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The New England Journal of Medicine Jan 1977
Topics: Adult; Diphenhydramine; Female; Humans; Trismus
PubMed: 830291
DOI: 10.1056/NEJM197701132960223 -
Research Communications in Chemical... Nov 1974
Topics: Amination; Chromatography, Gas; Chromatography, Thin Layer; Dealkylation; Diphenhydramine; Humans; Mass Spectrometry
PubMed: 4445562
DOI: No ID Found -
Journal of Emergency Nursing Oct 1996
Topics: Anti-Allergic Agents; Ciguatera Poisoning; Diphenhydramine; Humans; Micronesia; Poisoning
PubMed: 8997960
DOI: 10.1016/s0099-1767(96)80135-8 -
Journal of Clinical Pharmacology 1983One hundred eleven mildly to moderately insomniac patients participated in a double-blind, placebo-controlled study to establish the efficacy of diphenhydramine as an... (Clinical Trial)
Clinical Trial Comparative Study
One hundred eleven mildly to moderately insomniac patients participated in a double-blind, placebo-controlled study to establish the efficacy of diphenhydramine as an over-the-counter (OTC) sleep aid. A two-week crossover design was employed in which all patients received both diphenhydramine and placebo for one week each. The daily diphenhydramine dose was 50 mg at bedtime. Results obtained indicate that diphenhydramine improved various sleep parameters, including sleep latency, to a significantly higher degree than did placebo. In addition, patients on diphenhydramine reported feeling more restful the following morning and patients preferred the diphenhydramine drug to placebo despite experiencing more side effects. This study thus supports the use of 50 mg diphenhydramine as an OTC sleep aid in the treatment of temporary mild to moderate insomnia.
Topics: Adult; Aged; Clinical Trials as Topic; Diphenhydramine; Double-Blind Method; Female; Humans; Male; Middle Aged; Random Allocation; Sleep; Sleep Initiation and Maintenance Disorders
PubMed: 6348106
DOI: 10.1002/j.1552-4604.1983.tb02730.x -
AAPS PharmSciTech Mar 2011The purpose of this study was to formulate drug-loaded polyelectrolyte matrices constituting blends of pectin, chitosan (CHT) and hydrolyzed polyacrylamide (HPAAm) for...
The purpose of this study was to formulate drug-loaded polyelectrolyte matrices constituting blends of pectin, chitosan (CHT) and hydrolyzed polyacrylamide (HPAAm) for controlling the premature solvation of the polymers and modulating drug release. The model drug employed was the highly water-soluble antihistamine, diphenhydramine HCl (DPH). Polyelectrolyte complex formation was validated by infrared spectroscopy. Matrices were characterized by textural profiling, porositometry and SEM. Drug release studies were performed under simulated gastrointestinal conditions using USP apparatus 3. FTIR spectra revealed distinctive peaks indicating the presence of -COO(-) symmetrical stretching (1,425-1,390 cm(-1)) and -NH (3) (+) deformation (1,535 cm(-1)) with evidence of electrostatic interaction between the cationic CHT and anionic HPAAm corroborated by molecular mechanics simulations of the complexes. Pectin-HPAAm matrices showed electrostatic attraction due to residual -NH(2) and -COO(-) groups of HPAAm and pectin, respectively. Textural profiling demonstrated that CHT-HPAAm matrices were most resilient at 6.1% and pectin-CHT-HPAAm matrices were the least (3.9%). Matrix hardness and deformation energy followed similar behavior. Pectin-CHT-HPAAm and CHT-HPAAm matrices produced type IV isotherms with H3 hysteresis and mesopores (22.46 nm) while pectin-HPAAm matrices were atypical with hysteresis at a low P/P(0) and pore sizes of 5.15 nm and a large surface area. At t (2 h), no DPH was released from CHT-HPAAm matrices, whereas 28.2% and 82.2% was released from pectin-HPAAm and pectin-CHT-HPAAm matrices, respectively. At t (4 h), complete DPH release was achieved from pectin-CHT-HPAAm matrices in contrast to only 35% from CHT-HPAAm matrices. This revealed the release-modulating capability of each matrix signifying their applicability in controlled oral drug delivery applications.
