Loratadine

Identification

Summary

Loratadine is a second generation antihistamine used to manage the symptoms of allergic rhinitis.

Brand Names

Alavert, Alavert D, Allerclear, Claritin, Claritin-D, Diphen, Loradamed, Wal-itin, Wal-itin D

Generic Name

Loratadine

DrugBank Accession Number

DB00455

Background

Loratadine is a second generation antihistamine used to manage symptoms of allergic rhinitis.⁵ A lack of sedative and CNS adverse effects make loratadine, along with other second generation antihistamines, preferable over their 1st generation counterparts in many clinical situations.⁷

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Loratadine (DB00455)

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Weight

Average: 382.883
Monoisotopic: 382.144805697

Chemical Formula

C₂₂H₂₃ClN₂O₂

Synonyms

• Loratadina
• Loratadine
• Loratadinum

External IDs

• SCH-29851

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Pharmacology

Indication

Loratadine is a 2nd generation antihistamine and is used to manage symptoms of allergic rhinitis, wheal formation, urticaria, and other allergic dermatologic conditions.⁵⁶¹⁷

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Symptomatic treatment of	Allergic dermatologic disorders		••• •••			•••••••
Symptomatic treatment of	Allergic dermatologic disorders		••• •••			••••••• ••••••• ••••••• •••••• ••••••••••••••
Used in combination for symptomatic treatment of	Allergic rhinitis (ar)	Combination Product in combination with: Pseudoephedrine (DB00852)	••••••••••••			••••••• ••••••• •••••••• •••••••
Used in combination for symptomatic treatment of	Allergic rhinitis (ar)	Combination Product in combination with: Pseudoephedrine (DB00852), Acetaminophen (DB00316)	••••••••••••			••••••
Symptomatic treatment of	Allergic rhinitis (ar)		••••••••••••			••••••• ••••••••••••

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Pharmacodynamics

Like other 2nd generation antihistamines, loratadine is selective for peripheral H1 receptors.⁹ Loratadine does not penetrate effectively into the central nervous system and has poor affinity for CNS H1-receptors.⁹ These qualities result in a lack of CNS depressant effects such as drowsiness, sedation, and impaired psychomotor function.⁹

Mechanism of action

Histamine release is a key mediator in allergic rhinitis and urticaria.¹²⁷⁸ As a result, loratadine exerts it's effect by targeting H1 histamine receptors.

Loratadine binds to H1 histamine receptors found on the surface of epithelial cells, endothelial cells, eosinophils, neutrophils, airway cells, and vascular smooth muscle cells among others.⁷ H1 histamine receptors fall under the wider umbrella of G-protein coupled receptors, and exist in a state of equilibrium between the active and inactive forms.⁷⁸ Histamine binding to the H1-receptor facilitates cross linking between transmembrane domains III and V, stabilizing the active form of the receptor.⁷⁸ On the other hand, antihistamines bind to a different site on the H1 receptor favouring the inactive form.⁷⁸

Hence, loratadine can more accurately be classified as an "inverse agonist" as opposed to a "histamine antagonist", and can prevent or reduce the severity of histamine mediated symptoms.⁷⁸¹⁷

Target	Actions	Organism
AHistamine H1 receptor	antagonist	Humans
UPotassium voltage-gated channel subfamily H member 2	antagonist	Humans

Absorption

Loratadine is rapidly absorbed and achieves peak plasma concentration in 1-2 hours, while it's main metabolite achieves peak plasma concentration in 3-4 hours.⁶

In the rapid dissolve formulation, the pharmacokinetic parameters of loratadine are as follows¹⁷: Cmax = 2.56 ng/ml, Tmax = 1.14 hrs, AUC = 6.14 ng x hr/ml.

In the rapid dissolve formulation, the pharmacokinetic parameters of descarboethoxyloratadine are as follows¹⁷: Cmax = 3.72 ng/ml, Tmax = 1.97 hr, AUC = 49.1 ng x hr/ml.

