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The aim of this study was to evaluate the pharmacokinetics and pharmacodynamics of tapentadol (TAP) in red-eared slider turtles after a single intramuscular injection of 5 mg/kg. Turtles (n = 9) were randomly assigned to two treatment groups, according to an open, single-dose, single-treatment, unpaired, two-period crossover design. Group A (n = 5) received a single IM dose of TAP (5 mg/mL) at 5 mg/kg. Group B (n = 4) received a single IM injection of saline (equivalent to the opioid in volume). After a one-month wash-out period, the groups were rotated, and the experiment was repeated. TAP plasma concentrations were evaluated by a validated HPLC-FL method, while an infrared thermal stimulus was applied to the plantar surface of the turtles’ hind limbs to evaluate the thermal withdrawal latency (TWL). TAP plasma concentrations were detectable between 1 and 24 h (2141 – 42 ng/mL, respectively). The TAP-treated group showed a dramatic increase in TWL one hour after drug administration (15.31 ± 4.73 s). Subsequently, TWL decreased with time. Significant differences between the treatment and control groups were apparent up to 10 h following treatment. A linear relationship (r2 = 0.98) between the TAP plasma concentration and effect was found. Given these qualities, TAP appears to be an attractive option for antinociception in turtles because of its rapid onset and acceptable duration of effect.
Cimicoxib (CX) is a new non-steroidal anti-inflammatory drug from the “coxib” family, designed for dogs. In the available literature there is little information on the pharmacokinetics of CX. The aim of this study was to evaluate the effect of food intake on the pharmacokinetic characteristics of cimicoxib. Additionally, the pharmacokinetic profile after the administration of precise doses of CX (2 mg/kg b.w.) and an approximate dose (i.e. 80 mg tablet for animals of about 40 kg) were estimated. CX concentrations were determined by a HPLC validated method. The results of pharmacokinetic analysis were similar in both studies, regardless of the dose and the degree of filling of the gastrointestinal tract (fasted, fed). In addition, we estimated the duration of the minimum effective concentration (MEC), which turned out to be similar for all the concentrations tested. The results show that neither small variations in dosage nor the presence of food in the gastrointestinal tract change the therapeutic efficacy of the analgesic in terms of its blood concentration.
Diarrhea is a condition which causes malabsorption and dehydration. Recently, the anti-motility effect of several herbal compounds for the treatment of hypermotility-induced diarrhea has been studied. The root of Platycodon grandiflorum has been widely used in oriental medicine for the treatment of various chronic inflammatory diseases. The aim of the present study was to assess the effects of Platycodin D (PD), the major triterpene saponin in the root of P. grandiflorum, on gastrointestinal (GI) motility by assessing both gastric emptying (GE) and intestinal transit (IT) in mice with different treatment protocols. Mice were randomly allocated to 5 groups (n = 15/group) according to their treatment protocols (control, administered with antikinetics: atropine, dopamine, or with pro-kinetics: itoride, bethanechol) for each GE and IT test. Each group was subsequently divided into 3 subgroups (n = 5) pre-treated with different PD doses (0, 2.5, and 5 mg/kg). Pre-treatment with PD in the control treatment group of mice showed reduced GE and IT in a dose-dependent manner. At the maximum PD effect, GE and IT were reduced by 63% and 50%, respectively, compared with those in the normal control group. In the groups given atropine or dopamine, pre-treatment with PD further reduced GE and IT by 35% to 58%, respectively. The PD pre-treatment dramatically reduced the GI motility enhanced by itopride and bethanechol. On the whole, these results suggest that PD treatment might be beneficial in motility-induced diarrhea.
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