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At least 19 recordsLinked to original sources
PubMed1991

Evaluation of triflupromazine as a sedative in camels (Camelus dromedarius).

Effects of administration of triflupromazine were evaluated in 11 adult domesticated camels (Camelus dromedarius) weighing 403 +/- 29.5 kg (Mean +/- SE). Six camels were used to evaluate sedative properties of the drug and its effects on haematological and blood biochemical parameters. In the remaining 5 camels, effects on haemodynamics, acid base status and blood gases were studied. In all the animals triflupromazine was administered intramuscularly in the gluteal region at the rate of 2 mg/kg. Camels voluntarily sat down 48.9 +/- 5.4 min after administration of the drug but stood up again if disturbed. Drowsiness, drooping of lower lip and salivation were evident. The animals stood on their own and started walking with ataxia after 159 +/- 7 min and recovered completely from the effect of drug within 259 +/- 23 min. The drug caused a significant tachycardia and a moderate hypotension. The decrease in central venous pressure was also significant. Rectal temperature, respiratory rate, acid base status, blood gases, haemoglobin concentration, packed cell volume, total erythrocyte count, total leucocyte count, differential leukocyte count, blood urea nitrogen, plasma alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, alkaline phosphatase, blood glucose and plasma concentrations of sodium, potassium, chloride and inorganic phosphate were not significantly affected by triflupromazine.

Animals↗
PubMed2004

Romifidine-ketamine anaesthesia in atropine and triflupromazine pre-medicated buffalo calves.

The study was conducted on 10 buffalo calves with a weight of 98.5 +/- 3.9 kg and age 9.7 +/- 1.3 months. Ten trials of two treatments were carried out using a randomized block design. Atropine at the dose of 0.02 mg/kg bodyweight was administered in both the groups. The animals of group I received romifidine at the dose of 10 microg/kg i.v., 10 min after atropine administration, whereas, animals of group II received triflupromazine at the dose of 0.3 mg/kg i.m. and 10 min later romifidine at the dose of 10 microg/kg i.v. immediately followed by ketamine at the dose of 5 mg/kg i.v. The onset of action of romifidine in group I occurred within 2 min and the animals remained under mild sedation for 31 +/- 4.8 min. In group II, the triflupromazine-romifidine-ketamine combination induced anaesthesia for 14 +/- 2.3 min. Hypothermia, significant bradycardia and respiratory depression was noticed in both groups at different time intervals.

Adjuvants, Anesthesia↗
PubMed2004

Triflupromazine: a microbicide non-antibiotic compound.

The antipsychotic phenothiazine triflupromazine, possessing a methyl-thio substituent at position 10 and a fluorine moiety at position 2, exhibited significant antibacterial activity against 279 strains of Gram-positive and Gram-negative bacteria. The minimum inhibitory concentration (MIC) of the drug, according to the agar dilution method, was between 2 and 50 microg/ml for Staphylococcus aureus, and 5 and 100 microg/ml for shigellae and vibrios. Triflupromazine, when injected intraperitoneally into Swiss albino mice at a concentration of 30 microg/mouse (20 g), manifested a significant protection to the mice (p<0.001) when they were challenged with 50 median lethal dose (MLD) of Salmonella typhimurium NCTC 74. Moreover, there was a statistically significant reduction in the number of viable bacteria in organ homogenates and blood of mice treated with this phenothiazine compound.

Animals↗
PubMed1981

[Triflupromazine-effects in electroencephalogram (author's transl)].

Changes of EEG and Computer-EEG have been studied in a group of young patients premedicated intravenously with 10 mg of Triflupromazine, Druginduced changes of cerebral function caused especially variations of alpha-amplitude, in addition an increase of delta-delta/theta- and occasionally of beta-activity. The extend of EEG-changes depended on the individual weight-orientated dosage of Triflupromazine EEG-results and clinical data of quieting and sedative effects showed-with one exception-good correlation.

Adult↗
PubMed1976

Influence of dietary protein on the effect of coumaphos and triflupromazine interaction in sheep.

Coumaphos (8 or 15 mg/kg of body weight), triflupromazine HCl (1.1 mg/kg of body weight), or isotonic saline solution were given to 8 groups of sheep (5 per group) fed a low-or normal-dietary protein ration. One set of clinical signs, mortality rate, mean survival time, necropsy lesions, and plasma and erythrocyte cholinesterase (ChE) activity were monitored for each group. Observations suggested potentiation effect between the administered compounds. Inhibition of ChE activity was enhanced in groups given both drugs. Feeding of low-dietary protein ration adversely affected the development of clinical signs, mortality rate, mean survival time, and ChE activity. Recovery of ChE activity of triflupromazine HCl-treated animals was faster than in their respective controls, and sheep fed normal-dietary protein ration had faster ChE recovery than those fed the low-dietary protein ration. Inhibition of erythrocyte ChE found was a better index of organophosphorus toxicosis than that of plasma ChE.

Animals↗
PubMed1985

[Benefit and risk of high-dose metoclopramide in comparison to high-dose haloperidol or triflupromazine in cisplatin-induced vomiting].

