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Maeda, Toshiki, Akira Babazono, and Takumi Nishi. "Surveillance of First-Generation H1-Antihistamine Use for Older Patients with Dementia in Japan: A Retrospective Cohort Study." Current Gerontology and Geriatrics Research 2018 (July 2, 2018): 1–6. http://dx.doi.org/10.1155/2018/3406210.
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Background. This study aimed to investigate the rate of first-generation H1-antihistamines use for older adults with dementia in Japan. Methods. The study design was retrospective cohort using claims data between fiscal years 2010 and 2013. Subjects were 75 years or older, diagnosed with dementia, and given H1-antihistamines orally during the study period after being diagnosed with dementia. We investigated the cumulative number of oral H1-antihistamines administered and the relationship between first-generation H1-antihistamine use and each explanatory variable using crude and adjusted odds ratio. Results. The cumulative total for use of first-generation H1-antihistamine for older adults with dementia accounted for 32.1% of all antihistamine medication. The majority of first-generation H1-antihistamine prescriptions were indicated for cold treatment. Those with upper respiratory infection or asthma had a significantly positive relationship with first-generation H1-antihistamine use. Conclusion. The study showed that first-generation H1-antihistamine drugs were highly prescribed in older adults with dementia in Japan.
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Oyekan, P. J., H. C. Gorton, and C. S. Copeland. "Over-the-counter antihistamines in drug-related deaths: a population-based case series." International Journal of Pharmacy Practice 29, Supplement_1 (March 26, 2021): i30—i31. http://dx.doi.org/10.1093/ijpp/riab015.037.
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Abstract Introduction Antihistamines are not one of the medicine groups reported on in the Office for National Statistics drug-related death data. (1) However, there is concern that first-generation antihistamines are misused for their sedative properties. This is amplified by a recent social media challenge, which resulted in deaths due to diphenhydramine overdose. (2) The extent of the involvement of antihistamines in deaths is largely unknown. Aim We aimed to evaluate deaths related to antihistamines in England (2000–2019) by individual drug, medicine classification (POM, P, GSL), whether the drug was considered attributable to the death (known as implication rate), or incidental; and examine temporal trends. Methods Deaths are reported voluntarily by coroners to the National Programme on Substance Abuse Deaths (NPSAD) in cases where psychoactive drugs were detected at post-mortem and/or when the decedent was known to abuse drugs. NPSAD holds data on decedent demographics (gender, age, employment status, living arrangements), details pertaining to the death (cause(s) of death, manner of death, conclusion of inquest, toxicology reports) and past social and medical histories, including drugs prescribed. From this dataset, we extracted all cases where an antihistamine was detected at post-mortem between 2000 and 2019. We report descriptive statistics to describe the reporting of antihistamines in deaths. Results We identified 1666 antihistamine detections from 1537 individuals. The significant majority of these were sedative antihistamines which are classed as pharmacy medicines (P) (85.2%, p<0.01); deaths where prescription-only antihistamines were detected represented fewer than 7.0% of cases. Despite an increasing trend for antihistamine detections in deaths over time, the proportion of deaths where the detected antihistamine was implicated in causing the death declined over the same period (average implication rate 2000–2005: 58.7%; 2014–2019: 28.4%). Whilst death was deemed accidental in the majority of cases (66.1%), a significant proportion of cases were concluded as suicide (20.9%, p<0.01).Polydrug use was evident in the vast majority of cases (98.5%), with central nervous system depressants the most commonly co-administered substances (94.8% of cases). Conclusion We describe the first report regarding antihistamine-related mortality from England. From the NPSAD, we can obtain prescription source and toxicology reports, beyond those reported in national death data. Although incomplete, the response from coroners is good (89%), and provides sufficient cause for concern. The rising trend in antihistamine-related deaths may in-part be contributed to by the perceived negligible dangers associated with antihistamines, both from the general public and professionals. Awareness of the dangerous sedative properties that some antihistamines possess is however heightened in individuals who are deliberately seeking out these effects. An urgent review of sedating antihistamines currently assigned under the P classification is needed to achieve antihistamine harm reduction, balanced against the self-care they enable. References 1. Office for National Statistics. Deaths related to drug poisoning in England and Wales: 2019 registration [internet]. 2020 [cited 18 Oct 2020]. Available from: https://www.ons.gov.uk/peoplepopulationandcommunity/birthsdeathsandmarriages/deaths/bulletins/deathsrelatedtodrugpoisoninginenglandandwales/2019registrations 2. US FDA. Benadryl (diphenhydramine): Drug Safety Communication - Serious Problems with High Doses of the Allergy Medicine. 2020.
