Product Name

Loratadine

CAS Number

79794-75-5

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Product Name:
Loratadine
CAS Number:
79794-75-5
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).
Mode of Action:

Loratadine competes with free histamine and exhibits specific, selective peripheral H_ 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.

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.

Metabolism:

Hepatic

Toxicity:

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

IUPAC:
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
ATC:
R06AX13 R06AX27 C09AA03
PubChem:
3957
DrugBank:
DB00455 (APRD00384)
Formula:
C30H32Cl3NO
Molecular Mass:
382.883
Synonyms:
Loratadina [Spanish] Loratadinum [Latin]
SMILES:
CCOC(=O)N1CCC(CC1)=C1C2=C(CCC3=C1N=CC=C3)C=C(Cl)C=C2
AHFS Code:
04:08.00 24:32.04
InChi:
JCCNYMKQOSZNPW-UHFFFAOYSA-N
General Reference:
General Reference:

  1. See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6. Pubmed
  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
  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
  4. Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27. Pubmed

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