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PubMed1997

Microcirculatory disturbances of the pancreas in cerulein-induced acute pancreatitis in rats with reference to L-arginine, heparin, and procaine treatment.

Local microcirculatory dysfunction within the pancreatic gland might be an important factor in the conversion of oedematous to necrotizing pancreatitis. Therapeutic agents, improving the pancreatic blood flow, might be valuable in acute pancreatitis treatment. An influence of nitric oxide, heparin and procaine treatment on microcirculatory values in acute pancreatitis (AP) in rats was investigated. Acute pancreatitis was induced by i.p. injection of cerulein in four doses of 15 microg kg-1 each at 1-h intervals. The rats with pancreatitis were divided into five groups, 12 animals each. One group remained without treatment, four groups were treated i.p. either with NO synthase inhibitor L-NNA (2x25 mg kg-1 or heparin 2x2.5 mg kg-1 or L-arginine 2x100 mg kg-1 or procaine 2x25 mg kg-1. Five control groups, ten animals each, received saline, L-NNA, heparin, L-arginine or procaine only. Five hours after the first ceruleine injection microcirculatory values within the pancreas were measured by means of laser Doppler flowmetry. Acute pancreatitis caused a significant drop of microcirculatory value to 37% of the basal value. The L-NNA administration resulted in a further insignificant reduction of the pancreatic blood flow to 34%. An improvement of microcirculation was observed in rats with pancreatitis receiving heparin (76%) and L-arginine (72%). Procaine had no effect on microcirculatory disturbances within the pancreas in rats with pancreatitis. Cn-induced acute pancreatitis (AP) causes microcirculatory deterioration within the pancreas. Heparin and nitric oxide donor, L-arginine, might be considered as therapeutic agents, improving the diminished pancreatic tissue perfusion observed in acute pancreatitis. Procaine does not improve the pancreatic blood flow in acute pancreatitis.

Acute Disease↗
PubMed1990

Absorption and metabolism of procaine by the rat small intestine.

The aim of this study was to obtain information about the absorption of procaine in the rat small intestine (Fisher-Parsons preparation). In the range from 0.25-10 mmol.l-1 procaine in the luminal perfusate, much more of the unchanged drug was absorbed in segments of the ileum than of the duodenum and jejunum. Besides procaine, two metabolites, p-aminobenzoic acid (PABA) and acetylated p-aminobenzoic acid (AABA), formed in the intestinal mucosa, appeared in the absorbate. With increasing substrate concentration in the perfusate the PABA in the absorbate increased considerably in all three segments; from 0.75 mmol.l-1 procaine upwards the PABA produced was highest in the jejunum. AABA formed in the mucosa and measured in the absorbate did not increase in the same manner with increasing substrate concentration; in the absorbate of jejunal segments the amount of AABA was significantly higher than in duodenal and ileal segments. Taking into account that in rats the microclimate of the ileum differs considerably from that of the upper part of the small intestine, the marked difference observed in the absorption of procaine between ileal segments on the one side, and duodenal and jejunal segments on the other, can be explained on the basis of the "non-ionic diffusion" theory.

4-Aminobenzoic Acid↗
PubMed1987

Trifluoperazine-sensitive activation of the spontaneous transmitter release at the frog motor endplates by low doses of procaine.

Low concentrations of procaine (10(-6)-5 X 10(-5) mol/l) induced a significant increase of the spontaneous quantal transmitter release in the neuromuscular junctions of the frog cutaneous pectoris nerve-muscle preparation. The frequency of miniature endplate potentials (mepps) was increased although their size slightly decreased probably on the account of a partial block of Na+-channels at the postsynaptic membrane. The activatory effect of pre-caine was not altered under experimental conditions known to change the Ca2+ fluxes across the nerve terminal membrane such as using a Ca2+-free Ringer, or a Ca2+-channel blocker (D600), a high K+ Ringer or, finally, a low Na+ Ringer. In the presence of caffeine no change of procaine-induced activation appeared. Trifluoperazine (TFP), in a concentration known to specifically block calmodulin, completely blocked the procaine-induced increase of mepp frequency. These data suggest that procaine presumably by way of a calmodulin-dependent mechanism is related to the free cytosolic Ca2+ equilibrium. It is possible that procaine increases the free cytosolic Ca2+ concentration by blocking an active calmodulin-dependent Ca2+ extrusion mechanism.

Acetylcholine↗
PubMed1988

Procaine effects on sodium and chloride transport in frog skin.

