Ropivacaine Hydrochloride Alias
Ropivacaine Hydrochloride CAS
Ropivacaine Hydrochloride MF
Ropivacaine Hydrochloride MW
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The pKa of ropivacaine was 8.1, and the distribution rate was 141 (25 OC n- octanol / phosphate buffer pH7.4). The plasma concentration of this product depends on the dose, route of administration and the distribution of blood vessels at the injection site. In line with linear pharmacokinetics, the maximum plasma concentration and dose are complete, biphasic, fast phase half-life of 14 minutes, and a half-life of 4 hours at the end of the slow phase. Slow absorption is the limiting factor for ropivacaine removal, so the clearance of epidural medication is longer than that of intravenous drug use. The total scavenging rate of ropivacaine was 440ml/min.
The free plasma scavenging rate was 8L/min. The renal clearance rate was 1ml/min, the steady-state volume was 47L, and the terminal half-life was 1.8 hours. The metabolic rate of ropivacaine in the middle of the liver was 0.4. In plasma, the binding rate of non 1- protein is mainly about 6%. When continuous epidural injection, the increase of total plasma concentration of ropivacaine is related to the increase of the concentration of alpha 1- glycoprotein after operation, and the changes of unbound (pharmacological activity) concentration are much smaller than that of the total plasma concentration. Ropivacaine easily passes through the placenta, and it balances quickly when it is relatively unbound. Compared with the maternal body, ropivacaine and plasma protein are low in the fetus, and the total plasma concentration of the fetus is lower than that of the mother.
Ropivacaine is fully metabolized by aromatic hydroxylation, and 86% of the total dose of ropivacaine is excreted through urine after intravenous injection, and only 1% of them are associated with unmetabolized drugs. The main metabolite is 3- hydroxy ropivacaine, about 37% of which are excreted from urine in the form of conjugates, and about 1% ~ 3% of 4- hydroxy ropivacaine, N- alkyl metabolites and 4- hydroxy alkyl metabolites in urine. Conjugated and unbound 3- hydroxy ropivacaine showed only detectable concentrations in plasma. 3- hydroxy ropivacaine and 4- hydroxy ropivacaine have local anesthetic effect, but the anesthetic effect is weaker than ropivacaine. Ropivacaine has no evidence of racemization in vivo.