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1.
Eszopiclone is the single (S)-enantiomer of the cyclopyrrolone hypnotic zopiclone. It was marketed in the U.S. in December 2004. Its kinetics and possible mode of action, pivotal regulatory trials and its use in insomnia comorbid with other conditions are reviewed, together with trials in patients with obstructive sleep apnea syndromes. Safety and tolerability aspects are discussed, including its dysgeusic profile and effects on memory, cognitive and psychomotor function. U.S.-based pharmacoeconomic data are included together with the design features of key regulatory studies submitted for regulatory approval in Japan.  相似文献   

2.
Eszopiclone, a single-isomer, non-benzodiazepine hypnotic agent, is approved for use in the US for the treatment of insomnia for patients who have difficulty falling asleep (sleep latency) as well as for those who have difficulty staying asleep (sleep maintenance). Efficacy in sleep maintenance has not been consistently demonstrated with previous hypnotics, and long-term efficacy and safety data are lacking for these agents. In clinical trials, eszopiclone 3 mg significantly improved objective and subjective sleep measures in transient and chronic insomnia in adults. Nightly treatment with eszopiclone 1 mg effectively induced sleep in elderly patients and the 2-mg dose effectively induced and maintained sleep. The ability of eszopiclone 2 mg to significantly improve next-day functioning and daytime alertness (as demonstrated by a reduction in the number and duration of naps) in the elderly is an important finding in clinical trials, and is unique to the class of hypnotic agents for the treatment of insomnia. Eszopiclone was well tolerated in clinical trials < or = 12 months duration, with no clinically significant evidence of pharmacological tolerance, rebound insomnia or dependence. The most frequently reported adverse event was unpleasant taste. Eszopiclone is the only non-benzodiazepine sedative-hypnotic (in the Schedule IV class under the Controlled Substances Act) to be evaluated as a long-term treatment for chronic insomnia.  相似文献   

3.
Zaleplon: a review of its use in the treatment of insomnia   总被引:6,自引:0,他引:6  
Dooley M  Plosker GL 《Drugs》2000,60(2):413-445
Zaleplon is a pyrazolopyrimidine hypnotic agent which is indicated for the short term (2 to 4 weeks) management of insomnia. Zaleplon 5 and 10 mg at bedtime (usual recommended doses) significantly reduced sleep latency compared with placebo in clinical trials in nonelderly and elderly patients with insomnia. In general, sleep maintenance (sleep duration and number of awakenings) and sleep quality were not significantly different from placebo with zaleplon 5 and 10 mg/night. Zaleplon 20 mg/night significantly improved sleep latency and duration in nonelderly patients, but effects on number of awakenings were inconsistent and sleep quality generally did not improve. The relative hypnotic efficacy of zaleplon compared with that of triazolam and zolpidem is not yet clearly established. Tolerance to the hypnotic effects of zaleplon generally did not occur during 5 weeks' treatment, or during long term treatment (6 or 12 months) according to a small number of studies presented as abstracts. Zaleplon was well tolerated in clinical trials. The most common event was headache but the incidence was similar to that observed with placebo. Zaleplon 5 and 10 mg did not impair psychomotor function or memory even immediately after the dose in studies in volunteers or patients with insomnia. Zaleplon 20 mg, however, impaired psychomotor function and memory immediately after the dose but next-day effects were not observed. The psychomotor profile of zaleplon appears to be better than that of comparator agents. Rebound insomnia was not observed after sudden discontinuation of up to 12 months' treatment with zaleplon 5 and 10 mg/night and up to 4 weeks' treatment with zaleplon 20 mg/night. In addition, the potential for withdrawal syndrome with zaleplon appears to be low according to limited data. In conclusion, zaleplon 5, 10 and 20 mg administered at bedtime, or later if patients have difficulty sleeping, is an effective and well tolerated hypnotic agent. There was no evidence of next-day residual effects with the 5 and 10 mg dosages, and the incidence of withdrawal effects with zaleplon 5, 10 and 20 mg did not differ significantly to that observed with placebo. In addition, tolerance to the effects of zaleplon is unlikely to develop when administered for the recommended treatment period. The comparative efficacy and tolerability of zaleplon with other short acting nonbenzodiazepine hypnotics is difficult to establish. However, on the basis of current efficacy evidence and the lower incidence of residual effects with zaleplon 5 and 10 mg relative to comparator agents, this drug represents a useful option in the management of patients with insomnia who have difficulties initiating sleep.  相似文献   

