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Sibutramine

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	Sibutramine
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	Topics Sibutramine Topic Home 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 obesityObesity Obesity is a condition in which the natural energy reserve, stored in the fatty tissue of humans and mammals, is increased t... , as an appetite suppressant. It is a centrally-acting serotonin-norepinephrine reuptake inhibitorSerotonin-norepinephrine reuptake inhibitor Serotonin-norepinephrine reuptake inhibitors are a class of antidepressant used in the treatment of clinical depression and ... structurallyChemical structure Chemical structure refers to the spatial arrangement of atoms in a molecule and the chemical bonds that hold the atoms toget... related to amphetamineAmphetamine Amphetamine , also known as speed, is a synthetic stimulant used to suppress the appetite, control weight, and treat d... s, although its mechanism of actionMechanism of action In pharmacology, the term mechanism of action refers to the specific biochemical interaction through which a drug substance ... is distinct. Sibutramine is manufactured by Abbott LaboratoriesAbbott Laboratories Abbott Laboratories is a diversified pharmaceuticals and health care company.... . It is classified as a Schedule IVControlled Substances Act The Controlled Substances Act was enacted into law by the Congress of the United States as Title II of the Comprehensive Dr... controlled substance in the United StatesUnited States The United States of America, also known as the United States, the U.S., the U.S.A., and America, is... . Pharmacokinetics Sibutramine is well absorbed from the GI tractGastrointestinal tract The gastrointestinal tract or digestive tract, also referred to as the GI tract or the alimentary canal, o... (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 P450Cytochrome P450 oxidase Cytochrome P450 oxidase is a generic term for a large number of related, but distinct, oxidative enzymes important in animal... isozymeIsozyme Isozymes are enzymes that differ in amino acid sequence but catalyze the same chemical reaction.... CYP3A4CYP3A4 Cytochrome P450 3A4, a member of the cytochrome P450 mixed-function oxidase system, is arguably the most important enzyme in... resulting in 2 active primary and secondary amines (called active metabolites 1 and 2) with half-lives of 14 and 16 hours, respectively. Peak plasmaBlood plasma Blood plasma is the liquid component of blood, in which the blood cells are suspended.... 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 inhibitorNeurotransmitter uptake inhibitor A neurotransmitter uptake inhibitor is a drug which inhibits the reuptake of the neurotransmitter, thus extending the durati... that reduces the reuptake of serotoninSerotonin Serotonin is a monoamine neurotransmitter synthesized in serotonergic neurons in the central nervous system and enterochro... (by 53%), norepinephrineNorepinephrine Norepinephrine or noradrenaline is a catecholamine and a phenethylamine with chemical formula C8H11NO3.... (by 54%), and dopamineDopamine Dopamine is a chemical naturally produced in the body.... (by 16%), thereby increasing the levels of these substances in synaptic clefts and helping enhance ; the serotonergic action, in particular, is thought to influence appetite. Older anorecticAnorectic Anorectics, anorexigenics or appetite suppressants are drugs that reduce the desire to eat.... agents such as amphetamineAmphetamine Amphetamine , also known as speed, is a synthetic stimulant used to suppress the appetite, control weight, and treat d... and fenfluramineFenfluramine Overview Fenfluramine is a drug that was part of the Fen-Phen anti-obesity medication.... force the release of these neurotransmitters rather than affecting their reuptake. Despite having a mechanism of action similar to tricyclic antidepressantFacts About Tricyclic antidepressant Tricyclic antidepressants are a class of antidepressant drugs first used in the 1950s.... s, sibutramine has failed to demonstrate antidepressantAntidepressant An antidepressant is a medication designed to treat or alleviate the symptoms of clinical depression.... properties in animal studies. It was approved by the U.S. Food and Drug AdministrationFood and Drug Administration The Food and Drug Administration is an agency of the United States Department of Health and Human Services and is responsib... (FDA) in November 1997 for the treatment of obesity. Contraindications Sibutramine is contraindicated in: Psychiatric conditions as bulimia nervosaBulimia nervosa Summary Bulimia nervosa, more commonly known as bulimia, is an eating disorder.... , anorexia nervosaAnorexia nervosa