Identification

Name
Loratadine
Accession Number
DB00455  (APRD00384)
Type
Small Molecule
Groups
Approved
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. [PubChem]

Structure
Thumb
Synonyms
  • Loratadina
  • Loratadinum
External IDs
SCH-29851
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ClaritinTablet10 mg/1OralNavajo Manuracturing Company2016-09-17Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AllergyTablet10 mg/1OralSelder, S.A. de C.V.2014-12-16Not applicableUs
Allergy ReliefTablet10 mg/1OralMarc Glassman, Inc.2014-12-16Not applicableUs
Childrens Loratadine Sugar FreeSolution5 mg/5mLOralKroger2017-03-17Not applicableUs
Childrens Loratadine Sugar FreeSolution5 mg/5mLOralAmerisource Bergen2017-03-17Not applicableUs
Childrens Loratadine Sugar FreeSolution5 mg/5mLOralValue Merchandisers2017-03-17Not applicableUs
Childrens Loratadine Sugar FreeSolution5 mg/5mLOralWalgreen2017-03-17Not applicableUs
Childrens Loratadine Sugar FreeSolution5 mg/5mLOralRite Aid2017-03-17Not applicableUs
Childrens Loratadine Sugar FreeSolution5 mg/5mLOralPharmacy Vlaue Alliance Llc2017-03-17Not applicableUs
Childrens WalitinSolution5 mg/5mLOralWalgreen2016-12-12Not applicableUs
LoratadineTablet10 mg/1OralSt. Marys Medical Park Pharmacy2016-06-03Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
24 Hour Allergy ReliefTablet10 mg/1OralMeijer Distribution2014-12-30Not applicableUs
24 Hour Allergy RemedyTablet10 mgOralVita Health Products Inc2006-07-28Not applicableCanada
7 Select Allergy ReliefTablet10 mg/1Oral7 Eleven2014-05-14Not applicableUs
Alavert AllergyTablet, orally disintegrating10 mg/1OralWyeth Consumer Healthcare Llc2002-12-19Not applicableUs
Alavert AllergyTablet, orally disintegrating10 mg/1OralWyeth Consumer Healthcare Llc2002-12-19Not applicableUs
Allegy Relief 24 hour non drowsyTablet10 mg/1OralHannaford Brothers Company2006-09-072017-12-22Us
AllergyTablet10 mg/1OralRemedy Repack2017-10-11Not applicableUs
AllergyTablet10 mg/1OralMajor2005-02-21Not applicableUs
Allergy ReliefTablet10 mg/1OralInternational Laboratories, Llc2016-05-27Not applicableUs
Allergy ReliefTablet10 mg/1OralMeijer Distribution2017-07-12Not applicableUs
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Help I have allergiesTablet10 mg/1OralHelp Remedies, Inc.2009-07-01Not applicableUs
LoratadineTablet10 mg/1OralRebel Distributors2010-01-21Not applicableUs51660 0526 05 nlmimage10 bf16dfa6
LoratadineTablet10 mg/1OralCardinal Health2013-06-14Not applicableUs
LoratadineTablet10 mg/1OralApotex Corporation2017-11-21Not applicableUs
International/Other Brands
Aerotina / Alavert / Biloina / Civeran / Claritin / Fristamin / Histaloran / Lomilan / Loracert / Loradex / Loranox / Lorastine / Loratyne / Loritine / Nularef / Restamine / Roletra / Sensibit
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Alavert Allergy Sinus D-12Loratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, film coated, extended releaseOralWyeth Ltd.2004-01-30Not applicableUs00573 2660 24 nlmimage10 8d46c6b6
Allerclear-D 24 HourLoratadine (10 mg/1) + Pseudoephedrine sulfate (240 mg/1)Tablet, extended releaseOralCostco Wholesale2016-03-01Not applicableUs
Allergy and Congestion ReliefLoratadine (10 mg/1) + Pseudoephedrine sulfate (240 mg/1)Tablet, film coatedOralHannaford Brothers Company2009-06-032017-12-22Us
Allergy and Congestion ReliefLoratadine (10 mg/1) + Pseudoephedrine sulfate (240 mg/1)Tablet, extended releaseOralHyvee2003-06-30Not applicableUs
Allergy and congestion reliefLoratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralKroger2012-04-06Not applicableUs
Allergy and Congestion ReliefLoratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralL. Perrigo Company2012-01-23Not applicableUs
Allergy and Congestion ReliefLoratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralHyvee2012-03-192017-12-22Us
Allergy and Congestion ReliefLoratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralSafeway2012-10-182017-12-22Us
Allergy and Congestion ReliefLoratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)Tablet, extended releaseOralRite Aid2013-07-25Not applicableUs
Allergy and Congestion Relief Non DrowsyLoratadine (10 mg/1) + Pseudoephedrine sulfate (240 mg/1)Tablet, film coatedOralAmerisource Bergen2010-11-132017-12-22Us
Categories
UNII
7AJO3BO7QN
CAS number
79794-75-5
Weight
Average: 382.883
Monoisotopic: 382.144805697
Chemical Formula
C22H23ClN2O2
InChI Key
JCCNYMKQOSZNPW-UHFFFAOYSA-N
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
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
SMILES
CCOC(=O)N1CCC(CC1)=C1C2=C(CCC3=C1N=CC=C3)C=C(Cl)C=C2

