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At least 19 recordsLinked to original sources
PubMed1975

Determination of procaine and related local anesthetics. I. Partition chromatographic separation and assay of mixtures of procaine with tetracaine and with propoxycaine.

Determination of ionization and extraction constants for procaine, tetracaine, and propoxycaine led to selection of a simple partition chromatographic system for separation and assay of mixtures of these anesthetics. A 65% solution of chloroform in isooctane elutes tetracaine or propoxycaine from a pH 4:sodium bromide column; procaine is retained and subsequently eluted by chloroform as the bromide ion-pair. The anesthetics are then determined spectrophotometrically. Results of assay of standard and commercial formulations are presented.

Anesthetics, Local↗
PubMed1975

Determination of procaine and related local anesthetics. II. Collaborative study.

The ion-pairing chromatographic method reported previously for the isolation and spectrophotometric determination of the local anesthetics, alone and in combination, was studied collaboratively. Three solutions were assayed. One containing procaine as the single active component gave an average recovery of 99.8 plus or minus 1.7%. A mixture of procaine and tetracaine gave results of 99.3 plus or minus 1.6 and 98.9 plus or minus 8.82%, respectively. A third solution containing procaine and propoxycaine assayed 100.0 plus or minus 1.5 and 99.1 plus or minus 1.9%, respectively. It was shown that low results for tetracaine were due to loss during the final evaporative step. The method for samples containing tetracaine should be studied further. The other methods have been adopted as official first action.

Anesthetics, Local↗
PubMed1984

The effect of Tityus serrulatus scorpion toxin gamma on Na channels in neuroblastoma cells.

The effects of highly purified toxin gamma from the venom of the scorpion Tityus serrulatus (TiTx gamma) on nerve membrane ionic channels have been investigated using the suction electrodes voltage clamp technique on neuroblastoma cells. The amplitude of the normally voltage-dependent Na current is reversible reduced by approximately 50% after 15-105 nM TiTx gamma, whereas even the highest toxin concentrations have no significant effect on the outward K current in the presence of tetrodotoxin. TiTx gamma causes a transient inward current to appear at membrane potentials between -70 and -40 mV, a potential region in which no significant inward current is observed in control experiments. Tetrodotoxin (300 nM) rapidly blocks both the TiTx gamma-induced inward current and the remaining normally voltage-dependent Na current. The binding of radiolabelled TiTx gamma to the Na channels in the neuroblastoma cell membrane is prevented by native TiTx gamma with a K0.5 = 0.75 nM. Both activation and inactivation of the TiTx gamma-induced Na current are shifted 30-40 mV towards more negative potential values as compared to normally voltage-dependent Na current. The TiTx gamma-induced Na current exhibits sigmoidal activation kinetics and relatively slow, exponential inactivation kinetics. The local anesthetic procaine at an external concentration of 1 mM blocks more effectively the remaining normally voltage-dependent Na current than the TiTx gamma-induced Na current. Both Na current components are equally blocked by 1 mM of the local anesthetic propoxycaine. The relation between the effects of TiTx gamma on Nat channels and those of other known neurotoxins those of other known neurotoxins specific of this channel is discussed.(ABSTRACT TRUNCATED AT 250 WORDS)

Anesthetics, Local↗
PubMed1995

In vitro and in vivo effects of cocaine and selected local anesthetics on the dopamine transporter.

The effects of selected local anesthetics on in vitro and in vivo measurements of dopamine transporter activity were determined to investigate the role of local anesthetic activity in the neuronal actions of cocaine. Cocaine inhibited [3H]2-beta-carbomethoxy-3-beta-(4-fluorophenyl)tropane 1.5-naphthalenedisulfonate (CFT) binding and [3H]dopamine uptake with estimated Ki and IC50 values of 0.6 microM and 0.7 micorM, respectively. Of the local anesthetics tested, only dimethocaine showed full displacement of CFT binding (0-30 microM tested) and full inhibition of dopamine uptake (0-100 microM tested). Dimethocaine was only slightly less potent than cocaine with an estimated Ki of 1.4 micorM and an IC50 value of 1.2 microM for [3H]CFT binding and dopamine uptake. At a maximum concentration of 100 microM, the ester containing local anesthetics procaine, tetracaine, piperocaine and the amide containing local anesthetic dibucaine and bupivacaine partially inhibited dopamine uptake by 47-70%. The ester containing local anesthetic propoxycaine and the amide containing local anesthetics prilocaine, etidocaine, procainamide, and lidocaine inhibited dopamine uptake by 8-30% at 100 microM. A 10 min administration of cocaine, dimethocaine, or procaine in the dialysis solution produced dose-dependent, reversible increases in endogenous dopamine efflux from the striata of awake rats. Cocaine and dimethocaine produced similar 12-fold increases in dialysate dopamine at concentrations of 0.1 mM and 1 mM respectively. Procaine (10 mM) produced a 6-fold increase in dialysate dopamine while lidocaine (1 mM) produced a reproducible and reversible decrease (30%). These results show that the cocaine-like actions of certain local anesthetics such as dimethocaine and procaine result from their direct actions of dopamine uptake inhibitors.

