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PubMed2006

Comparison of the effects of mepivacaine and lidocaine on rat myocardium.

BACKGROUND AND OBJECTIVE: To compare the inotropic and lusitropic effect of lidocaine and mepivacaine on rat papillary muscle. METHODS: Effects of lidocaine and mepivacaine (10-8-10-3 M) were studied in rat left ventricular papillary muscles in vitro at a calcium concentration of 1 mmol, under low (isotony) and high (isometric) loads. RESULTS: Lidocaine induced a significant negative inotropic effect in isotonic and isometric conditions whereas mepivacaine did not. Mepivacaine only induced a negative inotropic effect when added as a bolus for the highest concentration and this effect was significantly more pronounced with lidocaine than with mepivacaine (active force at 10-3 M: 63 +/- 10 vs. 84 +/- 10% of baseline, P < 0.05). Increasing calcium concentration resulted in a greater positive inotropic effect in the control (199 +/- 11% of baseline) and mepivacaine groups (197 +/- 22% of baseline) when compared to the lidocaine group (163 +/- 19% of baseline, P < 0.05 vs. lidocaine and control groups), suggesting an impairment on intracellular Ca2+ handling by lidocaine. A negative lusitropic effect under low load was observed only for mepivacaine and suggested an impairment of sarcoplasmic reticulum function. Lidocaine and mepivacaine did not modify post-rest potentiation but significantly depressed the force-frequency relationship. CONCLUSIONS: The negative inotropic and lusitropic effects induced by lidocaine were more important than that of mepivacaine and may involve an impairment of intracellular Ca2+ handling.

Anesthetics, Local↗
PubMed1999

Pulmonary function changes after interscalene brachial plexus anesthesia with 0.5% and 0.75% ropivacaine: a double-blinded comparison with 2% mepivacaine.

UNLABELLED: The purpose of this investigation was to compare, in a prospective, double-blinded fashion, 0.5% and 0.75% ropivacaine with 2% mepivacaine to determine their effects on respiratory function during interscalene brachial plexus (IBP) anesthesia. With ethical committee approval and written, informed consent, 30 healthy patients presenting for elective shoulder capsuloplastic or acromioplastic procedures were randomized to receive IBP anesthesia by 20 mL of either 0.5% ropivacaine (n = 10), 0.75% ropivacaine (n = 10), or 2% mepivacaine (n = 10). Block onset time, pulmonary function variables, ipsilateral hemidiaphragmatic motion (ultrasonographic evaluation), and first requirement of postoperative analgesic were evaluated. Surgical anesthesia (loss of pinprick sensation from C4 to C7 and motor block of the shoulder joint) was achieved later with 0.5% ropivacaine than with either 0.75% ropivacaine or 2% mepivacaine (P < 0.05), whereas the first pain medication was requested later with both ropivacaine concentrations than with mepivacaine (P < 0.0005). No differences in quality of the block or patient acceptance were observed in the three groups. All 30 patients had ipsilateral hemidiaphragmatic paresis and large mean decreases in forced vital capacity (ropivacaine 0.5%: 40% +/- 17%, ropivacaine 0.75%: 41% +/- 22%, mepivacaine 2%: 39% +/- 21%) and forced expiratory volume at 1 s (ropivacaine 0.5%: 30% +/- 19%, ropivacaine 0.75%: 38% +/- 26%, mepivacaine 2%: 40% +/- 10%). We conclude that, when performing IBP anesthesia, 0.5% ropivacaine does not decrease the incidence of ipsilateral paresis of the hemidiaphragm compared with 0.75% ropivacaine and 2% mepivacaine. IMPLICATIONS: During the first 30 min after placing interscalene brachial plexus anesthesia, 0.5% ropivacaine does not provide clinically relevant advantages in terms of pulmonary function changes compared with either 0.75% ropivacaine or 2% mepivacaine. However, 0.75% ropivacaine allows a short onset, similar to that of mepivacaine, with long postoperative analgesia.

Adult↗
PubMed2003

Serum mepivacaine concentrations after intraoral injection in young children.

