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霜葉金蟲 (小有名氣)
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[求助]
急求外文一段摘要翻譯,謝謝
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| Triptans are a new class of compounds developed for the treatment of migraine attacks. The first of the class, sumatriptan, and the newer triptans (zolmitriptan, naratriptan, rizatriptan, eletriptan, almotriptan and frovatriptan) display high agonist activity at mainly the serotonin 5-HT1B and 5-HT1D receptor subtypes. As expected for a class of compounds developed for affinity at a specific receptor, there are minor pharmacodynamic differences between the triptans. Sumatriptan has a low oral bioavailability (14%) and all the newer triptans have an improved oral bioavailability and for one, risatriptan, the rate of absorption is faster. The half-lives of naratriptan, eletriptan and, in particular, frovatriptan (26 to 30h) are longer than that of sumatriptan (2h). These pharmacokinetic improvements of the newer triptans so far seem to have only resulted in minor differences in their efficacy in migraine. Double-blind, randomised clinical trials (RCTs) comparing the different triptans and triptans with other medication should ideally be the basis for judging their place in migraine therapy. In only 15 of the 83 reported RCTs were 2 triptans compared, and in 11 trials triptans were compared with other drugs. Therefore, in all placebo-controlled randomised clinical trials, the relative efficacy of the triptans was also judged by calculating the therapeutic gain (i.e. percentage response for active minus percentage response for placebo). The mean therapeutic gain with subcutaneous sumatriptan 6mg (51%) was more than that for all other dosage forms of triptans (oral sumatriptan 100mg 32%; oral sumatriptan 50mg 29%: intranasal sumatriptan 20mg 30%; rectal sumatriptan 25mg 31%; oral zolmitriptan 2.5mg 32%; oral rizatriptan 10mg 37%; oral eletriptan 40mg 37%; oral almotriptan 12.5mg 26%). Compared with oral sumatriptan 100mg (32%), the mean therapeutic gain was higher with oral eletriptan 80mg (42%) but lower with oral naratriptan 2.5mg (22%) or oral frovatriptan 2.5mg (16%). The few direct comparative randomised clinical trials with oral triptans reveal the same picture. Recurrence of headache within 24 hours after an initial successful response occurs in 30 to 40% of sumatriptan-treated patients. Apart from naratriptan, which has a tendency towards less recurrence, there appears to be no consistent difference in recurrence rates between the newer triptans and sumatriptan. Rizatriptan with its shorter time to maximum concentration (tmax) tended to produce a quicker onset of headache relief than sumatriptan and zolmitriptan. The place of triptans compared with non-triptan drugs in migraine therapy remains to be established and further RCTs are required. |
木蟲 (著名寫手)
Tiny
| 曲坦類藥物是一類新的化合物開發(fā)治療偏頭痛發(fā)作。第一個(gè)類,作為舒馬曲坦和新的曲坦類藥物(佐米曲坦)顯示高5 -羥色胺受體激動(dòng)劑主要活動(dòng)5-HT1B和5-HT1D受體亞型。如預(yù)期的一類化合物開發(fā)在一個(gè)特定的受體的親和力,會(huì)有小的藥效學(xué)差異曲坦類藥物。口服生物利用度作為舒馬曲坦低(14%)和所有的新曲坦類藥物口服生物利用度和改進(jìn),吸收的速度更快。。這些藥代動(dòng)力學(xué)改進(jìn)新的曲坦類藥物目前為止似乎只有微小差別導(dǎo)致其功效在偏頭痛。雙盲、隨機(jī)臨床試驗(yàn)比較不同與其他藥物曲坦類藥物和曲坦類藥物應(yīng)該是依據(jù)他們的位置來(lái)判斷在偏頭痛治療。在83年的報(bào)道只有15冥想是2曲坦類藥物比較,在11個(gè)試驗(yàn)與其他藥物比較曲坦類藥物。因此,在所有隨機(jī)安慰劑對(duì)照臨床試驗(yàn),相對(duì)有效性的鑒定由計(jì)算曲坦類藥物治療增益(即百分比響應(yīng)百分比響應(yīng)積極減去安慰劑)。平均治療增益與皮下作為舒馬曲坦6毫克(51%)超過(guò)所有其他劑型的曲坦類藥物(口服100毫克作為舒馬曲坦32%;口腔作為舒馬曲坦50毫克29%:鼻作為舒馬曲坦20 mg的30%;直腸作為舒馬曲坦25 mg 31%;口服佐米曲坦2.5毫克口服 32%;10毫克37%;口腔 40毫克37%;口腔12.5毫克的26%)。作為舒馬曲坦相比口服100毫克(32%),平均治療增益較高口服80毫克(42%),但較低的口服 2.5毫克(22%)或口頭 2.5毫克(16%)。為數(shù)不多的直接比較的隨機(jī)臨床試驗(yàn)顯示同樣的畫面口服曲坦類藥物。頭痛復(fù)發(fā)后24小時(shí)之內(nèi)最初成功的響應(yīng)發(fā)生在30 ~ 40%的病人治療作為舒馬曲坦。除了減少?gòu)?fù)發(fā)傾向,似乎沒有一致的差異之間的復(fù)發(fā)率較新的曲坦類藥物和作為舒馬曲坦。以其短時(shí)間最大濃度(達(dá)峰時(shí)間)傾向于產(chǎn)生更快緩解頭痛發(fā)作的比作為舒馬曲坦和佐米曲坦。曲坦類藥物的地方而非曲普坦藥物治療偏頭痛仍有待建立和進(jìn)一步需要冥想。 |

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