Aminobenzoates↗
PubMed1983

Effects of local anesthetics on fixed-interval responding in rhesus monkeys.

Several local anesthetics of both the ester and amide type were administered IM to rhesus monkeys trained to respond on a fixed-interval 5 min schedule of food delivery. With the exception of procainamide, all local anesthetics produced dose-related decreases in response rates. Effects on pattern of responding varied between local anesthetics. With some (cocaine, dimethocaine and lidocaine), rate-dependent effects were apparent. When control rates were low, these compounds increased rates; when control rates were high, they decreased rates. However, with others (procaine, chloroprocaine, tetracaine and propoxycaine) no rate-dependent effects were noted; i.e., these compounds had little or no effect on the pattern of responding, even at doses that substantially reduced response rates. Consistent with other experiments with these compounds, cocaine was the most potent of the group. In several instances, local anesthetics which had similar stimulus properties in other behavioral paradigms differed in terms of their effects on fixed-interval behavior.

Anesthetics, Local↗
PubMed1983

A comparison in rat and mouse heart of the ability of several local anesthetics to inhibit monoamine oxidase.

Several local anesthetics were examined and compared in rat and mouse heart for MAO inhibitory action. Procaine, chloroprocaine, procainamide and tetracaine were more potent in rat than mouse heart. Piperocaine, cyclomethycaine, hexylcaine and butacaine were somewhat more potent in mouse than rat heart. Propoxycaine and dibucaine were essentially equipotent in the two tissues. Since rat heart possesses primarily type A and mouse heart primarily type B MAO, these results suggest that some local anesthetics have a preferential action on one form of the enzyme while others have a preferential action on the other. Still another group has a non-preferential action.

Anesthetics, Local↗
PubMed1979

Schirmer test after topical anesthesia and the tear meniscus height in normal eyes.

The height of the inferior tear meniscus was measured in 86 normal eyes. A value greater than 0.1 mm was obtained in 93% of the eyes that were studied. However, attempts to correlate meniscus height with subsequent Schirmer test results showed that these measurements varied randomly. Schirmer tests that were conducted on 265 eyes without instillation of 0.5% proparacaine hydrochloride and on 466 eyes with proparacaine showed that topical anesthesia reduced mean test values by 40%. When proparacaine was used prior to testing, no decrease in tear production with advancing age was demonstrated, nor were results significantly different in males and females. Schirmer test values, ranging from 0 to 3 mm, were obtained in 15% of the normal volunteers when the test was performed after instillation of topical anesthesia and after blotting of the tear lake from the inferior cul-de-sac.

Adult↗
PubMed1983

Schirmer's test. A closer look.

In 50 normal subjects, results of kinetics studies of Schirmer's test demonstrated nonlinear wetting with an initial rapid phase of wetting followed by a progressive reduction in rate. This initial rapid phase of wetting indicated a reflex secretion of tears. In the majority of subjects, topical anesthesia with 0.5% proparacaine hydrochloride dampened the initial reflex secretion but could not completely suppress it. The data indicated that Schirmer's test with anesthesia was not capable of measuring a basic tear secretion independent of reflex components.

Adult↗
PubMed1995

Alteration of pulse configuration affects the pain response during diode laser photocoagulation.