In the conventional formulation, the pharmacokinetic parameters of loratadine are as follows¹⁷: Cmax = 2.11 ng/ml, Tmax = 1.00 hr, AUC = 4.64 ng x hr/ml

In the conventional formulation, the pharmacokinetic parameters of descarboethoxyloratadine are as follows¹⁷: Cmax = 3.66 ng/ml, Tmax = 1.97 hr, AUC = 48.4 ng x hr/ml

Volume of distribution

The volume of distribution of loratadine is 120 L/Kg.¹⁸

Protein binding

97 - 99% of the loratadine is bound to plasma proteins.¹⁷

Metabolism

Loratadine undergoes extensive first pass metabolism in the liver and is primarily metabolized by CYP3A4, CYP2D6, CYP1A1 and CYP2C19. Less involved CYP enzymes include CYP1A2, CYP2B6, CYP2C8, CYP2C9 and CYP3A5.¹⁰¹¹ CYP3A4 and CYP2D6 are mainly responsible for metabolizing loratadine to descarboethoxyloratadine.¹¹ This primary metabolite is 4 times more pharmacologically active than loratadine.⁶

In addition, a study demonstrates that descarboethoxyloratadine is first glucuronidated by UGT2B10, then hydroxylated by CYP2C8 to form 3-hydroxydesloratadine.¹⁵ Further glucuronidation of 3-hydroxydesloratadine facilitates excretion.¹⁶

Hover over products below to view reaction partners

• Loratadine
  • Descarboethoxyloratadine
    • hydroxylated metabolite, desloratadine
    • desloratadine glucuronide
      • 3-hydroxydesloratadine
        • 3-hydroxydesloratadine glucuronide
  • hydroxylated metabolite, loratadine

Route of elimination

Over a 10 day period, 40% of loratadine is excreted in the urine, and 42% is eliminated in the faeces.¹⁷

Half-life

The elimination half life is approximately 10 hours for loratadine and 20 hours for descarboethoxyloratadine.⁶

Clearance

The clearance of loratadine after single oral doses of 20 mg and 40 mg are 12 L/h/kg and 9 L/h/kg respectively.⁹ P-glycoprotein is involved in the clearance of many 2nd generation antihistamines, including loratadine, from the central nervous system. 1st generation antihistamines are not cleared by P-glycoprotein, which may help explain why they have a different central nervous system adverse effect profile compared to their 2nd generation counterparts.¹⁸¹³ It appears that an antihistamine with higher affinity for p-glycoprotein will have a lower incidence of CNS adverse effects.¹⁴

Adverse Effects

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Toxicity

Second generation antihistamines such as loratadine have very few adverse effects; however, insomnia, headache, fatigue, drowsiness and rash have been reported.⁷ Symptoms of loratadine overdose include gastrointestinal side effects, agitation, drowsiness, tachycardia, and headache.⁷ It is advised to obtain an ECG in the event of loratadine overdose.⁷

Pathways

Pathway	Category
Loratadine H1-Antihistamine Action	Drug action

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abametapir	The serum concentration of Loratadine can be increased when it is combined with Abametapir.
Aclidinium	Aclidinium may increase the anticholinergic activities of Loratadine.
Acrivastine	The risk or severity of QTc prolongation can be increased when Loratadine is combined with Acrivastine.
Adenosine	The risk or severity of QTc prolongation can be increased when Loratadine is combined with Adenosine.
Ajmaline	The risk or severity of QTc prolongation can be increased when Loratadine is combined with Ajmaline.

Food Interactions

No interactions found.

