Tìm theo
Crofelemer
Các tên gọi khác (2) :
  • Provir
  • SP-303
Thuốc Gốc
Small Molecule
CAS: 148465-45-6
Crofelemer, previously known as the investigational drug SP-303, is a novel proanthocyanidin purified from the bark latex of the Amazonian Croton tree Croton lechleri. It is marketed under the brand name Fulyzaq and indicated for the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy.
Dược Lực Học : Crofelemer is an inhibitor of secretory diarrhea via inhibition of the CFTR chloride transporter. Crofelemer is not an antimicrobial, and therefore does not drive the emergence of resistance; it does not inhibit motility, and therefore does not cause constipation or rebound diarrhea; and it is not systemically absorbed, reducing the potential for adverse drug interactions and toxicity.
Cơ Chế Tác Dụng : Crofelemer, previously known as the investigational drug SP-303, is a novel proanthocyanidin purified from the bark latex of the Amazonian Croton tree Croton lechleri. It is marketed under the brand name Fulyzaq and indicated for the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy. Crofelemer is an inhibitor of the cystic fibrosis transmembrane regulator chloride channel (CFTR), as evidenced by its activity on cell cultures, single cell patch clamps, single CFTR channels, and elaboration of mouse intestinal fluid secretion. Crofelemer also inhibits calcium activated chloride channels (CaCC), which in combination with CFTR, are expressed on the luminal side of intestinal cells. Crofelemer inhibition of both of these channels prevents water loss from diarrhea by inhibiting chloride secretion.
Dược Động Học :
▧ Absorption :
The absorption of crofelemer is minimal and crofelemer concentrations in plasma are below the level of quantitation (50 ng/mL).
▧ Volume of Distribution :
Since crofelemer is not significantly absorbed, volume of distribution was not quantified.
▧ Protein binding :
Since crofelemer is not significantly absorbed, protein binding was not quantified.
▧ Metabolism :
Since crofelemer is not significantly absorbed, no metabolites have been identified.
▧ Route of Elimination :
Since crofelemer is not significantly absorbed, the route of elimination has not been identified.
▧ Half Life :
Since crofelemer is not significantly absorbed, the half life was not determined.
▧ Clearance :
Since crofelemer is not significantly absorbed, clearance was not determined.
Độc Tính : The most common adverse effects are cough, flatulence, upper respiratory tract infection, bronchitis, and increased bilirubin.
Chỉ Định : For the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy.
Liều Lượng & Cách Dùng : Tablet, delayed release - Oral - 125MG
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : SALIX PHARMS
    Sản phẩm biệt dược : Fulyzaq
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04941
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03605
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/65649-802-02
Wikipedia
http://en.wikipedia.org/wiki/Crofelemer
RxList
http://www.rxlist.com/fulyzaq-drug.htm
Drugs.com
http://www.drugs.com/sfx/crofelemer-side-effects.html
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