눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P312
불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P321
(…) 처치를 하시오.
P330
입을 씻어내시오.
P332+P313
피부 자극이 생기면 의학적인 조치· 조언을 구하시오.
P337+P313
눈에 대한 자극이 지속되면 의학적인 조치· 조언를 구하시오.
P340
신선한 공기, 휴식, 호흡하기 쉬운 위치로 옮기고
P362
오염된 의복을 벗고 세척 후에 재사용하기
P403
환기가 잘 되는 곳에 보관하시오.
P403+P233
용기는 환기가 잘 되는 곳에 단단히 밀폐하여 저장하시오.
P405
밀봉하여 저장하시오.
P501
...에 내용물 / 용기를 폐기 하시오.
Almotriptan C화학적 특성, 용도, 생산
개요
Almotriptan was first marketed in Spain as a new medicine against acute attacks of
migraine. It is the fifth agent belonging to the “triptan” class to be launched after
sumatriptan, naratriptan, zolmitriptan and rizatriptan. This close structural analog of
sumatriptan can be prepared in six steps from 4-nitrobenzylsulfonyl chloride with a Fischer
indole synthesis as the key step. Almotriptan acts as a dual 5-HT1D/1B agonist with a 35 to
51-fold selectivity versus 5-HT1A and 5-HT7 receptors respectively as well as having
insignificant affinity for the most relevant nonserotonergic receptors (K1＞1μM). Its
agonistic effect on 5-HT,n receptors of trigeminal sensory neurons turns off neurogenic
inflammation by inhibiting the release of neuropeptides such as calcitonin gene-related
peptide, neurokinin A and substance P. Concomitantly, its action on the 5-HT1B receptors
in meningeal arteries relieves the vasodilatation of these vessels associated with migraine
attacks. Almotriptan causes selective concentration-dependent vasoconstriction of human
meningeal and temporal arteries (with EC50 of 0.03 and 0.7 μM) compared to basilar (EC50
= 3.5 μM) and pulmonary arteries (EC50＞10μM) or rabbit mesenteric and renal arteries
(EC50＞100 μM). Although it is predominantly cleared by the kidneys as unchanged drug
(45%) or transformed into inactive metabolites by monoamine oxidase A (MAO-A) and
CYP3A4 enzymes in the liver, almotriptan has the highest oral bioavailability (70%) of the
triptans and has a half-life of 3.5 h. The therapeutic dose of 12.5 mg is well tolerated,
shows a rapid onset of action (30 min) and low recurrence rate compared to sumatriptan.
용도
Serotonin 5HT1B /1D-receptor agonist
정의
ChEBI: An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position.
