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PubMed1996

[Potentiation of procaine-induced local sensory block by verapamil in rats].

We have studied the effects of calcium-channel blocker, verapamil, on procaine-induced local sensory block. Standardized tail-flick (TF) test was used to investigate the duration and intensity of procaine-induced local conduction block in rats. After obtaining baseline TF latencies (mean; 3.3 sec), two 100 microliters of 0.4% procaine alone, a combination of 0.4% procaine and verapamil (100 micrograms, or 200 micrograms), or a large dose of verapamil (200 micrograms) were injected to the opposite sites of the tail base and TF test was performed every five minutes for 45 minutes. A large dose of verapamil showed no prolongation of TF latencies. The administration of 0.4% procaine alone produced a significant increase of TF latencies and the peak effect of % MPE (percent maximum possible effect) was demonstrated at 4 minutes after the drug injection (mean % MPE; 37.0%). Coadministration of 0.4% procaine and two doses of verapamil produced significant increases of % MPE in a dose-dependent fashion. It was concluded that sensory block by procaine of the peripheral nerves is potentiated by coadministration of calcium-channel blocker, verapamil.

Anesthetics, Local↗
PubMedDate not supplied

Procain and diethylaminoethanol influence on the release of free oxygen radicals by polymorphonuclear leukocytes, in rabbits and humans.

The investigations were conducted on 3 groups of New Zealand rabbits: 1) controls; 2) injected with procain, i.m. 15 mg/kg body weight, daily, for 30 days; 3) injected with diethylaminoethanol (DEAE), 15 mg/kg body weight, daily, for 35 days. The study was made also on human leukocytes, isolated from the peripheral blood of 10 clinically healthy subjects (adults), procain and DEAE action being investigated in vitro. The free oxygen radicals (FOR) released by PMN leukocytes were evaluated by chemiluminescence, in vitro. Addition of procain or DEAE had no effect on the release of FOR by PMN leukocytes of control rabbits. In the experiment made on rabbits treated with procain or DEAE, the release of FOR by PMN leukocytes was much more reduced, as compared to controls. In the rabbits treated with procain, the intensity of the emitted light was 2.27 mV, in those treated with DEAE, 3.46 mV, while in the controls, the mean value was 6.74 mV. In the in vitro experiments performed on human PMN cells stimulated with opsonized zymosan (OZ), addition of procain or DEAE had an inhibiting effect on the FOR release. As compared to control, the means of the FOR values decreased from 59 to 41.2 mV in case of procain addition and from 67.7 to 50 mV in case of DEAE addition. The fact that the inflammation is associated with accumulation of free radicals, suggests the opportunity to test these substances, especially DEAE, as antioxidant agents.

Anesthetics, Local↗
PubMed1998

Procaine spinal anesthesia: a pilot study of the incidence of transient neurologic symptoms.

STUDY OBJECTIVES: To determine the approximate incidence of transient neurologic symptoms (TNS) [formerly known as transient radicular irritation (TRI)] associated with procaine spinal anesthesia, and whether fentanyl prolongs the duration of procaine spinal anesthesia. DESIGN: Unrandomized pilot study. SETTING: Community teaching hospital. PATIENTS: 106 consecutive patients scheduled for spinal anesthesia for procedures anticipated to last less than 90 minutes. INTERVENTIONS: All patients received 5% procaine for spinal anesthesia. Fentanyl 20 micrograms was added for procedures anticipated to last longer than 45 minutes (but less than 90 min). Intraoperatively the adequacy of duration, level, and intensity of anesthesia were observed. Time from injection of local anesthetic until knee-bending was recorded. Three days postoperatively, patients were questioned intensively in an effort to determine whether back pain and/or symptoms consistent with TNS had occurred. MEASUREMENTS AND MAIN RESULTS: Duration of anesthesia was adequate in all but one instance. The intensity and the sensory level of anesthesia were satisfactory with one exception, a woman who had an unexpectedly low sensory level (L1) after 60 mg of procaine for cerclage, and who was also was the only patients to develop TNS. The incidence of TNS (0.9%) was markedly less than that reported after lidocaine and similar to the incidence observed after bupivacaine. Mild back pain without radiation occurred in 11 patients (10%), an incidence that is similar to that seen after bupivacaine and lidocaine. Compared with procaine alone, the addition of fentanyl significantly (p = 0.0001) prolonged the time to bending knees from 72 minutes to 97 minutes. CONCLUSIONS: Procaine may be a useful alternative to lidocaine for short procedures, and it is less likely to produce TNS. Fentanyl prolongs motor block when added to procaine.

