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Loratadine, sold under the brand name Claritin among others, is a medication used to treat allergies.
Common side effects include sleepiness, dry mouth, and headache.
Loratadine was discovered in 1981 and came to market in 1993.
1 Medical uses
3 Adverse effects
5.1 Mechanism of action
7 Society and culture
7.1 Over-the-counter regulation
8 See also
10 External links
Loratadine is indicated for the symptomatic relief of allergy such as hay fever (allergic rhinitis), urticaria (hives), chronic idiopathic urticaria, For allergic rhinitis, loratadine is effective for both nasal and eye symptoms – sneezing, runny nose, and itchy or burning eyes.
Similarly to cetirizine, loratadine attenuates the itching associated with Kimura’s disease.
An example of a loratadine 10-mg tablet (Rx)
The drug is available in many different forms, including tablets, oral suspension, and syrup, Also available are quick-dissolving tablets, which are marketed as being faster to get into one’s circulatory system, but require special handling to avoid degrading in the package.
Patients with severe hepatic (liver) disorders may need to start with a lower dose. No dose adaptation is necessary for elderly or renally (kidney) impaired patients.
Loratadine is usually compatible with breast feeding (classified category L-2 by the American Academy of Pediatrics ).
As a “nonsedating” antihistamine, loratadine causes less (but still significant, in some cases) sedation and psychomotor retardation than the older antihistamines because it penetrates the blood/brain barrier to a smaller extent.
Other possible side effects include headache and antimuscarinic effects such as urinary retention, dry mouth, blurred vision, and gastrointestinal problems.
Substances that act as inhibitors of the CYP3A4 enzyme such as ketoconazole, erythromycin, cimetidine, and furanocoumarin derivatives (found in grapefruit) lead to increased plasma levels of loratadine — that is, more of the drug was present in the bloodstream than typical for a dose. This had clinically significant effects in controlled trials of higher-than-usual doses of loratadine (20 mg).
Antihistamines should be discontinued about 48 hr prior to skin allergy tests, since these drugs may prevent or diminish otherwise-positive reactions to dermal activity indicators.
Mechanism of action
Loratadine is a tricyclic antihistamine, which acts as a selective inverse agonist of peripheral histamine H 1 receptors.
Loratadine is given orally, is well absorbed from the gastrointestinal tract, and has rapid first-pass hepatic metabolism ; it is metabolized by isoenzymes of the cytochrome P450 system, including CYP3A4, CYP2D6, and, to a lesser extent, several others.
Loratadine’s peak effect occurs after 1-2 hours, and its biological half life is on average 8 hours (range 3 to 20 hours) with desloratadine ‘s half-life being 27 hours (range 9 to 92 hours), accounting for its long-lasting effect.
In structure, it is closely related to tricyclic antidepressants, such as imipramine, and is distantly related to the atypical antipsychotic quetiapine.
Schering-Plough developed loratadine as part of a quest for a potential blockbuster drug : a nonsedating antihistamine. However, by the time Schering submitted the drug to the U.S. Food and Drug Administration (FDA) for approval, the agency had already approved a competitor’s nonsedating antihistamine, terfenadine (trade name Seldane), and, therefore, put loratadine on a lower priority.
Loratadine was approved by the FDA in 1993. It was then subsequently approved for over-the-counter sales. Once it became an unpatented over-the-counter drug, the price dropped significantly.
Schering also developed desloratadine (Clarinex/Aerius), which is an active metabolite of loratadine.
Society and culture
In 1998, in an unprecedented action, the American insurance company Anthem petitioned the FDA to allow loratadine and two other antihistamines to be made available over the counter (OTC) while it was still under patent; the FDA granted the request, which was not binding on manufacturers.
As of 2017, loratadine was available under many brand names and dosage forms worldwide, including several combination drug formulations with pseudoephedrine, paracetamol, betamethasone, ambroxol, salbutamol, phenylephrine, and dexamethasone.
