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PubMed2003

Procaine and mepivacaine have less toxicity in vitro than other clinically used local anesthetics.

UNLABELLED: The neurotoxicity of local anesthetics can be demonstrated in vitro by the collapse of growth cones and neurites in cultured neurons. We compared the neurotoxicity of procaine, mepivacaine, ropivacaine, bupivacaine, lidocaine, tetracaine, and dibucaine by using cultured neurons from the freshwater snail Lymnaea stagnalis. A solution of local anesthetics was added to the culture dish to make final concentrations ranging from 1 x 10(-6) to 2 x 10(-2) M. Morphological changes in the growth cones and neurites were observed and graded 1 (moderate) or 2 (severe). The median concentrations yielding a score of 1 were 5 x 10(-4) M for procaine, 5 x 10(-4) M for mepivacaine, 2 x 10(-4) M for ropivacaine, 2 x 10(-4) M for bupivacaine, 1 x 10(-4) M for lidocaine, 5 x 10(-5) M for tetracaine, and 2 x 10(-5) M for dibucaine. Statistically significant differences (P < 0.05) were observed between mepivacaine and ropivacaine, bupivacaine and lidocaine, lidocaine and tetracaine, and tetracaine and dibucaine. The order of neurotoxicity was procaine = mepivacaine < ropivacaine = bupivacaine < lidocaine < tetracaine < dibucaine. Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, has the least-adverse effects on cone growth among clinically used local anesthetics. IMPLICATIONS: Systematic comparison was assessed morphologically in growth cones and neurites exposed to seven local anesthetics. The order of neurotoxicity was procaine = mepivacaine < ropivacaine = bupivacaine < lidocaine < tetracaine < dibucaine. Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, is the safest among clinically used local anesthetics.

Anesthetics, Local↗
PubMed1989

Some correlations between procaine-induced convulsions and monoamines in the spinal cord of rats.

The relationships between the convulsions induced by the local anesthetic procaine and monoamines in the spinal cord were investigated in rats. The levels of dopamine (DA) and serotonin (5-HT) in the spinal cord were time-dependently increased after procaine (170 mg/kg, i.p.), which induced clonic convulsions, but the level of norepinephrine (NE) was unchanged. The rats that died during convulsions had a marked increase in DA. Phenobarbital (25 mg/kg, s.c.) produced both depletion of DA and elevation of 5-HT in the spinal cord and completely protected rats against convulsions. A 5-HT precursor, 5-hydroxytryptophan (5-HTP; 20-80 mg/kg, i.p.), suppressed the convulsions in a dose-dependent manner as shown by a decrease in the incidence and a prolongation of the latency, but a DA precursor, 3,4-dihydroxyphenylalanine (L-DOPA; 20-80 mg/kg, i.p.), markedly shortened the latency. Furthermore, the effect of L-DOPA on the convulsions was inhibited by the combination of 5-HTP. alpha-Methyl-p-tyrosine (20-80 mg/kg, i.p.) or DL-p-chlorophenylalanine (20-80 mg/kg, i.p.), an inhibitor of NE and DA or 5-HT biosynthesis, had a slight effect on the convulsions. These results suggest that procaine causes significant elevations of rat spinal DA and 5-HT in the convulsive process and suggest that dopaminergic and serotonergic neurons may be associated with procaine-induced convulsions.

Animals↗
PubMed1990

Procaine inhibits cyclic AMP-induced steroidogenesis in isolated bovine adrenocortical cells.

Effects of procaine on dibutyryl adenosine 3',5'-cyclic monophosphate ((Bu)2cAMP)-, Ca2(+)- or forskolin-induced steroidogenesis were examined in isolated bovine adrenocortical cells. Procaine (less than 1.0 mM) caused a marked suppression of (Bu)2cAMP- or forskolin-induced steroidogenesis in the absence of extracellular Ca2+, but did not affect on Ca2(+)-induced steroidogenesis in the cells. (Bu)2cAMP decreased the cell associated 45Ca2+. However, procaine (300 microM) inhibited this effect of (Bu)2cAMP. These results suggest that procaine may abolish (Bu)2cAMP-induced Ca2+ release from intracellular calcium store(s) and inhibits steroidogenesis.

Adrenal Cortex↗
PubMed1990

Procaine (Gerovital): no effect on the rehabilitation result in patients with back or hip disease.

