Definition
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.
desloratadine is available off the shelf in Canada); Loratadine is a tricyclic antihistamine, which has a selective and peripheral H1-antagonist action. It has a long-lasting effect and does not normally cause drowsiness because it does not readily enter the central nervous system; An antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake; Loratadine is a drug used to treat allergies. It is marketed by Schering-Plough under several trade names such as Claritin, Clarityn or Claratyne depending on the market, by Lek as Lomilan and by Wyeth as Alavert. It is also available as a generic; Loratadine is a drug used to treat allergies. It is marketed by Schering-Plough under several trade names such as Claritin, Clarityn or Claratyne depending on the market, by Lek as Lomilan and by Wyeth as Alavert. It is also available as a generic. Its active metabolite, desloratadine, is also on the market, though loratadine itself is the only drug of its class available over the counter (at least in the U.S. as of 2005. Loratadine is available off the shelf in the UK [HMDB]
Description
Loratadine is a tricyclic antihistamine, which has a selective and peripheral H1-antagonist action. It has a long-lasting effect and does not normally cause drowsiness because it does not readily enter the central nervous system; An antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake; Loratadine is a drug used to treat allergies. It is marketed by Schering-Plough under several trade names such as Claritin, Clarityn or Claratyne depending on the market, by Lek as Lomilan and by Wyeth as Alavert. It is also available as a generic; Loratadine is a drug used to treat allergies. It is marketed by Schering-Plough under several trade names such as Claritin, Clarityn or Claratyne depending on the market, by Lek as Lomilan and by Wyeth as Alavert. It is also available as a generic. Its active metabolite, desloratadine, is also on the market, though loratadine itself is the only drug of its class available over the counter (at least in the U.S. as of 2005. Loratadine is available off the shelf in the UK.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic Half Life: 8.4 hours
- Uses/Sources: Used to treat allergies. 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).
- Health Effects: Loratadine causes sedation and psychomotor impairment.
- Symptoms: Somnolence, tachycardia, and headache. Psychomotor impairment, and antimuscarinic effects such as urinary retention, dry mouth, blurred vision, and gastrointestinal disturbances are the most common side effects.
- Treatment: Treatment of overdosage would reasonably consist of emesis (ipecac syrup), except in patients with impaired consciousness, followed by the administration of activated charcoal to absorb any remaining drug. If vomiting is unsuccessful, or contraindicated, gastric lavage should be performed with normal saline. Saline cathartics may also be of value for rapid dilution of bowel contents. Loratadine is not eliminated by hemodialysis. It is not known if loratadine is eliminated by peritoneal dialysis. (L1712)
- Route of Exposure: Rapidly absorbed following oral administration (40% bioavailability)
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD<sub>50</sub>=mg/kg (orally in rat)
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Potassium voltage-gated channel subfamily H member 2 Solute carrier family 22 member 2 |
9687576 9658196 11705456 |
|
Histamine H1 receptor | Like other H1-blockers, loratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Loratadine also has a weak affinity for acetylcholine and alpha-adrenergic receptors. |
7581058 11752352 1303772 15482930 10597865 15942272 8174605 |
Loratadine Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Lipidoses | 60.9 |
|
Breast carcinoma | 20.41 |
|
Carcinoma, squamous cell of head and neck | 16.25 |
|
Status Epilepticus | 13.45 |
|
Hepatocellular carcinoma | 13.2 |
|
Colorectal cancer | 12.08 |
|
Disease Progression | 11.84 |
|
Nervous System Diseases | 11.73 |
|
Liver Cirrhosis, Experimental | 11.6 |
|
Myocardial Reperfusion Injury | 11.58 |
|
Prostatic Neoplasms | 10.74 |
|
Reperfusion Injury | 10.66 |
|
Drug-Related Side Effects and Adverse Reactions | 9.28 | |
Acute lymphoblastic leukemia | 9.06 |
|
Retinal Detachment | 9.06 |
|
Prostatic Intraepithelial Neoplasia | 8.63 |
|
Endotoxemia | 8.04 |
|
Alzheimer's Disease | 7.92 |
|
Astrocytoma | 7.76 |
|
Atherosclerosis | 7.71 |
|