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PubMed1985

Different effects of centrally acting drugs on rabbit platelet aggregation: with special reference to selective inhibitory effects of antipsychotics and antidepressants.

Twenty-four drugs, consisting of antipsychotics, tricyclic antidepressants, other centrally acting drugs, and related compounds, were studied for their effects on aggregation of rabbit platelets. Phenothiazine neuroleptics, haloperidol, sultopride, tricyclic antidepressants, sulpiride, atropine, and propranolol showed a selective inhibitory effect on the collagen-induced aggregation, but not on aggregations induced by arachidonic acid (AA) or adenosine diphosphate (ADP). These drugs are thought to inhibit the liberation of AA from phospholipids in platelet membranes, suggesting that they might inhibit phospholipases. Mepyramine, promethazine, phentolamine, and clozapine inhibited the aggregations evoked by collagen and AA, but failed to inhibit the ADP-induced aggregation. These drugs might inhibit the generation of prostaglandin endoperoxides or thromboxanes. Phenobarbital, phenytoin, procaine, lidocaine, flurazepam, trihexyphenydil, and lithium carbonate did not inhibit any kind of aggregation at the concentrations used. The clinical and pharmacological significance of these findings is discussed; it seems that the inhibitory effects of antipsychotics and antidepressants on platelet aggregation are closely related to the specific clinical and psychotropic effects of these drugs, but not to other actions.

Animals↗

PubMed2006

Pharmacological and toxicological testing of the enantiomers of two chiral fomocaine alkylmorpholine derivatives in comparison to their in vitro interactions on drug metabolism in rats.

Between the stereoisomers of amide-type local anaesthetics differences have been noticed with respect to pharmacokinetics and side effects, but not regarding local anaesthetic capacity. Therefore, only S-(-)-ropivacaine has been introduced into clinical practice and with bupivacaine both the racemate and the S-(-)-enantiomer (levobupivacaine) are available by now. Based on this background, the aim of the present study was to evaluate if there are also dissimilarities to be found both in the toxicity and in the effectiveness of the enantiomers of two newly synthesized chiral fomocaine alkylmorpholine derivatives, OW3 and OW13, with an additional C2-chain in 2- or an additional C3-chain in 3-position at the morpholine ring, respectively. For this purpose, in vitro the interaction capacity with cytochrome P450 (CYP)-mediated monooxygenase and oxidase functions was investigated using rat liver 9000 g supernatants or microsomes. In vivo LD50, paresis of the N. ischiadicus and surface and conduction anaesthesia (cornea, N. ischiadicus) were tested in rats. The enantiomers of both OW3 and OW13 caused a concentration dependent inhibition of all CYP-mediated model reactions investigated. With all model reactions the (-)-enantiomer of OW3 was less effective than the (+)-form, whereas the opposite was the case with OW13. Also toxicity was lower with the (-)-enantiomer of OW3 and with the (+)-form of OW13 than with the respective counterparts. With both derivatives no clear-cut dissimilarities were noticed in the local anaesthetic capacity of the enantiomers. None of the four compounds caused paresis. Thus, similar to amide-type local anaesthetics, also with the enantiomers of chiral fomocaine alkylmorpholine derivatives differences in pharmacokinetic properties and toxicity could be demonstrated.

Anesthesia, Conduction↗

PubMedDate not supplied

[Effect of lithium chloride on several indices of cardiac function].

Used in a dose of 100 mg/kg lithium chloride modifies the ECG patterns in rats, rabbits and cats. It increases the voltage of P and R waves, the S-T interval and slows down the rhythm of cardiac contractions. In doses of 50-300 mg/kg the compound raises the coronary circulation rate in narcotized cats. The compound exerts an antiarrhythmic action in chlorocalcium arrhythmia in rats, in strophanthin-induced one in cats and frogs and the intensity of this action is not inferior to that produced by potassium chloride, quinidine, novacainamide, izoptin and even exceeds it.

Animals↗

PubMed1984

Mechanisms of toxicological interactions involving organophosphate insecticides.