BACKGROUND AND OBJECTIVE: The shape of the treatment pulse of the diode laser (810 nm) can be easily altered electronically in contrast to ion laser photocoagulators. We investigated whether changes in laser pulse shape influenced the subjective pain responses in patients undergoing retinal photocoagulation when only topical anesthesia was used. STUDY DESIGN/MATERIALS AND METHODS: Twenty consecutive patients required peripheral retinal photocoagulation for proliferative diabetic retinopathy or extensive retinal breaks. Three diode pulse waveforms including a square wave, shaped-wave, and an envelope of micropulses were compared to one another. Power was adjusted so that each waveform delivered the same total energy. The patients subjectively ranked the intensity of any pain they experienced for each group of lesions. Responses were compared to one another using an analysis of variance. RESULTS: 40% of patients found the standard square wave pulse to be significantly more painful (P < 0.05) than the shaped pulse mode and 30% found the square wave significantly more painful (P < 0.05) than the micropulse mode. CONCLUSION: Modification of the laser pulse waveform may ameliorate pain induced by diode laser photocoagulation of the retinal periphery.

Analysis of Variance↗
PubMed1994

Comparative toxicity of tetracaine, proparacaine and cocaine evaluated with primary cultures of rabbit corneal epithelial cells.

Cocaine was first used as a topical anesthetic for the eye by Dr Carl Koller in 1884. It became evident that this agent produced erosion of the corneal epithelium in high doses or with repeated use. Synthetic local anesthetics such as tetracaine and proparacaine were developed which were more potent and less toxic than cocaine, but still produced corneal epithelium defects if used chronically. This investigation was undertaken to compare and rank the cytotoxicity of the most commonly used ocular local anesthetics, tetracaine, proparacaine and cocaine, with primary cultures of rabbit corneal epithelial cells. Cultures were exposed to either low concentrations of local anesthetics for 4-24 hr or to higher concentrations of local anesthetics for 15-120 min. Plasma membrane integrity was evaluated by measuring leakage of the cytosolic enzyme, lactate dehydrogenase, into the medium. Cell shape changes were evaluated by observing morphological changes. Mitochondrial dehydrogenase activity and cell viability were assessed by measuring 3-(4,5-dimethythiazol-2yl)-2,5-diphenyl tetrazolium bromide reduction. The cytotoxicity of the local anesthetics as evaluated by the lactate dehydrogenase leakage cytotoxicity test was ranked as follows: tetracaine (EC50 = 0.96 mM) >> proparacaine (EC50 = 4.4 mM) > cocaine (EC50 = 9.7 mM). The mitochondrial reduction assay seemed to be more sensitive than the lactate dehydrogenase leakage test in predicting toxicity: tetracaine (EC50 = 0.81 mM) >> proparacaine (EC50 = 3.4 mM) > cocaine (EC50 = 7.1 mM). When corneal epithelial cells were treated with local anesthetics, marked morphological changes occurred at concentrations that did not cause a decrease in viability. This was especially true for cocaine-treated cells. Tetracaine and proparacaine have the same anesthetic potency in vivo, although tetracaine is considered to be more irritating than proparacaine. This in vitro study showed that tetracaine was approximately four times more toxic than proparacaine. Cocaine was less toxic in vitro than proparacaine and tetracaine when compared on an equimolar basis, but in vivo it may be more toxic because of the higher concentrations that must be used to obtain the same degree of anesthesia as well as its marked effects on cell morphology.

Anesthetics, Local↗
PubMed1994

A digitized fluorescence imaging study on the effects of local anesthetics on cytosolic calcium and mitochondrial membrane potential in cultured rabbit corneal epithelial cells.

