欣百达(盐酸度洛西汀肠溶胶囊)说明书
盐酸度洛西汀缓释胶囊说明书(英文)
3HIGHLIGHTS OF PRESCRIBING INFORMATIONThese highlights do not include all the information needed to use Cymbalta safely and effectively. See full prescribing information for Cymbalta.Cymbalta (duloxetine hydrochloride) Delayed-Release Capsules for Oral Use.Initial U.S. Approval: 2004WARNING: Suicidality and Antidepressant Drugs See full prescribing information for complete boxed warning. • Increased risk of suicidal thinking and behavior in children, adolescents, and young adults taking antidepressants for majordepressive disorder (MDD) and other psychiatric disorders. Cymbalta is not approved for use in pediatric patients (5.1). -----------------------------RECENT MAJOR CHANGES------------------------- Indications and Usage:Chronic Musculoskeletal Pain (1.5)11/2010 Dosage and Administration:Chronic Musculoskeletal Pain (2.1, 2.2) 11/2010 Dosing in Special Populations, Pregnancy (2.3)11/2010 Warnings and Precautions:Effect on Blood Pressure (5.9)11/2010 --------------------------INDICATIONS AND USAGE----------------------------- Cymbalta ® is a serotonin and norepinephrine reuptake inhibitor (SNRI) indicated for: • Major Depressive Disorder (MDD) (1.1) Efficacy was established in four short-term and one maintenance trial in adults (14.1). • Generalized Anxiety Disorder (GAD) (1.2)Efficacy was established in three short-term and one maintenance trial in adults (14.2). • Diabetic Peripheral Neuropathic Pain (DPNP) (1.3) • Fibromyalgia (FM) (1.4)• Chronic Musculoskeletal Pain (1.5) ------------------------DOSAGE AND ADMINISTRATION---------------------- • Cymbalta should generally be administered once daily without regard to meals. Cymbalta should be swallowed whole and should not be chewed or crushed, nor should the capsule be opened and its contents be sprinkled on food or mixed with liquids (2.1). Indication Starting Dose Target DoseMaximum Dose MDD (2.1, 2.2) 40 mg/day to 60 mg/day Acute Treatment: 40mg/day (20 mg twice daily) to 60 mg/day (once daily or as 30 mg twice daily); MaintenanceTreatment: 60 mg/day 120 mg/day GAD (2.1) 60 mg/day 60 mg/day (once daily)120 mg/day DPNP (2.1) 60 mg/day 60 mg/day (once daily)60 mg/day FM (2.1) 30 mg/day 60 mg/day (once daily)60 mg/day Chronic MusculoskeletalPain (2.1)30 mg/day 60 mg/day (once daily) 60 mg/day • Some patients may benefit from starting at 30 mg once daily. • There is no evidence that doses greater than 60 mg/day confers additional benefit, while some adverse reactions were observed to be dose-dependent. • Discontinuing Cymbalta: A gradual dose reduction is recommended to avoid discontinuation symptoms (5.6). -------------------------DOSAGE FORMS AND STRENGTHS------------------20 mg, 30 mg, and 60 mg capsules (3) ------------------------------CONTRAINDICATIONS------------------------------- • Use of a monoamine oxidase inhibitor concomitantly or in close temporal proximity (4.1) • Use in patients with uncontrolled narrow-angle glaucoma (4.2) -------------------------WARNINGS AND PRECAUTIONS---------------------- • Suicidality: Monitor for clinical worsening and suicide risk (5.1). • Hepatotoxicity: Hepatic failure, sometimes fatal, has been reported in patients treated with Cymbalta. Cymbalta should be discontinued in patients who develop jaundice or other evidence of clinically significant liver dysfunction and should not be resumed unless another cause can be established. Cymbalta should not be prescribed to patients with substantial alcohol use or evidence of chronic liver disease (5.2). • Orthostatic Hypotension and Syncope: Cases have been reported with duloxetine therapy (5.3). • Serotonin Syndrome, or Neuroleptic Malignant Syndrome (NMS)-like reactions: Serotonin syndrome or NMS-like reactions have been reported with SSRIs and SNRIs. Discontinue Cymbalta and initiate supportive treatment (5.4, 7.14).• Abnormal Bleeding: Cymbalta may increase the risk of bleeding events. Patients should be cautioned about the risk of bleeding associated with the concomitant use of duloxetine and NSAIDs, aspirin, or other drugs that affect coagulation (5.5, 7.4). • Discontinuation: May result in symptoms, including dizziness, nausea, headache, paresthesia, fatigue, vomiting, irritability, insomnia, diarrhea, anxiety, and hyperhidrosis (5.6). • Activation of mania or hypomania has occurred (5.7). • Seizures: Prescribe with care in patients with a history of seizure disorder (5.8).• Blood Pressure: Monitor blood pressure prior to initiating treatment and periodically throughout treatment (5.9). • Inhibitors of CYP1A2 or Thioridazine: Should not administer with Cymbalta (5.10).• Hyponatremia: Cases of hyponatremia have been reported (5.11). • Hepatic Insufficiency and Severe Renal Impairment: Should ordinarily not be administered to these patients (5.12). • Controlled Narrow-Angle Glaucoma: Use cautiously in these patients (5.12). • Glucose Control in Diabetes: In diabetic peripheral neuropathic pain patients, small increases in fasting blood glucose, HbA 1c , and totalcholesterol have been observed (5.12).