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The effects of dyadic combinations of endodontic medicaments on microbial growth inhibition.

In recent years dyadic combinations of endodontic medicaments have been used increasingly in clinical pediatric dentistry with little regard to the possibility of pharmacological antagonism of the components. In this investigation, a microbial growth inhibition assay was used to determine changes in antimicrobial activity in dyadic mixtures of endodontic medicaments. The combinations assayed were Ledermix (corticosteroid-antibiotic) and Calyxl (calcium hydroxide), Ledermix and Kri (iodoform), Kri and Calyxl, and formocresol and eugenol. All these compounds have antibacterial activity when used individually. In the dyadic combinations assayed, results showed that adding calcium hydroxide to another antibiotic preparation has deleterious effects on growth inhibition, and combining any two antimicrobial medicaments produces no additive or synergistic effects. It is concluded that it may be clinically advantageous to use endodontic medicaments in the dyadic combinations shown in this investigation.

Analysis of Variance↗

[Treatment of pulp diseases in milk teeth with chlorocamphomenthol].

The results of treatment with chlorcamphomenthol are assessed clinically in cases of grade II pulpopathy in milk molars of children aged from 3 to 9 years. Out of 64 teeth examined after 1 to 4 years in 60 cases (93.7%) the clinical condition of the tooth was satisfactory, and in 4 cases the tooth was lost. A high percent of good results encourages to the use of chlorcamphomenthol in endodontic treatment of milk teeth.

Camphor↗

Omega-dialkylaminoalkyl ethers of 3-exo-dialkylamino-(Z)-camphoroximes with antiarrhythmic and local anesthetic activities.

The synthesis of 3-exo-dialkylamino-(Z)-camphoroximes 7 starting from a mixture of 3-endo- and 3-exo-bromocamphornitrimine, hydroxylamine hydrochloride and excess secondary amine (dimethylamine, pyrrolidine, piperidine or morpholine) is described. Compounds 7 gave a series of omega-dialkylaminoalkyl ethers 9, 10 and 11 by reaction of 7 as sodium salts with omega-chloroalkyldialkylamines in DMF solution. Some of compounds 9, 10, 11 showed an appreciable antiarrhythmic and local anesthetic activity in rats and mice, respectively.

Amines↗

Spin state transitions of liver microsomal cytochrome P-450.

Spin state transitions of membrane-bound cytochrome P-450 were investigated by difference spectrophotometry using the 'D'-charge transfer absorbance band at 645 nm as a measure of the amount of hemin iron present in the 5-coordinated state. The magnitude of the 'D'-absorbance band in the absence of exogenous substrates, e.g., the concentration of native high spin cytochrome P-450, was evaluated from the difference in absorbance at 645 nm between ferric cytochrome P-450 and the carbon monoxide derivative of the pigment in its ferrous state. The contribution of the native high spin species to the total cytochrome P-450 content of microsomes was calculated to be between 40% and 65% after induction with phenobarbital and polycyclic hydrocarbons, respectively. Up to 80% of the cytochrome P-450 was found to be present in the high spin state after the addition of exogenous substrates. Further, the steady state concentrations of high spin cytochrome P-450, observed in the presence of reduced pyridine nucleotides, suggest that the rate limiting step for microsomal mixed function oxidation reactions is variable and dependent on the substrate under investigation.

Animals↗

[Enhancement of absorption of tetramethylpyrazine by synthetic borneol].

Sprague-Dawley rats were given ig tetramethylpyrazine phosphate (TMP) 5 mg/kg with or without previous borneol 5 mg/kg. The plasma TMP concentrations were analysed by GC method, and the data were treated by NONLIN program. The Cmax were 931 and 562 ng/ml, respectively, (P less than 0.01); while the AUC were 68,849 and 37,174, respectively, (P less than 0.05). It is suggested that the borneol enhances the absorption of the TMP but not in elimination.

Absorption↗

Endodontic treatment of infected primary teeth, using Maisto's paste.

A method of endodontic treatment, using a modification of Maisto's paste, is suggested for preservation of infected primary teeth. Adding more zinc-oxide reagent and other anti-bacterial materials to the original Walkhoff's paste (Kri 1), for pulp canal medication and final filling, seems to improve the pharmacological effect of the paste by reducing the resorption rate. The literature is reviewed and a case with a follow-up time of three and a half years is described, in which the tooth remained stable.

Anti-Infective Agents, Local↗

[Therapy of chronic apical periodontitis in traumatically injuring front teeth with ongoing root growth].

Because of the patient's age and the width of the apical foramen, conventional or surgical root canal fillings are frequently not indicated for the treatment of chronic apical periodontitis in teeth whose roots have not yet fully grown. Therefore resorbable paste fillings are applied either to induce deposition of apical hard substance or to bridge the time until root canal filling is possible. In a comparative clinical and radiological study in 171 young patients, Walkhoff's iodoform paste and calcium hydroxide were examined with regard to their inductive effect on the formation of an apical hard substance barrier.

Adolescent↗

The role of hydrogen-bonds in drug binding.

Hydrogen-bonds play a crucial role in determining the specificity of ligand binding. Their important contribution is explicitly incorporated into a computational method, called GRID, which has been designed to detect energetically favourable ligand binding sites on a chosen target molecule of known structure. An empirical energy function consisting of a Lennard-Jones, an electrostatic and a hydrogen-bonding term is employed. The latter term is found to be necessary because spherically symmetric atom-centred forces alone may not adequately reproduce the geometry of two interacting molecules. The hydrogen-bonding term is dependent on the length and orientation of the hydrogen-bond. Its functional form also varies according to the chemical nature of both the hydrogen-bond donor and acceptor atoms, and has been modelled to fit experimental observations of crystal structures. The mobility of the hydrogen-bonding hydrogens is considered analytically in calculating the hydrogen-bond energy. The hydrogen-bonding energy functions will be described and their application will be demonstrated on molecules of pharmacological interest where hydrogen-bonds influence the binding of ligands.

Camphor 5-Monooxygenase↗

Single turnover kinetics of the reaction between oxycytochrome P-450cam and reduced putidaredoxin.

A study of the single turnover kinetics of the reaction between oxycytochrome P-450cam and reduced putidaredoxin was performed using the inhibitor metyrapone to trap the cytochrome immediately after release of the product, 5-exo-hydroxycamphor. EPR determinations of the concentrations of reduced putidaredoxin and ferric metyrapone-bound cytochrome at the same time points showed that there is no time lag between the oxidation of reduced putidaredoxin and the appearance of metyrapone-bound cytochrome. This implies that the rate constant for electron transfer is smaller than the rate constant for the later processes involved in product formation and release, lumped into a single step. Taking this restriction into account and doing computer simulation of absorbance versus time curves, previously obtained at various putidaredoxin concentrations using stopped-flow spectrophotometry, allowed bounds to be determined for rate constants of the processes within the reaction. At 4 degrees C in buffer at pH 7.4 with 0.50 M KCl, the rate constant for the bimolecular association of the two enzymes is between 3 and 20/microM.s; the rate constant for dissociation is between 12 and 600/s; the rate constant for electron transfer is between 60 and 100/s; and the rate constant for the later processes is at least 200/s.

Camphor 5-Monooxygenase↗