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Shabanov, D. V., and Ju E. Lutkovskaya. "Actual antihistamine therapy." Meditsinskiy sovet = Medical Council, no. 16 (November 14, 2020): 26–35. http://dx.doi.org/10.21518/2079-701x-2020-16-26-35.
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The significance of the issues of allergic diseases is not in doubt. It is difficult to find a person who has not suffered at least some Allergy symptom, not everyone develops diseases, but most people face Allergy symptoms. The prevalence of various allergic diseases is increasing every year, currently reaching 30% of the population, and the world health organization predicts it will reach 50% in the next few decades. The most common nosologies are allergic rhinitis, bronchial asthma, atopic dermatitis, urticaria, but there are many other conditions of hypersensitivity. This article addresses the issues of inflammatory reactions in General and specifically allergic inflammation, discusses the main aspects of the pathogenesis of allergic rhinitis and urticaria, and questions of drug therapy for these diseases. Most people are sure that they can take anti-allergic medications for allergies, and most often they are referring to antihistamines. Unfortunately, even some medical specialists lack an understanding of the specifics of antihistamine therapy. some people still believe that there are three or four generations of antihistamines, and patients use drugs not as prescribed by doctors, but on the recommendation of friends or pharmacists. Irrational use of antihistamines leads to a decrease in effectiveness, and it is not uncommon to discredit specific drugs and groups of drugs in General. This article demonstrates the results of various European and Asian studies on the effectiveness and safety of antihistamines and bilastin in particular, as well as their own experience of using antihistamines in practice.
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Vuković, Milana, Dunja Vesković, Nemanja Todorović, Tatjana Roš, Jasmina Jovanović-Ljubičić, Danilo Kuzman, Mladena Lalić-Popović, Dejan Miljković, and Boris Milijašević. "Comparative analysis of the consumption of antihistamines for systemic use in the Republic of Serbia and Nordic countries in the period 2009-2019." Hospital Pharmacology - International Multidisciplinary Journal 10, no. 1 (2023): 1250–63. http://dx.doi.org/10.5937/hpimj2301250v.
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Introduction: According to the ATC system of drug classification, group R06 includes H1 antihistamines for systemic use, which are divided into drug groups of the 1st and 2nd generation. Aim: Since there are no national guidelines in Serbia, for treating most allergic diseases, our aim was to compare pharmaceutical products and treatment strategies of systemic antihistamines use in Serbia with that in the Nordic countries that have been recognized as countries with good pharmacoeconomic practice. Material and methods: Data on drug consumption in the Republic of Serbia, the Kingdom of Norway, the Republic of Finland, and the Kingdom of Denmark were collected from the publications of national drug regulatory agencies for the period from 2009 to 2019. Results: Loratadine was the most commonly consumed antihistamine in Serbia in 2009, making 72.32% of the total consumption of drugs in the R06 group. During observed period the consumption of cetirizine increased 21.8 times, levocetirizine increased 36.6 times, desloratadine increased 2.6 times. The most commonly used antihistamines in Serbia in 2016 were: loratadine with 34.86%, followed by desloratadine with 18.70%, and ketotifen with 14.52% of the total consumption of drugs in the R06 group. In 2019, the most commonly used antihistamines were levocetirizine, loratadine, desloratadine and cetirizine. In Norway as well as in Finland and Denmark, during all eleven years (2009-2019) cetirizine was the most consumed antihistamine with mild increase trend in consumption of 1.5-5.74-20.5%. The second most consumed antihistamine in Norway and in Finland was desloratadine and in Denmark, fexofenadine. A decrease in consumption was recorded in case of loratadine in all three Scandinavian countries. First generation antihistamines promethazine and dexchlorpheniramine showed a continuous but minimal downward trend. Conclusion: Unlike Norway, Sweden and Denmark, in Serbia in the last 11 years, the consumption trends of antihistamines have not been consistent and seem to depend on various factors such as price.
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Cho, Kyoo H., Ji E. Lee, Sook K. Song, and Phil Hyu Lee. "Chorea induced by antihistamine drugs." Movement Disorders 25, no. 4 (January 27, 2010): 519–20. http://dx.doi.org/10.1002/mds.22965.
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Kareva, E. N. "Pharmacological optimization of antihistamine profile." Russian Medical Inquiry 6, no. 2 (2022): 92–97. http://dx.doi.org/10.32364/2587-6821-2022-6-2-92-97.