4.
Ramelteon: a review of its use in insomnia   总被引:1,自引:0,他引:1  
Simpson D  Curran MP 《Drugs》2008,68(13):1901-1919
Ramelteon (Rozeremtrade mark) is the first melatonin receptor agonist to be approved for the treatment of insomnia; it is not classified as a controlled substance. In patients with chronic insomnia, objectively assessed latency to persistent sleep (LPS) at week 1 was improved with oral ramelteon 8 mg administered 30 minutes before bedtime, compared with placebo, and this effect was maintained throughout the duration of 5-week and 6-month clinical studies. Subjectively assessed sleep latency (sSL) improved in some, but not all, studies. When a statistically significant improvement in sSL occurred at week 1, the effect was maintained throughout the duration of the 5-week studies, but not at all timepoints throughout a 6-month study. Improvements in objectively assessed total sleep time (TST) and sleep efficiency (SE) were only reported during the first week of treatment. Improvements in other objective or subjective measures of sleep were not consistent. Ramelteon was generally well tolerated, did not impair next-day cognitive or motor performance and was not associated with withdrawal symptoms, rebound insomnia or abuse potential. Thus, ramelteon provides a well tolerated option for the treatment of patients with insomnia characterized by difficulty in sleep onset.  相似文献   

5.
Zolpidem: a review of its use in the management of insomnia   总被引:2,自引:0,他引:2  
Zolpidem (Ambien, Stilnox, Myslee, an imidazopyridine, is a nonbenzodiazepine hypnotic indicated for the short-term treatment of insomnia. Zolpidem improves sleep in patients with insomnia. Its overall tolerability is favourable when administered according to the manufacturer's prescribing information, with a low propensity to cause clinical residual effects, withdrawal, dependence or tolerance. In addition, most evidence suggests that the drug is associated with minimal rebound insomnia. In the only clinical trials that investigated the use of a hypnosedative drug in an 'as-needed' regimen, zolpidem produced a global improvement in sleep. Thus, zolpidem continues to be a useful therapeutic option in the pharmacological treatment of patients with insomnia.  相似文献   

6.
Lyseng-Williamson KA  Yang LP 《Drugs》2007,67(15):2231-2256
Topiramate (Topamax) is a structurally novel broad-spectrum antiepileptic drug (AED) with established efficacy as monotherapy or adjunctive therapy in the treatment of adult and paediatric patients with generalised tonic-clonic seizures, partial seizures with or without generalised seizures, and seizures associated with Lennox-Gastaut syndrome. The incidence and severity of many adverse events, including CNS-related events, may be reduced through the use of slow titration to effective and well tolerated dosages. It is associated with few clinically significant interactions with other drugs, is effective when used with other AEDs, is not associated with drug-induced weight gain and, at lower dosages, does not interfere with the effectiveness of oral contraceptives. Therefore, topiramate is a valuable option as monotherapy or adjunctive therapy in the treatment of epilepsy in adult and paediatric patients.  相似文献   

7.
Sanford M  McCormack PL 《Drugs》2011,71(13):1755-1770
Eldecalcitol (1α,25[OH](2)-2β-(3-hydroxypropyloxy)vitamin D(3); ED-71; Edirol?) is an orally administered analogue of active vitamin D (calcitriol) that is available in Japan for the treatment of osteoporosis. Two randomized, double-blind, multicentre trials were conducted in patients with osteoporosis. In a placebo-controlled, dose-ranging trial, eldecalcitol significantly reduced serum bone-specific alkaline phosphatase (BALP) and serum osteocalcin, markers of bone formation, more than placebo. Eldecalcitol at a 1.0?μg/day dosage, but not at lower dosages, also significantly reduced urinary type I collagen N-telopeptide (NTX), a marker of bone resorption, more than placebo. In a comparison with alfacalcidol (a prodrug of calcitriol), eldecalcitol produced significantly greater reductions in serum BALP and urinary NTX, and had a positive effect on CT markers of femoral biomechanical properties. In the comparison with alfacalcidol, eldecalcitol 0.75?μg/day significantly reduced the 3-year incidence of vertebral fractures, with an absolute risk reduction of 4.1% over this period, representing a relative risk reduction of 26%. There was no significant difference in the rate of non-vertebral fractures. In both trials, eldecalcitol treatment was also associated with an increase in bone mineral density, whereas patients who received the comparators generally had a reduction in bone mineral density. Increases in blood calcium (to >2.6?mmol/L) and urinary calcium (to >0.1?mmol/L glomerular filtrate) were the most clinically important treatment-emergent adverse events. In the placebo-controlled, dose-ranging trial, 23% and 25% of patients in the eldecalcitol 1?μg/day group had increased blood and urinary calcium compared with 7% and 7%, 6% [corrected] and 9%, and 0% and 1.9% in the eldecalcitol 0.5 and 0.75?μg/day, and placebo groups, respectively. In the comparison with alfacalcidol, 21.0% and 13.5% of eldecalcitol 0.75?μg/day and alfacalcidol 1.0?μg/day recipients had increased blood calcium, whereas hypercalcaemia (defined as a serum calcium >2.9?mmol/L) occurred in 0.4% and urolithiasis in 1.3% of eldecalcitol recipients over 36 months of treatment. Eldecalcitol is an efficacious treatment for patients with osteoporosis that should be further investigated in head-to-head trials with other recommended first-line pharmacological treatments.  相似文献   

