Mode of action of vasopressin on isolated proximal colon of the guinea-pig.
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Acetylcholine↗
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Results for “PROCAINE AND COMPOUNDS”
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Reperfusion effects on the magnesium-procaine arrested rabbit heart.
Rabbit hearts were subjected to cardiac arrest induced by injecting 3 isotonic cardioplegic solutions each of which contained in combination with procaine-HCl one of 3 different magnesium compounds. A period of 40 min arrest was followed by reperfusion of 15 min. A regular sinus rhythm returned after washout of the cardioplegic solution. The pattern of the essentially unaltered myocardial ultrastructure correlated with the well-preserved high-energy phosphate stores. The effects of magnesium and procaine on cell permeability and the consequences of the different fusion are discussed. The study stresses the importance of an adequate period of postischemic reperfusion of the heart in an unloaded state in support of myocardial recovery. The studies presented herein suggest further investigations of various concentrations of magnesium and procaine combined with different amounts of calcium in perfusates for the preservation of the heart and possibly of other organs.
Animals↗
Use of a novel cation-exchange restricted-access material for automated sample clean-up prior to the determination of basic drugs in plasma by liquid chromatography.
A new kind of silica-based restricted-access material (RAM) has been tested in pre-columns for the on-line solid-phase extraction (SPE) of basic drugs from directly injected plasma samples before their quantitative analysis by reversed-phase liquid chromatography (LC), using the column switching technique. The outer surface of the porous RAM particlescontains hydrophilic diol groups while sulphonic acid groups are bound to the internal surface, which gives the sorbent the properties of a strong cation exchanger towards low molecular mass compounds. Macromolecules such as proteins have no access to the internal surface of the pre-column due to their exclusion from the pores and are then flushed directly out. The retention capability of this novel packing material has been tested for some hydrophilic basic drugs, such as atropine, fenoterol, ipratropium, procaine, sotalol and terbutaline, used as model compounds. The influence of the composition of the washing liquid on the retention of the analytes in the pre-column has been investigated. The elution profiles of the different compounds and the plasma matrix as well as the time needed for the transfer of the analytes from the pre-column to the analytical column were determined in order to deduce the most suitable conditions for the clean-up step and develop on-line methods for the LC determination of these compounds in plasma. The cationic exchange sorbent was also compared to another RAM, namely RP-18 ADS (alkyl diol silica) sorbent with respect to retention capability towards basic analytes.
Automation↗
Spectrophotometric determination of procaine hydrochloride by means of iron (3+)-4-aminobenzohydroxamic acid complex.
A rapid, simple and reproducible method is presented, for the determination of procaine hydrochloride in bulk and in pharmaceutical preparations containing also corbadrine or caffeine. The method is based on the conversion of procaine into the corresponding hydroxamic acid which reacts with iron (III) forming a complex of violet colour stable at pH 2.0, with a maximum absorption at a wavelength of 540 nm, and with molar absorptivity (epsilon = 0.43 X 10(3) l mol-1 cm-1). The minimum detectable amount was 1.47 X 10(-4) M/l, and Lambert-Beer law is obeyed in the range 2.93 X 10(-4) - 4.106 X 10(-3) M/l. By the application of Bent-French method it has been established that the stoichiometric ratio of 4-aminobenzohydroxamic acid and iron (3+) in the complex is 3:1. No interference with degradation product of procaine (4-aminobenzoic acid) was observed.
Ferric Compounds↗
[EXPERIMENTAL BILIOGENIC SHOCK AND ITS CONTROL].
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Animals↗
Embryo-lethal and teratogenic effect of the new platinum compound DPR in pregnant mice.
Embryo-lethal and teratogenic effects caused by the cisplatin-procaine complex cis-diaminechloro-[2-(diethylamino) ethyl 4-amino-benzoate, N(4)]-chlorideplatinum(II) monohydrochloride monohydrate (DPR) were examined in CD-1 mice after a single administration of 7, 14, 21 or 28 mg/kg, injected on day 6, 9, 13 or 16 of pregnancy. At day 18 of pregnancy fetuses were removed and carefully examined for external, visceral and skeletal malformations under a dissecting microscope. A significant reduction of maternal weight gain was observed in pregnant mice after the administration of 21 (day 13) or 28 mg/kg (days 9 and 13) DPR. The exposure to DPR during the organogenesis and early histogenesis periods of prenatal development (administration on day 9 or 13) induced a significant reduction of the mean percentage of live fetuses and a significant increase of the mean percentage of dead and resorbed fetuses. A dose-dependent reduction of fetal body weight was observed in surviving specimens exposed to DPR on embryonic day 9, 13 or 16. The analysis of surviving fetuses killed on day 18 of gestation showed that a few, but statistically significant, external malformations and visceral anomalies were observed after administration of 21 or 28 mg/kg DPR on embryonic day 13. External malformations consisted of three hepato-omphalocele and six palatoschisis (one random palatoschisis was also observed at 21 mg/kg DPR given on day 9), while visceral anomalies included only renal pelvis dilatation. Skeletal anomalies affected fetuses independently of the day of treatment and were more frequent at the highest doses of DPR. They consisted of a delay in skull ossifications, vertebral and sternal anomalies, and formation of extra ribs. A low and non-significant incidence of skeletal malformations (asymmetric sternum) was noticed in fetuses. Our data demonstrated that DPR can cause embryotoxic effects if administered during the period of organogenesis and early histogenesis. Beside embryo-lethality, DPR induced growth retardation and malformations in surviving fetuses.
