scholarly journals Effect of moxifloxacin on pharmacokinetics of enalapril in rats

2021 ◽  
Vol 292 ◽  
pp. 03063
Author(s):  
Zhao Jing ◽  
Peng Jiarui ◽  
Zhang Yinxia

The purpose of this study was to investigate the effect of moxifloxacin on the pharmacokinetics of enalapril. Single administration experiment: 12 Wistar rats were randomly divided into two groups on average. Control group: enalapril (15mg/kg)+ normal saline combined group: enalapril (15mg/kg)+ moxifloxacin (80mg/kg), intragastric administration. Blood samples were measured by LC-MS/MS. Multiple administration experiment: 12 Wistar rats were randomly divided into two groups on average. The control group was given normal saline (day1-7)+ enalapril (day8,15mg/kg), and the combination group was given moxifloxacin (day1-7, 80mg/kg)+ enalapril (day8,15mg/kg) by intra-gastric administration. The treatments were the same as above. Pharmacokinetics parameters were calculated using Winnonlin 6.1 software and the two groups were compared using SPSS18.0 software. In single administration experiment compared with the control group, the AUC(0-t) and Cmax of enalapril were decreased by 31.99%(P<0.05), 42.57% (P<0.05) in the combined administration group. Quinolone antibiotics and ACEI drugs should not be taken at the same time during clinical treatment to avoid drug interactions that may occur when combined drugs are used.

Author(s):  
Sandeep Kumar Bandapati ◽  
Karuna Sree Podila ◽  
Yadala Venkata Rao

Background: Pain is an unpleasant sensation with varying subjective experience. Its management is always challenging for physicians particularly in case of chronic pain. Chronic pain and depression usually co-exist due to poor quality of life and increase in health care costs posing an individual to suffer from depression. Anti-depressants for pain management are being used successfully using since years. In this study venlafaxine, a newer anti-depressant drug was evaluated for anti-nociceptive activity, tail immersion test an analgesic animal model of albino mice.Methods: Randomly selected albino mice of either sex with reaction time of <6 seconds were included in the study and divided into 7 groups with 6 mice in each group. Grouping was done based on the drug received i.e., venlafaxine 15, 30 and 60 mg/kg, tramadol 10 and 20 mg/kg, control group (normal saline) and combination group venlafaxine 15 mg/kg+tramadol 10 mg/kg. Drugs were administered by intra-peritoneal route.Results: Venlafaxine (30 and 60 mg/kg), tramadol (20 mg/kg) and combination group venlafaxine (15 mg/kg+tramadol 10 mg/kg) has shown significant (p<0.001) increase in tail withdrawal latency compared to control group (normal saline) by tail immersion test. Venlafaxine potentiated anti-nociceptive activity of tramadol on concomitant administration with tramadol. Venlafaxine at 60 mg/kg has comparable anti-nociceptive effect to tramadol at 20 mg/kg.Conclusions: Venlafaxine at doses of 30 and 60 mg/kg is having anti-nociceptive effect, but less potent than tramadol.


Author(s):  
Rekha M. B. ◽  
Basavaraj Bhandare ◽  
Satyanarayana V. ◽  
Hemamalini M. B.

Background: Diabetes mellitus is a chronic metabolic disorder that develops due to insulin deficiency or insulin resistance. Recent animal and human studies have reported bromocriptine to be effective in the management of type 2 diabetes mellitus. The present study was done to evaluate the antihyperglycemic effect of bromocriptine in dexamethasone induced hyperglycemic rats.Methods: Male wistar rats were used and divided into 5 groups. Dexamethosone was used to induce hyperglycemia in group B-E. Group A was the untreated control group, group B was the standard control group, group C was the oral 10 mg/kg of bromocriptine dissolved in 0.9% normal saline, group D was the oral 20 mg/kg metformin dissolved in 0.9% normal saline, group E was the oral 10 mg/kg bromocriptine+20 mg/kg metformin dissolved in 0.9% normal saline. Fasting blood glucose, post prandial blood glucose and body weight was estimated on day 1, 15, 30.Results: It was seen that dexamethasone induced hyperglycemia and increase in body weight in male wistar rats, which were significantly controlled by oral bromocriptine and bromocriptine with metformin combination.Conclusions: Results obtained from this study showed that bromocriptine can be a promising drug with novel mechanism to treat type 2 diabetes mellitus.


