Mepivacaine Bupivacaine

Drugs such as lidocaine, mepivacaine, bupivacaine, ethidocaine, and procaine are primarily used for this purpose. 

Epidural anesthesia This term is understood to be an introduction of local anesthetic into the spinal cord membrane of the intervertebral space. It is used during obstetrical and gynecological interventions that do not require a fast development of anesthesia. Drugs such as lidocaine, mepivacaine, bupivacaine, ethidocaine, and chloroprocaine are used for this purpose. 

Amide linkage (amides of benzoic acid) Lidocaine Mepivacaine Bupivacaine Etidocaine... 

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

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

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

Local Anesthetics. Local anesthetics used in anesthesiology are currently amide derivatives (lidocaine, mepivacaine, prilocaine, bupivacaine, levobupivacaine. 

Spinal anesthesia Spinal anesthesia is the introduction of local anesthetics directly into the spinal fluid, which causes a sympathetic blockage, or loss of feeling as well as muscle relaxation resulting from the interaction of anesthetic with every spinal nerve tract. This method is used during major surgical interventions. As a rule, lidocaine, mepivacaine, and bupivacaine are used for this purpose. 

Amide-type agents include articaine, lidocaine, bupivacaine, prilocaine, mepivacain and ropiva-caine. These are metabolized in the liver by microsomal enzymes with amidase activity. The amide group is preferred for parenteral and local use. If by accident rapidly administered intravascularly these agents, especially bupivacaine but also lidocaine, can produce serious and potentially lethal adverse effects including convulsions and cardiac arrest. They can more easily accumulate after multiple administrations. Intravenous lidocaine is sometimes used for regional anesthesia, for infiltration procedures, for the induction of nerve blockade and for epidural anesthesia. However, it is also used as an antiarrhythmic. Bupivacaine is a long-acting local anesthetic used for peripheral nerve blocks and epidural anesthesia. 

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. 

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-... 

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

The action of several anesthetics has also been associated with a modulation of K+ channels. In addition to blocking Na+ currents in spinal neurones of the superficial dorsal horn the local anesthetics bupivacaine, lidocaine and mepivacaine reduce transient, A-type K+ currents in these cells whereas delayed rectifier K+ currents proved to be resistant (Olschewski et al., 1998). Since the A-type K+ current determines the frequency pattern of repetitively firing neurones (Hille, 2001) their suppression in dorsal... 

MIPs used as chiral stationary phases in o-CEC, p-CEC as well as in rod-CEC have shown high selectivity but relatively low efficiency. Most of the reported enantiomer separations on these phases were performed without pressurization of the flow system. Only Schweitz et al. described on the enantiomer separation of propranolol and metoprolol (print molecule R-propranolol or S-metoprolol) [57] and ropivacaine, mepivacaine and bupivacaine (print molecule S-ropivacaine) [58] by... 

Luduena FP, Hoppe JO (1952) Local anaesthetic activity, toxicity and irritancy of 2-alkoxy analogs of procaine and tetracaine. J Pharm Exp Ther 104 40-53 Luduena FP, Hoppe JO, Coulston F, Drobeck HP (1960) The pharmacology and toxicology of mepivacaine, a new local anesthetic. Toxicol Appl Pharmacol 2 295-315 Luduena FP, Bogado EF, Tullar BF (1972) Optical isomers of mepivacaine and bupivacaine. Arch Int Pharmacodyn 200 359-369... 

The tests allow judgement of the propensity of local anesthetics to induce symptoms of hepatic porphyria. The local anesthetics lidocaine, bupivacaine, etido-caine, mepivacaine, prilocaine and pyrocaine belong to this group, but procaine, butacaine, oxybuprocaine, proxymethacaine and tetracaine had no (or very slight) porphyrinogenic effect. 

A healthy 17-year-old man received an interscalene brachial plexus block using mepivacaine 600 mg and bupivacaine 150 mg. He became disorientated and showed signs of local anesthetic toxicity, for which he was given midazolam 5 mg. Flumazenil 0.5 mg was given 23 minutes after the end of the procedure, causing opisthotonos. 

A 59-year-old woman, grade ASA I, had psychiatric effects associated with local anesthetic toxicity after receiving bupivacaine 50 mg and mepivacaine 75 mg for an axillary plexus block. She complained of dizziness and a near death experience (464). 

Bupivacaine displaces mepivacaine from protein binding sites on alphai acid glycoprotein in vitro (29). 

Hartrick CT, Dirkes WE, Coyle DE, Raj PP, Denson DD. Influence of bupivacaine on mepivacaine protein binding. Clin Pharmacol Ther 1984 36(4) 546-50. 

---