Abnormalities, Drug-Induced↗
Practical kinetics II: quantitation of procaine stability by TLC.
This work illustrates further application of TLC as a tool in kinetic investigations of organic molecules. The procedure consists of: (a) streaking or spotting a known volume of reaction solution on thin-layer plates, (b) developing the plates, (c) eluting the compound under study from the adsorbent, and (d) assaying the material in solution. Procaine was examined regarding its hydrolysis at above ambient temperatures. The reaction was monitored spectrally and by the TLC technique. Velocity constants derived by the two methods were similar in value. Rate constants obtained from procaine samples eluted from silica gel plates following development were in good agreement with those previously reported in the literature.
Buffers↗
Xylocain (lidocaine, lignocaine), its discovery and Gordh's contribution to its clinical use.
Hans v. Euler, while investigating how genes and enzymes were chemically related in some chlorofylldefective mutants of barley, isolated gramine, an indole. Erdtman synthetized isogramine and found it to have weak anesthetic properties. He then together with Löfgren synthetized other amino-amides, but no one of them could compete with the existing local anesthetics of the ester-type, derivatives of para-aminobenzoic acid, e.g. procaine. Later Löfgren and Lundqvist followed up these studies and found an amid compound lidocaine (2-dimethylaminoacet-2, 6-xylidide). Lidocaine represented such a significant advance over procaine in clinical tests preformed by T. Gordh that it was introduced for clinical use. It has now during a half century been the standard local anesthetic drug. All local anesthetics are neurotoxic in high enough doses. Xylocain, however, has had an excellent record of safety. Only during the last years have there been reports on possible toxic irritation and damage by Xylocain used for spinal anesthesia. The aetiology is still not clear In this connection two early observations by Gordh and his coworkers are discussed.
Alkaloids↗
Sodium channel neurotoxins as probes of the knockdown resistance mechanism.
A simple paralysis bioassay was used to measure the effects of sodium channel blockers and activators on third instar larvae of three strains of the house fly, Musca domestica. The pyrethroid-resistant strains kdr and super-kdr, which are thought to have rediced neural sensitivity to pyrethroids, displayed 28-fold and greater than 909-fold resistance to deltamethrin when compared to the pyrethroid-susceptible NAIDM strain. The kdr and super-kdr strains were also at least 16-fold resistant to the plant alkaloid aconitine. Previous studies on the interaction of pyrethroids and neurotoxins similar to aconitine with the sodium channel reported that these two classes of ligands bind to different receptor sites. Thus, our results demonstrate that the kdr and super-kdr resistance mechanisms modify the sensitivity of the insect nervous system to toxins which act at two distinct binding sites on the sodium channel. In contrast, the pyrethroid-resistant strains showed no cross resistance to tetrodotoxin, Leiurus quinquestriatus scorpion venon, or procaine, which suggests that the binding sites for these compounds are not altered.
Aconitine↗
Further studies on F1-ATPase inhibition by local anesthetics.
We have measured the inhibitory potencies of several local anesthetics (procaine, lidocaine, tetracaine and dibucaine) and related compounds (chlorpromazine, procainamide and propranolol) on the ATPase activities of bovine heart submitochondrial particles and purified F1 extracted from these particles. All of these agents cause inhibition of ATPase in F1 as well as in submitochondrial particles. A linear relationship is found between the log of the octanol/water partition coefficients and the log of the concentrations required for 50% inhibition of F1. Sedimentation velocity ultracentrifugation and polyacrylamide gel electrophoresis showed that 1.0 mM tetracaine caused partial dissociation of the F1 complex. Complete reversibility of the enzyme inhibitory effects was demonstrated, however. This work shows that local anesthetics can affect protein structure and enzyme activity without the mediation of lipid.
Adenosine Triphosphatases↗
Effect of procaine, calcium, magnesium and potassium on the acetylcholine release from the sweat nerve endings in human skin.
