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PubMed1999

Fluorimetric determination of procaine in pharmaceutical preparations based on its reaction with fluorescamine.

A simple spectrofluorimetric analysis of a local anaesthetic named procaine using a specific labelling reagent for primary amino groups, has been developed. Because procaine shows very weak native fluorescence, the technique of spectrofluorimetry has been very much limited for its determination. A detail study of the variables affecting the derivatisation reaction (pH, fluorescamine (FC) concentration, temperature, reaction time), have minuciously been studied. The minimum detectable quantity is estimated as 7.7 ng ml(-1), with a relative standard deviation of 2.16% (ten determinations) for a procaine concentration of 100 ng ml(-1). The present method can be employed for the analysis of procaine by direct fluorescence measurements, without the interference from other compounds. The applicability of the present methodology have been demonstrated analysing three pharmaceutical preparations containing the analyte with satisfactory results.

Anesthetics, Local↗
PubMed2002

Benzathine penicillin G and procaine penicillin G in piglets: comparison of intramuscular and subcutaneous injection.

The disposition of penicillin G in piglets is described after intramuscular or subcutaneous injection of depot preparations. The piglets were injected with 33,000 IU/kg or 100,000 IU/kg benzathine + procaine penicillin G intramuscularly or subcutaneously, or 100,000 IU/kg procaine penicillin G intramuscularly or subcutaneously. Intramuscular injection of benzathine + procaine penicillin resulted in higher maximum concentrations in plasma (Cmax) than did subcutaneous injection. The mean residence time (MRT) of penicillin G was longer when the drugs were injected subcutaneously rather than intramuscularly. The plasma concentration versus time profiles of the subcutaneous injections of benzathine + procaine penicillin revealed secondary peaks, possibly reflecting a certain degree of inflammation at the injection site.

Animals↗
PubMed2000

Buprenorphine or procaine for pain relief in acute pancreatitis. A prospective randomized study.

BACKGROUND: To assess the analgesic efficacy and side effects of buprenorphine and procaine in patients with acute pancreatitis. METHODS: Forty patients (average age, 50 years; 23 male) with acute pancreatitis or an acute bout of a chronic pancreatitis were prospectively randomized to receive buprenorphine or procaine for pain relief. Both analgesics were administered as constant intravenous (i.v.) infusions and additional analgesics were given on demand. Pain scores were assessed on a visual analogue scale. Close clinical control and laboratory checks were performed during the three-day study period. RESULTS: Patients receiving buprenorphine were significantly less likely to demand additional analgesics (1 versus 14 patients; P < 0.0001). The pain scores for patients in the buprenorphine group were significantly lower over the treatment period in comparison to procaine (P < 0.05). The reduction of pain score was significantly greater during the initial two treatment days using buprenorphine (day 1: 55 versus 25, P < 0.0001; day 2: 62 versus 40, P = 0.005). Side effects were comparable for both groups with the exception of a slightly higher sedation rate under buprenorphine. CONCLUSIONS: Constant i.v. application of buprenorphine is more effective than the recommended procaine for pain relief in acute pancreatitis.

Acute Disease↗
PubMed1986

Differential effects of procaine and phenethyl alcohol on excision repair of DNA in u.v.-irradiated Escherichia coli.

Experiments were performed to investigate the involvement of the cell membrane in the excision DNA repair process in Escherichia coli. Two membrane-binding drugs, procaine and phenethyl alcohol (PEA), inhibited liquid-holding recovery (LHR) in u.v.-irradiated E. coli wild-type and recA strains. In uvrB and polA strains where, after u.v.-irradiation, LHR was absent the two drugs had no effect. Both drugs markedly reduced the removal of u.v.-induced thymine dimers in the DNA of wild-type cells (H/r30). Analysis by alkaline sucrose gradients revealed that PEA inhibited the incision step in excision repair. In contrast, procaine had no effect on incision but apparently inhibited the late steps in excision repair. PEA dissociated DNA from the cell membrane, whereas procaine did not. The results suggest that the two drugs PEA and procaine inhibit LHR and the excision repair process operating on u.v.-induced damage in E. coli by at least two different mechanisms each of which may involve the cell membrane.

Cell Membrane↗
PubMed1999

Pre-ischaemic administration of procaine suppresses ischaemic glutamate release and reduces neuronal damage in the gerbil hippocampus.

