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PubMed1998

Caffeine- and noradrenaline-induced contractions of human vas deferens: contrasting effects of procaine, ryanodine and W-7.

1. The effects of ryanodine, procaine, and N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) on noradrenaline (NA)- and caffeine-induced contractions of human vas deferens were investigated. 2. In the presence of nifedipine (1 microM), NA ( 100 microM) evoked biphasic contractions. Caffeine (20 mM) evoked repeatable tonic contractions. 3. Ryanodine (30 microM) inhibited the initial but not the secondary component of NA contractions. Procaine (1 and 10 mM) inhibited both components. Contractions induced by caffeine were unaffected by ryanodine or procaine. 4. The calmodulin antagonist W-7 (100 microM) reduced, in a reversible manner, both components of NA-induced response. Caffeine-induced contractions were also reduced in most preparations (8 of 11). In all preparations, contractions induced by caffeine were markedly inhibited after the washout of W-7. Higher doses of W-7 (300 microM) induced an increase in basal tension. 5. These results indicate that NA contracts the longitudinal muscle of human vas deferens by a ryanodine-sensitive calcium-induced calcium release (CICR) mechanism and, in addition, a ryanodine-insensitive pathway: both are sensitive to procaine. In contrast, contraction induced by caffeine is mediated by a pathway that is atypically insensitive to either ryanodine or procaine. The sensitivity of NA- and caffeine-induced contraction to W-7 suggests a role for calcium and its interaction with calmodulin in the response to both agents. The paradoxical action of W-7 is discussed.

Anesthetics, Local↗
PubMed1998

Quantification of penicillin-G and procaine in equine urine and plasma using high-performance liquid chromatography.

A rapid and sensitive method for the extraction and quantification of penicillin-G and procaine in horse urine and plasma samples has been successfully developed. The method involves the use of solid-phase extraction (SPE) for penicillin-G, liquid-liquid extraction (LLE) for procaine, and high-performance liquid chromatography (HPLC) for the quantification of penicillin-G and procaine. The new method described here has been successfully applied in the pharmacokinetic studies of procaine, penicillin-G and procaine-penicillin-G administrations in the horse.

Animals↗
PubMedDate not supplied

Minimal blocking concentrations of bupivacaine and procaine in an exclusively nociceptive system in humans.

BACKGROUND AND OBJECTIVES: Prior to this investigation, there was no approach to compare both the potency of local anesthetics and their time course of action in a reproducible nociceptive system in humans. We tested whether the vascularly isolated vein segment is appropriate for such an approach. METHODS: In six healthy men, a hand vein segment was vascularly isolated and intraluminally stimulated with electropulses of constant current intensity. The subjects rated pain between threshold and maximally tolerable pain on a visual analogue scale. For determining minimal blocking concentrations (a measure of potency), the vein segment was continuously perfused with Tyrode's solution with increasing concentrations of bupivacaine or procaine for at least 10 minutes each until pain was completely blocked. Subsequently, the respective local anesthetic was rinsed off with Tyrode's solution to determine the time course of recovery. RESULTS: Both bupivacaine and procaine blocked pain in a concentration-related fashion, the minimal blocking concentrations being 1.6 (0.6-1.9; median and range) mmol/L for bupivacaine and 15.0 (7.5-22.5) mmol/L for procaine. Whereas the onset of block (time of 50% block) did not differ significantly between bupivacaine and procaine [43 s (range, 3-80) vs 53 s (range, 30-115)], local anesthesia lasted significantly longer after application of bupivacaine [278 s (range, 215-325)] than after procaine [183 s (range, 125-225)]. CONCLUSIONS: The vascularly isolated vein segment is well suited to compare in vivo the properties of local anesthetics with a minimally invasive approach at a reproducible nociceptive system in humans.

Adult↗
PubMed1980

Effects of disease and acetazolamide on procaine hydrolysis by red blood cell enzymes.