Adult↗
PubMed1988

Vagotomy by the local anesthetic procaine hydrochloride: a study in the rat.

Transmission of nerve impulses is prevented by the local anesthetic procaine hydrochloride. This study was undertaken in rat models, in which the vagus nerve mediates gastric acid secretion, to examine the action of 1 mL of 5% oral procaine on this secretion. The H+ output (mean +/- SEM) associated with pylorus ligation for 1 h (61 +/- 7 mumol) was depressed by vagotomy or procaine (4.7 +/- 0.5 mumol and 5.8 +/- 0.7 mumol, respectively; p less than 0.001). In the rat without pylorus ligation, reserpine (0.1 mg/kg, ip) stimulated H+ output .4 +/- 0.7 mumol; p less than 0.001). Vagotomy or procaine depressed .4 +/- 0.5 and 3 +/- 0.5 mumol, respectively versus 12.4 +/- 0.7 mumol han 0.001), and reserpine failed to influence this action. In the same in (1 unit/kg, ip) stimulated H+ output (36 +/- 3.1 versus 12 +/- 0.6 than 0.001), but had no effect on its depression by vagotomy (3 +/- /- 0.5 mumol) or procaine (4 +/- 0.4 versus 3.9 +/- 0.4 mumol). In the gastric diversion rat, a model for collecting gastric secretion from just distal to the pyloric sphincter into a plastic bag, the effect of vagotomy on the N+ output was similar to that of procaine (3.5 +/- 0.4 and 2.9 +/- 0.3 mumol, respectively, versus 14.8 +/- 0.5 mumol; mean +/- SEM.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed2006

A sequential injection fluorometric procedure for the determination of procaine in human blood and pharmaceuticals.

An automated procedure for the assay of procaine hydrochloride in human blood and pharmaceuticals was developed using a sequential injection (SI) technique with fluorometric detection and fluorescamine as the fluorescence probe. A few microliters of fluorescamine and procaine hydrochloride solutions were used in the SI system leading to the formation of a derivative, which was then excited by a 400-nm LED and whose emitted fluorescence was monitored at a wavelength of 494 nm. A linear calibration graph was obtained with 10-200 ng mL(-1) (procaine) by loading 10.0 microL of sample solution and 5.0 microL of fluorescamine solution (both 0.125 % m/v). A detection limit of 2.6 ng mL(-1), defined as 3 times the blank standard deviation (3sigma), was achieved along with a sampling frequency of 25 h(-1) and a precision of 2.1 % RSD at the 50.0 ng mL(-1) level. Procaine contents in injection solutions from various pharmaceutical manufactures were analyzed and reasonable agreement was achieved between the values obtained by using the present procedure and the documented spectrophotometry, and both were coincident with the nominal concentrations. In addition, the degradation of procaine in human blood was investigated. A fast degradation of procaine in human blood was observed for the first 30 min, while afterwards the degradation was retarded.

Buffers↗
PubMed1984

Inhibition of dog kidney Na+, K+-ATPase activity by procaine, tetracaine and dibucaine.