Author(s):  
VANITA KANASE ◽  
SUNITA VISHWAKARMA

Objective: The objective of the study was to evaluate the antidepressant activity of ethanolic extract of dried leaves of Lagerstroemia speciosa L. (EELS) on acute restraint stress (ARS)-induced depression-like behavior and biochemical alterations in albino Wistar rats. Methods: Thirty rats were randomly divided into five experimental groups. Group-I (normal control) rats received normal saline (2.0 ml/kg, p.o.) daily for 14 days; Group-II (stress control) rats received normal saline (2.0 ml/kg, p.o.) daily for 14 days and subjected to restraint stress on the 13th day. Group-III (standard drug-treated) rats received imipramine (15 mg/kg, p.o.) daily for 14 days and subjected to restraint stress on the 13th day. Groups-IV and V rats were treated with EELS (100 mg/kg and 300 mg/kg, p.o.) daily for 14 days subjected to ARS on the 13th day. Stress-like behavior was assessed by subjecting the rats to behavioral paradigms such as tail-suspension test (TST) and open field test (OFT), 40 min post-restraint stress procedure. Pretest of 10 min for forced swim test (FST) was also given to each rat simultaneously. Then, 23.5 h later, the relevant samples were administered and the main test performed 30 min later. Oxidative stress parameters such as superoxide dismutase (SOD), catalase (CAT), malondialdehyde (MDA), and extent of lipid peroxidation (LPO) were analyzed in restraint stress-induced animals and control group, following FST on the 15th day. Statistical Analysis: Expression of data was done as a mean standard error of the mean. The normally distributed data were subjected to one-way analysis of variance followed by Dunnett’s test. *p<0.05 was considered statistically significant. Results: It was observed that L. speciosa L. showed a significant dose-dependent decrease in duration of immobility time in TST and FST when compared with the control group in a dose-dependent manner. The results of OFT also showed a dose-dependent increase in locomotor activity. In addition to behavioral tests, EELS also normalized oxidative stress markers such as CAT, SOD, MDA, and LPO in a dose-dependent manner. Conclusion: The results suggest that the ethanolic extract of L. speciosa L. leaves possesses significant antidepressant property, may be recommended as a supplement for the antidepressant activity.


2020 ◽  
Vol 4 (3) ◽  
pp. 370-374
Author(s):  
Kasang Naman ◽  
Habibat Oseni ◽  
Emmanuel Enoh

The antianaemic potential of methanolic leaf extracts of Mucuna pruriens was investigated using phenylhydrazine (PHZ) induced anaemic albino Wistar rats.  Fifteen rats used for the study were randomized into five experimental groups. To induced anaemia, the rats (except the normal control, Group E), received 60 mg/kg of the haemolytic agent Phenylhydrazine intraperitoneally (i.p) for two consecutive days. Anaemic Wistar rats in groups A and B received a daily oral dose of 500 and 250 mg/kg of the methanolic leaf extract of Mucuna pruriens. Nweze et al. (2016) had reported a median lethal dose greater than 5000 mg/kg for the methanol leaf extract of Mucuna pruriens. Groups C and D received Vitamin B12 (10 mg/kg) and normal saline (1 ml/kg), respectively. Normal control rats also received normal saline (1 ml/kg). Extract or normal saline was administered per os (p.o) while vitamin B12 was administered i.p. for a duration of 21 days. Packed cell volume (PCV) and haemoglobin concentration were determined weekly for three weeks. The result of the study indicated that both the methanolic leaf extract of Mucuna pruriens and Vitamin B12 significantly (p < 0.05) increased the packed cell volume and haemoglobin concentrations in treated rats compared to the negative control group of rats. This indicated that the methanolic leaf extract of Mucuna pruriens has anti-anaemic properties and could be utilized in the management of anaemia


2020 ◽  
Vol 10 (2) ◽  
pp. 66
Author(s):  
Ira Widjiastuti ◽  
Setyabudi Setyabudi ◽  
Nia Nur Haliza

