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Eksp Klin Farmakol [journal]
- [Molecular mechanisms of action of bisphosphonates and strontium ranelate]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):43-6.
Bisphosphonates are chemical analogs of isoprene lipids, which competitively decrease the activity of farnesyl diphosphate synthase in osteoclasts and thus retard prenylation. The non-prenylated small GTPases cannot attach to the membrane of osteoclasts, which decreases their resorptive function and accelerates apoptosis. Strontium ranelate activates the Wnt signal pathway (with participation of calcium-sensitive receptor), increases the replication activity (by changing the function of RANKL/RANK/OPG system) thus suppressing the apoptosis of osteoblasts, and retards the resorptive function by accelerating the apoptosis of osteoclasts.
- [Study of the influence of original multicomponent gels on the process of pathological scar formation using new methodological approach]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):38-42.
A new method of the quantitative macroscopic assessment of the process of a complex infected wound healing has been created. It was verified by example of the influence of original multicomponent gels consisting of cycloferon, amino acid glycine, glycyram (ammonium salt of glycyrrhizic acid), and vegetable oils on the process of infected wound healing and pathological scar formation. Simultaneously, the wound healing was monitored by the conventional histomorphological method. The proposed gels more effectively prevent the formation of pathological scars in comparison to reference preparation Contractubex.
- [Possibilities of the pharmacological correction of adaptive reactions of human organism in short-term moving from middle to high altitude]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):32-7.
It was assessed the efficacy of drugs belonging to the class of actoprotectors and antihypoxants, which are prescribed for short-term adaptation of the human organism moving from middle altitude (1670 m) to high altitude (3750 m). Volunteers stayed at the middle altitude for 15 days before moving to the high altitude. Prior to climbing, upon arrival at high altitude, and on the 3rd day, the state of the CNS, cardiovascular system, red and white blood growth, and some indices of the energy exchange metabolism were assessed. Drugs or placebo were administered in tablets after the first testing (one hour before moving to high altitude), upon arrival at altitude (next day, after breakfast), and on the third day (one hour before last testing). It is established that a combination of metaprote and ladasten (in doses of 0.125 and 0.1 g, respectively) favors acceleration of the short-term adaptation, which is manifested by the improved tolerance of physical activity at high altitude and the acceleration of white and red blood growth. In case of the combined administration of both actoprotectors, the adaptive reactions of tolerance and blood system were more pronounced in comparison to the administration of hypoxen (0.5 g) alone. A distinguishing feature of the reaction of the human organism upon taking the combination of actoprotectors was that adaptation of the energy supply system (judging from metabolites studied) already took place in the first hours of staying at high altitudes, while the adaptation upon taking 0.5 g hypoxen was observed on the 3rd day and the adaptive reactions in placebo group were still developing on the 3rd day.
- [Distribution of 4-methyl-2,6-diisobornilphenol in rat tissues]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):28-31.
We have studied the distribution of the new compound 4-methyl-2,6-diisobornylphenol in rats after a single oral administration in a dose of 20 mg/kg. The pharmacokinetic parameters have been estimated by the noncompartmental method. It is established that the drug is nonuniformly distributed in the body and has a high affinity for liver and heart. A low penetration of 4-methyl-2,6-diisobornilphenol has been found in brain tissue. The accumulation of 4-methyl-2,6-diisobornilphenol in adipose tissues has not been found. It been showed that the drug is slowly eliminated from the body, especially from the heart tissues for which the mean retention time is MRT = 45 h.
- [Application of immunomodulators in the treatment of mandibular fractures in elderly patients with incomplete secondary adentia]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):23-7.
The aim of the work was to study the experience of using complex pharmacotherapy in the treatment of mandibular fractures in elderly patients with incomplete secondary periodontitis, which were divided into two groups. In the first group, patients (n = 46; average age 69.0 ± 3.6) were treated using the authors' original device combined with application of antimicrobial MetrogilDenta gel onto gums two times a day during ten days. Patients in the second group (n = 52; average age 61.0 ± 3.1) were treated with the same device combined with (i) application of MetrogilDenta antimicrobial gel onto gums two times a day during ten days, (ii) application of 1.5 ml of Cycloferon 5% liniment by cotton pellet for 20 min during the same 10 days (30 minutes after the antimicrobial gel), and (iii) intramuscular injections of 6 mg of synthetic immunomodulator Polyoxidonium once a day for 3 days, then once every two days (for a total of 17 days). It is established that the use of the combination of interferon inducers of immunomodulator group--Cycloferon in the form of liniment and synthetic immunomodulator Polyoksidonium together with MetrogilDenta antimicrobial gel--led to the most pronounced regression of inflammatory and destructive processes in periodontal tissues (in 7.1%, đ = 0.05), optimized the state of local immunity of the oral cavity, and normalized microflora in periodontal pockets in elderly patients with incomplete secondary adentia.