Procaine hydrolysis in vitro has been studied in whole blood, plasma, and washed erythrocytes. Esterase activity was higher in whole blood than in either diluted plasma or resuspended erythrocytes. Eserine and echothiophate specifically inhibited plasma procaine esterase activity, while acetazolamide blocked hydrolysis of procaine by washed erythrocytes. Kinetic studies in whole blood also identified 2 different enzymes. Procaine esterase activity associated with red blood cells was not impaired in patients with renal failure or hepatic cirrhosis, but procaine half-life (t 1/2) in whole blood of normal subjects was longer after 250 mg acetazolamide.

Acetazolamide↗
PubMed1984

Augmentation of peritoneal dialysis clearance with procaine.

Local anesthetic procaine in a 0.25% concentration was used as the adjunct to the dialysis fluid during peritoneal dialysis in rabbits. Procaine increased peritoneal clearance of urea (2.213 +/- 0.187 ml/min to 3.544 +/- 0.41 ml/min) and inulin (0.528 +/- 0.079 ml/min to 0.852 +/- 0.213 ml/min). Effect of the drug persisted, despite its lack, during the following cycles. Procaine influenced transmesothelial transfer of urea and inulin in vitro. The effect of the drug was biphasic. During the first 20 min a decrease of both solutes fluxes was observed. Then the transport rate of urea and inulin started to grow. The effect of procaine was independent of the membrane's side to which the drug was added. At least two sites of procaine action (vascular system and mesothelium) during peritoneal dialysis are proposed.

Animals↗
PubMed1990

Procaine and lidocaine stimulate corticotropin-releasing hormone secretion by explanted rat hypothalami through a sodium conductance-independent mechanism.

We have previously shown that procaine and lidocaine stimulate corticotropin-releasing hormone (CRH) secretion by explanted rat hypothalami. This effect was of interest in light of the fact that both lidocaine and CRH administration to experimental animals can produce kindled seizures which cross-sensitize with electrically kindled seizures, and of recent data suggesting that limbic hyperexcitability, perhaps mediated through CRH, may be involved in the pathophysiology of affective illness. Because a prominent effect of the local anesthetics is to decrease neuronal firing by blocking sodium conductance, we were surprised by the capacity of these agents to cause CRH secretion and pituitary-adrenal activation and wished to further elucidate the possible mechanism(s) of these effects. To accomplish this, we first explored the effect of the sodium channel blocker tetrodotoxin (TTX) on basal and stimulated immunoreactive CRH (iCRH) secretion by explanted rat hypothalami. In contrast to procaine and lidocaine, TTX inhibited rather than stimulated iCRH secretion. Moreover, TTX inhibited lidocaine-induced iCRH secretion but had no influence on the response of the CRH neuron to procaine. To explore other potential mechanisms of action, we examined the effect of the calcium channels blocker verapamil and of pharmacologic antagonists to serotonergic, alpha-adrenergic and cholinergic receptors. The latter was particularly of interest because of structural similarities between procaine or lidocaine and acetylcholine (ACh) and because it has been shown that these anesthetic agents interact with the ACh receptor. Verapamil and blockade of serotonergic, alpha-adrenergic and cholinergic receptors did not inhibit the effects of procaine or lidocaine on iCRH secretion, whereas both GABA and dexamethasone exerted inhibitory effects.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1981

Reversible blockade of myelinated and non-myelinated cardiac afferents in cats by instillation of procaine into the pericardium.

Pericardial local anaesthesia was instituted in 33 chloralosed cats through catheters implanted into the pericardium. The activity of 1531 single fibres teased from either vagus in the neck was identified and classified according to source. Random testing with 2% procaine instilled into the pericardium revealed that only cardiac afferents could be blocked. Arterial and other receptors were unaffected. Blocking concentrations were determined for 38 non-myelinated cardiac afferents (mean conduction velocity 1.3 m.s-1) and for 43 myelinated fibres (mean conduction velocity 19 m.s-1). Blocking concentrations varied widely but equally for both fibre categories between 0.05% and 2.0% procaine. Non-myelinated fibres required a mean concentration of 0.26% procaine for block, whereas myelinated fibres needed a mean concentration of 0.45% (P less than 0.01). The large overlap in the frequency distributions of the blocking concentrations for both sets of fibres, would not, however, allow the blocking of one fibre category without affecting the other. Additionally two cardiac sympathetic afferents were blocked at 0.25 and 0.5% procaine. Mean times for block onset and recovery for non-myelinated fibres were 3.05/1.98 min and for myelinated fibres 1.4/0.59 min, respectively. Pericardial local anaesthesia is selective for cardiac afferents but does not allow for differential block of a given fibre category. A 1% solution of procaine will eliminate the heart as a reflexogenic area.

