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At least 19 recordsLinked to original sources
PubMed1977

Clinical effects of carticaine, a new local anesthetic. A survey and a double-blind investigation comparing carticaine with lidocaine in epidural analgesia.

Carticaine, a new local anesthetic of the amide type, differs from those previously known in that it contains a thiophene ring. The physico-chemical properties of the compound, its pharmacology and its toxicology are reviewed from the litererture. A controlled, double-blind investigation in which carticaine was compared with lidocaine for the purpose of throwing light on the effect of the new local anesthetic in epidural analgesia is presented. Carticaine and lidocaine 2% with adrenaline 1:200 000 were used in the investigation. It was not possible to show any stastically significant difference as regards latency, spread, duration, or motor blockade obtained with the two substances. Marked differences in the type of side effects or their frequency were not noted. From this investigation and a scrutiny of the published clinical studies on the effect of carticaine, it is concluded that its clinical properties are comparable to those of lidocaine.

Aged↗
PubMed2000

Effect of carticaine on the sarcoplasmic reticulum Ca2+-dependent adenosine triphosphatase.

The sarcoplasmic reticulum Ca2+-ATPase (calcium-dependent adenosine triphosphatase) transports Ca2+ from the myoplasm to the reticulum lumen at the expense of free energy from ATP hydrolysis. Carticaine is a local anesthetic of frequent use in dentistry which is now entering other clinical fields. We studied the action of carticaine on the sarcoplasmic reticulum (SR) skeletal muscle Ca2+-ATPase. SR vesicles from rabbit fast skeletal muscle were used. Carticaine inhibits the enzymatic activity. The inhibition of the enzymatic activity depends on pH, [Ca2+] and the presence of calcimycin. Half-maximal carticaine concentration that inhibits the ATPase activity tends to a maximal value upon increasing [Ca2+]. Carticaine concentrations required to inhibit the enzymatic activity at myoplasmic calcium concentration are lower than usual clinical doses: Ki=6.0+/-1.4 mM carticaine (n=5) for 0.1 microM [Ca2+]. ATP-dependent calcium uptake is also inhibited by the local anesthetic: Ki=30.5+/-3.4 mM (n=4). Besides, carticaine inhibits the phosphorylation of the enzyme by inorganic phosphate (Pi): Ki=20.0+/-3.4 (n=5) - 33.2+/-4.6 (n=4) mM, for [Pi] 1-4 mM. Carticaine increases the membrane permeability to Ca2+. Ca2+ efflux from preloaded vesicles is prevented by Ca2+ and Mg2+. Our results suggest that the diffusion of the local anesthetic into muscle fibers might trigger undesired effects such as sustained contraction of the masticatory muscles.

Anesthetics, Local↗
PubMed2005

Effect of carticaine on the sarcoplasmic reticulum Ca2+-adenosine triphosphatase. II. Cations dependence.

Ca2+-ATPase is a major intrinsic protein in the sarcoplasmic reticulum (SR) from skeletal muscles. It actively transports Ca2+ from the cytoplasm to the SR lumen, reducing cytoplasmic [Ca2+] to promote muscle relaxation. Carticaine is a local anesthetic widely used in operative dentistry. We previously showed that carticaine inhibits SR Ca2+-ATPase activity and the coupled Ca(2+) uptake by isolated SR vesicles, and increases the rate of Ca2+ efflux from preloaded vesicles. We also found that these effects were antagonized by divalent cations, and concluded that they were mainly due to the direct interaction of carticaine with the Ca2+-ATPase protein. Here we present additional results on the modulation of the above effects of carticaine by Ca2+ and Mg2+. The activating effect of Ca2+ on the ATPase activity is competitively inhibited by carticaine, indicating a decreased Ca2+ binding to the high affinity Ca2+ transport sites. The activating effect of Mg2+ on the phosphorylation of Ca2+-ATPase by orthophosphate is also inhibited by carticaine. The anesthetic does not affect the reaction mechanism of the cations acting as cofactors of ATP in the catalytic site. On the basis of the present and our previous results, we propose a model that describes the effect of carticaine on the Ca2+-ATPase cycle.

Anesthetics, Local↗
PubMed2002

Carticaine versus lidocaine for peribulbar anesthesia in cataract surgery.

