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At least 109 records · Page 6Linked to original sources
PubMedDate not supplied

[Study of the effect of rimantadine on the course of mixed viral-bacterial infection in albino mice].

The results of the study of rimantadine effectiveness in a viral-bacterial infection in white mice caused by a mixture of influenza A2 virus (10 LD50) and hemolytic streptococcus group A (350 million bacteria). The drug showed no prophylactic or therapeutic effect in the mixed infection, whereas in influenza infection in the animals which served as a positive control rimantadine had marked antiviral activity (P less than 0.001). It is assumed that the lack of the drug effectiveness against the mixed infection is due to the formation in the animals of virus-microbe complexes which are conducive to an increase of infectious virus titers and virus resistance to various treatments.

Adamantane↗
PubMedDate not supplied

Metabolic reduction of 1-nitrosoadamantane by rabbit liver microsomes. Properties of a C-nitroso reductase system.

Washed microsomes from rabbit liver reduced 1-nitrosoadamantane to N-hydroxy-1-aminoadamantane in the presence of a cofactor solution under aerobic conditions; no further reduction of the hydroxylamino metabolite to 1-aminoadamantane (amantadine) occurred. Reduced pyridine nucleotide cofactors are needed for the metabolic reduction. The rate of formation of N-hydroxy-1-aminoadamantane depended upon the microsomal protein content, the time of incubation and the concentration of 1-nitrosoadamantane incubated. The metabolic reduction occurred in air as well as under nitrogen or carbon monoxide. Cupric chloride, mercuric chloride, cysteamine, FAD, and FMN decreased significantly the C-nitroso reductase. The properties of the C-nitroso reductase differed from those of other microsomal reductive pathways.

Adamantane↗
PubMed1977

Induction of the platelet release reaction by 1.3-dimethyl-5-aminoadamantane, a new adamantane derivative.

The amantadine derivative 1.3-dimethyl-5-aminoadamantane, D 145, induces in high concentrations of 2-10 mM the release reaction. Adenine nucleotides and 5-hydroxytryptamine (5-HT) are liberated to the same extent and in the same ratio as found after thrombin-induced release. The time course of release is very slow; maximal release is reached in 15-20 min. The process is temperature-dependent and dependent on energy derived from glycolysis and oxidative phosphorylation. Extracellular Ca++ does not promote the release process. D 145, in accordance with the mother-substance amantadine, inhibits 5-HT uptake non-competitively, KI = 0.15mM. In concentrations of 0.1-1 mM D 145 triggers only the liberation of 5-HT, adenine nucleotides are not liberated. The ADP induced platelet aggregation is completely inhibited after preincubation with a 1 mM solution of D 145.

Adamantane↗
PubMed1977

[Antiviral agents / 9th communication: virustatically active N-(1-adamantyl)-thiourea derivatives based on cyclic secondary amines (author's transl)].

By nucleophilic addition of pyrrolidine (2a), piperidine (2b), 3-hydroxypiperidine (2c), and 4-hydroxypiperidine (2d) on 1-adamantyl-isothiocyanate (1), the N',N'-disubstituted N-(1-adamantyl)-thiourea derivatives 3a, 3b, 3c, and 3d are accessible. Particularly 3d exhibits remarkable antiviral activity vaccinia and herpes virus.

Adamantane↗
PubMed1979

[Pharmacological study on treptilamine in man/study on tolerability (author's transl)].

N,N-Diethyl-N-(2-[alpha(tricyclo[2,2,1,0(2,6]hept-3-ylidene)-benzyloxy]-ethyl)amine hydrochloride (treptilamine) which in experiments on animals showed distinct spasmolytic effects, has been investigated first in 6 volunteers with regard to compatibility using different doses p.o. and i.v. In connection with this previous study a double blind study including placebo was performed for verification of the observed effects. In the plot study 30, 40 and 50 mg were applied orally and 10, 15 and 20 mg treptilamine were used i.v. The double blind study was designed for 20 volunteers at dosages of 40 mg p.o. and 15 mg i.v. against placebo. In the pilot study systolic blood pressure decreased significantly 5 to 15 min after i.v. application of the substance for 5 or 30 min. The range of accommodation was restricted depending on the dose used. No alteration of circulation was observed after oral application at any dose. All volunteers felt tired. A significant decrease of systolic blood pressure (15 mmHg for 10 min immediately after application) occurred after 15 mg of substance were applied i.v. in the double blind study. No effect on circulation could be seen after placebo. The range of accommodation was restricted in a significant way both after i.v. application (40%) and after oral application (30%). Two of five volunteers recorded a burning sensation in the venous wall which was followed by drowsiness. One volunteer felt increasingly tired after oral application. No influence of the substance could be seen on the clinicochemical parameters examined.

Accommodation, Ocular↗
PubMedDate not supplied

[Use of rimantadine in familial foci during an epidemic of influenza caused by A1 virus].

The therapeutic and prophylactic efficacy of rimantadine in familial foci during influenza A1 outbreaks was studied. The observations included 28 experimental foci and 26 control (altogether 146 subjects varying in ages from 4 to 71 years). The foci were selected at random (the alphabet principle). In the experimental foci the patients were treated with rimantadine given in single doses of 300 mg on the first day, 200 mg on the second, and 100 mg each on the 3rd and 4th days. The contacts were also given rimantadine, 100 mg each for 7 to 10 days. In the control foci the patients received symptomatic drugs and contacts were only observed by physicians. Rimantadine was shown to be effective therapeutically if the treatment was started on the first day of the disease. As compared with the control group, in the treated patients the temperature became normal and the main symptoms of the disease regressed within shorter periods of time. The prophylactic effect was also positive: in experimental foci repeated diseases occurred only in 3 subjects (6%) and in controls 13 subjects (30%). The prophylactic effectiveness of the drug is also indicated by a decline in the number of inapparent forms: in experimental foci 26%, in control 56%. The drug may be recommended for treatment and prevention of influenza in familial foci when the disease is caused by A1 virus.

Adamantane↗
PubMed1976

On the structure-activity relationship of antiviral substances.

The significance of the study on structure-activity relationship in the antiviral substances is considered for: 1. directed synthesis of highly active and selective antivirals; 2. elucidation of the mechanism of action of antiviral substances by revealing the chemical structures which determine the inhibition of a given step in the virus growth cycle. The basic trends in conducting directed synthesis of antiviral substances are pointed out: synthesis of new inhibitors with a broad antiviral spectrum, as well as improvement by structural modifications of known ones. The basic methodological approaches in the structure-activity studies are considered. A classification of the available antiviral synthetic substances is presented.

Anti-Bacterial Agents↗