Desloratadine
Identification
- Summary
Desloratadine is a second generation tricyclic antihistamine used to treat seasonal and non seasonal allergic rhinitis, pruritus, and urticaria.
- Brand Names
- Aerius, Clarinex, Clarinex-D, Neoclarityn
- Generic Name
- Desloratadine
- DrugBank Accession Number
- DB00967
- Background
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
- 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.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination for symptomatic treatment of Allergic rhinitis (ar) Combination Product in combination with: Montelukast (DB00471) •••••••••••• ••••••• •••• •••••• Used in combination for symptomatic treatment of Asthma Combination Product in combination with: Montelukast (DB00471) •••••••••••• ••••••• •••• •••••• Symptomatic treatment of Chronic idiopathic urticaria •••••••••••• Used in combination for symptomatic treatment of Common cold Combination Product in combination with: Ibuprofen (DB01050), Caffeine (DB00201), Phenylephrine (DB00388) ••• ••• ••••••• ••••••• •••••• Used in combination to treat Nasal congestion Combination Product in combination with: Phenylephrine (DB00388) ••• ••• •••••••• ••••• - Associated Therapies
- Contraindications & Blackbox Warnings
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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.
Target Actions Organism AHistamine H1 receptor antagonistHumans - 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
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- 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.
- Pathways
Pathway Category Desloratadine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Desloratadine is combined with 1,2-Benzodiazepine. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Desloratadine. Acetophenazine The risk or severity of CNS depression can be increased when Desloratadine is combined with Acetophenazine. Aclidinium The risk or severity of adverse effects can be increased when Desloratadine is combined with Aclidinium. Acrivastine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Desloratadine. - Food Interactions
- Take with or without food. The absorption is unaffected by food.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Images
- International/Other Brands
- Claramax
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aerius Tablet, film coated 5 mg Oral N.V. Organon 2021-02-08 Not applicable EU Aerius Tablet, orally disintegrating 5 mg Oral N.V. Organon 2021-02-08 Not applicable EU Aerius Solution 0.5 mg/ml Oral N.V. Organon 2021-02-08 Not applicable EU Aerius Tablet, film coated 5 mg Oral N.V. Organon 2021-02-08 Not applicable EU Aerius Tablet, orally disintegrating 5 mg Oral N.V. Organon 2021-02-08 Not applicable EU - Generic Prescription Products
- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aerius Syrup 0.5 mg / mL Oral Bayer Not applicable Not applicable Canada Aerius Tablet 5 mg Oral Bayer 2002-01-10 Not applicable Canada Aerius Kids Syrup 0.5 mg / mL Oral Bayer 2005-03-21 Not applicable Canada AERIUS TABLET 5 mg Tablet, film coated 5 mg Oral ORGANON SINGAPORE PTE. LTD. 2001-12-26 Not applicable Singapore AIRISTAR FILM-COATED TABLET 5MG Tablet, film coated 5 mg Oral PHARMAKOE PTE. LTD. 2020-05-11 Not applicable Singapore - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Aerinaze Desloratadine (2.5 mg) + Pseudoephedrine sulfate (120 mg) Tablet, multilayer, extended release Oral N.V. Organon 2021-01-27 Not applicable EU Aerinaze Desloratadine (2.5 mg) + Pseudoephedrine sulfate (120 mg) Tablet, multilayer, extended release Oral N.V. Organon 2021-01-27 Not applicable EU AERINAZE Desloratadine (2.5 MG) + Pseudoephedrine sulfate (120 mg) Tablet, extended release Oral N.V. Organon 2015-07-01 Not applicable Italy Aerinaze Desloratadine (2.5 mg) + Pseudoephedrine sulfate (120 mg) Tablet, multilayer, extended release Oral N.V. Organon 2021-01-27 Not applicable EU Aerinaze Desloratadine (2.5 mg) + Pseudoephedrine sulfate (120 mg) Tablet, multilayer, extended release Oral N.V. Organon 2021-01-27 Not applicable EU - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Clobetex Desloratadine (5 mg/1) + Clobetasol propionate (0.5 mg/1g) Kit Topical PureTek Corporation 2020-06-11 Not applicable US DICOMEX 2.5 MG/5 ML 150 ML SURUP Desloratadine (2.5 mg/5ml) Syrup Oral ATABAY KİMYA SAN. VE TİC. A.