Identification

Name
Desloratadine
Accession Number
DB00967  (APRD00324)
Type
Small Molecule
Groups
Approved, 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
External IDs
SCH 34117 / SCH-34117
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ClarinexTablet, orally disintegrating5 mg/1OralSchering Corporation2007-08-042007-08-04Us
ClarinexSolution0.5 mg/1mLOralMerck Sharp & Dohme Limited2004-09-01Not applicableUs
ClarinexTablet, film coated5 mg/1OralRebel Distributors2002-02-08Not applicableUs
ClarinexTablet, film coated5 mg/1OralMerck Sharp & Dohme Limited2001-12-21Not applicableUs00085 1264 01 nlmimage10 cc07e63f
ClarinexTablet, film coated5 mg/1OralPhysicians Total Care, Inc.2002-06-03Not applicableUs54868 462420180907 15195 1javdl3
ClarinexTablet, orally disintegrating5 mg/1OralSchering Corporation2006-03-032006-03-03Us
ClarinexTablet, film coated5 mg/1OralA-S Medication Solutions2001-12-212017-08-31Us50090 076520180913 8702 ho94k9
Clarinex ReditabsTablet, orally disintegrating2.5 mg/1OralSchering Corporation2008-02-192008-02-19Us
NeoclaritynSolution0.5 mg/mlOralMerck Sharp & Dohme B.V.2001-01-15Not applicableEu
NeoclaritynTablet, orally disintegrating2.5 mgOralMerck Sharp & Dohme B.V.2001-01-15Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEu
DesloratadineTablet5 mg/1OralAv Kare, Inc.2012-07-052018-01-16Us76439 0107 10 nlmimage10 083f0448
DesloratadineTablet, film coated5 mg/1OralPaddock Laboratories, Inc.2014-01-102015-10-31Us
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AeriusSyrup0.5 mgOralBayerNot applicableNot applicableCanada
AeriusTablet5 mgOralBayer2002-01-10Not applicableCanada
Aerius KidsSyrup0.5 mgOralBayer2005-03-21Not applicableCanada
Allergy Control DesloratadineTablet5 mgOralPharmascience IncNot applicableNot applicableCanada
Allernix Multi SymptomTablet5 mgOralTeva2012-01-31Not applicableCanada
Desloratadine Allergy ControlTablet5 mgOralDominion Pharmacal2014-03-10Not applicableCanada
Desloratadine Allergy ControlTablet5 mgOralPharmascience Inc2009-12-24Not applicableCanada
Desloratadine TabletsTablet5 mgOralApotex Corporation2010-05-27Not applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Aerius Dual Action 12 HourDesloratadine (2.5 mg) + Pseudoephedrine sulfate (120 mg)Tablet, extended releaseOralBayer2010-02-01Not applicableCanada
Aerius Dual Action 24 HourDesloratadine (5 mg) + Pseudoephedrine sulfate (240 mg)Tablet, multilayer, extended releaseOralBayerNot applicableNot applicableCanada
Clarinex-D 12 HourDesloratadine (2.5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralMerck Sharp & Dohme Limited2006-02-01Not applicableUs00085 1322 01 nlmimage10 cf07e78f
Clarinex-D 12 HourDesloratadine (2.5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralPhysicians Total Care, Inc.2006-11-29Not applicableUs54868 570820180907 15195 tb11qk
Clarinex-D 24 HourDesloratadine (5 mg/1) + Pseudoephedrine sulfate (240 mg/1)Tablet, film coated, extended releaseOralPhysicians Total Care, Inc.2006-07-112012-06-30Us
Clarinex-D 24 HourDesloratadine (5 mg/1) + Pseudoephedrine sulfate (240 mg/1)Tablet, film coated, extended releaseOralMerck Sharp & Dohme Limited2005-03-032014-04-30Us0085 131720180913 8702 1mlazbd
International/Other Brands
Claramax / NeoClarityn
Categories
UNII
FVF865388R
CAS number
100643-71-8
Weight
Average: 310.821
Monoisotopic: 310.123676325
Chemical Formula
C19H19ClN2
InChI Key
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

Pharmacology

Indication

For 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.

