药品行政保护品种介绍——心血管系统药物(三)(续二)

普伐他丁钠通用名:普伐他丁钠(pravastatin sodium),商品名:美百乐镇(Mevalotin)片剂.化学名:[+]-(3R,5R)-3,5-二羟基-7{(1S,2S,6S,8S,8 α R)-6-羟基-2-甲基-8[(S)-2-甲基丁酰氧基]-1,2,6,7,8,8 α-六氢-1-萘基}庚酸钠.     

氟伏沙明联合认知行为治疗儿童青少年情绪障碍的疗效

目的评价氟伏沙明联合认知行为治疗青少年抑郁情绪障碍的疗效和不良反应。方法将60例特发于青少年时期的情绪障碍患者随机分成研究组和对照组,研究组（n=30）予氟伏沙明联合认知行为治疗,对照组（n=30）给予氟伏沙明片单一治疗。氟伏沙明25mg/d起,平均52.10mg/d,疗程8周。采用儿童抑郁障碍自评量表（DSRSC）、儿童大体评定量表（CGAS）及不良反应量表（TESS）评定疗效及不良反应。结果经8周治疗,研究和对照组患儿总显效率分别为89%和75%,二组比较差异有显著性（P〈0.05）;第6、8周末DSRSC减分率研究组（59.06±5.84,79.11±7.40）与对照组（54.41±6.21,73.29±6.45）比较均有显著性差异（Pa〈0.01）,二组CGAS评分比较自治疗4周起存在显著性差异（P〈0.05）,TESS二组比较无显著性差异（P〉0.05）。结论氟伏沙明联合认知行为疗法治疗青少年抑郁障碍的疗效较好。     

反相高效液相色谱法测定人血浆中马来酸氟伏沙明浓度

目的:建立高效液相色谱法测定人血浆中马来酸氟伏沙明浓度。方法:以安定为内标,待测血浆样品经乙醚萃取后,用高效液相色谱法紫外进行检测。色谱柱为 Discovery~(?)RP Amide C_(16)(5μm,150 mm×4.6 mm),柱温35 ℃;流动相为乙腈-0.05 mol·L~(-1)醋酸铵(40:60),流速1.2 mL·min~(-1);检测波长250 nm。结果:血浆中马来酸氟伏沙明浓度线性范围为1.56～99.6 ng·mL~(-1),最低定量浓度1.56 ng·mL~(-1);回收率为95.7%～106.1%。结论:本法分离效果良好,灵敏度高,回收率高,能满足于人体血药浓度测定及药代动力学研究。     

Olanzapine plus fluvoxamine and olanzapine alone for the treatment of an acute exacerbation of schizophrenia

The objective of the present study was to compare the efficacy and adverse effects of olanzapine plus fluvoxamine and those of olanzapine alone, in schizophrenic patients with acute exacerbation. A randomized, placebo-controlled, 6-week trial was carried out at a University Hospital in Bangkok, Thailand. The efficacy and adverse effects were assessed biweekly by using the Brief Psychiatric Rating Scale (BPRS) and the Udvalg for Kliniske Undersogelser side-effect scale, respectively. Twenty schizophrenic patients with acute exacerbation were randomly assigned to receive olanzapine plus fluvoxamine or olanzapine alone. The study found that the means of BPRS total and BPRS general psychopathology score changes were significantly larger in olanzapine plus fluvoxamine group (P = 0.037 and P = 0.045, respectively). The incidence of treatment adverse effects is comparable. In conclusion, the study findings suggest that fluvoxamine augmentation to olanzapine is well tolerated and more effective than olanzapine alone for short-term (6-week) treatment of an acute exacerbation of schizophrenia. Due to a number of limitations, further studies are warranted to confirm.     

Increased libido in a woman treated with fluvoxamine: a case report

OBJECTIVE: The aim of this paper is to describe a case of increased libido during fluvoxamine therapy. METHOD: Single case report. RESULTS: The patient, a 27-year-old married Japanese woman with borderline personality disorder, developed an increased libido with the administration of fluvoxamine. The increased libido disappeared after fluvoxamine was discontinued. CONCLUSION: The present findings suggest that fluvoxamine can cause increased libido in some patients.     