8.
McCormack PL 《Drugs》2010,70(16):2073-2088
Dienogest (Visanne?) is a synthetic oral progestogen with unique pharmacological properties that is indicated at a dosage of 2?mg/day for the treatment of endometriosis. It is generally highly selective for the progesterone receptor and displays strong progestational effects and moderate antigonadotrophic effects, but no androgenic, glucocorticoid or mineralocorticoid activity. Dienogest has moderate affinity for progesterone receptors (10% that of progesterone) and at a dosage of 2?mg/day only moderately suppresses estradiol levels. It has high oral bioavailability and a half-life suitable for once-daily administration. In randomized clinical trials, oral dienogest was significantly more effective than placebo in reducing pelvic pain in patients with confirmed endometriosis. In trials comparing oral dienogest for 16 or 24 weeks with gonadotropin-releasing hormone (GnRH) agonists commonly used in the treatment of endometriosis, dienogest was noninferior to depot leuprorelin in reducing pelvic pain and was not significantly different from intranasal buserelin and depot triptorelin in improving combined symptoms/signs scores or revised American Fertility Society (rAFS) staging scores, respectively. Improvements were also noted in some measures of health-related quality of life. The efficacy of dienogest was sustained during long-term treatment for more than 1 year. Dienogest was generally well tolerated and was not considered to be associated with clinically relevant androgenic effects. It appeared to have fewer hypoestrogenic effects than the GnRH agonists. Dienogest was associated with a high incidence of abnormal menstrual bleeding patterns, although this was generally well tolerated by patients, with few discontinuing therapy, and the bleeding intensity and frequency decreased over time. Therefore, oral dienogest offers an effective, generally well tolerated therapeutic option for the long-term treatment of endometriosis.  相似文献   

9.
Curran MP  Perry CM 《Drugs》2004,64(18):2125-2141
Cabergoline is a synthetic ergoline dopamine agonist with a high affinity for dopamine D2 receptors and a long elimination half-life. This agent provides continuous dopaminergic stimulation with once-daily administration. Adjuvant oral cabergoline is usually well tolerated and effective in controlling symptoms in patients with advanced Parkinson's disease experiencing response fluctuations to long-term levodopa therapy. In patients with early Parkinson's disease, cabergoline (with or without levodopa) is well tolerated and effective in controlling disease symptoms, and may reduce the risk of developing drug-induced motor complications. Data from two pharmacoeconomic analyses suggest that cabergoline may be a cost-effective treatment option versus levodopa in patients with early Parkinson's disease, and highlight the need for further evaluation of the drug in this indication.  相似文献   

10.
Adapalene: a review of its use in the treatment of acne vulgaris   总被引:3,自引:0,他引:3  
Waugh J  Noble S  Scott LJ 《Drugs》2004,64(13):1465-1478
Adapalene (Differin) is a retinoid agent indicated for the topical treatment of acne vulgaris. In clinical trials, 0.1% adapalene gel has proved to be effective in this indication and was as effective as 0.025% tretinoin gel, 0.1% tretinoin microsphere gel, 0.05% tretinoin cream and 0.1% tazarotene gel once every two days; however, the drug was less effective than once-daily 0.1% tazarotene gel. It can be used alone in mild acne or in combination with antimicrobials in inflammatory acne and has proved efficacious as maintenance treatment. Adapalene has a rapid onset of action and a particularly favourable tolerability profile compared with other retinoids. These attributes can potentially promote patient compliance, an important factor in treatment success. Adapalene is, therefore, assured of a role in the first-line treatment of acne vulgaris.  相似文献   

