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Meridia: profile and news
S&P 500 February Winners & Losers Mar 1, 2006 Doctor censured for fatal mistake Feb 20, 2006 Manitoba doctor censured for prescribing pain-relief patch that ... Feb 21, 2006 Rescuers detect sounds underneath mud slide Feb 20, 2006 Police investigate narcotics theft Mar 3, 2006 Risk of Overdose Deaths Linked to Fentanyl Pain Patch Under ... Feb 15, 2006 FDA OKs skin patch to treat depression Feb 28, 2006 Oakmont doctor appealing drugs-for-sex conviction Mar 2, 2006 Stonewall woman accused of providing drugs that led to man's death Feb 24, 2006 Two face charges they stole narcotics Feb 22, 2006 Doctor denies drug, fraud allegations Feb 24, 2006 Mylan posts higher profit Feb 2, 2006 Mylan stock up on strong results, upgrade Feb 3, 2006 Buy J&J and Avoid the Winner's Curse Feb 6, 2006 UPDATE 1-Mylan posts higher profit, helped by pain patch Feb 2, 2006 Mylan posts higher profit Feb 2, 2006 Overdose Deaths Linked to Fentanyl Pain Patch Being Investigated ... Feb 1, 2006 Buy J&J and Avoid the Winner's Curse Feb 6, 2006 JJ Chief Expects Threat From Generic Drug Rivals Jan 24, 2006 Europe Clears J&J Pain Patch Jan 30, 2006 Profits up, but sales down at J&J in 4Q Jan 25, 2006 J&J posts quarterly profit, but sales fall Jan 24, 2006 J&J posts unexpected sales dip, shares fall Jan 24, 2006 UPDATE 1-Mylan posts higher profit, helped by pain patch Feb 2, 2006 Mylan stock up on strong results, upgrade Feb 3, 2006 J&J posts quarterly profit, helped by devices Jan 24, 2006 J&J Reports Higher Profit, Matches Expectations Jan 24, 2006 J&J reports higher 4Q profit Jan 24, 2006 Devices sales boost J&J profits Jan 24, 2006 JJ Plans to Take Pass on Guidant Jan 24, 2006 J&J's revenues drop; Guidant deadline looms Jan 24, 2006 J&J profit soars 79 pct., despite a dip in revenue Jan 25, 2006 Johnson & Johnson Reports Full-Year and Fourth-Quarter 2005 ... Jan 24, 2006 Top Worldwide Jan 24, 2006 J&J Sales Come in Light Jan 24, 2006 UPDATE: J&J Meets 4th-quarter Profit Target, Misses On Revenue Jan 24, 2006 Johnson & Johnson: Fourth Quarter and Year End 2005 Financial ... Jan 24, 2006 Other information Indication For the treatment of obesity Pharmacology Sibutramine is an orally administered agent for the treatment of obesity. Sibutramine exerts its pharmacological actions predominantly via its secondary (M1) and primary (M2) amine metabolites. The parent compound, sibutramine, is a potent inhibitor of serotonin and norepinephrine reuptake in vivo, but not in vitro. However, metabolites M1 and M2 inhibit the reuptake of these neurotransmitters both in vitro and in vivo. In human brain tissue, M1 and M2 also inhibit dopamine reuptake in vitro, but with ~3-fold lower potency than for the reuptake inhibition of serotonin or norepinephrine. Sibutramine, M1 and M2 exhibit no evidence of anticholinergic or antihistaminergic actions. In addition, receptor binding profiles show that sibutramine, M1 and M2 have low affinity for serotonin (5-HT1, 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C), norepinephrine (b, b1, b3, a1 and a2), dopamine (D1 and D2), benzodiazepine, and glutamate (NMDA) receptors. These compounds also lack monoamine oxidase inhibitory activity in vitro and in vivo. Mechanism Of Action Sibutramine produces its therapeutic effects by norepinephrine (NE), serotonin reuptake (5-hydroxytryptamine, 5-HT) and dopamine reuptake inhibition. Sibutramine and its major pharmacologically active metabolites (M1 and M2) do not act via release of monoamines. Drug Category Appetite Depressants; Antidepressants; Anorexigenic Agents; Stimulants; ATC:A08AA10 Brand Names/Synonyms Reductil; Medaria; Sibutraminum [Latin]; Sibutramina [Spanish]; Cyclobutanemethanamine, 1-(4-chlorophenyl)-N,N-dimethyl-alpha-(2-methylpropyl)-; Meridia; Medaria Dosage Forms CAPSULE Absorption Rapid absorption following oral administration. Absolute bioavailability is not know, but at least 77% of a single oral dose of sibutramine is absorbed. Interactions Interactions for Sibutramine: CNS Active Drugs The use of Sibutramine in combination with other CNS-active drugs, particularly serotonergic agents, has not been systematically evaluated. Consequently, caution is advised if the concomitant administration of Sibutramine with other centrally-acting drugs is indicated. In patients receiving monoamine oxidase inhibitors (MAOIs) (e.g., phenelzine, selegiline) in combination with serotonergic agents (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline, venlafaxine), there have been reports of serious, sometimes fatal, reactions ("serotonin syndrome;" see below). Because Sibutramine inhibits serotonin reuptake, Sibutramine