Serzone

This page contains recent news articles, when available, and an overview of Serzone but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.

Overview:

Serzone (when available)

Pharmacology and use:
Nefazodone, an antidepressant synthetically derived phenylpiperazine, is used to treat major depression. Although it is structurally similar to trazodone, nefazodone has a mechanism of action different from other antidepressants and, hence, lacks the risk for major cardiovascular toxicity seen with tricyclics and insomnia and inhibition of REM sleep seen with the selective serotonin reuptake inhibitors. For the treatment of depression

Mechanism Of Action:
Within the serotonergic system, nefazodone acts as an antagonist at type 2 serotonin (5-HT₂) post-synaptic receptors and, like fluoxetine-type antidepressants, inhibits pre-synaptic serotonin (5-HT) reuptake. These mechanisms increase the amount of serotonin available to interact with 5-HT receptors. Within the noradrenergic system, nefazodone inhibits norepinephrine uptake minimally. Nefazodone also antagonizes alpha(1)-adrenergic receptors, producing sedation, muscle relaxation, and a variety of cardiovascular effects. Nefazodone's affinity for benzodiazepine, cholinergic, dopaminergic, histaminic, and beta or alpha(2)-adrenergic receptors is not significant.

News Articles on Nefazodone

Noticing the Not-So-Obvious  -  20 Apr 2009
Nefazodone (Serzone), another newer antidepressant, appears to block a specific serotonin receptor. Bupropion (Wellbutrin) is an effective antidepressant, ADVANCE for Physician Assistants

I Servizi Sociali Italiani sottrangono una bimba alla mamma a ...  -  ‎Apr 15, 2009‎
Escitalopram (Lexapro), Bupropione (Wellbutrin), Venlafaxina (Effexor), Nefazodone (Serzone), Mirtazapina (Remeron), Giornalmente arrivano nuovi nomi. ECPlanet

How can I find an antidepressant that works?  -  ‎Feb 24, 2009‎
I was also taking 50mg of Serzone if that makes any difference. I am currently taking Prozac-5mg, Serzone -50mg, and Klonopin as needed (reluctantly, CNN

Panik atağı ne tetikler  -  ‎Mar 3, 2009‎
...(Anafranil, tofranil, ludiomil, insidon, laroxyl, tolvon... gibi ) Yeni kuşak ,ilaçlar ( efexör, seroxat, cipram, remeron, prozac, lustral, serzone, Haberanaliz.net

Side effects blunt antidepressants gains  -  Feb 3, 2009
The lowest rates–between 20 and 30 percent–were with Wellbutrin (buproprion) and Serzone (nefazodone). The latter has been linked to liver problems and is Enid News & Eagle,

I Took Serzone for Over 10 Years With No Side Effects  -  Dec 11, 2008
I like the Serzone because it kept me from bouncing around. What people should worry about is Ambien, now I took that for 6 or 7 years and finally quit NewsBlaze,

2008 Media Follies!  -  Dec 18, 2008
...anti-depressant drugs on the market, including Prozac, Effexor, Serzone, and Paxil, and concluded that they’re no better than taking a sugar pill. Media Channel,

Depressing News for Drugmakers  -  Nov 19, 2008
...such as Eli Lilly's Prozac, Wyeth's (NYSE: WYE) Effexor, and Bristol-Myers Squibb's (NYSE: BMY) Serzone. Since they're usually available more cheaply, Motley Fool

Federal Preemption: Not the Rite Aid Rx for Michigan's Joe and Dianne  -  Oct 30, 2008
Serzone, another of several medicines that were prescribed off-label, was linked to liver toxicity and, in some cases, failure. Serzone was voluntarily InjuryBoard.com,

Pharmaceutical Industry Hustlers – Part I  -  Nov 5, 2008
For instance, Ms Bass explains that Drs Schatzberg and Keller worked as a team a decade ago to promote Bristol-Myers Squibb's antidepressant Serzone. Scoop.co.nz,

Achieving Happiness: Drugs may not be best depression treatment  -  Nov 9, 2008
Zoloft, Wellbutrin, Effexor, Cymbalta, Lexapro, Serzone, Celexa, Remeron and Paxil. The NEJM researchers stated that not publicizing unfavorable studies Annapolis Capital,