Procaine, a tertiary amine, has previously been shown to stimulate reversibly transepithelial Na transport across frog skin after application from the epithelial side. In the present study with intracellular recording from principal, i.e. amiloride-sensitive cells, we demonstrate that the stimulation results from increase in apical membrane Na permeability. A second effect of procaine (10-25 mmol/l) in the outside perfusion solution is a reversible increase of transepithelial conductance which drastically exceeds the predicted response of the transcellular Na pathway. It requires presence of chloride on the epithelial side and depends on the non-ionized molecule of procaine. Abolition of apical membrane Na uptake by amiloride or Na-free mucosal incubation decreases the magnitude but does not prevent the stimulatory effect of procaine. The origin of this gain in conductance from stimulation of a Cl-specific pathway is demonstrated by a highly significant correlation between the increases in electrically determined tissue conductance and partial Cl conductance, obtained from measurements of influx and efflux of Cl-36. Measurements with microelectrodes indicate that the stimulated Cl-specific pathway is distinct from the principal cells. Since procaine activates a conductive pathway with similar response pattern as spontaneously existing Cl conductance, it might be a valuable tool for investigating mode and way of Cl movement across epithelial tissues.

Animals↗
PubMed1989

Effects of tetracaine and procaine on skinned muscle fibres depend on free calcium.

The local anaesthetics, tetracaine and procaine have previously been found to block, induce or potentiate Ca2+ release from the sarcoplasmic reticulum (SR) of skeletal muscle depending on the preparation, experimental conditions and design. We now show that low concentrations of tetracaine and procaine block SR Ca2+ release whereas high concentrations induce release from the SR of amphibian and mammalian skinned fibres. Both actions depend on pCa, such that a shift in pCa can alter their effect from blocking to releasing Ca2+. In skinned fibres with Ca2+-loaded SR, tetracaine (1 mM) produced a tonic contraction with a time to half-peak of 15-20 s and a magnitude reaching 80% of maximum force. Ca2+ release by tetracaine or procaine occurred at pCa less than or equal to 6.5 and was not blocked by Ruthenium Red (RR) (25 mM). This action of tetracaine was attributed to SR Ca2+ release rather than to a displacement of bound Ca2+ because fibres lacking a functional SR due to pre-treatment with quercetin (100 mM), A 23187 (100 micrograms ml-1) or Triton X-100 (1%) did not contract after additions of tetracaine. Lower concentrations of tetracaine (0.5 mM) and procaine (less than or equal to 10 mM) blocked contractions due to caffeine (at pCa greater than or equal to 6.73), sulphydryl oxidizing agents, or Ca2+-induced Ca2+ release (CICR). The inhibition of CICR as a function of pCa was difficult to measure quantitatively since lowering pCa to elicit CICR twitches was sufficient to initiate tetracaine-induced tonic contractions. Experiments with isolated SR vesicles showed that 1 mM tetracaine inhibited CICR, over a wide range of pCa but 3-5 mM tetracaine induced rapid Ca2+ release. The opposite effects of tetracaine and procaine depend mostly on their concentration in SR vesicles and/or pCa in skinned fibres. Blockade of release seems to occur via the CICR pathway, and induction of release through an increase in SR membrane permeability.

Animals↗
PubMed1995

Comparison of the reinforcing efficacy of cocaine and procaine in rhesus monkeys responding under a progressive-ratio schedule.

Rhesus monkeys (n = 5) were prepared with chronic IV catheters and trained to lever press under a PR schedule of drug injection. The schedule consisted of five components, each made up of four trials (i.e., 20 trials total). Each trial within a component had the same response requirement. The response requirement in the first component was 120/trial and doubled in successive components to a maximum of 1920 in the fifth. A trial ended with an injection or the expiration of a 12-min limited hold (LH). The inter-trial interval (ITI) was 15 or 30 min. Following an injection or expiration of the LH, all stimulus lights were extinguished and responding had no consequence for the remainder of the trial. A session ended when either all 20 injections were self-administered or the response requirement was not met within the LH for two consecutive trials. The number of injections/session and responses/session increased with dose for cocaine (0.012-0.1 mg/kg per injection) and procaine (0.12-2.0 mg/kg per injection) at both ITI values. At the 15-min ITI, responding decreased again at higher doses in some monkeys with cocaine and in all monkeys with procaine. At maximum, cocaine maintained significantly more injections and responses/session when the ITI was 30 min than when it was 15 min. In contrast, the increase in ITI did not increase the maximum maintained by procaine. Cocaine was approximately 10-fold more potent than procaine and maintained at maximum significantly more injections and responses than procaine when ITI was 30 min but not when the ITI was 15 min.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed2001

Intrathecal fentanyl does not modify the duration of spinal procaine block.