Animals↗
PubMed1994

Alteration of autonomic influence on left ventricular contractility by epicardial superfusion with hexamethonium and procaine.

OBJECTIVE: Since portions of autonomic nerves and receptors are located superficially on the heart, it is possible that neuromodulatory substances in pericardial fluid may modulate cardiac contractile function by altering autonomic neurotransmission. The aim of the study was to examine this hypothesis in anaesthetised dogs instrumented to measure left ventricular pressure and volume (conductance catheter). METHODS: The effects of electrical stimulation of cardiac sympathetic efferents in the ansa subclavia (n = 6), or parasympathetic efferents in the vagus (n = 6), on left ventricular contractility were evaluated during epicardial superfusion with Tyrode solution, or Tyrode solution containing hexamethonium (1 x 10(-4) M), or procaine (2%). The slope of the end systolic pressure-volume relationship (Ees), a load independent measure of left ventricular contractility, and the position of the relationship (Vmid) were obtained by rapid transient vena caval occlusion. RESULTS: Ansa subclavia stimulation increased Ees from 4.8(SD 1.8) to 8.3(3.0) mm Hg.ml-1 (p < 0.05), and Vmid shifted to the left, from 9(10) to 0(16) ml (p < 0.05). This response was abolished by epicardial superfusion with procaine, but not with hexamethonium. Vagal stimulation decreased Ees from 13.3(7.4) to 6.3(4.2) mm Hg.ml-1 (p < 0.05) and Vmid shifted to the right, from 12(10) to 18(8) ml (p < 0.05). These changes were abolished by both procaine and hexamethonium. Procaine did not affect the positive inotropic response to intravenous noradrenaline nor the cardiac depressor response to intravenous methylcholine, indicating that the myocardial contractile response was intact during epicardial superfusion with procaine. CONCLUSIONS: Neuromodulatory substances in the pericardial space may alter left ventricular contractility by modifying cardiac efferent autonomic neurotransmission on the epicardial surface of the heart.

Animals↗
PubMed1984

Haemodynamic effects of intravenous procaine as a supplement to general anaesthesia in patients with valvular heart disease.

The effect of intravenous procaine, 2 mg/kg/min, on the cardiovascular function of nine patients scheduled for cardiac valve replacement was studied under enflurane-pancuronium anaesthesia. Procaine infusion was started after intubation during steady-state anaesthesia, and continued until start of cardiopulmonary by-pass. Systemic vascular resistance decreased steadily from 198.2 +/- 28.7 to 133.0 +/- 17.2 kPa X s/l (P less than 0.05). A simultaneous decline in mean arterial pressure from 10.13 +/- 0.68 to 7.47 +/- 0.48 kPa was observed (P less than 0.01). Cardiac index, heart rate, central venous pressure, pulmonary arterial mean pressure and pulmonary capillary wedge pressure were all unaffected by procaine as well as by surgical stimulation. It is concluded that continuous procaine infusion as an adjuvant to general anaesthesia effectively abolishes the hypertensive and tachycardiac response to surgical stimulation. The limiting factor in the amount of infused procaine appears to be the hypotension caused by vasodilation, not myocardial depression or convulsions.

Adjuvants, Anesthesia↗
PubMed1984

Some effects of procaine at the toad end-plate are not consistent with a simple channel-blocking model.

