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Identification
NameDesloratadine
Accession NumberDB00967  (APRD00324)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Desloratadine is a second generation, tricyclic antihistamine that which has a selective and peripheral H1-antagonist action. It is the active descarboethoxy metabolite of loratidine (a second generation histamine). Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.

Structure
Thumb
Synonyms
8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
8-chloro-6,11-dihydro-11-(4-Piperidinylidene)-5H-benzo(5,6)cyclohepta(1,2-b)pyridine
Descarboethoxyloratadine
DESLORATADINE
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Clarinextablet, film coated5 mg/1oralMerck Sharp & Dohme Corp.2001-12-21Not applicableUs
Clarinextablet, film coated5 mg/1oralPhysicians Total Care, Inc.2002-06-03Not applicableUs
Clarinextablet, film coated5 mg/1oralRebel Distributors Corp2002-02-08Not applicableUs
Clarinexsolution.5 mg/mLoralMerck Sharp & Dohme Corp.2004-09-01Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Desloratadinetablet, orally disintegrating5 mg/1oralDr. Reddy's Laboratories Limited2013-01-11Not applicableUs
Desloratadinetablet, film coated5 mg/1oralMylan Pharmaceuticals Inc.2012-07-02Not applicableUs
Desloratadinetablet5 mg/1oralVirtus Pharmaceuticals2012-07-01Not applicableUs
Desloratadinesolution.5 mg/mLoralTaro Pharmaceuticals U.S.A., Inc.2015-07-01Not applicableUs
Desloratadinetablet5 mg/1oralVirtus Pharmaceuticals2015-06-12Not applicableUs
Desloratadinetablet5 mg/1oralAv Pak2013-10-09Not applicableUs
Desloratadinetablet, film coated5 mg/1oralLupin Pharmaceuticals, Inc.2013-02-14Not applicableUs
Desloratadinetablet5 mg/1oralAv Pak2015-11-25Not applicableUs
Desloratadinetablet5 mg/1oralbryant ranch prepack2012-07-01Not applicableUs
Desloratadinetablet5 mg/1oralAv Kare, Inc.2015-11-24Not applicableUs
Desloratadinetablet, film coated5 mg/1oralSun Pharmaceutical Industries Limited2010-11-24Not applicableUs
Desloratadinetablet5 mg/1oralAv Kare, Inc.2012-07-05Not applicableUs
Desloratadinetablet5 mg/1oralBelcher Pharmaceuticals,LLC2012-05-15Not applicableUs
Desloratadinetablet5 mg/1oralSandoz Inc2013-07-01Not applicableUs
Desloratadinetablet, orally disintegrating2.5 mg/1oralDr. Reddy's Laboratories Limited2013-01-11Not applicableUs
Desloratadinetablet, film coated5 mg/1oralPaddock Laboratories, LLC2014-01-10Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aeriustablet5 mgoralBayer Inc Consumer Care2002-01-10Not applicableCanada
Aeriussyrup0.5 mgoralBayer Inc Consumer CareNot applicableNot applicableCanada
Aerius Kidssyrup0.5 mgoralBayer Inc Consumer Care2005-03-21Not applicableCanada
Allergy Control Desloratadinetablet5 mgoralPharmascience IncNot applicableNot applicableCanada
Allernix Multi Symptomtablet5 mgoralTeva Canada Limited2012-01-31Not applicableCanada
Desloratadine Allergy Controltablet5 mgoralPharmel Inc2014-03-10Not applicableCanada
Desloratadine Allergy Controltablet5 mgoralPharmascience Inc2009-12-24Not applicableCanada
Desloratadine Tabletstablet5 mgoralApotex Inc2010-05-27Not applicableCanada
Unapproved/Other Products Not Available
International Brands
NameCompany
ClaramaxNot Available
NeoClaritynNot Available
Brand mixtures
NameLabellerIngredients
Aerius Dual Action 12 HourBayer Inc Consumer Care
Aerius Dual Action 24 HourBayer Inc Consumer Care
Clarinex-D 12 HourMerck Sharp & Dohme Corp.
SaltsNot Available
Categories
UNIIFVF865388R
CAS number100643-71-8
WeightAverage: 310.821
Monoisotopic: 310.123676325
Chemical FormulaC19H19ClN2
InChI KeyInChIKey=JAUOIFJMECXRGI-UHFFFAOYSA-N
InChI
InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2
IUPAC Name
13-chloro-2-(piperidin-4-ylidene)-4-azatricyclo[9.4.0.0³,⁸]pentadeca-1(11),3(8),4,6,12,14-hexaene
SMILES
ClC1=CC2=C(C=C1)C(=C1CCNCC1)C1=C(CC2)C=CC=N1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzocycloheptapyridines. These are aromatic compounds containing a benzene ring and a pyridine ring fused to a seven membered carbocycle.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzocycloheptapyridines
Sub ClassNot Available
Direct ParentBenzocycloheptapyridines
Alternative Parents
Substituents
  • Benzocycloheptapyridine
  • Chlorobenzene
  • Benzenoid
  • Pyridine
  • Piperidine
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Azacycle
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the relief of symptoms of seasonal allergic rhinitis, perennial (non-seasonal) allergic rhinitis. Desloratidine is also used for the sympomatic treatment of pruritus and urticaria (hives) associated with chronic idiopathic urticaria.