Products

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Product Images

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International/Other Brands

Aerotina / Alavert / Biloina / Civeran / Fristamin / Histaloran / Lomilan / Loracert / Loradex / Loranox / Lorastine / Loratyne / Loritine / Nularef / Restamine / Roletra / Sensibit

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Loratadine	Tablet	10 mg/1	Oral	Northwind Pharmaceuticals	2014-10-27	Not applicable
Loratadine Allergy Relief	Tablet	10 mg/1	Oral	Clinical Solutions Wholsesale	2003-08-28	2017-06-28
Loratadine antihistamine	Tablet	10 mg/1	Oral	bryant ranch prepack	2008-10-15	Not applicable
Loratadineantihistamine antihistamine	Tablet	10 mg/1	Oral	Remedy Repack	2015-02-19	2017-01-23
Loratadineantihistamine antihistamine	Tablet	10 mg/1	Oral	Remedy Repack	2013-05-29	2016-07-11

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
24 / 7 Life Non-Drowsy Allergy Relief	Tablet	10 mg/1	Oral	Lil' Drug Store Products, Inc.	2020-12-17	Not applicable
24 / 7 Life Non-Drowsy Allergy Relief	Tablet	10 mg/1	Oral	Lil' Drug Store Products, Inc.	2022-10-24	Not applicable
24 Hour Allergy Relief	Tablet	10 mg/1	Oral	Meijer Distribution Inc	2014-12-30	2016-05-21
24 Hour Allergy Remedy	Tablet	10 mg	Oral	Vita Health Products Inc	2006-07-28	Not applicable
7 Select Allergy Relief	Tablet	10 mg/1	Oral	7-Eleven	2014-05-14	2020-10-31

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
12 Hour Allergy and Congestion	Loratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)	Tablet, film coated, extended release	Oral	Walgreen Company	2018-05-05	Not applicable
ADOREM GRIPA TABLETAS	Loratadine (5 mg) + Acetaminophen (500 mg) + Phenylephrine hydrochloride (10 mg)	Tablet	Oral	LABORATORIOS SIEGFRIED S.A.S.	2006-11-10	2010-06-18
Alavert Allergy and Congestion D-12 hour	Loratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)	Tablet, film coated, extended release	Oral	Foundation Consumer Brands	2021-12-15	Not applicable
Alavert Allergy Sinus D-12	Loratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)	Tablet, film coated, extended release	Oral	Haleon US Holdings LLC	2004-01-30	Not applicable
Alavert Allergy Sinus D-12	Loratadine (5 mg/1) + Pseudoephedrine sulfate (120 mg/1)	Tablet, film coated, extended release	Oral	Physicians Total Care, Inc.	2007-04-26	2012-06-30

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
AlloPAX	Loratadine (3 g/3g) + Levocetirizine dihydrochloride (3 g/3g)	Kit	Transdermal	PharmaGenetico LLC	2015-06-30	Not applicable
Help I have allergies	Loratadine (10 mg/1)	Tablet	Oral	Help Remedies, Inc.	2009-07-01	Not applicable
Loratadine	Loratadine (10 mg/1)	Tablet	Oral	Rebel Distributors	2010-01-21	Not applicable
Nazirex Compounding Kit	Loratadine (1 g/1g) + Levocetirizine dihydrochloride (1 g/1g)	Kit	Topical	Alvix Laboratories	2015-03-18	2015-07-01

Categories

ATC Codes

R06AX13 — Loratadine

• R06AX — Other antihistamines for systemic use
• R06A — ANTIHISTAMINES FOR SYSTEMIC USE
• R06 — ANTIHISTAMINES FOR SYSTEMIC USE
• R — RESPIRATORY SYSTEM