Background: Pulp inflammation can be treated with pulp capping by calcium hydroxide as the gold standard. Pulp capping by calcium hydroxide could causing tissue necrosis followed by inflammation. Calcium hydroxide combined with propolis which have anti-inflammatory effects through inhibition of the Nf-kB pathway and pro-inflammatory cytokines. That process will inhibit the increase of vascular permeability and neutrophil chemotaxis. Inflammatory process can accelerate by controlling the amount of neutrophil cells as a acute phase marker, so the healing process occurs more quickly. Therefore it is necessary to study the amount of neutrophil cells in the pulp perforation of Wistar rats after applicated by combination of calcium hydroxide-propolis. Purpose: To analyze the difference amount of neutrophil cells on the Wistar rats pulp perforation after applicated by calcium hydroxide-propolis combination compared with calcium hydroxide-aquadest Method: M1 tooth perforated for all groups with three types tratment: no medication (control group), calcium hydroxide-aquadest 1: 1 (P-1 group), and calcium hydroxide-propolis 1: 1.5 (P-2 group) and closed with cention. Observations were made on the 1st, and 3rd day with HE staining. Results: One Way ANOVA shown a significant difference (p <0.05) of the average amount of neutrophil cells between all treatment groups on 1st day (p=0,000) and 3rd day (p=0,000). The amount of neutrophil cells in the calcium hydroxide-propolis (P-2) combination group was lower than control group and calcium hydroxide-aquadest (P-1) group on the 1st and 3rd day. Conclusion: The amount of neutrophil cells after application of calcium hydroxide-propolis is lower than calcium hydroxide-aquadest application.


1965 ◽  
Vol 20 (3_suppl) ◽  
pp. 1049-1053 ◽  
Author(s):  
Robert G. Gibby ◽  
Robert G. Gibby ◽  
George B. Kish ◽  
George C. Theologus

The effect of strychnine sulfate upon spontaneous locomotor activity in an open field was determined for 20 naive male Wistar rats. The experimental Ss were injected ip with 1.0 cc/kg of a 01% solution of strychnine sulfate in normal saline and the control Ss received a similar injection of 1.0 cc/kg of normal saline. All Ss were given 2 trials 7 days apart in the open field, with the injections preceding the second trial. The behavioral change from Trial 1 to Trial 2 for the control group was compared with that for the experimental group. Strychnine sulfate significantly reduced spontaneous locomotor activity in rats. A significant correlation was found between scores on the first and second trials of the experimental Ss. It was suggested that the concept of “orienting-exploratory behavior” could account for reduced locomotor activity.


Author(s):  
M. A. Dodokhova ◽  
I. M. Kotieva ◽  
А. V. Safronenko ◽  
V. G. Trepel ◽  
M. S. Alkhuseyn–Kulyaginova ◽  
...  

Introduction. The aim of the study was to evaluate the effect of hybrid organotin compounds bis(3,5–di– tert–butyl–4–hydroxyphenylthiolate) dimethylol (Me3) and ((3,5–di–tert–butyl–4–hydroxyphenylthiolate) triphenylolol (Me5) on the level of markers of oxidative stress and apoptotic processes in the mitochondria during acute and subchronic intragastric administration to Wistar rats (females) in the maximum tolerated dose. Materials and methods. The objects of study were hybrid organotin compounds, the administration was carried out at the maximum tolerated dose of 2000 mg/kg (Me3) and 750 mg/kg (Me5) with a single and multiple intragastric administration. The study was conducted on 60 Wistar rats (females) weighing 190-210g. The concentration of cytochrome C (ng / g protein), caspase-9(ng / g protein), 8-hydroxy-2' — deoxyguanosine (8-OHdG) (ng/g protein), malondialdehyde (MDA) (nM / g protein)was determined in mitochondrial liver samples using test systems by enzyme immunoassay; by the biochemical method-the amount of protein (mg / ml) — by the biuretic method. Results. Me3 in both series of the experiment showed itself as a more pronounced antioxidant than Me5, which did not show its antioxidant properties. In group I animals, there were no statistically significant differences in the level of MDA and Cit C in relation to the control group, no mitDNA damage was detected, but K9 activity increased by 17%. With the introduction of Me5, the value of the MDA indicator increased by 55.5%, 8 — OHdG by 12.4% and Cit C by 66.2%. In group IV, the amount of MDA as the final product of lipid peroxidation (POL) increased by 13.6%, in group V by 22.5%. With the introduction of Me3, the level of Cit C was reduced by 23.5%, with the introduction of Me5, on the contrary, it was slightly increased. K9 activity was reduced in both experimental groups, by 9.6% and 17.3%, respectively. Discussion. Hybrid OOS containing a fragment of 2,6-di-tert-butylphenol have a dual structure. The tin-containing component is prooxidant, and the radical of the spatially hindered phenol, on the contrary, is antioxidant. It is the different ratio of the described fragments in the molecules of the substances under study, in our opinion, that led to the appearance of different degrees of influence on the metabolism of mitochondria. Conclusion. Both substances that modulate changes in oxidative stress and the activity of apoptotic processes are recommended for further research as antitumor medicinal agents.