Listing of brands
As of 2017 brands included: Actalor, Actidin, Aerotina, Alaspan, Alavert, Albatrina, Alerdina, Alerfast, Alergan, Alergiano, Alergiatadina, Alergin Ariston, Alergipan, Alergit, Alergitrat L, Aleric Lora, Alermuc, Alernitis, Alerpriv, Alertadin, Alertine, Aleze, Algac, Algecare, Algistop, Alledryl, Aller-Tab, Allerfre, Allerget, Allergex Non Drowsy, Allergyx, Allerhis, Allernon, Allerta, Allertyn, Allohex, Allor, Allorat, Alloris, Alor, Analor, Anhissen, Anti-Sneeze, Antial, Antil, Antimin, Ao Hui Feng, Ao Mi Xin, Ao Shu, Ardin, Atinac, Avotyne, Axcel Loratadine, Bai Wei Le, Bang Nuo, Bedix, Belodin, Benadryl, Besumin, Bi Sai Ning, Bi Yan Tong, Biliranin, Biloina, Biolorat, Bollinol, Boots Hayfever Relief, Boots Hooikoortstabletten, Boots Once-a-Day Allergy Relief, Carin, Carinose, Chang Ke, Civeran, Clara, Claratyne, Clarid, Clarihis, Clarihist, Clarilerg, Clarinese, Claritin, Claritine, Clarityne, Clarityne SP, Clarotadine, Clatatin, Clatine, Clear-Atadine, Clear-Atadine Children’s, Clistin, Contral, Cronitin, Da Sheng Rui Li, Dao Min Qi, Dayhist, Debimin, Desa, Devedryl, Dexitis, Dimegan, Dimens, Dimetapp Children’s ND Non-Drowsy Allergy, Doliallérgie Loratadine, Effectine, Eladin, Elo, Emilora, Encilor, Eradex, Erolin, Ezede, Fei Ge Man, Finska, Flonidan, Flonidan Control, Florgan, Folerin, Frenaler, Fristamin, Fu Lai Xi, Fucole Minlife, Genadine, Glodin, Gradine, Halodin, Helporigin, Hisplex, Histaclar, Histafax, Histalor, Horestyl, Hua Chang, Hysticlar, Igir, Immunix, Immunex, Inclarin, Inversyn, Jin Su Rui, Jing Wei, Ke Mi, Klarihist, Klinset, Klodin, Kui Yin, Lallergy, Larotin, Latoren, Laura, LD, Lei Ning, Lesidas, Liberec, Lisaler, Logadine, Logista, Lohist, Lolergi, Lolergy, Lomidine, Lomilan, Loptame, Lora, Lora-Lich, Lora-Mepha Allergie, Loracare, Loracil, Loraclear, Loradad, Loraderm, Loradin, Loradine, Lorado Pollen, Loradon, Lorafix, Lorahexal, Lorahist, Lorakids, Loralab-D, Loralerg, Loralivio, Loramax, Loramin, Loramine, Loran, Lorange, Loranil, Lorano, Loranox, Lorantis, LoraPaed, Lorastad, Lorastamin, Lorastine, Lorastyne, Lorat, Loratab, Loratadim, Loratadin, Loratadina, Loratadine, Loratadinum, Loratadyna, Loratan, Loratin, Loraton, Loratrim, Loratyne, Lorchimin, Lordamin, Lordinex, Loremex, Loremix, Lorfast, Lorid, Loridin, Lorihis, Lorimox, Lorin, Lorine, Loristal, Lorita, Loritex, Loritin, Lorly, Lormeg, Lorsedin, Lortadine, Losta, Lostop, Lotadin, Lotadine, Lotarin, Lotin, Megalorat, Mildin, Min Li Ke, Minlife, Mintapp, Mosedin, Mudantil L, Nasaler, Neoday, Niltro, Non-Drowsy Allergy Relief, Nosedin, Noseling, Novacloxab, NT-Alergi, Nufalora, Nularef, Numark Allergy, Omega, Oradin, Oradine, Oramine, Orin, Orinil, Pollentyme, Pressing, Pretin, Primorix, Profadine, Pulmosan Aller, Pylor, Rahistin, Ralinet, Ramitin, Refenax, Restamine, Rhinigine, Rihest, Rinalor, Rinconad, Rinityn, Rinolan, Riprazo, Rityne, Roletra, Rotadin, Rui Fu, Run Lai, Rupton, Sensibit, She Tai, Shi Nuo Min, Shi Tai Shu, Shu Rui, Shun Ta Xin, Silora, Sinaler, Sohotin, Soneryl, Sunadine, Symphoral, Tabcin, Tai Ming Ke, Ticevis, Tidilor, Tinnic, Tirlor, Toral, Triaminic, Tricel, Tuulix, Urtilar, Utel, Vagran, Winatin, Xanidine, Xepalodin, Xian Ning, Xin Da Yue, Xing Yuan Jia, XSM, Xue Fei, Yi Fei, Yi Shu Chang, Yibang, Zhengshu, Zhi Min, Zifar, Zoratadine, and Zylohist.
