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20-September-2008 09:55:56 - Sibutramine Sibutramine Systematic IUPAC name 1-4-chlorophenyl-N,N-dimethyl-a-2-methylpropyl- cyclobutanemethanamine Identifiers CAS number 106650-56-0 ATC code A08AA10 PubChem 5210 DrugBank APRD00456 Chemical data Formula C17H26ClN Mol. mass 279.85 g/mol Pharmacokinetic data Bioavailability Resorption 77%, considerable first-pass metabolism Metabolism Hepatic CYP3A4-mediated Half life sibutramine approx. 1 hour Metabolite 1: 14 hours Metabolite 2: 16 hours Excretion Biliary sibutramine and active metabolites, renal inactive metabolites Therapeutic considerations Pregnancy cat. CAU CUS - no human data existing, inconclusive evidence of teratogenic potential in animal studies Legal status Schedule IVUS Routes Oral Sibutramine trade name Meridia in the USA, Leptos in India, Reductil in Europe and other countries, usually as sibutramide hydrochloride monohydrate, is an orally administered agent for the treatment of obesity, as an appetite suppressant. It is a centrally-acting serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines,1 although its mechanism of action is distinct.2 Sibutramine is manufactured by Abbott Laboratories. It is classified as a Schedule IV controlled substance in the United States. Contents 1 Pharmacokinetics 2 Pharmacodynamics 3 Contraindications 4 Side effects 5 Interactions 6 Dosage 7 Safety concerns 8 References 9 External links Pharmacokinetics Sibutramine is well absorbed from the GI tract 77%, but undergoes considerable first-pass metabolism reducing its bioavailability. The drug itself reaches its peak plasma level after 1 hour and has also a half-life of 1 hour. Sibutramine is metabolized by cytochrome P450 isozyme CYP3A4 resulting in 2 active primary and secondary amines called active metabolites 1 and 2 with half-lives of 14 and 16 hours, respectively. Peak plasma concentrations of active metabolites 1 and 2 are reached after 3 to 4 hours. The following metabolic pathway mainly results in two inactive conjugated and hydroxylated metabolites called metabolites 5 and 6. Metabolites 5 and 6 are mainly excreted in the urine. Pharmacodynamics Sibutramine is a neurotransmitter reuptake inhibitor that reduces the reuptake of serotonin by 53%, norepinephrine by 54%, and dopamine by 16%, thereby increasing the levels of these substances in synaptic clefts and helping enhance satiety; the serotonergic action, in particular, is thought to influence appetite. Older anorectic agents such as amphetamine and fenfluramine force the release of these neurotransmitters rather than affecting their reuptake.2 Despite having a mechanism of action similar to tricyclic antidepressants, sibutramine has failed to demonstrate antidepressant properties in animal studies. It was approved by the U.S. Food and Drug Administration FDA in November 19973 for the treatment of obesity. Contraindications Sibutramine is contraindicated in: Psychiatric conditions as bulimia nervosa, anorexia nervosa, serious depression or preexisting mania Patients with a history of or a predisposition to drug or alcohol abuse Hypersensitivity to the drug Patients below 18 years of age Concomitant treatment with a MAO inhibitor, antidepressant or other centrally active drugs, particularly other anoretics Hypertension that is not sufficiently controlled caution in controlled hypertension Existing pulmonary hypertension Existing damage on heart valves, coronary heart disease, congestive heart failure, serious arrhythmias, previous myocardial infarction Stroke or transient ischemic attack TIA Hyperthyroidism overactive thyroid gland Closed angle glaucoma Seizure disorders Enlargement of the prostate gland with urinary retention relative