Administration of apparently nontoxic doses of organophosphorus compounds can greatly alter the toxicity of other compounds. These might include other organophosphates, as well as other drug or nondrug xenobiotics. Mechanisms of toxicologic interactions are discussed. Emphasis is placed upon organophosphate inhibition of noncritical tissue esterases and alterations in the metabolism and toxicity of selected ester and amide containing xenobiotics.

Acetaminophen↗

PubMedDate not supplied

The use of 13C NMR spectroscopy in forensic drug analysis.

13C NMR spectroscopy has been used for analysis of fourteen compounds which, according to Swedish laws are defined as narcotic drugs or are substances often found in combination with these drugs. The carbon-13 NMR method seems to be well suited for analysis of complex forensic drug mixtures because no preliminary separation of components is required.

Amphetamine↗

PubMed2006

Assessment of genotoxicity of 14 chemical agents used in dental practice: ability to induce chromosome aberrations in Syrian hamster embryo cells.

To assess the genotoxicity of 14 chemical agents used as locally applied agents in dental practice, the ability of these agents to elicit chromosome aberrations was examined using Syrian hamster embryo (SHE) cells. Chromosome aberrations in SHE cells were induced by treatment with three of eight chemical agents used as endodontic medicaments, i.e. ethylenediaminetetraacetic acid (EDTA), formocresol (a mixture of formalin and tricresol), and sodium arsenite. The other five chemical agents, i.e. chloramphenicol, p-chlorophenol, p-phenolsulfonic acid, sodium hypochlorite, and tetracycline hydrochloride exhibited a negative response for chromosome aberrations. Assessment of three dyes used for disclosing dental plaque showed chromosome aberrations induced by basic fuchsin but not by acid fuchsin and erythrosine B. Three local anesthetics, lidocaine hydrochloride, prilocaine hydrochloride, and procaine hydrochloride, were negative for chromosome aberrations. Among the ten chemical agents that exhibited a negative response in the assay, p-chlorophenol, sodium hypochlorite, and erythrosine B induced chromosome aberrations in SHE cells when treated in the presence of exogenous metabolic activation. The percentages of cells with polyploidy or endoreduplication were enhanced by formocresol, sodium arsenite, p-chlorophenol, p-phenolsulfonic acid, sodium hypochlorite, erythrosine B, prilocaine hydrochloride, and procaine hydrochloride in the absence or presence of exogenous metabolic activation. Our results indicate that the chemical agents that had a positive response in the present study are potentially genotoxic to mammalian cells.

Anesthetics↗

PubMedDate not supplied

Dynamics of local-anesthetic compounds in regional anesthesia.

The clinical effectiveness and safety of compounded mixtures of lidocaine + bupivacaine and chloroprocaine + bupivacaine for either epidural or brachial-plexus block was studied in 48 adult patients. Of the several alternatives, chloroprocaine + bupivacaine with epinephrine was found the best choice for patients with typical plasma cholinesterase.

Adolescent↗

PubMed1993

An acetylcholine receptor regulatory site in BC3H1 cells: characterized by laser-pulse photolysis in the microsecond-to-millisecond time region.

When a neurotransmitter binds to its specific receptor, the protein forms transmembrane channels through which ions flow, leading to changes in transmembrane voltage that trigger signal transmission between neurons. How do inhibitors affect this process? Interesting and extensive information comes from investigations of the acetylcholine receptor, the best known of these proteins. This receptor is inhibited by cationic inhibitors, including local anesthetics, and acetylcholine at high concentrations. The accepted mechanism, elegant in its simplicity, is that these compounds enter the receptor-channel after it opens and block inorganic ion flux. This mechanism requires that the inhibitors affect only the apparent rate constant for channel closing (k'cl). An alternative mechanism invokes a specific regulatory (inhibitory) site to which inhibitors bind before the channel opens and the signal is transmitted. This mechanism requires that the inhibitors affect the apparent rate constants for both channel opening (k'op) and closing. The effect of inhibitors on k'op has not been determined previously. This report describes the use of a newly developed laser-pulse photolysis technique with a dead time of approximately 120 microseconds to determine the effect of a local anesthetic, procaine, one of the best studied cationic inhibitors of the acetylcholine receptor, on both k'op and k'cl. Both k'op and k'cl were found to decrease with increasing procaine concentration. This effect of the inhibitor of k'op cannot be explained by the open-channel-blocking mechanism but is consistent with the existence of a regulatory (inhibitory) receptor site.