- [Hepatoprotective effect of Hypecoum erectum extract on experimental D-galactosamine-induced damage of rat liver]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):18-22.
Hepatoprotective properties of the extract derived from the herbs of Hypecoum erectum L. have been studied on a model of D-galactosamine-induced hepatitis in rats. It is established that Hypecoum erectum extract in a dose of 50 mg/kg diminishes the development of cytolysis and cholestasis syndromes, as manifested by maximum decrease in the following indices after 7 days of the experiment: ALT activity by 26%; AST activity by 44%; alkaline phosphatase activity by 30%; β-lipoproteins by 21%; and bilirubin by 29% (p < 0.05). The Hypecoum erectum extract (i) increases the energy potential of hepatocytes, manifested by increasing the ATP content by 70% (p = 0.001) and normalizing the ratio of lactate and pyruvate in the liver homogenate; (ii) inhibits lipid peroxidation, manifested by decreasing the content of malonic dialdehyde in the liver homogenate and diene conjugates in the blood serum on the average by 30% (p < 0.05); (iii) activates the antioxidant system of the organism, increasing the catalase activity in liver homogenates by 58% (p < 0.05) and 11% and the content of reduced glutathione in the blood by 56% (p < 0.05) and 36% (p < 0.05), respectively, on the 3rd and 7th days of the experiment.
- [Cardioprotective properties of new glutamic acid derivative under stress conditions]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):13-7.
The effect of new glutamic acid derivative on the cardiac ino- and chronotropic functions has been studied in experiments on rats exposed to 24-hour immobilization-and-pain stress. It is established that glutamic acid derivative RGPU-238 (glufimet) at a dose of 28.7 mg/kg increases the increment of myocardial contractility and relaxation rates and left ventricular pressure in stress-tested animals by 13 1,1, 72.4, and 118.6%, respectively, as compared to the control group during the test for adrenoreactivity. Compound RGPU-238 increases the increment of the maximum intensity of myocardium functioning by 196.5 % at 30 sec of isometric workload as compared to the control group. The cardioprotective effect of compound RGPU-238 is 1.5 - 2 times higher than that of the reference drug phenibut.
- [Studying the neuroprotective effect of the novel glutamic acid derivative neiroglutam on focal cerebral ischemia in rats]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):8-12.
We have studied the neuroprotective effect of the novel glutamic acid derivative neiroglutam on reversible focal cerebral ischemia in rats. The neuroprotective drug action was assessed by the ability to reduce the severity of neurological deficit (1, 2, 3, 5 and 7 days), forelimb fine-motor disorders (in the ladder test), hind limb motor activity (beam-walking test), and volume of the infarct zone upon 7-day pathologic exposure. It was found that the therapeutic administration of neiroglutam (26 mg/kg, i.p., for 7 days) reduces the volume of necrosis of cerebral tissues in case of focal brain ischemia in animals (on the average by 38%, (p < 0.05) and decreases the severity of motor disorders, which indicates the presence of neuroprotective effect of this compound.
- [Effect of S-amlodipine nicotinate on the cerebral circulation in rats under conditions of ischemic and hemorrhagic brain injury]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(9):3-7.
We have performed a comparative study of the effects of S-amlodipine nicotinate and nimodipine on the local cerebral blood flow were studied in intact rats and those with model ischemic and hemorrhagic brain injury. It is established that S-amlodipine nicotinate produces a somewhat more pronounced enhancement of cerebral blood flow in rats with ischemic and hemorrhagic brain injury than in intact animals. In addition, S-amlodipine nicotinate significantly exceed nimodipine with respect to cerebrovascular activity in rats with brain pathology of both ischemic and hemorrhagic nature.
- [Experimental study of pinostrobine oxime biotransformation]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):39-44.
We have experimentally studied pathways of elimination of an oximized derivative of phytoflavonoid pinostrobine by HPLC/mass spectrometry. Four potential metabolites of pinostrobine oxime have been found and there was an attempt to determine their molecular structures on the basis of their fragmentation under positive electrospray ionization conditions. It is established that pinostrobine oxime is removed from the organism mainly unchanged and also in the form of glucuronated derivative.