Ropivacaine drug data and news

Ropivacaine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Ropivacaine
Brand Names/Synonyms Ropivacaine; Ropivacaine [INN]; Ropivacaina [Spanish]; Ropivacainum [INN-Latin]; Ropivacaina [INN-Spanish]; Naropin; S-Ropivacaine
Indication Used in obstetric anesthesia and regional anesthesia for surgery
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Description Not Available
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.
Mechanism Of Action 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. In general, the progression of anesthesia is related to the diameter, myelination and conduction velocity of affected nerve fibers.
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Dosage Forms LIQUID; SOLUTION
Drug_Category Anesthetics; Local Anesthetics; ATC:N01BB09
Absorption Not Available
Interactions Interactions for Ropivacaine: Ropivacaine should be used with caution in patients receiving other local anesthetics or agents structurally related to amide-type local anesthetics, since the toxic effects of these drugs are additive. Cytochrome P4501A2 is involved in the formation of 3-hydroxy ropivacaine, the major metabolite. In vivo, the plasma clearance of ropivacaine was reduced by 70% during coadministration of fluvoxamine (25 mg bid for 2 days), a selective and potent CYP1A2 inhibitor. Thus strong inhibitors of cytochrome P4501A2, such as fluvoxamine, given concomitantly during administration of Ropivacaine, can interact with Ropivacaine leading to increased ropivacaine plasma levels. Caution should be exercised when CYP1A2 inhibitors are coadministered. Possible interactions with drugs known to be metabolized by CYP1A2 via competitive inhibition such as theophylline and imipramine may also occur. Coadministration of a selective and potent inhibitor of CYP3A4, ketoconazole (100 mg bid for 2 days with ropivacaine infusion administered 1 hour after ketoconazole) caused a 15% reduction in in-vivo plasma clearance of ropivacaine.
Toxicity Not Available
Organisms Affected Humans and other mammals
Chemical IUPAC Name N-(2,6-dimethylphenyl)-1-propyl-piperidine-2-carboxamide
Chemical Formula C17H26N2O
Molecular Weight 274.401 g/mol
Smiles String CCCN1CCCCC1C(=O)NC2=C(C=CC=C2C)C
Melting Point Not Available
Water Solubility 57.6 mg/L
State Solid
LogP/Hphobicity 3.537
Isoelectric Point 8.07
Biotransformation Hepatic
Half Life ~4.2 hrs
Protein Binding [%] 94%, mainly to a1-acid glycoprotein
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Drug Reference http://www.drugs.com/cons/Ropivacaine.html
http://www.rxlist.com/cgi/generic2/ropiva.htm
Drug Type Approved Drug
Accession No APRD00492
CAS Registry Number 84057-95-4
KEGG Compound ID C07532
PubChem ID SID:213495
PharmGKB ID PA451271
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2229418

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