Therapy plus Zoloft helps anxious kids  -  Nov 1, 2008
...citalopram (Celexa), fluoxetine (Prozac), fluvoxamine (Luvox), mirtazapine (Remeron), nefazodone (Serzone), paroxetine (Paxil), sertraline (Zoloft), Daily Herald,

Glenna Todovich Releases her sons story to Show Pharmacuetical ...  -  Nov 10, 2008
The List:Prozac, Paxil, Zoloft, Wellbutrin, Celexa, Luvox,Buspar,Serzone, Remeron (she told). He was also diagnosed with OCD at some point and put on Live-PR.com (Pressemitteilung),

Antidépresseurs: mêmes efficacités, effets secondaires différents  -  Nov 18, 2008
...la duloxétine (Cymbalta), la fluvoxamine (Luvox), la mirtazapine (Remeron), le trazodone (Desyrel), le néfazodone (Serzone), la venlafaxine (Effexor). PsychoMédia,

Are Antidepressant Drugs Actually Worth Taking  -  Oct 10, 2008
...on the other four—fluoxetine (Prozac), paroxetine (Paxil), venlafaxine (Effexor), and nefazodone (formerly sold in the United States as Serzone). Discover Magazine,

8 Sep, 2008, 0000 hrs IST,Rajrishi Singhal, ET Bureau  -  Sep 7, 2008
According to various estimates, 10% of all medication errors can be attributed to confusion over drug names – Serzone (an anti-depressant) is often mistaken Economic Times,

Learn about the World CNS Therapeutics Market  -  Sep 4, 2008
...to Develop CNS Therapies II-65 Aspect Medical Acquires Exclusive Rights to Cordance Technology II-65 Bristol-Myers Pulls Out Serzone from the US Market MarketWatch

Drug Companies Routinely Bury Studies Showing Their Drugs Don't Work  -  Aug 20, 2008
The actual amount varied from a low of 11 percent for Glaxo SmithKline's Paxil to a high of 69 percent for Bristol-Myers-Squibb's Serzone. Natural News.com,

Ακατάλληλα τα αντικαταθλιπτικά  -  Aug 28, 2008
Η έ�?ευνα εξέτασε τα αντικαταθλιπτικά Ladose (πε�?ιέχει την ουσία φλουοξετίνη, γνωστό ως Prozac), Serzone (νεφαζοδόνη) και Effexor (βενλαφαξίνη). medNutrition,

Tenn. nabs $3.5M in law suit settlement  -  Jul 29, 2008
According to the settlement, the company also misreported sales prices for Serzone, an antidepressant, which reduced the amount of rebates paid to state Bizjournals.com,

State gets $12M in drug company settlement  -  Jul 15, 2008
The drug company also was accused of misreporting prices for Serzone, an antidepressant, so consequently rebates to Medicaid were less. Atlanta Journal Constitution,

Minnesota to get $4 million in Bristol-Myers Squibb settlement  -  Jul 22, 2008
The company was also accused of misreporting sales of an antidepressant called Serzone. Bristol-Myers didn't admit any wrongdoing in the settlement, Pioneer Press,

BRISTOL-MYERS SQUIBB SETTLES FOR $389 MILLION  -  Jul 31, 2008
The allegations are that BMS engaged in a number of improper marketing pricing practices, including: * Misreporting sales prices for Serzone, UC Daily News,

Wyoming gets share of drug pricing settlement  -  Jul 30, 2008
...uses which the Federal Food and Drug Administration has not approved, and also misinterpreted sales prices for Serzone, an anti-depressant, Jackson Hole Star-Tribune,

Maryland Reaches Multi-Million Dollar Settlement with Bristol ...  -  Jul 28, 2008
Misreporting sales prices for Serzone, an antidepressant, resulting in the improper reduction of the amount of rebates paid to the state Medicaid programs. Southern Maryland Online,

Iowa gets $1.9 million drugs settlement  -  Jul 25, 2008
The company also was accused of overcharging state Medicaid programs for the anti-depression medicine Serzone. On Thursday, a company spokeswoman released a DesMoinesRegister.com,

