loratadine Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
histamine-H1 receptor antagonists, tricyclic compounds 1605 79794-75-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • loratadine
  • claritin
  • loracert
  • loradex
  • loratidine
  • loratyne
A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.
  • Molecular weight: 382.89
  • Formula: C22H23ClN2O2
  • CLOGP: 5.05
  • LIPINSKI: 1
  • HAC: 4
  • HDO: 0
  • TPSA: 42.43
  • ALOGS: -4.46
  • ROTB: 2

Drug dosage:

DoseUnitRoute
10 mg O

Approvals:

DateAgencyCompanyOrphan
April 12, 1993 FDA BAYER HEALTHCARE LLC

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Extra dose administered 419.47 30.69 76 1839 1283 3382661
Accidental exposure to product by child 371.46 30.69 69 1846 1342 3382602
Somnolence 244.16 30.69 94 1821 32110 3351834
Drug hypersensitivity 241.81 30.69 96 1819 35584 3348360
Urticaria 200.32 30.69 79 1836 28648 3355296
Drug ineffective 191.30 30.69 119 1796 115971 3267973
Product use issue 181.54 30.69 63 1852 15938 3368006
Toxicity to various agents 162.82 30.69 79 1836 46975 3336969
Completed suicide 147.33 30.69 65 1850 31049 3352895
Cardiac arrest 132.27 30.69 58 1857 27261 3356683
Overdose 126.27 30.69 60 1855 33918 3350026
Palpitations 117.19 30.69 48 1867 19035 3364909
Intentional overdose 116.87 30.69 45 1870 15180 3368764
Dizziness 116.73 30.69 75 1840 76437 3307507
Suicide attempt 111.59 30.69 44 1871 15803 3368141
Angioedema 110.01 30.69 43 1872 15092 3368852
Coma 92.37 30.69 36 1879 12516 3371428
Dyspnoea 87.97 30.69 71 1844 102863 3281081
Torsade de pointes 85.45 30.69 24 1891 3005 3380939
Electrocardiogram QT prolonged 83.10 30.69 32 1883 10763 3373181
Seizure 80.28 30.69 47 1868 40353 3343591
Epilepsy 77.22 30.69 27 1888 6918 3377026
Generalised tonic-clonic seizure 73.35 30.69 27 1888 8015 3375929
Failure of child resistant mechanism for pharmaceutical product 72.86 30.69 10 1905 20 3383924
Bezoar 69.54 30.69 13 1902 258 3383686
Abortion spontaneous 69.08 30.69 28 1887 10757 3373187
Drug interaction 68.93 30.69 45 1870 46767 3337177
Respiratory arrest 67.65 30.69 28 1887 11340 3372604
Hypersensitivity 67.64 30.69 37 1878 27863 3356081
Pneumonia aspiration 61.70 30.69 23 1892 7065 3376879
Pruritus 61.65 30.69 42 1873 46791 3337153
Gastrooesophageal reflux disease 60.25 30.69 26 1889 11665 3372279
Alanine aminotransferase increased 56.30 30.69 31 1884 23609 3360335
Headache 55.25 30.69 52 1863 91928 3292016
Condition aggravated 53.55 30.69 36 1879 39197 3344747
Metabolic acidosis 53.49 30.69 22 1893 8756 3375188
Asthma 52.40 30.69 24 1891 12378 3371566
Exposure during pregnancy 51.87 30.69 31 1884 27532 3356412
Obstructive airways disorder 50.77 30.69 14 1901 1635 3382309
Arrhythmia 49.91 30.69 22 1893 10375 3373569
Pain 49.86 30.69 44 1871 71513 3312431
Confusional state 49.78 30.69 34 1881 37964 3345980
Aspartate aminotransferase increased 48.38 30.69 27 1888 21086 3362858
Swelling face 47.93 30.69 22 1893 11394 3372550
Incorrect dose administered 46.75 30.69 23 1892 13891 3370053
Syncope 46.07 30.69 28 1887 25605 3358339
Hepatic function abnormal 45.15 30.69 21 1894 11206 3372738
Dysarthria 44.99 30.69 20 1895 9614 3374330
Blood pressure increased 44.42 30.69 26 1889 22204 3361740
Nausea 43.71 30.69 54 1861 129591 3254353
Poisoning 42.33 30.69 16 1899 5096 3378848
Expired product administered 40.51 30.69 12 1903 1807 3382137
Fatigue 39.91 30.69 47 1868 107193 3276751
Vomiting 39.71 30.69 43 1872 89488 3294456
Blood lactic acid increased 39.57 30.69 11 1904 1322 3382622
Malaise 39.33 30.69 37 1878 65140 3318804
Cough 39.23 30.69 30 1885 39828 3344116
Cardio-respiratory arrest 38.81 30.69 21 1894 15419 3368525
Eczema 38.13 30.69 14 1901 4112 3379832
Walking disability 37.58 30.69 8 1907 312 3383632
Heart rate increased 37.24 30.69 20 1895 14466 3369478
Pyrexia 36.03 30.69 39 1876 81076 3302868
Insomnia 35.28 30.69 27 1888 35871 3348073
Multiple drug therapy 35.23 30.69 6 1909 68 3383876
Hypersensitivity vasculitis 34.91 30.69 11 1904 2036 3381908
Intercepted medication error 34.82 30.69 9 1906 820 3383124
Feeling abnormal 34.52 30.69 24 1891 27501 3356443
Stress cardiomyopathy 34.25 30.69 10 1905 1432 3382512
Death 33.99 30.69 52 1863 152272 3231672
Ventricular fibrillation 33.85 30.69 13 1902 4320 3379624
Erythema multiforme 33.66 30.69 12 1903 3241 3380703
Heart rate irregular 33.41 30.69 12 1903 3312 3380632
Urinary retention 33.05 30.69 15 1900 7557 3376387
Aggression 32.90 30.69 17 1898 11368 3372576
Hypokalaemia 32.54 30.69 18 1897 13787 3370157
Abdominal pain upper 31.89 30.69 22 1893 24894 3359050
Tunnel vision 31.74 30.69 7 1908 323 3383621
Loss of consciousness 31.74 30.69 23 1892 28124 3355820
Cholestasis 31.22 30.69 13 1902 5324 3378620
Shock 31.10 30.69 14 1901 6923 3377021