The antiemetic efficacy of metoclopramide (MCL, Paspertin, loading infusion 0.5 mg/kg body wt./h over 2 h, maintenance infusion 0.25 mg/kg/h over 24 h) has been compared with haloperidol (HAL, Haldol, 1/10 of MCL dosage) and with triflupromazine (TFP, Psyquil, 1/2 of MCL dosage) in two sequential analyses, against the emetic effects of cisplatin (60-90 mg/m2). After treating 14 and 8 pairs of patients respectively, MCL was significantly (alpha = 0.05) more effective than HAL or TFP. Only 1 of the 14 patients in the HAL group and 0 of 8 in the TFP group were totally protected against emesis, in contrast to 6 of 14 patients and 3 of 8 in the MCL groups. In order to quantify the benefit/risk relationship of the antiemetic drugs studied the number of prevented emetic episodes (in comparison to previous insufficient treatment) was related to the incidence of major undesired effects (i.e. dystonia and/or akathisia). This relationship was 17.8 and 12.1 for the two MCL groups; for HAL and TFP it was only 5.8 and 4.6, respectively. The high antiemetic selectivity of MCL against cisplatin-induced emesis is probably related to the still unknown action of MCL on the gastrointestinal motility. A high neuroleptic potency, with or without additional anticholinergic activity, is apparently not essential for high antiemetic protection against cisplatin.

Cisplatin↗
PubMed2004

19F NMR spectroscopic study on the binding of triflupromazine to bovine and human serum albumins.

The 19F NMR spectrum of triflupromazine hydrochloride (TFZ) in a buffer solution (pH 6.8) showed a single sharp signal of the TFZ CF3 group at 13.5 ppm from the external trifluoroacetic acid. The addition of 1 mM HSA or BSA to the sample solution caused a split of the CF3 signal into two broadened signals shifted to slightly lower (0.2 ppm) and higher (0.7 ppm) fields, respectively, from the original position. Denaturation of the albumins by guanidine hydrochloride (3M) restored the two broadened signals to a slightly broadened single signal, indicating that TFZ has at least two binding sites on HSA and BSA, respectively. From the competitive binding 19F NMR experiments using Warfarin (Site-I ligand), l-tryptophan (Site-II ligand), NaCl, and oleate, the signal at high field was assigned to the TFZ bound to Site II. Comparison of the signal intensity revealed that the affinity of TFZ for Site II on HSA was considerably higher than that on BSA. The low-field signal could be identified as a weight-averaged signal between nonspecifically bound TFZ to HSA (BSA) and free TFZ in the water phase. In the presence of physiological concentrations of NaCl, major binding of TFZ to HSA and BSA was considered to be nonspecific. The present work indicates that 19F NMR is very useful for obtaining important detailed information regarding the binding of fluorinated drugs to serum albumins.

Animals↗
PubMed2005

Effects of phosphatidylserine and phosphatidylethanolamine content on partitioning of triflupromazine and chlorpromazine between phosphatidylcholine-aminophospholipid bilayer vesicles and water studied by second-derivative spectrophotometry.

To assess the affinity of psychotropic phenothiazine drugs, triflupromazine (TFZ) and chlorpromazine (CPZ), for the membranes of central nervous system and the other organs in the body, the partition coefficients (Kps) of these drugs to phosphatidylcholine (PC)-phosphatidylserine (PS) and PC-phosphatidylethanolamine (PE) small and large unilamellar vesicles (SUV, LUV) were examined by a second-derivative spectrophotometric method, since PS is abundantly contained in the membranes of the central nervous system and PE is distributed widely in the membranes of the organs in the body. Size and preparation methods of the vesicles did not affect the Kp values at each aminophospholipid content suggesting that the partition of the phenothiazine drugs was not affected by the structural differences in the vesicles such as their curvature or asymmetric distribution of the phospholipids between the outer and inner layers of the bilayer membranes. However, the Kp values of both drugs increased remarkably according to the PS content in the bilayer membranes, i.e., the Kp values for the vesicles of 30 mol% PS content were about 3 times of that for the vesicles of PC alone, while both Kp values slightly reduced with the increase in the content of PE in the bilayer membranes of PC-PE vesicles. The results indicate that both drugs have higher affinity for the PC-PS bilayer membranes than for the PC and PC-PE membranes, which can offer an evidence for the fact that TFZ and CPZ are predominantly distributed and accumulated in the brain and nerve cell membranes that contain PS abundantly.

Chlorpromazine↗
PubMed2006

Effects of inorganic ions on the binding of triflupromazine and chlorpromazine to bovine serum albumin studied by spectrometric methods.

