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20-September-2008 09:55:57 - Loratadine Loratadine Systematic IUPAC name Ethyl 4-8-chloro-5,6-dihydro-11H- benzo5,6cyclohepta1,2-bpyridin- 11-ylidine-1-piperidinecarboxylate Identifiers CAS number 79794-75-5 ATC code R06AX13 PubChem 3957 DrugBank APRD00384 Chemical data Formula C22H23ClN2O2 Mol. mass 382.88 g/mol SMILES eMolecules PubChem Pharmacokinetic data Bioavailability N/A due to extensive first-pass metabolism Metabolism hepatic Half life 8 hours metabolites 12-24 hours Excretion 40% as conjugated metabolites into urine similar amount into the feces Therapeutic considerations Pregnancy cat. B1AU BUS Legal status ?CA GSLUK OTCUS Routes oral Loratadine is a drug used to treat allergies, and marketed for its non-sedating properties. It is marketed by Schering-Plough under several trade names such as Claritin, Claritin-D, Claritine, Clarityn, Clarityne or Fristamin depending on the market; by Lek as Lomilan; by Sandoz as Symphoral; by Ranbaxy as Roletra; by Pliva as Rinolan; by Teva as AllergyX; and by Wyeth as Alavert. It is also available as a generic. In a version marketed as Claritin-D or Clarinase, loratadine is combined with pseudoephedrine, a decongestant; this makes it somewhat useful for colds as well as allergies, but adds potential side-effects of insomnia, nervousness and anxiety. Contents 1 Regulation and clinical trials 2 Drug profile 2.1 Forms 2.2 Indications 2.3 Mechanism of action 2.4 Pharmacokinetics 2.5 Side-effects 2.6 Cautions and contradications 3 References 4 External links 5 See also Regulation and clinical trials Schering-Plough developed Loratadine as part of a quest for a blockbuster drug, a nonsedating antihistamine. However, by the time Schering submitted the drug to the FDA for approval, the agency had already approved a competitor's nonsedating antihistamine, Seldane terfenadine, and therefore put Loratadine on a lower priority as a me too drug.1 Trials also raised questions about whether there was any dose at which Loratadine was simultaneously nonsedating and highly effective. Reviewing a randomized, double-blind trial, Dr. Sherwin D. Straus of the FDA argued at one point that 10 milligrams is not very different than placebo clinically, and that the reason for making the dose so low was that at higher, more effective doses, it became sedating.1 Schering counters that The innovation of Claritin and the basis for its success are not only that it works, but also that it was the first antihistamine to provide effective relief of allergy symptoms without sedation and with an impeccable safety profile.1 Loratadine was eventually approved by the FDA, and in 2001, its last year on patent, it accounted for 28% of Schering's total sales. Although an FDA advisory panel ruled that Loratadine was safe enough to be sold over the counter, Schering opposed such a decision on the grounds that it would reduce the price that could be charged for the drug.2 The drug continued to be available only by prescription in the U.S. until it went off patent in 2002. It was then immediately approved for over-the-counter sales. Once it became an unpatented over-the-counter drug, the price dropped precipitously, and insurance companies no longer paid for it. In response, Schering launched an expensive advertising campaign to convince users to switch to Clarinex Desloratadine, which is a metabolized form of Loratadine. A 2003 study comparing the two drugs found that There is no clinical advantage to switching a patient from loratadine to desloratadine. 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.3 In the U.S. and UK, loratadine is the only drug of its class available over the counter though it is no longer the only second generation antihistamine available in this manner. In the UK, larger quantities are only available over the counter; they are P-Line and can only be sold in the presence of a pharmacist. However, packets of up to and including 7 tablets are available off the shelf GSL.Desloratadine is an over the counter drug in Canada, but is a prescription drug in the U.S.. Further information: desloratadine Drug profile Loratadine 10 mg Rx Loratadine 10 mg Rx Forms Loratadine is available as tablets, oral suspension and syrup, and also in combination with pseudoephedrine. Also available are quick-dissolving tablets, which are marketed as being faster to get into one's circulatory system but which require special handling to avoid degrading in the package. Indications Loratadine is indicated for the symptomatic relief of allergy such as hay fever allergic rhinitis, urticaria hives, 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. Mechanism of action Loratadine is a tricyclic antihistamine, which selectively antagonizes peripheral histamine H1-receptors. Histamine is responsible for many features of allergic reactions. Loratadine has a long-lasting effect and does not normally cause drowsiness because it does not readily enter the central nervous system see Side-effects section below. Pharmacokinetics Loratadine is given orally, is well absorbed from the gastrointestinal tract, and 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. Loratadine's peak effect occurs in 1-2 hours, and its biological half-life is on average 8 hours with its metabolite's half-life being 28 hours. About 40% is excreted as conjugated metabolites into the urine, and a similar amount is excreted into the feces. Traces of unmetabolised loratadine can be found in the urine. Side-effects Non-sedating antihistamine As a non-sedating antihistamine, loratadine causes less sedation and psychomotor impairment than the older antihistamines because it penetrates the blood brain barrier only to a slight extent. Although drowsiness is rare, patients should nevertheless be advised that it can occur and may affect performance of skilled tasks e.g. driving; excess alcohol should be avoided. Most common side-effects Drowsiness, headache, psychomotor impairment, and antimuscarinic effects such as urinary retention, dry mouth, blurred vision, and gastrointestinal disturbances are the most common side effects. Other rarer side-effects Hypotension, extrapyramidal effects, dizziness, confusion, depression, sleep disturbances, tremor, convulsions, palpitation, arrhythmias, hypersensitivity reactions including bronchospasm, angioedema, and anaphylaxis, rashes, and photosensitivity reactions, blood disorders, liver dysfunction, and angle-closure glaucoma are less common side effects. Cautions and contradications Loratadine should be used with caution in hepatic disease and dose reduction may be necessary in renal impairment. Caution may be required in epilepsy. Children and the elderly are more susceptible to side-effects see Side-effects section above. Loratadine is a category L-2 classified by the American Academy of Pediatrics as a drug Usually Compatible With Breast-feeding4 and category B in pregnancy5. References ^ a b c The Claritin Effect; Prescription for Profit - New York Times ^ Patents and Prescription Drugs ^ See S 2003. Desloratadine for allergic rhinitis. Am Fam Physician 68 10: 2015-6. PMID 14655812. ^ Transfer of drugs and other chemicals into human milk 2001. Pediatrics 108 3: 776-89. PMID 11533352. ^ STEPS - November 15, 2003 - American Family Physician External links Loratadine - MedlinePlus Drug Information, U.S. National Library of Medicine, National Institutes of Health Claritin loratadine drug description - RxList Internet Drug Index Claritin - patient information leaflet DrugBank: Loratadine - Wishart DS et al., DrugBank: a comprehensive resource for in silico drug discovery and exploration. Nucleic Acids Res. 2006 1;34 The Claritin Effect; Prescription for Profit - a New York Times Magazine article about the marketing of Claritin as a blockbuster drug See also v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratidine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 Burimamide Ciproxifan Clobenpropit Conessine Impentamine Iodophenpropit Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 Retrieved from http://en..org/wiki/Loratadine Categories: H1 receptor antagonists | Carbamates Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Español Français Magyar Nederlands 日本語 Polski Português РуÑ?Ñ?кий СрпÑ?ки / Srpski Svenska ไทย УкраїнÑ?ька This page was last modified on 15 August 2008, at 15:11
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