11.
Keating GM  Perry CM 《Drugs》2005,65(15):2151-2178
The Group 1, 1 beta-methyl carbapenem ertapenem (Invanz) is approved for parenteral use in patients with complicated intra-abdominal infection (cIAI), community-acquired pneumonia (CAP) and acute pelvic infection caused by susceptible strains of certain designated organisms in both the US and the EU. Additional approved indications in the US include complicated skin and skin structure infection (cSSSI) and complicated urinary tract infection (cUTI). Ertapenem is approved for use in adults in both the US and the EU and in paediatric patients aged >or=3 months in the US.Ertapenem has a broad spectrum of in vitro activity against Gram-negative pathogens, including extended-spectrum beta-lactamase (ESBL)- and AmpC-producing Enterobacteriaceae, Gram-positive pathogens and anaerobic pathogens. It has similar efficacy to comparator antibacterials such as piperacillin/tazobactam in cSSSI (including diabetic foot infection), cIAI and acute pelvic infection and ceftriaxone with or without metronidazole in cIAI, cUTI and CAP. The drug has also shown efficacy in the treatment of paediatric patients with complicated community-acquired bacterial infections. Ertapenem has a convenient once-daily administration schedule and is generally well tolerated. Thus, ertapenem is an important option for the empirical treatment of complicated community-acquired bacterial infections in hospitalised patients.  相似文献   

12.
Keam SJ 《Drugs》2008,68(14):2021-2057
Doripenem, a parenteral, broad-spectrum antibacterial agent of the carbapenem family, is indicated as empirical therapy in serious bacterial infections in adults. Doripenem is indicated in Japan for use as a single agent in intra-abdominal infections (IAIs), lower respiratory tract infections (including nosocomial pneumonia), complicated urinary tract infections (cUTIs) and a variety of other bacterial infections, such as complicated skin and skin structure infections (cSSSIs), obstetric and gynaecological infections, serious ear, nose and throat infections, sepsis and endocarditis, dental and oral surgical infection, and ophthalmic infection caused by various susceptible strains of Gram-negative, Gram-positive or anaerobic bacteria. Doripenem is indicated in the US for the treatment of complicated IAIs (cIAIs) or cUTIs, including pyelonephritis, caused by susceptible strains of designated pathogens, and in the EU for the treatment of nosocomial pneumonia (including ventilator-associated pneumonia [VAP]), cIAIs or cUTIs.Doripenem has a broad spectrum of in vitro activity against Gram-positive and Gram-negative bacteria, including extended-spectrum beta-lactamase (ESBL)- and AmpC-producing Enterobacteriaceae, and anaerobic pathogens. The drug also has a low propensity to select for resistance and is suitable for the prolonged infusions that may be required to achieve pharmacodynamic/pharmacokinetic targets for bactericidal activity (and therefore efficacy) against pathogens with increased MICs (minimum concentrations required to inhibit the pathogens). Doripenem is no less effective than other antibacterial agents, including meropenem, imipenem/cilastin, piperacillin/tazobactam or levofloxacin in a wide range of serious bacterial infections, such as complicated lower respiratory infections, nosocomial pneumonia (including VAP), cIAIs and cUTIs, and is well tolerated. Thus, doripenem is a valuable addition to the options available for the empirical treatment of serious bacterial infections in hospitalized patients.  相似文献   

13.
Quetiapine: a review of its use in the treatment of bipolar depression   总被引:5,自引:0,他引:5  
Keating GM  Robinson DM 《Drugs》2007,67(7):1077-1095
Quetiapine (Seroquel) is the only atypical antipsychotic approved in the US for use as monotherapy in both bipolar mania and depression, offering potential compliance advantages. Monotherapy with oral quetiapine 300 mg/day is effective in the treatment of patients with bipolar I or II depression. Rapid and sustained improvements in depressive and anxiety symptoms are seen with quetiapine, as well as improvements in health-related quality of life (HR-QOL). Quetiapine is generally well tolerated in bipolar depression and is not associated with an increased risk of treatment-emergent mania. Thus, despite the current lack of data from active comparator trials, quetiapine monotherapy should be considered a first-line option for the acute treatment of bipolar depression.  相似文献   