The effects of inorganic salts, NaCl, NaBr, NaI, Na2SO4, KCl, KBr, KI, on the binding constants (Ks) of psychotropic phenothiazine drugs, triflupromazine (TFZ) and chlorpromazine, to bovine serum albumin (BSA) were examined by using second-derivative spectrophotometry. All of the salts examined, with the exception of Na2SO4, decreased the K values significantly, depending on the concentration of the salt, e.g., the decrease in the K values of both drugs were about 40% for 0.1 M NaCl. The results obtained with Na2SO4 indicated that neither Na+ nor SO4(2-) had any affect on the binding of the phenothiazines to BSA. Based on the Na2SO4 results and the finding that the effect of each potassium salt on binding was quite similar to that of the corresponding sodium salt, the effects of these halogen salts can be considered to be derived from their anions, although the phenothiazines are positively charged at pH 7.4. The effectiveness of the anions was determined to occur in the following order: I->>Br->Cl-; these results coincided with the published order of the binding affinity of these anions to albumin. The 19F-NMR spectra of TFZ in the presence of each of these halogen salts revealed a concentration-dependent decrease in the intensity of the signal at 13.8 ppm that had previously been assigned to the TFZ bound to Site II. Consequently, the effects of these anions on the binding of positively charged phenothiazine drugs are thought to be local steric effects caused by the binding of these anions to Site II.

Antipsychotic Agents↗
PubMed1994

[Phenothiazine derivatives, chlorpromazine and triflupromazine, produce different effects on sympathetic nerve activity in urethane-anesthetized rabbits].

UNLABELLED: This study was designed to evaluate effects of chlorpromazine (CPZ) or triflupromazine (TPZ) on renal sympathetic nerve activity and hemodynamics in urethane-anesthetized rabbits. METHODS: Thirty-five rabbits were divided into the following two groups: CPZ group (N = 10) and TPZ group (N = 25), challenged by an intravenous injection of either CPZ (0.4 mg.kg-1) or TPZ (0.2 mg.kg-1), respectively. Each experimental group was further divided into the following groups. CPZ group was divided into CPZ-INTACT group of animals with neuraxis intact (N = 6) and CPZ-SAD group of animals with combined denervation of the carotid sinus and aortic nerves (N = 4). TPZ group was divided into TPZ-INTACT group of rabbits with neuraxis intact (N = 8), TPZ-VAGOTOMY group of only cervical vagotomy (N = 6), TPZ-SADV group with combined denervation of the carotid sinus and aortic nerves with cervical vagotomy (N = 5) and TPZ-VI group with right cervical vagotomy but having the intact left vagus (N = 6). In the last group, right afferent vagal nerve activity was measured simultaneously. Mean blood pressure, central venous pressure, heart rate and renal sympathetic nerve activity were measured at the same time. RESULTS: In the CPZ-INTACT group, the agent caused a decrease in mean blood pressure and significant increases in sympathetic nerve activity and heart rate, but no significant change in central venous pressure. This increase in sympathetic nerve activity and heart rate disappeared in the SAD animals in spite of hypotension. Animals of the TPZ-INTACT group showed an abrupt decrease in sympathetic nerve activity in response to hypotension, but did not exhibit a remarkable change in heart rate and central venous pressure. However, in contrast, animals with severed cervical vagi showed a sympathetic augmentation after the TPZ injection. These sympathetic changes were abolished in the SADV animals. In the TPZ-VI group, TPZ elicited a decline in sympathetic nerve activity similar to that observed in INTACT animals, but afferent vagal nerve activity increaed simultaneously with sympathetic depression. CONCLUSION: These results indicate that a reflex increase in sympathetic nerve activity which occurred during hypotension after CPZ injection may have been mediated by the arterial baroreceptor reflex and that a sympathetic reduction after TPZ administration may have resulted from a reciprocal interaction between an excitation through the sino-aortic nerves and an inhibition via the vagal nerves.

Anesthesia↗
PubMed1999

Effects of Particle Size and Cholesterol Content on the Partition Coefficients of Chlorpromazine and Triflupromazine between Phosphatidylcholine-Cholesterol Bilayers of Unilamellar Vesicles and Water Studied by Second-Derivative Spectrophotometry.

Phosphatidylcholine(PC)-cholesterol (0-30 mol%) unilamellar vesicles of several sizes (20-600 nm) were prepared in buffer (pH 7.4) solutions by sonication or extrusion methods. The vesicle size was measured by a dynamic light-scattering method. Absorption spectra of chlorpromazine (CPZ) and triflupromazine (TFZ) in the presence of these vesicles showed a bathochromic shift according to the increase in vesicle concentration, but the counterbalance of the baseline was incomplete due to the intensive light scattering by the vesicles; thus, no isosbestic point could be observed. In the second-derivative spectra, the residual background signal effects were eliminated and three derivative isosbestic points were clearly observed for both drugs. The derivative intensity change (DeltaD) induced by the addition of the vesicles was measured at the lambda(max) of each drug. From the relationship between the DeltaD value and the lipid concentration, the partition coefficients (K(p)) of CPZ and TFZ between these vesicles and water (buffer) were calculated. The results revealed that the vesicle size (20-600 nm) and preparation method do not affect the K(p) values, and although the incorporation of cholesterol into the PC bilayers induces a decrease of the K(p) values, the vesicle size also did not affect the K(p) values in vesicles of the same cholesterol content. Copyright 1999 Academic Press.

Journal Article↗