Pharmacology

Indication

A self-medication that is used alone or in combination with pseudoephedrine sulfate for the symptomatic relief of seasonal allergic rhinitis. Also used for the symptomatic relief of pruritus, erythema, and urticaria associated with chronic idiopathic urticaria in patients (not for children under 6 unless directed by a clincian).

Structured Indications
Pharmacodynamics

Loratadine is a long acting second generation antihistamine that is similar in structure to cyproheptadine and azatadine. The pharmacology of loratadine is similar to other antihistamines, but unlike other H1-blockers, loratidine is shown to exhibit competitive, specific, and selective antagonism of H1 receptors. The exact mechanism of this interaction is unknown, but disposition of the drug suggests that loratadine's prolonged antagonism of histamine may be due to the drug's slow dissociation from the receptor or the formation of the active metabolite, desloratadine. Loratadine does not penetrate the CNS effectively and has a low affinity for CNS H1-receptors.

Mechanism of action

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.

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Human
UPotassium voltage-gated channel subfamily H member 2Not AvailableHuman
Absorption

Rapidly absorbed following oral administration (40% bioavailability)

Volume of distribution
Not Available
Protein binding

97-99%

Metabolism

Hepatic

Route of elimination
Not Available
Half life

8.4 hours

Clearance
Not Available
Toxicity

somnolence, tachycardia, and headache LD50=mg/kg (orally in rat)