Topics: Acrylic Resins; Administration, Oral; Anti-Allergic Agents; Chitosan; Computer Simulation; Diphenhydramine; Dosage Forms; Drug Carriers; Drug Delivery Systems; Excipients; Models, Molecular; Pectins; Polymers; Porosity; Spectroscopy, Fourier Transform Infrared; Surface Properties
PubMed: 21225384
DOI: 10.1208/s12249-010-9576-8 -
Journal of Clinical Psychopharmacology Oct 2002Sedation is the principal side effect of first generation H1 antihistamines, and recent studies have suggested that this side effect should limit the clinical... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
Sedation is the principal side effect of first generation H1 antihistamines, and recent studies have suggested that this side effect should limit the clinical application of these drugs. The sedative effect also underlies the use of these first-generation drugs as nonprescriptive remedies for insomnia. In both cases, the potential for tolerance to the sedative effect of these drugs is an important issue for which there are few objective data. In the study reported here, 15 healthy men age 18 to 50 years received either diphenhydramine 50 mg or placebo twice a day for 4 days in a randomized, double-blind, crossover trial design. Dependent measures included objective and subjective assessments of sleepiness and computer-based tests of psychomotor performance. Both objective and subjective measures of sleepiness showed significantly higher levels on day 1 for diphenhydramine compared to placebo. By day 4, however, levels of sleepiness on diphenhydramine were indistinguishable from placebo. Similarly, diphenhydramine produced significant impairment of performance that was completely reversed by day 4. These data provide the first objective confirmation that tolerance develops to the sedative effect of a prototypical first-generation H1 antihistamine, diphenhydramine. On this dosing regimen, tolerance was complete by the end of 3 days of administration. While other antihistamines and dosing regimens may differ, these results suggest that tolerance to the sedation produced by these drugs develops with remarkable rapidity.
Topics: Adolescent; Adult; Cross-Over Studies; Diphenhydramine; Disorders of Excessive Somnolence; Double-Blind Method; Drug Tolerance; Histamine H1 Antagonists; Humans; Male; Middle Aged; Psychomotor Disorders; Reference Values; Time Factors
PubMed: 12352276
DOI: 10.1097/00004714-200210000-00012 -
Pharmacotherapy 1997Although paradoxic excitation may rarely occur in children and adults with conventional dosages of antihistamines, few case reports have appeared in the literature. We...
Although paradoxic excitation may rarely occur in children and adults with conventional dosages of antihistamines, few case reports have appeared in the literature. We cared for a 46-year-old patient who became extremely agitated after receiving a dose of intravenous diphenhydramine.
Topics: Adult; Breast Neoplasms; Diphenhydramine; Female; Histamine H1 Antagonists; Humans; Middle Aged; Psychomotor Agitation
PubMed: 9399617
DOI: No ID Found -
Luminescence : the Journal of... Jun 2020Simple and rapid synchronous fluorometric methods were adopted and validated for the simultaneous analysis of a binary mixture of diphenhydramine (DIP) and ibuprofen...
Simple and rapid synchronous fluorometric methods were adopted and validated for the simultaneous analysis of a binary mixture of diphenhydramine (DIP) and ibuprofen (IBU) (Mix I) or DIP and phenylephrine (PHE) (Mix II) in their co-formulated pharmaceuticals without prior separation. Analysis of Mix I is based on the measurement of the peak amplitudes (D ) of synchronous fluorescence intensities at 265.1 nm for DIP and 260 nm for IBU. The relationship between the concentration and the amplitude of the first-derivative synchronous fluorescence spectra showed good linearity over the concentration ranges 0.50-10.00 μg ml and 0.50-7.90 μg ml for DIP and IBU, respectively. Analysis of Mix II was based on measurement of the peak amplitude (D ) synchronous fluorescence intensities at 230 nm for DIP and at 253.9 nm for PHE. Moreover, for Mix II, the peak amplitude (D ) synchronous fluorescence intensities were measured at 227.9 nm for DIP and at 264.9 nm for PHE. Calibration plots were rectilinear over the concentration range 0.30-3.50 μg ml and 0.03-0.75 μg ml for DIP and PHE, respectively. The proposed methods were successfully applied to determine the studied compounds in pure form and in pharmaceutical preparations.