Ş. 2017-05-02 Not applicable Turkey
Categories
- ATC Codes
- R06AX27 — Desloratadine
- Drug Categories
- Anticholinergic Agents
- Antihistamines for Systemic Use
- Benzocycloheptenes
- Central Nervous System Depressants
- Cholinergic Agents
- Dibenzocycloheptenes
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H1 Antagonists, Non-Sedating
- Loratadine and derivatives
- Moderate Risk QTc-Prolonging Agents
- Neurotransmitter Agents
- P-glycoprotein inhibitors
- Piperidines
- QTc Prolonging Agents
- 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)
- Affected organisms
- Humans and other mammals
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[9.4.0.0^{3,8}]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
- 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. [Article]
- 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. [Article]
- See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6. [Article]
- 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. [Article]
- 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. [Article]
- DuBuske L: Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy. Am J Clin Dermatol. 2007;8(5):271-83. [Article]
- 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. [Article]
- 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. [Article]
- External Links
- Human Metabolome Database
- HMDB0015102
- KEGG Drug
- D03693
- PubChem Compound
- 124087
- PubChem Substance
- 46507996
- ChemSpider
- 110575
- BindingDB
- 50073179
- 275635
- ChEBI
- 291342
- ChEMBL
- CHEMBL1172
- ZINC
- ZINC000000001261
- Therapeutic Targets Database
- DAP000331
- PharmGKB
- PA164776964
- PDBe Ligand
- Y5R
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Desloratadine
- PDB Entries
- 8x64
- FDA label
- Download (200 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Diagnostic Asthma 1 4 Completed Other Allergic Reaction 2 4 Completed Other Perennial Allergic Rhinitis (PAR) / Seasonal Allergic Rhinitis 3 4 Completed Other Seasonal Allergic Rhinitis 3 4 Completed Treatment Acquired Cold Urticaria 1
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
Form Route Strength Syrup Oral 2.5 mg Film, soluble Oral 5 MG Syrup Oral 0.5 MG/ML Syrup Oral 0.5 mg / mL Tablet; tablet, extended release Oral Tablet, delayed release Oral Tablet Oral Tablet, multilayer, extended release Oral Tablet, orally disintegrating Oral 2.5 mg Tablet, orally disintegrating Oral 5 mg Syrup Oral 0.5 mg/ ml Solution Oral 0.5 mg/ml Granule Syrup Oral 2.5 mg/5ml Tablet, film coated Oral 5.00 mg Solution Oral 50.000 mg Tablet Oral 5.000 mg Tablet, effervescent Oral Solution Oral 0.050 g Capsule, coated Oral Solution Oral 0.5 mg/1mL Tablet, film coated Oral 5 mg/1 Tablet, orally disintegrating Oral 5 mg/1 Tablet, orally disintegrating Oral 2.5 mg/1 Tablet, extended release Oral Tablet, film coated, extended release Oral Kit Topical Granule Oral Syrup Oral 50.00 mg Syrup Oral 0.5 mg/mg Capsule Nasal Tablet, effervescent Syrup Oral 0.5 mg Tablet, film coated Oral Syrup Oral Tablet Oral 5.00 mg Syrup Oral Tablet, coated Oral Syrup Oral 150 ml Syrup Oral 5000000 mg Solution Oral 0.05 g Solution Oral 50 mg Tablet Oral 500000 mg Tablet, delayed release Oral 5 mg Solution Oral Syrup Oral 50 mg Tablet, orally disintegrating Oral Tablet Oral 5 mg/1 Tablet, film coated Oral Tablet, chewable Oral Syrup Oral 2.500 mg/5ml Tablet, film coated Oral 5 mg Capsule Oral 5 mg Tablet, coated Oral 500000 mg Suspension Oral Capsule, liquid filled Oral Tablet Oral 5.0 mg Syrup Oral 50.000 mg Solution Oral 25 mg Capsule Oral 5.000 mg Solution Oral 0.050 mg Syrup Oral 0.050 g Capsule Oral Solution Oral Syrup Oral 0.05 g Tablet, film coated Oral 500000 mg Tablet Oral 5 mg Syrup Oral 0.5 mg/1ml Tablet, coated Oral 5 mg - Prices
