Ropivacaine Bupivacaine

Some other anesthetics with similar structures are prilocaine, tetracaine, ropivacaine, bupivacaine, chloroprocaine, and mepivacaine ... 

Infiltration Field block Lidocaine Ropivacaine Bupivacaine Levobupivacaine... 

Anesthetic Agents Under Development. Ropivacaine (AL-381) (22, R = similar in stmcture to mepivacaine and bupivacaine, has... 

T. Arvidsson and E. Eklund, Determination of free concenti ation of ropivacaine and bupivacaine in blood plasma by ultrafilti ation and coupled-column liquid cliromatogra-phy , 7. Chromatogr. B 668 91-98 (1995). 

C)jHi)N 87-62-7) see Bupivacaine Etidocaine LicIocaine Lidoflazine Mepivacaine Pilsicainide Pyrrocaine Ropivacaine hydrochloride Tocainide Xipamide... 

Berggren S, Hoogstraate J, Fagerholm U and Lennernas H (2004) Characterization of Jejunal Absorption and Apical Efflux of Ropivacaine, Lidocaine and Bupivacaine in the Rat Using In Situ and In Vitro Absorption Models. Eur J Pharm Sci 21 pp 553-560. 

When using PFT with a neutral selector, it is quite difficult to avoid any entrance of the chiral selector into the ionization source, particularly at a high pH, where EOF is important. The use of BGE at low pH and/or coated capillary to minimize EOF is therefore mandatory. However, the coaxial sheath gas, which generally assists the ionization process, leads to an aspirating phenomenon of the chiral selector in the MS direction. Javerfalk et al. were the first to apply PFT with a neutral methyl-/i-CD for the separation of racemic bupivacaine and ropivacaine with a polyacrylamide-coated capillary and an acidic pH buffer (pH 3). Cherkaoui et al. employed another neutral CD (HP-/1-CD) with a PVA-coated capillary for the analysis of amphetamines and their derivatives. To prevent a detrimental aspiration effect, analyses were carried out without nebulization pressure. Numerous other studies presented excellent results such as the enantioselective separation of adrenoreceptor antagonist drugs using tandem mass spectrometry (MS/MS) the separation of clenbuterol enantiomers after solid-phase extraction (SPE) of plasma samples or the use of CD dual system for the simultaneous chiral determination of amphetamine, methamphetamine, dimethamphetamine, and p-hydroxymethamphetamine in urine. 

The local anesthetics can be broadly categorized on the basis of the chemical nature of the linkage contained within the intermediate alkyl chain group. The amide local anesthetics include lidocaine (7.5), mepivacaine (7.6), bupivacaine (7.7), etidocaine (7.8), prilocaine (7.9), and ropivacaine (7.10) the ester local anesthetics include cocaine (7.11), procaine (7.12), benzocaine (7.13), and tetracaine (7.14). Since the pharmacodynamic interaction of both amide and ester local anesthetics with the same Na" channel receptor is essentially idenhcal, the amide and ester functional groups are bioisosterically equivalent. However, amide and ester local anesthetics are not equal from a pharmacokinetic perspective. Since ester links are more susceptible to hydrolysis than amide links. 

Amide linked local anaesthetics e.g. lidocaine, bupivacaine, dibucaine, prilocaine, ropivacaine. 

A further property which is of central importance in diffusion is the tissue-binding capacity (or affinity) of a drug. Drugs that are highly lipid-soluble and protein-bound, such as bupivacaine and ropivacaine, are extensively bound to tissue. This limits the rate at which they are transferred from their intracellular sites of action to the vascular compartment. When tissue affinity is great the local anaesthetic effect is prolonged. 

Lidocaine (lignocaine) Prilocaine Bupivacaine Levobupivacaine Ropivacaine... 

Of all the local anaesthetics available, levobupivacaine and ropivacaine have the most favourable pharmacological characteristics for use in obstetrics. They have the lowest potential for cardiotoxicity and, unlike lidocaine and prilocaine, there is little risk of cumulation when they are administered by epidural infusion at effective doses. Elimination of all amides is prolonged in the neonate, exceeding 20 h in the case of bupivacaine. 

When used for spinal anaesthesia, 0.75% ropivacaine produces less intense sensory and motor block than 0.5% bupivacaine. It is suitable for regional, spinal and epidural block but not for regional intravenous anaesthesia. The addition of adrenaline (epinephrine) does not prolong the duration of anaesthesia in brachial plexus or epidural block. Ropivacaine is indistinguishable from bupivacaine when used in obstetric anaesthesia. Its direct myocardial toxicity is somewhat less than that of bupivacaine. 

Local anesthetics have weak direct neuromuscular blocking effects that are of little clinical importance. However, their effects on cardiac cell membranes are of major clinical significance, and some local anesthetics are widely used as antiarrhythmic agents (eg, lidocaine) (see Chapter 14) at concentrations lower than those required to produce nerve block. Others of the same amide class (eg, bupivacaine, ropivacaine) can cause lethal arrhythmias if high plasma concentrations are inadvertently achieved. 