The authors measured plasma concentrations of mepivacaine in 36 children from the ages of 2 to 5 years who received dental care under light general anesthesia. The subjects were randomly assigned to receive either 2 percent mepivacaine hydrochloride with 1:20,000 levonordefrin or 3 percent mepivacaine hydrochloride without vasoconstrictor. The volume of anesthetic injected depended on the planned procedures for each patient. Blood samples (3 mL) were drawn from an intravenous line before and 5, 10, 20, 30, 45, and 60 minutes after mepivacaine injection. The serum was collected and analyzed by gas-liquid chromatography. Mean serum concentrations, normalized to a dose of 1 mg/kg body weight, reached a peak of 0.67 +/- 0.42 microgram/mL (mean +/- SD) after 3 percent mepivacaine and 0.63 +/- 0.21 microgram/mL after 2 percent mepivacaine with levonordefrin. Levonordefrin had no significant effect on the plasma concentrations. However, because of the higher concentration of mepivacaine in the 3 percent formulation, it was potentially 1.5 times as toxic (P < 0.002) on a volume basis. Statistical analysis also suggested that the maximum recommended dose of 3 mg/lb could result in potentially toxic blood concentrations in a small percentage of pediatric patients. The authors conclude that 3 percent mepivacaine should not be used when relatively large volumes of local anesthetic must be administered to small children and recommend that the maximum dose of mepivacaine not exceed 5 mg/kg.

Analysis of Variance↗
PubMed1996

Local distribution of mepivacaine after distal interphalangeal joint injection in horses.

OBJECTIVE: To evaluate the distribution of mepivacaine hydrochloride after distal interphalangeal (DIP) joint injection in horses. DESIGN: Prospective, uncontrolled study. ANIMALS: 10 adult horses. PROCEDURE: 30 minutes before euthanasia, 8 ml of 2% mepivacaine hydrochloride was injected into the dorsal pouch of a forelimb DIP joint. Synovial tissue from the DIP joint and podotrochlear (navicular) bursa and bone tissue from the medullary cavity of the distal sesamoid (navicular) bone were taken from both forelimbs immediately after death. All synovial and bone specimens were analyzed for tissue concentration of mepivacaine by high-performance liquid chromatography. Synovial tissue and bone specimen concentrations from the injected forelimb were compared with corresponding specimens from the noninjected forelimb. All synovial tissue and bone specimen concentrations were compared with an estimated effective tissue concentration of mepivacaine (0.3 microgram/mg) for local anesthesia. RESULTS: Specimen concentrations of mepivacaine from the injected forelimb were significantly greater (P < 0.05) than those in the corresponding tissues of the contralateral noninjected forelimb. All DIP joint and navicular bursa synovial tissue specimens from the injected forelimb had greater than the estimated effective tissue concentration of mepivacaine for local anesthesia. Of the 10 navicular bone specimens from the injected forelimb, 4 were higher and 2 were within 20% of the estimated effective tissue concentration of mepivacaine for local anesthesia. CONCLUSIONS: Mepivacaine hydrochloride deposited into the DIP joint should anesthetize pain arising from navicular bursa synovia and may decrease pain arising from the medullary cavity of the navicular bone. CLINICAL RELEVANCE: DIP joint injection of mepivacaine hydrochloride is not specific for DIP joint pain.

Animals↗
PubMedDate not supplied

Addition of dexmedetomidine prolongs duration of vasodilation induced by sympathetic block with mepivacaine in dogs.

BACKGROUND AND OBJECTIVES: The aim of this study was to examine the duration of vasodilation induced by sympathetic block with the addition of dexmedetomidine to mepivacaine. METHODS: We measured right and left brachial artery blood flow (BABF) before and after stellate ganglion block used as a sympathetic block in dogs. The experimental protocol was designed as follows: (1) left stellate ganglion block using 1.0 mL 0.5% mepivacaine (n = 8), (2) left stellate ganglion block using the addition of dexmedetomidine 0.5 microg to 1.0 mL 0.5% mepivacaine (n = 8), and (3) left stellate ganglion block using the addition of dexmedetomidine 0.5 microg to 1.0 mL physiological saline solution (n = 8). RESULTS: Left stellate ganglion block with mepivacaine alone increased left BABF significantly from 5 minutes through 50 minutes after the block (baseline, 100%; peak at 10 minutes after SGB, 181 +/- 27%; P <.01). Left stellate ganglion block with the addition of dexmedetomidine to mepivacaine induced a significant increase of left BABF from 5 minutes through 90 minutes after the block (baseline, 100%; peak at 10 minutes after SGB, 174 +/- 36%; P <.01). Left and right BABF did not change significantly after stellate ganglion block with dexmedetomidine only. Right BABF decreased significantly after left stellate ganglion block with mepivacaine alone or the addition of dexmedetomidine to mepivacaine throughout the study. CONCLUSIONS: The addition of dexmedetomidine prolongs the duration of vasodilation induced by stellate ganglion block with mepivacaine used for sympathetic block in dogs.