Miniature end-plate currents (m.e.p.c.s) were recorded extracellularly from toad sartorius muscle fibres exposed to solutions containing procaine at pH 5.4, 7.4 and 9.9. The decay phase of m.e.p.c.s was analysed to determine whether the effects of procaine were consistent with a sequential channel-blocking model. Averaged m.e.p.c.s measured in the presence of procaine were biphasic, decaying as the sum of two exponential components. However, about 10-15% of m.e.p.c.s decayed as single exponentials and were not biphasic. At pH 9.9 the relative amplitudes of the fast and slow phases were generally consistent with the decay time constants, according to the predictions of the blocking model. Such a correlation was not found at pH 5.4 or 7.4. In addition, the rate of decay of m.e.p.c.s at pH 5.4 did not increase as predicted with procaine concentration. These results demonstrate that the sequential blocking model is unable to account for all of the effects of procaine on m.e.p.c. decay. In addition, the finding that some m.e.p.c.s are single exponentials, while most are biphasic, suggests a heterogeneity of receptor-channel complexes.

Animals↗
PubMed1981

Selective inhibition of carbohydrate transport by the local anesthetic procaine in Escherichia coli.

Maltose and lactose transport systems have been used to investigate the action of procaine on insertion and activity of membrane proteins and translocation of exported proteins in Escherichia coli. Procaine mildly inhibited growth on lactose. The level of inhibition was consistent with the small reduction observed in active and facilitated transport functions of the lac permease. However, procaine caused a severe reduction of growth rate on maltose, as well as an inhibition of induction of maltose regulon activities. In both constitutive and inducible strains, the synthesis of both maltose transport activity (malB operon) and amylomaltase activity (malA operon) was inhibited. Coordinate inhibition of soluble and membrane products was not observed with the lac operon. beta-Galactosidase synthesis proceeded normally during growth on procaine, whereas, the appearance of new transport activity was reduced. Regardless of carbon source, procaine specifically inhibited the appearance of ompF protein in the membrane fraction.

Bacterial Outer Membrane Proteins↗
PubMed1991

Cardiac nerve blockade by infusion of procaine into the pericardial space of conscious dogs.

A technique was developed to produce acute, reversible cardiac nerve blockade (CNB) in the conscious dog by infusion of 2% procaine into the pericardial (PC) space. During CNB, reflex changes in heart rate (HR) in response to intravenous bolus injections of phenylephrine (100 micrograms) and nitroglycerin (300 micrograms) and the reflex tachycardia and hypotension after a 50-micrograms bolus injection of veratridine into the left atrium were abolished. In response to CNB, HR increased from 79 +/- 10 to 142 +/- 10 beats/min and mean arterial pressure (MAP) increased from 101 +/- 5 to 117 +/- 6 mmHg. Baseline values for plasma arginine vasopressin (AVP), plasma renin activity (PRA), and plasma norepinephrine (NE) were unchanged by CNB, but there was a small increase in plasma cortisol levels (1.4 +/- 0.3 to 2.3 +/- 0.3 micrograms/dl) during CNB. There was no significant change in the baseline levels of any of these hormones during PC infusion of 0.9% saline. To control for the possibility that procaine leaked into the systemic circulation, identical amounts of procaine were infused intravenously. Systemic administration of procaine caused a rise in MAP but had no effect on HR and did not alter plasma levels of AVP, PRA, NE, or cortisol. The relationship between plasma osmolality and plasma AVP, as well as the drinking response to a 60-min infusion of hypertonic NaCl, was unaltered by CNB. We conclude that PC procaine infusion is an effective technique for producing acute, reversible blockade of the cardiac nerves in the conscious dog.

Animals↗
PubMedDate not supplied

Effects of lidocaine and procaine on canine nasal blood vessels.