Drug Categories

• Anti-Allergic Agents
• Antihistamines for Systemic Use
• Antipruritics
• Benzocycloheptenes
• BSEP/ABCB11 Substrates
• Cytochrome P-450 CYP1A2 Substrates
• Cytochrome P-450 CYP2B6 Substrates
• Cytochrome P-450 CYP2C19 Inhibitors
• Cytochrome P-450 CYP2C19 Inhibitors (weak)
• Cytochrome P-450 CYP2C19 Substrates
• Cytochrome P-450 CYP2C8 Inhibitors
• Cytochrome P-450 CYP2C8 Inhibitors (moderate)
• Cytochrome P-450 CYP2C8 Substrates
• Cytochrome P-450 CYP2C9 Substrates
• Cytochrome P-450 CYP2D6 Inhibitors
• Cytochrome P-450 CYP2D6 Inhibitors (weak)
• Cytochrome P-450 CYP2D6 Substrates
• Cytochrome P-450 CYP3A Inhibitors
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Inhibitors
• Cytochrome P-450 CYP3A4 Inhibitors (weak)
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A5 Substrates
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Dermatologicals
• Dibenzocycloheptenes
• Histamine Antagonists
• Histamine H1 Antagonists
• Histamine H1 Antagonists, Non-Sedating
• Loratadine and derivatives
• Neurotransmitter Agents
• P-glycoprotein inhibitors
• P-glycoprotein substrates
• Piperidines
• Potential QTc-Prolonging Agents
• QTc Prolonging Agents

Chemical TaxonomyProvided by Classyfire

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 / Organochlorides / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds

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Substituents

Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Benzocycloheptapyridine / Carbamic acid ester / Carbonic acid derivative / Carbonyl group / Heteroaromatic compound / Hydrocarbon derivative / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organochloride / Organohalogen compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Piperidine / Piperidinecarboxylic acid / Pyridine

show 12 more

Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

Not Available

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

7AJO3BO7QN

CAS number

79794-75-5

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[9.4.0.0^{3,8}]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

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. [Article]
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. [Article]
3. Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41. [Article]
4. Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27. [Article]
5. Tenn MW, Steacy LM, Ng CC, Ellis AK: Onset of action for loratadine tablets for the symptomatic control of seasonal allergic rhinitis in adults challenged with ragweed pollen in the Environmental Exposure Unit: a post hoc analysis of total symptom score. Allergy Asthma Clin Immunol. 2018 Jan 16;14:5. doi: 10.1186/s13223-017-0227-4. eCollection 2018. [Article]
6. Barenholtz HA, McLeod DC: Loratadine: a nonsedating antihistamine with once-daily dosing. DICP. 1989 Jun;23(6):445-50. [Article]
7. Randall KL, Hawkins CA: Antihistamines and allergy. Aust Prescr. 2018 Apr;41(2):41-45. doi: 10.18773/austprescr.2018.013. Epub 2018 Apr 3. [Article]
8. Church MK, Church DS: Pharmacology of antihistamines. Indian J Dermatol. 2013 May;58(3):219-24. doi: 10.4103/0019-5154.110832. [Article]
9. Clissold SP, Sorkin EM, Goa KL: Loratadine. A preliminary review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1989 Jan;37(1):42-57. [Article]
10. Ghosal A, Gupta S, Ramanathan R, Yuan Y, Lu X, Su AD, Alvarez N, Zbaida S, Chowdhury SK, Alton KB: Metabolism of loratadine and further characterization of its in vitro metabolites. Drug Metab Lett. 2009 Aug;3(3):162-70. Epub 2009 Aug 1. [Article]
11. Zhang YF, Chen XY, Zhong DF, Dong YM: Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects. Acta Pharmacol Sin. 2003 Jul;24(7):715-8. [Article]
12. Naclerio RM: The role of histamine in allergic rhinitis. J Allergy Clin Immunol. 1990 Oct;86(4 Pt 2):628-32. doi: 10.1016/s0091-6749(05)80227-1. [Article]
13. Obradovic T, Dobson GG, Shingaki T, Kungu T, Hidalgo IJ: Assessment of the first and second generation antihistamines brain penetration and role of P-glycoprotein. Pharm Res. 2007 Feb;24(2):318-27. doi: 10.1007/s11095-006-9149-4. Epub 2006 Dec 19. [Article]
14. Conen S, Theunissen EL, Vermeeren A, van Ruitenbeek P, Stiers P, Mehta MA, Toennes SW, Ramaekers JG: The role of P-glycoprotein in CNS antihistamine effects. Psychopharmacology (Berl). 2013 Sep;229(1):9-19. doi: 10.1007/s00213-013-3075-z. Epub 2013 Apr 7. [Article]
15. Kazmi F, Barbara JE, Yerino P, Parkinson A: A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement. Drug Metab Dispos. 2015 Apr;43(4):523-33. doi: 10.1124/dmd.114.062620. Epub 2015 Jan 16. [Article]
16. Aratyn-Schaus Y, Ramanathan R: Advances in high-resolution MS and hepatocyte models solve a long-standing metabolism challenge: the loratadine story. Bioanalysis. 2016 Aug;8(16):1645-62. doi: 10.4155/bio-2016-0094. Epub 2016 Jul 27. [Article]
17. Health Canada Product Monograph: Claritin (loratadine) [Link]
18. Comparative Pharmacology of the H1 Antihistamines [Link]

