Loratadine chemical structure
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Loratadine

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, 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 US and UK) as of 2005. more...

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It is sometimes combined with pseudoephedrine to add a decongestant aspect to the treatment, making it somewhat useful for colds as well as allergies.

Available forms

Loratadine is available as tablets and oral suspension, and also in combination with pseudoephedrine. Also available are quick-dissolving tablets, which are advertised as being faster to get into one's system but which require special handling to avoid degrading in the package.

Mechanism of action

Loratadine is a tricyclic antihistamine, which has a selective and peripheral H1-antagonist action. It has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.

Pharmacokinetics

Loratadine is rapidly absorbed from the gastro-intestinal tract and it has rapid first-pass hepatic metabolism. Loratadine is almost totally bound to plasma proteins. Its metabolite, desloratadine (descarboethoxyloratadine), is also active, but binds to plasma proteins only moderately. The half-life of loratadine is on average 8 hours, and its metabolites 28 hours. About 40% is excreted as conjugated metabolites into the urine and similar amount into the feces. Traces of unmetabolised loratadine can be found in the urine.

Recommended dosage

  • Adults and children 15+ years: 10mg once every 24 hours.
  • Children 2-14 years:
    • Bodyweight above 30kg: 10mg once every 24 hours.
    • Bodyweight below 30kg: 5mg once every 24 hours.

(From product packaging for Clarityn tablets.)

Side-effects

Most common side-effects are fatigue, drowsiness, dry mouth, headache, and gastrointestinal disturbances.

Loratadine vs. desloratadine

A November 2003 article published in the journal American Family Physician about the safety, tolerability, effectiveness, price, and simplicity of desloratadine concluded the following:

Desloratadine is similar in effectiveness to fexofenadine and would be expected to produce results similar to loratadine and other nonsedating antihistamines.Thus Desloratidine is of faster onset of action than Loratidine as the Loratidine is activated in the liver into Desloratidine (which was introduced into the american market under the name Aerius by Schering Plough corporation). However, it may be an option for patients whose medical insurance no longer covers loratadine if the co-pay is less than the cost of the over-the-counter product.

External links and references

  • Desloratadine for Allergic Rhinitis, a November 2003 article from American Family Physician
  • Packaging directions in PDF Format. Product Packaging for Claritin 24 hour tablets. URL accessed on January 3, 2005.


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Schering-Plough goes to court to protect loratadine patent - OTC/Natural Health Category News - Claritin - Brief Article
From Drug Store News, 2/18/02

KENILWORTH, N.J. -- Schering-Plough announced Jan. 31 that it has filed separate suits against Johnson & Johnson's McNeil Consumer Healthcare and American Home Products' Whitehall-Robins Healthcare for an alleged patent infringement on the company's prescription loratadine product, Claritin. According to Schering-Plough, the suits "seek to prevent McNeil and Whitehall from manufacturing, using, selling or otherwise making a loratadine product until after the expiration of the metabolite patent [desloratadine]." Desloratadine is listed as the active ingredient in Clarinex, a prescription-only allergy remedy that is expected to be Claritin's successor.

In 1998 Wellpoint Health Networks of California petitioned the U.S. Food and Drug Administration to force the Rx-to-OTC switch of Claritin, Allegra (Aventis Pharmaceuticals) and Zyrtec (Pfizer)--an unprecedented move-based on the fact that such a move would save hundreds of millions in U.S. health care costs. On May 11, 2001, two FDA advisory committees recommended that the three products were safe enough to be switched. FDA has yet to issue a final ruling.

McNeil and Whitehall filed new drug applications with the understanding that the patent for loratadine expires December 2002. Schering-Plough is attempting to win extended exclusivity to market loratadine by enforcing its loratadine-metabolite patent on desloratadine, which doesn't expire until October 2004.

"We filed a new drug application with the FDA to introduce an OTC form of loratadine," explained Mark Gutsche, a McNeil spokesman. "We believe our position respects Schering-Plough's patent on loratacline, which is scheduled to expire this year."

"Whitehall is confident in [its] position that the claims of [the loratadine] patent are invalid and/or not infringed," said Fran Sullivan, a Whitehall-Robins' spokesman.

Claritin has posted annual prescription sales totaling more than $2 billion, according to industry estimates. Schering-Plough was already facing a sharp drop in its sales of Claritin by year's end, as competition from generic drug manufacturers moved into the business. Availability of loratadine as an OTC remedy would exacerbate this sales decline.

"The more important story is that J&J and American Home (Wyeth) are major pharmaceutical companies who are pursuing an alternative to the existing switch system," commented Steve Francesco, publisher of Switch magazine. "If this turns out to be successful, [it creates] a template to do third party switches for other products."

Other drug categories that may be open to this switch strategy include digestives, birth control remedies and cox-2 inhibitors, Francesco said. This list includes acid reflux-remedy Prilosec, which pulled in more than $4 billion in annual sales for AstraZeneca.

COPYRIGHT 2002 Reproduced with permission of the copyright holder. Further reproduction or distribution is prohibited without permission.
COPYRIGHT 2002 Gale Group

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