• Conditions that Slow Gastric Emptying: Use cautiously in these patients(5.12).• Urinary Hesitation and Retention (5.13).---------------------------------ADVERSE REACTIONS----------------------------• Most common adverse reactions (≥5% and at least twice the incidence ofplacebo patients): nausea, dry mouth, somnolence, fatigue, constipation,decreased appetite, and hyperhidrosis (6.3). To report SUSPECTED ADVERSE REACTIONS, contact Eli Lilly and Company at 1-800-LillyRx (1-800-545-5979) or FDA at 1-800-FDA-1088or /medwatch.---------------------------------DRUG INTERACTIONS----------------------------• Potent inhibitors of CYP1A2 should be avoided (7.1). • Potent inhibitors of CYP2D6 may increase duloxetine concentrations (7.2). • Duloxetine is a moderate inhibitor of CYP2D6 (7.9). --------------------------USE IN SPECIFIC POPULATIONS--------------------- • Pregnancy and Nursing Mothers: Use only if the potential benefit justifies the potential risk to the fetus or child (2.3, 8.1, 8.3). See 17 for PATIENT COUNSELING INFORMATION and Medication GuideRevised: 03/20114 FULL PRESCRIBING INFORMATION: CONTENTS*Drugs7.17 CNSWARNING: SUICIDALITY AND ANTIDEPRESSANT DRUGS7.18 Drugs Highly Bound to Plasma ProteinUSAGEAND1 INDICATIONS8 USE IN SPECIFIC POPULATIONSDisorderDepressive1.1 M ajor8.1 P regnancyDisorderAnxiety1.2 G eneralized8.2 Labor and Delivery1.3 Diabetic Peripheral Neuropathic Pain8.3 N ursingMothers1.4 F ibromyalgiaUse8.4 P ediatric1.5 Chronic Musculoskeletal PainUse8.5 G eriatricADMINISTRATION 8.6 G ender2 DOSAGEANDTreatment 8.7 S moking2.1 I nitialStatusTreatment 8.8 R ace2.2 M aintenance/Continuation/Extended2.3 Dosing in Special Populations 8.9 H epaticInsufficiencyCymbalta 8.10 Severe2.4 D iscontinuingImpairmentRenal2.5 Switching Patients to or from a Monoamine Oxidase Inhibitor9 DRUG ABUSE AND DEPENDENCE3 DOSAGE FORMS AND STRENGTHS 9.2 Abuse4 CONTRAINDICATIONS 9.3 Dependence4.1 Monoamine Oxidase Inhibitors 10 OVERDOSAGE4.2 Uncontrolled Narrow-Angle Glaucoma 10.1 Signs and Symptoms5 WARNINGS AND PRECAUTIONS 10.2 Management of Overdose5.1 Clinical Worsening and Suicide Risk 11 DESCRIPTION5.2 H epatotoxicity12 CLINICAL PHARMACOLOGY5.3 Orthostatic Hypotension and Syncope12.1 Mechanism of Action5.4 Serotonin Syndrome or Neuroleptic Malignant Syndrome12.2 Pharmacodynamics(NMS)-like Reactions12.3 PharmacokineticsBleeding5.5 A bnormal5.6 Discontinuation of Treatment with Cymbalta 13 NONCLINICAL TOXICOLOGY5.7 Activation of Mania/Hypomania 13.1 Carcinogenesis,Mutagenesis, and Impairment of Fertility5.8 S eizures 14 CLINICAL STUDIES5.9 Effect on Blood Pressure 14.1 MajorDisorderDepressive5.10 Clinically Important Drug Interactions 14.2 GeneralizedAnxietyDisorder5.11 Hyponatremia 14.3 Diabetic Peripheral Neuropathic Pain5.12 Use in Patients with Concomitant Illness 14.4 Fibromyalgia5.13 Urinary Hesitation and Retention 14.5 Chronic Musculoskeletal PainTests5.14 Laboratory16 HOW SUPPLIED/STORAGE AND HANDLING6 ADVERSEREACTIONS 16.1 HowSupplied6.1 Clinical Trial Data Sources 16.2 Storage6.2 Adverse Reactions Reported as Reasons for Discontinuation of17 PATIENT COUNSELING INFORMATIONTreatment in Placebo-Controlled Trials17.1 Information on Medication Guide6.3 Most Common Adverse Reactions17.2 Clinical Worsening and Suicide Risk6.4 Adverse Reactions Occurring at an Incidence of 5% or MoreAdministration17.3 MedicationAmong Duloxetine-Treated Patients in Placebo-Controlled17.4 Continuing the Therapy PrescribedTrialsBleeding17.5 Abnormal6.5 Adverse Reactions Occurring at an Incidence of 2% or More17.6 Concomitant MedicationsAmong Duloxetine-Treated Patients in Placebo-ControlledSyndrome17.7 SerotoninTrials17.8 Pregnancy and Breast Feeding6.6 Effects on Male and Female Sexual Function17.9 Alcohol6.7 Vital Sign Changes17.10 Orthostatic Hypotension and Syncope6.8 W eightChanges17.11 Interference with Psychomotor PerformanceChanges6.9 L aboratoryChanges6.10 Electrocardiogram6.11 Other Adverse Reactions Observed During the Premarketing * Sections or subsections omitted from the full prescribing information are notand Postmarketing Clinical Trial Evaluation of Duloxetine listed.6.12 Postmarketing Spontaneous ReportsINTERACTIONS7 DRUG7.1 Inhibitors of CYP1A27.2 Inhibitors of CYP2D67.3 Dual Inhibition of CYP1A2 and CYP2D67.4 Drugs that Interfere with Hemostasis (e.g., NSAIDs, Aspirin,and Warfarin)7.5 L orazepam7.6 T emazepam7.7 Drugs that Affect Gastric Acidity7.8 Drugs Metabolized by CYP1A27.9 Drugs Metabolized by CYP2D67.10 Drugs Metabolized by CYP2C97.11 Drugs Metabolized by CYP3A7.12 Drugs Metabolized by CYP2C197.13 Monoamine Oxidase Inhibitors7.14 SerotonergicDrugs7.15 Triptans7.16 AlcoholFULL PRESCRIBING INFORMATIONWARNING: SUICIDALITY