You are on page 1of 4

DRUG PROFILE

LORATADINE

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

Synonyms

Loratadina [Spanish]

Loratadinum [Latin]

Brand mixtures

Chlor-Tripolon ND SRT

Loratadine + Pseudoephedrine Sulfate

Claritin Allergy + Sinus Extra Strength

Loratadine + Pseudoephedrine Sulfate

Liberator

MRR.COLLEGE OF PHARMACY Page 25


DRUG PROFILE

Categories

Antipruritics

Anti-Allergic Agents

Antihistamines

Histamine H1 Antagonists, Non-Sedating

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

Substructures

Alkanes and Alkenes

Carbamates and Derivatives

Phenylpropenes

Pyridines and Derivatives

Ethers

Benzene and Derivatives

Aryl Halides

Halobenzenes

Isoprenes

Heterocyclic compounds

Aromatic compounds

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).

Pharmacodynamics

MRR.COLLEGE OF PHARMACY Page 26


DRUG PROFILE

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.

Absorption

Rapidly absorbed following oral administration (40% bioavailability)

Volume of distribution :Not Available

Protein binding :97-99%

Metabolism : Hepatic

Substrate :Enzymes

Product :Loratadine

Cytochrome P450 3A4

Half life: 8.4 hours

Toxicity

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

Affected organisms

Humans and other mammals

MRR.COLLEGE OF PHARMACY Page 27


DRUG PROFILE

Drug Interactions

Nefazodone -Increased risk of cardiotoxicity

Tacrine

The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the
anticholinergic, Loratadine, may be reduced due to antagonism. The interaction may be
beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both
agents.

Trimethobenzamide

Trimethobenzamide and Loratadine, two anticholinergics, may cause additive anticholinergic


effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.

Triprolidine

Triprolidine and Loratadine, two anticholinergics, may cause additive anticholinergic effects and
enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for
enhanced anticholinergic and CNS depressant effects.

Trospium

Trospium and Loratadine, two anticholinergics, may cause additive anticholinergic effects and
enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.

Food Interactions

Take on empty stomach: 1 hour before or 2 hours after meals.

MRR.COLLEGE OF PHARMACY Page 28

You might also like