PURPOSE: To compare carticaine 4% and lidocaine 2% for peribulbar anesthesia in cataract surgery. SETTING: Ain Shams and Cairo University Hospitals, Cairo, Egypt. METHODS: This prospective double-blind randomized study comprised 200 cataract patients assigned to 1 of 2 groups of 100 each based on type of anesthesia: carticaine 4% or lidocaine 2%. The efficacy, safety, and duration of the motor and the analgesic block produced by carticaine 4% adrenaline hyaluronidase mixture and lidocaine 2% adrenaline hyaluronidase mixture used as peribulbar anesthesia were compared. The mean time for satisfactory block, need for supplementary injections, incidence of intraoperative and postoperative pain, and postoperative complications were evaluated. The data were analyzed using the Student t test and Mann-Whitney U test for intergroup differences. The chi-square or Fisher exact test was used to assess eye movement scores, the need for supplementary injections, the onset of postoperative pain, and the incidence of postoperative complications. RESULTS: The mean time for satisfactory anesthesia was 7.5 minutes +/- 1.68 (SD) for lidocaine 2% and 2.5 +/- 1.53 minutes for carticaine 4% (P <.001). The need for supplementary injections was 28% in the lidocaine group and 4% in the carticaine group (P <.001). The mean onset of postoperative pain was 2.00 +/- 0.86 hours in the lidocaine group and 5.52 +/- 1.80 hours in the carticaine group (P <.05). There were no cases of postoperative neurotoxicity or extraocular muscle dysfunction in either group. CONCLUSIONS: Carticaine 4% adrenaline hyaluronidase mixture was an effective and safe agent for peribulbar anesthesia. It was more efficient than lidocaine 2% adrenaline hyaluronidase mixture in the onset and quality of anesthesia as well as postoperative analgesia.

Anesthesia, Local↗
PubMed1986

[Epidural anesthesia with carticaine in cesarean section. A comparison with bupivacaine].

The feasibility of 1.5% carticaine, an amide-type local anaesthetic agent, for epidural anaesthesia for Caesarean section was studied in 15 parturients. As a control, epidural anaesthesia in 15 parturients was done with 0.5% bupivacaine. The quality of anaesthesia before delivery was good in both groups. One additional dose of carticaine had to be given after delivery in order for the anaesthesia to last until the end of the operation. Apgar-scores, maternal and fetal pH and blood-gas values were similar in both groups. Maternal arterial serum concentration of bupivacaine at the time of delivery was 1.25 microgram/ml, while that of carticaine was only 0.48 microgram/ml. The lower serum concentration of carticaine is due to its rapid metabolization. The ratio of the unmetabolized drug to that of the metabolite found in maternal serum at the time of delivery was 0.75. Umbilical venous-maternal arterial serum concentration ratio in bupivacaine patients was 0.28 and in carticaine patients 0.32. The results suggest that carticaine is a feasible drug for Caesarean section.

Adult↗
PubMed1980

Carticaine: action of the local anesthetic on myelinated nerve fibres.

Unlike other clinically used local anesthetics, carticaine contains a thiophene ring. Current voltage relations of peak sodium current INa and steady state potassium current IK were measured in voltage clamp experiments on the node of Ranvier of Rana esculenta. The dependence of the maximum sodium conductance on external concnetration of carticaine is described by an apparent dissociation constant KNa = 0.065 mM at pH = 7.3. An apparent dissociation constant KK = 0.147 mM at pH = 7.3 was calculated on the basis of the action of carticaine on the maximum potassium conductance. Similar to other amine local anesthetics, carticaine blocks sodium channels at a lower concentration than potassium channels, but lower concentrations of the thiophene derivative than of the benzene derivatives are needed to block the ionic channels. The partition coefficients in-octanol/Soerensen buffer at pH = 7.35 follow the sequence lidocaine (46) more than carticaine (17) more than procaine (2). Therefore, the action of these local anesthetics on sodium channels and potassium channels seems not to follow mere lipid solubility properties of the neutral drug. Increasing the pH from 6.3 to 8.3 favoured the neutral drug form and enhanced the block of both ionic channels but the relative reduction of the ionic currents was larger for potassium currents.

Animals↗
PubMed1980

[Carticaine and mepivacaine. a double blindstudy on longterm and diffusion action during blockade of the brachial plexus (author's transl)].