Gerovital was compared with placebo and another procaine preparation in a double blind study of 88 rehabilitation patients suffering from back or hip disease. In an open part of the study procaine from intramuscularly injected Gerovital disappeared from the plasma within 15-30 minutes. In patients treated with Gerovital or another procaine no clinical, physiological or psychological benefits were found in addition to the improvements following rehabilitation compared with placebo treatment. Clinical examination showed that the benefits of rehabilitation were similar in patients receiving Gerovital, another procaine and placebo.

Aged↗
PubMedDate not supplied

Morpho-functional aspects of the influence of procaine and diethylaminoethanol treatment on the immune system of rabbits.

Research was conducted in 24 male rabbits divided into three equal groups: 1) Controls; 2) Given daily i.m. injections with 15 mg/kg body weight of procaine for 30 days; 3) Given daily i.m. injections with 15 mg/kg body weight of diethylaminoethanol (DEAE) for 35 days. Blood samples were taken from the auricular vein to perform haematological investigations: before treatment, during treatment and for another 7 weeks after termination of treatment. At the end of the experiment, the animals were sacrificed in order to collect: 1) leukocytes, macrophages and lymphocytes from their spleen, for the purpose of immunological investigations, and 2) fragments of bone marrow (femur), thymus and spleen, for histopathological investigations. The result of haematological investigations indicated a statistically significant increase of circulating lymphocytes had occurred in rabbits treated with DEAE. There was an increase of percentage as well as of number of circulating lymphocytes. The increase occurred gradually in the course of treatment and continued after treatment was terminated. There were higher values than the initial ones by 44.4% and 66.4%, respectively, during the second and the fourth week after termination of treatment. Afterwards, the values started decreasing, so that by the end of the experiment (week 7 after termination), the values came close to those before treatment. Immunological findings indicated that T lymphocytes collected from rabbits treated with procaine or DEAE did not synthesize migration inhibition factors. Procaine and DEAE were found, in vitro, not to have a polyclonal stimulating effect over T lymphocytes. A study of blastic differentiation showed lymphocytes from treated rabbits to incorporate a larger amount of tritiated thymidine, by 52.6% in the procaine group and by 90% in the DEAE group, than those from non-treated rabbits. Histopathological examination indicated signs of a more intense activity in tissue formations involved in cell proliferation in the lymphoid organs collected from DEAE treated rabbits.

Anesthetics, Local↗
PubMed2005

[Spectral study and determination of metoclopramide and procaine hydrochloride by sequential injection analysis].

A sequential injection spectrophotometric method is proposed for the determination of metoclopramide or procaine hydrochloride, based on the reactions of metoclopramide and procaine hydrochloride with cerium(IV) in sulfuric acid medium. Red intermediate products were observed and were found unstable so that their analytical use is only possible by sequential injection technology. For metoclopramide, the detection limit is 6.5 microg x mL(-1), and the linear range of determination is 9.7-116.6 microg x mL(-1) with a sampling frequency of 45 h(-1). For procaine hydrochloride, the detection limit is 7.4 microg x mL(-1), and the linear range of the determination is 10.0-130.0 microg x mL(-1) with a sampling frequency of 45 h(-1). The method has been applied to the determination of metoclopramide and procaine hydrochloride in tablets and injections with satisfactory results as compared with standard method.

Cerium↗
PubMedDate not supplied

Comparative effects of subarachnoid hyperbaric bupivacaine and tetracaine-procaine for cesarean delivery.

Hyperbaric solutions of 0.75% bupivacaine (8.25% dextrose), and 1% tetracaine mixed with an equal volume of 10% procaine were compared in a double-blind study of 22 parturients undergoing elective cesarean delivery and spinal anesthesia. The onset of sensory anesthesia and motor block was similar in the two groups. The maximal level of sensory anesthesia to pinprick was significantly higher after the use of the tetracaine-procaine mixture. The adequacy of anesthesia was similar in both groups as indicated by the lack of differences with regard to anesthetic supplementation between the groups. However, a significantly shorter duration of sensory anesthesia and motor blockade occurred in the group in which bupivacaine was employed. The incidence of hypotension was higher in those patients receiving the tetracaine-procaine mixture as indicated by the use of significantly higher total doses of ephedrine to maintain baseline blood pressure in this group. No differences in Apgar scores or blood gases were noted between the two groups of patients. This study suggests that hyperbaric 0.75% bupivacaine offers certain advantages over hyperbaric tetracaine-procaine when used in equal volumes for spinal anesthesia cesarean delivery.