AND ANTIDEPRESSANT DRUGSAntidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of Cymbalta or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Cymbalta is not approved for use in pediatric patients. [see Warnings and Precautions (5.1), Use in Specific Populations (8.4), and Information for Patients (17.2).]USAGE1 INDICATIONSAND1.1 Major Depressive DisorderCymbalta is indicated for the treatment of major depressive disorder (MDD). The efficacy of Cymbalta was established in four short-term and one maintenance trial in adults [see Clinical Studies (14.1)].A major depressive episode (DSM-IV) implies a prominent and relatively persistent (nearly every day for at least 2 weeks) depressed or dysphoric mood that usually interferes with daily functioning, and includes at least 5 of the following 9 symptoms: depressed mood, loss of interest in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, or a suicide attempt or suicidal ideation.DisorderAnxiety1.2 GeneralizedCymbalta is indicated for the treatment of generalized anxiety disorder (GAD). The efficacy of Cymbalta was established in three short-term trials and one maintenance trial in adults [see Clinical Studies (14.2)].Generalized anxiety disorder is defined by the DSM-IV as excessive anxiety and worry, present more days than not, for at least 6 months. The excessive anxiety and worry must be difficult to control and must cause significant distress or impairment in normal functioning. It must be associated with at least 3 of the following 6 symptoms: restlessness or feeling keyed up or on edge, being easily fatigued, difficulty concentrating or mind going blank, irritability, muscle tension, and/or sleep disturbance.1.3 Diabetic Peripheral Neuropathic PainCymbalta is indicated for the management of neuropathic pain (DPNP) associated with diabetic peripheral neuropathy [see Clinical Studies (14.3)].1.4 FibromyalgiaCymbalta is indicated for the management of fibromyalgia (FM) [see Clinical Studies (14.4)].PainMusculoskeletal1.5 ChronicCymbalta is indicated for the management of chronic musculoskeletal pain. This has been established in studies in patients with chronic low back pain (CLBP) and chronic pain due to osteoarthritis [see Clinical Studies (14.5)].ADMINISTRATIONAND2 DOSAGECymbalta should be swallowed whole and should not be chewed or crushed, nor should the capsule be opened and its contents sprinkled on food or mixed with liquids. All of these might affect the enteric coating. Cymbalta can be given without regard to meals.2.1 Initial TreatmentMajor Depressive Disorder — Cymbalta should be administered at a total dose of 40 mg/day (given as20 mg twice daily) to 60 mg/day (given either once daily or as 30 mg twice daily). For some patients, it may be desirable to start at 30 mg once daily for 1 week, to allow patients to adjust to the medication before increasing to 60 mg once daily. While a 120 mg/day dose was shown to be effective, there is no evidence that doses greater than 60 mg/day confer any additional benefits. The safety of doses above 120 mg/day has not been adequately evaluated [see Clinical Studies (14.1)].Generalized Anxiety Disorder — For most patients, the recommended starting dose for Cymbalta is 60 mg administered once daily. For some patients, it may be desirable to start at 30 mg once daily for 1 week, to allowpatients to adjust to the medication before increasing to 60 mg once daily. While a 120 mg once daily dose was shown to be effective, there is no evidence that doses greater than 60 mg/day confer additional benefit. Nevertheless, if a decision is made to increase the dose beyond 60 mg once daily, dose increases should be in increments of 30 mg once daily. The safety of doses above 120 mg once daily has not been adequately evaluated [see Clinical Studies (14.2)].Diabetic Peripheral Neuropathic Pain — The recommended dose for Cymbalta is 60 mg administered once daily. There is no evidence that doses higher than 60 mg confer additional significant benefit and the higher dose is clearly less well tolerated [see Clinical Studies (14.3)]. For patients for whom tolerability is a concern, a lower starting dose may be considered.Since diabetes is frequently complicated by renal disease, a lower starting dose and gradual increase in dose should be considered for patients with renal impairment [see Clinical Pharmacology (12.3) and Dosage and Administration (2.3)].Fibromyalgia — The recommended dose for Cymbalta is 60 mg administered once daily. Treatment should begin at 30 mg once daily for 1 week, to allow patients to adjust to the medication before increasing to 60 mg once daily. Some patients may respond to the starting dose. There is no evidence that doses greater than 60 mg/day confer additional benefit, even in patients who do not respond to a 60 mg dose, and higher doses are associated with a higher rate of adverse