The effects of intracerebroventricular administration of procaine 2 mumol on ischaemic release of neurotransmitter amino acids in the gerbil hippocampal CAI region were investigated using a microdialysis-high-performance liquid chromatography procedure. Histological outcome was examined by comparing delayed neuronal death between animals treated with procaine before ischaemia and animals treated after ischaemia. Transient forebrain ischaemia for 3 min produced increases in dialysate amino acid concentrations. Aspartate, glutamate and glycine reached 331%, 394% and 233% of pre-ischaemic values. Basal concentrations were restored immediately by reperfusion. Pre-ischaemic administration of procaine suppressed peak release and improved histological outcome. However, post-ischaemic administration did not protect against ischaemic neuronal death. Improvement in ischaemic neuronal damage by pre-ischaemic administration of procaine may be related to suppression of excitatory amino acid release.

Amino Acids↗
PubMed1982

Kinetics of the actions of caffeine and procaine on the Ca2+-gated cation channel in sarcoplasmic reticulum vesicles.

The effects of caffeine and procaine on the Ca2+-gated cation channel in sarcoplasmic reticulum (SR) vesicles were studied by measuring choline influx. The choline influx in SR vesicles was measured by following the change in light scattering intensity using a stopped flow apparatus. From the kinetic analysis of the rate of choline influx, the following results were obtained. (1) The rate of choline influx was enhanced when Ca2+ bound to the Ca2+-receptor site of the Ca2+-gated cation channel. (2) Caffeine enhanced the choline influx by increasing only the affinity of Ca2+ for the receptor site of the channel and thus regulated the equilibrium between open and closed states of the channel. The affinity increased about 14-fold upon caffeine binding. The dissociation constant of caffeine was 10 mM. (3) In contrast, procaine itself blocked the choline influx mediated by the Ca2+-gated cation channel. The blockade followed a single-site titration curve with a Ca2+-dependent dissociation constant of 0.44 mM at 2 x 10(-6) M Ca2+. The Ca2+-dependence was explained by assuming that procaine would bind to the inhibitory site only when the channel was open. (4) Procaine also inhibited the choline influx enhanced by caffeine. The blockade could be explained on the basis of the above kinetic model.

Animals↗
PubMed1978

Intravenous procaine for general anesthesia in dogs: a new look at an old technic.

New anesthetics have been introduced during the last 25 years which are not without inherent disadvantages. They are expensive, and some produce nephrotoxicity and possibly hepatotoxicity. Although the use of procaine intravenously as an anesthetic has been discarded, probably because of a convulsive effect, it is believed this disadvantage can be controlled by concomitant use of other drugs. Hence procaine, preceded by thiamylal, was administered to dogs to test its anesthetic capability, reversibility, and effects on the cardiovascular and central nervous systems. Blood levels of procaine were measured and correlated with these physiologic responses. Convulsive doses were ten times those producing anesthesia. There were no detrimental effects which would preclude a reevaluation in humans. Intravenous procaine produces definite general anesthesia, and it has the additional advantages of being rapidly hydrolyzed and providing antiarrhythmic effects. It may prove useful in modern anesthesia.

Anesthesia, General↗
PubMed1993

A study of the disposition of procaine penicillin G in feedlot steers following intramuscular and subcutaneous injection.

The disposition of an aqueous suspension of procaine penicillin G (300,000 U/mL) was studied in feedlot steers. Four groups of three steers were used. Steers in groups 1 and 2 received procaine penicillin G once daily for 5 days intramuscularly (i.m.) at a dose of 24,000 U/kg (group 1) or of 66,000 U/kg (group 2). The injection on the last day was administered in the gluteal muscle. Steers in group 3 (i.m. neck injection) and group 4 [subcutaneous (s.c.) injection] each received a single dose of procaine penicillin G at a dose of 66,000 U/kg. From every animal, after the last injection in groups 1 and 2 and following the single injection in groups 3 and 4, a series of blood samples was taken at fixed time intervals. The plasma from these samples was analysed for penicillin G by a high performance liquid chromatography (HPLC) assay in order to determine the disposition of penicillin. The maximum plasma concentration (Cmax) and the area under the curve (AUC) were significantly different between groups 1 and 2, but we found no difference in the disappearance rate constant between these two groups. Group 4 single s.c. injections produced a lower mean Cmax (1.85 +/- 0.27 microgram/mL) than the mean Cmax (4.24 +/- 1.08 micrograms/mL) produced in group 3 by i.m. injections into the neck muscle or the mean Cmax (2.63 +/- 0.27 microgram/mL) produced in group 2 by i.m. injections into the gluteal muscle. However the mean Cmax produced by i.m. injections into the neck muscles (group 3) was higher than the mean Cmax produced by i.m. injections into the gluteal muscle (group 2). Additionally, the disappearance t1/2 was longer (18.08 h) in group 4 following the s.c. injection and shorter (8.85 h) in group 3 following the i.m. neck injection, than the t1/2 following administration of the same dose i.m. into the gluteal muscle (15.96 h) in group 2. In this study, when procaine penicillin G was injected into the gluteal muscle, doses of 66,000 U/kg were necessary to produce plasma concentrations that were above a minimum inhibitory concentration (MIC) for penicillin G of 1.0 microgram/mL as compared to doses of 24,000 U/kg.