Anorexia nervosa is a psychiatric diagnosis that describes an eating disorder characterized by low body weight and body imag... , serious depressionClinical depression Clinical depression is a state of sadness, melancholia or despair that has advanced to the point of being disruptive to an i... or preexisting maniaMania Mania is a medical condition characterised by severely elevated mood.... Patients with a history of or a predisposition to drug or alcohol abuse HypersensitivityHypersensitivity Overview Hypersensitivity is an immune response that damages the body's own tissues.... to the drug Patients below 18 years of age Concomitant treatment with a MAO inhibitor, antidepressantAntidepressant An antidepressant is a medication designed to treat or alleviate the symptoms of clinical depression.... or other centrallyCentral nervous system The central nervous system represents the largest part of the nervous system, including the brain and the spinal cord.... active drugs, particularly other anoretics HypertensionHypertension Hypertension or high blood pressure is a medical condition where the blood pressure is chronically elevated.... that is not sufficiently controlled (caution in controlled hypertension) Existing pulmonary hypertensionPulmonary hypertension Overview In medicine, pulmonary hypertension is an increase in blood pressure in the pulmonary artery or lung vasculature.... Existing damage on heart valves, coronary heart disease, congestive heart failure, serious arrhythmias, previous myocardial infarction StrokeStroke A stroke, also known as cerebrovascular accident, is an acute neurologic injury in which the blood supply to a part of... or transient ischemic attackTransient ischemic attack A transient ischemic attack is caused by the temporary disturbance of blood supply to a restricted area of the brain, resul... (TIA) HyperthyroidismHyperthyroidism Hyperthyroidism is the clinical syndrome caused by an excess of circulating free thyroxine or free triiodothyronine , or b... (overactive thyroid gland) Closed angle glaucomaGlaucoma Glaucoma is a group of diseases of the optic nerve involving loss of retinal ganglion cells in a characteristic pattern of o... SeizureSeizure Seizures are temporary abnormal electrophysiologic phenomena of the brain, resulting in abnormal synchronization of electri... disorders Enlargement of the prostateFacts About Prostate The prostate is an exocrine gland of the male mammalian reproductive system.... gland with urinary retentionUrinary retention Urinary retention also known as ischuria is a lack of ability to urinate.... (relative C.I.) PheochromocytomaPheochromocytoma A pheochromocytoma is a neuroendocrine tumor of the medulla of the adrenal glands originating in the chromaffin cells, whic... PregnantPregnancy Pregnancy is the carrying of one or more embryos or fetuses by female mammals, including humans, inside their bodies.... and lactatingBreastfeeding Breastfeeding is the process of a woman feeding an infant or young child with milk from her breasts, usually directly from t... women (relative C.I.) Side effects Frequently encountered side effectAdverse drug reaction An adverse drug reaction is a term to describe the unwanted, negative consequences sometimes associated with the use of medi... s are: dry mouth, paradoxically increased appetite, nauseaNausea Nausea is the sensation of unease and discomfort in the stomach with an urge to vomit. ... , strange taste in the mouthDysgeusia Dysgeusia is the distortion or decrease of the sense of taste.... , anorgasmiaAnorgasmia Anorgasmia is a form of sexual dysfunction, sometimes classified as a psychiatric disorder, where the patient cannot achieve... and delayed ejaculationDelayed ejaculation Delayed ejaculation, also known as retarded ejaculation, is a form of sexual dysfunction in men, characterised by the ma... , upset stomach, constipation, trouble sleeping, dizziness, drowsiness, menstrual cramps/pain, headache, flushing, or joint/muscle pain. Sibutramine can substantially increase blood pressureBlood pressure Blood pressure is the pressure exerted by the blood on the walls of the blood vessels.... 