Unit description Cost Unit Clarinex Reditabs 30 5 mg Dispersible Tablet Box 150.0USD box Clarinex Reditabs 30 2.5 mg Dispersible Tablet Box 147.14USD box Clarinex-D 24 Hour 5-240 mg 24 Hour tablet 5.0USD tablet Clarinex-d 24 hour tablet 4.8USD tablet Clarinex 5 mg tablet 4.57USD tablet Clarinex-D 12 Hour 2.5-120 mg 12 Hour tablet 3.2USD tablet Clarinex-d 12 hour tablet 3.08USD tablet Clarinex 0.5 mg/ml Syrup 0.48USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5178878 No 1993-01-12 2010-01-12 US CA2294352 No 2008-05-06 2018-07-01 Canada CA2267136 No 2000-11-28 2018-02-06 Canada US7405223 Yes 2008-07-29 2020-01-07 US US6100274 Yes 2000-08-08 2020-01-07 US US6514520 Yes 2003-02-04 2018-12-01 US US7618649 Yes 2009-11-17 2021-06-19 US US6709676 No 2004-03-23 2021-02-18 US US8187630 No 2012-05-29 2020-12-19 US US6979463 No 2005-12-27 2022-03-28 US US7820199 Yes 2010-10-26 2022-09-28 US US5607697 Yes 1997-03-04 2015-12-07 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 3.2 Not Available - Predicted Properties
Property Value Source Water Solubility 0.00395 mg/mL ALOGPS logP 3.48 ALOGPS logP 3.97 Chemaxon logS -4.9 ALOGPS pKa (Strongest Basic) 9.73 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 24.92 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 101.04 m3·mol-1 Chemaxon Polarizability 34.35 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.965 Caco-2 permeable - 0.5121 P-glycoprotein substrate Substrate 0.7758 P-glycoprotein inhibitor I Inhibitor 0.6694 P-glycoprotein inhibitor II Non-inhibitor 0.794 Renal organic cation transporter Inhibitor 0.6979 CYP450 2C9 substrate Non-substrate 0.8554 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.5634 CYP450 1A2 substrate Inhibitor 0.7786 CYP450 2C9 inhibitor Non-inhibitor 0.738 CYP450 2D6 inhibitor Non-inhibitor 0.7377 CYP450 2C19 inhibitor Non-inhibitor 0.7837 CYP450 3A4 inhibitor Non-inhibitor 0.8332 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6083 Ames test Non AMES toxic 0.6514 Carcinogenicity Non-carcinogens 0.9367 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.0370 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7382 hERG inhibition (predictor II) Inhibitor 0.8016
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 174.4086093 predictedDarkChem Lite v0.1.0 [M-H]- 170.64888 predictedDeepCCS 1.0 (2019) [M-H]- 174.4086093 predictedDarkChem Lite v0.1.0 [M-H]- 170.64888 predictedDeepCCS 1.0 (2019) [M+H]+ 175.7465093 predictedDarkChem Lite v0.1.0 [M+H]+ 173.00688 predictedDeepCCS 1.0 (2019) [M+H]+ 175.7465093 predictedDarkChem Lite v0.1.0 [M+H]+ 173.00688 predictedDeepCCS 1.0 (2019) [M+Na]+ 175.0881093 predictedDarkChem Lite v0.1.0 [M+Na]+ 179.10002 predictedDeepCCS 1.0 (2019) [M+Na]+ 175.0881093 predictedDarkChem Lite v0.1.0 [M+Na]+ 179.10002 predictedDeepCCS 1.0 (2019)
Targets
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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. [Article]
- DuBuske L: Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy. Am J Clin Dermatol. 2007;8(5):271-83. [Article]
- 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. [Article]
- 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. [Article]
Transporters
- 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
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54