Associated Conditions
Pharmacodynamics

Desloratadine 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 action

Like 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.

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

82-87%

Metabolism
Not Available
Route of elimination

Desloratadine (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 life

50 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Desloratadine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Desloratadine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Desloratadine.
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Desloratadine.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Desloratadine.
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative and stimulatory activities of Desloratadine.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Desloratadine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Desloratadine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Desloratadine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Desloratadine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when Desloratadine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Food Interactions
  • Take without regard to meals.

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
Human Metabolome Database
HMDB0015102
KEGG Drug
D03693
PubChem Compound
124087
PubChem Substance
46507996
ChemSpider
110575
BindingDB
50073179
ChEBI
291342
ChEMBL
CHEMBL1172
Therapeutic Targets Database
DAP000331
PharmGKB
PA164776964
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Desloratadine
ATC Codes
R06AX27 — Desloratadine
AHFS Codes
  • 04:08.00 — Second Generation Antihistamines
FDA label
Download (200 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentFasting1
1CompletedTreatmentFed1
1CompletedTreatmentHealthy Volunteers4
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentPost-nasal Drip / Rhinorrhea / Seasonal Allergic Rhinitis (SAR)1
2, 3CompletedTreatmentAllergies1
3CompletedNot AvailableAllergic Rhinitis (AR)2
3CompletedTreatmentAllergic Rhinitis (AR)2
3CompletedTreatmentAllergic Rhinoconjunctivitis1
3CompletedTreatmentAsthma Bronchial / Rhinitis, Allergic, Seasonal1
3CompletedTreatmentAtopic Dermatitis (AD)1
3CompletedTreatmentAtopics / Chronic Idiopathic Urticaria1
3CompletedTreatmentChronic Urticaria1
3CompletedTreatmentDermal Pruritus / Dermatitis, Eczematous / Skin Inflammation1
3CompletedTreatmentPerennial Allergic Rhinitis (PAR)1
3CompletedTreatmentSeasonal Allergic Rhinitis (SAR)3
3CompletedTreatmentUrticarias2
3Not Yet RecruitingTreatmentCold1
3TerminatedTreatmentCutaneous Hypersensitivity1
3Unknown StatusTreatmentAllergic Rhinitis (AR)1
4CompletedNot AvailableAllergies2
4CompletedNot AvailablePerennial Allergic Rhinitis (PAR) / Seasonal Allergic Rhinitis (SAR)3
4CompletedNot AvailableSeasonal Allergic Rhinitis (SAR)2
4CompletedDiagnosticAsthma Bronchial1
4CompletedOtherSeasonal Allergic Rhinitis (SAR)1
4CompletedTreatmentAcquired Cold Urticaria1
4CompletedTreatmentAllergic Airway Disease1
4CompletedTreatmentAllergic Rhinitis (AR)1
4CompletedTreatmentChronic Idiopathic Urticaria1
4CompletedTreatmentChronic Idiopathic Urticaria / Urticarias1
4CompletedTreatmentConjunctivitis, Seasonal Allergic1
4CompletedTreatmentHypersensitivity1
4CompletedTreatmentRhinitis, Allergic, Seasonal1
4CompletedTreatmentSeasonal Allergic Rhinitis (SAR)3
4CompletedTreatmentUrticarias4
4TerminatedTreatmentUrticarias1
Not AvailableCompletedNot AvailableRhinitis1
Not AvailableCompletedNot AvailableRhinitis / Urticarias2
Not AvailableCompletedTreatmentAsthma Bronchial1
Not AvailableSuspendedTreatmentAsthma Bronchial / Rhinitis1