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Antihistamines are the first-line treatment for allergic diseases. The optimization of pharmacological properties of these pharmacotherapeutics is provided by the synthesis of new molecules with better safety profile (no penetration via the blood-brain barrier or less risk of drug interactions) or more selective affinity to H1-receptors (active optical isomer). In real clinical practice, drugs with extrahepatic metabolism have an advantage, the effectiveness of which does not depend on concomitant therapy, and the maximum concentration is reached in the shortest possible time, which ensures a rapid onset of action. Comfort use and, therefore, adherence to treatment is also an essential aspect of pharmacotherapy. Current orodispersible H1-receptor antagonists have a clinically significant antihistamine effect and agree with patient expectations due to comfort use and no need to take them with water. As a result, these medications are suitable for specific categories of individuals, e.g., children, patients with difficulty of swallowing, and people practicing an active lifestyle. KEYWORDS: histamine, antihistamines, levocetirizine, pharmacokinetics, pharmacodynamics, orodispersible forms, compliance. FOR CITATION: Kareva E.N. Pharmacological optimization of antihistamine profile. Russian Medical Inquiry. 2022;6(2):92–97 (in Russ.). DOI: 10.32364/2587-6821-2022-6-2-92
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Tsarev, S. V. "Antihistamine therapy in pediatric practice." Medical Council, no. 11 (July 16, 2018): 136–39. http://dx.doi.org/10.21518/2079-701x-2018-11-136-139.
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The article considers the role of histamine in the pathogenesis of allergic diseases and other pathological conditions. The mechanisms that contribute to the development of skin itching are considered separately. The article also shows the role and function of H1-histamine receptor blockers in the treatment of allergic diseases and pseudo allergic reactions. The mechanism of action, indications, contraindications and side effects of the antihistamine therapy are presented. The article also discusses the difference in first and second-generation antihistamines and shows the possible advantages of the first-generation drugs in paediatric practice. The article presents data on the use of dimethindene maleate (Fenistil) in children’s practice, including the use for the relief of skin itching of various genesis.
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Stahl, Stephen M. "Selective Histamine H1 Antagonism: Novel Hypnotic and Pharmacologic Actions Challenge Classical Notions of Antihistamines." CNS Spectrums 13, no. 12 (December 2008): 1027–38. http://dx.doi.org/10.1017/s1092852900017089.
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Numerous “antihistamines” as well as various psychotropic medications with antihistamine properties are widely utilized to treat insomnia. Over-the-counter sleep aids usually contain an antihistamine and various antidepressants and antipsychotics with antihistamine properties have sedative-hypnotic actions. Although widely used for the treatment of insomnia, many agents that block the histamine H1 receptor are also widely considered to have therapeutic limitations, including the development of next-day carryover sedation, as well as problems with chronic use, such as the development of tolerance to sedative-hypnotic actions and weight gain. Although these clinical actions are classically attributed to blockade of the H1 receptor, recent findings with H1 selective agents and H1 selective dosing of older agents are challenging these notions and suggest that some of the clinical limitations of current H1-blocking agents at their currently utilized doses could be attributable to other properties of these drugs, especially to their simultaneous actions on muscarinic, cholinergic, and adrenergic receptors. Selective H1 antagonism is emerging as a novel approach to the treatment of insomnia, without tolerance, weight gain, or the need for the restrictive prescription scheduling required of other hypnotics.
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Lisni, Ida, Ani Anggriani, and Regina Puspitasari. "KAJIAN PERESEPAN OBAT ANTIHISTAMIN PADA PASIEN RAWAT JALAN DI SALAH SATU RUMAH SAKIT DI BANDUNG." Jurnal Riset Kefarmasian Indonesia 2, no. 2 (May 1, 2020): 52–62. http://dx.doi.org/10.33759/jrki.v2i2.77.
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Histamine is one of the factors that cause acute and chronic disorders, so it is necessary to investigate further the mechanism of antihistamines in the treatment of allergic diseases. Antihistamines are substances that can reduce or block the effects of histamine on the body by blocking histamine receptors. Antihistamines are one of the drugs that are often prescribed to children to the elderly. Thus the application of therapy in medicine is needed to ensure the use of appropriate drugs to prevent the occurrence of medication errors so that the goal of therapeutic effectiveness can be achieved. The purpose of this study was to determine the prescribing pattern of antihistamine drugs and assess the accuracy of the administration of antihistamines based on dose accuracy and potential drug interactions. Prescribing studies of this drug are descriptive quantitative and qualitative by using data sources in the form of patient prescription sheets taken retrospectively. The results of quantitative research data show that patients 57.23% were female, the highest age was 55-59 years old 12.26%, the most widely used drug was setirizine 72.48%, dose accuracy 89.60% and more doses 10.40%, the potential for drug interactions occurred in 27.83%, The drug that has the most potential for interaction is setirizine with theophylline.