Settlement restores money to Medicaid  -  Jul 22, 2008
...drug Abilify for uses not approved of by the federal Food and Drug Administration; and misreporting sales prices for the antidepressant drug Serzone. The News Journal,

Georgia awarded $5M in Bristol-Myers Squibb settlement  -  Jul 21, 2008
...and misreporting sales prices for Serzone, an antidepressant, resulting in the improper reduction of the amount of rebates paid to the state Medicaid MSN Money

The Latest on Antidepressants: Be Careful Where You Get Your Facts  -  Jul 31, 2008
...evaluating four of the newer antidepressants--fluoxetine (Prozac), venlafaxine (Effexor), nefazodone (Serzone), and paroxetine (Paxil). Beliefnet.com,

Utah Gets $2 Million From Drug Company's Cheating  -  Jul 30, 2008
Bristol-Myers Squibb is also accused of misreporting sales prices of an antidepressant, Serzone, in order to reduce rebate payments to state Medicaid KUTV,

ND gets part of drug company settlement  -  Aug 2, 2008
...to induce them to purchase Bristol-Myers Squibb products; misreporting the price of antidepressant medication Serzone and promoting the use of Abilify, Jamestown Sun,

Forum Communications and Wire Reports  -  Aug 1, 2008
...to induce them to purchase Bristol-Myers Squibb products; misreporting the price of antidepressant medication Serzone; and promoting the use of Abilify, Grand Forks Herald,

超收處方藥物費制藥商賠款和解  -  Jul 26, 2008
...藥Abilify推銷給�?兒科病人或是用來治療癡呆相關精神症狀，這些用途未經食�?藥物管�?�局批准；錯報抗抑鬱劑Serzone 新浪網,

Recent Developments  -  Jul 5, 2008
By Anonymous Prozac, and similar selective serotonin reuptake inhibitor antidepressants Seroxat, Effexorand Serzone, work no better than placebo for most RedOrbit,

Surge in antidepressant use touches off health debate  -  Apr 15, 2008
35 clinical trials for the antidepressants Prozac, Effexor, Serzone and Paxil that had been submitted for review to the Food and Drug Administration. Minneapolis Star Tribune,

Anti-depressants: which research should we believe?  -  Apr 18, 2008
...venlafaxine (Seroxat), nefazodone (Effexor), and paroxetine (Serzone). Kirsch had used freedom of information law to retrieve the data. Psychminded.co.uk,

Millions Recovered in 2007 for State Medicaid Program  -  Mar 27, 2008
...part of a multi-state settlement over illegal marketing and pricing practices including the antipsychotic drug Abilify, and the anti-depressant Serzone. Inside INdiana Business (press release),

Brand Names/Synonyms:
Serzone is also known by the following brand names and/or synonymsCHEMBANK1803; Dutonin; Nefazodona [Spanish]; Nefazodone; Nefazodone Hcl; Nefazodone Hydrochloride; Nefazodonum [Latin]; Serzone

Drug Category:
Serzone is categorized under the following by the FDA: Antidepressants; Analgesics; Serotonin Agents; ATC:N06AX06

Dosage Forms:
Tablets

Absorption:
rapidly and completely absorbed, its absolute bioavailability is low, about 20%

