Details of the Drug

General Information of Drug (ID: DMF3AN7)

Drug Name
Loratadine
Synonyms
Aerotina; Alarin; Alavert; Alerpriv; Allertidin; Anhissen; Biloina; Bonalerg; Civeran; Claratyne; Clarinase; Claritin; Claritine; Clarityn; Clarityne; Clarium; Fristamin; Histaloran; Lergy; Lertamine; Lesidas; Lisino; Loracert; Loradex; Loradif; Loranox; Lorantis; Lorastine; Loratadina; Loratadinum; Loratidine; Loratyne; Loraver; Lorfast; Loritine; Lowadina; Nularef; Optimin; Polaratyne; Pylor; Restamine; Rhinase; Rinomex; Roletra; Sanelor; Sensibit; Sohotin; Tadine; Velodan; Versal; Zeos; Bedix Loratadina; Claratyne Cold; Claratyne Decongestant; Clarinase Reperabs; Claritin D; Claritin Hives Relief; Claritin Hives Relief Reditab; Claritin Reditabs; Claritin reditab; Clarityne Dy Repetabs; Loratadina [Spanish]; Loratadine Redidose; Loratadine Wyeth Brand; Loratadinum [Latin]; Sinhistan Dy; Talorat Dy; Wyeth Brand of Loratadine; L 9664; Sch 29851; Sch29851; Alavert (TN); AllergyX (TN); Children's Claritin; Claritin (TN); Claritine (TN); Clarityn (TN); Clarityne (TN); Clarityne-D; Flonidan (TN); Fristamin (TN); Lomilan (TN); Lorfast (TN); Rinolan (TN); Roletra (TN); Sch-29851; Symphoral (TN); Tidilor (TN); Alavert, Claritin, Loratadine; Loratadine [USAN:BAN:INN]; Loratadine (JAN/USAN/INN); Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidine-1-carboxylate; Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylate; 1-Piperidenecarboxylic acid, 4-(8-chloro-5,6-duhydro-11H-benzo [5,6]cyclohepta[1,2-b]-pyridin-11-ylidene)-, ethyl ester; 1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-, ethyl ester; 1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester; 1-piperidinecarboxylic acid,4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-,ethyl ester; 4-(8-Chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylic Acid Ethyl Ester; 4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene-1-piperidinecarboxylic acidethyl ester; 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cycloheptal[1,2-b]pyridin-11-ylidene-1-piperidinecarboxylic acid ethyl ester
Indication
Disease Entry ICD 11 Status REF
Allergy 4A80-4A85 Approved [1], [2]
Allergic rhinitis CA08.0 Discontinued in Phase 2 [3]
Therapeutic Class
Antihistamines
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 382.9
Topological Polar Surface Area (xlogp) 5.2
Rotatable Bond Count (rotbonds) 2
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 6.14 mcgh/L [4]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 2.56 mcg/L [4]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1.14 h [4]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [5]
Clearance
The clearance of drug is 12 L/h/kg [6]
Elimination
40% of loratadine is excreted in the urine, and 42% is eliminated in the faeces [7]
Half-life
The concentration or amount of drug in body reduced by one-half in 10 hours [4]
Metabolism
The drug is metabolized via the liver [8]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.43615 micromolar/kg/day [9]
Vd
The volume of distribution (Vd) of drug is 120 L/kg [10]
Water Solubility
The ability of drug to dissolve in water is measured as 0.005 mg/mL [5]
Chemical Identifiers
Formula
C22H23ClN2O2
IUPAC Name
ethyl 4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidine-1-carboxylate
Canonical SMILES
CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1
InChI
InChI=1S/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5-6,9-10,12-13H2,1H3
InChIKey
JCCNYMKQOSZNPW-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3957
ChEBI ID
CHEBI:6538
CAS Number
79794-75-5
DrugBank ID
DB00455
TTD ID
D06ABF
VARIDT ID
DR00541
INTEDE ID
DR0977
ACDINA ID
D00374