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Loratadine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Loratadine.Experimental, Illicit
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Loratadine.Experimental
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Loratadine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Loratadine.Experimental, Illicit
AbirateroneThe serum concentration of Loratadine can be increased when it is combined with Abiraterone.Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Loratadine.Approved
AmiodaroneThe serum concentration of Loratadine can be increased when it is combined with Amiodarone.Approved, Investigational
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Loratadine.Approved, Investigational
AmphetamineAmphetamine may decrease the sedative activities of Loratadine.Approved, Illicit
AprepitantThe serum concentration of Loratadine can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Loratadine.Approved, Investigational
ArtemetherThe metabolism of Loratadine can be decreased when combined with Artemether.Approved
AtazanavirThe metabolism of Loratadine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Loratadine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Loratadine is combined with Atorvastatin.Approved
BenzphetamineBenzphetamine may decrease the sedative activities of Loratadine.Approved, Illicit
Benzylpenicilloyl PolylysineLoratadine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Loratadine.Approved
BetaxololThe metabolism of Loratadine can be decreased when combined with Betaxolol.Approved
BoceprevirThe metabolism of Loratadine can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Loratadine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Loratadine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Loratadine.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Loratadine.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Loratadine.Approved, Investigational
BupropionThe metabolism of Loratadine can be decreased when combined with Bupropion.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Loratadine.Approved
CapecitabineThe metabolism of Loratadine can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Loratadine can be increased when combined with Carbamazepine.Approved, Investigational
CelecoxibThe metabolism of Loratadine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Loratadine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Loratadine.Withdrawn
ChloroquineThe metabolism of Loratadine can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Loratadine.Illicit, Withdrawn
ChlorpromazineThe metabolism of Loratadine can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Loratadine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Loratadine.Approved
CimetidineThe metabolism of Loratadine can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Loratadine can be decreased when combined with Cinacalcet.Approved
CitalopramThe metabolism of Loratadine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Loratadine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Loratadine can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Loratadine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Loratadine can be decreased when combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Loratadine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Loratadine can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Loratadine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Loratadine can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Loratadine.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Loratadine.Approved, Investigational
CrisaboroleThe metabolism of Loratadine can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Loratadine can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Loratadine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Loratadine.Approved
DabrafenibThe serum concentration of Loratadine can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe metabolism of Loratadine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Loratadine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Loratadine can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Loratadine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Loratadine can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Loratadine can be decreased when combined with Desipramine.Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Loratadine.Approved, Illicit
DiethylpropionDiethylpropion may decrease the sedative activities of Loratadine.Approved, Illicit
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Loratadine.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Loratadine.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Loratadine.Experimental
DihydroergotamineThe metabolism of Loratadine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Loratadine can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Loratadine can be decreased when combined with Diphenhydramine.Approved
DosulepinThe metabolism of Loratadine can be decreased when combined with Dosulepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Loratadine.Approved, Investigational
DoxycyclineThe metabolism of Loratadine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Loratadine can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Loratadine can be decreased when combined with Duloxetine.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Loratadine.Approved
EfavirenzThe metabolism of Loratadine can be decreased when combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Loratadine can be decreased when combined with Eliglustat.Approved
EnzalutamideThe serum concentration of Loratadine can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Loratadine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Loratadine.Approved
ErythromycinThe metabolism of Loratadine can be decreased when combined with Erythromycin.Approved, Vet Approved
EtravirineThe metabolism of Loratadine can be decreased when combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Loratadine.Approved
FelodipineThe metabolism of Loratadine can be decreased when combined with Felodipine.Approved, Investigational
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Loratadine.Approved
FloxuridineThe metabolism of Loratadine can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Loratadine can be decreased when combined with Fluconazole.Approved
FluorouracilThe metabolism of Loratadine can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Loratadine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvastatinThe metabolism of Loratadine can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Loratadine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Loratadine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Loratadine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Loratadine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Loratadine can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe metabolism of Loratadine can be decreased when combined with Gemfibrozil.Approved
GepefrineGepefrine may decrease the sedative activities of Loratadine.Experimental
HaloperidolThe metabolism of Loratadine can be decreased when combined with Haloperidol.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Loratadine.Approved, Investigational
HydroxyamphetamineHydroxyamphetamine may decrease the sedative activities of Loratadine.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Loratadine.Approved
IdelalisibThe metabolism of Loratadine can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Loratadine can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Loratadine can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Loratadine can be decreased when combined with Indinavir.Approved
Iofetamine I-123Iofetamine I-123 may decrease the sedative activities of Loratadine.Approved
IrbesartanThe metabolism of Loratadine can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Loratadine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Loratadine can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Loratadine can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Loratadine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Loratadine can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Loratadine can be decreased when combined with Ketoconazole.Approved, Investigational
LapatinibThe metabolism of Loratadine can be decreased when combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Loratadine.Approved
LeflunomideThe metabolism of Loratadine can be decreased when combined with Leflunomide.Approved, Investigational
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Loratadine.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Loratadine.Approved, Investigational
LobeglitazoneThe metabolism of Loratadine can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Loratadine can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Loratadine can be decreased when combined with Lorcaserin.Approved