Development of a fluvoxamine detection system using a Quenchbody,a novel fluorescent biosensor

The misuse of psychotropic drugs intended for medical treatment represents a recent worldwide public health concern. Quenchbody (Q‐body) is a novel fluoroimmunosensor that can detect an antigen immediately without additional reagents or washing steps. Here, we describe creating Q‐bodies for the detection of the antidepressant fluvoxamine (FLV) and determining optimal conditions to achieve the highest fluorescence intensity (FI). We prepared five Q‐bodies with the fluorophore labeled at either the N‐ or C‐ terminus and with different linker lengths. Fluorescence was measurable within minutes, indicating the interaction of Q‐bodies with FLV. The normalized FI (FI ratio) of the N‐terminus labeled Q‐body increased approximately 1.5‐fold upon FLV addition; Q‐bodies labeled at the C‐terminus did not significantly increase FI. Among the fluorescence dyes used in this study, Rhodamine 6G labeled Q‐body showed the best FI ratio. EC₅₀ values of the N‐terminus labeled Q‐bodies were similar (23.2–224nM) regardless of linker length or labeling dye. We examined whether the Q‐body could be applicable to serum matrix instead of phosphate‐buffered saline. The intact serum interfered strongly with the Q‐body fluorescence. However, the FI ratios of the Q‐body for FLV‐spiked serum filtrate, for which proteins were removed by filtration, showed a dose‐dependency for detecting FLV levels. Deproteinization, which does not interfere with Q‐body fluorescence measurements, is likely necessary to detect serum FLV with high sensitivity. This study demonstrates the potential of Q‐body probes as a tool towards developing creative immunoassay applications.     

Interaction between carbamazepine and fluvoxamine.

In 3 patients the addition of fluvoxamine to a constant dosage of carbamazepine (CZP) caused a substantial rise of plasma CZP accompanied by symptoms of intoxication. As this drug combination may occur increasingly in the future, this probably pharmacokinetic interaction is of practical relevance.     

Hypnotic action of flunitrazepam in the rat: Does 5-HT mechanism play a role?

This study examined whether pharmacological manipulation of serotonergic (5-HT) systems would affect the hypnotic action of flunitrazepam in rats. Flunitrazepam, a potent hypnotic, was used alone or combined with parachlorophenylalanine (pCPA), an inhibitor of the synthesis of 5-HT, 8-OH-DPAT, a 5-HT_1A receptor agonist and fluvoxamine, an inhibitor of the reuptake of 5-HT. Flunitrazepam increased the amount of orthodox sleep, the latency of rapid eye movement (REM) sleep and decreased the amount of REM sleep. The drug pCPA decreased the total sleep time and the amount of orthodox and REM sleep. Administration of flunitrazepam to pCPA-pretreated rats induced orthodox sleep in an identical way to that found in the controls. The drug 8-OH-DPAT increased wakefulness and the latency of REM sleep. The association of flunitrazepam with 8-OH-DPAT abolished the increase in waking seen after 8-OH-DPAT alone. In contrast, the combined treatment with flunitrazepam and 8-OH-DPAT resulted in a lengthening of the latency of REM sleep significantly greater than that observed with the same dose of each drug alone. Fluvoxamine increased the latency and decreased the amount of REM sleep. The association of fluvoxamine with flunitrazepam induced a decrease in REM sleep, equal to the sum of the effects of the two drugs alone. Fluvoxamine did not modify the other effects of flunitrazepam. The present experiments demonstrate that the association of pCPA, 8-OH-DPAT and fluvoxamine, did not alter the hypnogenic effect of flunitrazepam. The possibility of an involvement of 5-HT mechanisms in the effect of flunitrazepam on the phasic events in sleep is questionable.     

Fluvoxamine in the treatment of demented elderly patients: a double-blind, placebo-controlled study.

The efficacy of fluvoxamine on cognitive functioning and behavioral changes was evaluated in a double-blind, placebo-controlled study of 46 elderly demented patients. The patients had a DSM-III diagnosis of primary degenerative dementia or multi-infarct dementia and were aged greater than or equal to 65 years. Twenty-two patients were given 150 mg fluvoxamine per day and 24 received placebo tablets; 14 and 15 patients, respectively, completed 6 weeks of treatment. Within treatments, there were no significant changes in median scores on neuropsychological tests (picture recall and recognition, trail making and finger tapping) or the GBS scale scores (degrees of dementia) or GBS subscale score (clinical profiles, including symptoms common in dementia, motor, emotional and intellectual functioning). Between treatments, the median changes in psychometric test scores did not differ significantly. However, within and between treatments, there were trends favoring fluvoxamine on symptoms common in dementia (confusion, irritability, anxiety, fear-panic, mood level and restlessness). In conclusion, the study does not support the hypothesis that fluvoxamine improves cognitive functioning or behavioral changes in elderly dementia patients.     

Efficacy of combination treatment of fluvoxamine and tiapride for repetitive behaviors in frontotemporal lobar degeneration

The present study reports a 63‐year‐old right‐handed man with frontotemporal lobar degeneration (FTLD) who manifested severe repetitive and disinhibited behaviors. Combination treatment of fluvoxamine and tiapride decreased the frequency of these behaviors. The results indicate that these drugs are effective for the treatment of repetitive and disinhibited behaviors for patients with FTLD. The behaviors caused by FTLD are discussed in terms of obsessive–compulsive spectrum disorder.