14.
Duggan ST  McKeage K 《Drugs》2011,71(16):2193-2212
Bazedoxifene (Conbriza?, Viviant?) is the first third-generation selective estrogen receptor modulator (SERM) and it is approved for the treatment of postmenopausal osteoporosis in the EU and Japan. Bazedoxifene contains an indole-based core binding domain that binds with high affinity to estrogen receptors and exhibits favourable effects on bone and lipid profiles, with no clinically relevant endometrial or breast stimulation. Oral bazedoxifene once daily reduced the incidence of new vertebral fractures in patients with postmenopausal osteoporosis in a large, well designed trial of 3 years' duration; both bazedoxifene and raloxifene were significantly more effective than placebo. Neither bazedoxifene nor raloxifene reduced the incidence of nonvertebral fractures in the overall study population; however, bazedoxifene, but not raloxifene, reduced the rate of nonvertebral fractures in high-risk patients. Moreover, data from patients who continued to receive the drug during a 2-year extension phase of this trial indicate that bazedoxifene continues to provide protection against new vertebral fractures for up to 5 years. Bazedoxifene also increases bone mineral density and reduces the levels of bone turnover markers. Bazedoxifene was generally well tolerated and did not detrimentally affect the reproductive tract or breast tissue in clinical trials, thereby demonstrating a favourable risk-benefit profile. A pharmacoeconomic analysis conducted from an EU perspective predicted bazedoxifene to be cost effective in some EU countries. Therefore, bazedoxifene presents another useful option for the treatment of postmenopausal osteoporosis, especially in those at high risk for osteoporotic fracture.  相似文献   

15.
Naftidrofuryl (Praxilene) is a vasodilator that has been used in the treatment of intermittent claudication for >30 years in Europe to improve walking distance and provide symptomatic relief. However, earlier trials had inconsistencies in design and the clinical relevance of the treatment effect has been controversial. Recent randomised, double-blind, placebo-controlled trials, however, have generally been conducted in accordance with updated methodology guidelines. In these studies, naftidrofuryl 200mg three times daily improved pain-free and maximal walking distances and health-related quality of life by a significantly greater extent than placebo in patients with intermittent claudication. The magnitude of these effects appears to support claims that the effects of naftidrofuryl are clinically relevant in these patients.  相似文献   

16.
Tolterodine: a review of its use in the treatment of overactive bladder   总被引:3,自引:0,他引:3  
Clemett D  Jarvis B 《Drugs & aging》2001,18(4):277-304
Tolterodine is a competitive muscarinic receptor antagonist that shows in vivo selectivity for the bladder over the salivary glands compared with oxybutinin. Results of randomised double-blind placebo-controlled studies indicate that tolterodine 4 mg/day (administered as immediate-release tablets 2mg twice daily or extended-release capsules 4mg daily) is superior to placebo in improving micturition diary variables in patients with overactive bladder. Moreover, tolterodine 2mg twice daily is as effective as oxybutynin 5mg 3 times daily. Maximum treatment effects with both drugs occurred after 5 to 8 weeks of treatment and improvements were maintained during long term treatment for up to 24 months. In a pooled analysis of four 12-week studies, equivalent and significant reductions in micturition frequency (-2.3 and -2.0 vs -1.4, p < 0.001) and the incidence of urge incontinence episodes (-1.6 and -1.8 vs -1.1, p < 0.05) were reported for tolterodine 2mg twice daily and oxybutynin 5mg 3 times daily compared with placebo. Functional bladder capacity was also significantly increased. Improvements in patient perceptions of their urgency symptoms and of problems caused by their bladder condition were significantly greater during treatment with tolterodine than with placebo. Tolterodine was generally well tolerated in clinical trials of up to 24 months' duration. Dry mouth was the most frequent adverse event. The incidence (40 vs 78%, p < 0.001) and intensity of this event was lower with tolterodine 2mg twice daily than oxybutynin 5mg 3 times daily. Additionally, a 23% lower incidence of dry mouth was reported with once daily extended-release tolterodine capsules than with twice daily immediate-release tablets (p < 0.02). The incidence of adverse CNS events with tolterodine was low and similar to that of placebo. Tolterodine was well tolerated in elderly patients and no serious tolerability concerns were identified. CONCLUSION: Tolterodine is the first antimuscarinic agent to specifically developed for the treatment of overactive bladder. The functional selectivity of tolterodine for the bladder translates into good efficacy and tolerability in patients, including the elderly, with overactive bladder. Tolterodine is as effective as oxybutynin in improving micturition diary variables but is associated with a significantly lower incidence and intensity of dry mouth. This favourable tolerability profile, together with sustained clinical efficacy during long term treatment, places tolterodine as valuable treatment for the symptoms of overactive bladder.  相似文献   

