Tìm theo
Flunarizine
Các tên gọi khác (3) :
  • 1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
  • Flunarizina
  • Flunarizinum
Thuốc điều trị đau nửa đầu
Thuốc Gốc
Small Molecule
CAS: 52468-60-7
ATC: N07CA03
CTHH: C26H26F2N2
PTK: 404.4948
Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H26F2N2
Phân tử khối
404.4948
Monoisotopic mass
404.206405252
InChI
InChI=1S/C26H26F2N2/c27-24-12-8-22(9-13-24)26(23-10-14-25(28)15-11-23)30-19-17-29(18-20-30)16-4-7-21-5-2-1-3-6-21/h1-15,26H,16-20H2/b7-4+
InChI Key
InChIKey=SMANXXCATUTDDT-QPJJXVBHSA-N
IUPAC Name
1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
Traditional IUPAC Name
flunarizine
SMILES
FC1=CC=C(C=C1)C(N1CCN(C\C=C\C2=CC=CC=C2)CC1)C1=CC=C(F)C=C1
Độ tan chảy
251.5
Độ hòa tan
1.68e-03 g/l
logP
5.78
logS
-5.4
pKa (Strongest Basic)
7.6
PSA
6.48 Å2
Refractivity
120.3 m3·mol-1
Polarizability
44.2 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity.
Cơ Chế Tác Dụng : Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. Flunarizine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Dược Động Học :
▧ Absorption :
85% following oral administration.
▧ Protein binding :
99% bound to plasma proteins
▧ Metabolism :
Hepatic, to two metabolites via N-dealylation and hydroxylation.
▧ Half Life :
18 days
Độc Tính : -Flunarizine should be used with care in patients with depression or those being prescribed other agents, such as phenothiazines, concurrently, which may cause extrapyramidal side-effects. -Acute overdosage has been reported and the observed symptoms were sedation, agitation and tachycardia. -Treatment of acute overdosage consists of charcoal administration, induction of emesis or gastric lavage, and supportive measures. No specific antidote is known.
Chỉ Định : Used in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.
Tương Tác Thuốc :
  • Triprolidine The CNS depressants, Triprolidine and Flunarizine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral
Tablet - Oral - 5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Italfarmaco
    Sản phẩm biệt dược : Flugeral
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Fluxarten
  • Công ty : Polifarma
    Sản phẩm biệt dược : Gradient
  • Công ty : Janssen
    Sản phẩm biệt dược : Sibelium
  • Công ty : AtralCipan
    Sản phẩm biệt dược : Zinasen
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04841
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=941361
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507129
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01303
ChemSpider
http://www.chemspider.com/Chemical-Structure.819216.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017702
PharmGKB
http://www.pharmgkb.org/drug/PA164776636
Wikipedia
http://en.wikipedia.org/wiki/Flunarizine
Drugs.com
http://www.drugs.com/international/flunarizine.html
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