PharmacodynamicsDesloratadine is a long-acting second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergies. Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness.
Mechanism of actionLike other H1-blockers, Desloratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding82-87%
MetabolismNot Available
Route of eliminationDesloratadine (a major metabolite of loratadine) is extensively metabolized to 3-hydroxydesloratadine, an active metabolite, which is subsequently glucuronidated. Approximately 87% of a 14C-desloratadine dose was equally recovered in urine and feces.
Half life50 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.965
Caco-2 permeable-0.5121
P-glycoprotein substrateSubstrate0.7758
P-glycoprotein inhibitor IInhibitor0.6694
P-glycoprotein inhibitor IINon-inhibitor0.794
Renal organic cation transporterInhibitor0.6979
CYP450 2C9 substrateNon-substrate0.8554
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5634
CYP450 1A2 substrateInhibitor0.7786
CYP450 2C9 inhibitorNon-inhibitor0.738
CYP450 2D6 inhibitorNon-inhibitor0.7377
CYP450 2C19 inhibitorNon-inhibitor0.7837
CYP450 3A4 inhibitorNon-inhibitor0.8332
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6083
Ames testNon AMES toxic0.6514
CarcinogenicityNon-carcinogens0.9367
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.0370 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7382
hERG inhibition (predictor II)Inhibitor0.8016
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Schering corp
  • Doctor reddys laboratories ltd
  • Schering plough corp
  • Orchid healthcare
Packagers
Dosage forms
FormRouteStrength
Tabletoral5 mg
Tablet (extended-release)oral
Tablet (immediate and extended release)oral
Syruporal0.5 mg
Solutionoral.5 mg/mL
Tablet, film coatedoral5 mg/1
Tablet, extended releaseoral
Tabletoral5 mg/1
Tablet, orally disintegratingoral2.5 mg/1
Tablet, orally disintegratingoral5 mg/1
Prices
Unit descriptionCostUnit
Clarinex Reditabs 30 5 mg Dispersible Tablet Box150.0USD box
Clarinex Reditabs 30 2.5 mg Dispersible Tablet Box147.14USD box
Clarinex-D 24 Hour 5-240 mg 24 Hour tablet5.0USD tablet
Clarinex-d 24 hour tablet4.8USD tablet
Clarinex 5 mg tablet4.57USD tablet
Clarinex-D 12 Hour 2.5-120 mg 12 Hour tablet3.2USD tablet
Clarinex-d 12 hour tablet3.08USD tablet
Clarinex 0.5 mg/ml Syrup0.48USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2267136 No2000-11-282018-02-06Canada
CA2294352 No2008-05-062018-07-01Canada
US5178878 No1993-01-122010-01-12Us
US5607697 Yes1995-12-072015-12-07Us
US6100274 Yes2000-01-072020-01-07Us
US6514520 Yes1998-12-012018-12-01Us
US6709676 No2001-02-182021-02-18Us
US6979463 No2002-03-282022-03-28Us
US7405223 Yes2000-01-072020-01-07Us
US7618649 Yes2001-06-192021-06-19Us
US7820199 Yes2002-09-282022-09-28Us
US8187630 No2000-12-192020-12-19Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP3.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00395 mg/mLALOGPS
logP3.48ALOGPS
logP3.97ChemAxon
logS-4.9ALOGPS
pKa (Strongest Basic)9.73ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area24.92 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity101.04 m3·mol-1ChemAxon
Polarizability34.35 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Zoltan Toth, “Processes for preparation of polymorphic forms of desloratadine.” U.S. Patent US20040242619, issued December 02, 2004.

