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PubMed1999

Spinal procaine with and without epinephrine and its relation to transient radicular irritation.

PURPOSE: To document the clinical characteristics of procaine with or without the addition of epinephrine. METHODS: In this randomized, prospective, double blind study, 62 patients received spinal anesthesia with 100 mg procaine and either 0.3 mg epinephrine (EPI group) or 0.3 ml NaCl 0.9% (SALINE group). Sensory anesthesia to needle prick was evaluated q 1 min for 10 min, q 3 min for 33 min and q 5 min until regression to L4. Motor block was assessed with the Bromage scale. Patients were questioned, by telephone, for transient radicular irritation (TRI) 48 hr later. RESULTS: Time to reach highest sensory level and number of segments blocked showed no difference. Mean time for regression of the sensory level to T10 was longer in EPI (83 +/- 23 vs 66 +/- 20 min, P < 0.01). Time to recuperate to full flexion of knees and feet (Bromage 4) was longer in EPI (126 +/- 37 vs 100 +/- 30 min, P < 0.01). Patients in EPI received more ephedrine. Eighteen patients had nausea (15 EPI/3 SALINE, P < 0.0015). One patient had TRI, incidence: 1.67%, 95% CI (< 1%-9%). CONCLUSION: Spinal procaine is appropriate for surgery of short duration. Epinephrine prolongs sensory and motor blocks by 25%. However, it is associated with a high incidence of nausea.

Adult↗
PubMed2001

Spinal anesthesia: a comparison of procaine and lidocaine.

PURPOSE: To compare spinal procaine to spinal lidocaine with regard to their main clinical characteristics and incidence of transient radicular irritation (TRI). METHODS: In this randomized, double-blind, prospective study, patients (two groups, n=30 each) received either 100 mg of lidocaine 5% in 7.5% glucose (Group L) or 100 mg of procaine 10% diluted with 1 ml cerebrospinal fluid (Group P). After spinal anesthesia, segmental level of sensory block was assessed by pinprick. Blood pressure and the height of the block were noted each minute for the first ten minutes, then every three minutes for the next 35 min and finally every five minutes until regression of the block to L4. Motor blockade was evaluated using the Bromage scale. To evaluate the presence of TRI, each patient was questioned 48 hr after surgery. RESULTS: Time to highest sensory level and to maximum number of segments blocked showed no difference between groups. Mean time for sensory regression to T10 and for regression of the motor block were shorter in Group P. Eighty minutes following injection, sensory levels were lower in Group P. Five patients had inadequate surgical anesthesia in Group P and only one in Group L. No patient in Group P had TRI (95% CI 10-12%) while eight (27%) in Group L did (95% CI 12-46%). CONCLUSIONS: Procaine 10% was associated with a clinical failure rate of 14.2%. This characteristic must be balanced against an absence of TRI, which occurs more frequently with the use of lidocaine 5%.

Adult↗
PubMed1998

A comparison of procaine penicillin with sulbactam-ampicillin in the treatment of peritonsillar abscesses.

The clinical efficacy of procaine penicillin and sulbactam-ampicillin was compared in patients with peritonsillar abscesses after peroral abscess drainage. Forty-two patients were randomly assigned to receive either procaine penicillin or sulbactam-ampicillin intramuscularly on an outpatient basis. The mean time required for clinical symptoms (throat pain, dysphagia and fever) to resolve was compared. No statistically significant difference was found between the clinical recoveries of patients using either antibiotic (P > 0.05). The authors conclude that intramuscular procaine penicillin can be safely prescribed on an outpatient basis to most patients with peritonsillar abscess after incision and drainage. In contrast, a broader spectrum and more expensive antibiotic, such as sulbactam-ampicillin, should be reserved for non-responders.

Adult↗
PubMed1979

Reappraisal of intravenous procaine as a short-acting anesthetic adjuvant.

