Loratadine

• Catalog No.: DB00455
• CAS Number: 79794-75-5
• M. F.: C22H23ClN2O2
• M. W.: 382.88322

SYNONYMS

• IUPAC name: ethyl 4-{13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-2-ylidene}piperidine-1-carboxylate
• IUPAC Traditional name: loratadine
• Brand Name: Clarityne; Loraver; Loradex; Lowadina; Clarityn; Bedix Loratadina; Biloina; Claritin Reditabs; Lergy; Loratyne; Lorfast; Nularef; Optimin; Polaratyne; Rhinase; Sensibit; Lomilan; Aerotina; Alarin; Alavert; Alerpriv; Allertidin; Claratyne; Clarinase; Claritin; Claritin-D; Lertamine; Loracert; Loradif; Loranox; Lorantis; Lorastine; Pylor; Rinomex; Sinhistan Dy; Sohotin; Talorat Dy; Velodan; Zeos; Roletra; Bonalerg; Civeran; Clarinase Reperabs; Claritine; Fristamin; Histaloran; Lesidas; Lisino; Loritine; Restamine; Sanelor; Tadine; Versal
• Synonyms: Loratadinum [Latin]; Loratadina [Spanish]

DATABASE IDS

• CAS Number: 79794-75-5
• PubChem SID: 46507853
• PubChem CID: 3957

PROPERTIES

• Hydrophobicity(logP): 3.8
• Solubility: 0.000011 mg/ml

DETAILS

Description (English)

• Drug 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]
• 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).
• Pharmacology: 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.
• Toxicity: somnolence, tachycardia, and headache LD₅₀=mg/kg (orally in rat)
• Affected Organisms: Humans and other mammals
• Biotransformation: Hepatic
• Absorption: Rapidly absorbed following oral administration (40% bioavailability)
• Half Life: 8.4 hours
• Protein Binding: 97-99%
• References: See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6. [Pubmed] ; 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] ; Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41. [Pubmed] ; Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27. [Pubmed]
• External Links: Wikipedia; RxList; Drugs.com

REFERENCES

• See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6. Pubmed
• Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27. Pubmed
• 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
• Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41. Pubmed