止敏吐膠囊80毫克

国家: 台湾

语言: 中文

来源: 衛生福利部食品藥物管理署 (Ministry of Health and Welfare, Food And Drug Administration)

有效成分:

APREPITANT

可用日期:

美商默沙東藥廠股份有限公司台灣分公司 台北市信義區信義路五段106號12樓 (86683720)

ATC代码:

A04AD12

药物剂型:

膠囊劑

组成:

APREPITANT (9200095800) MG

每包单位数:

鋁箔盒裝

类:

製　劑

处方类型:

須由醫師處方使用

厂商:

ALKERMES PHARMA IRELAND LIMITED MONKSLAND ATHLONE CO. WESTMEATH, IRELAND IE

治疗领域:

aprepitant

疗效迹象:

與其他止吐藥劑併用，可以防止由高致吐性及中致吐性癌症化療藥物在初次或重覆使用時所引起的急性或延遲性噁心與嘔吐。

產品總結:

有效日期: 2024/05/14; 英文品名: EMEND CAPSULES 80MG

授权日期:

2004-05-14

资料单张

EMEND™ CAPSULES
(APREPITANT)
THERAPEUTIC CLASS
EMEND
*
(aprepitant), is a substance P neurokinin 1 (NK
1
) receptor antagonist.
COMPOSITION
Each capsule of EMEND for oral administration contains either 80 mg,
or 125 mg of aprepitant.
Each capsule of EMEND contains the following inactive ingredients:
sucrose, microcrystalline
cellulose, hydroxypropyl cellulose and sodium lauryl sulfate. The
capsule shell excipients are
gelatin and titanium dioxide, and may contain sodium lauryl sulfate
and silicon dioxide. The 125-
mg capsule shell also contains red ferric oxide and yellow ferric
oxide.
CLINICAL PHARMACOLOGY
_MECHANISM OF ACTION_
Aprepitant has a unique mode of action; it is a selective high
affinity antagonist at human
substance P neurokinin 1 (NK
1
) receptors. Counter-screening assays showed that aprepitant
was at least 3,000-fold selective for the NK
1
receptor over other enzyme, transporter, ion
channel and receptor sites including the dopamine and serotonin
receptors that are targets for
existing chemotherapy induced nausea and vomiting (CINV) therapies.
NK
1
-receptor antagonists have been shown pre-clinically to inhibit emesis
induced by cytotoxic
chemotherapeutic agents, such as cisplatin, via central actions.
Preclinical and human Positron
Emission Tomography (PET) studies with aprepitant have shown that it
is brain penetrant and
occupies brain NK
1
receptors. Preclinical studies show that aprepitant has a long
duration of
central activity, inhibits both the acute and delayed phases of
cisplatin-induced emesis, and
augments
the
antiemetic
activity
of
the
5-HT
3
-receptor
antagonist
ondansetron
and
the
corticosteroid dexamethasone against cisplatin-induced emesis.
_PHARMACOKINETICS _
_ABSORPTION_
The mean absolute oral bioavailability of aprepitant is approximately
60 to 65% and the mean
peak plasma concentration (C
max
) of aprepitant occurred at approximately 4 hours (T
max
). Oral
administration of the capsule with a standard breakfast had no
clinically meaningful effect on the
bioavailability of apr