Tìm theo
Ropivacaine
Các tên gọi khác (6 ) :
  • (S)-(−)-1-propyl-2',6'-pipecoloxylidide
  • (S)-ropivacaine
  • L-N-n-propylpipecolic acid-2,6-xylidide
  • Ropivacaina
  • Ropivacaine
  • Ropivacainum
Thuốc gây mê
Thuốc Gốc
Small Molecule
CAS: 84057-95-4
ATC: N01BB09
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C17H26N2O
PTK: 274.4011
Ropivacaine is a local anaesthetic drug belonging to the amino amide group. The name ropivacaine refers to both the racemate and the marketed S-enantiomer. Ropivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Naropin. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H26N2O
Phân tử khối
274.4011
Monoisotopic mass
274.204513464
InChI
InChI=1/C17H26N2O/c1-4-11-19-12-6-5-10-15(19)17(20)18-16-13(2)8-7-9-14(16)3/h7-9,15H,4-6,10-12H2,1-3H3,(H,18,20)/t15-/s2
InChI Key
InChIKey=ZKMNUMMKYBVTFN-GGYSOQFKNA-N
IUPAC Name
(2S)-N-(2,6-dimethylphenyl)-1-propylpiperidine-2-carboxamide
Traditional IUPAC Name
ropivacaine
SMILES
CCCN1CCCC[[email protected]]1C(=O)NC1=C(C)C=CC=C1C
Độ hòa tan
57.6 mg/L
logP
2.90
logS
-3
pKa (strongest acidic)
13.62
pKa (Strongest Basic)
7.82
PSA
32.34 Å2
Refractivity
85.59 m3·mol-1
Polarizability
32.67 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.07
Dược Lực Học : Ropivacaine, a local anesthetic agent, is indicated for the production of local or regional anesthesia or analgesia for surgery, for oral surgery procedures, for diagnostic and therapeutic procedures, and for obstetrical procedures.
Cơ Chế Tác Dụng : Ropivacaine is a local anaesthetic drug belonging to the amino amide group. The name ropivacaine refers to both the racemate and the marketed S-enantiomer. Ropivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Naropin. [Wikipedia] Local anesthetics such as Ropivacaine block the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. Specifically, they block the sodium-channel and decrease chances of depolarization and consequent action potentials. In general, the progression of anesthesia is related to the diameter, myelination and conduction velocity of affected nerve fibers.
Dược Động Học :
▧ Absorption :
Bioavailability is 87%–98% following epidural administration.
▧ Protein binding :
94%, mainly to a1-acid glycoprotein
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Ropivacaine is extensively metabolized in the liver, predominantly by aromatic hydroxylation mediated by cytochrome P4501A to 3-hydroxy ropivacaine. After a single IV dose approximately 37% of the total dose is excreted in the urine as both free and conjugated 3-hydroxy ropivacaine. In total, 86% of the ropivacaine dose is excreted in the urine after intravenous administration of which only 1% relates to unchanged drug.
▧ Half Life :
Approximately 4.2 hours.
▧ Clearance :
* 387 +/- 107 mL/min * unbound plasma clearance=7.2 +/- 1.6 L/min
Độc Tính : Systemic exposure to excessive quantities of ropivacaine mainly result in central nervous system (CNS) and cardiovascular effects – CNS effects usually occur at lower blood plasma concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations. CNS effects may include CNS excitation (nervousness, tingling around the mouth, tinnitus, tremor, dizziness, blurred vision, seizures) followed by depression (drowsiness, loss of consciousness, respiratory depression and apnea). Cardiovascular effects include hypotension, bradycardia, arrhythmias, and/or cardiac arrest – some of which may be due to hypoxemia secondary to respiratory depression.
Chỉ Định : Used in obstetric anesthesia and regional anesthesia for surgery.
Tương Tác Thuốc :
  • Fluvoxamine Increases the effect and toxicity of ropivacaine
Liều Lượng & Cách Dùng : Solution - Epidural
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Naropin
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