reactions [see Clinical Studies (14.4)].Chronic Musculoskeletal Pain — The recommended dose for Cymbalta is 60 mg once daily. Dosing may be started at 30 mg for one week, to allow patients to adjust to the medication before increasing to 60 mg once daily. There is no evidence that higher doses confer additional benefit, even in patients who do not respond to a 60 mg dose, and higher doses are associated with a higher rate of adverse reactions [see Clinical Studies (14.5)].2.2 Maintenance/Continuation/ExtendedTreatmentMajor Depressive Disorder — It is generally agreed that acute episodes of major depression require several months or longer of sustained pharmacologic therapy. Maintenance of efficacy in MDD was demonstrated with Cymbalta as monotherapy. Cymbalta should be administered at a total dose of 60 mg once daily. Patients should be periodically reassessed to determine the need for maintenance treatment and the appropriate dose for such treatment [see Clinical Studies (14.1)].Generalized Anxiety Disorder — It is generally agreed that episodes of generalized anxiety disorder require several months or longer of sustained pharmacological therapy. Maintenance of efficacy in GAD was demonstrated with Cymbalta as monotherapy. Cymbalta should be administered in a dose range of 60-120 mg once daily. Patients should be periodically reassessed to determine the continued need for maintenance treatment and the appropriate dose for such treatment [see Clinical Studies (14.2)].Diabetic Peripheral Neuropathic Pain — As the progression of diabetic peripheral neuropathy is highly variable and management of pain is empirical, the effectiveness of Cymbalta must be assessed individually. Efficacy beyond 12 weeks has not been systematically studied in placebo-controlled trials.Fibromyalgia — Fibromyalgia is recognized as a chronic condition. The efficacy of Cymbalta in the management of fibromyalgia has been demonstrated in placebo-controlled studies up to 3 months. The efficacy of Cymbalta was not demonstrated in longer studies; however, continued treatment should be based on individual patient response.Chronic Musculoskeletal Pain — The efficacy of Cymbalta has not been established in placebo-controlled studies beyond 13 weeks.2.3 Dosing in Special PopulationsHepatic Insufficiency — It is recommended that Cymbalta should ordinarily not be administered to patients with any hepatic insufficiency [see Warnings and Precautions (5.12) and Use in Specific Populations (8.9)].Severe Renal Impairment — Cymbalta is not recommended for patients with end-stage renal disease or severe renal impairment (estimated creatinine clearance <30 mL/min) [see Warnings and Precautions (5.12) and Use in Specific Populations (8.10)].Elderly Patients — No dose adjustment is recommended for elderly patients on the basis of age. As with any drug, caution should be exercised in treating the elderly. When individualizing the dosage in elderly patients, extra care should be taken when increasing the dose [see Use in Specific Populations (8.5)].Pregnant Women — There are no adequate and well-controlled studies in pregnant women; therefore, Cymbalta should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus [see Use in Specific Populations (8.1)].Lilly maintains a pregnancy registry to monitor the pregnancy outcomes of women exposed to Cymbalta while pregnant. Healthcare providers are encouraged to register any patient who is exposed to Cymbalta during pregnancy by calling the Cymbalta Pregnancy Registry at 1-866-814-6975 or by visitingNursing Mothers — Because the safety of duloxetine in infants is not known, nursing while on Cymbalta is not recommended [see Use in Specific Populations (8.3)].Cymbalta2.4 DiscontinuingSymptoms associated with discontinuation of Cymbalta and other SSRIs and SNRIs have been reported. A gradual reduction in the dose rather than abrupt cessation is recommended whenever possible [see Warnings and Precautions (5.6)].2.5 Switching Patients to or from a Monoamine Oxidase InhibitorAt least 14 days should elapse between discontinuation of an MAOI and initiation of therapy with Cymbalta. In addition, at least 5 days should be allowed after stopping Cymbalta before starting an MAOI [see Contraindications (4.1) and Warnings and Precautions (5.4)].3 DOSAGE FORMS AND STRENGTHSCymbalta is available as delayed release capsules:20 mg opaque green capsules imprinted with “Lilly 3235 20mg”30 mg opaque white and blue capsules imprinted with “Lilly 3240 30mg”60 mg opaque green and blue capsules imprinted with “Lilly 3237 60mg”60 mg opaque green and blue capsules imprinted with “Lilly 3270 60mg”4 CONTRAINDICATIONS4.1 Monoamine Oxidase InhibitorsConcomitant use in patients taking monoamine oxidase inhibitors (MAOIs) is contraindicated due to the risk of serious, sometimes fatal, drug interactions with serotonergic drugs. These interactions