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [11], [12], [13]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [14]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [15]
Cytochrome P450 2D6 (CYP2D6)
Main DME 		DECB0K3 CP2D6_HUMAN Substrate [16]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [17]
Mephenytoin 4-hydroxylase (CYP2C19)
Main DME 		DEGTFWK CP2CJ_HUMAN Substrate [18]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [19]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [19]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Substrate [19]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [20]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Allergy
ICD Disease Classification 4A80-4A85
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histamine H1 receptor (H1R) DTT HRH1 6.74E-01 0.13 0.43
P-glycoprotein 1 (ABCB1) DTP P-GP 6.54E-01 1.95E-01 4.04E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 5.57E-01 -7.89E-02 -7.93E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 4.32E-01 4.39E-02 4.30E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 8.46E-01 -6.63E-03 -4.49E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.57E-01 9.43E-03 1.29E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 9.62E-01 2.57E-02 1.10E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.70E-01 2.98E-02 1.22E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 2.35E-01 2.78E-02 2.09E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.76E-01 1.26E-01 8.27E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Loratadine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Arn-509 DMT81LZ Moderate Increased metabolism of Loratadine caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [98]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Loratadine caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [99]
Voriconazole DMAOL2S Moderate Decreased metabolism of Loratadine caused by Voriconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [100]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Loratadine caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [101]
Clarithromycin DM4M1SG Minor Decreased metabolism of Loratadine caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [102]
Troleandomycin DMUZNIG Minor Decreased metabolism of Loratadine caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [102]
Tucatinib DMBESUA Moderate Decreased metabolism of Loratadine caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [103]
Mifepristone DMGZQEF Moderate Decreased metabolism of Loratadine caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [100]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Loratadine caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [104]
MK-8228 DMOB58Q Moderate Decreased metabolism of Loratadine caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [105]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Loratadine caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [106]
Oxcarbazepine DM5PU6O Moderate Increased metabolism of Loratadine caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [107]
Rufinamide DMWE60C Moderate Increased metabolism of Loratadine caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [98]
Itraconazole DMCR1MV Minor Decreased metabolism of Loratadine caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [108]
Terbinafine DMI6HUW Moderate Decreased metabolism of Loratadine caused by Terbinafine mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [109]
Miconazole DMPMYE8 Minor Decreased metabolism of Loratadine caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [108]
Ketoconazole DMPZI3Q Minor Decreased metabolism of Loratadine caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [108]
Boceprevir DMBSHMF Moderate Decreased metabolism of Loratadine caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [110]
Telaprevir DMMRV29 Moderate Decreased metabolism of Loratadine caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [111]
Rifapentine DMCHV4I Moderate Increased metabolism of Loratadine caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [112]
Efavirenz DMC0GSJ Moderate Increased metabolism of Loratadine caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [113]
Etravirine DMGV8QU Moderate Increased metabolism of Loratadine caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [114]
Darunavir DMN3GCH Moderate Decreased metabolism of Loratadine caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [115]
Conivaptan DM1V329 Moderate Decreased metabolism of Loratadine caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [116]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Loratadine caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [98]
Brigatinib DM7W94S Moderate Increased metabolism of Loratadine caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [117]
PF-06463922 DMKM7EW Moderate Increased metabolism of Loratadine caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [118]
Selpercatinib DMZR15V Moderate Decreased metabolism of Loratadine caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [98]
Lumefantrine DM29GAD Moderate Decreased metabolism of Loratadine caused by Lumefantrine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [100]
Idelalisib DM602WT Moderate Decreased metabolism of Loratadine caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [119]
IPI-145 DMWA24P Moderate Decreased metabolism of Loratadine caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [120]
Exjade DMHPRWG Moderate Decreased metabolism of Loratadine caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [121]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Loratadine caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [98]
Imatinib DM7RJXL Moderate Decreased metabolism of Loratadine caused by Imatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [122]
Dasatinib DMJV2EK Moderate Decreased metabolism of Loratadine caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [123]
Modafinil DMYILBE Minor Increased metabolism of Loratadine caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [124]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Loratadine caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [125]
Abametapir DM2RX0I Moderate Decreased metabolism of Loratadine caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [126]
Lefamulin DME6G97 Moderate Decreased metabolism of Loratadine caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [127]
Enzalutamide DMGL19D Moderate Increased metabolism of Loratadine caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [128]
Bosentan DMIOGBU Moderate Increased metabolism of Loratadine caused by Bosentan mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [129]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Loratadine and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [130]
Celecoxib DM6LOQU Moderate Decreased metabolism of Loratadine caused by Celecoxib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [131]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Loratadine caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [98]
Larotrectinib DM26CQR Moderate Decreased metabolism of Loratadine caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [100]
Armodafinil DMGB035 Minor Increased metabolism of Loratadine caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [124]
LEE011 DMMX75K Moderate Decreased metabolism of Loratadine caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [132]
Pitolisant DM8RFNJ Moderate Increased metabolism of Loratadine caused by Pitolisant mediated induction of CYP450 enzyme. Somnolence [MG42] [98]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Loratadine and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [130]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Loratadine and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [130]
Amiodarone DMUTEX3 Moderate Increased plasma concentrations of Loratadine and Amiodarone due to competitive inhibition of the same metabolic pathway. Ventricular tachyarrhythmia [BC71] [133]
⏷ Show the Full List of 51 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Aspartame E00402 134601 Flavoring agent
Caprylic acid E00017 379 Emulsifying agent; Flavoring agent; Surfactant
D&C red no. 27 E00381 83511 Colorant
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Kyselina citronova E00014 311 Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sodium stearate E00453 2724691 Emulsifying agent; Gelling agent; Glidant; Modified-release agent; Stiffening agent; lubricant
Sodium stearyl fumarate E00545 23665634 lubricant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Ascorbic acid E00579 54670067 Acidulant; Antioxidant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Butylhydroxyanisole E00308 24667 Antimicrobial preservative; Antioxidant
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Dextrin E00359 62698 Binding agent; Diluent; Microencapsulating agent; Stiffening agent; Suspending agent; Viscosity-controlling agent
Eisenoxyd E00585 56841934 Colorant
Glycerin E00026 753 Antimicrobial preservative; Emollient; Flavoring agent; Humectant; Lubricant; Plasticizing agent; Solvent; Suppository base; Tonicity agent; Viscosity-controlling agent
Hexahydric alcohol E00083 5780 Diluent; Flavoring agent; Humectant; Plasticizing agent
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium bicarbonate E00424 516892 Alkalizing agent; Diluent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Water E00035 962 Solvent
⏷ Show the Full List of 29 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Loratadine 10 mg tablet 10 mg Disintegrating Tablet Oral
Loratadine 5 mg tablet 5 mg Chewable Tablet Oral
Loratadine 10 mg tablet 10 mg 24 HR Oral Tablet Oral
Loratadine 10 mg capsule 10 mg Oral Capsule Oral
Loratadine 10 mg tablet 10 mg Disintegrating Oral Tablet Oral
Loratadine 5 mg tablet 5 mg Disintegrating Oral Tablet Oral
Loratadine 10 mg tablet 10 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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