Loratadine , sold under the Claritin trademark among others, is a drug used to treat allergies. These include allergic rhinitis (hay fever) and itching. It is also available in combination with pseudoephedrine, decongestants, known as loratadine/pseudoephedrine. It was taken by mouth.
Common side effects include drowsiness, dry mouth, and headaches. Serious side effects are rare and include allergic reactions, seizures, and liver problems. Use during pregnancy seems safe but has not been well studied. Not recommended in children less than two years old. This is in the family of second generation antihistamines.
Loratadine was discovered in 1981 and began to be marketed in 1993. It is on the World Health Organization's Essential Medicines List, the most effective and safe medication needed in the health system. Loratadine is available as a generic drug. Wholesale costs in developing countries are around 0.01 to 0.06 USD per dose by 2015. In the United States, it is available at the counter.
Video Loratadine
Medical use
Loratadine is indicated to alleviate allergic symptoms such as fever (allergic rhinitis), urticaria (itching), chronic idiopathic urticaria, and other skin allergies. For allergic rhinitis (hay fever), loratadine is effective for both nasal and eye symptoms: sneezing, runny nose, itchy or burning eyes.
Similarly for cetirizine, loratadine debilitates the itch associated with Kimura disease. It is marketed because of its less soothing nature.
Form
These drugs are available in various forms, including tablets, oral suspensions, and syrups, and in combination with pseudoephedrine. Also available fast dissolving tablets, which are marketed as faster to get into a person's circulatory system, but require special handling to avoid a decrease in the package.
Maps Loratadine
Contraindications
Patients with severe liver disease (liver) may need to start with a lower dose. No dose adaptation is required for elderly or renal (kidney) patients.
Loratadine is usually compatible with breastfeeding (classified category L-2 by the American Academy of Pediatrics). In the US, it is classified as category B in pregnancy, which means animal reproduction studies have failed to show fetal risks but no adequate and well-controlled studies in pregnant women have been performed.
Adverse effects
As a "non-penating" antihistamine, loratadine causes less (but still significantly, in some cases) psychomotor sedation and retardation than older antihistamines because it penetrates the blood/brain barrier to a lesser extent.
Other possible side effects include headache and antimuscarinic effects such as urinary retention, dry mouth, blurred vision, and gastrointestinal problems.
Interactions
Substances acting as CYP3A4 enzyme inhibitors such as ketoconazole, erythromycin, cimetidine, and furanocoumarin derivatives (found in grapefruit) lead to elevated plasma loratadine levels. This has a significant clinical effect in controlled trials of higher-than-usual loratadine dose (20 mg).
Antihistamines should be discontinued about 48 hours before allergy tests on the skin, as they can prevent or reduce a positive reaction to dermal activity indicators.
Pharmacology
Action mechanism
Loratadine is a tricyclic antihistamine, which acts as a selective inverse agonist of peripheral histamine H 1 . The potential of a second generation histamine antagonist is (from weakest to weakest) desloratadine (K i 0.4 nM) & gt; levoceterizine (K i 3Ã, nM) & gt; cetirizine (K i 6Ã, nM) & gt; fexofenadine (K i 10Ã, nM) & gt; terfenadine & gt; loratadine. However, the onset of action varies significantly and clinical efficacy is not always directly related to the potential receptor H 1 .
Pharmacokinetics
Loratadine is administered orally, well absorbed from the gastrointestinal tract, and has a rapid first liver metabolism; it is metabolized by cytochrome P450 isoenzyme systems, including CYP3A4, CYP2D6, and, to a lesser extent, some others. Loratadine is almost entirely (97-99%) bound to plasma proteins. Desloratadine metabolites, which are largely responsible for the antihistaminergic effect, bind to plasma proteins by 73-76%.
The peak effects of Loratadine occur after one to two hours, and the biological half-life averages 8 hours (range 3 to 20 hours) with a half-life of desloratadine is 27 hours (range 9 to 92 hours), calculated for long-term effects. About 40% are excreted as conjugated metabolites into the urine, and the same amount is excreted into the feces. Non-metabolized loratadine traces can be found in the urine.
In structure, it is closely related to tricyclic antidepressants, such as imipramine, and is considerably associated with atypical antipsychotic quetiapine.
History
Schering-Plow developed loratadine as part of a potentially blockbuster drug search: nonsedated antihistamines. However, at the time Schering submitted the drug to the US Food and Drug Administration (FDA) for approval, the agency had approved a competitor's non-combatant antihistamine, terfenadine (trade name Seldane), and, therefore, placed loratadine at a lower priority.
Loratadine was approved by the FDA in 1993. It was available only by prescription in the US until its patent was cut in 2002. It was then approved for over-the-counter sale. After being a drug without a prescription, the price drops significantly.
Schering also developed desloratadine (Clarinex/Aerius), which is an active metabolite of loratadine.
Society and culture
Exceeding counting rule
In 1998, in an unprecedented act, the American insurance company, Anthem, requested the FDA to allow loratadine and two other antihistamines to be made available on the counter (OTC) while it was still under patent; The FDA granted the request, which is not binding on producers. In the US, Schering-Plow made OTC loratadine available in 2002. Since 2015 loratadine is available in many OTC countries.
Brand
In 2017 loratadine is available under many brand names and dosage forms worldwide, including some combination drug formulations with pseudoephedrine, paracetamol, betamethasone, ambroxol, salbutamol, phenylephrine, and dexamethasone.
Marketing
Claritin brand marketing is important in the history of advertising drugs directly to consumers.
The first television commercial for the drug was aired in the US in 1983 by Boots, and sparked controversy. The FDA responds with strong regulation requiring disclosure of side effects and other information. These rules make pharmaceutical manufacturers refuse to spend money on advertising that should highlight the negative aspects.
In the mid-1990s, the marketing team for Claritin at Schering-Plow discovered how to overcome this rule. They create brand awareness ads that never really say what the drug is, but instead show bright images, and voiceover says things like "Finally, the sunny day is here" and "It's time for Claritin" and repeats time telling viewers to "ask your doctor" about Claritin. The first ads managed to make people aware of the brand and improve the recipe, which led Schering-Plow and others to aggressively pursue advertising strategies.
This trend, along with advice from his lawyers who could not win the first amendment case on this issue, caused the FDA to issue new rules for TV commercials in 1997. Instead of entering a "short summary" that takes a full page in a magazine ad and will too long to explain in TV commercials, drug makers are allowed to refer viewers to print ads, 1-800 numbers or websites, and encourage people to talk to their doctors if they want additional information.
Schering-Plow invested $ 322 million in direct-to-consumer Claritin advertising in 1998 and 1999, far more than any other brand. Overall, spending on advertising directly to consumers by the pharmaceutical industry increased from $ 360 million in 1995 to $ 1.3 billion in 1998, and in 2006, was $ 5 billion.
See also
- Benzocycloheptenes
- Desloratadine (loratidine secondary amine)
- Azatadine (loratidine minus the chlorine and esters)
References
External links
- Loratadine - MedlinePlus Drug Information, National US Medical Library, National Institutes of Health
- Description of the drug Claritin (loratadine) - RxList (Internet Drug Index)
- US. National Library of Medicine: Drug Information Portal - Loratadine
Source of the article : Wikipedia
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