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ClozapineThis page contains recent news articles, when available, and an overview of Clozapine but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.Overview: Clozapine (when available) Clozapine is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Clozapine is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Clozapine acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Clozapine. Clozapine's antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects. Clozapine's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Clozapine's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug. For the management of severely ill schizophrenic patients who fail to respond adequately to standard drug treatment for schizophrenia Mechanism Of Action: The mechanism of action of Clozapine, as with other drugs used to treat schizophrenia, is unknown. However, it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of dopamine Type 2 (D2) and serotonin Type 2 (5HT2) receptor antagonism. News Articles on Clozapine Old Schizophrenia Drug Fights Violence as Effectively as Second ... - Jul 1, 2008 But Dr. Swartz and colleagues noted that some of those studies had included the second-generation drug clozapine (Clozaril) and the older antipsychotic MedPage Today, Aripiprazole may enhance clozapine treatment of schizophrenia - Jun 25, 2008 NEW YORK (Reuters Health) - Although aripiprazole augmentation of clozapine therapy in schizophrenic patients does not lead to a significant overall Therapeutics Daily (subscription) (press release), Experts Analyze Real Meaning of CATIE Study Findings - Jun 6, 2008 So when results showed that, with the exception of clozapine, SGAs had only marginal superiority over perphenazine, the response from quarters with vested Psychiatric News, Newer antipsychotics have lower diabetes risk - Jun 20, 2008 Increased risk varied, from a non-significant 16% with risperidone up to 39% with clozapine, with a high degree of heterogeneity between studies. Pulse, People With Dementia Should Avoid Certain Drugs - Jun 27, 2008 Antipsychotics, such as Chlorpromazine (Thorazine), Clozapine (Clozaril), Mesoridazine (Serentil), Pimozide (Orap), Promazine (Sparine), RedOrbit, ADA: Metabolic Monitoring Guidelines for Antipsychotics Largely ... - Jun 10, 2008 Her study included 18176 adults initiating aripiprazole (Abilify), clozapine (Clozaril, FazaClo), olanzapine (Zyprexa, Zydis), quetiapine (Seroquel), MedPage Today, Pharmacologic Options for Treatment-Resistant Depression: Charles ... - Jun 9, 2008 ...[15] No controlled trial data exist for ziprasidone or clozapine, although open-label studies are available. And of course, after our initial pilot Medscape (subscription) Comparison of antipsychotic medication effects on reducing ... - Jun 30, 2008 Over the past decade a growing research literature has suggested that second-generation antipsychotics such as clozapine, olanzapine, risperidone, British Journal of Psychiatry (subscription), FDA requests boxed warnings on “conventional� antipsychotics - Jun 16, 2008 Atypical antipsychotic drugs that have been required to carry a boxed warning include Clozaril (clozapine) , FazaClo (clozapine), Geodon (ziprasidone), Food Consumer, Menopausal melatonin and isoflavones - 02 Jun 2008 Folic acid, clozapine and quetiapine were used as internal standards. The contents of the commercial capsules were extracted with aqueous methanol and the separationsNOW.com (subscription), Influence of 5-HT 2C receptor and leptin gene polymorphisms ... - May 31, 2008 However, the mean age of patients receiving olanzapine (37.6 years) and clozapine (36.2 years) was significantly lower than that of the remaining patients British Journal of Psychiatry (subscription), High-dose and combination antipsychotic prescribing in acute adult ... - May 31, 2008 In 56 (22%) of the 259 cases where the reason given was poor response to monotherapy, the combination included clozapine. At the 1-year audit, 1287 patients British Journal of Psychiatry (subscription), First- v. second-generation antipsychotics and risk for diabetes ... - May 31, 2008 Although clozapine was first introduced in 1956 and withdrawn shortly after because of severe side-effects, there was a small risk of not detecting pre-1966 British Journal of Psychiatry (subscription), The Surgeon General's Report on Mental Health - May 15, 2008 Antipsychotic medications, other than clozapine, should be used as the first-line treatment to reduce psychotic symptoms for persons experiencing an acute About - News & Issues, UNM psychiatrist receives national honors - May 6, 2008 According to a Health Sciences Center Web site profile, Bustillo is the director of the Clozapine Clinic and is an attending psychiatrist in the Bizjournals.com, MEDICINES KILL SCHIZOPHRENIC - May 7, 2008 West Cumbria coroner John Taylor will now pass on concerns raised by Mr Date’s family to his doctor about the cumulative effect of taking Clozapine – an NW Evening Mail, New-Onset Schizophrenia: Pharmacologic Treatment - May 15, 2008 A number of industry-sponsored trials have been conducted in first-episode patients to compare clozapine to chlorpromazine (15), olanzapine and haloperidol Focus (subscription) Excess of transmission of the G allele of the -1438A/G ... - May 30, 2008 The -1438A/G polymorphism of the 5-HT2A gene has been found to be associated with clinical response to clozapine and other second generation antipsychotics. 