Animals↗

PubMedDate not supplied

Tissue fluid penetration and anti-treponemal activity of trospectomycin (a new spectinomycin analog) in the rabbit syphilis model.

The antitreponemal activity of trospectomycin (a novel 6'-propyl analog of spectinomycin) was correlated with concentrations in serum and tissue chamber fluid in a cutaneously-infected rabbit model of syphilis. After single-dose intramuscular (im) injections of trospectomycin, spectinomycin hydrochloride, and aqueous procaine penicillin G(APPG), concentrations of the drugs in paired specimens of serum and tissue fluid were determined and correlated with response of Treponema pallidum-infected lesions. Lesions responded most rapidly in APPG-treated animals. Rapid response correlated with more prolonged levels of APPG in both serum and tissue fluid. Trospectomycin, when given in single doses exceeding 40 mg/kg, surpassed penicillin in peak serum levels (greater than 60 micrograms/ml at 1 hr) but not in duration of activity. Higher and prolonged concentrations of trospectomycin in tissue fluid correlated with more effective clearance of treponemes from cutaneous lesions. Animals treated with less than 40 mg of trospectomycin/kg or with 20-80 mg/kg of the parent compound (spectinomycin hydrochloride) had cutaneous lesions that were persistently darkfield-positive, as confirmed by three or more consecutive smears.

Animals↗

PubMed2000

The development of a semi-preparatory scale supercritical-fluid chromatograph for high-throughput purification of 'combi-chem' libraries.

A unique separator was developed which allowed automatic separation and peak collection using semi-preparative supercritical fluid chromatography (SFC). A peak detector switched the effluent between waste and special collection cassettes. Up to 50 mg of various solutes were injected onto a 21-mm I.D. Cyano column. The entire flow path was contained and no aerosols were generated. Collection efficiency was as high as 95%. Peak purity was often greater than 99. 9%. Typical run times were less than 10 min. An analytical SFC was used to screen the performance of a wide range of mobile and stationary phases for the elution of more than 60 miscellaneous small drug compounds. The best 'universal' gradient employed 0.4% isobutyl or isopropylamine dissolved in methanol, then mixed from 5 to 55% into carbon dioxide at 10%/min. Flow rate was 50 ml/min. The analytical SFC was shown to be a good predictor of the semi-prep instrumental performance.

4-Aminobenzoic Acid↗

PubMedDate not supplied

Interaction of muscle relaxants and local anesthetics at the neuromuscular junction.

The effects on neuromuscular (NM) function of combinations of relaxants (d-tubocurarine, pancuronium, and succinylcholine) and local anesthetics (cocaine, procaine, lidocaine, etidocaine, and a quaternized derivative of procaine, procaine methobromide) were investigated using the rat's phrenic nerve--hemidiaphragm preparation. Combinations of ineffective concentrations of NM blocking agents with ineffective concentrations of local anesthetics caused a greater than 90% NM block. Preliminary administration of ineffective concentrations of local anesthetics significantly ( p less than 0.001) decreased the ED50 of NM blocking agents. The administration of ineffective concentrations of NM blocking agents caused a similar decrease of the ED50 of local anesthetics. Concentrations of d-tubocurarine and pancuronium which alone produced partial NM block had additive effects. These findings suggest that the interaction of NM blocking agents and local anesthetics consists of true potentiation caused by the different sites of action of the two types of compounds at the NM junction. The degree of potentiation may be enough to cause clinically significant NM block in patients who at the same time receive high enough doses of both agents. In vitro the NM block caused by the combinations of local anesthetics and NM blocking agents can be reversed by 4-aminopyridine.