Our data in 74 patients demonstrate that procaine hydrochloride is a safe anesthetic adjuvant in doses of 1 mg/kg/min even when total doses are 5 to 7 g. Blood pressure, heart rate, electrocardiographic variables, and blood gases were not adversely affected. Patients had no nausea or untoward postanesthesia symptoms. Emergence from anesthesia was rapid, within less than 15 minutes in all patients, and most were fully awake before leaving the operating room. In two patients in whom blood levels were studied the drug disappeared within 40 minutes. Procaine is inexpensive, $1.16 for 10 g, and it is not a known liver or kidney toxin. Until studies on cardiovascular dynamics and analgesic effects as in whom a low plasma cholinesterase activity is present or suspected. The clinical appraisal in 56 patients indicates its usefulness in suppressing premature venticular contractions and cough reflexes during endoscopic procedures in the respiratory tract. Procaine can be used to advantage in supplementing general anesthesia in outpatient surgery because of its brief action. For these reasons, the drug merits further study.

Adolescent↗
PubMed1990

A comparative study of the effects of procaine, lidocaine, tetracaine and dibucaine on the functions and ultrastructure of isolated rat liver mitochondria.

The effects of procaine, lidocaine, tetracaine and dibucaine (10(-5) - 10(-2) M) were tested on isolated rat liver mitochondria by measurements of the respiratory rates and of the membrane potential and by electron microscopy. A general concentration-dependent stimulation of the basal state (respiration before ADP addition) was observed for all local anesthetics studied. Up to the concentration of 10(-3) M, the order of stimulation was: procaine less than lidocaine less than dibucaine less than tetracaine. However, with the exception of dibucaine, which inhibited state-3 respiration (ADP present) in a strictly concentration-dependent manner, the other drugs had a biphasic effect: slight stimulation of state 3 at low and moderate concentrations (less than or equal to 10(-3) M) and inhibition at higher concentrations. Nevertheless, due to a stronger stimulation of the basal state, the acceptor control ratio decreases progressively (uncoupling effect) as the concentration of the drugs increases. The only exception to this observation is procaine in the range of 10(-5) - 10(-4) M, where the stimulation of the two respiration states (although small) is approximately equal and thus the uncoupling effect is absent or negligible. Membrane potential recordings suggested that membrane integrity and phosphorylation capacity were negatively affected at high drug concentrations (greater than 10(-3) M), especially in the case of tetracaine and dibucaine, when 5 x 10(-3) M even produced the collapse of the membrane potential and complete loss of the phosphorylation ability. Electron microscopy confirmed these effects, showing an abundance of either swollen or supercondensed mitochondria, with many membrane ruptures. The action mechanisms of the tertiary amines studied are discussed in terms of interaction of drug with the lipid bilayer and with the membrane proteins. It is concluded that both the inhibitory and the uncoupling effects are dependent, in the first place, on the degree of hydrophobicity of each local anesthetic.

Animals↗
PubMed1981

Location and effect of procaine on lecithin/cholesterol membranes using X-ray diffraction methods.

X-ray diffraction studies were made on lecithin/cholesterol multilayers with very high water content and containing the local anaesthetic procaine. Narrow-angle diffraction experiments show that the procaine molecules are located with the uncharged aromatic amine group approx. 10 A from the centre of the bilayer. The polar tertiary amine group of these molecules is almost certainly located in the polar head-group region of the membrane. Wide-angle diffraction experiments show that the incorporation of procaine molecules into such lipid membranes produces an approx. 30% increase in the spread of acyl chain separation, although the average spacing between the chains is slightly reduced.

Chemical Phenomena↗
PubMed1987

Locations and dynamical perturbations for lipids of cationic forms of procaine, tetracaine, and dibucaine in small unilamellar phosphatidylcholine vesicles as studied by nuclear Overhauser effects in 1H nuclear magnetic resonance spectroscopy.