Analgesics, Non-Narcotic↗
PubMedDate not supplied

Simultaneous determination of mepivacaine, tetracaine, and p-butylaminobenzoic acid by high-performance liquid chromatography.

INTRODUCTION: The purpose of the present study was to develop a simple method for the simultaneous determination of mepivacaine, tetracaine, and p-butylaminobenzoic acid (BABA) in human plasma using high-performance liquid chromatography (HPLC) with a multiwavelength detector. METHODS: Human blood samples containing heparin, as an anticoagulant, and physostigmine (100 microg/ml), as an anticholinesterase, or human plasma containing physostigmine were spiked with various concentrations of mepivacaine, tetracaine and, in some cases, BABA. Blood samples were centrifuged and plasma was deproteinized with trifluoroacetic acid (TFA; 7%). After centrifugation, the pH was adjusted to 4.5 and an aliquot of 20, 50 or 100 microl was injected into the HPLC apparatus. The detection was done simultaneously at wavelengths of 214 and 300 nm. Analytical chromatography was done on a Waters microBondapak C(18) reverse-phase column (3.9 x 300 mm; particle size 10 microm) with a 30-min increasing linear gradient of 20-40% acetonitrile+0.05% TFA in H(2)O+0.05% TFA at a flow rate of 1 ml/min. The Waters HPLC system included two pumps, an automatic injector, a column oven, and a M490 multiwavelength detector. Quantification was done using integration of peak areas with peaks of authentic mepivacaine, tetracaine, and BABA standards. RESULTS: Calibration curves for standards of mepivacaine, tetracaine, and BABA were linear in the concentration ranges from 0.1 to 100 microg/ml, and the correlation coefficients exceeded.99 for all compounds. The lower limits of detection were 100 ng/ml for mepivacaine and 50 ng/ml for tetracaine and BABA. The yields for mepivacaine, tetracaine, and BABA were 91+/-2.1%, 82+/-3.3%, and 88+/-2.0% (mean+/-S.E.M., n=6), respectively. Degradation of tetracaine by human plasma at 37 degrees C was inhibited by physostigmine. DISCUSSION: The method is sensitive enough to allow blood concentration determinations of mepivacaine and tetracaine or its metabolite, BABA, following local anesthesia induced by these two drugs, especially when their toxic effect may be present. This method also may be useful in forensic medicine for determination of the cause of death after local anesthesia with mepivacaine and/or tetracaine.

4-Aminobenzoic Acid↗
PubMed2000

Anesthetic efficacy and heart rate effects of the intraosseous injection of 3% mepivacaine after an inferior alveolar nerve block.

OBJECTIVE: The purpose of this study was to determine the anesthetic efficacy and heart rate effects of an intraosseous injection of 3% mepivacaine after an inferior alveolar nerve block. STUDY DESIGN: Through use of a repeated-measures design, each of 48 subjects randomly received 2 combinations of injections at 2 separate appointments. The combinations were (1) an inferior alveolar nerve block (with 1.8 mL of 3% mepivacaine) + intraosseous injection with 1.8 mL of 3% mepivacaine and (2) an inferior alveolar nerve (with 1. 8 mL of 3% mepivacaine) + mock intraosseous injection. The first molar was blindly pulp tested at 2-minute cycles for 60 minutes postinjection. Anesthesia was considered successful with 2 consecutive 80 readings. Heart rate (pulse rate) was measured with a pulse oximeter. RESULTS: All subjects had lip numbness with both of the inferior alveolar nerve + intraosseous techniques. Anesthetic success for the first molar was significantly increased for 30 minutes with intraosseous injection of mepivacaine in comparison with the inferior alveolar nerve block alone (mock intraosseous injection). Subjects receiving the intraosseous injection of mepivacaine experienced minimal increases in heart rate. CONCLUSIONS: The intraosseous injection of 1.8 mL of 3% mepivacaine, when used to augment an inferior alveolar nerve block, significantly increased anesthetic success for 30 minutes in the first molar. The 3% mepivacaine had a minimal effect on heart rate and would be useful in patients with contraindications to epinephrine use.