External Links

Human Metabolome Database

HMDB0005000

KEGG Drug

D00364

PubChem Compound

3957

PubChem Substance

46507853

ChemSpider

3820

BindingDB

22876

RxNav

28889

ChEBI

6538

ChEMBL

CHEMBL998

ZINC

ZINC000000537931

Therapeutic Targets Database

DAP000101

PharmGKB

PA450266

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

Wikipedia

Loratadine

MSDS

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Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Other	Allergic Rhinitis (AR)	1
4	Completed	Other	Healthy Subjects (HS)	1
4	Completed	Treatment	Allergic Conjunctivitis (AC)	1
4	Completed	Treatment	Allergic Rhinitis (AR)	2
4	Completed	Treatment	Allergic Rhinitis (AR) / Allergy to Tree Pollen / Seasonal Allergic Rhinitis	1

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

• Amerisource Health Services Corp.
• AstraZeneca Inc.
• Cardinal Health
• Catalent Pharma Solutions
• Chain Drug
• Concern Stirol
• CVS Pharmacy
• Direct Dispensing Inc.
• Dispensing Solutions
• Diversified Healthcare Services Inc.
• H.J. Harkins Co. Inc.
• Major Pharmaceuticals
• Merck & Co.
• Neuman Distributors Inc.
• Novartis AG
• Nucare Pharmaceuticals Inc.
• Patient First Corp.
• PD-Rx Pharmaceuticals Inc.
• Physicians Total Care Inc.
• Prepak Systems Inc.
• Prescript Pharmaceuticals
• Professional Co.
• S&P Healthcare
• Southwood Pharmaceuticals
• Walgreen Co.
• West-Ward Pharmaceuticals
• Wockhardt Ltd.
• Wyeth Pharmaceuticals

