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The Journal of Pharmacy and Pharmacology Apr 1985During a multiple dosing regimen, the area under the promethazine blood concentration-time profile progressively decreased indicating auto-induction of metabolism. The...
During a multiple dosing regimen, the area under the promethazine blood concentration-time profile progressively decreased indicating auto-induction of metabolism. The increase in promethazine clearance (mean 35%) was not reflected in changes in either elimination half-life or minimum blood concentrations during the dosing interval. This was attributed to a deep compartment in the disposition of promethazine in the rabbit. The changes in promethazine clearance were accompanied by proportionally larger changes in the clearance of the monodesmethylpromethazine metabolite. The effect of promethazine pretreatment on the clearance of antipyrine was also studied and was found to be significantly increased by a mean of 17% following pretreatment with promethazine. However, the changes in the clearance of antipyrine did not highly correlate with those of promethazine and monodesmethylpromethazine. This may indicate that promethazine induces metabolic systems in the rabbit for which antipyrine is not a good substrate.
Topics: Animals; Antipyrine; Biotransformation; Half-Life; Kinetics; Male; Promethazine; Rabbits
PubMed: 2860221
DOI: 10.1111/j.2042-7158.1985.tb05052.x -
Spectrochimica Acta. Part A, Molecular... Jun 2018The binding nature of amphiphilic drugs viz. promethazine hydrochloride (PMT) and adiphenine hydrochloride (ADP), with human hemoglobin (Hb) was unraveled by...
The binding nature of amphiphilic drugs viz. promethazine hydrochloride (PMT) and adiphenine hydrochloride (ADP), with human hemoglobin (Hb) was unraveled by fluorescence, absorbance, time resolved fluorescence, fluorescence resonance energy transfer (FRET) and circular dichroism (CD) spectral techniques in combination with molecular docking and molecular dynamic simulation methods. The steady state fluorescence spectra indicated that both PMT and ADP quenches the fluorescence of Hb through static quenching mechanism which was further confirmed by time resolved fluorescence spectra. The UV-Vis spectroscopy suggested ground state complex formation. The activation energy (E) was observed more in the case of Hb-ADP than Hb-PMT interaction system. The FRET result indicates the high probability of energy transfer from β Trp37 residue of Hb to the PMT (r=2.02nm) and ADP (r=2.33nm). The thermodynamic data reveal that binding of PMT with Hb are exothermic in nature involving hydrogen bonding and van der Waal interaction whereas in the case of ADP hydrophobic forces play the major role and binding process is endothermic in nature. The CD results show that both PMT and ADP, induced secondary structural changes of Hb and unfold the protein by losing a large helical content while the effect is more pronounced with ADP. Additionally, we also utilized computational approaches for deep insight into the binding of these drugs with Hb and the results are well matched with our experimental results.
Topics: Binding Sites; Diphenylacetic Acids; Fluorescence; Fluorescence Resonance Energy Transfer; Hemoglobins; Humans; Hydrogen Bonding; Molecular Docking Simulation; Molecular Dynamics Simulation; Promethazine; Protein Binding; Spectrometry, Fluorescence
PubMed: 29562212
DOI: 10.1016/j.saa.2018.03.023 -
Deutsche Medizinische Wochenschrift... Oct 1977
Topics: Drug Combinations; Promethazine; Urea
PubMed: 21066
DOI: No ID Found -
British Medical Journal Apr 1967
Topics: Child; Electroencephalography; Humans; Male; Promethazine
PubMed: 6020998
DOI: 10.1136/bmj.2.5543.31 -
Anesthesia and Analgesia 1959
Topics: Analgesia; Anesthesia; Anesthesia and Analgesia; Anesthesiology; Pain Management; Promethazine; Thiopental
PubMed: 13851943
DOI: No ID Found -
The Journal of Pharmacy and Pharmacology Feb 1971
Topics: Adult; Eye; Hand; Humans; Male; Motor Skills; Promethazine; Vision, Ocular
PubMed: 4396874
DOI: 10.1111/j.2042-7158.1971.tb08627.x -
Canadian Journal of Anaesthesia =... Jan 1991This randomized, double-blind study evaluated the antiemetic efficacy and the side-effects of promethazine pretreatment (0.5 mg.kg-1 IV + 0.5 mg.kg-1 IM) versus... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