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Assadi, Sara, Latif Rahman, Mark Kong, and Sukaina Asad. "Could the Use of Antihistamines Have Triggered Reversible Cerebral Vasoconstriction Syndrome? A Case Report." Case Reports in Acute Medicine 4, no. 2 (June 28, 2021): 50–57. http://dx.doi.org/10.1159/000517115.
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A 38-year-old woman presented to the emergency department with recurrent severe headaches. Although initial computer tomography (CT) brain imaging was unremarkable, a later CT venogram demonstrated a small subarachnoid haemorrhage. Magnetic resonance angiogram (MRA) brain imaging subsequently confirmed reversible cerebral vasoconstriction syndrome (RCVS). In the acute setting, RCVS rarely falls into a differential diagnosis for headache presentations, as in this case. The radiological variability can make diagnosis of RCVS challenging. However, there are clinical consistencies that can aid physicians into accurately diagnosing RCVS. A thorough history, including a medication history, can help identify potential triggers of RCVS. As in this case, the combination of commonly used drugs, including antihistamines, provides a plausible trigger for RCVS. The direct vasoactive role of antihistamines is unclear, yet there is suggestion for its ability to potentiate the vasoactive action of other drugs. In this case we propose a causal relationship between the use of antihistamine and the development of RCVS.
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Li, Meng, Junyuan Zhang, Siman Ma, Zhen Jiang, Xin Di, and Xingjie Guo. "Chiral separation of five antihistamine drug enantiomers and enantioselective pharmacokinetic study of carbinoxamine in rat plasma by HPLC-MS/MS." New Journal of Chemistry 44, no. 15 (2020): 5819–27. http://dx.doi.org/10.1039/d0nj00095g.
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Centanni, S., and P. Santus. "The Role of Antihistamine Drugs in Allergic Disorders." Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents 2, no. 3 (September 1, 2003): 284–95. http://dx.doi.org/10.2174/1568014033483743.
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Sutherland, David C. "Antihistamine agents: new options or just more drugs?" Medical Journal of Australia 151, no. 3 (August 1989): 158–62. http://dx.doi.org/10.5694/j.1326-5377.1989.tb139603.x.
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Spasov, A. A., M. V. Chernikov, V. A. Anisimova, T. A. Kuz’menko, and M. M. Osipova. "Search for antihistamine drugs among imidazobenzimidazoles and triazolobenzimidazoles." Pharmaceutical Chemistry Journal 34, no. 2 (February 2000): 48–52. http://dx.doi.org/10.1007/bf02524356.
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Piplani, Sakshi, Puneet Singh, David A. Winkler, and Nikolai Petrovsky. "Potential COVID-19 Therapies from Computational Repurposing of Drugs and Natural Products against the SARS-CoV-2 Helicase." International Journal of Molecular Sciences 23, no. 14 (July 12, 2022): 7704. http://dx.doi.org/10.3390/ijms23147704.
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Repurposing of existing drugs is a rapid way to find potential new treatments for SARS-CoV-2. Here, we applied a virtual screening approach using Autodock Vina and molecular dynamic simulation in tandem to screen and calculate binding energies of repurposed drugs against the SARS-CoV-2 helicase protein (non-structural protein nsp13). Amongst the top hits from our study were antivirals, antihistamines, and antipsychotics, plus a range of other drugs. Approximately 30% of our top 87 hits had published evidence indicating in vivo or in vitro SARS-CoV-2 activity. Top hits not previously reported to have SARS-CoV-2 activity included the antiviral agents, cabotegravir and RSV-604; the NK1 antagonist, aprepitant; the trypanocidal drug, aminoquinuride; the analgesic, antrafenine; the anticancer intercalator, epirubicin; the antihistamine, fexofenadine; and the anticoagulant, dicoumarol. These hits from our in silico SARS-CoV-2 helicase screen warrant further testing as potential COVID-19 treatments.
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Renz, Cheryl L., Dominique Laroche, John D. Thurn, Henry A. Finn, James P. Lynch, Ronald Thisted, and Jonathan Moss. "Tryptase Levels Are Not Increased during Vancomycin-induced Anaphylactoid Reactions." Anesthesiology 89, no. 3 (September 1, 1998): 620–25. http://dx.doi.org/10.1097/00000542-199809000-00010.
