Identification

Name
Desloratadine
Accession Number
DB00967
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.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 310.821
Monoisotopic: 310.123676325
Chemical Formula
C19H19ClN2
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
  • Desloratadina
  • Desloratadine
External IDs
  • SCH 34117
  • SCH-34117

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
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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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
Humans
Absorption

Desloratadine administered orally for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean Tmax of approximately 3 hours, a mean steady-state Cmax of 4 ng/ml, and a mean steady-state AUC of 56.9 ng*hr/ml. A similar profile was observed using 10 ml of an oral solution containing 5 mg of desloratadine. Food was found not to affect desloratadine absorption.

Volume of distribution
Not Available
Protein binding

Desloratadine is bound approximately 82 to 87% to plasma proteins, while its active metabolite, 3-hydroxydesloratadine, is bound approximately 85 to 89%.

Metabolism

Desloratadine is metabolized to the active metabolite 3-hydroxydesloratadine, which is subsequently glucuronidated.

Route of elimination

Approximately 87% of a 14C-desloratadine dose was equally recovered in urine and feces as metabolic products.

Half-life

Desloratadine has a mean plasma elimination half-life of approximately 27 hours.

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Information regarding desloratadine overdose is limited, although somnolence has been reported. In case of overdose, symptomatic and supportive treatment, including removing the unabsorbed drug, is recommended; note, however, that desloratadine and its active metabolite 3-hydroxydesloratadine cannot be eliminated by hemodialysis.

In animal studies, lethality was observed at or above doses of 250 mg/kg in rats and of 353 mg/kg in mice (oral LD50), doses that represent 120 and 290 times the human exposure based on the recommended daily oral dose. In monkey, no deaths occurred at doses up to 250 mg/kg, representing an exposure roughly 810 times that of the recommended dose in humans.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Desloratadine H1-Antihistamine ActionDrug action
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.
DrugInteraction
AcebutololThe risk or severity of QTc prolongation can be increased when Desloratadine is combined with Acebutolol.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Desloratadine.
AcetophenazineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Acetophenazine.
AclidiniumAclidinium may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Desloratadine.
AdenosineThe risk or severity of QTc prolongation can be increased when Adenosine is combined with Desloratadine.
AgomelatineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Agomelatine.
AjmalineThe risk or severity of QTc prolongation can be increased when Ajmaline is combined with Desloratadine.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Desloratadine.
AlfuzosinThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Desloratadine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with or without food. The absorption is unaffected by food.

Products

Product Images
International/Other Brands
Claramax
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ClarinexTablet, orally disintegrating5 mg/1OralSchering Corporation2007-08-042007-08-04US flag
ClarinexSolution0.5 mg/1mLOralMerck Sharp & Dohme Corp.2004-09-01Not applicableUS flag
ClarinexTablet, film coated5 mg/1OralPhysicians Total Care, Inc.2002-06-03Not applicableUS flag54868 462420180907 15195 1javdl3
ClarinexTablet, orally disintegrating5 mg/1OralSchering Corporation2006-03-032006-03-03US flag
ClarinexTablet, film coated5 mg/1OralMerck Sharp & Dohme Corp.2001-12-21Not applicableUS flag00085 1264 01 nlmimage10 cc07e63f
ClarinexTablet, film coated5 mg/1OralA-S Medication Solutions2001-12-212017-10-26US flag50090 076520180913 8702 ho94k9
ClarinexTablet, film coated5 mg/1OralRebel Distributors2002-02-08Not applicableUS flag
Clarinex ReditabsTablet, orally disintegrating2.5 mg/1OralSchering Corporation2008-02-192008-02-19US flag
DesloratadineTablet, orally disintegrating2.5 mg/1OralAnesta Corporation2015-05-01Not applicableUS flag
DesloratadineTablet, orally disintegrating5 mg/1OralAnesta Corporation2015-05-01Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DasseltaTablet, film coated5 mgOralKrka, D.D., Novo Mesto2011-11-28Not applicableEU flag
DesloratadineTablet, film coated5 mg/1OralA-S Medication Solutions2013-02-25Not applicableUS flag
DesloratadineSolution0.5 mg/1mLOralTaro Pharmaceuticals U.S.A., Inc.2015-07-012015-07-01US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AeriusSyrupOralBayerNot applicableNot applicableCanada flag
AeriusTabletOralBayer2002-01-10Not applicableCanada flag
Aerius KidsSyrupOralBayer2005-03-21Not applicableCanada flag
Allergy Control DesloratadineTabletOralPharmascience IncNot applicableNot applicableCanada flag
Allernix Multi SymptomTabletOralTEVA Canada Limited2012-01-312020-05-11Canada flag
Desloratadine Allergy ControlTabletOralDominion Pharmacal2014-03-102020-05-06Canada flag
Desloratadine Allergy ControlTabletOralPharmascience Inc2009-12-24Not applicableCanada flag
Desloratadine TabletsTabletOralApotex Corporation2010-05-27Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Aerius Double Action 12 HourDesloratadine (2.5 mg) + Pseudoephedrine sulfate (120 mg)Tablet, extended releaseOralBayer2010-02-01Not applicableCanada flag
Aerius Dual Action 24 HourDesloratadine (5 mg) + Pseudoephedrine sulfate (240 mg)Tablet, multilayer, extended releaseOralBayerNot applicableNot applicableCanada flag
Clarinex-D 12 HourDesloratadine (2.5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralPhysicians Total Care, Inc.2006-11-29Not applicableUS flag54868 570820180907 15195 tb11qk
Clarinex-D 12 HourDesloratadine (2.5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralMerck Sharp & Dohme Corp.2006-02-01Not applicableUS flag00085 1322 01 nlmimage10 cf07e78f
Clarinex-D 24 HourDesloratadine (5 mg/1) + Pseudoephedrine sulfate (240 mg/1)Tablet, film coated, extended releaseOralMerck Sharp & Dohme Corp.2005-03-032014-04-30US flag0085 131720180913 8702 1mlazbd
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 flag
ClobetexDesloratadine (5 mg/1) + Clobetasol propionate (0.5 mg/1g)KitTopicalPureTek Corporation2020-06-11Not applicableUS flag