The potency of local anesthetics as inhibitors of Na+, K+-ATPase and K+- NPPase activities correlated with lipid solubility. The order of potencies was: dibucaine greater than tetracaine much greater than procaine. Na+-ATPase activity was remarkably more sensitive to inhibition by tetracaine and procaine, and inhibitory potency did not correlate with lipid solubility. The order of potencies for inhibition of Na+-ATPase activity was: tetracaine greater than dibucaine greater than procaine. We examined interactions between the local anesthetics and monovalent cations in an attempt to explain this observation. Inhibition of Na+-K+-ATPase by tetracaine and dibucaine was competitive with respect to Na+, and inhibition of Na+-ATPase activity by all three agents was competitive with respect to Na+. Inhibition of Na+, K+-ATPase activity by procaine and tetracaine was competitive with respect to K+, and inhibition of K+- NPPase activity by all three agents was competitive with respect to K+. Dibucaine, the most lipid soluble agent, was equipotent as an inhibitor of all three activities and was generally less effective as a competitor with respect to activation by monovalent cations. These results suggest that dibucaine may interact nonspecifically with membrane lipids to inhibit enzyme activity whereas less lipid soluble agents, such as tetracaine and procaine, may interact more selectively with cation binding sites. It appears that the presence of K+ in the assay medium specifically decreases the inhibitory potency of tetracaine and procaine. Direct competition between these agents and K+ may prevent inhibition or, alternately, the presence of K+ may convert the enzyme to a conformation less susceptible to inhibition by agents of low to intermediate lipid solubility.

4-Nitrophenylphosphatase↗
PubMed1996

Procaine microinjection into the lower midbrain increases brown fat and body temperatures in anesthetized rats.

A tonic inhibitory mechanism on heat production was studied by microinjecting procaine into various regions of the brain while recording temperature changes of the interscapular brown adipose tissue (IBAT) and rectum in urethane-anesthetized rats at room temperature of 23-25 degrees C. Procaine microinjected bilaterally (10%, 1.0 mu l/site, 1.5 mm to midline) into the midbrain and the upper- to mid-pontine area of the reticular formation increased temperatures of the IBAT and rectum. The highest temperature rise (1.02 +/- 0.11 degrees C for IBAT, 0.64 +/- 0.06 degrees C for rectum) with the shortest onset latency (1.5 +/- 0.3 min for IBAT, 4.6 +/- 1.1 min for rectum) was observed when procaine was injected into the lower midbrain (the area between 6 and 7 mm posterior to the bregma, and 6.5 to 8.5 mm deep from the cortical surface). These regions include the retrorubral field, pedunculopontine tegmental nucleus, and rubrospinal tract. Procaine-induced IBAT and rectal temperature increases were dose-dependent, and reproduced reliably from the same injection site of the same animal. Intravenous indomethacin, a prostaglandin H synthase inhibitor, did not affect procaine-induced temperature rise, and propranolol, a beta-blocker, completely blocked it. These results suggest that microinjected procaine exerts its local anesthetic effect and release a tonic inhibition resulting in a disinhibition-induced temperature increase through the enhanced central sympathetic outflow. They support the hypothesis that a bilateral tonic inhibitory mechanism on heat production exists in the lower midbrain.

Adipose Tissue, Brown↗
PubMed1975

Effects of procaine hydrochloride, diazepam, and diphenylhydantoin on seizure development in cortical and subcortical structures in rats.

Procaine HCl and diphenylhydantoin (DPH) increased the duration and propagation of epileptiform afterdischarges (ADs) produced by electrical stimulation of the amygdala in rats. Procaine and DPH also increased the rate of seizure development (kindling) produced by repeated stimulation of the amygdala. Procaine and to a limited extentDPH would themselves act as convulsants in well kindled subjects. Diazepam, on the other hand, retarded or blocked amygdaloid kindling. Diazepam trigered a high frequency (20-30 c/sec) rhtthm in the amygdala, hippocampus and preoptic area. None of these drugs had any significant effect on potentials evoked in secondary limbic sites by single electrical pulses applied to the amygdala. Also, none of these drugs had any effect on recruiting or post-tetanic potentiation (PTP) in secondary sites produced by amygdala stimulation and none of the drugs had any effect on amygdaloid AD thresholds. The effects of these drugs on the responses evoked by anterior neocortex stimulation were quite different. Diazepam had no effect on any of the characteristics of the discharge or convulsion even at twice the dose levels used for the amygdala group. Procaine and DPH, however, blocked not only the eonvulsion but the AD as well. Eighty percent of the procaine- and DPH-treated rats failed to respond with neocortical AD even at current levels as high as 2000 muA. The few cortically stimulated subjects that did respond with an AD showed a subcortical rather than a neocortical seizure response. DPH had no effect on recruiting or PTP of the transcallosal response. Both procaine and DPH produced a weak but significant increase in the amplitude of the transcallosal evoked potential, while diazepam produce a weak decrement in that response.