Adult↗
PubMed1999

Anesthetic efficacy and heart rate effects of the supplemental intraosseous injection of 2% mepivacaine with 1:20,000 levonordefrin.

OBJECTIVE: The purpose of this study was to determine the anesthetic efficacy and heart rate effects of a supplemental intraosseous injection of 2% mepivacaine with 1:20,000 levonordefrin. STUDY DESIGN: Through use of a repeated-measures design, 40 subjects randomly received 3 combinations of injections at 3 separate appointments. The combinations were as follows: inferior alveolar nerve (IAN) block (with 3% mepivacaine) + intraosseous injection of 1.8 mL of 2% mepivacaine with 1:20,000 levonordefrin; IAN block + intraosseous injection of 1.8 mL of 2% lidocaine with 1:100,000 epinephrine (positive control); IAN block + mock intraosseous injection (negative control). Each first molar, second molar, and second premolar was blindly tested with a pulp tester at 2-minute cycles for 60 minutes after injection. Anesthesia was considered successful when 2 consecutive readings of 80 were obtained. Heart rate (pulse rate) was measured with a pulse oximeter. RESULTS: One hundred percent of the subjects had lip numbness with the IAN block + intraosseous mock technique and IAN block + intraosseous techniques. The anesthetic success rates for IAN block + mock intraosseous injection, IAN block + intraosseous lidocaine, and IAN block + intraosseous mepivacaine, respectively, were as follows: 80%, 100%, and 100% for the first molar; 90%, 100%, and 100% for the second molar; 77%, 97%, and 97% for the second premolar. For the first molar and second premolar, the differences were significant (P< .05) when the intraosseous mepivacaine and lidocaine techniques were compared with the IAN block + mock intraosseous injection. There were no significant differences between the intraosseous mepivacaine and lidocaine techniques. Eighty percent of the subjects had a mean increase in heart rate of 23-24 beats per minute with the intraosseous injection of the mepivacaine and lidocaine solutions; there were no significant differences between results with the 2 solutions. CONCLUSIONS: We concluded that intraosseous injection of 1.8 mL of 2% lidocaine with 1:100,000 epinephrine or 2% mepivacaine with 1:20,000 levonordefrin, used to supplement an IAN block, significantly increased anesthetic success in first molars and second premolars. The 2 solutions were equivalent with regard to intraosseous anesthetic success rate, failure rate, and heart rate increase after IAN block.

Adult↗
PubMedDate not supplied

Addition of clonidine increases duration and magnitude of vasodilative effect induced by sympathetic block with mepivacaine in dogs.

BACKGROUND AND OBJECTIVES: The aim of this study is to examine the duration and magnitude of vasodilative effect induced by sympathetic block with the addition of clonidine to mepivacaine. METHODS: We measured mean arterial pressure (MAP), heart rate (HR), and right and left brachial artery blood flow (BABF) before and after stellate ganglion block (SGB) in dogs. The experimental protocol was designed as follows: (1) left SGB using 1.0 mL 0.5% mepivacaine (n = 6) and (2) left SGB using the addition of clonidine 0.5 microg to 1.0 mL 0.5% mepivacaine (n = 6). RESULTS: MAP and HR did not change significantly throughout the study in either group. Left SGB with mepivacaine increased left BABF significantly from 10 minutes through 50 minutes after SGB (baseline, 100%; peak at 10 minutes after SGB, 176% +/- 28%; P <.01). Left SGB with the addition of clonidine to mepivacaine induced a significant increase of left BABF from 10 minutes through 70 minutes after SGB (baseline, 100%; peak at 10 minutes after SGB, 223% +/- 42%; P <.01). The values of left BABF after SGB with the addition of clonidine to mepivacaine were significantly higher than those of SGB with mepivacaine alone from 10 minutes through 80 minutes after SGB (P <.05). Right BABF decreased significantly after SGB throughout the study in both groups. CONCLUSIONS: The addition of clonidine increases both duration and magnitude of the vasodilative effect induced by sympathetic block over that caused by mepivacaine alone.