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Background Anaphylaxis, mediated by immunoglobulin E, may be clinically indistinguishable but is mechanistically different than chemically mediated anaphylactoid reactions induced by drugs such as morphine, curare, and vancomycin. A test to distinguish anaphylactic from anaphylactoid reactions would clarify therapeutic and medicolegal issues. Tryptase levels identify anaphylactic reactions but have not been evaluated in vivo during anaphylactoid reactions. A prospective, randomized, double-blinded, placebo-controlled trial of antihistamine chemoprophylaxis for rapid vancomycin infusion was performed, and plasma tryptase was measured using a new immunoassay. Histamine release was established by measurement of plasma histamine and the ability of prophylactic H1 and H2 antagonists to prevent common histamine-associated side effects. Tryptase levels were compared with histamine levels and clinical symptoms. Methods Before elective arthroplasty, 40 patients received vancomycin infusion (1 g over 10 min) and pretreatment with either antihistamines (1 mg/kg diphenhydramine and 4 mg/kg cimetidine) or placebo. Changes in tryptase (at peak histamine and 10 min after vancomycin infusion), histamine levels, and histamine-mediated symptoms were assessed using Fisher's exact test, the Student's t test, or the paired t test, as appropriate. Logistic regression models were used to quantify the association of clinical symptoms with antihistamine treatment and serum levels. Results Plasma tryptase levels were unchanged (99% CI, -0.5 to 1.6) independent of increased histamine levels, antihistamine pretreatment, clinical symptoms, or all of these. Histamine levels >1 ng/ml were significantly associated with hypotension, moderate-to-severe rash, and stopped infusion. Antihistamine pretreatment significantly decreased the incidence and severity of the reactions. Conclusion Plasma tryptase levels were not significantly elevated in confirmed anaphylactoid reactions, so they can be used to distinguish chemical from immunologic reactions.
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Kubanov, A. A., and V. V. Chikin. "The benefit of H2 receptors antagonist Rupatadine in treatment for urticaria." Vestnik dermatologii i venerologii 90, no. 3 (June 24, 2014): 116–20. http://dx.doi.org/10.25208/0042-4609-2014-90-3-116-120.
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Second generation antihistamine drugs are mainly used for the therapy of patients suffering from urticaria; however, they are efficient in 45-60% of cases only. New drugs for treatment of urticaria need to be developed and implemented, and second generation antihistamine drug Rupatadine is one of them. At the same time, Rupatadine efficiently inhibits the inflammatory action of the platelet-activating factor. Due to its double action, Rupatadine used perorally in the dose of 10 mg once a day is an efficient drug for treatment of urticaria, and its safety was confirmed by clinical trials.
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Upasana, Khatri, Saini Sunil, and Bharkatiya Meenakshi. "Levo Cetirizine - the Drug with Numerous Plus to Cure Allergic Syndrome Compared to other Treatment Systems." Journal of Pharmaceutical Research 21, no. 4 (December 15, 2022): 105–13. http://dx.doi.org/10.18579/jopcr/v21i4.ms221204.
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Many drugs are available to treat allergic condition. This review focused on why antihistaminics are best choice for treatment of allergic disorder especially allergic rhinitis (AR). AR is a chronic inflammatory disease. AR can be detected by its characteristics of nasal congestion, nasal itching, sneezing, rhinorrhoea, pruritis, redness, tearing and itching of eyes. This is very common and increases day after day. Allergic rhinitis is not lethal but interferes with daily schedule in a sustained manner. It is also observed that after COVID-19, stimuli reactions such as allergic condition, breathing difficulties and nasal irritation are quite common. It is very necessary to treat AR with an effective and powerful medicine because nowadays, many factors trigger these responses such as the environment, food products, pollution, etc. Before treatment of any symptoms it is very necessary to know it pathogenesis. Hence, in this review, we discuss the introduction of AR, its pathogenesis, diagnostics, classification and treatment. We also understand why levocetirizine, a third-generation antihistamine, is superior to all other antihistamines and the most favourable in paediatric patients in many ways. Keywords: Allergic rhinitis, Antihistaminic, Levocetirizine, COVID19, Asthma, Nasal congestion
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Gushchin, Igor S., and Ekaterina N. Medunitsyn. "Bilastine as a modern antihistamine for the treatment of allergic rhinitis and urticaria." Russian Journal of Allergy 17, no. 1 (February 15, 2020): 93–100. http://dx.doi.org/10.36691/raj.2020.17.1.010.
