U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C22H23ClN2O2.ClH
Molecular Weight 419.344
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LORATADINE HYDROCHLORIDE

SMILES

Cl.CCOC(=O)N1CCC(CC1)=C2C3=C(CCC4=C2N=CC=C4)C=C(Cl)C=C3

InChI

InChIKey=DUWMKTXPAFUTGI-UHFFFAOYSA-N
InChI=1S/C22H23ClN2O2.ClH/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;1H

HIDE SMILES / InChI

Description

Loratadine is a derivative of azatadine and 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. Loratadine competes with free histamine and exhibits specific, selective peripheral H1 antagonistic activity. 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. Loratadine has low affinity for cholinergic receptors and does not exhibit any appreciable alpha-adrenergic blocking activity in-vitro. Loratadine also appears to suppress the release of histamine and leukotrienes from animal mast cells, and the release of leukotrienes from human lung fragments, although the clinical importance of this is unknown.

CNS Activity

CNS Non-penetrant
1014
Curator's Comment: The second generation antihistamines were less soluble in lipid and thus less readily penetrated the blood-brain barrier

Approval Year

1993
136
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
CLARITIN

Approved Use

Uses temporarily relieves these symptoms due to hay fever or other upper respiratory allergies: •runny nose •itchy, watery eyes •sneezing •itching of the nose or throat

Launch Date

1993
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
4 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021165s014lbl.pdf
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DESLORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
27.1 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2958516/
40 mg 1 times / day steady-state, oral
dose: 40 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
10.8 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22806583/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
56.9 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021165s014lbl.pdf
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DESLORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
96 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2958516/
40 mg 1 times / day steady-state, oral
dose: 40 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
34.4 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22806583/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
27 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021165s014lbl.pdf
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DESLORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
14.4 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2958516/
40 mg 1 times / day steady-state, oral
dose: 40 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
11 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/22806583/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
84.5%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021165s014lbl.pdf
5 mg 1 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DESLORATADINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
unhealthy, 29
n = 103
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 29
Sex: M+F
Population Size: 103
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
Other AEs: Somnolence, Headache...
Other AEs:
Somnolence (10%)
Headache (9%)
Fatigue (5%)
Dry mouth (4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Other AEs: Fatigue, Fever...
Other AEs:
Fatigue (2%)
Fever (7%)
Headache (5%)
Influenza-like symptoms (2%)
Constipation (2%)
Diarrhea (3%)
Dyspepsia (2%)
Loose stools (2%)
Stomatitis (2%)
Tooth disorder (2%)
Vomiting (5%)
Earache (2%)
Drowsiness (7%)
Infection viral (2%)
Allergic rhinitis (2%)
Coughing (3%)
Epistaxis (3%)
Pharyngitis (3%)
Rash (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10929922/
unhealthy, 35.3
n = 331
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 35.3
Sex: M+F
Population Size: 331
Sources:
https://pubmed.ncbi.nlm.nih.gov/10929922/
Other AEs: Headache...
Other AEs:
Headache (4.2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/10929922/
AEs

AEs

AESignificanceDosePopulation
Somnolence 10%
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
unhealthy, 29
n = 103
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 29
Sex: M+F
Population Size: 103
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
Dry mouth 4%
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
unhealthy, 29
n = 103
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 29
Sex: M+F
Population Size: 103
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
Fatigue 5%
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
unhealthy, 29
n = 103
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 29
Sex: M+F
Population Size: 103
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
Headache 9%
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
unhealthy, 29
n = 103
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 29
Sex: M+F
Population Size: 103
Sources:
https://pubmed.ncbi.nlm.nih.gov/2572617/
Allergic rhinitis 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Constipation 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Dyspepsia 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Earache 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Fatigue 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Infection viral 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Influenza-like symptoms 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Loose stools 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Rash 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Stomatitis 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Tooth disorder 2%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Coughing 3%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Diarrhea 3%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Epistaxis 3%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Pharyngitis 3%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Headache 5%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Vomiting 5%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Drowsiness 7%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Fever 7%
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
unhealthy, 3.6
n = 60
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 3.6
Sex: M+F
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/20-641S007_Loratadine_medr.pdf
Headache 4.2%
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/10929922/
unhealthy, 35.3
n = 331
Health Status: unhealthy
Condition: seasonal allergic rhinitis
Age Group: 35.3
Sex: M+F
Population Size: 331
Sources:
https://pubmed.ncbi.nlm.nih.gov/10929922/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587
substrate
1037