Adrenergic alpha-Agonists↗
PubMed1998

Mechanical and electrophysiological effects of mepivacaine on direct myocardial depression in vitro.

The effects of various concentrations (20, 50, and 100 mumol litre-1) of mepivacaine were studied in isolated guinea pig and rat right ventricular papillary muscles by measuring the effects on myocardial contractility and electrophysiological parameters. Mepivacaine produced dose-dependent depression of peak force during 0.5 to 3 Hz stimulation rates in guinea pig papillary muscles. Conduction block was frequently noted, especially at higher stimulation rates (2 and 3 Hz) with mepivacaine 50 and 100 mumol litre-1. In rat papillary muscle experiments, about 20% depression of peak force was shown at rested state contraction. Shortening of action potential (AP) duration (APD50: about 10%, APD90: about 10%) and rate-dependent depression of dV/dt max was observed with mepivacaine 100 mumol litre-1. In 26 mmol litre-1 K+ Tyrode's solution, mepivacaine 50 and 100 mumol litre-1 produced a dose-dependent depression of early (50 mumol litre-1: about 20%, 100 mumol litre-1: about 30%) and late (50 mumol litre-1: about 30%, 100 mumol litre-1: about 50%) force development. In slow APs, neither shortening of AP duration nor changes of dV/dt max were shown by mepivacaine 100 mumol litre-1. An approximate 30% depression of contracture induced by rapid cooling after 2 Hz stimulation rates was observed with mepivacaine 100 mumol litre-1. It may be concluded that the direct myocardial depressant effect of mepivacaine is likely to be caused by inhibition of Ca2+ release from the sarcoplasmic reticulum. The Na+ channel blocking action may contribute indirectly to the depression of contractility.

Anesthetics, Local↗
PubMed2002

Comparison of mepivacaine and lidocaine for intravenous regional anaesthesia: pharmacokinetic study and clinical correlation.

BACKGROUND: Limitations to the use of lidocaine for intravenous regional anaesthesia (IVRA) include lack of optimal intraoperative analgesia and systemic toxic reactions. This randomized double-blind study was conducted to compare intraoperative and postoperative analgesia, adverse effects, and plasma concentrations of mepivacaine or lidocaine, on release of the tourniquet in patients undergoing IVRA for distal upper limb surgery. METHODS: Forty-two adult patients were randomly allocated to receive either a 0.5% lidocaine solution 3 mg kg(-1) (n=20) or mepivacaine 5 mg kg(-1) (n=22). Plasma concentrations of both anaesthetic agents were measured at 5, 10, 20, 30, 45, and 60 min after deflation of the tourniquet by gas chromatography. RESULTS: Although plasma concentrations of mepivacaine and lidocaine were comparable 5 min after deflation, concentrations of lidocaine decreased significantly thereafter, whereas plasma concentrations of mepivacaine were similar over the 60-min study period. Supplementary analgesia during the intraoperative period was required by 45% of patients in the lidocaine group as compared with 9% in the mepivacaine group (P=0.02). No adverse effects were observed in patients given mepivacaine. In the lidocaine group, adverse effects were observed in 10% of the patients. The total ischaemia time, volume of the local anaesthetic, and duration of the surgical procedure were not significantly different between the two groups. CONCLUSIONS: Mepivacaine 5 mg kg(-1) ensured better intraoperative analgesia than lidocaine 3 mg kg(-1) when used for IVRA. Plasma concentrations of lidocaine decreased significantly between 5 and 60 min following tourniquet deflation, whereas blood concentrations of mepivacaine remained below the toxic concentration.

Adult↗
PubMed1975

Newborn blood levels of lidocaine and mepivacaine in the first postnatal day following maternal epidural anesthesia.

