Tìm theo
Fospropofol
Các tên gọi khác (1) :
  • Fospropofol
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 258516-87-9
CTHH: C13H21O5P
PTK: 288.2766
Fospropofol is a water soluble prodrug and is converted to propofol in the liver. Fospropofol is a short acting hypnotic/sedative/anesthetic agent. Unlike propofol, does not cause injection-site pain as it is unable to activate TRPA1. FDA approved in December 2008. Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H21O5P
Phân tử khối
288.2766
Monoisotopic mass
288.112660294
InChI
InChI=1S/C13H21O5P/c1-9(2)11-6-5-7-12(10(3)4)13(11)17-8-18-19(14,15)16/h5-7,9-10H,8H2,1-4H3,(H2,14,15,16)
InChI Key
InChIKey=QVNNONOFASOXQV-UHFFFAOYSA-N
IUPAC Name
[2,6-bis(propan-2-yl)phenoxymethoxy]phosphonic acid
Traditional IUPAC Name
fospropofol
SMILES
CC(C)C1=CC=CC(C(C)C)=C1OCOP(O)(O)=O
Độ hòa tan
3.02e-01 g/l
logP
3.6
logS
-3
pKa (strongest acidic)
1.44
pKa (Strongest Basic)
-5
PSA
75.99 Å2
Refractivity
72.88 m3·mol-1
Polarizability
29 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-2
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.2 - 9.0
Dược Lực Học : Fospropofol is a prodrug of propofol, a sedative hypnotic drug. Unlike propofol, fospropofol is water soluble and can be administered in an aqueous solution. 1.86 mg of fospropofol is the molar equivalent for 1mg of propofol.
Cơ Chế Tác Dụng : Fospropofol is a water soluble prodrug and is converted to propofol in the liver. Fospropofol is a short acting hypnotic/sedative/anesthetic agent. Unlike propofol, does not cause injection-site pain as it is unable to activate TRPA1. FDA approved in December 2008. Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act. After in-vivo conversion of fospropofol into propofol by endothelial alkaline phosphatase, propofol crosses the blood-brain barrier, binds to GABA-A receptors and acts as an agonist. By binding to GABA-A receptor, it will cause an increase in chloride conductance, thus inhibiting the firing of new action potentials in the post-synaptic neuron.
Dược Động Học :
▧ Absorption :
Adequate sedation achieved after 7 minutes with a IV bolus dose of 10mg/kg. It takes 21-45 minutes for patients to recover for fospropopol-induced sedation. Following an intravenous bolus administration of 6 mg/kg in a healthy subject, the pharmacokinetic parameters of fospropofol are as follows: Cmax = 78.7 μg/mL; Tmax = 4 minutes; AUC(0-∞) = 19.0 μg ⋅ h/mL;
▧ Volume of Distribution :
Fospropofol = 0.33±0.069 L/kg; Propofol metabolite = 5.8 L/kg.
▧ Protein binding :
Both fospropofol and its active metabolite propofol are highly protein bound (approximately 98%), primarily to albumin. Fospropofol does not affect the binding of propofol to albumin.
▧ Metabolism :
Fospropofol is metabolized into propofol, formaldehyde, and phosphate by endothelial alkaline phosphatase. The metabolite, formaldehyde, is quickly oxidized into formic acid by glutathione dependent and independent dehydrogenases and erythrocytes. Excess formic acid is eliminated via oxidation to carbon dioxide through the tetrahydrofolate pathway. Propofol is further metabolized into propofol glucuronide, quinol-4-sulfate, quinol-1-fluronide, and quinol-4-glucuronide. The cytochrome P450 enzyme system is not involved with the metabolism of fospropofol.
▧ Route of Elimination :
Chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney. There is negligible renal elimination of unchanged fospropofol (<0.02%).
▧ Half Life :
When given to a patient, the half-lives are as follows: Fospropofol = 0.81 hours; Propofol metabolite = 1.13 hours
▧ Clearance :
Total body clearance (CLp), Fospropofol, healthy subject = 0.28 L/h/kg; CLp, fospropofol, patients = 0.31 L/h/kg; CLp/F, propofol, healthy subjects or patients = 2.74 L/h/kg.
Độc Tính : Overdosage may lead to cardiorespiratory depression, formic acid toxicity (methanol toxicity-like effects), and/or phosphate-induced hypocalemia. Most common adverse reactions (> 20%) are paresthesia and pruritus.
Chỉ Định : For monitored anaesthesia care sedation in patients undergoing diagnostic procedures like bronchoscopy and colonscopy or minor surgical procedures like arthroscopy and bunionectomy.
Liều Lượng & Cách Dùng : Injection, solution - Intravenous - 35 mg/mL
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aquavan
  • Công ty : Eisai Inc.
    Sản phẩm biệt dược : Lusedra
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06716
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04257
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/62856-350-08
PharmGKB
http://www.pharmgkb.org/drug/PA165958389
Wikipedia
http://en.wikipedia.org/wiki/Fospropofol
RxList
http://www.rxlist.com/lusedra-drug.htm
Drugs.com
http://www.drugs.com/ppa/fospropofol.html
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