Interactions:
DRUG INTERACTIONS Drugs Highly Bound to Plasma Protein Because nefazodone is highly bound to plasma protein,administration of SERZONE to a patient taking another drug that is highly protein bound may cause increased free concentrations of the other drug, potentially resulting in adverse events. Conversely, adverse effects could result from displacement of nefazodone by other highly bound drugs. Warfarin: There were no effects on the prothrombin or bleeding times or upon the pharmacokinetics of R-warfarin when nefazodone (200 mg BID) was administered for 1 week to subjects who had been pretreated for 2 weeks with warfarin. Although the coadministration of nefazodone did decrease the subjects� exposure to S-warfarin by 12%, the lack of effects on the prothrombin and bleeding times indicates this modest change is not clinically significant. Although these results suggest no adjustments in warfarin dosage are required when nefazodone is administered to patients stabilized on warfarin, such patients should be monitored as required by standard medical practices. CNS-Active Drugs Monoamine Oxidase Inhibitors Haloperidol: When a single oral 5-mg dose of haloperidol was coadministered with nefazodone (200 mg BID) at steady state, haloperidol apparent clearance decreased by 35% with no significant increase in peak haloperidol plasma concentrations or time of peak. This change is of unknown clinical significance. Pharmacodynamic effects of haloperidol were generally not altered significantly. There were no changes in the pharmacokinetic parameters for nefazodone. Dosage adjustment of haloperidol may be necessary when coadministered with nefazodone. Lorazepam: When lorazepam (2 mg BID) and nefazodone (200 mg BID) were coadministered to steady state, there was no change in any pharmacokinetic parameter for either drug compared to each drug administered alone. Therefore, dosage adjustment is not necessary for either drug when coadministered. Triazolam/Alprazolam Alcohol: Although nefazodone did not potentiate the cognitive and psychomotor effects of alcohol in experiments with normal subjects, the concomitant use of SERZONE and alcohol in depressed patients is not advised. Buspirone: In a study of steady-state pharmacokinetics in healthy volunteers, coadministration of buspirone (2.5 or 5 mg BID) with nefazodone (250 mg BID) resulted in marked increases in plasma buspirone concentrations (increases up to 20-fold in Cmax and up to 50-fold in AUC) and statistically significant decreases (about 50%) in plasma concentrations of the buspirone metabolite 1-pyrimidinylpiperazine. With 5-mg BID doses of buspirone, slight increases in AUC were observed for nefazodone (23%) and its metabolites hydroxynefazodone (17%) and mCPP (9%). Subjects receiving nefazodone 250 mg BID and buspirone 5 mg BID experienced lightheadedness, asthenia, dizziness, and somnolence, adverse events also observed with either drug alone. If the two drugs are to be used in combination, a low dose of buspirone (eg, 2.5 mg QD) is recommended. Subsequent dose adjustment of either drug should be based on clinical assessment. Pimozide: Pharmacokinetics of Nefazodone in �Poor Metabolizers� and Potential Interaction with Drugs that Inhibit and/or Are Metabolized by Cytochrome P450 Isozymes. Fluoxetine: When fluoxetine (20 mg QD) and nefazodone (200 mg BID) were administered at steady state there were no changes in the pharmacokinetic parameters for fluoxetine or its metabolite, norfluoxetine. Similarly, there were no changes in the pharmacokinetic parameters of nefazodone or HO-NEF; however, the mean AUC levels of the nefazodone metabolites mCPP and triazoledione increased by 3- to 6-fold and 1.3-fold,respectively. When a 200-mg dose of nefazodone was administered to subjects who had been receiving fluoxetine for 1 week, there was an increased incidence of transient adverse events such as headache, lightheadedness, nausea, or paresthesia, possibly due to the elevated mCPP levels. Patients who are switched from fluoxetine to nefazodone without an adequate washout period may experience similar transient adverse events. The possibility of this happening can be minimized by allowing a washout period before initiating nefazodone therapy and by reducing the initial dose of nefazodone. Because of the long half-life of fluoxetine and its metabolites, this washout period may range from one to several weeks depending on the dose of fluoxetine and other individual patient variables. Phenytoin: Pretreatment for 7 days with 200 mg BID of nefazodone had no effect on the pharmacokinetics of a single 300-mg oral dose of phenytoin. However, due to the nonlinear pharmacokinetics of phenytoin, the