34.抗癲癇藥物Lamotrigine與下列那一種藥物併用時,Lamotrigine的代謝半衰期可以被延長?
(A)Phenytoin
(B)Topiramate
(C)Valproic acid
(D)Tiagabine
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統計: A(858), B(280), C(4807), D(233), E(0) #722421
統計: A(858), B(280), C(4807), D(233), E(0) #722421
詳解 (共 9 筆)
#1231461
valproic acid 是傳統抗抗癲癇藥物中唯一的CYP inhibitor,也就是唯一會抑制代謝的抗癲癇藥
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#1517472
valproic ㊀CYP2C9
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#5211732
(A)Phenytoin:阻斷Na+通道;大發作、心律不整(Class IB)、毛地黃中毒【→齒齦增生、軟骨症、巨球型貧血、SJS、致畸胎;劑量:眼球震顫、運動失調】
(B)Topiramate:阻斷Na+通道、抑制T-type Ca2+;局部、陣攣性、預防性頭痛【→體重下降、腎結石、青光眼、骨質疏鬆、降低口服避孕藥(Ethinyl estradiol)濃度】
(C)Valproic acid:阻斷Na+通道、抑制GABA-T、抑制T-type Ca2+;廣效性、躁鬱症;唯一抑制代謝的抗癲癇藥【→肝毒性、禿頭、體重上升、抑制血小板凝集、胎兒神經管缺陷】
(D)Tiagabine:阻斷GABA回收;血漿蛋白結合律95%【→波峰性僵直Spike-wave stupor】
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#3455907
Foye's medichem-7th 課本:
The presence of valproate increases the lamotrigine half-life substantially by inhibiting N-glucuronidation, necessitating a reduction in dose to avoid toxicity.
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#993068
Coadministration with valproic acid has been shown to significantly increase the plasma concentrations of lamotrigine.
The mechanism is competitive inhibition of lamotrigine glucuronidation by valproic acid.
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