inhibitor
1767

activator
22
substrate
1217

inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C19
1478

CYP1A2
1524

CYP2C8
911

P-gp
1461
CYP1A1
349

CYP2C19
991

CYP1A2
1054

CYP2B6
664

CYP2C8
693

CYP3A5
395

P-gp
1537
CYP3A1/2
3

CYP2B1
26

CYP2B2
15

CYP1A1
108
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A1
218
 no
CYP1A2
1692
 no
CYP2C9
1819
 no
CYP3A4
1925
 no
CYP2D6
1891
 yes [IC50 0.61 uM]
CYP2C19
1553
 yes [IC50 0.76 uM]
P-gp
1650
 yes [IC50 11 uM]
CYP2C8
965
 yes [IC50 3.36 uM]
CYP2B1
41
 yes
CYP2B2
16
 yes
CYP2C9
1819
 yes
CYP3A1/2
4
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1737
 major
yes (co-administration study)
Comment: Coadministration with either ketoconazole, erythromycin (both CYP3A4 inhibitors) increased AUC of drug by 307%, 40%, respectively; coadministration with cimetidine (CYP2D6 and CYP3A4 inhibitor) increased AUC of drug by 103%
Page: 1.0
CYP1A1
349
 minor
CYP1A2
1054
 minor
CYP2B6
664
 minor
CYP2C19
991
 minor
CYP2C8
693
 minor
CYP2C9
1037
 minor
CYP3A5
395
 minor
CYP2D6
1217
 minor
yes (co-administration study)
Comment: coadministration with cimetidine (CYP2D6 and CYP3A4 inhibitor) increased AUC of drug by 103%
Page: 1.0
P-gp
1537
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
NO15960
https://www.001chemical.com/chem/79794-75-5
3B Scientific (Wuhan) Corp
3B2-0771
http://www.3bsc.com/index/pro_info.php?id=20127
3B Scientific (Wuhan) Corp
3B1-00337
http://www.3bsc.com/index/pro_info.php?id=20549
AA Blocks
AA00ICZV
https://www.aablocks.com/goods/Goods/detail?id=AA00ICZV
AEchem Scientific Corp., USA
AE1-019802
http://www.aechemsc.com/info_products/AE1-019802.php
AHH Chemical co.,ltd
API-1744
http://www.ahhchemical.com/product/API-1744.html
AK Scientific, Inc. (AKSCI)
71291
http://www.aksci.com/item_detail.php?cat=71291
AK Scientific, Inc. (AKSCI)
HTS028367
http://www.aksci.com/item_detail.php?cat=HTS028367
AK Scientific, Inc. (AKSCI)
J10034
http://www.aksci.com/item_detail.php?cat=J10034
Aaron Chemicals
AR00IDRN
http://www.aaronchem.com/79794-75-5
AbMole Bioscience
M5752
http://www.abmole.com/products/loratadine.html
Accela ChemBio Inc
SY052751
http://www.accelachem.com/cn/search.html?keyword=SY052751&attname=GoodsCode
Achemo Scientific Limited
AC-14832
http://www.achemo.com/product_view.asp?ID=4722
Achemo Scientific Limited
AC-74979
http://www.achemo.com/search/?Keyword= 79794-75-5
Achemtek
0104-001717
http://www.achemtek.com/79794-75-5
Acorn PharmaTech
ACN-048230
http://www.acornpharmatech.com/
Adooq BioScience
A10538
https://www.adooq.com/loratadine.html
Alfa Chemistry
AP79794755
https://reagents.alfa-chemistry.com/product/loratadine-cas-79794-75-5-16699.html
Angene
AGN-PC-0UFD74
http://www.angenechemical.com/productshow/AGN-PC-0UFD74.html
ApexBio Technology
A2960
http://www.apexbt.com/loratadine-22071.html
Ark Pharm
AK-88666
http://www.arkpharminc.com/products/79794-75-5.html
AstaTech, Inc.
34558
http://www.astatechinc.com/CPSResult.php?CRNO=35766
Aurum Pharmatech LLC
M-5196
http://www.Aurumpharmatech.com/Product/ProductDetails/M_5196
AvaChem Scientific
2987
http://www.avachem.com/productSearch.asp?2987
Avantor Inc
100573-700
https://us.vwr.com/store/catalog/product.jsp?catalog_number=100573-700
Axon MedChem
1299
https://www.axonmedchem.com/product/1299
BLD Pharm
BD22650
http://www.bldpharm.com/products/79794-75-5.html
BLD Pharm
BD341540
http://www.bldpharm.com/products/79794-75-5.html
BOC Sciences
1020719-57-6
https://www.bocsci.com/loratadine-d5-cas-1020719-57-6-item-472497.html
BOC Sciences
1398065-63-8
https://www.bocsci.com/loratadine-d5-ethyl-d5-cas-1398065-63-8-item-7891.html
BioChemPartner
BCP22338
http://www.biochempartner.com/79794-75-5-BCP22338
