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News About Doxylamine

20-September-2008 09:55:57 - Doxylamine Doxylamine Systematic IUPAC name N,N-dimethyl-2- 1-phenyl-1-pyridin-2-yl-ethoxy- ethanamine Identifiers CAS number 469-21-6 ATC code R06AA09 PubChem 3162 DrugBank APRD00937 Chemical data Formula C17H22N2O Mol. mass 270.369 g/mol Pharmacokinetic data Bioavailability ? Metabolism Hepatic Half life variable; 6-12 hours Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status OTC Routes Oral Doxylamine succinate is one of the many sedating antihistamines used by itself as a short-term sedative, in combination with other drugs as a night-time cold and allergy relief drug, and a preparation is prescribed in combination with vitamin B6 pyridoxine to prevent morning sickness in pregnant women. Contents 1 Indications 2 Metabolites 3 Formulations 4 Side effects 5 Toxcicity 6 References Indications Doxylamine is a member of the ethanolamine class of antihistamines and has anti-allergy power superior to almost every other antihistamine on the market, with the exception of diphenhydramine Benadryl.1 It is also the most effective over-the-counter sedative available in the United States,2 and is more sedating than some prescription hypnotics. In a study, it was found that doxylamine succinate is possibly more effective than the barbiturate phenobarbital for use as a sedative.3 For this reason, doxylamine has sometimes been used off label in a manner similar to diphenhydramine for the reduction of anxiety symptoms. The dosage required to induce hypnosis sleep can be as low as 6.25 mg, but is usually effective in dosages of up to 25 mg. Higher doses are not recommended by the United States Food and Drug Administration, although single dosage recommendations of up to 50 mg are common in countries like Australia, where it is marketed under the names Restavit and Dozile. Metabolites The 2 main metabolites are desmethyldoxylamine and didesmethyldoxylamine. Formulations It is the sedating ingredient of NyQuil. In Commonwealth countries, such as Australia, Canada, and the United Kingdom, doxylamine is available prepared with paracetamol acetaminophen and codeine under the brand name Dolased , Syndol or Mersyndol, as treatment for tension headache and other types of pain. Doxylamine succinate is used in general over-the-counter sleep-aids branded as Somnil, Dozile, Donormyl, Restavit and Unisom-2. In the United States doxylamine succinate is the active ingredient in the over-the-counter sleep-aid tablets branded as Unisom; however, according to the manufacturer's website, the gel-cap form contains diphenhydramine hydrochloride instead. It is also available in combination with vitamin B6 and folic acid under the brand name Evanorm marketed by Ion Healthcare. In Canada, doxylamine succinate and pyridoxine vitamin B6 are the ingredients of Diclectin, which is used to prevent morning sickness. Side effects Doxylamine succinate is a potent anticholinergic and has a side-effect profile common to such drugs, including dry mouth, ataxia, urinary retention, and drowsiness. Other drugs with well known anticholinergic effects include many antipsychotic and tricyclic antidepressant drugs. Toxcicity Doxylamine succinate is generally safe for administration to healthy adults. Typical preparations that contain Doxylamine range between 6.25mg to 25.0mg. The LD50 is estimated to be between 50-500 mg/kg in humans.4 Symptoms of overdose may include dry mouth, dialated pupils, insomnia, euphoria, hallucinations, and seizures. Fatalities, while rare, have been recorded.5 References ^ DrugBank: DB00366 Doxylamine ^ DrugBank: DB00366 Doxylamine ^ DrugBank: DB00366 Doxylamine ^ http://hazard.com/msds/mf/baker/baker/files/d8882.htm ^ http://www.medsafe.govt.nz/Profs/DataSheet/d/Dozilecap.htm 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/Doxylamine Categories: Antiemetics | Antihistamines 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 ไทย This page was last modified on 7 August 2008, at 21:02

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