Tìm theo
Cevimeline
Các tên gọi khác (4 ) :
  • 2-Methyspiro(1,3-oxathiolane-5,3)quinuclidine
  • Cevimelina
  • Cevimelinum
  • Sni 2011
Thuốc Gốc
Small Molecule
CAS: 107233-08-9
ATC: N07AX03
ĐG : Astellas Pharma Inc. , http://www.astellas.com
CTHH: C10H17NOS
PTK: 199.313
Cevimeline is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors. It is indicated by the Food and Drug Administration for the treatment of dry mouth associated with Sjögren's syndrome. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H17NOS
Phân tử khối
199.313
Monoisotopic mass
199.103084861
InChI
InChI=1S/C10H17NOS/c1-8-12-10(7-13-8)6-11-4-2-9(10)3-5-11/h8-9H,2-7H2,1H3/t8?,10-/m1/s1
InChI Key
InChIKey=WUTYZMFRCNBCHQ-LHIURRSHSA-N
IUPAC Name
(2R)-5'-methyl-4-azaspiro[bicyclo[2.2.2]octane-2,2'-[1,4]oxathiolane]
Traditional IUPAC Name
cevimeline
SMILES
CC1O[C@@]2(CS1)CN1CCC2CC1
Độ tan chảy
201-203 °C (HCl salt)
Độ hòa tan
Very soluble
logP
1.3
logS
-1.9
pKa (Strongest Basic)
8.59
PSA
12.47 Å2
Refractivity
55.92 m3·mol-1
Polarizability
21.89 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Cevimeline is a cholinergic agonist which binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands and increase tone of the smooth muscle in the gastrointestinal and urinary tracts.
Cơ Chế Tác Dụng : Cevimeline is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors. It is indicated by the Food and Drug Administration for the treatment of dry mouth associated with Sjögren's syndrome. [Wikipedia] Muscarinic agonists such as cevimeline bind and activate the muscarinic M1 and M3 receptors. The M1 receptors are common in secretory glands (exocrine glands such as salivary and sweat glands), and their activation results in an increase in secretion from the secretory glands. The M3 receptors are found on smooth muscles and in many glands which help to stimulate secretion in salivary glands, and their activation generally results in smooth muscle contraction and increased glandular secretions. Therefore, as saliva excretion is increased, the symptoms of dry mouth are relieved.
Dược Động Học :
▧ Absorption :
Rapidly absorbed with peak concentration after 1.5 to 2 hours
▧ Volume of Distribution :
* 6 L/kg
▧ Protein binding :
< 20%
▧ Metabolism :
Primarily hepatic, isozymes CYP2D6 and CYP3A4 are responsible for the metabolism of cevimeline. Approximately 44.5% of the drug is converted to cis and trans-sulfoxide, 22.3% to glucuronic acid conjugate, and 4% to N-oxide of cevimeline. Approximately 8% of the trans-sulfoxide metabolite is then converted into the corresponding glucuronic acid conjugate.
▧ Route of Elimination :
After 24 hours, 84% of a 30 mg dose of cevimeline was excreted in urine.
▧ Half Life :
5 ± 1 hours
Chỉ Định : For the treatment of symptoms of dry mouth in patients with Sjögren's Syndrome.
Tương Tác Thuốc :
  • Conivaptan Conivaptan may increase the serum concentration of CYP3A4 substrates such as cevimeline. Upon completion/discontinuation of conivaptan, allow at least 7 days before initiating therapy with drugs that are CYP3A4 substrates.
  • Tacrine The acetylcholinesterase inhibitor, Tacrine, may increase the adverse/toxic effects of Cevimeline, a cholinergic agonist. Monitor for increased cholinergic effects and toxicity.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Evoxac 30 mg capsule
    Giá bán buôn : USD >2.69
    Đơn vị tính : capsule
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Evoxac
  • Công ty :
    Sản phẩm biệt dược : Saligren
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00185
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00661
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/63395-201-13
PharmGKB
http://www.pharmgkb.org/drug/PA164754754
Wikipedia
http://en.wikipedia.org/wiki/Cevimeline
RxList
http://www.rxlist.com/cgi/generic/cevimeline.htm
Drugs.com
http://www.drugs.com/cdi/cevimeline.html
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