may include hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes that include extreme agitation progressing to delirium and coma. These reactions have also been reported in patients who have recently discontinued serotonin reuptake inhibitors and are then started on an MAOI. Some cases presented with features resembling neuroleptic malignant syndrome [see Dosage and Administration (2.5) and Warnings and Precautions (5.4)].GlaucomaNarrow-Angle4.2 UncontrolledIn clinical trials, Cymbalta use was associated with an increased risk of mydriasis; therefore, its use should be avoided in patients with uncontrolled narrow-angle glaucoma [see Warnings and Precautions (5.12)].PRECAUTIONSAND5 WARNINGS5.1 Clinical Worsening and Suicide RiskPatients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern, however, that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment.Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18-24) with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants compared to placebo in adults aged 65 and older.The pooled analyses of placebo-controlled trials in children and adolescents with MDD, obsessive compulsive disorder (OCD), or other psychiatric disorders included a total of 24 short-term trials of 9 antidepressant drugs in over 4400 patients. The pooled analyses of placebo-controlled trials in adults with MDD or other psychiatric disorders included a total of 295 short-term trials (median duration of 2 months) of 11 antidepressant drugs in over 77,000 patients. There was considerable variation in risk of suicidality among drugs, but a tendency toward an increase in the younger patients for almost all drugs studied. There were differences in absolute risk of suicidality across the different indications, with the highest incidence in MDD. The risk of differences (drug vs placebo), however, were relatively stable within age strata and across indications. These risk differences (drugplacebo difference in the number of cases of suicidality per 1000 patients treated) are provided in Table 1.Table 1Age Range Drug-Placebo Difference in Number of Cases of Suicidalityper 1000 Patients TreatedIncreases Compared to Placebo<18 14 additional cases18-24 5 additional casesDecreases Compared to Placebo25-64 1fewercase ≥65 6fewercasesNo suicides occurred in any of the pediatric trials. There were suicides in the adult trials, but the numberwas not sufficient to reach any conclusion about drug effect on suicide.It is unknown whether the suicidality risk extends to longer-term use, i.e., beyond several months. However,there is substantial evidence from placebo-controlled maintenance trials in adults with depression that the use ofantidepressants can delay the recurrence of depression.All patients being treated with antidepressants for any indication should be monitored appropriatelyand observed closely for clinical worsening, suicidality, and unusual changes in behavior, especially duringthe initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases.The following symptoms, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness,impulsivity, akathisia (psychomotor restlessness), hypomania, and mania, have been reported in adult and pediatricpatients being treated with antidepressants for major depressive disorder as well as for other indications, bothpsychiatric and nonpsychiatric. Although a causal link between the emergence of such symptoms and either theworsening of depression and/or the emergence of suicidal impulses has not been established, there is concern thatsuch symptoms may represent precursors to emerging suicidality.Consideration should be given to changing the therapeutic regimen, including possibly discontinuing themedication, in patients whose depression is persistently worse, or who are experiencing emergent suicidality orsymptoms that might be precursors to worsening depression or suicidality, especially if these symptoms are severe,abrupt in onset, or were not part of the patient’s presenting symptoms.If the decision has been made to discontinue treatment, medication should be tapered, as rapidly as isfeasible, but with recognition that discontinuation can be associated with certain symptoms [see Dosage andAdministration (2.4) and Warnings and Precautions (5.6) for descriptions of the risks of discontinuation ofCymbalta].Families and caregivers of patients being treated with antidepressants for major depressive disorderor other indications, both psychiatric and nonpsychiatric, should be alerted about the need to monitorpatients for the emergence of agitation, irritability, unusual changes in behavior, and the other symptomsdescribed above, as well as the emergence of suicidality, and to report such symptoms immediately to healthcare providers. Such monitoring should include daily observation by families and caregivers. Prescriptionsfor Cymbalta should be written for the