Seroquel 是5-HT 受体阻断剂。它的副作用列于下表。注意这是短程，大批量(七百多人人群治疗的副作用。
Seroquel
CLINICAL PHARMACOLOGYPharmacodynamicsSEROQUEL is an antagonist at multiple neurotransmitter receptors in the brain: serotonin 5HT1A and 5HT2 (IC50s=717 & 148nM respectively), dopamine D1 and D2 (IC50s=1268 & 329nM respectively), histamine H1 (IC50=30nM), and adrenergic α 1 and α 2 receptors (IC50s=94 & 271nM, respectively). SEROQUEL has no appreciable affinity at cholinergic muscarinic and benzodiazepine receptors (IC50s>5000 nM).
The mechanism of action of SEROQUEL, as with other drugs having efficacy in the treatment of schizophrenia and bipolar disorder, is unknown. However, it has been proposed that the efficacy of SEROQUEL in schizophrenia and its mood stabilizing properties in bipolar depression and mania are mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5HT2) antagonism. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other effects of SEROQUEL. SEROQUEL’s antagonism of histamine H1 receptors may explain the somnolence observed with this drug.
SEROQUEL’s antagonism of adrenergic α 1 receptors may explain the orthostatic hypotension observed with this drug.
Clinical Efficacy DataBipolar DisorderDepression The efficacy of SEROQUEL for the treatment of depressive episodes associated with bipolar disorder was established in 2 identical 8-week, randomized, double-blind, placebo-controlled studies (N=1045). These studies included patients with either bipolar I or II disorder and those with or without a rapid cycling course. Patients randomized to SEROQUEL were administered fixed doses of either 300 mg or 600 mg once daily.
The primary rating instrument used to assess depressive symptoms in these studies was the Montgomery-Asberg Depression Rating Scale (MADRS), a 10 item clinician-rated scale with scores ranging from 0 to 60. The primary endpoint in both studies was the change from baseline in MADRS score at week 8. In both studies, SEROQUEL was superior to placebo in reduction of MADRS score. Improvement in symptoms, as measured by change in MADRS score relative to placebo, was seen in both studies at Day 8 (Week 1) and onwards. In these studies, no additional benefit was seen with the 600 mg dose. For the 300 mg dose group, statistically significant improvements over placebo were seen in overall quality of life and satisfaction related to various areas of functioning, as measured using the Q-LES-Q(SF).
Mania The efficacy of SEROQUEL in the treatment of acute manic episodes was established in 3 placebo-controlled trials in patients who met DSM-IV criteria for Bipolar I disorder with manic episodes. These trials included patients with or without psychotic features and excluded patients with rapid cycling and mixed episodes. Of these trials, 2 were monotherapy (12 weeks) and 1 was adjunct therapy (3 weeks) to either lithium or divalproex. Key outcomes in these trials were change from baseline in the Young Mania Rating Scale (YMRS) score at 3 and 12 weeks for monotherapy and at 3 weeks for adjunct therapy. Adjunct therapy is defined as the simultaneous initiation or subsequent administration of SEROQUEL with lithium or divalproex.
The primary rating instrument used for assessing manic symptoms in these trials was YMRS, an 11-item clinician-rated scale traditionally used to assess the degree of manic symptomatology (irritability, disruptive/aggressive behavior, sleep, elevated mood, speech, increased activity, sexual interest, language/thought disorder, thought content, appearance, and insight) in a range from 0 (no manic features) to 60 (maximum score).
The results of the trials follow:
MonotherapyIn two 12-week trials (n=300, n=299) comparing SEROQUEL to placebo, SEROQUEL was superior to placebo in the reduction of the YMRS total score at weeks 3 and 12. The majority of patients in these trials taking SEROQUEL were dosed in a range between 400 and 800 mg per day.