LorpiprazoleThe serum concentration of Loratadine can be increased when it is combined with Lorpiprazole.Approved
LosartanThe metabolism of Loratadine can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Loratadine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Loratadine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Loratadine can be increased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Loratadine can be decreased when combined with Lumefantrine.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Loratadine.Illicit, Investigational, Withdrawn
ManidipineThe metabolism of Loratadine can be decreased when combined with Manidipine.Approved, Investigational
MephedroneMephedrone may decrease the sedative activities of Loratadine.Investigational
MephentermineMephentermine may decrease the sedative activities of Loratadine.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Loratadine.Experimental
MethadoneThe metabolism of Loratadine can be decreased when combined with Methadone.Approved
MethamphetamineMethamphetamine may decrease the sedative activities of Loratadine.Approved, Illicit
MethotrimeprazineThe metabolism of Loratadine can be decreased when combined with Methotrimeprazine.Approved
MethoxyphenamineMethoxyphenamine may decrease the sedative activities of Loratadine.Experimental
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Loratadine.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Loratadine.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Loratadine.Approved, Investigational
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Loratadine.Experimental
MidomafetamineMidomafetamine may decrease the sedative activities of Loratadine.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Loratadine can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Loratadine can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Loratadine can be decreased when combined with Mirabegron.Approved
MitotaneThe serum concentration of Loratadine can be decreased when it is combined with Mitotane.Approved
MMDAMMDA may decrease the sedative activities of Loratadine.Experimental, Illicit
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Loratadine.Approved
NefazodoneThe metabolism of Loratadine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Loratadine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Loratadine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Loratadine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Loratadine can be decreased when combined with Nicardipine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Loratadine.Approved, Investigational
NilotinibThe metabolism of Loratadine can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Loratadine.Approved
OlaparibThe metabolism of Loratadine can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Loratadine can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Loratadine can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Loratadine can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Loratadine can be increased when it is combined with Panobinostat.Approved, Investigational
ParoxetineThe metabolism of Loratadine can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Loratadine.Approved
Peginterferon alfa-2bThe serum concentration of Loratadine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Loratadine can be increased when combined with Pentobarbital.Approved, Vet Approved
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Loratadine.Approved, Investigational, Vet Approved, Withdrawn
PhenobarbitalThe metabolism of Loratadine can be increased when combined with Phenobarbital.Approved
PhenterminePhentermine may decrease the sedative activities of Loratadine.Approved, Illicit
PhenytoinThe metabolism of Loratadine can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Loratadine can be decreased when combined with Pioglitazone.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Loratadine.Approved
PosaconazoleThe metabolism of Loratadine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Loratadine.Approved
PrimidoneThe metabolism of Loratadine can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe metabolism of Loratadine can be decreased when combined with Promazine.Approved, Vet Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Loratadine.Approved
PseudoephedrinePseudoephedrine may decrease the sedative activities of Loratadine.Approved
PyrimethamineThe metabolism of Loratadine can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinidineThe metabolism of Loratadine can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Loratadine can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Loratadine can be decreased when combined with Rabeprazole.Approved, Investigational
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Loratadine.Approved, Investigational
RifabutinThe metabolism of Loratadine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Loratadine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Loratadine can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Loratadine.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Loratadine.Approved
RitobegronRitobegron may decrease the sedative activities of Loratadine.Investigational
RitonavirThe metabolism of Loratadine can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Loratadine can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Loratadine can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneThe metabolism of Loratadine can be decreased when combined with Rosiglitazone.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Loratadine.Approved
RucaparibThe metabolism of Loratadine can be decreased when combined with Rucaparib.Approved, Investigational
SaquinavirThe metabolism of Loratadine can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Loratadine can be decreased when used in combination with Sarilumab.Approved
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Loratadine.Approved
SecobarbitalThe metabolism of Loratadine can be increased when combined with Secobarbital.Approved, Vet Approved
SertralineThe metabolism of Loratadine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Loratadine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Loratadine.Approved
SiltuximabThe serum concentration of Loratadine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Loratadine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Loratadine.Approved
SorafenibThe metabolism of Loratadine can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Loratadine can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Loratadine can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Loratadine can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Loratadine can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Loratadine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamoxifenThe metabolism of Loratadine can be decreased when combined with Tamoxifen.Approved
TelaprevirThe metabolism of Loratadine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Loratadine can be decreased when combined with Telithromycin.Approved
TerbinafineThe metabolism of Loratadine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Loratadine.Experimental
TeriflunomideThe metabolism of Loratadine can be decreased when combined with Teriflunomide.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Loratadine.Approved, Withdrawn
TicagrelorThe metabolism of Loratadine can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Loratadine can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Loratadine can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Loratadine can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Loratadine can be decreased when combined with Tolbutamide.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Loratadine.Approved
TopiroxostatThe metabolism of Loratadine can be decreased when combined with Topiroxostat.Approved, Investigational
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Loratadine.Approved, Investigational
TranylcypromineThe metabolism of Loratadine can be decreased when combined with Tranylcypromine.Approved
TrimethoprimThe metabolism of Loratadine can be decreased when combined with Trimethoprim.Approved, Vet Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Loratadine.Approved, Investigational, Nutraceutical
Valproic AcidThe metabolism of Loratadine can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Loratadine can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Loratadine can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Loratadine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Loratadine can be decreased when combined with Verapamil.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Loratadine.Approved, Investigational
VoriconazoleThe metabolism of Loratadine can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe metabolism of Loratadine can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Loratadine can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take on empty stomach: 1 hour before or 2 hours after meals.