Animals↗
PubMed1971

On the neuromuscular paralysis produced by procaine.

1. The effects of procaine on neuromuscular transmission in the rat phrenic nerve diaphragm preparation have been examined using intracellular recording techniques.2. The paralysis produced by procaine resembled that produced by tubocurarine and it is concluded that this effect of procaine results from a change in post-junctional sensitivity to transmitter; at low rates of stimulation procaine did not depress the transmitter release.3. During high frequency stimulation of the phrenic nerve a distinct form of prejunctional failure was observed. It is suggested that this depression results from a combination of local anaesthesia and anoxia and that it would explain reports of a reduction in the amount of transmitter released when assayed in a conventional manner.

Anesthesia, Local↗
PubMed1971

Changes in the time course of transmitter action produced by procaine.

1. In addition to reducing the sensitivity of the end-plate to transmitter, procaine produced changes in the time course of the end-plate potential. The time to peak potential was reduced by procaine, whether recording from fibres paralysed by tubocurarine or from fibres paralysed by high magnesium concentration. The rate of decay of potential was also markedly reduced. Similar observations were made recording spontaneous miniature end-plate potentials.2. Procaine did not produce any marked change in the electrical constants of muscle fibres.3. In the presence of procaine the accumulation of charge at the end-plate was prolonged; the rate of decay of charge was reduced. It is suggested that the prolonged end-plate potentials arise from a prolongation of the end-plate current.

Animals↗
PubMed1974

Effects of procaine and lignocaine on electrical and mechanical activity of smooth muscle of sheep carotid arteries.

1 Procaine in concentrations up to 20 mM facilitated or induced electrical and mechanical activity in arterial smooth muscle, even with tetrodotoxin present.2 Procaine (up to 20 mM) caused relaxation when electrical activity was blocked by prior potassium depolarization.3 Procaine (1 mM) reduced mechanical responses to noradrenaline (1 muM) which were not accompanied by action potentials. It generally reduced mechanical responses to noradrenaline (1 mM) while increasing electrical activity induced by this.4 Lignocaine (1 mM) did not facilitate electrical activity significantly; it relaxed arteries in saline or potassium-rich solution and reduced mechanical responses to noradrenaline.5 High concentrations of procaine (at least 80 mM) or lignocaine (at least 20 mM) blocked electrical activity and caused contraction followed by relaxation and complete unresponsiveness.

Animals↗
PubMed1977

The systemic use of procaine in the treatment of the elderly: a review.

This article is a review and evaluation of the world literature on the systemic use of procaine in the treatment of the aging process and the common chronic diseases of later life. Included are data from 285 articles and books, describing treatment in more than 100,000 patients in the past 25 years. Except for a possible antidepressant effect, there is no convincing evidence that procaine (or Gerovital, of which procaine is the major component) has any value in the treatment of disease in older patients. If procaine has an antidepressant effect, there is some likelihood that this accounts for the reports of decreased complaints referable to the musculoskeletal, cardiovascular, endocrine sexual, gastrointestinal and respiratory systems.

4-Aminobenzoic Acid↗
PubMed1984

Penicillin concentrations in serum and cerebrospinal fluid after intramuscular injection of aqueous procaine penicillin 0.6 MU with and without probenecid.

Paired specimens of cerebrospinal fluid and serum were taken from 21 patients to estimate penicillin concentrations two to three hours after the last dose of a course of 14-21 daily intramuscular injections of procaine penicillin 0.6 MU. Of 10 patients treated with procaine penicillin alone, eight had no detectable penicillin and two had sub-treponemicidal concentrations (less than 0.018 mg/l) in the cerebrospinal fluid. Of 11 patients treated with procaine penicillin as above and probenecid 2 g a day by mouth, three had no detectable penicillin, two had sub-treponemicidal concentrations, and six had treponemicidal concentrations of penicillin in the cerebrospinal fluid. All 21 patients had treponemicidal concentrations of penicillin in the serum. This dose of procaine penicillin alone or with probenecid is therefore not recommended for treating neurosyphilis.

Biological Assay↗
PubMed1978

Increased sensitivity of frog skeletal muscle to procaine in the presence of organic anions.