7thSpace Interactive (press release), Medication-Induced Weight Gain and Dyslipidemia in Patients With ... - May 15, 2008 These adverse outcomes have been most associated with clozapine and olanzapine (3, 15). In most cases, weight gain and abdominal adiposity may be central to Focus (subscription) APA: Narcolepsy Drug Seems to Limit Olanzapine Weight Gain - May 6, 2008 Weight gain is a major adverse effect of olanzapine, clozapine (Clozaril), and other atypical anti-psychotics. Dr. Roerig said it appears to occur because MedPage Today, Corcept Therapeutics Announces First Quarter 2008 Results - May 12, 2008 The group of medications known as atypical antipsychotics, including olanzapine, risperidone, clozapine and quetiapine, are widely used to treat CNNMoney.com New Link To Schizophrenia Discovered - May 8, 2008 Most importantly, according to Savonenko, some of the deficits improved after treatment with the antipsychotic drug clozapine. Because schizophrenia is a Science Daily (press release) ACADIA Pharmaceuticals, Inc. Q1 2008 Earnings Call Transcript - May 5, 2008 ...that ACP-104 is generally safe and well tolerated and displays a favorable side effect profile, relative to that commonly seen with Clozapine. Seeking Alpha, Neurochemical May Underlie Lack of Motivation in Psychosis - May 8, 2008 ...risperidone (Risperdal) (two), quetiapine (Seroquel) (two), clozapine (Clozaril) (one), aripiprazole (Abilify) (two), and amisulpride (one). MedPage Today, Nurse care for schizophrenia patients - May 6, 2008 Caring such patients undergoing therapy with antipsychotic drugs like clozapine and benzodiazepines involves careful monitoring of the patient's News-Medical.net, Sexual Dysfunction in Schizophrenia - May 15, 2008 ...one could speculate that antipsychotics with a strong affinity to the D4 receptor (like clozapine) present with a higher risk for sexual dysfunction. Focus (subscription) The Surgeon General's Report on Mental Health - May 15, 2008 Also known as second-generation antipsychotics, they include these chemical classes: dibenzoxazepine (eg, clozapine), thienobenzodiazepine (eg, olanzapine), About - News & Issues, The Surgeon General's Report on Mental Health - May 7, 2008 Studies with mostly younger schizophrenia patients suggest that the newer “atypical� antipsychotics, such as clozapine, risperidone, olanzapine, About - News & Issues, FDA tells Aryx Therapeutics it can test schizophrenia drug - 23 Apr 2008 This drug, ATI-9242, based on clozapine, is meant to treat the symptoms of schizophrenia without interacting with other drugs or causing side effects like Bizjournals.com, Dangerous anti-psychotic drug lost by patient - 23 Apr 2008 Police say a quantity of the prescription drug Clozapine was mislaid by a patient some time since yesterday, possibly in the Longshaw Street area. Widnes and Runcorn World, Clozapine Better Than "High-Dose" Olanzapine for the Treatment of ... - Mar 24, 2008 After initial assessment, the patients received treatment with either clozapine or "high-dose" olanzapine and were monitored for improvement of their DG News Can Atypical Antipsychotics Reduce Suicide Risk in Patients With ... - Apr 15, 2008 This, in turn, prevents any definitive conclusions; the sole exception is clozapine, which should be considered when suicide risk is detected. Psychiatric Times, Which drugs best for schizophrenia? - Apr 13, 2008 In 1989, he switched to the newer drug clozapine, and in 1996, Zyprexa was added to his regimen. Miller says he hasn’t had an “episode� for 12 years and he Gazette Online, Tomato growers' blocking of raise for pickers is shameful - Apr 21, 2008 Finally, in the 1990s, a new medication came on the market — Clozapine. After being treated only six months with this "atypical" drug, Dave was able to Tampabay.com, Seaforth man died from drug cocktail - Apr 17, 2008 A quantity of the prescription medication Clozapine was also “within fatal range�, he said. A wrap of white powder was found in Mr Jones’ possession, icSeftonandWestLancs, Newland convicted of deception to obtain a dangerous drug - Apr 9, 2008 Lehmkuhl told the News the pills in question were actually