Distribution and elimination of lidocaine and mepivacaine were studies in 114 subjects after obstetric epidural anesthesia, Epinephrine significantly lowered the concentrations of lidocaine in the mothers' circulations by about 33 per cent, and the concentrations of mepivacaine by about 22 per cent. It also significantly altered their concentrations in the newborns' circulations at delivery and in the first 4 hours after birth. More mepivacaine than lidocaine crossed the placenta. The mepivacaine concentration in the cord blood was 36 to 47 per cent higher, and the mean fetal to maternal ratio for mepivacaine without epinephrine was 0.64, in contrast to 0.52 for the equivalent lidocaine group. Of importance was the long persistance of either drug in the newborns' circulation. Detectable levels of lidocaine and mepivacaine were present until 8 and 24 hours after birth, respectively. Pharmacokinetic models revealed that the long-term rate of disappearance of lidocaine was approximately three times as fast as that of mepivacaine. Computed half-times averaged 3 hours for lidocaine and 9 hours for mepivacaine.

Adult↗
PubMed2002

Diffusion of mepivacaine between adjacent synovial structures in the horse. Part 1: forelimb foot and carpus.

This paper tests the hypothesis that the local analgesic agent mepivacaine diffuses between adjacent equine synovial structures in the forelimb and with greater frequency than latex, gelatine dye or contrast media. We report the incidence of diffusion of mepivacaine between the distal interphalangeal joint (DIPJ) and navicular bursa (NB) of the forelimbs and between the intercarpal (IC) and radiocarpal (RC) joints of 31 fresh equine cadavers. The DIPJ of one forelimb and the NB of the contra lateral forelimb and the RC joint of one forelimb and the IC joint of the contra lateral forelimb were injected with mepivacaine. After flexion and extension of the joints, synovial fluid was obtained from the synovial structures adjacent to the injected synovial structures. The concentration of mepivacaine in these samples was determined using an enzyme linked immunosorbent assay. For samples obtained by dilution of synovial fluid, the concentration of mepivacaine was determined by comparing the concentrations of urea in the diluted synovial fluid and the concentration of serum urea. Mepivacaine diffused from the DIPJ to the NB or from the NB to the DIPJ in 25/25 (100%) limbs. Mepivacaine diffused from the IC to RC joints in 24/25 (96%) limbs and from the RC to IC joints in 21/25 (84%) limbs. It was detected at concentrations >0.3 mg/l in 9/25 (36%) of IC joints after RC joint injection and in 25/25 (100%) of the NB after DIPJ injection; at concentrations >100 mg/l in 2/25 (8%) of IC and RC joints and 12/25 (48%) of NB following DIPJ injection; and at concentrations >300 mg/l in 1/25 (4%) in the IC joints following RC joint injection and in 11/25 (44%) of DIPJ following NB injection. The results show greater diffusion of mepivacaine between adjacent synovial structures than assumed from previous anatomical, latex injection and contrast arthrographic studies. This study showed that commonly performed intrasynovial analgesic techniques in the forelimb of the horse are not as specific as previously reported.

Anesthetics, Local↗
PubMed1999

Dose response relationships for isobaric spinal mepivacaine using the combined spinal epidural technique.

UNLABELLED: Mepivacaine, a local anesthetic with similar physiochemical properties to those of lidocaine, is an adequate alternative for patients undergoing ambulatory procedures, and is associated with a lower incidence of transient neurologic symptoms (TNS) than lidocaine. We studied the dose-response characteristics of isobaric intrathecal mepivacaine using the combined spinal epidural technique for patients undergoing ambulatory arthroscopic surgery of the knee. Seventy-five patients were randomized prospectively to receive one of three doses of isobaric mepivacaine for spinal anesthesia: 30 mg (2 mL 1.5%), 45 mg (3 mL 1.5%), or 60 mg (4 mL 1.5%). An observer, blinded to the dose, recorded sensory level to pinprick and motor response until resolution of the block. In addition, the incidence of TNS was determined. An initial intrathecal dose of 30 mg of isobaric mepivacaine 1.5% produced satisfactory anesthesia in 72% of ambulatory surgical patients undergoing unilateral knee arthroscopy with a significantly shorter duration of sensory (158 +/- 32 min) and motor blockade (116 +/- 38 min) than doses of 45 and 60 mg. An intrathecal dose of 45 mg produced satisfactory anesthesia in all patients with a shorter duration of sensory (182 +/-38 min) and motor blockade (142 +/- 37 min) than 60 mg of mepivacaine 1.5% (203 +/- 36 min and 168 +/- 36 min, respectively). The incidence of TNS was 7.4% overall (1.2%-13.6% confidence intervals), less than the rates previously reported after spinal anesthesia with lidocaine in ambulatory surgical patients undergoing knee arthroscopy. We conclude that mepivacaine can be used as an adequate alternative to lidocaine for ambulatory procedures. IMPLICATIONS: This study evaluated the postoperative duration of spinal anesthesia after varying doses of isobaric mepivacaine and the incidence of transient radiating back and leg pain. We found that 45 mg of mepivacaine provided adequate anesthesia, a timely discharge, and a lower incidence of back pain than that previously reported after lidocaine spinals.