The choice of local anesthetic for infiltration, peripheral nerve blocks, and central neuraxis (spinal/epidural) blockade is usually based on the duration of action required. Procaine and chloroprocaine are short-acting lidocaine, mepivacaine, and prilocaine have an intermediate duration of action and tetracaine, bupivacaine, levobupivacaine, and ropivacaine are long-... 

The cardiovascular effects of local anesthetics result in part from direct effects of these drugs on the cardiac and smooth muscle membranes and from indirect effects on the autonomic nervous system. As described in Chapter 14, local anesthetics block cardiac sodium channels and thus depress abnormal cardiac pacemaker activity, excitability, and conduction. At extremely high concentrations, local anesthetics can also block calcium channels. With the notable exception of cocaine, local anesthetics also depress myocardial contractility and produce direct arteriolar dilation, leading to systemic hypotension. Cardiovascular collapse is rare, but has been reported after large doses of bupivacaine and ropivacaine have been inadvertently administered into the intravascular space. 

It has been suggested that bupivacaine may be more cardiotoxic than other long-acting local anesthetics (eg, ropivacaine). This reflects the fact that bupivacaine-induced blockade of sodium channels is potentiated by the long action potential duration of cardiac cells compared with nerve fibers. The most common electrocardiographic finding in patients with bupivacaine intoxication is a slow idioventricular rhythm with broad QRS complexes and eventually electromechanical dissociation. 

Resuscitation from bupivacaine cardiovascular toxicity is extremely difficult even for experienced clinicians. Recent studies suggest that propofol can be useful in resuscitating patients acutely exposed to toxic levels of bupivacaine. The (S)-isomer, levobupivacaine, appears to have a lower propensity for cardiovascular toxicity than the racemic mixture or the (7 >isomer and has been approved for clinical use. The clinical effects of ropivacaine are similar to those of bupivacaine, but ropivacaine is allegedly associated with a lower potential for cardiovascular toxicity. Ropivacaine is available only as the ( SJ-stereoisomer, which has inherently less affinity for the cardiac sodium channel. However, both cardiac toxicity and CNS toxicity have been reported when large doses of ropivacaine were used for peripheral nerve blocks. 

Prilocaine, ropivacaine, mepivacaine, levobupivacaine Like bupivacaine ... 

Kanai Y, Katsuki H, Takasaki M Comparisons of the anesthetic potency and intracellular concentrations of S(-) and / (+) bupivacaine and ropivacaine in crayfish giant axon in vitro. Anesth Analg 2000 90 415. [PMID 10648331]... 

In addition to levobupivacaine, ropivacaine is a new long-lasting amide-type LA that has been produced in order to address the enantioselectivity of the cardiotoxicity of bupivacaine. Ropivacaine, which is an (S)-enantiomer containing an n-propyl instead of the butyl moiety of bupivacaine, was launched in 2000. Clinical data indicate a late onset and long duration of action and the anesthetic potency of ropivacaine is comparable to that of bupivacaine (for review see McClellan and Faulds, 2000 Whiteside and Wildsmith, 2001). In animal models, the... 

Fig. 13 Chromatograms of the online extraction of a human plasma sample spiked with bupivacaine and ropivacaine at 75 pmol 1. 1 and ethycaine at 40 pmol L on the MIP and the reference polymer REF, both prepared using toluene as the porogen [52]...

Cobb Z, Sellergren B, Andersson LI (2007) Water-compatible molecularly imprinted polymers for efficient direct injection on-line solid-phase extraction of ropivacaine and bupivacaine from human plasma. Analyst 132(12) 1262—1271... 

Borgeat A, Ekatodramis G, Blumenthal S. Interscalene brachial plexus anesthesia with ropivacaine 5 mg/mL and bupivacaine 5 mg/mL effects on electrocardiogram. Reg Anesth Pain Med. 2004 29 557-563. 

Liisanantti O, Luukkonen J, Rosenberg PH. High-dose bupivacaine, levobupivacaine and ropivacaine in axillary brachial plexus block. Acta Anaesthesiol Scand. 2004 48 601-606. 

Zink W, Seif C, BohlJR, et al. The acute myotoxic effects of bupivacaine and ropivacaine after continuous peripheral nerve blockades. Anesth Analg. 2003 97 1173-1179. 

PCRA is typically accomplished by inserting a small catheter into the affected site, and then attaching the catheter to some type of pump that enables the patient to self-administer small amounts of medication as needed. For example, a PCA system has been used to deliver local anesthetics such as bupivacaine and ropivacaine into the subacromial space following acromial decompression surgery.3,27 Likewise, PCRA can be used to deliver a local anesthetic to the area around a peripheral nerve (sciatic, popliteal, and so forth), and... 

Evron S, Glezerman M, Sadan O, et al. Patient-controlled epidural analgesia for labor pain effect on labor, delivery and neonatal outcome of 0.125% bupivacaine vs 0.2% ropivacaine. IntJ Obstet Anesth. 2004 13 5-10. 

Gogarten W, Van de Velde M, Soetens E, et al. A multicentre trial comparing different concentrations of ropivacaine plus sufentanil with bupivacaine plus sufentanil for patient-controlled epidural analgesia in labour. Eur J Anaesthesiol. 2004 21 38M5. 

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