Locations and dynamical perturbations for lipids of local anesthetics (procaine . HCl, tetracaine . HCl, and dibucaine . HCl) in sonicated egg yolk phosphatidylcholine (PC) vesicles have been studied by 1H-1H nuclear Overhauser effect (NOE) measurements. It was found that tetracaine and dibucaine bind much strongly to the neutral lipids than does procaine and that their mobilities are lowered to such an extent that spin diffusion is transmitted (i.e., omega 2 tau c2 much greater than 1). The intermolecular NOEs between drugs and PC were more effective in the case of dibucaine than with tetracaine, indicating that dibucaine binds to the lipids more strongly than tetracaine; this order agrees well with that of anesthetic potency. However, it was only tetracaine that gave any appreciable dynamical perturbation to the PC vesicles when they were monitored by the extent of transfer of the negative NOE from alpha-methylene protons to choline methyls, olefinic methines, acyl methylenes and terminal methyl protons. This finding was interpreted as being due to the differences in the locations of these drugs in small unilamellar vesicles: (1) procaine interacts with lipids very weakly at the outer surface of the vesicles; (2) tetracaine binds to the lipids both at the outer and inner halves of the bilayer, inserting its rod-like molecule in a forest of acyl chains of PC; (3) dibucaine binds tightly to the polar head-group of PC, which resides only at the outer half of the bilayer vesicles. It was concluded that the relative order of anesthetic potency within these drugs can be correlated not with the ability to affect membrane fluidity but with the ability to bind to lipids at the polar head-group of the bilayer vesicles.

Cations↗
PubMed1988

Electrophysiological effects of cocaine and procaine on dorsal raphe serotonin neurons.

The effects of cocaine and procaine on the spontaneous activity of serotonin (5-hydroxytryptamine, 5-HT) neurons in the dorsal raphe nucleus of the chloral hydrate anesthetized male rat were characterized using extracellular single-unit and microiontophoretic recording techniques. Intravenous cocaine elicited a potent, dose-dependent inhibition of 5-HT cell firing with a cumulative dose to 50% inhibition of cell firing of 0.66 +/- 0.11 mg/kg (means +/- S.E.M.; N = 17). In contrast, systemic administration of the local anesthetic procaine did not significantly alter cell firing in cumulative doses up to 16 mg/kg (N = 10). Microiontophoretic application of cocaine, but not procaine, also depressed spontaneous cell firing of 5-HT-containing neurons and potentiated the inhibitory effects of 5-HT in the dorsal raphe nucleus. The depressant effects on 5-HT neurons following systemic or microiontophoretic application of cocaine may result from autoinhibition of 5-HT neurons, presumably as a consequence of cocaine-induced 5-HT reuptake inhibition.

Animals↗
PubMed1988

Effect of procaine injection into the ventromedial hypothalamic area (VMH) of the rat on serum insulin, glucose and corticosterone and gastric emptying rate.

Bilateral injection of procaine into the VMH resulted in a decrease in serum glucose and immunoreactive insulin levels in both food-deprived rats and meal-fed rats. Corticosterone levels and gastric emptying rate were unaffected by these VMH procaine injections. Since it is likely that the procaine disrupted only those neurons whose cell bodies and synapses lay in the region of the VMH, the results suggest that the two major factors in the etiology of the 'VMH syndrome' following electrolytic lesions, rapid emptying and insulin hyperresponsivity, are dependent upon destruction of fibers of passage through the VMH. Finally, the results further support the proposal that the VMH exerts tonic excitatory control over liver glucose output.

Animals↗
PubMed1995

Effect of intramedullary procaine injection on tracheal tone and phrenic neurogram.

To map the superficial locations which are involved in the control of respiration and tracheal smooth muscle tone in ventrolateral medulla, we examined the effects of local anesthesia on phrenic activity and tracheal tone in twelve anesthetized, paralyzed, and artificially ventilated dogs. 0.5 microliter of 5% procaine was injected 0.3 to 0.5 mm below the surface unilaterally to the ventral superficial layer (from the rostral part of the trapezoid body to the caudal hypoglossal rootlets and lateral from the pyramids to 5.5 mm from the midline), which included rostral, intermediate and caudal areas, and the area lateral to the hypoglossal rootlets. The peak amplitude of the integrated phrenic neurogram was decreased by procaine injection to the intermediate area and the area lateral to the hypoglossal rootlets. Tracheal tone decreased only by procaine injection to the intermediate area. In the intermediate area, some injections decreased either phrenic output alone or tracheal tone alone. These results suggest that the two ventral medullary areas, i.e. the intermediate and caudolateral parts, contain neural structures which are involved in the shaping of phrenic output, but only the intermediate area is involved in the regulation of tracheal tone. It is also suggested that, in the intermediate area, the structures responsible for the maintenance of respiration and tracheal tone are, at least in part, separable.

