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 419.3449
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LORATADINE HYDROCHLORIDE

SMILES

CCOC(=O)N1CCC(=C2c3ccc(cc3CCc4cccnc42)Cl)CC1.Cl

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
Molecular Formula C22H23ClN2O2
Molecular Weight 382.884
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula ClH
Molecular Weight 36.4609
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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
1062
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
2575
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8043
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

7.3457277E11
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
1601

inhibitor
1467
substrate
936

inhibitor
1604

activator
20
substrate
1118

inhibitor
1702
inhibitor
1475

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C19
1325

CYP1A2
1383

CYP2C8
818

P-gp
1330
CYP1A1
325

CYP2C19
910

CYP1A2
972

CYP2B6
616

CYP2C8
634

CYP3A5
367

P-gp
1400
CYP3A1/2
3

CYP2B1
23

CYP2B2
12

CYP1A1
98
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A1
192
 no
CYP1A2
1532
 no
CYP2C9
1648
 no
CYP3A4
1772
 no
CYP2D6
1738
 yes [IC50 0.61 uM]
CYP2C19
1392
 yes [IC50 0.76 uM]
P-gp
1514
 yes [IC50 11 uM]
CYP2C8
865
 yes [IC50 3.36 uM]
CYP2B1
38
 yes
CYP2B2
13
 yes
CYP2C9
1648
 yes
CYP3A1/2
4
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1601
 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
325
 minor
CYP1A2
972
 minor
CYP2B6
616
 minor
CYP2C19
910
 minor
CYP2C8
634
 minor
CYP2C9
936
 minor
CYP3A5
367
 minor
CYP2D6
1118
 minor
yes (co-administration study)
Comment: coadministration with cimetidine (CYP2D6 and CYP3A4 inhibitor) increased AUC of drug by 103%
Page: 1.0
P-gp
1400
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1507
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
Central nervous system effects of H1-receptor antagonists in the elderly.
1999 Feb
The acute and sub-chronic effects of levocetirizine, cetirizine, loratadine, promethazine and placebo on cognitive function, psychomotor performance, and weal and flare.
2001
[The effect of second generation histamine antagonists on the heart].
2001
Applications of new liquid chromatography-tandem mass spectrometry technologies for drug development support.
2001 Aug 10
Polarographic behaviour of loratadine and its direct determination in pharmaceutical formulation and human plasma by cathodic adsorptive stripping voltammetry.
2001 Jul
Evaluation of quality of life in children and teenagers with allergic rhinitis: adaptation and validation of the Rhinoconjunctivitis Quality of Life Questionnaire (RQLQ).
2001 Jul-Aug
Pharmacokinetic and safety profile of desloratadine and fexofenadine when coadministered with azithromycin: a randomized, placebo-controlled, parallel-group study.
2001 Mar
Synergistic antiallergic activity of combined histamine H1- and cysteinyl leukotriene1-receptor blockade in human bronchus.
2001 May 11
[Childhood asthma and viral infection: interactions and therapeutic possibilities].
2001 May-Jun
[Approaches to prevention and treatment of latex allergy].
2001 Nov-Dec
The costs of nonsedating antihistamine therapy for allergic rhinitis in managed care: an updated analysis.
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
Clinical evidence for antileukotriene therapy in the management of allergic rhinitis.
2002 Apr
Comparison of five new antihistamines (H1-receptor antagonists) in patients with allergic rhinitis using nasal provocation studies and skin tests.
2002 Apr
Are antihistamines useful in managing asthma?
2002 Feb
Medical management of Cronkhite-Canada syndrome.
2002 Feb
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
LC determination of loratadine and related impurities.
2002 Jun 20
Fixed drug eruption due to loratadine.
2002 Mar
Med-psych drug-drug interactions update.
2002 Mar-Apr
Influence of zafirlukast and loratadine on exercise-induced bronchoconstriction.
2002 May
The cost of treating allergic rhinitis.
2002 May
Ventricular tachycardia following ingestion of a commonly used antihistamine.
2002 May 6
Patents

Patents

04863931
87
JP2005509620A
46
JP2005511724A
14
JP2009526755A
410
JP4746318B2
15

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.
Substance Class Chemical
Created
by admin
on Sat Jun 26 13:55:21 UTC 2021
Edited
by admin
on Sat Jun 26 13:55:21 UTC 2021
Record UNII
RTQ46SZY8H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LORATADINE HYDROCHLORIDE
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
LORATADINE HYDROCHLORIDE [WHO-DD]
Common Name English
Code System Code Type Description
PUBCHEM
10112775
Created by admin on Sat Jun 26 13:55:21 UTC 2021 , Edited by admin on Sat Jun 26 13:55:21 UTC 2021
PRIMARY
FDA UNII
RTQ46SZY8H
Created by admin on Sat Jun 26 13:55:21 UTC 2021 , Edited by admin on Sat Jun 26 13:55:21 UTC 2021
PRIMARY
CAS
444995-23-7
Created by admin on Sat Jun 26 13:55:21 UTC 2021 , Edited by admin on Sat Jun 26 13:55:21 UTC 2021
PRIMARY
Related Record Type Details
Structure of LORATADINE
INNOVATOR->PARENT
Related Record Type Details
Structure of LORATADINE
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