Categories

ATC Codes
R06AX27 — Desloratadine
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Amine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Benzocycloheptapyridine / Heteroaromatic compound / Hydrocarbon derivative / Organic nitrogen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
benzocycloheptapyridine (CHEBI:291342)

Chemical Identifiers

UNII
FVF865388R
CAS number
100643-71-8
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

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]
Human Metabolome Database
HMDB0015102
KEGG Drug
D03693
PubChem Compound
124087
PubChem Substance
46507996
ChemSpider
110575
BindingDB
50073179
RxNav
275635
ChEBI
291342
ChEMBL
CHEMBL1172
ZINC
ZINC000000001261
Therapeutic Targets Database
DAP000331
PharmGKB
PA164776964
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Desloratadine
AHFS Codes
  • 04:08.00 — Second Generation Antihistamines
FDA label
Download (200 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableAllergies2
4CompletedNot AvailablePerennial Allergic Rhinitis (PAR) / Seasonal Allergic Rhinitis (SAR)3
4CompletedNot AvailableSeasonal Allergic Rhinitis (SAR)2
4CompletedDiagnosticAsthma1
4CompletedOtherSeasonal Allergic Rhinitis (SAR)1
4CompletedTreatmentAcquired Cold Urticaria1
4CompletedTreatmentAllergic Airway Disease1
4CompletedTreatmentAllergic Rhinitis (AR)1
4CompletedTreatmentChronic Idiopathic Urticaria2
4CompletedTreatmentChronic Idiopathic Urticaria / Urticaria1

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
Film, solubleOral5 MG
Syrup500 mcg/1mL
SyrupOral0.5 MG/ML
Syrup0.5 mg/ml
Tablet, orally disintegratingOral
Tablet, film coated5 mg
Tablet, extended releaseOral2.5 mg
TabletOral2.5 mg
Tablet, multilayer, extended releaseOral
Tablet
Granule2.5 mg
TabletOral
Syrup2.5 mg/5ml
Tablet, effervescentOral2.5 mg
SolutionOral0.5 mg/1mL
Tablet, film coatedOral5 mg/1
Tablet, orally disintegratingOral5 mg/1
Tablet, orally disintegratingOral2.5 mg/1
Tablet, extended releaseOral
Tablet, film coated, extended releaseOral
KitTopical
Tablet, coatedOral30 mg
GranuleOral20 mg
TabletOral500 mg
Capsule, coatedOral250 mg
Tablet, film coatedOral5 mg
Syrup0.5 mg/mg
Tablet, effervescentOral120 mg
Tablet, effervescent60 mg
Capsule2.5 mg
Tablet, effervescent2.5 mg
Tablet, effervescent5 mg
SyrupOral
SolutionOral25 mg
Capsule, coatedOral2.5 mg
SyrupOral25 mg
SyrupOral50 mg
Syrup150 ml
SolutionOral0.05 g
SolutionOral50 mg
Tablet, coatedOral5 mg
Tablet, orally disintegrating2.5 MG
Tablet, orally disintegrating5 MG
Tablet, coated5 MG
TabletOral5 mg/1
Tablet, film coatedOral
Tablet, chewableOral2.5 mg
SyrupOral2.5 mg/5ml
SolutionOral
SuspensionOral0.025 g
SolutionOral0.5 mg/ml
Tablet, orally disintegratingOral2.5 mg
Tablet, orally disintegratingOral5 mg
SyrupOral0.025 g
SyrupOral0.05 g
Syrup
Tablet, coatedOral2.5 mg
TabletOral5 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)Region
US5178878No1993-01-122010-01-12US flag
CA2294352No2008-05-062018-07-01Canada flag
CA2267136No2000-11-282018-02-06Canada flag
US7405223Yes2008-07-292020-01-07US flag
US6100274Yes2000-08-082020-01-07US flag
US6514520Yes2003-02-042018-12-01US flag
US7618649Yes2009-11-172021-06-19US flag
US6709676No2004-03-232021-02-18US flag
US8187630No2012-05-292020-12-19US flag
US6979463No2005-12-272022-03-28US flag
US7820199Yes2010-10-262022-09-28US flag
US5607697Yes1997-03-042015-12-07US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

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

Targets

Details
1. Histamine H1 receptor
Kind
Protein
Organism
Humans
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]

Transporters

Details
1. P-glycoprotein 1
Kind
Protein
Organism
Humans
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 27, 2020 11:12

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