Store at -20°C,unstable in solution, ready to use.
용해도
Ethanol: 100 mg/mL (242.97 mM)
안전
위험 및 안전 성명
위험 및 사전주의 사항 (GHS)
그림문자(GHS):
신호 어:
Warning
유해·위험 문구:
암호
유해·위험 문구
위험 등급
범주
신호 어
그림 문자
P- 코드
H302
삼키면 유해함
급성 독성 물질 - 경구
구분 4
경고
P264, P270, P301+P312, P330, P501
H315
피부에 자극을 일으킴
피부부식성 또는 자극성물질
구분 2
경고
P264, P280, P302+P352, P321,P332+P313, P362
H319
눈에 심한 자극을 일으킴
심한 눈 손상 또는 자극성 물질
구분 2A
경고
P264, P280, P305+P351+P338,P337+P313P
H335
호흡 자극성을 일으킬 수 있음
특정 표적장기 독성 - 1회 노출;호흡기계 자극
구분 3
경고
예방조치문구:
P261
분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P301+P312
삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P302+P352
피부에 묻으면 다량의 물로 씻으시오.
P305+P351+P338
눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
페소테로딘 C화학적 특성, 용도, 생산
개요
Fesoterodine, launched for the treatment of OAB, is an orally
active pro-drug that is converted in vivo to its active metabolite 5-HMT
through hydrolysis by non-specific esterases. 5-HMT is also an active
metabolite of tolterodine (Detrol), which has been marketed for the
treatment of OAB since 1998. 5-HMT is a potent muscarinic antagonist,
with essentially equivalent affinity for M1, M2, M3, M4, and M5
receptors (Ki＝0.32, 0.63, 1.26, 2, and 0.63 nM, respectively). The binding
of 5-HMT is stereoselective; the corresponding S-enantiomer has at least
100 times lower binding affinity for all five receptors. Fesoterodine is
supplied as its fumarate salt in an extended release tablet form. The
recommended starting dose is 4 mg once daily. On the basis of individual
response and tolerability, the dose may be increased to 8 mg once
daily. Following oral administration, fesoterodine is not detected in the
peripheral blood, thereby indicating a rapid and complete bioconversion
to 5-HMT. Bioavailability of 5-HMT is about 52%. After single- or
multiple-dose oral administration of fesoterodine in doses from 4 to
28 mg, plasma concentrations of 5-HMT are proportional to the dose.
Maximum plasma levels are reached after approximately 5 h. No
accumulation occurs after multiple-dose administration. 5-HMT is further metabolized in the liver through oxidation of the hydroxymethyl
group and oxidative cleavage of N-alkyl groups mediated by CYP2D6
and CYP3A4. 5-HMT and its metabolites are primarily eliminated through renal excretion. The most common adverse events associated with fesoterodine include dry mouth, constipation, and dyspepsia. Fesoterodine is contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma.
