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Eksp Klin Farmakol [journal]
- [Efficiency of remaxol in preventing unwanted side effects of the antiviral therapy in patients with chronic hepatitis C]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):44-6.
The article briefly addresses issues pertaining to the problem of complications encountered in antiviral therapy of patients with chronic hepatitis C. Data on the effectiveness of remaxol as a means of preventing the development of complication in patients with chronic viral hepatitis C in early stages of antiviral treatment.
- [Effect of cytoflavin on some physiological values in patients with toxicohypoxic encephalopathy]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):40-3.
The effect of cytoflavin upon bolus intravenous administration on the state of hemodynamic values and liquid sectors of the organism was studied in patients with toxicohypoxic encephalopathy caused by heavy acute poisoning. It is established that the bolus administration of cytoflavin is less effective than dropwise intravenous injection.
- [In vivo evaluation of the metabolic ratio of CYP2C9 and CYP1A2 drug markers after administration of afobazole in comparison to standard inducers and inhibitors of cytochromes]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):36-9.
The effect of subchronic peroral administration in effective doses of afobazole (5 mg/kg), and cytochrome P450 inductors (rifampicin, 13.4 mg/kg; phenytoin, 10.4 mg/kg) and inhibitors (fluconazole, 35.7 mg/kg; ciprofloxacin, 44.0 mg/kg) on the metabolic ratio (MR) of drugs-markers of CYP2C9 and CYP1A2 activity was studied in rats. Afobazole did not change the MR of compounds metabolized by the P450 isoforms studied. After peroral administration of standard P450 inductors and inhibitors, statistically significant bidirectional effects were identified, which demonstrated the expedience of administering a complex of selected compounds, markers, and CYP2C9 and CYP1A2 activity modificators for comparative evaluation of the effects of new drugs in rats. It is recommended to evaluate the activity of CYP1A2 by determining the MR for one of two caffeine metabolites, paraxanthine or theobromine, and the activity of CYP2C9 by determining the MR of metabolite Exp-3174 to losartan.
- [Pharmacokinetic evaluation of a new prolonged dosage form of afobazole in comparison to commercially available tablets]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):33-5.
Afobazole pharmacokinetics upon oral administration of tablets prepared according to various technologies was studied in rabbits. The main pharmacokinetic parameters were determined.
- [Estimating the anti-inflammatory activity of drugs by changes in the agranulocyte/granulocyte index]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):28-32.
It is suggested to assess the anti-inflammatory activity using the ratio of the sums of agranulocytes and granulocytes. On the model of carrageenan-induced inflammation in the rat limbs, the anti-inflammatory activity of NSAIDs and their combinations with antihypoxants was characterized in terms of limb size, leukogram, and the proposed index of anti-inflammatory activity. A high anti-inflammatory activity was observed for a combination of hypoxen with diclofenac and acetylsalicylic acid and a combination of metaprot with diclofenac.
- [Effect of 3-oxypyridine and succinic acid derivatives on clinical manifestations of inflammatory diseases of the uterus and its appendages]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):23-7.
Two-week-long, prospective, placebo-controlled, single-blind randomized study of the effects of intravenous emoxipin (150 mg daily), reamberin (400 ml daily) and mexidol (300 mg daily) infusion on the dynamics of clinical symptoms of non-complicated recrudescence of inflammatory diseases of the uterus and its appendages (IDUA) in comparison to the standard therapy was performed. It was established that emoxipin, reamberin and mexidol administration appreciably improved the clinical state dynamics of women with recrudescence of IDUA. The effect was associated with more pronounced decrease in severity of genital and abdominal symptoms versus standard therapy results.
- [Study of tolerance of central muscarinic receptor blockers]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):19-22.
The tolerance of five central muscarinic receptor antagonists has been studied in experimental animals. According to the effect on orientation-exploratory reaction, drugs were arranged in the following order of increasing toxicity: procyclidine < trihexiphenidyl < benactizine < atropine < scopolamine. For the same therapeutic index, trihexiphenidyl and benactizine were characterized by the maximum tolerance (TD50/ED50 > 10) in mice. Scopolamine and atropine exhibited anticonvulsant activity at doses exceeding the threshold values by a factor of 6.3 and 3.9, respectively. For procyclidine, the average anticonvulsant dose was threefold lower than the threshold value. Benactizine and procyclidine had maximum tolerance levels in rats. The TD50/ED50 ratio for these drugs was greater than 3 (against 0.5 - 0.7 in groups treated with trihexiphenidyl, atropine and scopolamine).
- [Anticonvulsant and neuroprotective effects of cyclopentyladenosine on the model of convulsive status in rats]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):13-8.
The neuroprotective and anticonvulsant effects of cyclopentyladenosine (CPA) have been studied on a new experimental model of the convulsive status in rats aged 3-4 months and 10 days. The convulsive status was modeled by intracerebroventricular injection of ferakril (water-soluble polymer of polyacrylic acid) solution. It is established that prophylactic administration of CPA results in a relatively lower degree of neurological deficit, both in the acute phase and on the next day, compared to the untreated control. Considering that adenosine receptor agonists are analogs of the natural metabolites that have minimal side effects and expressed neuroprotective properties, the use of agents of this group is perspective for both prevention and treatment of seizure conditions in neurology and neurosurgery.
- [Some aspects of the psychostimulant effect of a phenyl derivative of glutamic acid (RGPU-135, glutarone) in experimental animals]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):7-12.
Hydrochloride of beta-phenylglutamic acid (RGPU-135, glutarone, neuroglutamine) administered in dosis 13 mg/kg and 26 mg/kg doses increases exercise performance of outbred mice in repeated forced dynamic load test, reduces the intensity of fatigue, and accelerates adaptation to loading. In contrast, beta-phenylethylamine (20 mg/kg) under the same conditions decreases the exercise performance and adaptation capacity and accelerates the development of fatigue. The RGPU-135 compound, similar to typical psychostimulants, in a dose of 26 mg/kg increases the spontaneous motion activity of inbred C57BL/6 mice with the active phenotype of stress response, but not in the BALB/c line mice with the passive phenotype. The RGPU-135 exhibits a psychostimulant activity without an "exhaustive" effect characteristic of psychostimulants.
- [The antiamnestic effect of nootropic substances in rats]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2013; 76(11):3-6.
It has been established in experiments in rats that some nootropic substances (oxyracetam, aniracetam, nooglutil, mexidol, new 3-hydroxypyridine derivative SK-170, piracetam and noopept) produce marked antiamnestic effect on various models of amnesia (induced by microwave irradiation, acute hypoxia, and motion sickness). At the same time, meclophenoxate exhibited antiamnestic effect in the first and second models of amnesia, while 9-aminoacridine derivative HTOS-404 was only effective in the model of amnesia caused by microwave irradiation. The antiamnestic effect of nooglutil and SK-170 was caused to a significant degree by activation of non-NMDA receptors of excitatory amino acids (generally AMPA receptors), while the effect of mexidol was related to GABA(A) receptors.