C.I. Pheochromocytoma Pregnant and lactating women relative C.I. Side effects Frequently encountered side effects are: dry mouth, paradoxically increased appetite, nausea, strange taste in the mouth, upset stomach, constipation, trouble sleeping, dizziness, drowsiness, menstrual cramps/pain, headache, flushing, or joint/muscle pain. Sibutramine can substantially increase blood pressure and pulse in some patients. Therefore all patients treated with sibutramine should have regular monitoring of blood pressure and pulse. The following side effects are infrequent but serious and require immediate medical attention: cardiac arrhythmias, paresthesia, mental/mood changes e.g., excitement, restlessness, confusion, depression, rare thoughts of suicide. Symptoms that require urgent medical attention are seizures, problems urinating, abnormal bruising or bleeding, melena, hematemesis, jaundice, fever and rigors, chest pain, hemiplegia, abnormal vision, dyspnea and edema. Currently, no case of pulmonary hypertension has been noted, although related compounds such as Fen-Phen have shown this rare but clinically significant problem. Interactions Sibutramine has a number of clinically significant interactions. The concomitant use of sibutramine and monoamine oxidase inhibitors MAOIs, such as selegiline is not indicated, as it may increase the risk of serotonin syndrome, a somewhat rare but serious adverse drug reaction.4 Sibutramine should not be taken less than two weeks after stopping or before starting use of an MAOI. Taking both sibutramine and certain medications used in the treatment of migraines-such as ergolines and triptans-, as well as opioids, may also increase the risk for serotonin syndrome, as may the use of more than one serotonin reuptake inhibitor at the same time.4 The concomitant use of sibutramine and drugs which inhibit CYP3A4, such as ketoconazole and erythromycin, may increase plasma levels of sibutramine.5 Sibutramine has no effect on the efficacy of hormonal contraception.4 Dosage 10 mg once daily usually in the morning, if this proves insufficient the dose may be increased to 15 mg daily after 4 weeks. Safety concerns Studies are ongoing into reports of sudden death, heart failure, renal failure and gastrointestinal problems. Despite a petition by Ralph Nader-founded NGO Public Citizen,6 the FDA made no attempts to withdraw the drug, but was part of a Senate hearing in 2005.7 Similarly, Dr. David Graham, FDA whistleblower, testified before a Senate Finance Committee hearing that sibutramine may be more dangerous than the conditions it is used for.8 A large randomized-controlled study with 10,742 patients SCOUT examined whether or not sibutramine reduces the risk for cardiovascular complications in people at high risk for heart disease and concluded that Six-week treatment with sibutramine appears to be efficacious, tolerable and safe in this high-risk population for whom sibutramine is usually contraindicated.9 References ^ New Drugs 2002. Australian Prescriber 25 1: 22. PDF ^ a b Heal DJ, Aspley S, Prow MR, Jackson HC, Martin KF, Cheetham SC 1998. Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes Relat Metab Disord 22 Suppl 1: S18-28; discussion S29. PMID 9758240. ^ U.S. Food and Drug Administration November 24, 1997. FDA APPROVES SIBUTRAMINE TO TREAT OBESITY. Press release. Retrieved on 2007-04-29. ^ a b c Meridia Side Effects, and Drug Interactions. RxList.com 2007. Retrieved on 2007-04-29. ^ Portuguese Cloridrato de sibutramina monoidratado. Bula. Sibutramine hydrochloride monohydrate-label information. Medley 2007. ^ Wolfe, Sidney M.; Larry D. Sasich, Elizabeth Barbehenn March 19, 2002. Petition to FDA to ban the diet drug sibutramine MERIDIA HRG Publication #1613. Public Citizen. Retrieved on 