Analgesia, Obstetrical↗
PubMed1989

Interaction of 8-(N,N-diethylamino)octyl 3,4,5-trimethoxybenzoate hydrochloride, ryanodine and procaine with muscarinic cholinergic M2 receptor sites in smooth muscle.

We have characterized muscarinic cholinergic receptor sites and interaction of various modulators of intracellular Ca mobilization, such as 8-(N,N-diethylamino)octyl 3,4,5-trimethoxybenzoate hydrochloride (TMB-8), ryanodine, procaine and related drugs with the receptor sites, using a binding assay method with [3H]quinuclidinyl benzilate [( 3H]QNB) in guinea pig tenia cecum membrane fraction. [3H]QNB bound to a single population of sites, and the binding profile of pirenzepine suggest that the receptor sites are probably the M2 type. All the test drugs examined except for ryanodine displaced the [3H]QNB binding, and the slope factors were not different from unity. Affinities of these drugs were comparable to the concentrations usually used to modulate intracellular Ca mobilization. A Scatchard plot of [3H]QNB binding in the presence of TMB-8 or procaine showed that the apparent dissociation constant for [3H]QNB was increased without change in maximum binding. Neither TMB-8 nor procaine had any effect on the rate of dissociation of [3H]QNB from the steady-state complex. These results suggest that TMB-8 and procaine, and possibly other drugs, may interact directly with the muscarinic cholinergic M2 receptor sites in a competitive manner. In contrast, ryanodine had no effect on the [3H]QNB binding up to at least 100 microM. No interaction of ryanodine with M2 receptor sites lends a further support that the drug could be a useful probe for studying intracellular Ca mobilization.

Alkaloids↗
PubMed1979

Procaine as an acetylcholine agonist in snail neuron.

Low concentrations of procaine (10(-5) M) are capable of provoking changes in the membrane potential of snail neurons. This effect is produced by direct application to the membrane and is characterized by a short response time and rapid reversibility. The resulting potential change has the same properties as that which follows acetylcholine application, including the same change of membrane resistance, the same relationship with membrane potential, the same ionic dependence and, finally, the same pharmacological sensitivity. The identity between the acetylcholine and procaine responses holds both for cells depolarized and cells hyperpolarized by acetylcholine. This procaine sensitivity involves only about two-thirds of the cells and it is concluded that procaine activates the cholinergic receptor on these cells.

Acetylcholine↗
PubMedDate not supplied

Comparative experimental research into the nootropic action of procaine and pyracetam.

Procaine exerts a positive influence in different tests that prove its nootropic effects: it improves the learning process in small animals, increases the resistance to hypoxemia induced by curarization and hypobarism, augments the effort endurance. The effect is clearly shown at the dose of 5 mg/kg b.w. in subchronic treatment (five to eight days). A higher dose of procaine--25 mg/kg b.w.--does not influence significantly these tests, but ensures a partial protection against gastric ulcers induced by contention. The efficiency is inferior to pyracetam. Neither procaine nor pyracetam succeeds in protecting against supramaximal electroshock or in influencing EEG changes due to hexobarbital. As shown by EEG, the two substances have different mechanisms of action: procaine triggers cortical inhibitory effects while pyracetam manifests itself by activating phenomena.

Animals↗
PubMed1984

Effects of procaine on the isolated dog coronary artery.

In order to search into the mechanism of the potassium contracture of the dog coronary artery the effects of procaine were studied in the isolated smooth muscle preparation of the dog coronary artery. Procaine is a substance which is known to specifically inhibit the calcium-induced calcium release mechanism. A dose-related relaxation of the potassium contracture was observed with procaine. However, the increase in La3+-resistant 45Ca uptake as measured by the Karaki and Weiss' method (1979) was not inhibited. As reported in a previous paper, caffeine induced a phasic contraction of the fully-depolarized preparation in a calcium-free EGTA containing medium. Procaine produced a dose-related inhibition of this contraction. These findings suggest that the potassium contracture of the dog coronary artery is dependent on the calcium-induced calcium release mechanism. Since the potassium contracture of this preparation can be relaxed by calcium antagonists, it may be inferred that the calcium influx through the voltage-dependent channels may represent the initiation mechanism of the calcium-induced calcium release process.