BioCrick
BCC1262
http://www.biocrick.com/Loratadine-BCC1262.html
BioSynth
Q-100833
https://www.biosynth.com/en/products/life-science/other-biochemicals/products/Q-100833.html
CSNpharm
CSN12956
https://www.csnpharm.com/products/loratadine.html
Chem Scene
CS-0887
http://www.chemscene.com/79794-75-5.html
ChemMol
30101835
http://www.chemmol.com/chemmol/30101835.html
ChemMol
44001626
http://www.chemmol.com/chemmol/44001626.html
ChemMol
49408235
http://www.chemmol.com/chemmol/49408235.html
ChemMol
97900024
http://www.chemmol.com/chemmol/97900024.html
ChemReagents
80006240
http://www.chemreagents.com/Product/Product.asp?ProductID=80006240
Chemenu
CM110558
http://www.chemenu.com/products/CM110558
Chemspace
CSSB00000693942
https://chem-space.com/CSSB00000693942
Clearsynth
CS-O-03616
http://www.clearsynth.com/en/CSO03616.html
Clearsynth
CS-O-07780
http://www.clearsynth.com/en/CSO07780.html
Clearsynth
CS-O-01778
https://www.clearsynth.com/en/CSO01778.html
DC Chemicals
DC9104
http://www.dcchemicals.com/product_show-Loratadine.html
Enamine
Z1741979837
https://www.enaminestore.com/catalog/Z1741979837
Finetech
FT-0627976
http://www.finetechnology-ind.com/prod/detail/pub/79794-75-5.html
Glentham Life Sciences
GP7681
http://www.glentham.com/products/product/GP7681/
LGC Standards
LGCAMP0257.00-02
https://www.lgcstandards.com/US/en/p/LGCAMP0257.00-02
LGC Standards
LGCFOR0257.00
https://www.lgcstandards.com/US/en/p/LGCFOR0257.00
LGC Standards
MM0257.00-0250
https://www.lgcstandards.com/US/en/p/MM0257.00-0250
Lab Network
LN00188253
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00188253
Matrix Scientific
89794
https://www.matrixscientific.com/089794.html
MedChem Express
HY-17043
https://www.medchemexpress.com/Loratadine.html
Molcore
CS15960
https://www.molcore.com/product/79794-75-5
OChem
3802
http://www.ocheminc.com/index.php?act=psearch&pid=794L755
Oakwood
214656
http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=95655&ExtHyperLink=1
Selleck Chemicals
S1358
http://www.selleckchem.com/products/Loratadine.html
Sigma-Aldrich
BP874_SIAL
https://www.sigmaaldrich.com/catalog/product/sial/bp874?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
PHR1376_SIAL
https://www.sigmaaldrich.com/catalog/product/sial/phr1376?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
Y0000603_SIAL
https://www.sigmaaldrich.com/catalog/product/sial/y0000603?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
L9664_SIGMA
https://www.sigmaaldrich.com/catalog/product/sigma/l9664?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
1370270_USP
https://www.sigmaaldrich.com/catalog/product/usp/1370270?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule
S533555
http://www.smolecule.com/products/s533555
Synblock Inc
AB06849
http://www.synblock.com/product/79794-75-5.html
TCI (Tokyo Chemical Industry)
L0223
http://www.tcichemicals.com/eshop/en/us/commodity/L0223/index.html
THE BioTek
bt-273709
https://www.thebiotek.com/product/inhibitors/bt-273709
Tocris
1944
https://www.tocris.com/products/loratidine_1944
TripleBond
CL0028
http://www.triplebond-canada.com/prod/1411/
VladaChem
VL272222-1g
https://www.vladachem.com/product.php?products=79794-75-5
Yuhao Chemical
RT4149
http://www.chemyuhao.com/165739-83-3.html
abcr GmbH
AB261650
http://www.abcr.com/shop/en/AB261650
eNovation Chemicals
D378653
https://www.enovationchem.com/ProductDetails.asp?ProductID=D378653
eNovation Chemicals
D488439
https://www.enovationchem.com/ProductDetails.asp?ProductID=D488439
iChemical
EBD53298
http://www.ichemical.com/products/79794-75-5.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
mcule
MCULE-5073177964
https://mcule.com/MCULE-5073177964/
PubMed