Pharmacoeconomics

Manufacturers
  • Schering corp
  • Doctor reddys laboratories ltd
  • Schering plough corp
  • Orchid healthcare
Packagers
  • Apotheca Inc.
  • A-S Medication Solutions LLC
  • Cima Laboratories Inc.
  • Lake Erie Medical and Surgical Supply
  • Schering Corp.
  • Schering-Plough Inc.
  • Southwood Pharmaceuticals
Dosage forms
FormRouteStrength
SyrupOral0.5 mg
Tablet, extended releaseOral
Tablet, multilayer, extended releaseOral
TabletOral5 mg
Tablet, film coatedOral5 mg/1
Tablet, film coated, extended releaseOral
Tablet, film coatedOral5 mg
SolutionOral0.5 mg/1mL
TabletOral5 mg/1
Tablet, orally disintegratingOral2.5 mg/1
Tablet, orally disintegratingOral5 mg/1
SolutionOral0.5 mg/ml
Tablet, orally disintegratingOral2.5 mg
Tablet, orally disintegratingOral5 mg
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)
US5178878No1993-01-122010-01-12Us
CA2294352No2008-05-062018-07-01Canada
CA2267136No2000-11-282018-02-06Canada
US7405223Yes2000-01-072020-01-07Us
US6100274Yes2000-01-072020-01-07Us
US6514520Yes1998-12-012018-12-01Us
US7618649Yes2001-06-192021-06-19Us
US6709676No2001-02-182021-02-18Us
US8187630No2000-12-192020-12-19Us
US6979463No2002-03-282022-03-28Us
US7820199Yes2002-09-282022-09-28Us
US5607697Yes1995-12-072015-12-07Us

Properties

State
Solid
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 RuleNoChemAxon
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)

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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0940000000-d20368a648c20c37e1a0
MS/MS Spectrum - , positiveLC-MS/MSsplash10-08fr-0095000000-2816aba50d0b94d568cf
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0940000000-9a0f5f4d81f4c42c85bb
MS/MS Spectrum - , positiveLC-MS/MSsplash10-08fr-0095000000-5b3f7555b72461661fa1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0bt9-0094000000-536b5a1d05f7479c2b04

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzocycloheptapyridines
Sub Class
Not Available
Direct Parent
Benzocycloheptapyridines
Alternative Parents
Pyridines and derivatives / Piperidines / Benzenoids / Aryl chlorides / Heteroaromatic compounds / Dialkylamines / Azacyclic compounds / Organopnictogen compounds / Organochlorides / Hydrocarbon derivatives
Substituents
Benzocycloheptapyridine / Aryl chloride / Aryl halide / Piperidine / Pyridine / Benzenoid / Heteroaromatic compound / Secondary amine / Secondary aliphatic amine / Azacycle
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
benzocycloheptapyridine (CHEBI:291342)

Targets

Details
1. Histamine H1 receptor
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 catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
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
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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]
  2. Nicolas JM, Whomsley R, Collart P, Roba J: In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem Biol Interact. 1999 Nov 15;123(1):63-79. [PubMed:10597902]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Evidence is supported by in vitro studies.
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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]
  2. Barecki ME, Casciano CN, Johnson WW, Clement RP: In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes. Drug Metab Dispos. 2001 Sep;29(9):1173-5. [PubMed:11502723]
  3. Kazmi F, Yerino P, Barbara JE, Parkinson A: Further Characterization of the Metabolism of Desloratadine and Its Cytochrome P450 and UDP-glucuronosyltransferase Inhibition Potential: Identification of Desloratadine as a Relatively Selective UGT2B10 Inhibitor. Drug Metab Dispos. 2015 Sep;43(9):1294-302. doi: 10.1124/dmd.115.065011. Epub 2015 Jul 1. [PubMed:26135009]
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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]
  2. Barecki ME, Casciano CN, Johnson WW, Clement RP: In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes. Drug Metab Dispos. 2001 Sep;29(9):1173-5. [PubMed:11502723]
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
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]

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
Uniprot Name
Multidrug resistance protein 1
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]

Drug created on June 13, 2005 07:24 / Updated on October 15, 2018 04:36