In a double blind study, using supraclavicular plexus blockade as a model, the latency and diffusion of carticaine in comparison with mepivacain was investigated. Up to 16 min after first eliciting paraesthesiae and injection somewhat more plexus blocks were complete with carticain than with mepivacaine. This difference was statistically valid only for motor block and not for sensory block. However, the relative proportion of complete motor and sensory block increased with mepivacain after 16 min and surpassed the results for carticaine. This difference is statistically significant for sensory block and for sensory and motor block combined. It is also valid for the results up to 30 min. The failure rate was significantly higher for carticaine than for mepivacaine. From these results the course and the failures are attributed to a poorer diffusion of carticaine.

Adolescent↗
PubMed1978

A comparative study of carticaine and prilocaine in epidural anaesthesia.

Carticaine and prilocaine (without adrenaline) in epidural anaesthesia were compared in a double blind study. Carticaine and prilocaine were used in 2 % concentration without adrenaline. The latency time was not significantly different, but carticaine was a shorter acting local anaesthetic. The motor block in both series was similar. Carticaine is a good and reliable analgesic in short operations but in operations longer than one and a half hours catheter technique, adrenaline addition or local anaesthetics of longer duration ought to be used.

Aged↗
PubMed1978

[Methaemoglobin-behaviour due to carticaine (= Ultracain) (author's transl)].

The influence of carticaine on the formation of methaemoglobin was investigated in 22 patients undergoind spinal (n = 10) or epidural (n = 12) anaesthesia. Carticaine in a dose of 1,35 mg/kg, as used for spinal anaesthesia, did not influence the concentration of methaemoglobin. Carticaine in a dose of 5 mg/kg however, as used for epidural anaesthesia, increased the formation of methaemoglobin slightly at 30 min after injection. This increase is of little clinical importance since the upper limits of the normal range were not reached.

Adolescent↗
PubMed1978

[Comparative studies of the local anaesthetic action of carticaine 1% and mepivacaine 1% (author's transl)].

The actions of carticaine 1% and mepivacaine 1% in peripheral nerve block were investigated in double-blind study. Bilateral ulnar nerve blocks were performed in 14 healthy subjects (age range 20-30 years), and latency, duration, and intensity of anaesthesia were quantitatively determined. There were no differences in latency of nerve block, but a significant difference in the duration of effect: Mepivacaine acted for nearly twice as long as Carticaine. In addition, several incomplete blocks were noted with Carticaine. On the basis of these results mepivacaine is preferred in peripheral nerve block because of its longer and more reliable action.

Adult↗
PubMed1978

A comparison of carticaine and lidocaine in spinal anaesthesia.

The effects of Lidocaine and the new local anaesthetic carticaine in spinal anaesthesia were compared in a double blind study in 120 elderly male patients scheduled for small urological procedures. The variables investigated were: analgesia examined by pin prick method, loss of tactile sensation, motor block, and skin temperature on the big toe. Both local anaesthetics seem to act similarly, but the loss of tactile sensation and motor block began somewhat earlier with carticaine. The differences have hardly any clinical significance. The incidence of hypotension and postanaesthetic headache was similar in each group.

Aged↗
PubMed1986

[Comparative evaluation of carticaine and bupivacaine in epidural anesthesia in cesarean section].

Lumbar epidural anaesthesia with Carticain (Ultracain) has been applied in 25 Caesarean Sections. The resulting data (waiting period, effective length and quality of the analgesia, blood pressure drop, postoperative phase, newborn state, side effects) have been compared with those of Bupivacain (Marcain) used for the same purpose. Carticain is fitted for purposes of obstetrical anaesthesia, even more than Bupivacain, owing to its slighter blood-pressure diminishing effect, and shorter waiting period.

Adult↗
PubMed1977

Clinical assessment of a new local anesthetic agent-carticaine.

The combination of 4 per cent carticaine 5 mug per milliliter with epinephrine is an effective agent acting in the standard lidocaine-epinephrine-mepivacaine-epinephrine range. Like lidocaine, it is of no clinical value without the addition of epinephrine and its vasodilator properties are greater than those of mepivacaine or prilocaine. Its onset time is reasonably rapid, its duration and extent are satisfactory for clinical purposes, and no toxic reactions were noted in the 100 injections given. However, its predictability for +4 anesthesia is poor, and there is wide variation in the onset time. Finally, the success rate compared with that for lidocaine, mepivacaine, or prilocaine for the same dosage and areas, with the use of the same criteria, is not good enough in my opinion to qualify carticaine as a general-purpose anesthetic on a par with standard lidocaine.