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 arrhythmiaCardiac arrhythmia Cardiac arrhythmia is a group of conditions in which the muscle contraction of the heart is irregular or is faster or slower... s, paresthesiaParesthesia Summary Paresthesia or paraesthesia is a sensation of tingling, pricking, or numbness of a person's skin with no apparent long... , mental/mood changes (e.g., excitement, restlessness, confusion, depression, rare thoughts of suicideSuicide Suicide is the act of willfully ending one's own life.... ). Symptoms that require urgent medical attention are seizureSeizure Seizures are temporary abnormal electrophysiologic phenomena of the brain, resulting in abnormal synchronization of electri... s, problems urinating, abnormal bruising or bleeding, melenaMelena Summary In medicine, melena or melaena refers to the black, "tarry" feces that are associated with gastrointestinal hemorrhage.... , hematemesisHematemesis Hematemesis or haematemesis is the vomiting of fresh red blood.... , jaundiceJaundice Jaundice, also known as icterus , is a yellowing of the skin, sclera and mucous membranes caused by increased levels ... , feverFever Overview Fever is a frequent medical symptom that describes an increase in internal body temperature to levels that are above normal... and rigorRigor (medicine) Rigor or chills is shaking occurring during a high fever.... s, chest painChest pain In medicine, chest pain is a symptom of a number of serious conditions and is generally considered a medical emergency, unle... , hemiplegiaHemiplegia Hemiplegia is a condition where a vertical half of a patient's body is weak or paralyzed, i.e.... , abnormal vision, dyspneaDyspnea Dyspnea or shortness of breath is perceived difficulty breathing or pain on breathing.... and edemaEdema Edema or oedema, formerly known as dropsy or hydropsy, is swelling of any organ or tissue due to accumulat... . Currently, no case of pulmonary hypertensionPulmonary hypertension In medicine, pulmonary hypertension is an increase in blood pressure in the pulmonary artery or lung vasculature.... has been noted, although related compounds (such as Fen-PhenFen-phen Fen-phen was an anti-obesity medication which consisted of two drugs: fenfluramine and phentermine.... ) 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 inhibitorMonoamine oxidase inhibitor Monoamine oxidase inhibitors are a class of antidepressant drugs prescribed for the treatment of depression.... s (MAOIs, such as selegilineFacts About Selegiline Selegiline is a drug used for the treatment of early-stage Parkinson's disease and senile dementia.... ) is not indicated, as it may increase the risk of serotonin syndromeSerotonin syndrome Serotonin toxicity is an iatrogenic toxidrome.... , a somewhat rare but serious adverse drug reactionAdverse drug reaction An adverse drug reaction is a term to describe the unwanted, negative consequences sometimes associated with the use of medi... . 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 migraineMigraine Overview Migraine is a painful neurological condition, of which the most common symptom is an intense and disabling episodic headache... s—such as ergolineErgoline Ergoline is a chemical compound whose structural skeleton is contained in a diverse range of alkaloids and a few psychedelic... s and triptanTriptan Triptans are a family of tryptamine drugs used as abortive medication in the treatment of migraine and cluster headaches.... s—, as well as opioidOpioid An opioid is any agent that binds to opioid receptors, found principally in the central nervous system and gastrointestinal ... s, may also increase the risk for serotonin syndrome, as may the use of more than one serotonin reuptake inhibitor at the same time. The concomitant use of sibutramine and drugs which inhibit CYP3A4CYP3A4 Cytochrome P450 3A4, a member of the cytochrome P450 mixed-function oxidase system, is arguably the most important enzyme in... , such as ketoconazoleKetoconazole Ketoconazole is a synthetic antifungal drug used to prevent and treat skin and fungal infections, especially in immunocompro... and erythromycinErythromycin Erythromycin is a macrolide antibiotic which has an antimicrobial spectrum similar to or slightly wider than that of penicil... , may increase plasma levels of sibutramine. Sibutramine has no effect on the efficacy of hormonal contraceptionHormonal contraception Hormonal contraception refers to birth control methods that act on the hormonal system.... . 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 failureRenal failure Overview Renal failure is the condition where the kidneys fail to function properly.... and gastrointestinal problems. Despite a petition by Ralph NaderRalph Nader Ralph Nader is an American attorney and political activist.... -founded NGO Public CitizenPublic Citizen Overview * Consumer Project on Technology* Global Trade Watch... , the FDA made no attempts to withdraw the drug, but was part of a Senate hearing in 2005. Similarly, Dr. David GrahamDavid Graham (whistleblower) Dr. David Graham is an Associate Director at the Food and Drug Administration's Office of Drug Safety.... , FDA "whistleblower", testified before a Senate Finance Committee hearing that sibutramine may be more dangerous than the conditions it is used for. 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." External links (Manufacturer's website)