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Clinical Pharmacology and Therapeutics Jan 1989The time course of diphenhydramine concentrations and effects on both mental performance and subjective feelings of drowsiness were assessed in 15 healthy men. Subjects... (Clinical Trial)
Clinical Trial
The time course of diphenhydramine concentrations and effects on both mental performance and subjective feelings of drowsiness were assessed in 15 healthy men. Subjects received single oral doses of diphenhydramine, 50 mg, and placebo in this double-blind crossover study. Diphenhydramine plasma concentrations and central nervous system actions were assessed for 24 hours after each treatment. Cognitive impairment was assessed with an automobile driving simulator and digit symbol substitution scores, whereas drowsiness was self-assessed on a visual analog scale. Diphenhydramine produced significant feelings of drowsiness for up to 6 hours after the dose, whereas significant mental impairment was apparent for only 2 hours. Despite the difference in duration of these effects, drowsiness and mental impairment have parallel slopes when effects are related to diphenhydramine concentrations. These data suggest that although the apparent diphenhydramine concentration thresholds to produce drowsiness are lower (30.4 to 41.5 ng/ml) than those needed to produce mental impairment (58.2 to 74.4 ng/ml), these effects have profiles consistent with their being manifestations of the same pharmacologic effect.
Topics: Adult; Diphenhydramine; Humans; Male; Psychomotor Performance; Reaction Time; Sleep Stages
PubMed: 2910633
DOI: 10.1038/clpt.1989.3 -
Annals of Emergency Medicine Oct 2020Acute urticaria is a frequent presentation in emergency departments (EDs), urgent care centers, and other clinical arenas. Treatment options are limited if... (Randomized Controlled Trial)
Randomized Controlled Trial
STUDY OBJECTIVE
Acute urticaria is a frequent presentation in emergency departments (EDs), urgent care centers, and other clinical arenas. Treatment options are limited if diphenhydramine is the only intravenous antihistamine offered because of its short duration of action and well-known adverse effects. We evaluate cetirizine injection, the first second-generation injectable antihistamine, for acute urticaria in this multicenter, randomized, noninferiority, phase 3 clinical trial.
METHODS
Adult patients presenting to EDs and urgent care centers with acute urticaria requiring an intravenous antihistamine were randomized to either intravenous cetirizine 10 mg or intravenous diphenhydramine 50 mg. The primary endpoint was the 2-hour pruritus score change from baseline, with time spent in treatment center and rate of return to treatment centers as key secondary endpoints. Frequency of sedation and anticholinergic adverse effects were also recorded.
RESULTS
Among 262 enrolled patients, the 2-hour pruritus score change from baseline for intravenous cetirizine was statistically noninferior to that for intravenous diphenhydramine (-1.6 versus -1.5; 95% confidence interval -0.1 to 0.3), and in favor of cetirizine. Treatment differences also favored cetirizine for mean time spent in treatment center (1.7 versus 2.1 hours; P=.005), return to treatment center (5.5% versus 14.1%; P=.02), lower change from baseline sedation score at 2 hours (0.1 versus 0.5; P=.03), and adverse event rate (3.9% versus 13.3%).
CONCLUSION
Intravenous cetirizine is an effective alternative to intravenous diphenhydramine for treating acute urticaria, with benefits of less sedation, fewer adverse events, shorter time spent in treatment center, and lower rates of revisit to treatment center.
Topics: Administration, Intravenous; Adolescent; Adult; Aged; Aged, 80 and over; Canada; Cetirizine; Diphenhydramine; Double-Blind Method; Female; Humans; Male; Middle Aged; Treatment Outcome; United States; Urticaria
PubMed: 32653333
DOI: 10.1016/j.annemergmed.2020.05.025 -
Biopharmaceutics & Drug Disposition Apr 1990Eight healthy volunteers received 50 mg of dimenhydrinate, a theoclate salt of diphenhydramine, orally, sublingually, and intravenously on three separate occasions in... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Eight healthy volunteers received 50 mg of dimenhydrinate, a theoclate salt of diphenhydramine, orally, sublingually, and intravenously on three separate occasions in random sequence. Plasma diphenhydramine concentrations during 12 h after each dose were measured by gas-liquid chromatography with nitrogen-phosphorous detection. Mean peak plasma concentrations after sublingual administration were slightly lower than after oral dosage (38.3 vs 47.8 ng ml-1), and the time of peak concentration was similar (2.6 vs 2.3 h after dose). These differences did not reach statistical significance. The mean total area under the plasma concentration-time curve (AUC) for sublingual administration was slightly but not significantly smaller than after oral dosage (221 vs 270 h ng ml-1). Systemic availability of diphenhydramine after sublingual dimenhydrinate, measured by the ratio of oral AUC to intravenous AUC, was slightly less than after oral dimenhydrinate (0.58 vs 0.69, NS), and both were significantly less than 1.0. Thus sublingual and oral administration of dimenhydrinate result in comparable, but incomplete, systemic availability of diphenhydramine.