Amygdala↗
PubMed1976

Conformational aspects of the antifibrillatory activity of procaine.

The effects of procaine and four semi-rigid conformational analogs (compounds 1,2,3 and 4) were tested and compared on isolated rabbit atria. Procaine and the four analogs produced positive inotropic effects at all dose levels tested. The antifibrillatory activity of procaine and its analogs arranged in decreasing order of activity was compound 4 greater than 3 greater than 2 greater than 1 greater than procaine. The antifibrillatory activity of the compounds correlated to the distance between the ring nitrogen and the ester oxygen; that is, as the N-O distance increased the concentration required to reduce the following frequency decreased. However, the compound became more toxic as the N-O distance increased. Our data do not confirm the commonly regarded direct relationship between local anesthetic activity and antifibrillatory activity of procaine. Differences in activity displayed by the isomers of procaine could reflect differences in the ability of these analogs to bind to receptors responsible for the respective actions.

Animals↗
PubMed1983

A comparison of the subjective and cardiovascular effects of cocaine and procaine in humans.

Four normal adult volunteers were given intravenous injections of 16, 32 and 48 mg cocaine, procaine, or saline, once daily in a balanced order. An additional dose of procaine, 96 mg, was also given. Heart rate, blood pressure, and responses on the Profile of Mood States (POMS), Addiction Research Center Inventory (ARCI), and a locally developed drug effects rating scale were measured before and periodically after drug or placebo injection. The profile of action of cocaine was significantly different from that produced by both saline and the lower doses of procaine. Although responses on the ARCI and POMS after all doses of procaine were similar to those obtained after placebo, three of the subjects identified 48 and 96 mg procaine as cocaine, and rated these two drugs similarly at the higher procaine doses.

Adult↗
PubMed2005

The modulation effects of d-amphetamine and procaine on the spontaneously generated action potentials in the central neuron of snail, Achatina fulica Ferussac.

The modulation effects of d-amphetamine and procaine on the spontaneously generated action potentials were studied on the RP1 central neuron of giant African snails (Achatina fulica Ferussac). Extra-cellular application of d-amphetamine or procaine reversibly elicited bursts of potential (BoP). Prazosin, propranolol, atropine or d-tubocurarine did not alter the BoP elicited by either d-amphetamine or procaine. KT-5720 or H89 (protein kinase A inhibitors) blocked d-amphetamine-elicited BoP, whereas they did not block the procaine-elicited BoP. U73122, neomycin (phospholipase C inhibitors) blocked the procaine-elicited BoP, whereas they did not block the d-amphetamine-elicited BoP in the same neuron. These results suggest that BoP elicited by d-amphetamine or procaine were associated with protein kinase A and phospholipase C activity in the neuron.

Action Potentials↗
PubMed1997

Monocarboxylic acids enhance the anesthetic action of procaine by decreasing intracellular pH.

Sodium monocarboxylates are known to enhance the anesthetic action of procaine, and also decrease intracellular pH (pHi). We studied the effect of 30 mM Na monocarboxylates (formate, acetate, propionate, butyrate, and salicylate) on the pHi and on the anesthetic action of procaine HCl using giant axons of crayfish (Procambarus clarkii). The pHi was measured using pH sensitive microelectrode method and the anesthetic action was evaluated by the change in the action potential (AP) amplitude. The tested acids except for formate showed apparent decrease in pHi and enhancement of the action of 2 mM procaine. Other organic acids (maleate and benzensulfonate) did not affect pHi and anesthetic action of procaine. In the bicarbonate free solution, pHi increased and the anesthetic action was weakened. The EC25 values (the concentration of procaine which depresses the AP amplitude by 25%) of acetate, propionate, and bicarbonate free solution were coincided with the predicted EC25 values from the simple simulation on intracellular procaine increase according to the pHi change. But the EC25 value of salicylate group was less than half of the predicted. These results suggested that the enhancing action of straight chain monocarboxylic acids is due to pHi decrease, and salicylate has other additional mechanisms.