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Acetylcholine↗
THE EFFECTS OF GANGLION-BLOCKING AND POSTGANGLIONIC SYMPATHOLYTIC DRUGS ON PREPARATIONS OF THE GUINEA-PIG VAS DEFERENS.
The contractions of the guinea-pig isolated vas deferens elicited by electrical stimulation of the hypogastric nerve were completely blocked by the following drugs: guanethidine, bretylium, dimethylphenylpiperazinium hydrochloride, nicotine, pempidine, hexamethonium, hemicholinium, D-tubocurarine and procaine. However, when the vas deferens was stimulated through an electrode in its lumen, the contractions in response to frequent, short stimuli (50 shocks/sec, 1 msec duration) were blocked by guanethidine, bretylium and dimethylphenylpiperazinium, but were not affected by the remaining drugs, except that procaine and hemicholinium each caused some reduction in the responses. When the preparation was stimulated transmurally with shocks of 200 msec duration at 1 shock/sec, the contractions were unaffected by any of the above drugs, except hemicholinium which again caused a slow reduction of up to 50% of the original response. It is concluded that nicotine, pempidine, hexamethonium, D-tubocurarine and hemicholinium probably block the response to stimulation of the hypogastric nerve by acting on peripheral ganglia in its pathway. Hemicholinium appears to have an additional effect in depressing the responses of the smooth muscle of the vas deferens to direct electrical stimulation, and procaine may act both on the ganglia and at the nerve terminals.
Animals↗
Release of highly water-soluble medicinal compounds from inert, heterogeneous matrixes. I: Physical mixture.
The release from a matrix compressed from a physical mixture of hydrogenated castor oil and ephedrine hydrochloride or procaine hydrochloride has been investigated. The effects on release of the concentration of medicinal compound, particle size of medicinal compound, agitation of dissolution medium, and porosity and tortuosity of the matrix are presented. An attempt is made to fit the experimental data to an acceptable diffusion model.
Castor Oil↗
Anticonvulsant properties of some new derivatives of phensuccinimide.
Anticonvulsant properties of two new derivatives, of phenylsuccinimide, N-morpholinomethyl-3-bromophenyl-succinimide(IL-7) and N-amino-3-bromophenylsuccinimide (IL-16), were studied. It was stated that both compounds have similar acute toxicity and act longer than phensuximide. They are especially active in maximal electroshock seizure (MES) test. Their effectiveness against convulsions produced by pentetrazole is less than that of phensuximide. Their effectiveness against procaine and strychnine is similar, only one of tested compounds has very high potency against strychnine. This compound, IL-16, has also a different pattern of effect-time which is probably due to its different pharmacokinetic behaviour.
Animals↗
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↗
Effect of papain-induced emphysema on permeability of rat lung to drugs.
To investigate the effect of a papain-induced emphysema-like condition on pulmonary absorption of drugs, rats were exposed to either papain aerosol or distilled water aerosol (control) intermittently for 2 wk, and rates of drug absorption from damaged and control lungs were compared. To measure absorption rates, 0.1 ml of drug solution (0.1-10 mM) was administered through a tracheal cannula to anesthetized animals, and after various times lungs were assayed for unabsorbed compound. In absorption experiments with the lipoid-insoluble compounds, mannitol, p-aminohippuric acid, and procaine amide ethobromide, all three drugs were absorbed from the lungs about twice as rapidly in papain-treated rats as in control. In contrast, procaine amide, a relatively lipoid-soluble drug, was absorbed at the same rate in both control and papain-treated animals. The results suggest that papain-induced lung damage increases the porosity of the pulmonary epithelium.
Aerosols↗
[Lysosomotropic compounds inhibiting the multiplication of Junin virus].
A number of lysosomotropic compounds of diverse chemical structure, ammonium chloride, procaine and chlorpheniramine, were found to inhibit the infection of Vero cells by Junín virus. Viral replication was almost totally inhibited by 15 mM ammonium chloride, when added either before or within the first hour of infection and a significant inhibition (97.8%) was observed when it was added 8 hours after infection. These results agree with a model which postulates that arenavirus entry occurs by receptor-mediated endocytosis.
Ammonium Chloride↗
[Ion pair HPLC determination of p-aminobenzoic acid as an impurity in procaine and procainamide hydrochlorides].
A simple, specific and sensitive high-performance liquid chromatographic method for the determination of p-amino benzoic acid (PABA) as impurity in procaine and procainamide hydrochlorides has been developed. The compounds were chromatographed on reversed phase C-18 using water-methanol-acetonitrile solvent system containing sodium lauryl sulphate ion-pair reagent.
4-Aminobenzoic Acid↗