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Ropivacaine

产品号 DB00296 公司名称 DrugBank
CAS号 84057-95-4 公司网站 http://www.ualberta.ca/
分子式 C17H26N2O 电 话 (780) 492-3111
分子量 274.40114 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 181

产品价格信息

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产品别名

标题
Ropivacaine
IUPAC标准名
(2S)-N-(2,6-dimethylphenyl)-1-propylpiperidine-2-carboxamide
IUPAC传统名
@ropivacaine
商标名
Naropin
别名
Ropivacainum [INN-Latin]
Ropivacaine [INN]
Ropivacaina [Spanish]
Ropivacaina [INN-Spanish]
S-Ropivacaine

产品登记号

CAS号 84057-95-4

产品性质

疏水性(logP) 3
溶解度 57.6 mg/L

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description 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]
Indication Used in obstetric anesthesia and regional anesthesia for surgery.
Pharmacology 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.
Toxicity 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.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic
Absorption Bioavailability is 87%–98% following epidural administration.
Half Life Approximately 4.2 hours.
Protein Binding 94%, mainly to a1-acid glycoprotein
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.
Clearance * 387?+/- 107 mL/min
* unbound plasma clearance=7.2 +/- 1.6 L/min
References
Weinberg G, Ripper R, Feinstein DL, Hoffman W: Lipid emulsion infusion rescues dogs from bupivacaine-induced cardiac toxicity. Reg Anesth Pain Med. 2003 May-Jun;28(3):198-202. [Pubmed]
Picard J, Meek T: Lipid emulsion to treat overdose of local anaesthetic: the gift of the glob. Anaesthesia. 2006 Feb;61(2):107-9. [Pubmed]
Rosenblatt MA, Abel M, Fischer GW, Itzkovich CJ, Eisenkraft JB: Successful use of a 20% lipid emulsion to resuscitate a patient after a presumed bupivacaine-related cardiac arrest. Anesthesiology. 2006 Jul;105(1):217-8. [Pubmed]
External Links
Wikipedia
RxList
Drugs.com

参考文献

  • Weinberg G, Ripper R, Feinstein DL, Hoffman W: Lipid emulsion infusion rescues dogs from bupivacaine-induced cardiac toxicity. Reg Anesth Pain Med. 2003 May-Jun;28(3):198-202. Pubmed
  • Picard J, Meek T: Lipid emulsion to treat overdose of local anaesthetic: the gift of the glob. Anaesthesia. 2006 Feb;61(2):107-9. Pubmed
  • Rosenblatt MA, Abel M, Fischer GW, Itzkovich CJ, Eisenkraft JB: Successful use of a 20% lipid emulsion to resuscitate a patient after a presumed bupivacaine-related cardiac arrest. Anesthesiology. 2006 Jul;105(1):217-8. Pubmed