Action Potentials↗
PubMed2003

Spectrophotometric determination of procaine hydrochloride in pharmaceutical products using 1,2-naphthoquinone-4-sulfonic acid as the chromogenic reagent.

Spectrophotometric determination of procaine hydrochloride is described. The procaine hydrochloride reacts with 1,2-naphthoquinone-4-sulfonic acid in pH 3.60 buffer solution to form a salmon pink compound, and its maximum absorption wavelength is at 484 nm, epsilon(484)=5.22 x 10(3).The absorbance for procaine hydrochloride from 0.30 to 100 microg ml(-1) obeys Beer's law. The linear regression equation of the calibration graph is C=19.23A-0.03, with a linear regression correlative coefficient is 0.9996, the detection limit is 0.28 microg ml(-1); recovery is from 98.0 to 105.2%. Effects of pH, surfactant, organic solvent, foreign ions, and standing time on the determination of procaine hydrochloride have been examined. This method is rapid and simple, and can be used for the determination of procaine hydrochloride in injection solution of procaine hydrochloride. The results obtained by this method agreed with those by the official method (dead-stop titration).

Hydrogen-Ion Concentration↗
PubMed1999

Complex formation between the anionic polymer (PAA) and a cationic drug (procaine HCI): characterization by microcalorimetric studies.

PURPOSE: Due to the importance of drug-polymer interactions in, inter alia, drug loading/release, supramolecular assemblies and DNA delivery for gene therapy, the aim of this study was therefore to establish the mechanism of interaction between a model polymer (Polyacrylic acid, PAA) and a model drug (procaine HCl). METHODS: This was performed by studying the effect of salt (KCl) concentration on their heat released values using Isothermal Titration Microcalorimetry (ITM). The integrated released heat data were computer fitted to a one class binding model and the thermodynamic parameters (Kobs, deltaH, and N) were determined. RESULTS: As the KCl concentration was increased, Kobs decreased thus establishing the salt dependence of the interaction. The linear variation of deltaGobs with deltaSobs indicated that their interaction was entropically driven. The stoichiometry of the interaction was calculated to be one procaine molecule per monomer of PAA. Dissection of the total observed free energy at each KCI concentration indicated that the contribution of the non-electrostatic attractions to the interaction of PAA with procaine HCl was greater than those of the electrostatic attractions. CONCLUSIONS: We have shown that the interaction between PAA and procaine HCl is dependent upon the presence of counterions (monovalent ions) and is mainly entropically driven. The calculated stoichiometry indicated that one procaine HCl molecule neutralised one carboxylic acid group on PAA. Although electrostatic interactions were necessary for initiating complex formation, the non-electrostatic forces were dominant in stabilising the PAA-procaine HCl complex.

Acrylic Resins↗
PubMedDate not supplied

Intrathecal fentanyl-induced pruritus is more severe in combination with procaine than with lidocaine or bupivacaine.

BACKGROUND AND OBJECTIVES: Fentanyl is used as an additive to prolong intrathecal anesthesia with both lidocaine and low-dose bupivacaine in the outpatient setting to minimize voiding or discharge delays. Pruritus is the most common side effect. When using procaine as a substitute for lidocaine, we perceived an increased frequency and severity of pruritus. We compared prospectively the frequency and severity of itching with combinations of fentanyl with lidocaine, bupivacaine, and procaine. METHODS: After institutional review board approval, 135 patients requesting neuraxial anesthesia were asked to evaluate the presence and severity (using a 100 point verbal pruritus score [VPS]) of itching 30 minutes after injection of their spinal anesthetic, on arrival to the postanesthesia care unit (PACU), and at the time of resolution of their block. Choice of anesthetic drug and dose and the use of intravenous sedation was left to the discretion of the attending and resident anesthesiologist. RESULTS: Thirty-three patients received lidocaine and fentanyl, 47 received bupivacaine and fentanyl, and 55 received procaine and fentanyl. In the lidocaine group, 21% of patients experienced pruritus compared with 55% of the bupivacaine group and 55% of the procaine group (P =.003). The average VPS at 30 minutes postblock was 18.4 in the procaine group compared with 0 and 5.5 in the lidocaine and bupivacaine groups (P =.06). On admission to the PACU, it was 37 compared with 16 and 20 for lidocaine and bupivacaine, respectively (P =.006). CONCLUSION: Procaine produces a higher frequency of pruritus than that seen with lidocaine-fentanyl combinations and a greater severity of pruritus than seen with lidocaine-fentanyl and bupivacaine-fentanyl spinal anesthesia. Reg Anesth Pain Med 2001;26:252-256.