Clozapine and Clindamycin, prescription drugs Lehmkuhl said were stolen by Blubaugh from Mount Vernon News, The Muscarinic Hypothesis of Schizophrenia: Implications for ... - Apr 15, 2008 Looking at atypical antipsychotics, in vitrostudies show that clozapine and olanzapine have strong binding affinity for muscarinic ACh receptors, Psychiatric Times, New Findings in Early-Onset Schizophrenia - Apr 2, 2008 A recent 12-week study compared clozapine with high-dose olanzapine (up to 30 mg/d) in 39 children and adolescents aged 10 to 18 with schizophrenia who were Psychiatric Times, Improvement in Refractory Obsessive Compulsive Disorder With ... - Apr 1, 2008 Treatment with clozapine (400 mg), which he had already received for more than 1 year (in combination with paroxetine [60 mg] for 13 weeks) resulted only in Am J Psychiatry (subscription) Neuroleptic-induced movement disorders in a naturalistic ... - Apr 18, 2008 Methods: A naturalistic population of 99 schizophrenia inpatients using conventional antipsychotics and clozapine was evaluated.Subjects with NIMDs were 7thSpace Interactive (press release), The Development and Use of Modern Psychotherapeutic Medications - Apr 15, 2008 In their article, Eduardo J. Aguilar, MD, PhD, and his colleagues focus on the use of existing antipsychotics, beyond clozapine, to reduce the risk of Psychiatric Times, Medications and Quality of Life With Schizophrenia - Apr 15, 2008 ...doing more this summer," said John, a 39-year-old man with a 15-year history of schizophrenia, on beginning his seventh month of clozapine treatment. Psychiatric Times, Corcept Therapeutics Announces Fourth Quarter 2007 Results - Mar 27, 2008 The group of medications known as atypical antipsychotics, including olanzapine, risperidone, clozapine and quetiapine, are widely used to treat FOXBusiness Is Your Medicine Making You Fat? - Mar 26, 2008 The anti-psychotics, for example haloperidol and clozapine, affect metabolism and can add as many as five pounds a week. Insulin and anti-diabetic drugs Jamaica Observer, Man, 30 died at his flat of drugs overdose - Apr 11, 2008 Dr Richard Prescott, who conducted the post mortem examination on Mr Monks, said that clozapine, a drug prescribed to control the effects of schizophrenia, Blackburn Citizen, The anti-psychotic myth exposed? - Apr 2, 2008 Neuroleptics – such as Clozapine, Olanzapine, Risperidone and Seroquel – are the “primary treatment� for psychosis, particularly schizophrenia. Psychminded.co.uk, Antidepressants, Mood Stabilizers can Cause Weight Gain - Apr 1, 2008 Dr.Lau listed the anti-psychotics most likely to be associated with weight gain as: Clozaril, or clozapine; Zyprexa, Seroquel or quetiapine; Risperdal, MedIndia, FDA Orders Drug Safety Plans - Mar 31, 2008 ...myeloma medication thalidomide (Thalomid), the anti-psychotic medication clozapine (Clozaril), and the abortifacient drug mifepristone (Mifeprex). Newsinferno.com, Psychiatric pills can pack on pounds - Mar 31, 2008 Lau said the anti-psychotics most likely to be associated with weight gain are: Clozaril, or clozapine; Zyprexa, Seroquel or quetiapine; Risperdal, United Press International 10 Deadliest Drugs - Mar 27, 2008 Rounding out the top 10 are two antipsychotic medications, clozapine and risperidone (Risperdal); interferon-beta, a drug that helps regulate the immune WXii 12.com, Killer allowed longer visits to St. Catharines - Apr 15, 2008 The switch to antipsychotic medication Clozapine in May 2007, the board said, resulted in “significant improvement� in Hemphill’s mental state. St. Catharines Standard, Novartis to expand its business - Apr 7, 2008 Novartis International AG is a multinational pharmaceutical company based in Basel, Switzerland that manufactures different important drugs (clozapine, Pravda, ACADIA Pharmaceuticals to Present Preclinical Data on ACP-104, ACP ... - Apr 4, 2008 ACP-104, or N-desmethylclozapine, is the major metabolite of clozapine that ACADIA is developing as a novel stand-alone therapy for schizophrenia. PharmaLive.com (press release), Psychiatric drugs causing weight gain: doctors - Mar 30, 2008 Lau, of the University of Calgary, says the antipsychotics most likely to be associated with weight gain and diabetes are Clozaril (clozapine), Zyprexa, GlobalTV, Brand Names/Synonyms: Clozapine is also known by the following brand names and/or synonymsAsaleptin; Clozapin; Clozapine; Clozaril; Fazaclo ODT; HF-1854; Iprox; Leponex; Lepotex; W-801 Drug Category: Clozapine is categorized under the following by the FDA: Antipsychotics; Antipsychotics; ATC:N05AH02 Dosage Forms: TABLET Absorption: rapid and almost complete Interactions: Interactions for Clozapine: The risks of using Clozapine in combination with other drugs have not been systematically evaluated. Pharmacodynamic-related Interactions: The