Dosage Forms

Form	Route	Strength
Tablet, chewable	Buccal	10 mg
Tablet, film coated, extended release	Oral
Solution	Oral	1.000 mg
Tablet, film coated	Oral
Tablet	Oral
Kit	Transdermal
Tablet, effervescent	Oral
Tablet, orally disintegrating	Oral
Suspension	Oral	1 mg/ml
Solution	Oral	100.000 mg
Syrup	Oral	100.000 mg
Capsule	Oral
Liquid	Oral	5 mg/5mL
Tablet, orally disintegrating	Oral	10 mg/1
Tablet	Oral
Syrup	Oral	5 mg/5ml
Tablet, chewable	Oral	5 mg/1
Tablet, multilayer, extended release	Oral
Tablet, chewable	Oral	10 mg/1
Kit	Oral
Syrup	Oral	5 mg / 5 mL
Tablet, orally disintegrating	Oral	10 mg
Tablet, orally disintegrating	Oral	5 mg
Tablet, orally disintegrating	Oral	5 mg/1
Syrup	Oral	1 mg / mL
Film, soluble	Oral	10 MG
Tablet, sugar coated	Oral
Tablet, film coated	Oral	10 mg
Syrup	Oral
Capsule, liquid filled	Oral
Tablet, delayed release	Oral
Cream; kit; liquid; ointment; tablet; tablet, chewable; tablet, film coated	Oral; Topical
Syrup	Oral	0.100 g
Solution	Oral
Tablet, effervescent	Oral	10 MG
Tablet, film coated	Oral
Tablet, film coated	Oral	5 MG
Solution	Oral	0.100 g
Tablet, film coated	Oral	10 mg/1
Solution	Oral	100 mg
Suspension	Oral	1 mg/1ml
Syrup	Oral	0.10 g
Tablet	Oral	10.000 mg
Granule	Oral
Solution	Oral	1 mg
Suspension	Oral
Syrup	Oral	1.0 mg/ml
Tablet	Oral	10.0 mg
Tablet	Oral	10 mg
Tablet	Oral	1000000 mg
Syrup	Oral	100 mg
Syrup	Oral	1 MG/ML
Solution	Oral	0.1 g
Tablet, soluble	Oral	10 mg
Syrup	Oral	0.1 g
Capsule, liquid filled	Oral	10 mg/1
Solution	Oral	5 mg/5mL
Tablet	Oral	10 mg/1
Tablet	Oral	5 mg/1
Tablet, extended release	Oral
Capsule, coated	Oral
Capsule	Oral	10 mg
Solution	Oral	100.00 mg
Solution	Oral
Kit	Topical
Tablet	Oral	10 mg / tab
Syrup	Oral
Tablet	Oral	10000 MG
Suspension	Oral
Powder, for solution	Oral
Capsule, extended release
Tablet	Oral	10.00 mg
Tablet, soluble	Oral
Tablet, coated	Oral
Syrup	Oral	100.00 mg
Syrup	Oral	5 ml/5ml
Syrup	Oral	5 mg/5ml
Tablet, coated	Oral	10 mg

Prices

Unit description	Cost	Unit
Claritin 30 10 mg tablet Box	29.99USD	box
Lisinopril 100% powder	21.6USD	g
Zestril 40 mg tablet	2.48USD	tablet
Claritin-d 12 hour tablet sa	2.46USD	tablet
Prinivil 40 mg tablet	2.4USD	tablet
Zestril 30 mg tablet	2.4USD	tablet
Zestril 5 mg tablet	1.54USD	tablet
Lisinopril 30 mg tablet	1.51USD	tablet
Claritin 10 mg tablet	1.48USD	tablet
Claritin-d 24 hour tablet sa	1.43USD	tablet
Zestril 10 mg tablet	1.43USD	tablet
Claritin 10 mg reditabs	1.4USD	tablet
Lisinopril 40 mg tablet	1.26USD	tablet
Zestril 20 mg tablet	1.25USD	tablet
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Alavert d-12 allergy-sinus tablet	0.68USD	tablet
Alavert 10 mg tablet	0.64USD	tablet
Lisinopril 2.5 mg tablet	0.64USD	tablet
CVS Pharmacy loratadine 10 mg tablet	0.52USD	tablet
Loratadine 10 mg tablet	0.47USD	tablet
CVS Pharmacy allergy relief 10 mg tablet	0.44USD	tablet
Qc loratadine 10 mg tablet	0.08USD	tablet
Allergy relief 10 mg tablet	0.07USD	tablet

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Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US6132758	No	2000-10-17	2018-06-01

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	134-136 °C	https://www.chemicalbook.com/ChemicalProductProperty_US_CB5283770.aspx
water solubility	<1 mg/ml at 25°C	https://www.chemicalbook.com/ChemicalProductProperty_US_CB5283770.aspx