The effects of lidocaine and procaine on contractile responses of isolated canine nasal mucosal blood vessels to field stimulation and methoxamine were investigated. Analysis of cumulative dose-response curves showed that the two local anesthetics antagonized methoxamine and inhibited the field-stimulation response. The latter effect was interpreted as due to the blockade of Na+ channels. This would inhibit nerve conduction induced by field stimulation. The former effect on methoxamine is probably caused by the effect of these anesthetics on the mobilization of Ca++ needed for smooth muscle contraction. Preincubation of the nasal mucosa with low doses of procaine or lidocaine shifts the methoxamine dose-response curve to the right. With higher doses, the maximal response is also reduced. The shift of the dose-response curve showed that procaine or lidocaine can change the alpha-adrenergic receptor affinity. Commercial 1% lidocaine with 1:100,000 epinephrine also inhibits field stimulation and antagonizes methoxamine contractions. Lidocaine can increase the basal tone of nasal mucosa, while procaine cannot. From these results, we conclude that procaine and lidocaine have common mechanisms in blocking Na+ channels but differ in their ability to modify Ca++ stores or channels.

Animals↗
PubMedDate not supplied

Intravenous procaine as a supplement to general anesthesia for carbon dioxide laser resection for carbon dioxide laser resection of laryngeal papillomas in children.

Procaine suppresses the cough reflex, decreases laryngeal irritability, and has general anesthetic properties. For these reasons, 14 pediatric patients undergoing CO2 laser resection of laryngeal papillomas were studied in which an intravenous infusion of procaine (1 mg/kg/min) was added to N2O-O2 halothane/enflurane general anesthesia immediately following endotracheal intubation. These patients were compared to nine patients receiving the same anesthesia without procaine. The mean age of both groups was 11 years. There was no difference between the groups in duration of anesthesia or surgery. Emergence, however, averaged 15 minutes in study patients compared to 36 minutes in the control group (p less than 0.01). There was no difference in anesthetic concentrations required to maintain satisfactory operative conditions in the two groups. Muscle relaxants were required intraoperatively in seven control patients but in none of the study patients. The surgeon ranked the operative conditions excellent in all study patients but poor in seven of the nine control patients. Five of the latter required postoperative treatment of laryngeal complications, including reintubation in three. Only one of the study patients had postoperative stridor. No evidence of procaine toxicity was noted in the study patients with total doses ranging from 500--3600 mg. Intravenous procaine is useful in pediatric patients having endoscopic laryngeal operations.

Anesthesia, Inhalation↗
PubMed2005

Spinal 2-chloroprocaine: a comparison with procaine in volunteers.

Recent studies using preservative-free 2-chloroprocaine (2-CP) for spinal anesthesia have shown it to be a reliable short-acting drug that provides similar anesthesia to lidocaine. In this randomized, double-blind, crossover study, we compared the characteristics of spinal 2-CP (30 mg) with those of procaine (80 mg) in eight volunteers to determine whether either drug produces spinal anesthetic characteristics ideal for outpatient surgery. By using sensation to pinprick, transcutaneous electrical stimulation, tolerance to thigh tourniquet, and motor blockade as surrogates for surgical efficacy, 2-CP compared similarly to procaine. Peak block height (T9 [range, T6 to T12] versus T6 [T4 to T8]; P = 0.0796), time to two-segment regression (51 +/- 17 min versus 53 +/- 10 min; P = 0.7434), tourniquet time tolerance (37 +/- 16 versus 49 min +/- 17 min; P = 0.1755), and time to return of motor strength (Bromage scale: 54 +/- 23 min versus 55 +/- 44 min, P = 0.9366; return of 90% quadriceps strength: 78 +/- 9 min versus 98 +/- 30 min; P = 0.0721) were all similar. Procaine did produce overall longer sensory blockade (P = 0.0011) and motor blockade at the gastrocnemius (P = 0.0004) and quadriceps (P = 0.0146) muscles. Times until the resolution of sensory blockade (103 +/- 12 min versus 151 +/- 26 min; P = 0.0003), ambulation (103 +/- 12 min versus 151 +/- 26 min; P = 0.0003), and micturition (103 +/- 12 min versus 156 +/- 23 min; P < 0.0001) were all prolonged after procaine. In conclusion, at the doses tested, spinal 2-CP (30 mg) may be a better choice for short outpatient procedures because it provides anesthesia with similar efficacy as procaine (80 mg) but with more rapid fulfillment of discharge criteria.

