79517-01-4
基本信息
SMS-201-995
SANDOSTATIN
SMS 201-995ac
Sandostatin LAR
r*))-(racetate(salt)
Octreotide (SMS 201-995)
M.W. 1019.24 C49H66N10O10S2
OCTREOTIDE (SMS 201-995), ACETATE
FCFWKTCT-OL (DISULFIDE BRIDGE: 2-7)
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見問題列表
本品的化學(xué)結(jié)構(gòu)上的第1、 4、8個氨基酸為非天然氨基酸,故不易受酶破壞,半衰期亦較長。皮下注射本品吸收迅速而完全,血藥濃度達(dá)峰值時間為0.5小時,分布容積為0.27L/kg,半衰期為1.5小時,代謝清除率為160ml/min。靜注時呈雙相消除,半衰期α相和β相分別為10 分鐘和90分鐘。血漿蛋白結(jié)合率為65%。
臨床上奧曲肽主要用于治療門脈高壓引起的食管靜脈曲張出蟲、肢端巨大癥、消化道出血如肝硬化、食管靜脈曲張出血、消化性潰瘍出血和應(yīng)激性潰瘍出血,胰腺疾病如重型急性胰腺炎、胰損傷或手術(shù)后胰腺瘺,以及預(yù)防胰腺手術(shù)后并發(fā)癥。還用于胃腸道瘺管,消化系內(nèi)分泌腫瘤如腸血管活性肽瘤、胃泌素瘤、胰高血糖素瘤、異位ACTH綜合征、類癌綜合征,肢端肥大癥,突眼性甲亢癥,全結(jié)腸切除后出現(xiàn)的持續(xù)性、頑固性腹瀉和艾滋病相關(guān)性腹瀉。鞘內(nèi)注射可治療癌性疼痛。
(2)治療門脈高壓引起的食管靜脈曲張出血:0.1mg靜脈注射, 以后0.5mg,每2小時1次靜脈滴注。
(3)應(yīng)激性潰瘍及消化道出血:0.1mg皮下注射,每日3次。
(4)重型胰腺炎:0.1mg皮下注射,每日4次,療程3~7天;胰損傷或手術(shù)后胰瘺,皮下注射,每次0.1mg,每8小時1次,連用7~14日。
(5)胃腸道瘺管和消化道內(nèi)分泌系統(tǒng)腫瘤的輔助治療:皮下注射0.1mg,每日3次,療程10~14天。
(6)消化系系內(nèi)分泌腫瘤、突眼性甲狀腺腫、肢端肥大癥及艾滋病相關(guān)性腹瀉:皮下注射0.1mg,每日3次,肢端肥大癥療程10~14天。用后主要有注射部位疼痛或針刺感,一般于15分鐘緩解。
消化道不良反應(yīng)有厭食、惡心、嘔吐、腹瀉、腹部痙攣疼痛等,偶見高血糖、膽石、糖耐量異常和肝功能異常(γ-谷氨酰轉(zhuǎn)移酶增高及轉(zhuǎn)氨酶輕度增高)等。腎、胰腺功能異常和膽石癥患者慎用。孕婦、哺乳期婦女和兒童禁用。
Octreotide-treated groups show a significant reduction in the tumor volume when compared with saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 μg/kg, i.p.). Octreotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC-bearing rats compared with the saline group. Octreotide-PPSG appears to inhibit the expression of SSTR2 and SSTR5 to a greater extent than that of Octreotide-soln treated group. A test dose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of the baseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-release formulation of octreotide acetatea (5 mg intramuscular, q 4 wk) is initiated.