As of 2017, in a combination drug with pseudoephedrine, it was available under the brands: Airet, Alavert D-12, Aldisa SR, Alerfast D, Alergical LP, Alergin Plus Ariston, Alerpriv D, Alledryl-D, Allerpid, Aseptobron Descongestivo, Bai Wei Qing, Benadryl 24 D, Ciprocort D, Claridex, Claridon, Clarinase, Clarinase Repetab, Claritine Active, Claritin Allergy + Sinus, Clarityne, Clarityne D, Clarityne-D, Clear-Atadine, Coderin, Cronase, De-Cold, Decidex Plus, Decongess I, Defonase, Demazin NS, Dimegan-D, Effectine D, Ephedrol, Fedyclar, Finska-LP, Frenaler-D, Hui Fei Shun, Ke Shuai, Claritin-D, Larotin D, Lertamine, Lohist-Extra, Lora Plus, Loralerg D, Loranil-D, Loratin D, Loratin Plus, Lordinex D, Loremix D, Lorexin-D, Lorfast-D, Loridin-D, Lorinase, Minlife -P, Mosedin plus sr, Narine Repetabs, Nasaler Plus, Nularef-D, Oradin Plus, Pretin-D, Primorix-D, Rhinos SR, QiKe, Rinomex, Sinaler D, Sudamin, Sudolor, Tricel-D, Zhuang Qi, Zoman-D, and Zoratadine-P.
As of 2017, in a combination drug with paracetamol, it was available as Sensibit D and in combination with paracetamol and pseudoephedrine, it was available as: Atshi, Clariflu, and Trimed Flu.
As of 2017, in a combination drug with betamethasone, it was available as Celestamincort, Celestamine NF, Celestamine NS, Celestamine* L, Ciprocort L, Claricort, Clarityne cort, Corticas L, Cortistamin-L, Histafax Compuesto, Histamino Corteroid L, Labsalerg-B, Lisaler Beta, and Sinaler B, and in combination with betamethadol with available as Nularef Cort.
As of 2017, in a combination drug with ambroxol, it was available as Aliviatos, Ambroclar, Antitusivo L Labsa, Bronar, Broncovital, Broquixol, Clarixol, Ideobron, Lorabrox, Lorfast-AM, Sensibit XP, and Toraxan, and in a combination drug with ambroxol and salbutamol as Sibilex.
As of 2017, in a combination drug with phenylephrine, it was available as Bramin-Flu, Clarityne D, Clarityne Plus, Clarityne-D, Histafax D, Brafelix, Loramine R, Loraped, Maxiclear Cold & Nasal, Maxiclear Hayfever & Sinus Relief, and Rinavent, and in combination with phenylephrine and paracetamol it was available as Sensibit D NF.
As of 2017, in a combination drug with dexamethasone it was available as Alerfast Forte and Frenaler Forte.
The marketing of the Claritin brand is important in the history of direct-to-consumer advertising of drugs.
The first television commercial for a drug was aired in the US in 1983 by Boots, and sparked controversy. The FDA responded with strong regulation requiring disclosure of side effects and other information. These rules made pharmaceutical manufacturers balk at spending money on ads that had to highlight negative aspects.
In the mid-1990s, the marketing team for Claritin at Schering-Plough found a way around these rules. They created brand awareness commercials that never actually said what the drug was for, but instead showed sunny images, and the voiceover said things like “At last, a clear day is here” and “It’s time for Claritin” and repeatedly told viewers to “ask your doctor” about Claritin.
This trend, along with advice from its attorneys that it could not win a first amendment case on the issue, led the FDA to issue new rules for TV commercials in 1997.
Schering-Plough invested $322 million in Claritin direct-to-consumer advertising in 1998 and 1999, far more than any other brand.
Azatadine (loratidine minus chlorine atom and ester)
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