Animals↗
PubMed1986

Metabolism of aspirin and procaine in mice pretreated with O-4-nitrophenyl methyl(phenyl)phosphinate or O-4-nitrophenyl diphenylphosphinate.

Concentrations of [carboxyl-14C]procaine in blood of mice were increased threefold for 27 min by exposure to O-4-nitrophenyl diphenylphosphinate 2 hr prior to [carboxyl-14C]procaine injection ip, while there was no effect of O-4-nitrophenyl methyl(phenyl)phosphinate pretreatment. There was no effect of either organophosphinate on the primary hydrolysis of [acetyl-l-14C]aspirin when assessed by the expiration of [14C]carbon dioxide; however, O-4-nitrophenyl diphenylphosphinate pretreatment produced transient increases in blood concentrations of both [carboxyl-14C]aspirin and [carboxyl-14C]salicylic acid following administration of [carboxyl-14C]aspirin. Liver carboxylesterase activity in O-4-nitrophenyl diphenylphosphinate pretreated mice was 11% of control activity. These results indicate the potential for drug interaction with O-4-nitrophenyl diphenylphosphinate but not with O-4-nitrophenyl methyl(phenyl)phosphinate. It appears that liver carboxylesterase activity has a minor role in hydrolysis of aspirin in vivo, but may be more important in procaine metabolism.

Animals↗
PubMed1986

Reversible disruption of lordosis via midbrain infusions of procaine and tetrodotoxin.

Behavioral effects of bilateral intracranial infusions of tetrodotoxin (1, 3.3 or 10 ng/rat), 50% procaine (2 microliters/rat) or phosphate-buffered saline (PBS-2 microliters/rat) into the dorsal midbrain of conscious, lightly-restrained female rats were evaluated. High levels of lordotic responsiveness were induced in ovariectomized animals treated with estradiol (E2) capsules or subcutaneous injections of estradiol benzoate (EB) followed by progesterone (P). The effect of each of the 3 infusates on lordosis was determined using manual stimulation and lordosis quotient determinations. In addition, the vocalization by an animal during lordosis measurements, paw withdrawal to pinch, righting reflex latency and recognition of a platform edge were also monitored. Within 2 minutes following procaine or tetrodotoxin (TTX) infusions in E2 implanted rats, lordotic responsiveness declined sharply. Whereas procaine-treated animals returned to control levels of responsiveness within 20 minutes, TTX infusions induced a more prolonged depression of lordosis lasting up to 8 hours. Infusions of PBS had no effect on any of the behaviors. In a separate group of animals treated with either E2 or EB + P and infused with 10 ng TTX the time course of the decline in lordotic responsiveness was identical for both steroid treatments. Paw withdrawal was unaffected by TTX while all other measured behaviors were disrupted along the same time course as lordosis. Collectively the above results implicate the requirement of sodium-dependent neuronal activity within dorsal midbrain for the maintenance of the lordosis reflex, along with other behavioral responses influenced by this brain region.

Animals↗
PubMed1990

Differential effects of atropine, procaine and dopamine in the rat ventral tegmentum on lateral hypothalamic rewarding brain stimulation.

Microinjections of the muscarinic antagonist, atropine, of dopamine, or of the local anesthetic, procaine, in the ventral tegmentum elevated frequency thresholds for lateral hypothalamic self-stimulation. The largest and most robust effects were observed following atropine (30 or 60 micrograms) microinjections. The most sensitive sites for the atropine effect were near dopamine cells. In order to determine if the effects of atropine can be reversed by pretreatment with a cholinergic agonist, carbachol (1-3 micrograms) was microinjected 15 min prior to atropine. Carbachol pretreatment attenuated the frequency threshold elevation of atropine by 47-95%. Since atropine is a local anesthetic, the effects of procaine on self-stimulation thresholds were tested as well. Procaine (100 or 250 micrograms) in ventral tegmentum elevated frequency thresholds by much less than atropine. Therefore, while atropine attenuates reward primarily through blockade of muscarinic receptors, the local anesthetic effect of atropine may enhance the threshold elevation. Dopamine (1-10 micrograms) also elevated frequency thresholds, but when dopamine injections were repeated daily, the threshold elevations were attenuated. This attenuation contrasted with the robust effects of atropine, and may reflect the development of autoreceptor subsensitivity. Hence, both dopaminergic and muscarinic receptors in ventral tegmentum are involved in lateral hypothalamic brain stimulation reward.