2007-04-29. ^ Bruce Japsen. FDA weighs decision on Meridia ; Health advisory likely for Abbott obesity drug. Chicago Tribune. Chicago, Ill.: Mar 13, 2005. pg. 1. ^ Hearing of 17 November 2004. Related CBS news item 19 November 2004. ^ Torp-Pedersen C, Caterson I, Coutinho W, et al 2007. Cardiovascular responses to weight management and sibutramine in high-risk subjects: an analysis from the SCOUT trial. Eur. Heart J. 28 23: 2915-23. doi:10.1093/eurheartj/ehm217. PMID 17595194. External links Meridia Manufacturer's website RxList v d e Stimulants Alkylamines Cyclopentamine Geranamine Isometheptene Octodrine Propylhexedrine Tuamine Alphapyrrolidinylalkiophenones α-PPP MDPPP MDPV MPBP MPHP MPPP MOPPP Pyrovalerone Cholinergics ABT-089 ABT-418 Anabasine Arecoline Cotinine Cytisine Dianicline Epibatidine Epiboxidine GTS-21 Ispronicline Nicotine Rivanicline Tebanicline Varenicline Convulsants Bicuculline DMCM Gabazine Pentetrazol Picrotoxin Strychnine Thujone Eugeroics Adrafinil Armodafinil Carphedon Modafinil Phenethylamines 4-Bromomethcathinone 4-Fluoroamphetamine 4-Fluoromethamphetamine 4-Fluoromethcathinone 4-Methylmethcathinone 4-MTA Aletamine Amfepentorex Amphechloral Amphetamine Dextroamphetamine, Adderall Amphetaminil Benzphetamine Bupropion Cathinone Chlorphentermine Clenbuterol Clobenzorex Clortermine Diethylpropion Dimethoxyamphetamine Dimethylamphetamine Dimethylcathinone Ephedrine Epinephrine Ethcathinone Ethylamphetamine Fenethylline Fenfluramine Fenproporex Fludorex Furfenorex Levomethamphetamine Lisdexamfetamine MDMA Mefenorex Methamphetamine Methcathinone Methoxyphedrine Methylone Octopamine Ortetamine Parahydroxyamphetamine PCA PIA PMA PMEA PMMA PPAP Phendimetrazine Phenmetrazine Phentermine Phenylephrine Phenylpropanolamine Propylamphetamine Pseudoephedrine Selegiline Synephrine Tiflorex Xylopropamine Phenylaminooxazoles 4-Methyl-aminorex Aminorex Clominorex Fenozolone Fluminorex Pemoline Thozalinone Piperazines 2C-B-BZP BZP GBR-12783 GBR-12935 GBR-13069 GBR-13098 GBR-13119 MeOPP MBZP Vanoxerine Piperidines 2-Benzylpiperidine Desoxypipradrol Diphemethoxidine Ethylphenidate HDMP-28 --Methyl-1-methyl-4β-2-naphthylpiperidine-3β-carboxylate Methylphenidate Dexmethylphenidate Nocaine Phacetoperane Pipradrol Tropanes 3α-Bis-4-fluorophenylmethoxytropane 3α-4-Chlorophenylphenylmethoxytropane 3-Pseudotropyl-4-fluorobenzoate Altropane IACFT Brasofensine CFT WIN 35,428 β-CIT RTI-55 Cocaethylene Cocaine β-CPPIT Dichloropane RTI-111 Difluoropine FE-β-CPPIT FP-β-CPPIT PIT PTT RTI-31 RTI-32 RTI-51 RTI-112 RTI-113 RTI-121 IPCIT RTI-126 RTI-150 RTI-171 RTI-177 RTI-336 Tesofensine Troparil β-CPT, WIN 35,065-2 WF-23 WF-33 WF-60 Xanthines Aminophylline Caffeine Dimethazan Paraxanthine Theobromine Theophylline Others Amineptine Bemegride Benzydamine BPAP Bromantane BTQ Clofenciclan Cypenamine Cyprodenate Diclofensine Dimethocaine Diphenyl prolinol Ethamivan Fencamfamine Feprosidnine Gilutensin GYKI-52895 Hexacyclonate Indanorex Indatraline LR-5182 Mazindol Mesocarb Naphthylisopropylamine Nikethamide Nomifensine Phthalimidopropiophenone Prolintane Sibutramine Yohimbine Zylofuramine See also Sympathomimetic amines v d e Antiobesity preparations A08 -- see also anorectic Centrally acting Phentermine - Fenfluramine - Amfepramone - Dexfenfluramine - Mazindol - Cathine - Clobenzorex - Sibutramine - cannabinoids Rimonabant, Taranabant Peripherally acting Orlistat Retrieved from http://en..org/wiki/Sibutramine Categories: Anorectics | Obesity | Stimulants | Phenethylamines 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 العربية Deutsch Español Français עברית 日本語 Norsk bokmål Polski Português Svenska Türkçe 中文 This page was last modified on 27 July 2008, at 22:00
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