References

Synthesis Reference

Alberto Stampa, Pelayo Camps, Gloria Rodriguez, Jordi Bosch, Maria del Carmen Onrubia, "Process for the preparation of loratadine." U.S. Patent US6084100, issued July 04, 2000.

US6084100
General References
  1. See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6. [PubMed:14655812]
  2. Menardo JL, Horak F, Danzig MR, Czarlewski W: A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4. [PubMed:9444440]
  3. Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41. [PubMed:1977506]
  4. Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27. [PubMed:11291777]
External Links
Human Metabolome Database
HMDB0005000
KEGG Drug
D00364
PubChem Compound
3957
PubChem Substance
46507853
ChemSpider
3820
BindingDB
22876
ChEBI
6538
ChEMBL
CHEMBL998
Therapeutic Targets Database
DAP000101
PharmGKB
PA450266
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Loratadine
ATC Codes
R06AX13 — Loratadine
AHFS Codes
  • 04:08.00 — Second Generation Antihistamines
FDA label
Download (232 KB)
MSDS
Download (51.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentProgressive Multiple Sclerosis1
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentHistamine H1 Antagonists, Non-Sedating1
1Not Yet RecruitingOtherHealthy Volunteers1
1TerminatedTreatmentRheumatoid Arthritis1
2CompletedTreatmentAllergic Rhinitis (AR)1
2CompletedTreatmentBone Pain in Stage I - III Breast Cancer1
2CompletedTreatmentChronic Urticaria1
2CompletedTreatmentRhinitis / Seasonal Rhinitis1
2RecruitingTreatmentAllergic Rhinitis (AR)1
2RecruitingTreatmentRhinitis, Allergic, Perennial1
2RecruitingTreatmentTransplant, Kidney1
2Unknown StatusSupportive CarePegfilgrastim-induced Back and Leg Pain1
3CompletedTreatmentAllergies / Conjunctivitis / Rhinitis / Rhinoconjunctivitis2
3CompletedTreatmentModerate or Severe Submental Fullness1
3CompletedTreatmentPerennial Allergic Rhinitis (PAR)1
3CompletedTreatmentRhinitis, Allergic, Seasonal1
3CompletedTreatmentSeasonal Allergic Rhinitis (SAR)6
3RecruitingTreatmentRhinitis, Allergic, Seasonal1
4CompletedNot AvailableHealthy Volunteers1
4CompletedTreatmentAllergic Rhinitis (AR)1
4CompletedTreatmentAllergic Rhinitis (AR) / Pollen Allergy / Rhinitis, Allergic, Seasonal / Severe Acute Respiratory Syndrome1
4CompletedTreatmentPerennial Allergic Rhinitis (PAR)1
4CompletedTreatmentRhinitis2
4CompletedTreatmentRhinitis, Allergic, Perennial1
4CompletedTreatmentSeasonal Allergic Rhinitis (SAR)1
Not AvailableCompletedNot AvailablePruritus / Rhinitis, Allergic, Perennial / Rhinitis, Allergic, Seasonal / Urticarias1
Not AvailableNot Yet RecruitingTreatmentRhinitis, Allergic, Perennial1
Not AvailableRecruitingNot AvailableLeukemias / Malignant Lymphomas1
Not AvailableRecruitingTreatmentMalignant Lymphomas1