Adjunct TherapyIn this 3-week placebo-controlled trial, 170 patients with acute bipolar mania (YMRS ≥20) were randomized to receive SEROQUEL or placebo as adjunct treatment to lithium or divalproex. Patients may or may not have received an adequate treatment course of lithium or divalproex prior to randomization. SEROQUEL was superior to placebo when added to lithium or divalproex alone in the reduction of YMRS total score.
The majority of patients in this trial taking SEROQUEL were dosed in a range between 400 and 800 mg per day. In a similarly designed trial (n=200), SEROQUEL was associated with an improvement in YMRS scores but did not demonstrate superiority to placebo, possibly due to a higher placebo effect.
SchizophreniaThe efficacy of SEROQUEL in the treatment of schizophrenia was established in 3 short-term (6-week) controlled trials of inpatients with schizophrenia who met DSM III-R criteria for schizophrenia. Although a single fixed dose haloperidol arm was included as a comparative treatment in one of the three trials, this single haloperidol dose group was inadequate to provide a reliable and valid comparison of SEROQUEL and haloperidol.
Several instruments were used for assessing psychiatric signs and symptoms in these studies, among them the Brief Psychiatric Rating Scale (BPRS), a multi-item inventory of general psychopathology traditionally used to evaluate the effects of drug treatment in schizophrenia. The BPRS psychosis cluster (conceptual disorganization, hallucinatory behavior, suspiciousness, and unusual thought content) is considered a particularly useful subset for assessing actively psychotic schizophrenic patients. A second traditional assessment, the Clinical Global Impression (CGI), reflects the impression of a skilled observer, fully familiar with the manifestations of schizophrenia, about the overall clinical state of the patient. In addition, the Scale for Assessing Negative Symptoms (SANS), a more recently developed but less well evaluated scale, was employed for assessing negative symptoms.
Table 1. 副作用试验Treatment-Emergent Adverse Experience
Incidence in 3- to 12-Week Placebo-Controlled Clinical
Trials for the Treatment of Schizophrenia and Bipolar
Mania (monotherapy)
Body System/
Preferred Term | SEROQUEL
(人数n=719) | PLACEBO
(n=404) | | Body as a Whole | | Headache | 21% | 14% | | Pain | 7% | 5% | | Asthenia | 5% | 3% | | Abdominal | 4% | 1% | | Back Pain | 3% | 1% | | Fever | 2% | 1% | | Cardiovascular | | Tachycardia | 6% | 4% | | Postural Hypotension | 4% | 1% | | Digestive | | Dry Mouth | 9% | 3% | | Constipation | 8% | 3% | | Vomiting | 6% | 5% | | Dyspepsia | 5% | 1% | | Gastroenteritis | 2% | 0% | | Gamma Glutamy 1 Transpeptidase Increased | 1% | 0% | | Metabolic and Nutritional | | Weight Gain Nervous | 5% | 1% | | Agitation | 20% | 17% | | Somnolence | 18% | 8% | | Dizziness | 11% | 5% | | Anxiety | 4% | 3% | | Respirator | | Pharyngitis | 4% | 3% | | Rhinitis | 3% | 1% | | Skin and Appendages | | Rash | 4% | 2% | | Special Senses | | Amblyopia | 2% | 1% | | 1Events for which the SEROQUEL incidence was equal to or less than placebo are not listed in the table, but included the following: accidental injury, akathisia, chest pain, cough increased, depression, diarrhea, extrapyramidal syndrome, hostility, hypertension, hypertonia, hypotension, increased appetite, infection, insomnia, leukopenia, malaise, nausea, nervousness, paresthesia, peripheral edema, sweating, tremor, and weight loss. |
原帖由 dorcasliu80 于 07-5-25 23:43 发表 ![]()
我的药物
Luvox, clonazepam 及 seroquel是属于SSRI 还是5-HT?
会有增胖的副作用吗？
还有Lamictal是属于哪一类型呢？
请大哥指点！
[ 本帖最后由 晔阳 于 07-5-26 01:01 编辑 ] |
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发表于 07-5-25 23:17:58
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