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Antihistamines have long been an integral part of the treatment of allergic rhinitis and urticaria. Treatment of these diseases is usually long-term, so the drugs of choice are H1-antihistamines of the second generation, which have high efficiency and a good safety profile in the absence of clinically significant side effects. The variety of drugs in this group makes it possible to personalize the therapy, using the drug taking into account the individual sensitivity of the patient. One of the antihistamines used in practical allergy at the present time is bilastine. The article presents the data of clinical studies devoted to the research of the effectiveness, safety and tolerability of Hj-antihistamine of the second generation - bilastine. Short-term and long-term use of bilastine in patients with rhinitis (rhinoconjunctivitis) and chronic urticaria has demonstrated it’s good effectiveness and safety, which are due to the pharmacological properties of the medicine and the peculiarities of its metabolism. A number of sources provide data on the high safety profile of bilastine not only in the standard therapeutic dosage, but also with its four-fold increase. The results of these studies are of particular importance, since the clinical recommendations for the management of urticaria in various countries, including Russia, provide for the possibility of increasing the dose of H1 -antihistamines in case of insufficient effectiveness of therapy. Studies have also shown that bilastine has no clinically pronounced side effects that could significantly limit the use of the medicine, including in patients with concomitant diseases, or negatively affect patient’s compliance. According to the results of clinical studies, bilastine is characterized as an effective, safe, well-tolerated medicine for long-term therapy of allergic rhinitis and urticaria.
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Tandra, Gabriella, Amy Yoone, Rhea Mathew, Minzhi Wang, Chadwick M. Hales, and Cassie S. Mitchell. "Literature-Based Discovery Predicts Antihistamines Are a Promising Repurposed Adjuvant Therapy for Parkinson’s Disease." International Journal of Molecular Sciences 24, no. 15 (August 2, 2023): 12339. http://dx.doi.org/10.3390/ijms241512339.
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Parkinson’s disease (PD) is a movement disorder caused by a dopamine deficit in the brain. Current therapies primarily focus on dopamine modulators or replacements, such as levodopa. Although dopamine replacement can help alleviate PD symptoms, therapies targeting the underlying neurodegenerative process are limited. The study objective was to use artificial intelligence to rank the most promising repurposed drug candidates for PD. Natural language processing (NLP) techniques were used to extract text relationships from 33+ million biomedical journal articles from PubMed and map relationships between genes, proteins, drugs, diseases, etc., into a knowledge graph. Cross-domain text mining, hub network analysis, and unsupervised learning rank aggregation were performed in SemNet 2.0 to predict the most relevant drug candidates to levodopa and PD using relevance-based HeteSim scores. The top predicted adjuvant PD therapies included ebastine, an antihistamine for perennial allergic rhinitis; levocetirizine, another antihistamine; vancomycin, a powerful antibiotic; captopril, an angiotensin-converting enzyme (ACE) inhibitor; and neramexane, an N-methyl-D-aspartate (NMDA) receptor agonist. Cross-domain text mining predicted that antihistamines exhibit the capacity to synergistically alleviate Parkinsonian symptoms when used with dopamine modulators like levodopa or levodopa–carbidopa. The relationship patterns among the identified adjuvant candidates suggest that the likely therapeutic mechanism(s) of action of antihistamines for combatting the multi-factorial PD pathology include counteracting oxidative stress, amending the balance of neurotransmitters, and decreasing the proliferation of inflammatory mediators. Finally, cross-domain text mining interestingly predicted a strong relationship between PD and liver disease.
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Nochaiwong, Surapon, Mati Chuamanochan, Chidchanok Ruengorn, and Kednapa Thavorn. "Evidence Gaps in Clinical Trials of Pharmacologic Treatment for H1-Antihistamine-Refractory Chronic Spontaneous Urticaria: A Systematic Review and Future Perspectives." Pharmaceuticals 15, no. 10 (October 10, 2022): 1246. http://dx.doi.org/10.3390/ph15101246.
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No data addressing issues concerning disparities in participant and trial characteristics and trial outcome reporting have been established in clinical trials for H1-antihistamine-refractory chronic spontaneous urticaria (CSU). To better harmonize and compare the different treatment interventions, we systematically evaluated the overall landscape of pharmacological treatments for H1-antihistamine-refractory CSU clinical trials published between 2000 and 2021. This systematic review included 23 randomized clinical trials involving 2480 participants from 22 countries. We found significant increases in the number of globally published and newly tested drugs, especially biologic drugs. Regarding relatively small trials, we found that people living with H1-antihistamine-refractory CSU who were identified as members of minority groups (non-white population), populations of regions other than North America/Europe, and populations of low- to lower/upper-middle-income countries are underrepresented. Most trials were designed to evaluate treatment efficacy and safety profiles; however, less than half of the included trials reported the patient’s perspective in terms of patient-reported outcomes. Disparities in outcome reporting, including clinimetric tools for assessing treatment response and outcome sets, were observed. To close the evidence gap in H1-antihistamine-refractory CSU trials, strategies for improving trial and participant enrollment and standardizing core outcome sets for trial reporting are needed.