Animals↗
PubMed1978

Effects of procaine-induced cardioplegia on myocardial ischemia, myocardial edema, and postarrest ventricular function. A comparison with potassium-induced cardioplegia and hypothermia.

The extent of myocardial protection afforded by a procaine cardioplegic solution during cardiac ischemia has been evaluated and compared with the protection seen using a potassium cardioplegic solution. An isolated cat heart model was employed, and ventricular function parameters, intramyocardial gas tensions, and postischemic myocardial edema were measured and compared following 60 minutes of induced ischemia at 37 degrees C. and 27 degrees C. There was no significant improvement in recovery of postarrest ventricular function when procaine cardioplegia was used during normothermic ischemia. When used at 27 degrees C., however, both cardioplegic solutions were associated with significantly better recovery of postarrest ventricular function, although there was less myocardial edema formation in the potassium-treated hearts. Results of this study indicate that procaine-induced cardioplegia provides myocardial protection during anoxic cardiac arrest which is additive to that afforded by hypothermia alone. In addition, procaine cardioplegia results in postarrest functional recovery which is similar to that seen with potassium cardioplegia.

Animals↗
PubMed1984

Serum concentration of penicillin in the horse after repeated intramuscular injections of procaine penicillin G alone or in combination with benzathine penicillin and/or phenylbutazone.

Twenty-one adult horses were randomly assigned into 7 groups of 3 and were treated for 5 days with procaine penicillin G, benzathine penicillin , or phenylbutazone in various combinations and dosage schedules. Serum concentration of penicillin was measured serially over a 7-day period. The highest mean peak serum concentration was 2.06 micrograms/ml. Comparable peak values were seen 2 to 4 hours after administration of 22,000 IU of procaine penicillin G/kg of body weight given once or twice daily. A minimum serum concentration of 0.25 micrograms/ml was selected as adequate for efficacy against organisms that can be considered sensitive to penicillin. Once daily administration of procaine penicillin G and, although peak concentrations were lower, some regimens of procaine and benzathine penicillin G did maintain this concentration. Concurrent phenylbutazone administration did not affect serum concentration of penicillin appreciably.

Animals↗
PubMedDate not supplied

[Effect of physiologic concentrations of local anesthetics of the procaine series on the structural and functional state of cerebral synaptosome membranes].

Studies are presented of the effect of procaine group anesthetics on rat brain synaptosome stability to dodecyl sulfate and on catalytic properties of the membrane bound alkaline phosphatase. The dose curves of detergent stability are characterized by two maxima, one at 3.10(-4) M for tetracaine, 2.10(-6) M for lidocaine and 5.10(-5) M for procaine; the other being at 10(-3) M for all anesthetics. The curves of Vmax and KM versus procaine concentration to exhibit the minimum at 5.10(-7) M and maximum at 3,2.10(-6) M. Procaine at 5.10(-7) M increases enthalpy and enthropy of membraneous alkaline phosphatase. It is suggested that interactions between anesthetics and centers of high affinity lead to synaptosome structural rearrangements, which affect the properties of membraneous enzymes.

Alkaline Phosphatase↗
PubMedDate not supplied

[Sensitivity in vitro of some bacterial strains to procaine].

The action range of procaine, this multipotent substance, may also be extended to the domain of bacteriology due to its bacteriostatic, bactericide, fungistatic and fungicide properties. The antibacterial activity of Höechst procaine hydrochlorate powder was determined on 15 bacterial strains and 2 Candida strains isolated from various human infections. The in vitro antibacterial effect of the powder was demonstrated by the diffusimetric and the dilution methods, determining the minimal inhibitory concentration and minimal bactericide concentration. Procaine had a high antibacterial activity against Streptococcus B hemolyticus gr. A and viridans, and against certain enterobacteria (E. coli Proteus). THe results show the possibility of using procaine also in the local treatment of infections caused by these agents.

Bacteria↗
PubMed1981

Protection of the myocardium during ischemic arrest. Dose-response curves for procaine and lignocaine in cardioplegic solutions.