Anesthetics, Local↗

PubMed1980

A study of the effects of amodiaquine on the guinea-pig isolated ileum.

Amodiaquine (3.5 . 10(-7) mol/l), a 4-amino-quinoline antimalarial, increases the responses of the guinea-pig isolated ileum to direct (acetylcholine, histamine, barium, chloride), partially (5-hydroxytryptamine, PGE1 and F2 alpha) and totally (electrical stimulations, nicotine) indirect agonists. Moreover it reverses inhibitions of the electrical induced contractions by acetylcholine antagonists (atropine), acetylcholine release blocking agents (morphine, tetrodotoxin, procaine, noradrenaline) and prostaglandin synthesis inhibitors (indomethacin, ibuprofen, flufenamine acid, hydrocortisone). From 2.7 . 10(-6) mol/l, it induces dose-related tonic contractions which are totally and reversibly abolished by indomethacin as well as by the prostaglandin antagonist, polyphloretin phosphate, but not by atropine, morphine and tetrodotoxin. This indicates that amodiaquine exerts both a direct muscular non selective ileal sensitization to various agonists and, but at higher concentrations, a contractile effect apparently dependent on prostaglandin synthesis and release. At even higher concentrations (5.4 . 10(-6) mol/l) an effect of amodiaquine on acetylcholine release was demonstrated by the observation of phasic contractions inhibited by atropine, morphine and tetrodotoxin. These effects are different from those found by us with several other antimalarial compounds in the same preparation.

Amodiaquine↗

PubMed1979

Mobilization of stored calcium for phasic contraction induced by norepinephrine in rabbit aorta.

In Ca-free solution norepinephrine (NE) produced only a phasic contraction in the media-intima layer of rabbit aorta. The second application of NE was almost ineffective. Incubation of the muscle with Ca for a short period (Ca loading) restored the ability to produce a phasic contraction in Ca-free solution. Various ions and compounds were applied to the muscle prior to the Ca loading or prior to NE application and it was found that these treatments variously affected the NE-induced phasic contraction. The data suggest that the NE-induced phasic contraction in Ca-free solution results from Ca release from cellular sites and that a hyperbolic relationship exists between the amount of Ca at these sites and the magnitude of the contraction. These sites take up extracellular Ca by a process sensitive to La3+ but not to D600; the Ca influx stimulated by high K solution, which is sensitive to D600 and also contributes to refilling of these sites; NE releases this stored Ca by a process sensitive to procaine, caffeine and theophylline and, in this manner, elicits a phasic contraction.

Animals↗

PubMed1977

[The effect of local anaesthetics on uterine blood flow and O2-consumption in pregnant sheep (author's transl)].

The local anesthetics bupivacaine, etidocaine, lignocaine and chloroprocaine were infused intravenously for 30 min to pregnant sheep, prepared for chronic studies. The amide compounds reached highere plasma concentrations than chloroprocaine. All local anaesthetics decreased uterine blood flow and O2 consumption without marked alterations of arterial or uterine venous blood gases. These changes were within the wide physiological range of variation, which was established in controls during 24 h. The findings may be of significance during paracervical block or pathological states of UBF or fetal homeostasis.

Anesthetics, Local↗

PubMed1956

Benzathine penicillin G in the treatment of syphilis.

Post-treatment observation of two years' duration has confirmed preliminary data which indicated that a single injection of 2.5 million units of benzathine penicillin G, in early infectious syphilis, produces results equal, if not superior, to those obtained with schedules employing 4.8 million units of procaine penicillin and aluminium monostearate.Preliminary data suggest that a single injection of 2.4 or 2.5 million units of benzathine penicillin G may be inadequate for the treatment of asymptomatic neurosyphilis.Delayed reactions do not appear to be induced by the long-sustained blood-levels following the administration of benzathine penicillin G.Repeated injections of PAM increase the risk of reaction to treatment.

Communicable Diseases↗

PubMed1983

Denzimol, a new anticonvulsant drug. I. General anticonvulsant profile.

