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PubMed1989

Effect of drugs on histamine radio-enzyme assay.

The effect of over 200 drugs and other compounds on histamine radio-enzyme assay was studied. Some muscle relaxants (e.g. alcuronium), some sympathomimetics (e.g. dopamine, isoxsuprine, tyramine and possibly phenylethylamine), antimalarial drugs, procaine, procainamide, Berenil and serotonin were potent compounds to interfere with this assay. In some special cases still potentially inhibitory drugs seemed to be some muscle relaxants (e.g. vecuronium, pancuronium and tubocurarine), antidepressants, antihistamines (e.g. cimetidine, ranitidine and diphenhydramine), chinidin, disopyramide, tolazoline and salazosulfapyridine.

Histamine↗
PubMed1983

Effect of anesthetic or analgesic drugs on lipogenic and lipolytic adipose tissue activities.

The effects of several anesthetic or analgesic agents (halothane, Na thiopental, ketamine, nitrous oxide, xylazine, and procaine) administered in vivo, on swine adipose tissue metabolism were measured. Adipose tissue samples were collected from the subcutaneous depot before and after administration of the anesthetic or analgesic agent. The rate of oxidation of glucose to CO2 and the lipogenic rate, or the basal and stimulated lipolytic rates, were measured on tissue slices incubated in vitro. There were no effects on the oxidation of glucose to CO2 or the incorporation into lipids except by procaine. Procaine depressed (P less than or equal to 0.05) the lipogenic rate (12%) and tended (P less than or equal to 0.1) to depress the oxidative rate (9%). The only observable effect on the lipolytic rates was a tendency (P less than or equal to 0.1) for ketamine to increase the stimulated lipolytic rate. The minimal effects on adipose tissue metabolism reported herein were obtained with short times of compound administration. Several agents (nitrous oxide, procaine, and xylazine) are not recommended because of poor analgesia.

Adipose Tissue↗
PubMed1984

The role of electrostatic interactions in modulating the local anaesthetic effects of amphipathic agents in frog skeletal muscle.

The local anaesthetic effect of cationic, anionic, and neutral alkyl amphipathic agents was similarly enhanced in an apparently nonspecific way by circumstances which modulate electrostatic interactions (acidity, modification of charged groups at the sarcolemmal surface by group-specific reagents, or changes in the calcium concentration), presumably as the result of secondary effects on the conformation of membrane proteins. However, the selective enhancement of the local anaesthetic effect of alkyl trimethylammonium compounds by perchlorate implies a more specific interaction which may influence the penetration of hydrophobic groups into the membrane interior.

Action Potentials↗
PubMed1969

The actions of some cholinomimetic drugs on the isolated taenia of the guinea-pig caecum.

1. The actions on the taenia of 4-(m-chlorophenylcarbamoyloxy)-2-butynyl-trimethylammonium chloride (McN-A-343), N-benzyl-3-pyrrolidyl acetate methobromide (AHR-602), tetramethylammonium (TMA) and choline phenyl ether have been examined and compared with the actions of acetylcholine, nicotine and 1,1-dimethyl-4-phenylpiperazinium (DMPP).2. Responses of the taenia to these agonists are quantitatively and often qualitatively dependent on the tone of the preparation. A method is described which makes allowance for the effect of tone on heights of contractions.3. Acetylcholine, McN-A-343 and AHR-602 produced only contractions; TMA produced contractions or biphasic responses; and choline phenyl ether, nicotine and DMPP produced contractions, relaxations or biphasic responses.4. The mode of action of these compounds has been analysed by means of hyoscine, ganglion-blocking drugs, tetrodotoxin and local anaesthetics.5. It is concluded that acetylcholine, McN-A-343, AHR-602, TMA and choline phenyl ether act on muscarinic receptors in the smooth muscle. Choline phenyl ether has an additional action on nicotinic receptors of cholinergic neurones. Nicotine and DMPP act on nicotinic receptors of cholinergic neurones and of inhibitory neurones. An action on the latter is sometimes also seen with TMA and choline phenyl ether.6. With nicotine or DMPP, and TMA or choline phenyl ether in the presence of hyoscine, part of the contraction phase of biphasic responses (in which a contraction follows relaxation) is best explained as being triggered by the initial relaxation-that is, as a "rebound contraction".7. None of the compounds tested appeared to exert an atropine-sensitive action on neurones.8. In the presence of hyoscine high concentrations of agonists can act on sites not involved with lower concentrations.

Acetylcholine↗
PubMed1988

The pH-dependent local anesthetic activity of diethylaminoethanol, a procaine metabolite.