PubMed

TitleDatePubMed
Stimulation of dopa decarboxylase activity in striatum of healthy human brain secondary to NMDA receptor antagonism with a low dose of amantadine.
1999 Dec 15
Central nervous system effects of H1-receptor antagonists in the elderly.
1999 Feb
Efficacy and safety of mizolastine 10 mg in a placebo-controlled comparison with loratadine in chronic idiopathic urticaria: results of the MILOR Study.
1999 Jan
Double-blind trials of azelastine nasal spray monotherapy versus combination therapy with loratadine tablets and beclomethasone nasal spray in patients with seasonal allergic rhinitis. Rhinitis Study Groups.
1999 Jun
Treatment with amantadine potentiated motor learning in a patient with traumatic brain injury of 15 years' duration.
1999 Sep
Loratadine blockade of K(+) channels in human heart: comparison with terfenadine under physiological conditions.
2000 Jan
Clinical prescribing of allergic rhinitis medication in the preschool and young school-age child: what are the options?
2001
The pharmacologic profile of desloratadine: a review.
2001
Desloratadine: a new approach in the treatment of allergy as a systematic disease--pharmacology and clinical overview. Introduction.
2001
Desloratadine in the treatment of chronic idiopathic urticaria.
2001
Desloratadine activity in concurrent seasonal allergic rhinitis and asthma.
2001
Decongestant efficacy of desloratadine in patients with seasonal allergic rhinitis.
2001
Safety of antihistamines in children.
2001
Effect of desloratadine and loratadine on rhinovirus-induced intercellular adhesion molecule 1 upregulation and promoter activation in respiratory epithelial cells.
2001 Aug
Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein.
2001 Aug
Once-daily desloratadine improves the signs and symptoms of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study.
2001 Jan
FDA panel recommends OTC status for second-generation antihistamines.
2001 Jul
[Azelastine in the treatment of allergic conjunctivitis].
2001 Jul-Aug
Pharmacology and clinical efficacy of desloratadine as an anti-allergic and anti-inflammatory drug.
2001 Mar
Loratadine and terfenadine interaction with nefazodone: Both antihistamines are associated with QTc prolongation.
2001 Mar
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
2001 Mar
Synergistic antiallergic activity of combined histamine H1- and cysteinyl leukotriene1-receptor blockade in human bronchus.
2001 May 11
[Seasonal allergic rhinitis. Nasal obstruction can also beh improved].
2001 May 3
Desloratadine reduces nasal congestion in patients with intermittent allergic rhinitis.
2001 Nov
Inhibition of depolarization-induced [3H]noradrenaline release from SH-SY5Y human neuroblastoma cells by some second-generation H(1) receptor antagonists through blockade of store-operated Ca(2+) channels (SOCs).
2001 Nov 1
Variant effect of first- and second-generation antihistamines as clues to their mechanism of action on the sneeze reflex in the common cold.
2001 Nov 1
Effect of specific immunotherapy versus loratadine on serum adhesion molecules.
2001 Oct
A double-blind, placebo-controlled, and randomized study of loratadine (Clarityne) syrup for the treatment of allergic rhinitis in children aged 3 to 12 years.
2001 Sep
Controlled clinical study of the efficacy of loratadine in Nigerian patients with allergic rhinitis.
2001 Sep
In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes.
2001 Sep
Pollen immunotherapy reduces the development of asthma in children with seasonal rhinoconjunctivitis (the PAT-study).
2002 Feb
A comparison of once daily fexofenadine versus the combination of montelukast plus loratadine on domiciliary nasal peak flow and symptoms in seasonal allergic rhinitis.
2002 Jan
Relationship between direct-to-consumer advertising and physician diagnosing and prescribing.
2002 Jan 1
Effect of desloratadine versus placebo on nasal airflow and subjective measures of nasal obstruction in subjects with grass pollen-induced allergic rhinitis in an allergen-exposure unit.
2002 Jun
Comparison of a nasal glucocorticoid, antileukotriene, and a combination of antileukotriene and antihistamine in the treatment of seasonal allergic rhinitis.
2002 Jun
Comparison of cetirizine, ebastine and loratadine in the treatment of immediate mosquito-bite allergy.
2002 Jun
LC determination of loratadine and related impurities.
2002 Jun 20
Influence of zafirlukast and loratadine on exercise-induced bronchoconstriction.
2002 May
Exercise-induced asthma: is there still a case for histamine?
2002 May
Ventricular tachycardia following ingestion of a commonly used antihistamine.
2002 May 6
Patents