It has been documented by several investigators that local anesthetics displace calcium from calcium binding sites and alter the functioning of different calcium regulating systems. Local anesthetics have also been shown to have adverse effects on mitochondrial function and interact with cytoskeletal elements. Few studies have addressed the role that a potential disturbance of calcium homeostasis and mitochondrial function may have on the toxicity caused by local anesthetics in corneal epithelial cells. This investigation was undertaken to evaluate the effects of tetracaine (TTC), proparacaine (PPC), and cocaine (CC) on cytosolic calcium and mitochondrial membrane potential in primary cultures of rabbit corneal epithelial cells. Previous studies by our laboratory documented that the local anesthetics produce toxicity after 30 to 60 min of treatment. In this study, the cells were treated for 15 min, a time when minimal cell damage occurred. The following concentrations of local anesthetics were used to treat the cells: TTC, 0.5-2.5 mM; PPC, 1-5 mM; and CC, 4-10 mM. We utilized the technology of digitized fluorescence imaging to measure changes in intracellular calcium ([Ca2+]i) with fura-2 and mitochondrial membrane potential (delta psi) with rhodamine 123. A dose-dependent increase in [Ca2+]i was evident after treatment with each local anesthetic. Concentrations equal or greater than 2.5 mM TTC dissipated delta psi. A rise in [Ca2+]i preceded any loss of delta psi caused by TTC. PPC at high concentrations (4-5 mM) occasionally dissipated delta psi but this was not a consistent finding. The effects of CC on delta psi could not be evaluated accurately because of the extensive morphological alterations that occurred after treatment. We conclude that TTC, PPC, and CC elevate [Ca2+]i before cytotoxicity occurs and disruptions in calcium homeostasis may contribute to their toxicity.

Anesthetics, Local↗
PubMed1980

The reinforcing properties of procaine, chloroprocaine and proparacaine in rhesus monkeys.

Responding was maintained under a fixed ratio 10 schedule of intravenous cocaine (six monkeys) or pentobarbital (two monkeys) delivery during a daily 3 h session. When responding was stable, intravenous doses of procaine (0.05--3.2 mg/kg), chloroprocaine (0.05--3.2 mg/kg), proparacaine (0.01--0.4 mg/kg), or saline were substituted for the cocaine or pentobarbital for six to ten sessions. Between each substitution, responding was again maintained by cocaine or pentobarbital. Procaine and chloroprocaine maintained rates of responding exceeding saline levels in all monkeys tested, with maximum rates generated by 0.2 mg/kg. Daily intake in mg/kg increased 3--10 times a dose was increased from 0.1 to 3.2 mg/kg per infusion. Within each session, there were periods of continuous responding resulting in multiple infusions, separated by intervals of no responding of varying duration. Nevertheless, the number of infusions occurring in each of the six 30 min periods was relatively constant for both drugs. Responding maintained by proparacaine was similar or slightly above that maintained by saline except at one dose (0.025 mg/kg) in one monkey. No signs of toxicity were observed with any of the drugs. These results indicate that procaine and chloroprocaine are strong positive reinforcers but that proparacaine has minimal reinforcing properties.

Anesthetics, Local↗
PubMed1980

Pupillary dilatation with single eyedrop mydriatic combinations.

We studied the mydiatic effect of three solutions containing a combination of two mydriatic drugs in 80 adult patients. The solutions tested were cyclopentolate HCl 0.5% with phenylephrine 2.5%, tropicamide 0.5% with phenylephrine 2.5%, and tropicamide 1.0% with phenylephrine 2.5%. We evaluated the effect of prior instillation of proparacaine 0.5% eyedrops. All three mydriatic combination solutions evaluated produced pupillary dilatation of about 7 mm within 60 minutes. Additional pupillary dilatation of 1 mm occurred when proparacaine was instilled before the mydriatic combination eyedrop. Mydriasis was resistant to bright light during indirect ophthalmoscopy in all patients. Pupils of younger patients dilated better than those of older patients, but sex and iris color were factors in the amount of pupillary dilatation obtained. Wide and sustained pupillary dilatation can be obtained for satisfactory indirect ophthalmoscopy by the instillation of one drop of proparacaine solution followed by a single drop of any of the three mydriatic combination solutions evaluated. By eliminating the need for multiple instillations of drugs, the use of a single eyedrop mydriatic combination is convenient in terms of time saved and also lessens the change of systemic drug toxicity.

Adolescent↗
PubMed1986

A proposed mechanism for increased tear-film osmolarity in contact lens wearers.

Contact lenses decrease corneal sensitivity and increase tear-film osmolarity. To determine whether the decrease in corneal sensitivity is responsible for the increase in tear-film osmolarity, we studied tear-film osmolarity in normal rabbits and rabbits with surgically induced keratoconjunctivitis sicca before and after the instillation of 0.5% proparacaine. Instillation of proparacaine resulted in a significant increase in tear-film osmolarity. Decreased corneal sensitivity, with a resultant decrease in tear secretory rates, is the most likely cause for increased tear-film osmolarity in wearers of hard contact and extended-wear soft contact lenses.

Animals↗