PURPOSE: To document the clinical characteristics of spinal procaine with or without the addition of fentanyl in light of the failure rate observed previously with procaine 10%. METHODS: In a randomized, prospective, double-blind study, 52 patients received spinal anesthesia with 100 mg procaine and either saline 0.9% (0.4 ml) (CONTROL group) or 20 microg fentanyl (0.4 ml) (FENTANYL group). Sensory anesthesia to needle prick was evaluated each minute for ten minutes, every three minutes for 33 minutes and every five minutes until regression to T10. Motor block was assessed with the Bromage scale. Patients were questioned by telephone for pain suggesting transient radicular irritation (TRI) 48 hr later. RESULTS: Mean time to reach highest sensory level, maximum number of segments blocked and mean time for regression of the sensory level to T10 showed no difference. Time to recuperate to full flexion of knees and feet (Bromage 4) showed no difference. Nine patients had nausea (five in CONTROL group and four in FENTANYL group) and nine had pruritus (three in CONTROL group and six in FENTANYL group). No patient reported pain suggesting TRI. CONCLUSION: Spinal procaine is appropriate for short-duration surgery. Fentanyl does not change the characteristics of the block or the incidence of side effects associated with spinal procaine.

Adolescent↗
PubMed2004

[Differentiation of peripheral and central hyperalgesic effects of systemic procaine].

OBJECTIVE: The aim of this study was to differentiate between the peripheral and central analgesic and antihyperalgesic properties of systemic procaine hydrochloride in standardized human pain models. METHOD: Subcutaneous injections of either 150 mg procaine hydrochloride or saline solution were administered at intervals of 2 weeks on a randomized and double blind basis. During the 90-min infusion and subsequent 60-min monitoring periods, touch sensitivity was determined and in addition two experimental hyperalgesic models were analyzed. RESULTS: While touch sensitivity was not affected by procaine hydrochloride, development of primary mechanical hyperalgesia was significantly reduced. CONCLUSION: The concentration of procaine hydrochloride used in our experiment elicited peripheral antihyperalgesic effects without central venous side effects. These results can account for the clinical effect of low-dose procaine hydrochloride in pain conditions exhibiting pronounced hyperalgesia.

Anesthetics, Local↗
PubMed1993

Ipsilateral hemiconvulsive seizure after unilateral injection of procaine into the substantia innominata of amygdaloid-kindled rats.

The effects of procaine injected into the substantia innominata (SI) and the amygdala (AM) were compared in AM-kindled rats. Intra-SI injection of procaine (ipsilateral to the kindled AM) caused immediate contralateral hemiparesis lasting for about 30 min, associated with EEG amplitude reduction. When the kindled AM was stimulated at the previously established generalized seizure triggering threshold (GST), 8/15 animals had ipsilateral hemiconvulsive seizure 5 min after the injection. In all the animals, afterdischarge was readily produced with a significant reduction in its duration. When procaine was injected into the kindled AM, there was no paresis or EEG change. AM stimulation at the GST did not evoke afterdischarge 5 min after the injection, although the kindled seizure was reactivated by a more intense stimulus. After 24 hr, all the animals, regardless of the site of procaine injection, responded to GST stimulation with a kindled seizure. The data suggest that: (1) the effect of intra-SI procaine is not due to drug diffusion to the kindled AM, and (2) the kindled AM can gain access to the contralateral hemispheric motor mechanism without participation of the ipsilateral SI.

Amygdala↗
PubMed1985

Dual effect of procaine in sea urchin eggs. Inducer and inhibitor of microtubule assembly.

An increase in the amount of cytoplasmic filamentous structures (cytoplasmic matrix and aster) which were recovered after hexylene glycol/Triton X-100 treatment of sea urchin eggs (Paracentrotus lividus) activated by 0.2-2.5 mM procaine was observed. At higher activator concentrations, an opposite effect was observed and formation of these cytoplasmic structures was inhibited in the presence of 10 mM procaine. This inhibitory effect was reversed by diluting the drug in the incubation medium. DNase I inhibition assays on egg homogenates which were performed at different time points of the activation process, show that the same amount of actin was induced to polymerize in eggs activated either by 2.5 or 10 mM procaine. However, colchicine-binding assays on the 100 000 g particulate fractions of these homogenates show that in eggs activated by 10 mM procaine, in contrast to those activated by 2.5 mM, tubulin polymerization was inhibited and microtubules were disassembled. These results show that the dual effect of procaine in the organization of the egg cytoskeleton appears to be related to its effect on the state of tubulin.

