Tìm theo
Fesoterodine
Các tên gọi khác (2) :
  • FESO
  • Fesoterodine
muscarinic antagonists, anti incontinence agents, antispasmodics, muscle relaxants genitourinary
Thuốc Gốc
Small Molecule
CAS: 286930-03-8
ATC: G04BD11
CTHH: C26H37NO3
PTK: 411.5769
Fesoterodine is an antimuscarinic prodrug for the treatment of overactive bladder syndrome.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H37NO3
Phân tử khối
411.5769
Monoisotopic mass
411.277344055
InChI
InChI=1S/C26H37NO3/c1-18(2)26(29)30-25-13-12-21(17-28)16-24(25)23(22-10-8-7-9-11-22)14-15-27(19(3)4)20(5)6/h7-13,16,18-20,23,28H,14-15,17H2,1-6H3/t23-/m1/s1
InChI Key
InChIKey=DCCSDBARQIPTGU-HSZRJFAPSA-N
IUPAC Name
2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate
Traditional IUPAC Name
fesoterodine
SMILES
CC(C)N(CC[C@H](C1=CC=CC=C1)C1=C(OC(=O)C(C)C)C=CC(CO)=C1)C(C)C
Độ hòa tan
Highly soluble
logP
5.7
logS
-5.3
pKa (strongest acidic)
14.98
pKa (Strongest Basic)
10.64
PSA
49.77 Å2
Refractivity
124.08 m3·mol-1
Polarizability
48.29 Å3
Rotatable Bond Count
11
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
0
Dược Lực Học : Fesoterodine is a prodrug. In-vivo it is broken down into its active metabolite, 5-hydroxymethyl tolterodine (5-HMT), by plasma esterases. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. Therefore, acting as a competitive muscarinic receptor antagonist, fesoterodine ultimately acts to decrease the detrusor pressure by its muscarinic antagonism, thereby decreasing bladder contraction and consequently, the urge to urinate.
Cơ Chế Tác Dụng : Fesoterodine is an antimuscarinic prodrug for the treatment of overactive bladder syndrome. Fesoterodine, once converted to its active metabolite, 5-hydroxymethyltolterodine, acts as a competitive antagonists at muscarinic receptors. This results in the inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.
Dược Động Học :
▧ Absorption :
Tmax (5-HMT): 5 hours post-adminitration of fesoterodine. AUC (0,∞)= 49.5 ng·h/ ml Bioavailability, 5-HMT = 52%
▧ Volume of Distribution :
IV, 5-HMT: 169 L
▧ Protein binding :
5-HMT: 50% to albumin and alpha1-acid glycoprotein
▧ Metabolism :
Metabolized by ubiquitous, nonspecific esterases to transform fesoterodine into 5-HMT Extensive metabolism via CYP2D6 and CYP3A4 into inactive metabolites
▧ Route of Elimination :
Renal: 70% of fesoterodine was recovered in urine as 5-HMT; 35% carboxy metabolite; 18% carboxy-N-desisopropylmetabolite, and 1% N-desisopropyl metabolite Fecal: 7% Hepatic: fesoterodine elimination via CYP2D6 and CYP3A4
▧ Half Life :
7-8 hours for the active metabolite 5-hydroxymethyl tolterodine
▧ Clearance :
5-HMT, healthy subjects: 14.4 L/h 5-HMT is also secreted into the nephron.
Độc Tính : Rat, Oral, LD50: ~ 681 mg/kg Mouse, Oral, LD50: ~ 316 mg/kg Rat, Intravenous, NOAEL: 10 mg/kg Mouse, Intravenous, NOAEL: 10 mg/kg
Chỉ Định : For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
Tương Tác Thuốc :
  • Conivaptan CYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Fesoterodine. Avoid fesoterodine doses greater than 4mg daily in patients who are also receiving strong CYP3A4 inhibitors.
  • Fluconazole Fluconazole is a moderate CYP3A4 inhibitor thus reducing clearance. Monitor for adverse effects when using concomitant therapy with fesoterodine.
  • Ketoconazole Ketoconazole is a potent CYP3A4 inhibitor thus reducing clearance. Avoid concomitant use with fesoterodine.
Liều Lượng & Cách Dùng : Tablet - Oral - 4 mg
Tablet - Oral - 8 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Pfizer
    Sản phẩm biệt dược : Toviaz
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06702
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6918558
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443256
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07226
ChemSpider
http://www.chemspider.com/Chemical-Structure.5293755.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54868-6175-0
PharmGKB
http://www.pharmgkb.org/drug/PA165958376
Wikipedia
http://en.wikipedia.org/wiki/Fesoterodine
RxList
http://www.rxlist.com/toviaz-drug.htm
Drugs.com
http://www.drugs.com/cdi/fesoterodine.html
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