Adjuvants, Anesthesia↗
PubMed1983

Variable interaction of heat and procaine in potentiation of radiation lethality in mammalian cells of neoplastic origin.

Mild hyperthermia in conjunction with procaine HCl acts as a potentiator of radiation lethality in HeLa cells, with little toxicity for unirradiated cells. The majority of irradiated cells responds extensively within a four hour period of treatment with the two agents. Potentiation of radiation lethality by the combined treatment was also found in a line of human melanoma cells, and to a lesser extent in a line of human ovarian carcinoma cells. The interaction of heat and procaine in the process of potentiation of radiation lethality was assessed from a series of radiation survival curves, with temperatures ranging from 37 to 42 degrees C and procaine concentrations from 1 to 3 mM. The interactive factor was obtained from the ratio of the Dose Reduction Factor (DRF) due to procaine in heated cells, to the DRF due to procaine in unheated cells; a ratio larger than unity denotes interaction of heat and procaine. The largest interaction was observed when individual agents exerted only a minimal radiopotentiating effect, as if increased effectiveness of one agent pre-empted the effectiveness of the other agent.

Cell Line↗
PubMed1975

An evaluation of procaine in the treatment of malignant hyperpyrexia.

Procaine has been advocated in the treatment of malignant hyperpyrexia, whereas lignocaine has been shown to worsen the condition. Using muscle from patients susceptible to malignant hyperpyrexia in vitro, it has been demonstrated that muscle contracture can occur with procaine on its own, and in one patient the halothane-induced contracture was potentiated by procaine. In other patients the concentration of procaine required to abolish the halothane-induced contracture was markedly above the clinical dose range. In a study of lignociane and procaine on a caffeinated rat muscle (a suggested model for malignant hyperpyrexia) no significant difference was found in the ability of these local anaesthetics to alter resting tension of halothane-treated muscle; with both drugs the resting tension rose in a dose-related manner. The use of procaine as the drug of first choice in patients with malignant hyperpyrexia is challenged.

Anesthesia, General↗
PubMedDate not supplied

Systemic toxic reactions to procaine penicillin G.

Systemic toxic were encountered in eight of 10,469 patients during or immediately following the intramuscular injection of 4,800,000 units of procaine penicillin G for the treatment of gonorrhea. Fear of imminent death, visual and auditory disturbances, violent combativeness, confusion, disorientation, and restlessness, disturbance in taste, cardiovascular changes, and grand mal seizures are the principal manifestations; these usually subside in two to 10 minutes spontaneously or after treatment. Symptoms and signs closely parallel systemic toxic reactions to local anesthetics. Pharmacokinetic analysis in dogs using 14C-procaine and 14C-procaine penicillin G showed rapid distribution of labeled drugs from plasma to cerebrospinal fluid for the intravenous as compared to the intramuscular route of administration. The animal studies were consistent with the hypothesis that the inadvertent intravenous administration of procaine penicillin G is responsible for the systemic toxic reactions. Plasma procainesterase (pseudocholinesterase) activity was assayed with an ultraviolet spectroscopic method. Substrates were procaine and procaine penicillin G. The plasma procainesterase activity of patients who had experienced systemic toxic reactions was significantly decreased as compared to that of controls, an observation not previously reported.

Adolescent↗