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José de Abajo, Francisco, and Luis Alberto García Rodríguez. "Risk of ventricular arrhythmias associated with nonsedating antihistamine drugs." British Journal of Clinical Pharmacology 47, no. 3 (March 1999): 307–13. http://dx.doi.org/10.1046/j.1365-2125.1999.00885.x.
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Poirier, Judes, Madeleine Roy, Giuseppe Campanella, Thérèse Cloutier, and Suzanne Paris. "DEBRISOQUINE METABOLISM IN PARKINSONIAN PATIENTS TREATED WITH ANTIHISTAMINE DRUGS." Lancet 330, no. 8555 (August 1987): 386. http://dx.doi.org/10.1016/s0140-6736(87)92396-8.
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Wolff, S. C., K. Brubaker, T. Navratil, E. H. Fulcher, J. R. Lankford, and J. L. Boyer. "Anticholinergic Effects of Antihistamine Drugs Used in the Clinic." Journal of Allergy and Clinical Immunology 119, no. 1 (January 2007): S153. http://dx.doi.org/10.1016/j.jaci.2006.11.535.
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Wesselhøft, R., L. Rasmussen, P. Jensen, P. Jennum, S. Skurtveit, I. Hartz, J. Reutfors, P. Damkier, M. Bliddal, and A. Pottegård. "Use of hypnotic drugs among Scandinavian children, adolescents, and young adults." European Psychiatry 65, S1 (June 2022): S82—S83. http://dx.doi.org/10.1192/j.eurpsy.2022.250.
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Introduction Hypnotic drug use in children and adolescents is widely debated. Objectives To describe use of hypnotic drugs (melatonin, z-drugs and sedating antihistamines) among 5-24-year-old Scandinavians during 2012 to 2018. Methods Aggregate-level data from public data sources in Sweden, Norway and Denmark. We calculated annual prevalence (users/1000 inhabitants) stratified by sex, age group and country. Quantity of use (Defined Daily Dose (DDD)/user/day) was estimated for Norway and Denmark. Results Melatonin was most frequently used, with an increase from 2012 to 2018 in all countries. Sweden presented the highest rise (7 to 25/1,000) compared to Denmark (6 to 12/1,000) and Norway (10 to 20/1,000). The increase was strongest for females and 15-24-year-olds. Melatonin use was twice as common for males under age 15 years, and slightly more common for females thereafter. The annual prevalence of sedating antihistamine use doubled from 7 to 13/1,000 in Sweden, whereas it was more stable in Norway and Denmark, reaching 8/1,000 and 3/1,000, respectively. Z-drug use decreased in all countries, lowering to 4/1,000 in Sweden and Norway in 2018 and 2/1,000 in Denmark. The quantity of hypnotic use in Norway and Denmark was 1 DDD/user/day for melatonin, as compared to 0.1-0.3 for z-drugs and antihistamines. Conclusions There is an increasing use of melatonin and sedating antihistamines among Scandinavian children, adolescents and young adults. The increase is more pronounced in Sweden compared to Norway and Denmark. This Scandinavian discrepancy could reflect variation in frequency of sleep problems or national variation in clinical practice or health care access. Disclosure No significant relationships.
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Nikiforova, G. N., V. M. Svistushkin, and A. V. Zolotova. "Allergic rhinitis. Modern opportunities of pathogenetic therapy." Medical Council, no. 8 (April 18, 2019): 83–88. http://dx.doi.org/10.21518/2079-701x-2019-8-83-88.
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Allergic rhinitis is a global public health problem at the present stage, given the high prevalence, the formation of therapy-resistant phenotypes, high comorbidity and the negative impact on all aspects of a patient’s life. Histamine is one of the main mediators of allergy, and therefore drugs number one in the treatment of patients with AR of all options are antihistamine drugs or H1-blockers. The innovative antihistamine drug of the second generation levocetirizine (Allerway®) prevents the development and facilitates the course of allergic reactions, also has anti-inflammatory and antiallergic action. Allerway® is bioequivalent to the original drug, has broad indications for use, has established itself as an effective drug with a good safety profile.
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Iakovlieva, L. V., O. G. Berdnik, and A. A. Gurtyakova. "Analysis of assortment and volumes of consumption of antihistamin preparations in Ukraine." Farmatsevtychnyi zhurnal, no. 1-2 (August 14, 2018): 12–21. http://dx.doi.org/10.32352/0367-3057.1-2.18.02.
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Over the past 30 years, the prevalence of allergic diseases has doubled every 10 years. According to WHO, currently about 5% of the world's adult population and 15% of children suffer from allergic diseases.