In solutions containing an organic anion in place of chloride, frog toe muscles displayed increased sensitivity to the local anaesthetic action of procaine. Twitch inhibition by procaine in all media was accompanied by suppression of action potentials without change in membrane resting potentials. The twitch depressant effect of procaine was greater in solutions with carboxylate anions than with alkyl sulfonates. The intensity and the rapidity of onset of the effects of organic anions was related to the size of their hydrophobic component. Procaine accentuated acetate-induced reductions in the [K]0 required to produce K contractures and in the time course of submaximum K contractures. These effects were not shared by benzocaine. They were antagonized by increased [Ca]0. The results indicate that separate agents can exert mutually enhancing actions from opposite surfaces of the sarcolemma to facilitate the inactivation of depolarization-induced excitation--contraction coupling as well as that of the potential-dependent sodium channel.

Action Potentials↗
PubMed1979

Differential effect of procaine on irradiated mammalian cells in culture.

HeLa and V-79 Chinese hamster cells temporarily stored in ampoules were treated with the local anesthetic procaine. Postirradiation treatment increased lethality in HeLa cells depending on drug concentration, duration of treatment and cell density, as measured by colony-forming ability upon plating. If present during irradiation only, procaine protected from irradiation. In V-79 cells procaine potentiated radiation lethality only in freshly trypsinized cells. Procaine effect was thus cell type specific and most likely involved the cell membrane.

Animals↗
PubMed1981

Alteration of lidocaine- or procaine-induced convulsions by manipulation of brain amines.

Lidocaine and procaine seizure thresholds were studied. The i.p. median convulsant dose (CD50) of lidocaine and procaine with saline pre-treatment was 95 and 240 mg/kg, respectively. Dopamine depletion by pre-treatment with d1-alpha-methyl-p-tyrosine plus dihydroxyphenylserine resulted in a significant drop of CD50 to 69 and 175 mg/kg for lidocaine and procaine, respectively. Serotonin depletion by pre-treatment with p-chlorophenylalanine resulted in a significant drop of CD50 to 68 mg/kg for lidocaine, but no significant change for procaine.

Animals↗
PubMed1996

Comparison of the toxicities of cisplatin and a new cisplatin-procaine complex to rat renal cortical slices.

1. Procaine has previously been shown to diminish the nephrotoxicity of cisplatin and the nephrotoxic effects of cisplatin and a new cisplatin complex (cis-diamminechloro-[2-(diethylamino) ethyl-4-aminobenzoate, N4]-chlorideplatinum (II) monohydrochloride monohydrate; DPR), that contains procaine hydrochloride were compared with rat renal cortical slices. 2. Cisplatin at 1 mM caused toxicity to the slices, as shown by an increase in the leakage of aspartate aminotransferase and lactate dehydrogenase from the slices into the incubation medium and a decrease in the reduction of a tetrazolium dye (MTT assay). Addition of procaine (1 mM) protected against cisplatin-induced toxicity. DPR either at 1 mM or at 4 mM had no effect either on the enzyme leakage or MTT reduction by the renal slices, but DPR at 10 mM produced a similar magnitude of enzyme leakage to cisplatin (1 mM). 3. DPR lowered the concentration of ATP and glutathione (GSH) in the slices but was less potent than cisplatin. Thiobarbituric acid reactive substances, indicators of lipid peroxidation, released into the medium were increased by the highest concentration of DPR (10 mM), which suggests that DPR has the potential to cause oxidative stress. 4. The results suggest that DPR was far less toxic than either cisplatin alone or a mixture of cisplatin and procaine.

Adenosine Triphosphate↗
PubMedDate not supplied

Pharmacokinetics of intravenous procaine infusion in humans.

Pharmacokinetic data during and following the continuous intravenous infusion of procaine are lacking. We studied 12 women undergoing hysterectomy during N2O-O2 and narcotic anesthesia. A constant infusion of 2% procaine was administered at a rate of 1 mg/kg/min to six patients (group I) and at a rate of 1.5 mg/kg/min to the other six (group II). Procaine plasma levels were determined by flame ionization gas-liquid chromatography. Using a two-compartment pharmacokinetic model, disposition kinetics were studied. Steady-state plasma levels were achieved within 20 to 30 minutes after commencement of the infusion. Following termination of the infusion the drug disappeared with a distribution half-life (t1/2 alpha) of 2.49 +/- 0.36 minutes and an elimination half-life (t1/2 beta) of 7.69 +/- 0.99 minutes at both infusion rates. In group I, the fraction of drug in the central compartment was 65%, the volume of distribution at steady-state was 0.79 +/- 0.14 L/kg, and total body clearance 0.08 +/- 0.01 L/kg/min. In group II, the fraction of drug in the central compartment was 82%, the volume of distribution at steady-state 0.34 +/- 0.07 L/kg, and the total body clearance 0.04 +/- 0.01 L/kg/min. These data indicate that procaine is a drug of limited distribution and tissue uptake with a short duration of action.

Adult↗