smallest quantity of capsules consistent with good patientmanagement, in order to reduce the risk of overdose.Screening Patients for Bipolar Disorder — A major depressive episode may be the initial presentation ofbipolar disorder. It is generally believed (though not established in controlled trials) that treating such an episodewith an antidepressant alone may increase the likelihood of precipitation of a mixed/manic episode in patients at riskfor bipolar disorder. Whether any of the symptoms described above represent such a conversion is unknown.However, prior to initiating treatment with an antidepressant, patients with depressive symptoms should beadequately screened to determine if they are at risk for bipolar disorder; such screening should include a detailedpsychiatric history, including a family history of suicide, bipolar disorder, and depression. It should be noted thatCymbalta (duloxetine) is not approved for use in treating bipolar depression.5.2 HepatotoxicityThere have been reports of hepatic failure, sometimes fatal, in patients treated with Cymbalta. These caseshave presented as hepatitis with abdominal pain, hepatomegaly, and elevation of transaminase levels to more thantwenty times the upper limit of normal with or without jaundice, reflecting a mixed or hepatocellular pattern of liverinjury. Cymbalta should be discontinued in patients who develop jaundice or other evidence of clinically significantliver dysfunction and should not be resumed unless another cause can be established.Cases of cholestatic jaundice with minimal elevation of transaminase levels have also been reported. Otherpostmarketing reports indicate that elevated transaminases, bilirubin, and alkaline phosphatase have occurred inpatients with chronic liver disease or cirrhosis.。
盐酸度洛西丁
作用机制
盐酸度洛西汀是一种5HT/去甲肾上腺素再摄取抑制剂，通过抑制5HT和去甲肾上腺素再摄取来提高这些神经 递质的含量，起到抗抑郁的作用。度洛西汀对抑郁症的其他躯体症状如全身疼痛和胃肠紊乱有疗效，因而比抗抑 郁药物具有优势，这些症状在现有常规疗法中未予治疗。
市场前景
Frost & Sullivan最新的健康战略分析预测，到2006年，美国抗抑郁症药物的收入最高可达140亿美元。度 洛西汀有望在2003年底正式进入美国市场销售。分析家预测，到2006年，度洛西汀年度最高销售额可达6亿美元。
行政保护
国家食品药品监督管理局药品行政保护公告 第九十二号（授权公告） 申请人所在国：美国 申请人：礼来公司 申请药品名称： 通用名：盐酸度洛西汀 （Duloxetine hydrochloride） 商品名：欣百达(Cymbalta)肠溶胶囊 授权号：B-US 授权日：2006年8月14日 药品行政保护办公室对该药品的申请文件进行实质审查后，认为符合行政保护条件，即日起授予行政保护， 特
谢谢观看
虽然新型抗抑郁剂不断上市，但5-羟色胺再摄制抑制剂的销售量约占全部抗抑郁剂的一半，且治疗成本较低； 再之度洛西汀具有新型的作用机制，即抑制去甲肾上腺素的再摄取。所以在我国开发度洛西汀有着良好前景。度 洛西汀在中国尚无销售数据，预计至中国上市头一年市场份额将占国内5亿元抗抑郁药市场的1%；按照本类药在 世界范围内的递增速度，在2009年将在国内达到5000万～1亿元人民币。它必产生很大的社会效益及经济效益。
盐酸度洛西丁
化学物质
01 理化性质
03 适应症
目录
02 主治功能 04 副作用
05 作用机制
07 行政保护
目录
06 9NOS.HCl;C18H20ClNOS；英文名是Cymbalta；分子量是333.88；CAS号是34-9。
盐酸度洛西汀肠溶胶囊
盐酸度洛西汀肠溶胶囊【药品名称】通用名称：盐酸度洛西汀肠溶胶囊英文名称：Duloxetine Hydrochloride Enteric-coated Capsules【成份】盐酸度洛西汀。
【适应症】用于治疗抑郁症。
【用法用量】1.起始治疗推荐欣百达的起始剂量为40mg/日(20mg一日三次)至60mg/日(一日一次或30mg一日二次)，不考虑进食情况。
现有的临床研究数据未证实剂量超过60mg/日将增加疗效。
2.维持/继续/长期治疗一般认为抑郁症的急性发作需要数月或更长时间的药物治疗，但尚没有充足的试验资料来确定患者应该连续服用度洛西汀治疗达多长时间。
对此类患者，应对其接受维持治疗的必要性以及相应所需的剂量作定期评估。
3.特殊人群肾脏功能受损患者的用量：对于晚期肾脏疾病(需要透析的)患者，或有严重肾脏功能损害(估计肌酐清除率【不良反应】以下不良反应数据基于所有关于盐酸度洛西汀肠溶胶囊临床试验资料。
一般不良反应头晕、恶心、头疼，也见于度洛西汀停药后，发生率≥5%。
在安慰剂对照的临床试验中，度洛西汀治疗伴随小的ALT、AST、CRK从基线至终点平均值升高;与对照组相比，度洛西汀治疗的病人可有罕见的、暂的异常值。
血糖调整-在3项治疗糖尿病性神经痛的临床试验中，平均糖尿病持续时间为12年，平均空腹血糖基线值为176mg/dL，平均血红蛋白(HBALC)基线值为7.81%。
在这3项试验的最初12周急性治疗期，度洛西汀治疗组和安慰剂对照组均稳定。
在治疗持续到52周时，度洛西汀治疗姐和安慰剂组均出现HBALC升高，度洛西汀治疗平均增高值比安慰组高0.3%。
尽管规治疗组病人显示轻度降低，但空腹血糖和总胆固醇显示小幅增高。
停药后，有报告停药后症状，最常见报告的症状包括下列临床试验中突然停服度洛西汀有头晕、恶心、头疼、感觉异常、呕吐、兴奋、梦魇、失眠、腹泻、焦虑、多汗和眩晕。
上市后使用度洛西汀治疗出现的自发不良反应报告下列不良反应发生率(0.01%-【禁忌】1.过敏度洛西汀肠溶胶囊禁用于已知对度洛西汀肠溶胶囊或产品中任何非活性成分过敏的患者。
度洛西汀片
盐酸度洛西汀肠溶胶囊产品简介一、产品介绍【适应症】治疗抑郁症【用法用量】起始治疗：推荐盐酸度洛西汀的起始剂量为40mg/日（20mg一日二次）至60mg/日（一日一次或30mg一日二次），不考虑进食情况。
现有的临床研究数据未证实剂量超过60mg/日将增加疗效。
维持／继续／长期治疗：一般认为抑郁症的急性发作需要数月或更长时间的药物治疗，但尚没有充足的试验资料来确定患者应该连续服用度洛西汀治疗达多长时间。
对此类患者，应对其接受维持治疗的必要性以及相应所需的剂量作定期评估。
特殊人群用药肾脏功能受损患者：用量一对于晚期肾脏疾病（需要透析的）患者，或有严重肾脏功能损害（估计肌酐清除率<30 mL/min的）患者，建议不用盐酸度洛西汀（见药理毒理）。
肝功能不全的患者：用量一建议有任何肝功能不全的患者避免服用盐酸度洛西汀（见药理毒理和注意事项）老年患者：用量一对于老年患者，建议不必根据年龄调整剂量。
与任何药物一样，治疗老年患者时应该慎重。
在老年患者中个体化调整剂量时，增加剂量时应该额外小心。
妊娠后三个月的女性患者：治疗一在妊娠后三个月内接触SSRIs或SNRls（五羟色胺和去甲肾上腺素再摄取抑制剂）的新生儿，产生的并发症会导致住院时间延长、需要呼吸支持和管道喂食（见注意事项）。
当孕期女性用度洛西汀治疗时，在妊娠后三个月，医生应对治疗的潜在风险和获益进行认真的评价。
医生应考虑在妊娠晚期逐渐减度洛西汀的用量。
度洛西汀停药已有报道盐酸度洛西汀及其他SSRI和SNRIs药物的停药反应（见注意事项）。
停药时应对这些症状进行监测。
建议尽可能的逐渐减药，而不是骤停药物。
由于减少药物剂量或停药而引起了无法耐受的症状时，可以考虑恢夏使用以往的的处方剂量。
随后再以更慢的的速度减药。
与单胺氧化酶抑制剂(MOA I）间的换药MOAT停药后至少14天才可开始盐酸度洛西汀的治疗。
盐酸度洛西汀停药后至少5天才可以开始MOAT的治疗（见禁忌和警告）。
欣百达与怡诺思比较PPT课件
医生评价和反馈
01
疗效评价
医生普遍认为欣百达和怡诺思在各自的治疗领域内具有显著疗效，能够
有效改善患者的症状和生活质量。
02
安全性评价
两种药物在安全性方面表现良好具体情况调整药物剂量和使用方法。
03
使用建议
医生会根据患者的具体病情和身体状况，选择合适的药物进行治疗。同
怡诺思临床应用案例
精神分裂症治疗
怡诺思是治疗精神分裂症的首选 药物之一。能够有效控制幻觉、 妄想等症状，改善患者的生活质
量。
双相情感障碍治疗
怡诺思在双相情感障碍的治疗中 也具有重要地位。能够稳定患者 的情绪，减少躁狂和抑郁的发作
频率。
焦虑症治疗
怡诺思也可用于焦虑症的治疗， 特别是对于伴有精神症状的焦虑
05 临床应用与案例分享
欣百达临床应用案例
慢性疼痛治疗
抑郁症辅助治疗
欣百达在治疗慢性疼痛方面表现出色， 如神经性疼痛、纤维肌痛等。通过调节 神经递质，有效缓解疼痛症状。
在抑郁症治疗中，欣百达可作为辅助 治疗药物，与抗抑郁药联合使用，提 高治疗效果。
焦虑障碍治疗
欣百达对于广泛性焦虑障碍、社交焦虑 障碍等有良好的治疗效果。能够显著改 善患者的焦虑情绪，提高生活质量。
药物相互作用少
怡诺思与其他药物的相互作用 较少，降低了联合用药时的风 险。
长期疗效稳定