Adult↗
PubMed1981

Comparison of the chronotropic responses to local anesthetics (procaine, lidocaine, prilocaine, mepivacaine and bupivacaine) of the canine sinus node in situ.

Effects of local anesthetics (procaine, lidocaine, prilocaine, mepivacaine and bupivacaine) on the sinus node of the nerve-intact dog heart were studied in situ by means of selective perfusion of the sinus node through the sinus node artery. The agents caused a dose-dependent decrease in heart rate and the order of their potency in decreasing the heart rate was as follows, bupivacaine greater than lidocaine=mepivacaine=prilocaine greater than procaine. The decrease in heart rate produced by these local anesthetics was not affected by prior administration of atropine. With procaine and prilocaine, the decrease in heart rate was followed by an increase which was inhibited by propranolol given into the sinus node artery or was suppressed in reserpine-pretreated dogs. Tetrodotoxin also prevented the positive chronotropic effect of procaine. From these results the following conclusion can be drawn: the negative chronotropic effects of these agents are induced mainly by a direct inhibitory action on the sinus node, and partly by blockade of sympathetic tone, and the interaction with the postganglionic adrenergic nerves plays an important role in the induction of the positive chronotropic responses to procaine and prilocaine.

Anesthetics, Local↗
PubMed1982

Dual effects of tetrachlorvinphos on procaine toxicity and procainesterase activity in rats.

The effect of tetrachlorvinphos (TCVP) on liver procainesterase (PROCase) and procaine toxicity was studied in rats. TCVP is an organophosphate with an inducible effect on drug metabolizing enzymes. A single oral dose of 500 mg/kg of TCVP caused a remarkable decrease in PROCase (40% of control) 24 hr later and increased the motality after injection of procaine (250 mg/kg, i.p.) from 54% to 87%. Conversely, it was observed that PROCase elevated to 140% of the control and mortality decreased from 54% to 25% on day 3. With repeated administration of TCVP (500 mg/kg/day) for 5 days, the PROCase activity that was inhibited on day 1 was gradually restored to normal levels by 5 days and the mortality altered to 25%. The inducible effect on PROCase was examined using desmethyl-TCVP, a metabolite of TCVP without inhibitory effect on the enzyme; PROCase activity was enhanced to 1.6-fold of the control and procaine concentration in the brain was reduced to 30% of the control, accompanied with no death of rats after procaine injection. Electrophoresis of the solubilized liver microsomal fraction confirmed the inducible effect of TCVP on PROCase; microsomal protein from the TCVP-treated rat was more deeply stained than that from the control, and the PROCase activity of two anodic bands increased in the TCVP-treated microsomes. These results indicate that TCVP has a dual action on PROCase, inducible and inhibitory, and that the direct inhibitory effect of TCVP might mask the increased amount of the enzyme induced by repeated administration of TCVP. The dual effect of TCVP on PROCase would cause the change in procaine toxicity.

Animals↗
PubMed1996

Kinetics of the inhibition of acetylcholinesterase from desert cobra (Walterinnesia aegyptia) venom by local anesthetics: procaine and tetracaine.

The kinetic parameters of W. aegyptia venom acetylcholinesterase (AChE) inhibition by procaine and tetracaine hydrochloride were investigated in the present study. Procaine and tetracaine reversibly inhibited the AChE activity in a concentration-dependent manner, the IC50 being about 0.28 and 0.04 mM, respectively. The Michaelis-Menten constant (K(m)) for the hydrolysis of acetylthiocholine iodide was found to be 0.051 mM with Vmax 10.2 mumole/min/mg protein. Both K(m) and Vmax were affected by procaine while only Vmax decreased with tetracaine. A Lineweaver-Burk plot and its secondary replot indicated that the nature of the inhibition is of the linear mixed type for procaine which is considered to be a mixture of competitive and noncompetitive types while the inhibition was noncompetitive for tetracaine. The values of Ki(slope) and K(intercept were estimated as 0.133 mM and 0.451 mM for procaine and 7.2 x 10(-3) mM for tetracaine, respectively, by the secondary replots of the Lineweaver-Burk plot.

Acetylcholinesterase↗