failure to observe a significant effect on the single-dose pharmacokinetics of phenytoin does not preclude the possibility of a clinically significant interaction with nefazodone when phenytoin is dosed chronically. However, no change in the initial dosage of phenytoin is considered necessary and any subsequent adjustment of phenytoin dosage should be guided by usual clinical practices. Desipramine: When nefazodone (150 mg BID) and desipramine (75 mg QD) were administered together there were no changes in the pharmacokinetics of desipramine or its metabolite, 2-hydroxy desipramine. There were also no changes in the pharmacokinetics of nefazodone or its triazoledione metabolite, but the AUC and Cmax of mCPP increased by 44% and 48%, respectively, while the AUC of HO-NEF decreased by 19%. No changes in doses of either nefazodone or desipramine are necessary when the two drugs are given concomitantly. Subsequent dose adjustments should be made on the basis of clinical response. Lithium: In 13 healthy subjects the coadministration of nefazodone (200 mg BID) with lithium (500 mg BID) for 5 days (steady-state conditions) was found to be well tolerated. When the two drugs were coadministered, there were no changes in the steady-state pharmacokinetics of either lithium, nefazodone, or its metabolite HO-NEF; however, there were small decreases in the steady-state plasma concentrations of two nefazodone metabolites, mCPP and triazoledione, which are considered not to be of clinical significance. Therefore, no dosage adjustment of either lithium or nefazodone is required when they are coadministered. Carbamazepine: The coadministration of nefazodone (200 mg BID) for 5 days to 12 healthy subjects on carbamazepine who had achieved steady state (200 mg BID) was found to be well tolerated. Steady-state conditions for carbamazepine, nefazodone, and several of their metabolites were achieved by day 5 of coadministration. With coadministration of the two drugs there were significant increases in the steady-state Cmax and AUC of carbamazepine (23% and 23%, respectively), while the steady-state Cmax and the AUC of the carbamazepine metabolite, 10, 11 epoxycarbamazepine, decreased by 21% and 20%, respectively. The coadministration of the two drugs significantly reduced the steady-state Cmax and AUC of nefazodone by 86% and 93%, respec-tively.Similar reductions in the Cmax and AUC of HO-NEF were also observed (85% and 94%),while the reductions in Cmax and AUC of mCPP and triazole-dione were more modest (13% and 44% for the former and 28% and 57% for the latter).Due to the potential for coadministration of carbamazepine to result in insufficient plasma nefazodone and hydroxynefazodone concentrations for achieving an antidepressant effect for SERZONE, it is recommended that SERZONE not be used in combination with carbamazepine (see CONTRAINDICATIONS and WARNINGS). General Anesthetics: Little is known about the potential for interaction between nefazodone and general anesthetics; therefore, prior to elective surgery, SERZONE should be discontinued for as long as clinically feasible. Other CNS-Active Drugs: The use of nefazodone in combination with other CNS-active drugs has not been systematically evaluated. Consequently, caution is advised if concomitant administration of SERZONE (nefazodone hydrochloride) and such drugs is required. Cimetidine When nefazodone (200 mg BID) and cimetidine (300 mg QID) were coadministered for one week, no change in the steady-state pharmacokinetics of either nefazodone or cimetidine was observed compared to each dosed alone. Therefore, dosage adjustment is not necessary for either drug when coadministered. Theophylline When nefazodone (200 mg BID) was given to patients being treated with theophylline (600-1200 mg/day) for chronic obstructive pulmonary disease,there was no change in the steady-state pharmacokinetics of either nefazodone or theophylline. FEV1 measurements taken when theophylline and nefazodone were coadministered did not differ from baseline dosage (ie, when theophylline was administered alone).Therefore, dosage adjustment is not necessary for either drug when coadministered. Cardiovascular-Active Drugs Digoxin: When nefazodone (200 mg BID) and digoxin (0.2 mg QD) were coadministered for 9 days to healthy male volunteers (n=18) who were phenotyped as CYP2D6 extensive metabolizers, Cmax, Cmin, and AUC of digoxin were increased by 29%, 27%, and 15%, respectively. Digoxin had no effects on the pharmacokinetics of nefazodone and its active metabolites. Because of the narrow therapeutic index of digoxin,caution should be exercised when nefazodone and digoxin are coadministered; plasma level monitoring for digoxin is