Predicted Properties

Property	Value	Source
Water Solubility	0.0134 mg/mL	ALOGPS
logP	4.8	ALOGPS
logP	4.55	Chemaxon
logS	-4.5	ALOGPS
pKa (Strongest Basic)	4.33	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	2	Chemaxon
Hydrogen Donor Count	0	Chemaxon
Polar Surface Area	42.43 Å2	Chemaxon
Rotatable Bond Count	2	Chemaxon
Refractivity	116.98 m3·mol-1	Chemaxon
Polarizability	41.68 Å3	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	1.0
Blood Brain Barrier	+	0.9754
Caco-2 permeable	-	0.5488
P-glycoprotein substrate	Substrate	0.7337
P-glycoprotein inhibitor I	Inhibitor	0.9505
P-glycoprotein inhibitor II	Inhibitor	0.8387
Renal organic cation transporter	Non-inhibitor	0.5143
CYP450 2C9 substrate	Non-substrate	0.8197
CYP450 2D6 substrate	Substrate	0.8918
CYP450 3A4 substrate	Substrate	0.677
CYP450 1A2 substrate	Non-inhibitor	0.9045
CYP450 2C9 inhibitor	Inhibitor	0.8949
CYP450 2D6 inhibitor	Non-inhibitor	0.9231
CYP450 2C19 inhibitor	Inhibitor	0.8994
CYP450 3A4 inhibitor	Non-inhibitor	0.831
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.9359
Ames test	Non AMES toxic	0.6884
Carcinogenicity	Non-carcinogens	0.915
Biodegradation	Not ready biodegradable	0.9963
Rat acute toxicity	2.8964 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.7531
hERG inhibition (predictor II)	Inhibitor	0.8456

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-004i-6059000000-3d596b5ab5499c4089ca
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-001r-0039000000-928ed9c6b46ba83ebe20
MS/MS Spectrum - , positive	LC-MS/MS	splash10-001r-1279000000-1c522c39e53b6bbfb9aa
MS/MS Spectrum - , positive	LC-MS/MS	splash10-001r-0039000000-928ed9c6b46ba83ebe20
MS/MS Spectrum - , positive	LC-MS/MS	splash10-067r-1292000000-3869907bd01f927b6f22
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-001i-0009000000-f3e737e148a290040627
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-001i-0009000000-4fb68fc54ede88aedd84
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-001r-0019000000-b3e96b96dece1aa1dca6
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-001i-5009000000-810a8984357284a1bd94
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-004m-0291000000-02c910217527e79e158b
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-001i-8279000000-0c7d83062cbd60912af6
1H NMR Spectrum	1D NMR	Not Applicable
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable
[1H,13C] 2D NMR Spectrum	2D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	199.044604	predicted	DarkChem Lite v0.1.0
[M-H]-	195.4247137	predicted	DarkChem Lite v0.1.0
[M-H]-	187.70808	predicted	DeepCCS 1.0 (2019)
[M+H]+	199.392804	predicted	DarkChem Lite v0.1.0
[M+H]+	184.3887636	predicted	DarkChem Lite v0.1.0
[M+H]+	190.0661	predicted	DeepCCS 1.0 (2019)
[M+Na]+	199.309204	predicted	DarkChem Lite v0.1.0
[M+Na]+	199.533504	predicted	DarkChem Lite v0.1.0
[M+Na]+	197.12764	predicted	DeepCCS 1.0 (2019)

Targets

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	290	N/A	N/A	A27481
Ki (nM)	414	N/A	N/A	A27842
Ki (nM)	37	N/A	N/A	A27844

Details

Binding Properties1. Histamine H1 receptor

Kind

Protein

Organism

Humans

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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
9. Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41. [Article]

Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	173	N/A	N/A	A27426
IC 50 (nM)	170	N/A	N/A	A18337
IC 50 (nM)	169.82	N/A	N/A	A27428 / A27431
IC 50 (nM)	173.78	N/A	N/A	A27432 / A27558

Details

Binding Properties2. Potassium voltage-gated channel subfamily H member 2

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Antagonist

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. [Article]
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. [Article]

×

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Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54