This randomized, double-blind study evaluated the antiemetic efficacy and the side-effects of promethazine pretreatment (0.5 mg.kg-1 IV + 0.5 mg.kg-1 IM) versus droperidol + placebo pretreatment (droperidol, 0.075 mg.kg-1 IV + physiological saline, 0.02 ml.kg-1 IM). One hundred unpremedicated ASA physical status I children ranging from two to ten years, and undergoing outpatient strabismus surgery were studied. All children received inhalational anaesthesia with halothane, nitrous oxide and oxygen. Neither opioids nor muscle relaxants were used. The incidence of vomiting and/or retching and the incidence of side-effects were determined in the post-anaesthesia recovery room (PARR), in the short-stay surgical unit (SSSU), and after discharge from the hospital (including the journey and the stay at home during the first postoperative day). Promethazine and droperidol were equally effective in reducing the incidence of vomiting before discharge to two and eight per cent respectively. On the contrary, the incidence of vomiting after discharge and overall were significantly less with promethazine (ten and ten per cent) than with droperidol pretreatment (54 and 56 per cent) (P less than 0.0001). Promethazine permitted the time to discharge from the hospital to be reduced to an average of three hours, without increasing the incidence of vomiting postdischarge. Promethazine pretreatment is much less expensive than droperidol pretreatment. The incidence of restlessness was significantly less with droperidol (eight per cent) than with promethazine (36 per cent) (P less than 0.001). Promethazine pretreatment demands the use of an analgesic like acetaminophen in order to reduce the incidence of postoperative pain and restlessness.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Ambulatory Surgical Procedures; Anesthesia Recovery Period; Child; Child, Preschool; Double-Blind Method; Droperidol; Female; Humans; Incidence; Injections, Intramuscular; Injections, Intravenous; Intraoperative Care; Male; Placebos; Promethazine; Quebec; Strabismus; Time Factors; Vomiting
PubMed: 1989740
DOI: 10.1007/BF03009164 -
Medicina 1997Promethazine is currently used for its antipsychotic and ansiolytic effects. It is a phenothiazine with anticalmodulin action, not toxic for human beings at therapeutic...
Promethazine is currently used for its antipsychotic and ansiolytic effects. It is a phenothiazine with anticalmodulin action, not toxic for human beings at therapeutic doses. The present results show that promethazine has trypanocidal effect on both epimastigote and trypomastigote stages of T. cruzi; two hundred microM inhibited epimastigote growth in culture medium and 2 microM immobilized and killed bloodstream trypomastigotes. When promethazine (55 mg/Kg/day) was used as treatment of T. cruzi infected mice, it proved effective in reducing parasitemia and it increased the survival of treated animals. Ultrastructural studies suggest that the lethal effect of this phenothiazine is related to a detergent effect that disrupts T. cruzi cell membrane.
Topics: Animals; Chagas Disease; Male; Mice; Microscopy, Electron; Promethazine; Trypanocidal Agents; Trypanosoma cruzi
PubMed: 9435371
DOI: No ID Found -
Anesthesia and Analgesia 1977Two hundred seventy patients received morphine 5 mg or 10 mg alone or with promethazine 6.25 mg, 12.5 mg, or 25 mg. Promethazine 25 mg alone also was studied. All drugs... (Clinical Trial)
Clinical Trial
Two hundred seventy patients received morphine 5 mg or 10 mg alone or with promethazine 6.25 mg, 12.5 mg, or 25 mg. Promethazine 25 mg alone also was studied. All drugs were given intravenously. Anxiety relief, sedation, patient acceptance, lack of recall, and side effects were the variables examined. Promethazine improved relief of anxiety, sedation, and patient acceptance when added to morphine. Doses of promethazine larger than 12.5 mg intravenously failed to improve these effects. Memory remained unaffected by any of the drugs.
Topics: Adolescent; Adult; Aged; Anxiety; Clinical Trials as Topic; Double-Blind Method; Humans; Injections, Intravenous; Mental Recall; Middle Aged; Morphine; Patient Acceptance of Health Care; Preanesthetic Medication; Promethazine; Sex Factors
PubMed: 337854
DOI: 10.1213/00000539-197711000-00011 -
Medical Hypotheses Jan 1996Evidence supporting the claim that specific phenothiazines, notably chlorpromazine and promethazine, may be used as sole agents for the treatment of cancer in man, has...
Evidence supporting the claim that specific phenothiazines, notably chlorpromazine and promethazine, may be used as sole agents for the treatment of cancer in man, has been reviewed. Selective destruction of cancerous tissue can be achieved by modulating energy metabolism in malignant cells. In the light of available information, the drug of choice is promethazine, the effects of which on the central nervous system are relatively weak. The maintenance of continuous pharmacological pressure against malignant growths forms an essential feature of the therapy. Protection against blood dyscrasias may be secured through the provision of adequate amounts of trace elements necessary for the function of enzyme systems which detoxicate active oxygen species. Tumour-cell death may be facilitated by nutritional supplements of specific polyunsaturated fatty acids. Interference from adventitious medications and drug resistance are discussed; appropriate therapy is outlined.
Topics: Antineoplastic Agents; Breast Neoplasms; Chlorpromazine; Cyclophosphamide; Female; Humans; Male; Neoplasms; Pancreatic Neoplasms; Phenothiazines; Promethazine
PubMed: 8746124
DOI: 10.1016/s0306-9877(96)90231-5