To test whether the products of procaine hydrolysis have local anesthetic actions resembling those of procaine, the authors compared the ability of procaine and its metabolites diethylaminoethanol (DEAE) and para-aminobenzoic acid (PABA) to block compound action potentials in excised, desheathed frog and rat sciatic nerves. Studies were performed in solutions of impermeant buffers at pH 7.4 (corresponding to mammalian physiologic pH) and at pH 9.2 (close to the pKa of procaine and DEAE) to test for extracellular pH-dependent increases in drug permeation and potency. Both procaine and DEAE inhibited compound action potentials at pH 7.4 and 9.2 in a reversible and dose-dependent manner, and both were approximately ten-fold more potent at pH 9.2 than at pH 7.4, procaine inhibiting the action potential height by 50% at 0.15 mM (pH 9.2) and 1.1 mM (pH 7.4), DEAE at 4 mM (pH 9.2) and 70 mM (pH 7.4). In contrast, PABA at concentrations up to 25 mM and at either pH failed to inhibit compound action potentials, and did not modify the effects of DEAE when both drugs were given together. Procaine produced greater use-dependent block at the higher pH and at higher stimulation rates (100 Hz vs. 40 Hz); DEAE produced almost no use-dependent block. These observations suggest: 1) that DEAE might account for some of the neuropharmacologic activity of procaine in techniques that favor the accumulation of metabolites (such as those requiring large doses or prolonged infusions); and 2) that alkalinization of procaine and DEAE solutions appears to increase their potency for both resting and use-dependent block of action potentials.

4-Aminobenzoic Acid↗
PubMed1977

Hepatic uptake of foreign compounds: influence of acute extrahepatic biliary obstruction.

Extrahepatic cholestasis produced by bile duct ligation decreased the net hepatic uptake of organic anions including sllfobromophthalein, sulfobromophthalein glutathione and phenol-3,6-dibromophthalein disulfonate, and the neutral organic compound, ouabain. The net hepatic uptake of procaine amide ethobromide, an organic cation was not similarly affected. Impairment of net hepatic uptake by bile duct ligation was demonstrated by reduced liver concentration and content of administered compound despite higher plasma concentration. Acute bile duct ligation did not alter the amount of hepatic cytoplasmic anion binding proteins. The impaired net hepatic uptake of sulfobromophthalein in bile duct-ligated rats was reversed by re-establishing bile flow. Deleterious effects of endogenous bile or bile constituents and specific alteration of membrane carrier proteins are considered possible contributing factors to the impaired net hepatic uptake process observed in bile duct-ligated rats.

Animals↗
PubMed1984

A comparison of the local anaesthetic effects of cationic, anionic, and neutral amphipathic agents in frog skeletal muscle.

Impermeant alkyl amphipathic agents reduced the excitability of frog twitch muscle fibers, indicating that local anaesthesia can be produced by perturbations within the external lamina of the sarcolemma. Cationic (n-alkyl trimethylammonium) and anionic (n-alkyl sulfonate) as well as permeant neutral (n-alkanol) agents have been compared with regard to their local anaesthetic potency. Small impermeant agents (fewer than six carbon atoms) alone were ineffective. Within each series the concentration required to reduce excitability was proportional to the length (hydrophobicity) of the hydrocarbon chain attached to the polar group. However, corresponding members of these three series of compounds differed considerably in their local anaethetic potency. Hence, charged groups as well as apolar moieties can influence local anaesthetic efficacy. The supra-additive character of the local anaesthesia produced by combining impermeant alkyl anions and cations indicates that these two types of amphipaths may produce their similar effects by perturbations at different membrane sites.

Action Potentials↗
PubMed1987

Sporicidal activity of local anaesthetics and their binary combinations with preservatives.

The sporicidal activity of 1% solutions of five local anaesthetics and five preservatives (cetrimide, chlorocresol, chlorhexidine, phenoxyethanol and phenylmercuric nitrate) at their pharmacopeial concentrations, alone and in binary combinations was determined against Bacillus subtilis and Aspergillus niger spores at different temperature levels by the surface viable count technique. The sporicidal activity of all tested systems were temperature dependent. A. niger spores were much more sensitive to the tested systems than B. subtilis spores. The temperature at which 99% of all spores were killed after 30 min exposure time of the anaesthetics were calculated. In case of the local anaesthetics alone against spores of A. niger the recorded temperatures were 30 degrees C for amethocaine, 45 degrees C for both amylocaine and cincochaine, 48 degrees C and 50 degrees C for lignocaine and procaine, respectively, in contrast to 58 degrees C in a control with saline solution. Much higher temperatures were calculated against B. subtilis spores. Cincochaine was the most effective local anaesthetic with a recorded temperature of 60 degrees C, where 99% killing occurred. Amylocaine and amethocaine showed temperatures of 84 degrees C and 90 degrees C, respectively. Procaine, lignocaine as well saline solution as a control caused a 99% killing effect at temperatures higher than 100 degrees C. Among the 25 tested binary combinations of local anaesthetics and preservatives, the highest incidence of potentiation of the sporicidal activity was recorded with chlorocresol combinations, while other combinations of the four remaining preservatives showed different types of interactions at different percentages.

Anesthetics, Local↗
PubMed1984

Adulterants in heroin/cocaine: implications concerning heroin-associated nephropathy.