2017 ◽  
Vol 16 (4) ◽  
pp. 65-72
Author(s):  
D. L. Sonin ◽  
I. N. Dementeva ◽  
S. G. Chefu

Objectives. The aim of the study was to investigate of the effect of administration of Notrombel, (one of the representatives of a new class of compounds, N,N'-substituted piperazines), on systemic hemodynamics and thrombin tolerance. Material and methods. The effect of daily intragastric administration for 14 days of Notrombel (0.01 mM/kg) and ASA (0.01 mM/kg) on the risk of spontaneous hemorrhages and thrombin tolerance (intravenous bolus thrombin administration at a dose of 50 units NIH/kg) was studied in male Wistar rats. The number of circulating platelets was determined before and 5 minutes after thrombin administration. The concentration of fibrinogen after 30 min was determined by the gravimetric method according to Rutberg R. A. Results. With the daily intragastric administration of Notrombel and ASA, spontaneous hemorrhages and increased bleeding were not observed. Blood pressure and heart rate did not differ from the control animals. Intravenous administration of thrombin caused thrombocytopenia and hypofibrinogenemia in all experimental animals. The severity of hypofibrinogenemia after thrombin administration was significantly less in rats treated with Notrombel (0.01 mM/kg) and ASA (0.01 mM/kg) than in the control group. There were no differences between Notreblel and ASA groups. Conclusions. Daily intragastric administration of Notrombel and ASA for 14 days did not cause spontaneous hemorrhages and were not associated with any adverse hemodynamic effect. Both Notrombel and ASA increased tolerance to thrombin. These data broaden the currently available knowledge related to the antithrombotic action of Notrombel.


2016 ◽  
Vol 19 (4) ◽  
pp. 809-817 ◽  
Author(s):  
K. Rycerz ◽  
A. Krawczyk ◽  
J. Jaworska-Adamu ◽  
M. Gołyński ◽  
K. Lutnicki ◽  
...  

Abstract Habanero pepper fruits contain capsaicin (CAP) characterised by a spicy taste. Astrocytes express vanilloid receptor (TRPV1), which interacts with cannabinoids including CAP. Only a few studies revealed that CAP leads to alterations of the arcuate nucleus (ARC) structures. The aim of this study was to analyse the GFAP (GFAP-IR) and S100β (S100β-IR) immunoreactive astrocytes of ARC in adult rats after intragastric administration of habanero pepper fruits. Adult, Wistar rats received a peanut oil – control group (C) – and oil suspension of habanero pepper fruits at a dose of 0.08 g dm/kg b.w. for 7 days – E1 group – and 28 days – E2 group. After euthanasia, the brains were embedded in paraffin blocks using a routine histological technique. Frontal slices of ARC were immunohistochemically stained for GFAP and S100β using specific antibodies in the peroxidase-antiperoxidase method. Astrocytes of ARC were morphologically and morphometrically analysed under a light microscope. The results of the study did not reveal statistically significant changes in the density of GFAP-IR cells in E1 and E2 groups of rats in comparison with group C. A statistically significant increase in the density of S100β-IR astrocytes was observed in the E1 group and a decrease in the E2 group. Astrocytes with expression of both studied proteins were characterised by morphological alterations in ARC in the E2 group. The obtained results suggest an influence of CAP contained in habanero pepper fruits on the reactivity of astroglia, which may have an impact on the astrocyte-neuron interactions in order to maintain a proper activity of nervous cells in ARC.


Author(s):  
Anton Bózner ◽  
Mikuláš Gažo ◽  
Jozef Dostál

It is anticipated that Japanese quail /Coturnix coturnix japonica/ will provide animal proteins in long term space flights. Consequently this species of birds is of research interest of international space program INTERCOSMOS. In the year 1987 we reported on an experiment /2/ in which the effect of chronic acceleration of 2 G hypergravitation, the hypodynamy and the simultaneous effect of chronic acceleration and the location in the centre of the turntable of the centrifuge on the protein fractions in skeletal muscles was studied. The ultrastructure of the heart muscle was now in this experiments examined as well.Japanese quail cockerels, aged 48 days were exposed to 2 G hypergravitation /group IV/ in a 6,4 m diameter centrifuge, to hypodynamy /group III/ and their combination /group V/, respectively for 6 days / Fig.1/. The hypodynamy in group III was achieved by suspending the birds in jackets without contact the floor. The group II was located in the centre ofthe turntable of the centrifuge. The control group I. was kept under normal conditions. The quantitative ultrastructure of myocard was evaluated by the methods of Weibel/3/ - this enables to determine the number, relative size and volume of mitochondria volume of single mitochondria, defficiency of mitochondrial cristae and volume of myofibrils.


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