The dose-response curve of procaine or lignocaine (lidocaine) added to the St. Thomas' Hospital cardioplegic solution was investigated with an isolated working rat heart preparation. In the absence of any cold cardioplegic protection, hearts failed to recover after as little as 30 minutes of ischemia. A single infusion (20 degrees C) of the basic St. Thomas' Hospital cardioplegic solution allowed hearts to recover to 60% or more of their preischemic control aortic flow after a 120 minute period of ischemia. Addition of procaine to the cardioplegic solution either increased or reduced the apparent protective properties of the solution with a bell-shaped dose-response curve being obtained. The optimum procaine concentration was 0.05 mM/L. At this concentration the protection afforded by the St. Thomas' Hospital solution was increased by up to two thirds. Substitution of lignocaine for procaine resulted in a similar dose-response curve with its optimum also at 0.05 mM/L. If a similar optimum exists for the human heart, the doses in current clinical use would appear to be too high. These results argue for determining the dose-response characteristics of all substances used in cardioplegic solutions.

Animals↗
PubMed1993

Depletion of intramuscularly and subcutaneously injected procaine penicillin G from tissues and plasma of yearling beef steers.

Withdrawal periods required when doses of 24,000 IU and 66,000 IU of procaine penicillin G/kg body weight were administered to yearling beef steers by intramuscular injection daily for five consecutive days were investigated. These dosages are in excess of product label recommendations, but are in the range of procaine penicillin G dosages that have been administered for the treatment of some feedlot bacterial diseases. The approved dose in Canada is 7,500 IU/kg body weight intramuscularly, once daily, with a withdrawal period of five days. Based on the tissue residue data from this study, the appropriate withdrawal period is ten days for the 24,000 IU/kg body weight dose and 21 days for the 66,000 IU/kg body weight dose when administered intramuscularly to yearling beef steers. In a related study, 18 yearling beef steers received 66,000 IU of procaine penicillin G/kg body weight administered by subcutaneous injection, an extra-label treatment in terms of both dose and route of administration, typical of current practice in some circumstances. Deposits of the drug were visible at subcutaneous injection sites up to ten days after injection, with more inflammation and hemorrhage observed than for intramuscular injections of the same dose. These results suggest that procaine penicillin G should not be administered subcutaneously at high doses; and therefore a withdrawal period was not established for subcutaneous injection.

Animals↗
PubMed1996

Procaine and timing of aortic declamping affect ventricular reperfusion fibrillation.

Both ventricular fibrillation and electric defibrillation are detrimental to the myocardium. Therefore, we studied the effect of procaine hydrochloride during crystalloid cardioplegia and the effect of performing all central anastomoses before aortic declamping in an attempt to prevent ventricular reperfusion fibrillation during coronary bypass operation. Seventy-four patients were randomised, first to receive procaine hydrochloride or saline during cardioplegia, and secondly, to have central anastomoses performed before and after aortic declamping. In patients receiving procaine in cardioplegic solution (n = 37), the mean ventricular fibrillation time was shorter (27 +/- 79 sec. vs 205 +/- 161 sec., P < 0.0001), the proportion of patients spontaneously achieving stable rhythm was higher (67.6% vs 13.5%, P < 0.0001) and the mean number of defibrillations was lower (0.3 +/- 0.7 vs 2.4 +/- 1.7, P < 0.0001) than in patients receiving placebo (n = 37). Although the aortic occlusion time was longer (112 +/- 28 min vs 91 +/- 26 min, P = 0.0015) in patients with central anastomoses made during cardiac arrest (n = 35) and the mean fibrillation time was shorter (53 +/- 87 sec. vs 173 +/- 179 sec., P = 0.0006) than compared with patients with central anastomoses made after declamping the aorta (n = 39), the mean number of defibrillations (1.2 +/- 1.7 vs 1.4 +/- 1.7, P = 0.59) and the cardiopulmonary bypass time (138 +/- 29 min vs. 132 +/- 34 min, P = 0.47) were not statistically different between these groups. There were no differences in arrhythmias, conduction defects or postoperative recovery between the study groups. We conclude that both procaine hydrochloride during cardioplegia and the performance of central anastomoses of vein grafts during aortic occlusion effectively reduce reperfusion ventricular fibrillation.

Adult↗