Topics: Administration, Oral; Administration, Sublingual; Adolescent; Adult; Biological Availability; Chromatography, Gas; Dimenhydrinate; Diphenhydramine; Female; Half-Life; Humans; Injections, Intravenous; Male; Middle Aged; Random Allocation
PubMed: 2328304
DOI: 10.1002/bdd.2510110302 -
Ugeskrift For Laeger Jun 1954
Topics: Diphenhydramine; Herpes Zoster; Herpesvirus 3, Human; Humans
PubMed: 13179331
DOI: No ID Found -
Medizinische Klinik Aug 1957
Topics: Diphenhydramine; Humans; Vomiting; Xanthines
PubMed: 13482960
DOI: No ID Found -
Archiv Fur Toxikologie 1956
Topics: Anti-Allergic Agents; Diphenhydramine
PubMed: 13382314
DOI: No ID Found -
The Journal of Pharmacy and Pharmacology Nov 1982
Topics: Animals; Diphenhydramine; Drug Interactions; Half-Life; Injections, Intraperitoneal; Kinetics; Male; Methaqualone; Rats
PubMed: 6129311
DOI: 10.1111/j.2042-7158.1982.tb06216.x -
Journal of Chromatography Apr 1990
Topics: Administration, Oral; Analysis of Variance; Chromatography, High Pressure Liquid; Diphenhydramine; Half-Life; Humans
PubMed: 2362001
DOI: 10.1016/s0378-4347(00)82546-3 -
Bioelectrochemistry (Amsterdam,... Oct 2011The performance characteristic of sensitive screen-printed (SPE) and carbon paste (CPE) electrodes was investigated for the determination of diphenhydramine...
The performance characteristic of sensitive screen-printed (SPE) and carbon paste (CPE) electrodes was investigated for the determination of diphenhydramine hydrochloride (DPH) drug in pure, pharmaceutical preparations and biological fluids. Different experimental conditions namely types of materials used to prepare the working electrode (plasticizer), titrant, pH, temperature and life time were studied. Under these conditions, the SPE shows the best performance than CPE with respect to total potential change and potential break at the end point. The SPE and CPE exhibit suitable response to DPH in a concentration range of 1.0.10(-2) to 1.0.10(-6) mol/L with a limit of detection 9.70.10(-7) and 9.80.10(-7) mol/L, respectively. The slope of the system was 55.2±1.0 and 54.7±1.0 mV/decade over pH range 3.0-8.0 and 3-7 for SPE and CPE, respectively. Selectivity coefficients for DPH relative to a numbers of potential interfering substances were investigated. The SPE and CPE show a fast response time of 10 and 16s and were used over a period of 2 months with a good reproducibility. The sensors were applied successfully to determine DPH in pharmaceutical preparations and biological fluids. The results are compared with the official method.
Topics: Anti-Allergic Agents; Diphenhydramine; Electrodes; Humans; Pharmaceutical Preparations; Potentiometry; Sensitivity and Specificity
PubMed: 21745764
DOI: 10.1016/j.bioelechem.2011.05.006 -
International Journal of Pharmaceutics Oct 2015Taste masking of bitter active substances is an emerging area in the pharmaceutical industry especially for paediatric/geriatric medications. In this study we introduce...
Taste masking of bitter active substances is an emerging area in the pharmaceutical industry especially for paediatric/geriatric medications. In this study we introduce the use of jet dispensing as a taste masking technology by printing mucosal thin films of three model bitter substances, Cetirizine HCl, Diphenylhydramine HCl and Ibuprofen. The process was used to dispense aqueous drugs/polymer solutions at very high speed where eventually the drugs were embedded in the polymer matrix. The in vivo evaluation of jet-dispensed mucosal films showed excellent taste masking for drug loadings from 20 to 40%. Jet dispensing was proved to make uniform, accurate and reproducible thin films with excellent content uniformity.
Topics: Administration, Oral; Cetirizine; Computer Systems; Diphenhydramine; Drug Delivery Systems; Humans; Ibuprofen; Taste; Technology, Pharmaceutical
PubMed: 25957704
DOI: 10.1016/j.ijpharm.2015.05.018