经过长期治疗，怡诺思的疗效 保持稳定，有助于患者长期康
复。
04 欣百达与怡诺思比较分析
成分与功效对比
欣百达主要成分及功效
含有特定的活性成分，主要针对某一 类疾病或症状有显著疗效。
怡诺思主要成分及功效
含有另一种不同的活性成分，针对另 一类疾病或症状进行治疗，疗效显著 。
盐酸度洛西汀肠溶胶囊的作用
盐酸度洛西汀肠溶胶囊的作用
随着社会压力的不断增长，有一些抗压能力比较弱的人群就容易患上抑郁症，这种疾病的患者是不可以单独进行生活的，否则就容易出现很多意外，目前来看治疗抑郁症疾病的方法不是很多，往往都是使用盐酸度洛西汀肠溶胶囊，这种胶囊可以帮助患者进行康复，下面让我们来看看盐酸度洛西汀肠溶胶囊的详细介绍吧。
第一，盐酸度洛西汀肠溶胶囊是不可以一次性停药的。
以往的例子表明，盐酸度洛西汀肠溶胶囊一次性停药会出现肝脏毒性一度洛西汀增加血清转氨酶水平的风险，并伴有胆红素升高，是严重肝脏损害的重要指标。
因此，盐酸度洛西汀肠溶胶囊停药建议尽可能的逐渐减药，而不是骤停药物，同时应注意观察患者有无上述症状的出现。
若患者由于减少药物剂量或停药而引起了无法耐受的症状时，可以考虑应用以往的处方剂量。
然后，临床医生再以一个更慢的速度减药。
第二，有研究者对盐酸度洛西汀肠溶胶囊的停药症状做过系统研究。
在抑郁症患者中进行的为期9周的安慰剂对照试验中，骤停药物，观察到度洛西汀治疗的患者发生率2%或明显高于骤停安慰剂的症状包括：头晕，恶心，头痛，感觉异常，呕吐，易怒，噩梦。
虽然上述不良反应具有自限性，但有些很严重。
因此，建议患者必须要逐步停药。
第三，抑郁症患者在停药后尽量保持心情舒畅，有乐观、豁达的精神、坚强战胜疾病的信心;注意保持充足的睡眠，避免过度劳累，注意劳逸结合，注意生活的规律性。
希望大家通过这篇文章能够了解到了关于盐酸度洛西汀肠
溶胶囊的信息，并且多去关注不同药物的相关资讯，扩大自己对药物的了解与认识。
盐酸度洛西汀肠溶胶囊20140728
盐酸度洛西汀肠溶胶囊项目立项论证意见稿1.简介盐酸度洛西汀(duloxetine hydrochloride/Cymbaha，以下简称为度洛西汀)是美国礼来Eli Lilly公司开发的一个5一羟色胺和去甲肾上腺素再摄取抑制剂。
5一羟色胺和去甲肾上腺素均属中枢神经递质，在调控情感和对疼痛的敏度方面起着重要作用。
度洛西汀能够抑制神经元对5一羟色胺和去甲肾上腺素的再摄取，由此提高这两种中枢神经递质在大脑和脊髓中的浓度，故可用于治疗某些心境疾病如抑郁症和焦虑症以及缓解中枢性疼痛如糖尿病外周神经病性疼痛和妇女纤维肌痛等。
度洛西汀也能作用于尿道中的5一羟色胺和去甲肾上腺素受体，从而增强尿道括约肌的神经性紧张程度和收缩能力，所以对妇女应激性尿失禁症治疗也有效。
度洛西汀为口服肠溶胶囊制剂，2004年8月首次在美国获得批准后，现已在70余个国家上市。
度洛西汀2006年的全球销售额即超过13亿美元，2007年和2008年的销售额又分别大幅增至2l亿和27亿美元，是近年世界范围内销售额增长最快的药物之一。
化学名称:盐酸度洛西汀;(S)-(+)-N-甲基-3-(1-萘氧基)-3-(2-噻吩)-丙胺盐酸盐Duloxetinehydrochloride;N-Methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine分子式：C18H19NOS.HCl;C18H20ClNOS分子量：333.88结构式：CAS：136434-34-9【用途】对于抑郁症、糖尿病性周围神经病引起疼痛以及紧张性尿失禁有疗效。
2.原料药来源国家局已批2家企业生产，0家进口原料药。
如下：1.盐酸度洛西汀(国药准字H261262上海万代制药有限公司86977746)2.盐酸度洛西汀 (国药准字H20130055江苏恩华药业股份有限公司86901435000170)3.国内上市批准情况国内盐酸度洛西汀主要为肠溶片和肠溶胶囊。
盐酸度洛西汀肠溶胶囊防治慢性偏头痛临床疗效分析
盐酸度洛西汀肠溶胶囊防治慢性偏头痛临床疗效分析闫巧眉【摘要】Objective Study of the clinical effect of chronic migraine disease using Duloxetine Hydrochloride Enteric Capsule prevention. Methods 112 cases in our hospital in 2012 April ~2013 April between the diagnosis and treatment of patients,according to the method of treatment will be divided into two groups,a control group of 56 patients using Lesong + fiunarizine combined therapy, the observation group of 56 patients on the basis of basic treatment,application of Duloxetine Hydrochloride Enteric Capsule treatment, comparison of two groups of patients with clinical curative effect. Results Through 3 months of treatment of two groups of patients, the observation group patients of migraine relief rate was significantly better than the control group, the differences between the two groups were significant, with statistical significance (P<0.05), the patients in the observation group were SAS, SDS score was lower than the control group obviously degree, the differences between the two groups were significant, with statistical significance (P<0.05). Conclusion Duloxetine Hydrochloride Enteric Capsule combined with fiunarizine, Lesong clinical effect of treatment of chronic migraine significantly,can effectively prevent the patients with depression and anxiety.%目的：研究慢性偏头痛疾病运用盐酸度洛西汀肠溶胶囊防治的临床效果。
临床度洛西汀适应证、用法用量、禁忌证、严重不良反应、相互作用及注意事项
临床度洛西汀适应证、用法用量、禁忌证、严重不良反应、相互作用及注意事项适应证与用法用量适应证①用于治疗抑郁症；②用于治疗广泛性焦虑障碍；③用于治疗慢性肌肉骨骼疼痛。
用法用量1）肠溶片：广泛性焦虑障碍：推荐的起始剂量为 60 mg/日，部分患者可能需要以 30 mg/日为起始剂量，一周后调整至 60 mg/日；对于 60 mg/日的剂量效果不佳的患者，可以考虑将剂量提高到 90 mg/日，最高可增至 120 mg/日。
维持治疗的剂量范围是 60～120 mg/日。
2）肠溶胶囊：①抑郁症：推荐的起始剂量为 40 mg/日（20 mg 一日二次）至60 mg/日（一日一次或 30 mg 一日二次），不考虑进食情况。
部分患者可能需要以 30 mg/日为起始剂量，一周后调整至 60 mg/日。
维持治疗的剂量范围是 60 mg/日。
②广泛性焦虑障碍：推荐的起始剂量为 60 mg/日，一些患者可能需要以 30 mg/日为起始剂量，一周后调整至 60 mg/日。
一些对于60 mg/日的剂量不能充分应答的患者，可以考虑将剂量提高到 90 mg/日，最高可增至 120 mg/日。
维持治疗的剂量范围是 60～120 mg/日。
禁忌证1）禁忌在已经用单胺氧化酶抑制剂（MAOI）治疗精神疾病的患者中使用度洛西汀，因为这会增加患者发生血清素综合征的风险。
停用 MAOI后14 日内禁用本药。
2）禁止对正在接受利奈唑胺或静脉注射亚甲蓝等单胺氧化酶抑制剂（MAOI）治疗的患者中使用度洛西汀治疗，因为这会增加患者发生血清素综合征的风险。
严重不良反应肝胆系统：肝毒性；血管系统：体位性低血压，跌倒和晕厥，血压升高；精神系统：躁狂症/低躁狂症的发作，癫痫发作，严重抑郁症，广泛性焦虑症；眼部：闭角型青光眼；泌尿系统：尿潴留；骨骼肌肉系统：纤维肌痛，骨关节炎引起的慢性疼痛，慢性腰背痛。
相互作用禁忌：度洛西汀-CYP1A2 抑制剂（强力）严重：度洛西汀-盐酸环丙沙星注意事项建议尽可能减少剂量而不是突然停止度洛西汀缓释胶囊停用后的不良反应包括：头晕、头痛、恶心、腹泻、感觉异常、烦躁不安、呕吐、失眠、焦虑、多汗症和疲劳等。
度洛西汀
下列噻吩化合物经Marmieh反应，然后用Yarnaguchi-Masher-Pohland(YMP)复合试剂LiAl2H2在乙醚中，于 -78℃进行不对称还原，而后加入氢溴酸，使还原产物以氢溴酸盐形式得到。再和1-氟萘进行烷基化反应，最后 去甲基化，产物以草酸盐的形式得到。
相关药品说AOIs)均抑制5-HT代谢，两药合用易出现严重不良反应，如中枢神经毒性或5HT综合征(其临床表现为高血压、高热、肌阵挛、激惹及烦躁不安、反射亢进、出汗、寒战及震颤)，甚至死亡。 禁止本药与MAOIs合用；停用MAOIs 14天后才能使用本药；停用本药5天后才能使用MAOIs。2.卷曲霉素、依诺沙 星、氟伏沙明及奎尼丁可抑制本药的代谢，增加本药血药浓度(或生物利用度)及毒性，两者合用须监测不良反应， 需要时减少本药剂量。3.本药与氟西汀、帕罗西汀合用，互相抑制代谢，两药的生物利用度、血药浓度均增加， 发生严重不良反应的危险性增加，合用时应调整两药剂量。4.本药可抑制三环类抗抑郁药(如阿米替林)的代谢， 两者合用，本药可增加后者的生物利用度、血药浓度及毒性。如必须合用，应密切监测三环类抗抑郁药的血药浓 度、中毒的症状及体征(抗胆碱能作用、过度镇静、意识混乱及心律失常)。5.本药可抑制吩噻嗪类药(奋乃静)的 代谢，增加后者的血药浓度及毒性(过度镇静、意识障碍、心律失常、直立性低血压、高热及锥体外系反应)。两 者合用应监测不良反应，必要时减少剂量。6.本药可抑制硫利达嗪的代谢，增加后者血药浓度及心脏毒性(QT间 期延长、尖端扭转性室性心动过速、心脏停搏)，两者不应合用。7.本药可抑制Ic类抗心律失常药的代谢，增加 后者的血药浓度及心脏毒性。两者合用应密切监测Ic类抗心律失常药的血药浓度及心电图。8.本药与中枢神经系 统抑制药合用，可引起精神运动性障碍恶化，禁止两者合用。食物不影响本药的血药峰浓度，但可减慢吸收，并 降低吸收度10% 。
抗抑郁药怡诺思、博乐欣、奥思平等说明书介绍
用于治疗各种抑郁 状态。也常用于治 疗强迫性神经症、 恐怖性神经症。
用于治疗严重抑郁 症及难治性抑郁症 。
用于治疗抑郁症及 焦虑性神经症。
用于治疗抑郁症 。