Pharmacoeconomics

Manufacturers
  • Schering plough healthcare products inc
  • Taro pharmaceuticals usa inc
  • Apotex inc richmond hill
  • L perrigo co
  • Ranbaxy laboratories ltd
  • Silarx pharmaceuticals inc
  • Taro pharmaceutical industries ltd
  • Teva pharmaceuticals usa inc
  • Wockhardt eu operations (swiss) ag
  • Wyeth consumer healthcare
  • Impax laboratories inc
  • Watson laboratories inc florida
  • Apotex inc etobicoke site
  • Mylan pharmaceuticals inc
  • Perrigo co
  • Sandoz inc
Packagers
Dosage forms
FormRouteStrength
TabletOral10 mg
TabletOral10 mg/1
LiquidOral5 mg/5mL
SolutionOral5 mg/5mL
Tablet, chewableOral5 mg/1
Tablet, multilayer, extended releaseOral
Tablet, orally disintegratingOral10 mg
Tablet, orally disintegratingOral5 mg
Tablet, orally disintegratingOral5 mg/1
SyrupOral1 mg
Tablet, extended releaseOral
Capsule, liquid filledOral10 mg/1
Tablet, orally disintegratingOral10 mg/1
Tablet, film coated, extended releaseOral
CapsuleOral10 mg
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral
Prices
Unit descriptionCostUnit
Claritin 30 10 mg tablet Box29.99USD box
Lisinopril 100% powder21.6USD g
Zestril 40 mg tablet2.48USD tablet
Claritin-d 12 hour tablet sa2.46USD tablet
Prinivil 40 mg tablet2.4USD tablet
Zestril 30 mg tablet2.4USD tablet
Zestril 5 mg tablet1.54USD tablet
Lisinopril 30 mg tablet1.51USD tablet
Claritin 10 mg tablet1.48USD tablet
Claritin-d 24 hour tablet sa1.43USD tablet
Zestril 10 mg tablet1.43USD tablet
Claritin 10 mg reditabs1.4USD tablet
Lisinopril 40 mg tablet1.26USD tablet
Zestril 20 mg tablet1.25USD tablet
Prinivil 20 mg tablet1.23USD tablet
Prinivil 10 mg tablet1.15USD tablet
Loratadine-d 24hr tablet1.11USD tablet
Prinivil 5 mg tablet1.11USD tablet
Lisinopril 20 mg tablet1.07USD tablet
Child's claritin 5 mg tablet chew1.02USD tablet
Lisinopril 10 mg tablet0.99USD tablet
Lisinopril 5 mg tablet0.96USD tablet
CVS Pharmacy loratadine-d 24hr tablet0.89USD tablet
Zestril 2.5 mg tablet0.79USD tablet
Tavist nd 10 mg tablet0.74USD tablet
Wal-itin 10 mg tablet0.7USD tablet
Alavert d-12 allergy-sinus tablet0.68USD tablet
Alavert 10 mg tablet0.64USD tablet
Lisinopril 2.5 mg tablet0.64USD tablet
CVS Pharmacy loratadine 10 mg tablet0.52USD tablet
Loratadine 10 mg tablet0.47USD tablet
CVS Pharmacy allergy relief 10 mg tablet0.44USD tablet
Qc loratadine 10 mg tablet0.08USD tablet
Allergy relief 10 mg tablet0.07USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6132758No1998-06-012018-06-01Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)134-136 °CPhysProp
water solubility0.000011 mg/mlNot Available
logP5.20SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0134 mg/mLALOGPS
logP4.8ALOGPS
logP4.55ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)4.33ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area42.43 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity116.98 m3·mol-1ChemAxon
Polarizability41.67 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9754
Caco-2 permeable-0.5488
P-glycoprotein substrateSubstrate0.7337
P-glycoprotein inhibitor IInhibitor0.9505
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterNon-inhibitor0.5143
CYP450 2C9 substrateNon-substrate0.8197
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.677
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorInhibitor0.8949
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9359
Ames testNon AMES toxic0.6884
CarcinogenicityNon-carcinogens0.915
BiodegradationNot ready biodegradable0.9963
Rat acute toxicity2.8964 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7531
hERG inhibition (predictor II)Inhibitor0.8456
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001r-1279000000-1c522c39e53b6bbfb9aa
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001r-0039000000-928ed9c6b46ba83ebe20
MS/MS Spectrum - , positiveLC-MS/MSsplash10-067r-1292000000-3869907bd01f927b6f22
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