Animals↗
PubMed1981

Comparison of the reinforcing properties of cocaine and procaine in rhesus monkeys.

Previous studies have shown that a variety of local anesthetics including procaine are self-administered at high rates by rhesus monkeys. In the present study two rhesus monkeys were given a mutually exclusive choice between various doses of intravenous cocaine and procaine. In almost all comparisons cocaine was preferred even when the procaine dose was 16 times that of cocaine. Other measures of performance such as rate of responding did not vary systematically with preference. These data provide further support for the idea that rate of responding under simple schedules of drug delivery is an unreliable measure of relative reinforcing efficacy. In addition, the consistent preference for cocaine over procaine in monkeys suggests that the infrequent abuse of procaine by humans may be related to its low reinforcing efficacy relative to drugs such as cocaine.

Animals↗
PubMed1983

Effects of procaine and oxyphenylbutazone on interferon-mediated inhibition of murine leukemia virus production.

Treatment of murine NIH/MOL, C cells which are chronically infected with Moloney murine leukemia virus (MuLV), with mouse interferon (IFN), causes inhibition of extracellular MuLV production. We tested the effect of procaine, a drug that is known to expand cellular membranes and to increase their fluidity, on IFN-mediated inhibition of MuLV production. We observed that procaine did not alleviate this inhibition when IFN was present during procaine treatment. However, if IFN was removed from the culture medium before procaine treatment, the inhibition of MuLV production was partially reversed. We also observed that procaine treatment caused an increase in the amount of MuLV production by cells which had not been treated with IFN. Oxyphenylbutazone (OPB) is an inhibitor of cyclooxygenase, a key enzyme in prostaglandin biosynthesis. New synthesis of prostaglandins is thought to be needed for the antiviral actions of IFN. We observed that OPB did not prevent the antiretroviral action of IFN on NIH/MOL, C cells. OPB also failed to alleviate the IFN-mediated inhibition of replication of vesicular stomatitis virus either in NIH/MOL, C cells or in the L929 cells.

Animals↗
PubMed1985

Basic science and clinical aspects of procaine HCl as a limbic system excitant.

The literature in animals and humans which indicate that systemic procaine HCl activates limbic tissue is reviewed. Studies in cats which suggest that procaine excites limbic cells by reducing neural inhibition are then described. Evidence that power spectral analysis of high frequency EEG bands (omega or 31-55 cps) in the temporal cortical EEG reflects degree of limbic (amygdala) excitation in animals and humans is reviewed. Studies in cats are described which show that procaine selectively increases omega band activity in the amygdala and temporal cortex in a dose related fashion which parallels dose related increases in amygdaloid neural activity. Preliminary results of combining intravenous procaine and omega band analysis of scalp EEG in humans to predict therapeutic response to carbamazepine in borderline personality and affective disorder patients are then described. The effects of procaine on omega are compared to the effects of direct electrical stimulation of human limbic system in complex partial seizure patients undergoing assessment for temporal lobectomy. The results tentatively support the hypothesis that some psychiatric patients have hyperexcitable limbic systems, and those that do, show a positive behavioural response to carbamazepine.

Animals↗
PubMed2005

An explanation for the efficacy of procaine in the treatment of sickle cell anaemia.

A study has been carried out into the effects of procaine on the activities (Na+,K+)- and (Ca2+,Mg2+)-ATPases of the human erythrocyte membrane. In general, procaine inhibited both types of ATPases activities but with characteristic inhibition profiles and varying degrees of efficacy. In addition, the effects of procaine on the transport of K+ and phosphate ions across the membrane of the human erythrocyte were monitored and compared. Procaine was found to stimulate K+ release and to inhibit phosphate uptake. At low concentrations, both processes were found to be concentration dependent. Stimulation of K+ release and inhibition of phosphate uptake reached plateaus at concentrations of 50 and 150 mM, respectively. The antisickling effect of procaine was explained mainly in the light of the changes it induces in the activities of membrane bound ATPases and the permeability properties of the erythrocyte membrane to cations and anions.

Anemia, Sickle Cell↗
PubMed2005

A study of the perturbation effects of the local anesthetic procaine on human erythrocyte and model membranes and of modifications of the sodium transport in toad skin.