Patents

04863931
26
JP2005509620A
48
JP2005511724A
14
JP2009526755A
447
JP4746318B2
18

Sample Use Guides

In Vivo Use Guide
Adults and children 6 years and over: 1 tablet daily; not more than 1 tablet in 24 hours
Route of Administration: Oral
In Vitro Use Guide
dose-dependent inhibition of histamine release was observed at loratadine dose above 7 UM. In the rat basophilic leukemia cells (RBL-2H3) experimental system, inhibition by loratadine increased when the concentration of extracellular Ca2+ was reduced from 1.8 to 0.45 mM. Loratadine also inhibited the Mn2+ influx into these cells, thus reflecting the Ca2+ influx.
Name Type Language
LORATADINE HYDROCHLORIDE
Common Name English
Loratadine hydrochloride [WHO-DD]
Common Name English
1-PIPERIDINECARBOXYLIC ACID, 4-(8-CHLORO-5,6-DIHYDRO-11H-BENZO(5,6)CYCLOHEPTA(1,2-B)PYRIDIN-11-YLIDENE)-, ETHYL ESTER, HYDROCHLORIDE (1:1)
Common Name English
Code System Code Type Description
PUBCHEM
10112775
Created by admin on Sat Dec 16 17:04:47 GMT 2023 , Edited by admin on Sat Dec 16 17:04:47 GMT 2023
PRIMARY
FDA UNII
RTQ46SZY8H
Created by admin on Sat Dec 16 17:04:47 GMT 2023 , Edited by admin on Sat Dec 16 17:04:47 GMT 2023
PRIMARY
SMS_ID
100000176868
Created by admin on Sat Dec 16 17:04:47 GMT 2023 , Edited by admin on Sat Dec 16 17:04:47 GMT 2023
PRIMARY
CAS
444995-23-7
Created by admin on Sat Dec 16 17:04:47 GMT 2023 , Edited by admin on Sat Dec 16 17:04:47 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of LORATADINE
NIH
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