Adult↗
PubMed1996

[Combined "3-in-1"/sciatic nerve block. Block effectiveness, serum level and side effects using 700 mg mepivacaine 1% without and with adrenaline and prilocaine 1%].

UNLABELLED: A high dose of local anaesthetic is necessary for the combined "3-in-1"/sciatic nerve block. Prilocaine is recommended for its low toxicity. However, in some patients prilocaine results in pronounced methaemoglobin formation due to toludine. Little has been known hitherto about the use of high-dose mepivacaine for the combined 3-1/sciatic nerve block. This study was undertaken to compare the use of 700 mg mepivacaine 1% and of 700 mg prilocaine 1%. METHODS: The study was approved by the ethics committee of our hospital. Once their informed consent had been obtained in writing 3 x 20 patients (ASA 1-2) undergoing planned surgery on the foot or ankle joint were enrolled in the study. The patients were randomized to the following three groups on a double-blind basis: group 1,700 mg mepivacaine without epinephrine; group 2,700 mg mepivacaine with 0.2 mg epinephrine (1:350,000); group 3,700 mg prilocaine 1%. Arterial blood samples for determination of local anaesthetic serum levels were collected over a 120-min period. We determined methaemoglobin and oxygen saturation before and 120 min after the blockade and continued these measurements for 6 h in group 3. At 15-min intervals, all patients were questioned about early signs of toxicity. The perioperative monitoring including blood pressure, ECG and pulse oximetry. Data were analysed using ANOVA and Student's t-test, P < 0.05 considered statistically significant. RESULTS: The blocking efficacy did not differ among the groups (groups 1, 2, 3:90%, 95%, 90%). The maximum mepivacaine serum level in group 1 was 3.91 micrograms/ml +/- 0.95 and 2.94 micrograms/ml +/- 0.58 in group 2 (Fig. 2). Over the entire observation period the addition of epinephrine resulted in a significant reduction of the serum level (between 60.3% at t = 15 min and 19.7% at t = 120 min). In the prilocaine group the maximum serum level was 2.07 micrograms/ml +/- 0.56, significantly less than in either mepivacaine group. No patient showed signs or symptoms of local anaesthetic toxicity. In the prilocaine group there was wide variation in methaemoglobin formation among the patient, with a median of 10.1% (Fig. 3, Table 3). Three patients showed a maximum methaemoglobinemia between 16% and 17%. Five patients were still cyanotic after 6 h when they were transferred to the ward. The fractional SaO2 values amounted to 88% (median) with a minimum of 80.3%. CONCLUSION: Both mepivacaine 1% and prilocaine 1% are appropriate local anaesthetics for the combined 3-in-1/sciatic nerve block at a dose of 700 mg. There was no difference in the blocking efficacy. No patient showed clinical signs or symptoms of a local anaesthetic toxicity. Following prilocaine we are sometimes faced with high methaemoglobinemia, which may necessitate prolonged monitoring.

Adult↗
PubMed2001

High doses of mepivacaine for brachial plexus block in patients with end-stage chronic renal failure. A pilot study.