mechanism of Clozapine induced agranulocytosis is unknown; nonetheless, the possibility that causative factors may interact synergistically to increase the risk and/or severity of bone marrow suppression warrants consideration. Therefore, Clozapine should not be used with other agents having a well-known potential to suppress bone marrow function. Given the primary CNS effects of Clozapine, caution is advised in using it concomitantly with other CNS-active drugs or alcohol. Orthostatic hypotension in patients taking clozapine can, in rare cases (approximately 1 case per 3,000 patients), be accompanied by profound collapse and respiratory and/or cardiac arrest. Some of the cases of collapse/respiratory arrest/cardiac arrest during initial treatment occurred in patients who were being administered benzodiazepines; similar events have been reported in patients taking other psychotropic drugs or even Clozapine by itself. Although it has not been established that there is an interaction between Clozapine and benzodiazepines or other psychotropics, caution is advised when clozapine is initiated in patients taking a benzodiazepine or any other psychotropic drug. Clozapine may potentiate the hypotensive effects of antihypertensive drugs and the anticholinergic effects of atropine-type drugs. The administration of epinephrine should be avoided in the treatment of drug induced hypotension because of a possible reverse epinephrine effect. Pharmacokinetic-related Interactions: Clozapine is a substrate for many CYP 450 isozymes, in particular 1A2, 2D6, and 3A4. The risk of metabolic interactions caused by an effect on an individual isoform is therefore minimized. Nevertheless, caution should be used in patients receiving concomitant treatment with other drugs that are either inhibitors or inducers of these enzymes. Concomitant administration of drugs known to induce cytochrome P450 enzymes may decrease the plasma levels of clozapine. Phenytoin, nicotine, and rifampin may decrease Clozapine plasma levels, resulting in a decrease in effectiveness of a previously effective Clozapine dose. Concomitant administration of drugs known to inhibit the activity of cytochrome P450 isozymes may increase the plasma levels of clozapine. Cimetidine, caffeine, and erythromycin may increase plasma levels of Clozapine, potentially resulting in adverse effects. Although concomitant use of Clozapine and carbamazepine is not recommended, it should be noted that discontinuation of concomitant carbamazepine administration may result in an increase in Clozapine plasma levels. In a study of schizophrenic patients who received clozapine under steady state conditions, fluvoxamine or paroxetine was added in 16 and 14 patients, respectively. After 14 days of co-administration, mean trough concentrations of clozapine and its metabolites, N-desmethylclozapine and clozapine N-oxide, were elevated with fluvoxamine by about three-fold compared to baseline concentrations. Paroxetine produced only minor changes in the levels of clozapine and its metabolites. However, other published reports describe modest elevations (less than two-fold) of clozapine and metabolite concentrations when clozapine was taken with paroxetine, fluoxetine, and sertraline. Therefore, such combined treatment should be approached with caution and patients should be monitored closely when Clozapine is combined with these drugs, particularly with fluvoxamine. A reduced Clozapine dose should be considered. A subset (3%-10%) of the population has reduced activity of certain drug metabolizing enzymes such as the cytochrome P450 isozyme P450 2D6. Such individuals are referred to as "poor metabolizers" of drugs such as debrisoquin, dextromethorphan, the tricyclic antidepressants, and clozapine. These individuals may develop higher than expected plasma concentrations of clozapine when given usual doses. In addition, certain drugs that are metabolized by this isozyme, including many antidepressants (clozapine, selective serotonin reuptake inhibitors, and others), may inhibit the activity of this isozyme, and thus may make normal metabolizers resemble poor metabolizers with regard to concomitant therapy with other drugs metabolized by this enzyme system, leading to drug interaction. Concomitant use of clozapine with other drugs metabolized by cytochrome P450 2D6 may require lower doses than usually prescribed for either clozapine or the other drug. Therefore, co-administration of clozapine with other drugs that are metabolized by this isozyme, including antidepressants, phenothiazines, carbamazepine, and Type 1C antiarrhythmics (e.g., propafenone, flecainide and encainide), or that inhibit this enzyme (e.g., quinidine), should be approached with caution. Chemical IUPAC Name: Not Available : |
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