should not be used concomitantly with a MAOI. At least 2 weeks should elapse between discontinuation of a MAOI and initiation of treatment with Sibutramine. Similarly, at least 2 weeks should elapse between discontinuation of Sibutramine and initiation of treatment with a MAOI. The rare, but serious, constellation of symptoms termed "serotonin syndrome" has also been reported with the concomitant use of selective serotonin reuptake inhibitors and agents for migraine therapy, such as Imitrex (sumatriptan succinate) and dihydroergotamine, certain opioids, such as dextromethorphan, meperidine, pentazocine and fentanyl, lithium, or tryptophan. Serotonin syndrome has also been reported with the concomitant use of two serotonin reuptake inhibitors. The syndrome requires immediate medical attention and may include one or more of the following symptoms: excitement, hypomania, restlessness, loss of consciousness, confusion, disorientation, anxiety, agitation, motor weakness, myoclonus, tremor, hemiballismus, hyperreflexia, ataxia, dysarthria, incoordination, hyperthermia, shivering, pupillary dilation, diaphoresis, emesis, and tachycardia. Because Sibutramine inhibits serotonin reuptake, in general, it should not be administered with other serotonergic agents such as those listed above. However, if such a combination is clinically indicated, appropriate observation of the patient is warranted. Drugs That May Raise Blood Pressure and/or Heart Rate: Concomitant use of Sibutramine and other agents that may raise blood pressure or heart rate have not been evaluated. These include certain decongestants, cough, cold, and allergy medications that contain agents such as ephedrine, or pseudoephedrine. Caution should be used when prescribing Sibutramine to patients who use these medications. Drugs That Inhibit Cytochrome P450(3A4) Metabolism: In vitro studies indicated that the cytochrome P450(3A4)-mediated metabolism of sibutramine was inhibited by ketoconazole and to a lesser extent by erythromycin. Clinical interaction trials were conducted on these substrates. The potential for such interactions is described below. Ketoconazole: Concomitant administration of 200 mg doses of ketoconazole twice daily and 20 mg sibutramine once daily for 7 days in 12 uncomplicated obese subjects resulted in moderate increases in AUC and Cmax of 58% and 36% for M1 and of 20% and 19% for M2, respectively. Erythromycin: The steady-state pharmacokinetics of sibutramine and metabolites M1 and M2 were evaluated in 12 uncomplicated obese subjects following concomitant administration of 500 mg of erythromycin three times daily and 20 mg of sibutramine once daily for 7 days. Concomitant erythromycin resulted in small increases in the AUC (less than 14%) for M1 and M2. A small reduction in Cmax for M1 (11%) and a slight increase in Cmax for M2 (10%) were observed. Cimetidine: Concomitant administration of cimetidine 400 mg twice daily and sibutramine 15 mg once daily for 7 days in 12 volunteers resulted in small increases in combined (M1 and M2) plasma Cmax (3.4%) and AUC (7.3%); these differences are unlikely to be of clinical significance. Alcohol: In a double-blind, placebo-controlled, crossover study in 19 volunteers, administration of a single dose of ethanol (0.5 mL/kg) together with 20 mg of sibutramine resulted in no psychomotor interactions of clinical significance between alcohol and sibutramine. However, the concomitant use of Sibutramine and excess alcohol is not recommended. Oral Contraceptives: The suppression of ovulation by oral contraceptives was not inhibited by Sibutramine. In a crossover study, 12 healthy female volunteers on oral steroid contraceptives received placebo in one period and 15 mg sibutramine in another period over the course of 8 weeks. No clinically significant systemic interaction was observed; therefore, no requirement for alternative contraceptive precautions are needed when patients taking oral contraceptives are concurrently prescribed sibutramine. Drugs Highly Bound to Plasma Proteins: Although sibutramine and its active metabolites M1 and M2 are extensively bound to plasma proteins (94%), the low therapeutic concentrations and basic characteristics of these compounds make them unlikely to result in clinically significant protein binding interactions with other highly protein bound drugs such as warfarin and phenytoin. In vitro protein binding interaction studies have not been conducted. Chemical IUPAC Name 1-[1-(4-chlorophenyl)cyclobutyl]-N,N,3-trimethyl-butan-1-amine Chemical Formula C17H26ClN Half Life 1.1 hours Drug Type Approved Drug # Accession No APRD00456 CAS Registry Number 106650-56-0 |
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