Adolescent↗
PubMed1976

[Comparative tests of tetracian and of the new local anesthetic carticain in spinal anesthesiasa double placebo study].

Onset of effect, degree of effect and duration of effect of Tetracain (Pantocain) and Carticain (Ultracain) in hyperbaric solutions were compared on 60 subjects with spinal anesthesias. In the double-blind trial with individual randomization, no difference was found regarding the onset of action (latency period), the intensity of analgesia and the extent of the muscle blocking. With 151 +/- 48.9 min., the duration of analgesia with Carticain was distinctly and significantly shorter than in the case of Tetracain with 278 +/- 108.9 min., but thoroughly sufficient for the nature and duration of the surgical operations on pour patients, even in the postoperative phase.

Adolescent↗
PubMed1977

[Placental transfer of carticaine (Ultracain) a new local anesthetic agent (author's transl)].

Serum levels of carticaine were measured in 9 parturient women after peridural anesthesia as well as in the newborns. The neonatal serum level of carticaine amounted to 32 +/- 7% of the maternal (ratio = 0,32). This proportion is compared to those given in the literature for the local anesthetics Lidocaine (0,52-0,58), Mepivacaine (0,64) and Bupivacaine (0,23-0,26).

Adolescent↗
PubMed1980

Effects of diclofenac-sodium and salicylate, carticaine, lidocaine and procaine in the cadmium- and heat-induced hemolysis.

In the present study we examined the utility, sensitivity and specificity of the cadmium- and heat-induced hemolysis, investigating the effects of diclofenac, salicylate and lidocaine, carticaine and procaine on the rabbit erythrocyte membrane. In the cadmium-induced hemolysis, which has not been reported, as far as we know, as a test model for local anesthetics, the studied local anesthetics have, to a large extent, protective effects on the erythrocyte membranes, probably based on an osmotic action at drug concentrations of 10(-4) to 10(-2) M. On the other hand, these local anesthetics amplify the heat-induced hemolysis to a variable extent. The studied antirheumatic drugs showed in the cadmium-induced hemolysis that they cannot have the same binding sites as the local anesthetics investigated. In the cadmium-induced hemolysis, the reaction products of the antirheumatic drugs with the membrane protein presumably cannot cause an increase in surface area/volume ratio of the erythrocytes, which is generally regarded as a cause for stabilization. This interpretation could be an explanation for the increase of the cadmium-induced hemolysis by the antirheumatic drugs studied. On the other hand, the antirheumatic drugs inhibited to a variable extent the heat-induced hemolysis.

Anesthetics, Local↗
PubMed1981

[Met-Hb formation and local anesthesia using bupivacaine, carticaine and etidocaine (author's transl)].

Hemoglobin-(= Met-Hb)formation by local anaesthesia and local anaesthetics is still a point for discussion. Until now met-hb-aemia only was proven to develop under local anaesthetics with relationship to aniline (Benzocaine, Citanest). Since aniline does not possess any oxidative properties, met-hb-formation only can occur after metabolism (phenylhydroxylamine or para-aminophenol), first of all amino- and nitro-groups [6, 14] will be made responsible for oxidation. Because of the fact that neither the relationship to aniline nor the benzol-structure is the pre-supposition for met-hb-formation, possibly other substances with amino- or nitro-groups may induce it. In consequence of incidental cyanosis under intra and extradural analgesia we studied the met-hb-behaviour after the use of different local anaesthetics. The aniline-related bupivacaine and etidocaine were opposed to the thiophene-related carticaine. In this examination we found neither an elevation of hemoglobin by the aniline-related nor by the thiophene-related substances.

Anesthesia, Local↗
PubMed1978

[Outpatient termination of pregnancy in the first trimester during paracervical blockade with Carticain (author's transl)].

Sparing termination of pregnancy with a low incidence of complications, using the drainage method in local anaesthesia, can be effected on an outpatient basis. Carticain, which is a rapidacting anaesthetic with good analgesic effect, enables practically painless dilatation of the cervical channel with subsequent evacuation, when combined with good psychological guidance of the patient. When questioned postoperatively, practically all patients were in favor of local anaesthesia. Another positive aspect, in their opinion, was the fact that they could be discharged after brief hospitalization. Furthermore, treatment on an outpatient basis is cost-saving.

Abortion, Legal↗