本品适用于治疗各种类型 抑郁症 (包括伴有焦虑的抑郁
症) 及广泛性焦虑症。
起始治疗
用法用 量
成人常用量开始一 次25mg，一日2～3 次，然后根据病情 和耐受情况逐渐增 至一日150～ 250mg，一日3次， 高量一日不超过 300mg，维持量一 日50～150mg。
抗抑郁药
--怡诺思、博乐欣、奥思平等说明书 介绍和学习
杭州第七人民医院 何俊
主要内容
五种抗抑郁药说明书介绍 抗抑郁药的分类、作用机制、不良反应 抑郁症的病因、机制、临床主要表现 抗抑郁药的临床合理选择和使用
盐酸阿米替林片 (25mg*100片/瓶,21元/瓶)
盐酸多塞平片 (25mg*100片/盒)
怡诺思缓释胶囊应该在早 晨或晚间一个相对崮定时 间和食物同时服用，每日 一次。起始剂量为每天75 毫克,最大剂量为每天225 毫克。当前应用盐酸文拉 法辛常释片治疗的抑郁症 患者可以换用每日治疗剂 量几乎等同的缓释胶囊， 如服用37.5mg文拉法辛每 日两次，可换用75mg的缓 释胶囊，每日一次。
盐酸阿米替林片
可有罕见的、暂 绝大多数的停药反应是轻
时的异常值。 度的并且无需治疗即可恢
1. 过敏：本品 禁用于对盐酸文拉法辛或
禁用于已知对度 任何赋形剂过敏的患者。
严重心脏病、近期 洛西汀或产品中 禁用于同时服用MAOls的患
有心肌梗死发作史 任何非活性成份 者：在停用MAOIs后至少14
、癫痫、青光眼、 过敏的患者。 天内不得开始使用文拉法
盐酸度洛西汀肠溶胶囊20140728
盐酸度洛西汀肠溶胶囊项目立项论证意见稿1.简介盐酸度洛西汀(duloxetine hydrochloride/Cymbaha，以下简称为度洛西汀)是美国礼来Eli Lilly公司开发的一个5一羟色胺和去甲肾上腺素再摄取抑制剂。
5一羟色胺和去甲肾上腺素均属中枢神经递质，在调控情感和对疼痛的敏度方面起着重要作用。
度洛西汀能够抑制神经元对5一羟色胺和去甲肾上腺素的再摄取，由此提高这两种中枢神经递质在大脑和脊髓中的浓度，故可用于治疗某些心境疾病如抑郁症和焦虑症以及缓解中枢性疼痛如糖尿病外周神经病性疼痛和妇女纤维肌痛等。
度洛西汀也能作用于尿道中的5一羟色胺和去甲肾上腺素受体，从而增强尿道括约肌的神经性紧张程度和收缩能力，所以对妇女应激性尿失禁症治疗也有效。
度洛西汀为口服肠溶胶囊制剂，2004年8月首次在美国获得批准后，现已在70余个国家上市。
度洛西汀2006年的全球销售额即超过13亿美元，2007年和2008年的销售额又分别大幅增至2l亿和27亿美元，是近年世界范围内销售额增长最快的药物之一。
化学名称:盐酸度洛西汀;(S)-(+)-N-甲基-3-(1-萘氧基)-3-(2-噻吩)-丙胺盐酸盐Duloxetinehydrochloride;N-Methyl-gama-(1-naphthalenyloxy)-2-thiophenepropanamine分子式：C18H19NOS.HCl;C18H20ClNOS分子量：333.88结构式：CAS：136434-34-9【用途】对于抑郁症、糖尿病性周围神经病引起疼痛以及紧张性尿失禁有疗效。
2.原料药来源国家局已批2家企业生产，0家进口原料药。
如下：1.盐酸度洛西汀(国药准字H261262上海万代制药有限公司86977746)2.盐酸度洛西汀 (国药准字H20130055江苏恩华药业股份有限公司86901435000170)3.国内上市批准情况国内盐酸度洛西汀主要为肠溶片和肠溶胶囊。
奥思平 说明书
奥思平说明书注意事项：一般注意事项肝脏毒性-度洛西汀有增加血清转氨酶水平的风险。
肝脏转氨酶升高导致0.4%(31/8454) 度洛西汀治疗的患者中断治疗。
这些患者出现转氨酶升高的时间中位数为2个月。
在抑郁症患者中进行的对照试验中，0.9%(8/930)用度洛西汀治疗的患者ALT升高超过正常上限3倍以上，而安慰剂组中为0.3%(2/652)。
所有安慰剂对照研究中，度洛西汀组中有1% (39/3732)的患者ALT升高超过正常上限3倍以上，而安慰剂组中为0.2%(6/2568)。
固定剂量的安慰剂对照研究中，有证据显示ALT升高超过正常上限3倍和AST升高超过正常上限5倍，与药物剂量有量效关系。
上市后监测还报道出现腹痛、肝肿大、伴有或无黄疸的转氨酶升高超过正常值上限20倍的肝炎病例，反映了混合性或肝细胞性损伤，也有出现转氨酶无明显升高的胆汁郁积型黄疸病例的报道。
在排除梗阻的情况下，通常认为转氨酶升高伴有胆红素升高，是严重肝脏损害的重要指标。
国外临床试验中，3名服用度洛西汀的患者，出现转氨酶、胆红素和碱性磷酸酶升高，提示存在梗阻情况。
上述患者有严重的过度饮酒的情况，这可能是出现上述异常指标的原因所在。
两名安慰剂治疗的患者也出现了转氨酶、胆红素升高的情况。
上市后报告显示转氨酶、胆红素和碱性磷酸酶升高也可以发生在患有慢性肝病或肝硬化患者中。
因为度洛西汀和酒精的相互作用可能引起肝损害或者加剧已有的肝病恶化，所以度洛西汀通常不用于有习惯性饮酒和慢性肝病患者的治疗。
在临床试验过程中观察到有些病人肝酶升高，这些现象通常是一过性的和自限性的，或者在停药恢复。
严重肝酶升高(>正常值上限的10倍)或肝损伤伴胆汁郁积，或混合型肝病罕有报道，有些病例与酒精滥用或既往肝病有关。
在酒精使用患者或既往有肝病史的患者中，度洛西汀应慎用。
对血压的影响-与安慰剂相比，度洛西汀治疗引起血压升高，平均升高：收缩压2 mm Hg，舒张压0.5 mm Hg ，偶尔有至少一次测量的收缩压大于140 mm Hg。
盐酸氟西汀胶囊使用说明书
盐酸氟西汀胶囊使用说明书请仔细阅读说明书并在医师指导下使用盐酸氟西汀胶囊使用说明书【药品名称】通用名称：盐酸氟西汀胶囊英文名称：Fluoxetine Hydrochloride Capsules【成份】盐酸氟西汀【性状】本品为胶囊，内含白色或类白色颗粒。
【适应症】各种抑郁性精神障碍、包括轻性或重性抑郁症、双相情感性精神障碍的抑郁症，心因性抑郁及抑郁性神经症。
【规格】20mg（按C17H18F3NO计算）【用法用量】一般只需每天早上一次口服20mg，必要时可加至每天40mg。
剂量和疗程遵医嘱。
【不良反应】常见不良反应为口干、食欲减退、恶心、失眠、乏力，少数病例可见焦虑、头痛。
【禁忌】禁用于已知对此药过敏者。
【注意事项】因本药半衰期较长，故肝肾功能较差者或老年病人，应适当减少剂量。
有癫痫史者、妊娠或哺乳期妇女慎用。
儿童应用时应遵照医嘱。
如出现皮疹或发热，应立即停药，并对症处理。
不宜与单胺氧化酶抑制剂（MAOI）并用；必要时，应停用本药5周后，才可换用单胺氧化酶抑制剂（MAOI）。
【药理毒理】盐酸氟西汀是一种选择性的5-羟色胺再摄取抑制剂（SSRI），其能有效地抑制神经元从突触间隙中摄取5-羟色胺，增加间隙中可供实际利用的这种神经递质，从而改善情感状态，治疗抑郁性精神障碍。
【药代动力学】本药口服后吸收很快，血浆氟西汀浓度约在6～8小时达峰。
大约95%与血浆蛋白结合。
主要在肝脏中代谢成活性代谢产物去甲氟西汀及其它代谢物，从肾脏由尿排出。
据文献报导，不论氟西汀还是其代谢产物去甲氟西汀排泄均很慢。
其半衰期：氟西汀短期给药为1～3天，长期给药为4～6天；去甲氟西汀短期、长期给药均为4～16天。
每天服药20mg，4周后稳态血浓度为：氟西汀540±282nmol/L，去甲氟西汀640±332nmol/L。
【贮藏】遮光，密封，阴凉干燥处保存。
【有效期】暂定24个月说明书字数：861。
欣百达抑郁症安全性篇
头痛
失眠 头晕
0.4%
0.5% 0.5%
欣百达常见的不良反应大多 是轻中度和一过性的。
欣百达的安全性数据
欣百达治疗抑郁症的常见不良事件与SSRI类似
Martinez JM et al (2009) American College of Neuropsychopharmacology 48th Annual Meeting; Hollywood, FL, USA; December 6 –10, 2009
欣百达引起的性功能改变比赛乐特少
安慰剂 欣百达 *
女性患者
70 治疗引起的性功能 障碍可能性(%) 60 50 40 30 *† *** 治疗引起的性功能 障碍可能性(%)
男性患者
70 60 50 40 30 20 10 0
n=52 n=114 n=57
(40–120 mg/day)
赛乐特 (20 mg/day)
欣百达，一种药物，两种递质，抑郁焦虑躯体三解决
60毫克14粒装 30毫克 7粒装
7 粒/ 盒
30mg
欣百达 （N=319） 怡诺思 （N=329）
研究期ll+lll
* P＜0.05
*
收缩压
舒张压
收缩压或舒张压
收缩压
舒张压
收缩压或舒张压
• •
欣百达出现持续性高血压，尤其是收缩压的升高显著低于怡诺思 欣百达血浆结合率高，外周游离极少，对血压影响较轻微。
- 1、下载文档前请自行甄别文档内容的完整性，平台不提供额外的编辑、内容补充、找答案等附加服务。
- 2、"仅部分预览"的文档,不可在线预览部分如存在完整性等问题,可反馈申请退款(可完整预览的文档不适用该条件!)。
- 3、如文档侵犯您的权益，请联系客服反馈,我们会尽快为您处理(人工客服工作时间：9:00-18:30)。
【欣百达性状】
欣百达内容物为白色或类白色球状肠溶颗粒。 30mg胶囊：不透明白色囊体和蓝色囊帽，囊体壳 上印“30mg”。 60mg胶囊：不透明白色囊体和蓝色囊帽，囊体壳 上印“60mg”。
【欣百达成份】 主要组成成分盐酸度洛西汀。
【欣百达适应症】 用于治疗抑郁症。
【欣百达规格】 （1）30mg;（2）60mg（以度 洛西汀计）。
疗的病人可有罕见的、暂的 异常值。
【百济药师馨提示】
过敏 度洛西汀肠溶胶囊禁用于已知对度洛西汀肠溶胶囊或 产品中任何非活性成分过敏的患者。 单胺氧化酶抑制剂 禁止与单胺氧化酶抑制剂（MAOIs）联用（见警告）
未经治疗的窄角型青光眼
【欣百达药代动力学】
度洛西汀肠溶胶囊消除半衰期大约为12小时（变化 范围为8-17小时），在治疗范围之内其药代动力学参 数与剂量成正比。一般于服药3天后达到稳态血药浓 度。度洛西汀主要经肝脏代谢，涉及两种P450酶： CYP2D6和CYP1A2。
【欣百达用法用量】 起始治疗 推荐欣百达的起始剂量为40mg/日（20mg一日三 次）至60mg/日（一日一次或30mg一日二次）， 不考虑进食情况。
【欣百达不良反应】
以下不良反应数据基于所有关于盐酸度洛西汀肠溶 胶囊临床试验资料。
一般不良反应头晕、恶心、头疼，也见于度洛西汀 停药后，发生率≥5%。在安慰剂对照的临床试验中， 度洛西汀治疗伴随小的ALT、AST、CRK从基线至 终点平均值升高；与对照组相比，度洛西汀治
百济新特药房资深药师倾力制作千个药品专辑 安全、有效、合理用药之 欣百达篇
商品名：欣百达 厂家：Eli Lilly and Company
【欣百达药品名称】 通用名称：盐酸度洛西汀肠溶胶囊 汉语拼音：Yansuan Duluoxiting Changrong
Jiaonang 商品名：欣百达 Cymbalta 英文名：Duloxetine Hydrochoride Enteric
欣百达价格、优惠
请参考百济新特药房 ()药品信息
数十位资深药师
实时免费解答用药难题
了解欣百达
享受贴心的药学服务
历经十年，服务专业，提倡合理用药，提供 优质药品。
国内首家“全国连锁专科药房”，也是全国大 型的专科医药连锁企业之一。
坚持“专注于重大慢性疾病用药，持续改善患 者健康”的经营理念。