recommended. Propranolol: The coadministration of nefazodone (200 mg BID) and propranolol (40 mg BID) for 5.5 days to healthy male volunteers (n=18), including 3 poor and 15 extensive CYP2D6 metabolizers, resulted in 30% and 14% reductions in Cmax and AUC of propranolol, respectively, and a 14% reduction in Cmax for the metabolite, 4-hydroxypropranolol. The kinetics of nefazodone, hydroxynefazodone, and triazoledione were not affected by coadministration of propranolol. However, Cmax, Cmin, and AUC of m-chlorophenylpiperazine were increased by 23%, 54%, and 28%, respectively. No change in initial dose of either drug is necessary and dose adjustments should be made on the basis of clinical response. HMG-CoA Reductase Inhibitors: When single 40-mg doses of simvastatin or atorvastatin, both substrates of CYP3A4, were given to healthy adult volunteers who had received SERZONE 200 mg BID for 6 days, approximately 20-fold increases in plasma concentrations of simvastatin and simvastatin acid and 3- to 4-fold increases in plasma concentrations of atorvastatin and atorvastatin lactone were seen. These effects appear to be due to the inhibition of CYP3A4 by SERZONE because, in the same study, SERZONE had no significant effect on the plasma concentrations of pravastatin, which is not metabolized by CYP3A4 to a clinically significant extent. There have been rare reports of rhabdomyolysis involving patients receiving the combination of SERZONE and either simvastatin or lovastatin, also a substrate of CYP3A4 (see ADVERSE REACTIONS: Postintroduction Clinical Experience). Rhabdomyolysis has been observed in patients receiving HMG-CoA reductase inhibitors administered alone (at recommended dosages) and in particular, for certain drugs in this class, when given in combination with inhibitors of the CYP3A4 isozyme. Caution should be used if SERZONEis administered in combination with HMG-CoA reductase inhibitors that are metabolized by CYP3A4, such as simvastatin, atorvastatin, and lovastatin, and dosage adjustments of these HMG-CoA reductase inhibitors are recommended. Since metabolic interactions are unlikely between SERZONE and HMG-CoA reductase inhibitors that undergo little or no metabolism by the CYP3A4 isozyme, such as pravastatin or fluvastatin, dosage adjustments should not be necessary. Immunosuppressive Agents There have been reports of increased blood concentrations of cyclosporine and tacrolimus into toxic ranges when patients received these drugs concomitantly with SERZONE. Both cyclosporine and tacrolimus are substrates of CYP3A4, and nefazodone is known to inhibit this enzyme. If either cyclosporine or tacrolimus is administered with SERZONE, blood concentrations of the immunosuppressive agent should be monitored and dosage adjusted accordingly. Pharmacokinetics of Nefazodone in �Poor Metabolizers� and Potential Interaction with Drugs that Inhibit and/or Are Metabolized by Cytochrome P450 Isozymes CYP3A4 Isozyme: Nefazodone has been shown in vitro to be an inhibitor of CYP3A4. This is consistent with the interactions observed between nefazodone and triazolam, alprazolam, buspirone, atorvastatin, and simvastatin, drugs metabolized by this isozyme. Consequently, caution is indicated in the combined use of nefazodone with any drugs known to be metabolized by CYP3A4. In particular, the combined use of nefazodone with triazolam should be avoided for most patients, including the elderly. The combined use of nefazodone with terfenadine, astemizole, cisapride, or pimozide is contraindicated (see CONTRAINDICATIONS and WARNINGS). CYP2D6 Isozyme: A subset (3% to 10%) of the population has reduced activity of the drug-metabolizing enzyme CYP2D6. Such individuals are referred to commonly as "poor metabolizers" of drugs such as debrisoquin, dextromethorphan, and the tricyclic antidepressants. The pharmacokinetics of nefazodone and its major metabolites are not altered in these "poor metabolizers." Plasma concentrations of one minor metabolite (mCPP) are increased in this population; the adjustment of SERZONE dosage is not required when administered to "poor metabolizers." Nefazodone and its metabolites have been shown in vitro to be extremely weak inhibitors of CYP2D6. Thus, it is not likely that nefazodone will decrease the metabolic clearance of drugs metabolized by this isozyme. CYP1A2 Isozyme: Nefazodone and its metabolites have been shown in vitro not to inhibit CYP1A2. Thus, metabolic interactions between nefazodone and drugs metabolized by this isozyme are unlikely.

Chemical IUPAC Name:
2-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-ethyl-4-(2-phenoxyethyl)-2,4-dihydro-1,2,4-triazol-3-one

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