Animals↗
PubMed1989

Selective procaine inhibition of rat chorda tympani responses to electric taste stimulation.

1. The lingual treatment of 1% procaine for 10 min selectively suppressed responses of the rat chorda tympani nerve to anodal current applied to the tongue with NaCl in the bathing medium to about 50% of control but the drug produced no significant suppression in responses to chemical taste stimuli. 2. The magnitude of suppression of response to anodal current varied with concentration of procaine and kind of bathing medium for the current stimulation (larger in the order of NaCl greater than KCl greater than CaCl2 greater than HCl). 3. Such ion specificity in procaine suppression suggests that responses of the chorda tympani nerve to anodal current are provoked through the taste cell (not direct action on the taste nerve), and that the receptor mechanisms for anodal current are at least partly different from that for chemical taste stimuli.

Animals↗
PubMed1987

Effects of procaine and caffeine on the contractility of enzymatically isolated myocytes and intact cardiac tissue.

1. Procaine and caffeine exerted opposite effects on the contractility of rat cardiac tissue. 2. Procaine enhanced and caffeine depressed isometric contractile force of right ventricular strips. 3. In enzymatically isolated cells, caffeine increased the frequency and decreased the amplitude of spontaneous contractions, while procaine retarded the beating rate but concomitantly raised the shortening amplitude of the myocyte. 4. Both drugs depressed the propagation velocity of the contractile waves. 5. The results are suggested to be due to the opposite effects of the two drugs on the Ca-release process of the sarcoplasmic reticulum.

Animals↗
PubMed1982

A potent, structurally specific stimulant action of procaine in bullfrog lung.

1. Local anesthetics with a procaine-like structure are exceptionally potent smooth muscle stimulation in Rana catesbeiana. 2. Procaine completely reverses the relaxant effect of 1 mM theophylline, an action that cannot be duplicated with carbachol, histamine or 5-hydroxytryptamine. 3. Stimulant activity is related to the procaine-like structure rather than local anesthetic potency, and is independent of pH between 7.0 and 8.4. 4. The high potency and structural specificity of this effect suggests an action at a specific receptor site rather than a diffuse action on membrane structure.

Acetylcholine↗
PubMed1989

Stopped-flow determination of procaine hydrochloride in pharmaceutical preparations.

A stopped-flow photometric method for the quantitative determination of procaine hydrochloride is proposed. It is based on the measurement of the rate of formation of a coloured product between procaine and sodium 1,2-naphthoquinone-4-sulphonate. The conversion of an equilibrium method to a kinetic method by the stopped-flow technique results in an improved detection limit and linear range, and in considerably increased sample throughput. A simple modular stopped-flow system has been used for this purpose. The results obtained on application of this method to the determination of procaine in various pharmaceutical preparations, show the suitability of the stopped-flow technique for routine pharmaceutical analyses.

Calibration↗
PubMedDate not supplied

A selective and sensitive kinetic method for the determination of procaine and benzocaine in pharmaceuticals.

A simple stopped-flow method for the determination of procaine and benzocaine which is suitable for their routine analysis in pharmaceutical samples is reported. The method is based on a condensation reaction between each compound and 4-dimethylaminocinnamaldehyde, which yields coloured compounds and which are monitored spectrophotometrically. The calibration graph generated is linear over the range 0.5-20 micrograms ml-1 (RSD 0.73%) for procaine and 0.5-15 micrograms ml-1 (RSD 0.40%) for benzocaine, and the selectivity is very high in both cases. The proposed methods were satisfactorily applied to the determination of the two drugs in various pharmaceutical samples. A procedure for resolution of procaine-benzocaine mixtures in mass ratios between 15:1 and 1:7 with a precision of ca 1% was developed in order to determine one compound in the presence of the other with no interference.

Benzocaine↗