The anticonvulsant profile of N-[beta-[4-(beta-phenylethyl)phenyl]-beta-hydroxyethyl]imidazole hydrochloride (denzimol, Rec 15-1533) has been evaluated in mice, rats and rabbits in comparison with some standard antiepileptic drugs. Denzimol suppressed electrically and chemically induced tonic seizures but did not prevent the clonic ones. In mice and rabbits the anticonvulsant activity of denzimol against maximal electroshock seizures was almost equal to that of phenytoin and phenobarbital with more rapid onset of action, whereas in rats the compound resulted in being the most potent and the less toxic one showing a longer duration of anticonvulsant activity than phenytoin. In the maximal pentetrazol seizures test in rats denzimol showed a profile similar to that of phenytoin and carbamazepine, but different from that of barbiturates and benzodiazepines so that it is suggested that its clinical application would be that of "grand mal" and psychomotor type seizures therapy.

Animals↗

PubMed1986

5-Hydroxytryptamine delays relaxation time of norepinephrine-induced vasoconstriction.

The effect of low concentration of 5-hydroxytryptamine (5-HT; 0.03-0.3 microM) on cellular and extracellular Ca2+ -dependent norepinephrine (NE; 5 microM)-induced vasoconstriction was assessed in isolated perfused rabbit ear artery. The most remarkable effect of 5-HT is a concentration-dependent enhancement of the duration of the extracellular Ca2+ -dependent NE-induced vasoconstriction. This effect of 5-HT is still present in 6-hydroxydopamine-pretreated arteries and in the presence of deoxycorticosterone and is not mimicked by the K+ channel blocker tetraethylammonium. Administration of nifedipine (0.3 microM) and EDTA (1 mM) failed to antagonize 5-HT-induced prolongation of relaxation kinetics of extracellular Ca2+ -dependent NE-induced vasoconstriction. On the other hand, this phenomenon was abolished by caffeine (15 mM) and markedly reduced by dibutyryl cyclic AMP (3 mM). 5-HT (0.3 microM), but not NE (30-50 nM), enhanced the vasoconstriction elicited by caffeine (15 mM) that was procaine sensitive and unaffected by nifedipine. These results suggest that 5-HT prolonged relaxation kinetics of NE-induced vasoconstriction through an impairment of cellular mechanisms that decrease the myoplasmic level of free Ca2+. A similar mechanism could be of relevance for 5-HT enhancement of vascular smooth muscle responsiveness to vasoactive agents.

Animals↗

PubMed1987

Ultralong-lasting nerve block: triethyldodecyl ammonium bromide is probably a neurotoxin rather than a local anesthetic.

The profile and duration of action of triethyldodecyl ammonium bromide (TEA-C12) on natural spike activity of rabbit aortic nerve was examined. To study the profile of action, a segment of the aortic nerve of anesthetized rabbits was placed in a perfusion chamber and exposed to increasing concentrations of TEA-C12 and, for comparison, of procaine. Total nerve activity was recorded continuously and its change related to drug concentrations (concentration/effect curves). The half-lives of onset time after drug administration and recovery following drug-washout were also determined. To study the duration of conduction block induced by TEA-C12, the aortic nerve of anesthetized rabbits was exposed to a concentration slightly higher than the minimal blocking concentration for an average time of 130 min after complete conduction block occurred. Three to 40 days later, the nerves were examined both neurophysiologically and neuropathologically. TEA-C12 blocked nerve activity in a concentration-related manner, as did procaine; however, the onset time (t1/2) was much slower for TEA-C12 (9.2 min) than for procaine (2.2 min). Most importantly, TEA-C12 block could not be reversed within 9 h of drug-washout, whereas all the procaine-blocked nerves completely recovered (t1/2 = 3.0 min). Nerve activity was completely blocked by TEA-C12 and nerve block was accompanied by severe morphological damage with complete loss of myelinated nerve fibers and severe axonal edema of the remaining axons for about 4 weeks. Nerve function completely recovered, but with only partial morphological restoration between day 30 and 40 after the initial block.(ABSTRACT TRUNCATED AT 250 WORDS)

Action Potentials↗