BACKGROUND AND OBJECTIVE: Patients with end-stage chronic renal failure are at risk of developing several serious postanaesthetic complications. Many anaesthesiologists perform brachial plexus anaesthesia with high doses of local anaesthetic in order to achieve an extensive blockade of the upper limb. Brachial plexus block is a suitable technique for anaesthesia for creation, repair or removal of vascular access for haemodialysis. The aim of this study was to measure mepivacaine plasma concentrations after axillary block with 650 mg plain mepivacaine in patients with end-stage chronic renal failure. METHODS: Mepivacaine plasma concentrations were assessed throughout a 150-min period, in 10 patients after axillary block with 650 mg plain mepivacaine (600 mg for axillary block and 50 mg for supplementation). RESULTS: Mepivacaine plasma concentrations expressed in microg mL(-1) as medians and their ranges were: 1.69 (1.23--7.78) at 5 min, 5.61 (4.36--8.19) at 30 min, 8.28 (3.83--11.21) at 60 min, 7.93 (5.63--11.1) at 90 min and 6.49 (5.56--8.35) at 150 min without any symptoms of toxicity. CONCLUSIONS: Brachial plexus anaesthesia with 650 mg plain mepivacaine did not result in serious systemic toxicity in these patients despite the high mepivacaine plasma concentrations found.

Aged↗
PubMed1999

Mepivacaine: its pharmacological effects and their relationship to analytical findings in the horse.

Mepivacaine is a local anaesthetic drug that is widely used in equine medicine and is classified by the Association of Racing Commissioners International (ARCI) as a Class 2 foreign substance that may cause regulators to impose significant penalties if residues are identified in post-race urine samples. Therefore, an analytical/pharmacological database was developed for this agent and its metabolites. Using an abaxial sesamoid local anaesthetic model, it was determined that the highest no-effect dose (HNED) for its local anaesthetic effect was 2 mg. Using enzyme-linked immunosorbent assay (ELISA) screening, it was determined that subcutaneous (s.c.) administration of the HNED of mepivacaine to eight horses yielded a peak urinary concentration of apparent mepivacaine of 63 ng/mL 2 h after injection. The major identified metabolite recovered from equine urine after dosing with mepivacaine is 3-hydroxymepivacaine. Therefore, 3-hydroxymepivacaine was synthesized, purified and characterized, and a quantitative mass spectrometric method was developed for this metabolite as isolated from horse urine. Following subcutaneous injection of the HNED of mepivacaine, the concentration of 3-hydroxymepivacaine recovered from horse urine reached a peak of about 64.6 ng/mL at 4 h after administration as measured by GC/MS. The concentration of mepivacaine or its metabolites after administration of a HNED dose are detectable by mass spectral techniques. Within the limits of this research, the study suggests that recovery of concentrations less than about 65 ng/mL of 3-hydroxymepivacaine from post-race urine samples may not be associated with a recent LA effect of mepivacaine.

Anesthetics, Local↗
PubMed1998

Pharmacokinetics of the enantiomers of bupivacaine and mepivacaine after epidural administration of the racemates.

UNLABELLED: We investigated the pharmacokinetics of the enantiomers of bupivacaine and mepivacaine after epidural injection of the racemate of each drug into six surgical patients. After epidural administration of either bupivacaine/HCl (115 mg) or mepivacaine/HCl (460 mg), blood samples were collected for 24 h. Unbound fractions were determined by using ultrafiltration for bupivacaine and equilibrium dialysis for mepivacaine. Concentrations in plasma, ultrafiltrate, and dialysate were determined by using stereoselective high-performance liquid chromatography. Peak plasma concentrations of R(+)-bupivacaine (389 +/- 93 ng/mL) and R(-)-mepivacaine (1350 +/- 430 ng/mL) were smaller than those of S(-)-bupivacaine (449 +/- 109 ng/mL, P < 0.0001) and S(+)-mepivacaine (1740 +/- 490 ng/mL, P < 0.002), respectively. However, the unbound peak concentrations of R(+)-bupivacaine (20 +/- 11 ng/mL) were larger than those of S(-)-bupivacaine (15 +/- 9 ng/mL, P < 0.005); unbound peak concentrations of R(-)-mepivacaine (485 +/- 158 ng/mL) and S(+)-mepivacaine (460 +/- 139 ng/mL) did not differ. These observations reflect differences in the systemic disposition (distribution and elimination) of the enantiomers, because the systemic absorption was not enantioselective with either drug. This study supports the opinion that the use of single enantiomers, rather than racemates, is preferable, particularly for bupivacaine. IMPLICATIONS: Measurements of the plasma concentrations of the enantiomers of bupivacaine and mepivacaine after epidural administration of the racemates demonstrated that the systemic disposition, but not the systemic absorption, of these drugs is enantioselective and supports the opinion that the use of single enantiomers, rather than racemates, is preferable.

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