 in the acquisition of dicloxacillin resistance in Listeria monocytogenes. J Antimicrob Chemother. 1990 May;25(5):751-8. [PubMed:2115510]
Kind
Protein
Organism
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Transferase activity, transferring acyl groups
Specific Function
Not Available
Gene Name
pbp1b
Uniprot ID
Q7CRA4
Uniprot Name
Penicillin-binding protein 1b
Molecular Weight
89479.92 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [PubMed:7447421]
Kind
Protein
Organism
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Transferase activity, transferring acyl groups
Specific Function
Not Available
Gene Name
pbp2a
Uniprot ID
Q8DNB6
Uniprot Name
Penicillin-binding protein 2a
Molecular Weight
80797.94 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [PubMed:7447421]
Kind
Protein
Organism
Streptococcus pneumoniae
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine-type d-ala-d-ala carboxypeptidase activity
Specific Function
Not Available
Gene Name
pbp3
Uniprot ID
Q75Y35
Uniprot Name
Penicillin-binding protein 3
Molecular Weight
45209.84 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [PubMed:7447421]
Kind
Protein
Organism
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Penicillin binding
Specific Function
Cell wall formation.
Gene Name
pbpA
Uniprot ID
Q8DR59
Uniprot Name
Penicillin-binding protein 1A
Molecular Weight
79700.9 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [PubMed:7447421]
Kind
Protein
Organism
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Not Available
Specific Function
Penicillin binding
Gene Name
penA
Uniprot ID
P0A3M6
Uniprot Name
Penicillin-binding protein 2B
Molecular Weight
73872.305 Da
References
  1. Williamson R, Hakenbeck R, Tomasz A: In vivo interaction of beta-lactam antibiotics with the penicillin-binding proteins of Streptococcus pneumoniae. Antimicrob Agents Chemother. 1980 Oct;18(4):629-37. [PubMed:7447421]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Yasuda K, Ranade A, Venkataramanan R, Strom S, Chupka J, Ekins S, Schuetz E, Bachmann K: A comprehensive in vitro and in silico analysis of antibiotics that activate pregnane X receptor and induce CYP3A4 in liver and intestine. Drug Metab Dispos. 2008 Aug;36(8):1689-97. doi: 10.1124/dmd.108.020701. Epub 2008 May 27. [PubMed:18505790]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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
  1. 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. [PubMed:15567297]
Kind
Protein
Organism
Human
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
  1. 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. [PubMed:15567297]

Drug created on June 13, 2005 07:24 / Updated on November 23, 2017 11:06