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
Piperidinecarboxylic acids / Pyridines and derivatives / Benzenoids / Aryl chlorides / Heteroaromatic compounds / Carbamate esters / Organic carbonic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds
show 4 more
Substituents
Benzocycloheptapyridine / Piperidinecarboxylic acid / Aryl chloride / Aryl halide / Piperidine / Pyridine / Benzenoid / Heteroaromatic compound / Carbamic acid ester / Carbonic acid derivative
show 12 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Details
1. Histamine H1 receptor
Kind
Protein
Organism
Human
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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Cieslewicz G, Gondorowicz K, Grzelewska-Rzymowska I, Rozniecki J, Wojciechowska B: [Effect of loratadine--selective antagonist of histamine (H1) receptor--on allergen-induced bronchoconstriction in atopic asthmatics]. Pneumonol Alergol Pol. 1992;60(11-12):11-5. [PubMed:1303772]
  3. 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. [PubMed:7581058]
  4. 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. [PubMed:8174605]
  5. Cavero I, Mestre M, Guillon JM, Heuillet E, Roach AG: Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans? Drug Saf. 1999;21 Suppl 1:19-31; discussion 81-7. [PubMed:10597865]
  6. Tamura T, Masaki S, Ohmori K, Karasawa A: Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology. 2005 Dec;75(1):45-52. Epub 2005 Jun 7. [PubMed:15942272]
  7. Grzelewska-Rzymowska I, Gondorowicz K, Cieslewicz G, Rozniecki J, Wojciechowska B: [Effect of loratadine (LO), a selective H1 antagonist, on histamine-induced bronchoconstriction]. Pneumonol Alergol Pol. 1992;60(11-12):16-21. [PubMed:1303773]
  8. Menardo JL, Horak F, Danzig MR, Czarlewski W: A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4. [PubMed:9444440]
  9. Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41. [PubMed:1977506]
  10. Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27. [PubMed:11291777]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the ...
Gene Name
KCNH2
Uniprot ID
Q12809
Uniprot Name
Potassium voltage-gated channel subfamily H member 2
Molecular Weight
126653.52 Da
References
  1. Crumb WJ Jr: Loratadine blockade of K(+) channels in human heart: comparison with terfenadine under physiological conditions. J Pharmacol Exp Ther. 2000 Jan;292(1):261-4. [PubMed:10604956]
  2. Taglialatela M, Pannaccione A, Castaldo P, Giorgio G, Zhou Z, January CT, Genovese A, Marone G, Annunziato L: Molecular basis for the lack of HERG K+ channel block-related cardiotoxicity by the H1 receptor blocker cetirizine compared with other second-generation antihistamines. Mol Pharmacol. 1998 Jul;54(1):113-21. [PubMed:9658196]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Warzecha H, Ferme D, Peer M, Frank A, Unger M: Bioconversion of the antihistaminc drug loratadine by tobacco cell suspension cultures expressing human cytochrome P450 3A4. J Biosci Bioeng. 2010 Mar;109(3):288-90. doi: 10.1016/j.jbiosc.2009.09.001. Epub 2009 Sep 29. [PubMed:20159579]
  2. Li C, Lee MY, Choi JS: Effects of silybinin, CYP3A4 and P-glycoprotein inhibitor in vitro, on the bioavailability of loratadine in rats. Pharmazie. 2010 Jul;65(7):510-4. [PubMed:20662320]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Barecki ME, Casciano CN, Johnson WW, Clement RP: In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes. Drug Metab Dispos. 2001 Sep;29(9):1173-5. [PubMed:11502723]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Barecki ME, Casciano CN, Johnson WW, Clement RP: In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes. Drug Metab Dispos. 2001 Sep;29(9):1173-5. [PubMed:11502723]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Transporters

Kind
Protein
Organism
Human
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
  1. 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. [PubMed:11454724]

Drug created on June 13, 2005 07:24 / Updated on January 19, 2018 10:48