The interaction of the local anesthetic procaine with human erythrocytes, isolated unsealed human erythrocyte membranes (IUM), isolated toad skins, and molecular models is described. The latter consisted of phospholipid multilayers built-up of dimyristoylphosphatidylcholine (DMPC) and of dimyristoylphosphatidylethanolamine (DMPE), representatives of phospholipid classes located in the outer and inner monolayers of the human erythrocyte membrane, respectively. Optical and scanning electron microscopy of human erythrocytes revealed that procaine induced the formation of stomatocytes. Experiments performed on IUM at 37 degrees C by fluorescence spectroscopy showed that procaine interacted with the phospholipid bilayer polar groups but not with the hydrophobic acyl chains. X-ray diffraction indicated that procaine perturbed DMPC structure to a higher extent when compared with DMPE, its polar head region being more affected. Electrophysiological measurements disclosed a significant decrease in the potential difference (PD) and in the short-circuit current (Isc) after the application of procaine to isolated toad skin, reflecting inhibition of active ion transport.

Anesthetics, Local↗
PubMed2003

The sensitivity of sodium channels in immature and mature rat CA1 neurones to the local anaesthetics procaine and lidocaine.

Sodium currents were recorded in CA1 hippocampal cells from new-born (P(4-10)) and older (P(>22)) rats, using whole-cell voltage clamp techniques. The effects of local anaesthetics (procaine and lidocaine) were studied in both cell populations. Parameters defining steady-state inactivation, removal of inactivation and the affinity of the anaesthetic molecules to the inactivated state were determined at both stages of maturation. Procaine and lidocaine induced a hyperpolarizing shift in steady-state inactivation curves, and slowed the rate of recovery from the inactivated state. Procaine disclosed differences between immature and older cells in what concerns block of the closed (resting) channels, drug affinity and binding to the inactivated state, i.e. the binding rate of procaine was found higher and the affinity lower in younger cells. The characteristics of procaine and lidocaine block on CA1 sodium currents differed in some particular aspects: magnitude of block on resting channels, shift in the voltage dependence and voltage sensitivity of steady-state inactivation, slow recovery from inactivation and use-dependent block.

Anesthetics, Local↗
PubMed2006

Simultaneous determination of procaine and para-aminobenzoic acid by LC-MS/MS method.

A sensitive high performance liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed for simultaneous determination of procaine and its metabolite p-aminobenzoic acid (PABA). N-Acetylprocainamide (NAPA) was used as an internal standard for procaine and PABA analysis. This assay method has also been validated in terms of linearity, lower limit of detection, lower limit of quantitation, accuracy and precision as per ICH guidelines. Chromatography was carried out on an XTerra MS C(18) column and mass spectrometric analysis was performed using a Quattro Micro mass spectrometer working with electro-spray ionization (ESI) source in the positive ion mode. Enhanced selectivity was achieved using multiple reaction monitoring (MRM) functions, m/z 237-->100, m/z 138-->120, and m/z 278-->205 for procaine, PABA and NAPA, respectively. Retention times for PABA, procaine and NAPA were 4.0, 4.7 and 5.8min, respectively. Linearity for each calibration curve was observed across a range from 100nM to 5000nM for PABA, and from 10nM to 5000nM for procaine. The intra- and inter-day relative standard deviations (RSD) were <5%.

4-Aminobenzoic Acid↗
PubMed2006

Flow injection amperometric determination of procaine in pharmaceutical formulation using a screen-printed carbon electrode.

A rapid and simple method for procaine determination was developed by flow injection analysis (FIA) using a screen-printed carbon electrode (SPCE) as amperometric detector. The present method is based on the amine/hydroxylamine oxidation from procaine monitored at 0.80 V on SPCE in sodium acetate solution pH 6.0. Using the best experimental conditions assigned as: pH 6.0, flow rate of 3.8 mL min(-1), sample volume of 100 microL and analytical path of 30 cm it is possible to construct a linear calibration curve from 9.0x10(-6) to 1.0x10(-4) mol L(-1). The relative standard deviation for 5.0x10(-5) mol L(-1) procaine (15 repetitions using the same electrode) is 3.2% and detection limit calculated is 6.0x10(-6) mol L(-1). Recoveries obtained for procaine gave a mean values from 94.8 to 102.3% and an analytical frequency of 36 injections per hour was achieved. The method was successfully applied for the determination of procaine in pharmaceutical formulation without any pre-treatment, which are in good accordance with the declared values of manufacturer and an official method based on spectrophotometric analysis.

Anesthetics, Local↗