Topics: Calibration; Diphenhydramine; Ibuprofen; Molecular Structure; Phenylephrine; Spectrometry, Fluorescence
PubMed: 31904176
DOI: 10.1002/bio.3750 -
Journal of Pharmaceutical Sciences Feb 1983Twelve healthy subjects received three single oral doses (250 mg) of methaqualone alone or in combination with diphenhydramine (25 mg). Blood samples were collected for...
Twelve healthy subjects received three single oral doses (250 mg) of methaqualone alone or in combination with diphenhydramine (25 mg). Blood samples were collected for a 48-hr period after each dose and analyzed for methaqualone and its major metabolite, 2-methyl-3-(2'-hydroxymethylphenyl)-4(3H)-quinazolinone. Peak blood concentrations ranging from 1.0 to 2.7 micrograms/ml occurred approximately 1-2 hr after the oral dose. The area under the blood level-time curve, peak plasma level, and elimination half-life for methaqualone were not significantly different (three-way ANOVA, p greater than 0.05) when methaqualone was administered alone, in combination with a diphenhydramine elixir or as a commercial product (capsule) containing both methaqualone and diphenhydramine. Statistically significant intersubject differences in the area under the curve were eliminated if the area was corrected for subject differences in elimination. Blood levels of the metabolite reached an average peak of 314 ng/ml (+/- 107) between 4 and 8 hr after the dose and remained elevated for the 48-hr sampling period. The areas under the blood level time curve of the metabolite were not significantly different for the three treatments. Diphenhydramine administered at the dosage level used in therapeutic combination products did not alter the blood levels of methaqualone or its metabolite. In addition, no significant differences in methaqualone availability from the two commercial formulations tested could be detected.
Topics: Adult; Capsules; Chromatography, Gas; Diphenhydramine; Drug Combinations; Drug Interactions; Female; Humans; Kinetics; Male; Methaqualone; Solutions
PubMed: 6834256
DOI: 10.1002/jps.2600720220 -
Drug Development and Industrial Pharmacy Apr 2023The aim of the present study was to formulate chitosan-coated alginate nanoparticles containing the drug diphenhydramine hydrochloride (DHH).
Chitosan-coated alginate (CCA) nanoparticles for augmentation of topical antihistaminic activity of diphenhydramine: optimization, skin histopathology and pharmacodynamic studies with in vitro/in vivo correlation.
OBJECTIVE
The aim of the present study was to formulate chitosan-coated alginate nanoparticles containing the drug diphenhydramine hydrochloride (DHH).
SIGNIFICANCE
Diphenhydramine hydrochloride (DHH) is the prototype of H-antihistaminic drugs. It is a lipophilic drug, that easily crosses the blood-brain barrier when taken orally causing decrements in alertness and performance. Multiple applications of topical drug products are required. Thus, drug incorporation in nanocarriers would increase the skin penetration powers increasing the drug efficacy.
METHODS
Chitosan-coated alginate (CCA) nanoparticles were prepared polyelectrolyte complex technique adopting 2 full factorial designs. Three factors, namely, alginate concentration, drug-to-alginate ratio and CaCl volume, each in two levels were studied. The prepared formulae were evaluated utilizing entrapment efficiency (EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and release. The characterization process was then followed by optimization.
RESULTS
At alginate conc. of 1%, drug to alginate ratio of 2:1 and CaCl volume of 4 mL, NP8 was chosen as a candidate formula. Histopathological examination on shaved rat dorsal skin disclosed the safety of NP8 with no signs of necrosis or even inflammation. The enhanced topical delivery of diphenhydramine hydrochloride enclosed in the developed nanoparticles was further proved by induction of allergic reaction using intradermal histamine injection. The results revealed the superior ability of NP8 to decrease the diameter of the formed wheal in comparison to the marketed DHH product.
CONCLUSION
Thus, CCA nanoparticles are considered candidate nanocarriers for fortifying the topical antihistaminic activity of DHH.
Topics: Rats; Animals; Chitosan; Diphenhydramine; Drug Carriers; Alginates; Calcium Chloride; Nanoparticles; Particle Size
PubMed: 37158038
DOI: 10.1080/03639045.2023.2211672