17.
Deeks ED  Perry CM 《Drugs & aging》2008,25(11):963-986
Zoledronic acid (Aclasta; Reclast), a third-generation nitrogen-containing bisphosphonate, is the first once-yearly treatment to have been approved for use in patients with postmenopausal osteoporosis or at high risk of fracture. Intravenous zoledronic acid 5 mg once yearly is effective in reducing the risk of several types of fracture in patients with postmenopausal osteoporosis or recent low-trauma hip fracture. Moreover, improvements in bone mineral density (BMD) and reductions in markers of bone turnover are also generally observed. Zoledronic acid is generally well tolerated. Additional comparative data are required to definitively position zoledronic acid with respect to other agents. In the meantime, intravenous zoledronic acid 5 mg once yearly is a convenient and effective treatment option that may have an advantage over some other agents, for which adherence to treatment regimens is a recognized problem.  相似文献   

18.
Moen MD  Keam SJ 《Drugs & aging》2011,28(1):63-82
Denosumab (Prolia?) is a human recombinant monoclonal antibody that is approved for the treatment of postmenopausal osteoporosis in women at high or increased risk of fracture in the US, the EU and several other countries. Denosumab has a novel mechanism of action; it binds to receptor activator of nuclear factor κB ligand and inhibits bone resorption by inhibiting osteoclast formation, function and survival. In postmenopausal women with osteoporosis, denosumab reduced the risk of vertebral, nonvertebral and hip fractures compared with placebo over 3 years in the large, phase III FREEDOM study. In postmenopausal women with low bone mineral density (BMD) or osteoporosis, treatment with denosumab increased BMD and decreased markers of bone turnover more than alendronate in those who were essentially treatment-naive in the 1-year DECIDE study and also in the 1-year STAND study, in which women were switched from alendronate to denosumab or continued alendronate treatment. Denosumab was generally well tolerated in clinical trials, although long-term effects of very low bone turnover remain to be established. Denosumab is administered once every 6 months via subcutaneous injection, which may be a preferred method of administration and may improve adherence to treatment compared with other osteoporosis treatments. Denosumab is a valuable new option for the treatment of postmenopausal osteoporosis in women at increased or high risk of fractures, and may be useful as a first-line treatment in women at increased risk of fractures who are unable to take other osteoporosis treatments.  相似文献   

19.
Risperidone: a review of its use in the treatment of bipolar mania   总被引:2,自引:0,他引:2  
Fenton C  Scott LJ 《CNS drugs》2005,19(5):429-444
Risperidone (Risperdal) is an atypical antipsychotic with high affinity for 5-hydroxytryptamine (5-HT)2A, dopamine D2 and alpha1- and alpha2-adrenergic receptors. Risperidone is now approved in the UK and the US for use in bipolar mania. Risperidone < or =6 mg/day, as monotherapy or adjunctive therapy with first-line mood stabilisers, significantly improves moderate and severe bipolar mania and improves global functioning over 3 weeks. Improvements in Young Mania Rating Scale (YMRS) scores in double-blind trials were greater with risperidone than with placebo over 3 weeks, and similar to those with haloperidol over 3 and 12 weeks. Risperidone was reasonably well tolerated. Limited data are available on the combination of risperidone and carbamazepine. Risperidone, as monotherapy or combined therapy with lithium or valproate semisodium, is an effective treatment option in bipolar mania.  相似文献   

20.
McCormack PL  Keating GM 《Drugs》2006,66(8):1129-1149
Eletriptan (Relpax) is an orally administered, lipophilic, highly selective serotonin 5-HT(1B/1D) receptor agonist ('triptan') that is effective in the acute treatment of moderate to severe migraine attacks in adults. It has a rapid onset of action and demonstrates superiority over placebo as early as 30 minutes after the administration of a single 40 or 80 mg oral dose. The efficacy of eletriptan 20 mg was similar to that of sumatriptan 100 mg, while eletriptan 40 and 80 mg displayed greater efficacy than sumatriptan 50 or 100 mg for most endpoints. Eletriptan 40 mg was generally superior to naratriptan 2.5 mg and equivalent to almotriptan 12.5 mg, rizatriptan 10 mg and zolmitriptan 2.5 mg, while eletriptan 80 mg was superior to zolmitriptan 2.5 mg for most efficacy parameters. Eletriptan 40 and 80 mg were consistently superior to ergotamine/caffeine. Eletriptan is generally well tolerated, reduces time lost from normal activities, improves patients' health-related quality of life and appears to be at least as, if not more, cost effective than sumatriptan. Eletriptan is therefore a useful addition to the triptan family and a first-line treatment option in the acute management of migraine attacks.  相似文献   

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