Heroin-associated nephropathy (HAN) is a complication of the intravenous use of heroin or cocaine. It has been postulated that one of the substances used to adulterate these drugs may be responsible for the renal injury. We examined data provided by the Drug Enforcement Administration (DEA) concerning the laboratory analysis of 12 366 samples of heroin/cocaine. These street-grade drugs were analyzed for the presence of various adulterants or secondary substances. Eleven adulterants were identified with a frequency of occurrence that exceeded 5%. Quinine, mannitol, lactose and procaine were the non-narcotic compounds most commonly found. Other substances found included caffeine, inositol, lidocaine, starches, methapyrilene, sucrose, acetylprocaine and dextrose. No specific substance including heroin or cocaine has yet been definitely implicated as causative of HAN. These data suggest that further animal research is needed to determine the effects of repeated intravenous injections of each of these commonly found substances on the kidney.

Cocaine↗
PubMed1987

The influence of various substances on the gliding motility of Mycoplasma mobile 163K.

Non-toxic concentrations of various substances were tested for their influence on the gliding motility of Mycoplasma mobile 163K. A significant inhibitory effect on motility was observed with agents acting on nucleic acid synthesis (mitomycin), protein synthesis (puromycin, chloramphenicol), energy metabolism (p-chloromercuribenzoate, iodoacetate) and with compounds reacting with the cytoplasmic membrane or contractile elements (albumin, cholesterol, EDTA, 2-propanol, procain, CaCl2, MgCl2, colchicin and KI). The surface-active compounds Triton X-100, Tego and SDS increased the gliding velocity significantly in some concentrations and incubation periods. The results suggest that the motility of M. mobile depends on a functional cytoplasmic membrane and that cytoskeletal elements are involved in the gliding mechanism.

Anti-Bacterial Agents↗
PubMed1992

[Local anesthetics. CVI. Preparation and effect of (+/-)-trans-[2-(piperidinomethyl) cyclopentyl] alkyl, alkoxy and halogen substituted esters of phenylcarbamic acid].

Within the framework of the research of potential local anaesthetics, five compounds from the group of (+/-)-trans-[2-(piperidino-methyl)cyclopentyl]alkyl, alkoxy and chloroalkyl esters of phenylcarbamic acid were prepared. The final compounds were obtained by addition of (+/-)-trans-2-(piperidinomethyl)cyclopentanol to the corresponding substituted phenylisocyanates. They were isolated in the form of salts with hydrochloric acid. Their structure was confirmed on the basis of interpretation of the results of UV and IR spectra. A pharmacological evaluation revealed that the final compounds were more effective than the employed standards cocaine and procaine, but they did not achieve the expected effect in comparison with the pattern compound pentacaine. The index of local-anaesthetic efficacy ranges from 1 to 8 in surface anaesthesia and 1 to 12 in infiltration anaesthesia. It is substantially lower even in comparison with analogical basic esters of alkoxyphenylcarbamic acid.

Anesthetics, Local↗
PubMed2004

Transplacental passage of Pt after treatment with the new triamine complex cis-diaminechloro-[2-(diethylamino) ethyl 4-amino-benzoate, N4]-chloride platinum (II) monohydrochloride monohydrate.

Cis-diaminechloro-[2-(diethylamino) ethyl 4-amino-benzoate, N4]-chloride platinum (II) monohydrochloride monohydrate (DPR) is a monofunctional Pt triamine complex synthesized starting from cisplatin and procaine hydrochloride, characterized by a good antitumor activity coupled with low toxic effects and able to impair prenatal development of mice but at doses outside or just in the upper range of therapeutic doses. In the present paper the transplacental passage of DPR-derived Pt was investigated in CD1 mice on days 9, 13, 16 and 18 of pregnancy, 24 h after ip administration of 21 mg/kg DPR. For comparison, groups of mice were treated with an equivalent Pt-containing dose of cisplatin (10.7 mg/kg). Similarly to cisplatin, small amounts of Pt were detected in fetuses on day 9. From day 13 of gestation the concentration of DPR- and cisplatin-derived Pt increased up to the highest fetal concentrations detected on day 16. On day 18 the concentration of Pt decreased. Most importantly, on days 13-18 of pregnancy cisplatin-derived Pt was always significantly higher than that assayed after DPR administration. In addition, on day 13 of pregnancy Pt exposure of fetuses was significantly higher when dams were treated with cisplatin (AUC(0.5-24)= 3.40 vs. 4.95 microg.h/g). Finally, it is worth noting that serum decay of Pt after DPR or cisplatin administration in adult female mice was similar with AUC0.13-2h s of 7.5 and 6.6 microg.h/ml, respectively. When we determined the concentration of Pt into the main organs of fetuses from dams treated with either DPR or cisplatin on day 18 of gestation, we observed a different organ distribution. In fact, while the concentration of DPR-derived Pt was greater in the heart (1.08+/-0.30 vs. 0.78 +/- 0.35 microg/g, p <0.10), an opposite situation was found in the kidney (0.51+/-0.20 vs. 0.69 +/- 0.22 microg/g, p <0.05). In conclusion, our data show that DPR may pass through the placenta with an efficiency significantly lower than that of cisplatin. This finding may represent one of the possible causes of the lower embryotoxic/teratogenic effect of DPR as compared to cisplatin.

Abnormalities, Drug-Induced↗