The pharmacokinetic profile of selected NSAIDs in southern black rhinoceros (Diceros bicornis minor) were studied. Phenylbutazone (PBZ), meloxicam (MEL), and firocoxib (FIR) were administered orally to five captive, black rhinoceros, and blood was collected at predetermined time points for NSAID quantification and noncompartmental pharmacokinetic (PK) analysis. Phenylbutazone 4.0 mg/kg PO q12h for three doses, MEL 0.3 mg/kg PO q24h administered twice, and a single oral dose of FIR 0.1 mg/kg, were tested with a minimum washout time of 2 wk. PBZ reached a median (range) peak concentration (C_max) of 9.42 (2.74-11.5) g/ml at a mean (range) time (T_max) of 6.00 (4.00 to >12.00) h, and the median (range) elimination half-life (T_1/2) was 6.07 (3.95-6.49) h. Phenylbutazone pharmacokinetic parameters for black rhinoceros in this study were similar to domestic horses. Meloxicam reached a median (range) C_max of 0.576 (0.357-0.655) µg/ml at a median (range) time (T_max) of 6.00 (4.00-12.00) h; the median (range) T_1/2 of MEL was 14.0 (12.4-17.9) h. These results demonstrate that once-daily administration of MEL at 0.3 mg/kg resulted in a serum concentration of greater than 0.200 µg/ml from 2 to 24 h in four animals, which is within the analgesic range (0.200-0.400 µg/ml) for this drug in other species postulated by other studies. A single dose of firocoxib (0.1 mg/kg) reached a median (range) peak concentration (C_max) of 15.7 (9.65-17.3) ng/ml at a median (range) T_max of 4.00 (4.00-6.00) h. The median (range) elimination T_1/2 of FIR was 4.96 (4.47-6.51) h, which is faster than in the horse. The data suggest that extrapolation from equine FIR dosage recommendations is inappropriate for black rhinoceros.

2024-09-01·Heliyon

Investigating the impact of paclobutrazol and tannic acid on floral development of in vitro -grown cannabis plantlets

Article

作者: Arouiee, Hossein ; Ajdanian, Ladan ; Phineas Jones, Andrew Maxwell ; Pepe, Marco ; Hesami, Mohsen ; Nemati, Hossein

Gibberellic acid (GA₃) is inhibitory to floral development of in vitro cannabis plants and inhibiting GA₃ biosynthesis promotes floral development. As such, paclobutrazol (PBZ), a potent GA₃ biosynthesis inhibitor may be useful for increasing floral biomass and expediting development, but due to health concerns, its use is prohibited in cannabis production. The present study was conducted to compare the use of PBZ with tannic acid (TA), a natural compound with potential GA₃ inhibiting characteristics. Results confirmed that PBZ significantly affected the number of flowers, percentage of flowering plantlet, and flower appearance time. Treatment using PBZ at a concentration of 10 μM resulted in the greatest number of flowers (7.95) compared to other treatments. Moreover, this compound at concentrations of 5 and 10 μM yielded the highest percentage of flowering plantlets, at 75 % and 70 %, respectively. Flowers also appeared 7-15 days sooner than other treatments. Additionally, the energy transfer efficiency in the photosynthetic system and chlorophyll concentration in plants treated with PBZ were considerably higher than those under other treatments. Under the PBZ treatment, the length of internode was significantly reduced. In contrast, TA generally had the opposite effect of PBZ, suggesting that it does not act as a GA₃ inhibitor in this context. Furthermore, positive effects of TA at a concentration of 10 μM were observed on total leaf area (840.08 mm²) and stem length (40.09 mm). The highest number of leaves (12.5) was found in the presence of TA at a concentration of 100 μM. TA at its highest concentration (1000 μM) had an inverse effect on cannabis growth and flowering but was likely due to toxicity rather than any inhibitory effects. Consequently, the obtained results confirm the importance of growth regulators and natural compounds on plant growth and can broaden our understanding for future research and achievement of objectives.

2024-08-01·Veterinary Research Communications

Evaluation of gastrointestinal tract lesions and serum malondialdehyde levels after repeated oral administration of phenylbutazone in horses

Article

作者: Tesena, Parichart ; Piyakul, Poonnada ; Sirireugwipas, Rannaree ; Wong-Aree, Kanokpich ; Vinijkumthorn, Ruethaiwan ; Preuksathaporn, Titirat ; Prapaiwan, Nawarus ; Chotikaprakal, Thanapon

AbstractPhenylbutazone (PBZ) is a widely used nonsteroidal anti-inflammatory drug for horses. However, because of its gastrointestinal side effects, its administration requires careful attention in veterinary practice. Malondialdehyde (MDA) is a serum biomarker associated with increased damage to the equine gastrointestinal system. This study investigated the hematological effects and alterations in the gastrointestinal tract and assessed serum MDA concentrations following repeated oral PBZ administration at clinical doses. Fourteen horses were randomly divided into control and treatment groups. All horses in the treatment group were administered 4.4 milligrams per kilogram of body weight of PBZ syrup orally twice a day for 7 days, whereas the control group received syrup as a placebo. The development of gastrointestinal side effects was investigated using gastroscopy, abdominal ultrasound, and fecal pH; serum MDA concentrations were assessed using a commercially available enzyme-linked immunosorbent assay kit. Data were compared between PBZ-treated and control horses before and after the treatment period. The treatment group exhibited decreased albumin and total protein concentrations. Moreover, this group exhibited a higher thickness of the right dorsal colon wall (p = 0.03) and had higher scores for squamous gastric ulcers (p = 0.01). Fecal pH was lower in the treatment group than in the control group after PBZ administration (p < 0.01). Although MDA concentrations were higher in the treatment group after PBZ administration, they did not differ significantly from those of the control group. This study highlighted the changes in hematological and gastrointestinal lesions resulting from PBZ administration in horses at clinical doses, even without clinical signs. However, MDA may not be an optimal biomarker for the early detection of gastrointestinal damage due to PBZ treatment in horses.

100 项与盐酸曲吡那敏相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02091	盐酸曲吡那敏	R06AC04 D04AA04	DB00792

研发状态

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适应症	国家/地区	公司	日期
哮喘	中国	石药集团欧意药业有限公司	1995-01-01
湿疹	中国	石药集团欧意药业有限公司	1995-01-01
季节性过敏性鼻炎	中国	石药集团欧意药业有限公司	1995-01-01
荨麻疹	中国	石药集团欧意药业有限公司	1995-01-01