US20040242619
General References
  1. Mann RD, Pearce GL, Dunn N, Shakir S: Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice. BMJ. 2000 Apr 29;320(7243):1184-6. [PubMed:10784544 ]
  2. Glass DJ, Harper AS: Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine. BMC Fam Pract. 2003 Aug 13;4:10. Epub 2003 Aug 13. [PubMed:12917016 ]
  3. See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6. [PubMed:14655812 ]
  4. Devillier P, Roche N, Faisy C: Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30. [PubMed:18336052 ]
  5. Bachert C: A review of the efficacy of desloratadine, fexofenadine, and levocetirizine in the treatment of nasal congestion in patients with allergic rhinitis. Clin Ther. 2009 May;31(5):921-44. doi: 10.1016/j.clinthera.2009.05.017. [PubMed:19539095 ]
  6. DuBuske L: Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy. Am J Clin Dermatol. 2007;8(5):271-83. [PubMed:17902729 ]
  7. Bachert C, Maurer M: Safety and efficacy of desloratadine in subjects with seasonal allergic rhinitis or chronic urticaria: results of four postmarketing surveillance studies. Clin Drug Investig. 2010;30(2):109-22. doi: 10.2165/11530930-000000000-00000. [PubMed:20067329 ]
  8. Simons FE, Prenner BM, Finn A Jr: Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. J Allergy Clin Immunol. 2003 Mar;111(3):617-22. [PubMed:12642846 ]
External Links
ATC CodesR06AX27
AHFS Codes
  • 04:08.00
PDB EntriesNot Available
FDA labelDownload (200 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Desloratadine.
AmphetamineAmphetamine may decrease the sedative activities of Desloratadine.
AzelastineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Desloratadine.
Benzylpenicilloyl PolylysineDesloratadine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Desloratadine.
Botulinum Toxin Type ADesloratadine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BDesloratadine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
BuprenorphineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CathinoneCathinone may decrease the sedative activities of Desloratadine.
Cimetropium BromideDesloratadine may increase the anticholinergic activities of Cimetropium Bromide.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
EluxadolineDesloratadine may increase the activities of Eluxadoline.
EthanolDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Desloratadine is combined with Glucagon recombinant.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Desloratadine.
HydrocodoneDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Desloratadine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Desloratadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Desloratadine.
LumacaftorThe serum concentration of Desloratadine can be decreased when it is combined with Lumacaftor.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
MethotrimeprazineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineDesloratadine may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Desloratadine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
MirabegronThe risk or severity of adverse effects can be increased when Desloratadine is combined with Mirabegron.
MirtazapineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MorphineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
OrphenadrineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
Potassium ChlorideDesloratadine may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleDesloratadine may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Desloratadine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Desloratadine.
RamosetronDesloratadine may increase the activities of Ramosetron.
RanolazineThe serum concentration of Desloratadine can be increased when it is combined with Ranolazine.
RopiniroleDesloratadine may increase the sedative activities of Ropinirole.
RotigotineDesloratadine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Desloratadine.
SaquinavirThe serum concentration of Desloratadine can be increased when it is combined with Saquinavir.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Desloratadine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Desloratadine.
SuvorexantDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Desloratadine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
TesmilifeneThe serum concentration of Desloratadine can be decreased when it is combined with Tesmilifene.
ThalidomideDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiotropiumDesloratadine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Desloratadine is combined with Topiramate.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Desloratadine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Desloratadine.
VerapamilThe serum concentration of Desloratadine can be increased when it is combined with Verapamil.
ZolpidemDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Wu RL, Anthes JC, Kreutner W, Harris AG, West RE Jr: Desloratadine inhibits constitutive and histamine-stimulated nuclear factor-kappaB activity consistent with inverse agonism at the histamine H1 Receptor. Int Arch Allergy Immunol. 2004 Dec;135(4):313-8. Epub 2004 Nov 24. [PubMed:15564772 ]
  2. Cieslewicz G, Gondorowicz K, Grzelewska-Rzymowska I, Rozniecki J: [Effect of loratadine, selective antagonist of histamine H1 receptors, on histamine-induced bronchoconstriction]. Pneumonol Alergol Pol. 1995;63(5-6):281-5. [PubMed:7581058 ]
  3. Letari O, Miozzo A, Folco G, Belloni PA, Sala A, Rovati GE, Nicosia S: Effects of loratadine on cytosolic Ca2+ levels and leukotriene release: novel mechanisms of action independent of the anti-histamine activity. Eur J Pharmacol. 1994 Feb 15;266(3):219-27. [PubMed:8174605 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  5. Devillier P, Roche N, Faisy C: Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30. [PubMed:18336052 ]
  6. DuBuske L: Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy. Am J Clin Dermatol. 2007;8(5):271-83. [PubMed:17902729 ]
  7. Simons FE, Prenner BM, Finn A Jr: Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. J Allergy Clin Immunol. 2003 Mar;111(3):617-22. [PubMed:12642846 ]
  8. Dhanya NB, Thasleem Z, Rai R, Srinivas CR: Comparative efficacy of levocetirizine, desloratidine and fexofenadine by histamine wheal suppression test. Indian J Dermatol Venereol Leprol. 2008 Jul-Aug;74(4):361-3. [PubMed:18797058 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein. Drug Metab Dispos. 2001 Aug;29(8):1080-3. [PubMed:11454724 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on July 01, 2016 03:05