Pharmacologic Action:

SourceCodeDescription
ATC R06AX13 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D000982 Antipruritics
MeSH PA D003879 Dermatologic Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D039563 Histamine H1 Antagonists, Non-Sedating
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Vasomotor rhinitis indication 8229003 DOID:4730
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Sneezing indication 76067001
Common cold indication 82272006 DOID:10459
Chronic idiopathic urticaria indication 302162004
Seasonal allergic rhinitis indication 367498001
Allergic conjunctivitis indication 473460002 DOID:11204
Urticaria off-label use 126485001
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Hepatic failure contraindication 59927004
Diabetes mellitus contraindication 73211009 DOID:9351
Kidney disease contraindication 90708001 DOID:2527
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Benign prostatic hyperplasia contraindication 266569009 DOID:2883
Retention of urine contraindication 267064002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Hypertensive urgency contraindication 443482000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.43 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 6.97 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 6.81 DRUG MATRIX
Cytochrome P450 2C19 Enzyme IC50 7.80 DRUG MATRIX
Multidrug resistance protein 1 Transporter Ki 4.94 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.77 WOMBAT-PK
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor EC50 5.52 CHEMBL
Bile acid receptor Nuclear hormone receptor IC50 5.51 CHEMBL
Sodium-dependent neutral amino acid transporter B(0)AT2 Transporter IC50 5.40 CHEMBL
Histamine H1 receptor GPCR Ki 6.46 CHEMBL
Histamine H1 receptor GPCR Kd 7.14 CHEMBL

External reference:

IDSource
DB00455 DRUGBANK_ID
4020716 VUID
N0000148306 NUI
C0065180 UMLSCUI
7216 IUPHAR_LIGAND_ID
D00364 KEGG_DRUG
7AJO3BO7QN UNII
5864 INN_ID
CHEMBL998 ChEMBL_ID
4020716 VANDF
N0000006315 NDFRT
N0000148306 NDFRT
003909 NDDF
45829 MMSL
28889 RXNORM
108652002 SNOMEDCT_US
386884002 SNOMEDCT_US
4994 MMSL
d03050 MMSL
015760 NDDF
3957 PUBCHEM_CID
D017336 MESH_DESCRIPTOR_UI
CHEBI:6538 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
allergy relief HUMAN OTC DRUG LABEL 1 0067-6066 TABLET 10 mg ORAL NDA 16 sections
allergy relief HUMAN OTC DRUG LABEL 1 0067-6122 TABLET 10 mg ORAL NDA 16 sections
good sense allergy relief HUMAN OTC DRUG LABEL 1 0113-0612 TABLET 10 mg ORAL ANDA 9 sections
good sense allergy and congestion relief HUMAN OTC DRUG LABEL 2 0113-1165 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 9 sections
Allergy and Congestion Relief HUMAN OTC DRUG LABEL 2 0113-2013 TABLET, EXTENDED RELEASE 5 mg ORAL ANDA 9 sections
Basic Care allergy relief HUMAN OTC DRUG LABEL 1 0113-7612 TABLET 10 mg ORAL ANDA 9 sections
Loratadine HUMAN OTC DRUG LABEL 1 0179-8317 TABLET 10 mg ORAL ANDA 9 sections
wal itin d HUMAN OTC DRUG LABEL 2 0363-0299 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 9 sections
Loratadine HUMAN OTC DRUG LABEL 1 0363-0522 TABLET 10 mg ORAL ANDA 9 sections
Loratadine HUMAN OTC DRUG LABEL 1 0363-0527 TABLET, ORALLY DISINTEGRATING 10 mg ORAL ANDA 9 sections
Wal itin D HUMAN OTC DRUG LABEL 2 0363-0617 TABLET, EXTENDED RELEASE 5 mg ORAL ANDA 9 sections
Wal itin HUMAN OTC DRUG LABEL 1 0363-0699 TABLET 10 mg ORAL ANDA 9 sections
Loratadine and Pseudoephedrine HUMAN OTC DRUG LABEL 2 0363-0725 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 9 sections
WAL-ITIN HUMAN OTC DRUG LABEL 1 0363-1686 CAPSULE, LIQUID FILLED 10 mg ORAL ANDA 8 sections
Wal-itin Allergy Relief HUMAN OTC DRUG LABEL 1 0363-2085 SOLUTION 5 mg ORAL ANDA 9 sections
Childrens Wal-itin HUMAN OTC DRUG LABEL 1 0363-2092 SOLUTION 5 mg ORAL ANDA 10 sections
Childrens Walitin HUMAN OTC DRUG LABEL 1 0363-2108 SOLUTION 5 mg ORAL ANDA 10 sections
Childrens Loratadine HUMAN OTC DRUG LABEL 1 0363-2131 SOLUTION 5 mg ORAL ANDA 10 sections
Wal-itin D HUMAN OTC DRUG LABEL 2 0363-2390 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
Loratadine HUMAN OTC DRUG LABEL 1 0378-8880 TABLET 10 mg ORAL ANDA 15 sections
LORATADINE HUMAN OTC DRUG LABEL 1 0536-1092 TABLET 10 mg ORAL ANDA 9 sections
ALAVERT ALLERGY HUMAN OTC DRUG LABEL 1 0573-2620 TABLET, ORALLY DISINTEGRATING 10 mg ORAL NDA 9 sections
ALAVERT ALLERGY HUMAN OTC DRUG LABEL 1 0573-2621 TABLET, ORALLY DISINTEGRATING 10 mg ORAL NDA 9 sections
ALAVERT ALLERGY SINUS D-12 HUMAN OTC DRUG LABEL 2 0573-2660 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 8 sections
Loratadine HUMAN OTC DRUG LABEL 1 0615-5586 TABLET 10 mg ORAL ANDA 9 sections
Loratadine HUMAN OTC DRUG LABEL 1 0781-5077 TABLET 10 mg ORAL ANDA 9 sections
allergy HUMAN OTC DRUG LABEL 1 0904-5728 TABLET 10 mg ORAL ANDA 9 sections
LORATADINE HUMAN OTC DRUG LABEL 1 0904-5793 TABLET 10 mg ORAL ANDA 9 sections
Loratadine ODT HUMAN OTC DRUG LABEL 1 0904-5806 TABLET, ORALLY DISINTEGRATING 10 mg ORAL ANDA 9 sections
Loratadine and Pseudoephedrine Sulfate HUMAN OTC DRUG LABEL 2 0904-5833 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 9 sections