The purpose of the study is to analyze the assortment of antihistamines in the pharmaceutical market of Ukraine, determine the availability for consumers by the indicator of Ca.s. and their volumes of consumption by ATS/DDD-methodology during 2014‒2017.
Represented in the pharmaceutical market of Ukraine antihistamines were analyzed according to the analytical system of research of the pharmaceutical market «Pharmstandard» of the company «MORION». As an indicator of socio-economic accessibility of antihistamines, an indicator of the adequacy of the solvency of Ca.s. Volumes of consumption of antihistamines were examined using the WHO recommended ATC/DDD methodology. Information on the DDD values is available on the WHO website: www.who.int/countries/ukr.
During the period under study, there was a decrease in the number of TNs against the background of an increase in the number of INNs of all three generations. The quantitative ratio of domestic and foreign producers has not changed significantly.
Based on the results of the Ca.s. found that antihistamines for the population of Ukraine for all four years are mainly high-availability drugs. And only 14.29% of fexofenadine preparations (in 2014) and 3.22% of desloratadine preparations (in 2015) are medium-accessible. The low indicator of the adequacy of solvency (Ca.s.) to 5%, confirms the availability of drugs group R06 and guarantees their consumption in the face of a decline in economic development in Ukraine.
The most consumed during the studied four years were LS of five INNs: Mebrogroline, Cetirizine, Loratadine, Levocetirizine and Desloratadine, related to all three generations of antihistamines. Consumption of this group of the most used drugs during the study period was 89.94%, 90.64%, 90.70% and 90.47%, respectively, over the years of total consumption of antihistamines.
During 2014‒2017 there is a decrease in the number of TN drugs against the background of an increase in the number of INN: from 172 TN on the basis of 16 INN in 2014 to 160 TN on the basis of 17 INNs in 2017. The quantitative ratio of domestic and foreign producers has not changed significantly. The assortment of antihistamine drugs for 2017 is quite wide. On the pharmaceutical market of Ukraine are represented drugs of all three generations. Depending on the manufacturer, the prices varied from low to high, namely the spread of prices from 1.65 UAH to 212.43 UAH in 2014 and from 4.76 UAH to 567.63 UAH in 2017, which made it possible to select individual drugs taking into account the active ingredients, dosage form and price.
According to the results of the Ca.s indices, it is established that antihistamines for the population of Ukraine for the entire four years are represented mainly by high-availability TN. And only 14.29% of fexofenadine preparations (in 2014) and 3.22% of desloratadine preparations (in 2015) are medium-accessible. The low indicator of the adequacy of solvency (Ca.s.) to 5%, confirms the availability of drugs group R06 and guarantees their consumption in the face of a decline in economic development in Ukraine.
According to the analysis of the consumption of antihistamines in DDDs/1000 inhabitants/day, the increase in the consumption of these drugs was observed every year from 9.64 in 2014 to 10.60 in 2017. At the same time, the consumption of the latest generation drugs increased: INN desloratadine (from 0.98 in 2014 to 1.27 in 2017) and INN levocetirizine (from 1.91 in 2014 to 2.53 in 2017), which have profitable pharmacokinetic characteristics and the optimal efficiency / safety ratio. The consumption of second-generation drugs remains stably large: loratadine (2.62 in both 2014 and 2017), cetirizine (from 1.78 in 2014 to 1.94 in 2017). Along with sufficiently high pharmacological activity, they have a relatively low cost, since they are mainly presented in the pharmaceutical market in the form of generic versions.
Against the background of the trend of increasing consumption of antihistamines in Ukraine over the last four years (from 9.64 DDDs/1000 inhabitants/day in 2014 to 10.60 DDDs/1000 inhabitants/day in 2017), it is established that in Ukraine there is a large number patients who do not receive in full, or do not receive quality adequate antihistamine therapy at all.
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Zakeri, Mina, Majid Monajjemi, and Ali Ebrahimi. "Thermodynamic investigation of promethazine, loratadine, cetirizine and buclizine as antihistamine drugs; monte carlo and semi-empirical studies." Nexo Revista Científica 33, no. 01 (July 20, 2020): 94–108. http://dx.doi.org/10.5377/nexo.v33i01.10050.
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In this article, we discussed about four antihistamine drug called promethazine, loratadine, cetirizine and buclizine. Promethazine in this list is the only one in first generation antihistamine classification with CNS sedation effect and the other three belongs to second generation antihistamine group which are non-sedation and used to treat in many different anti-allergenic fields. In the following we optimized potential, kinetic and total energy of these molecules at body temperature (310 k˚) and environment temperature (298 k ˚) using Mont Carlo method in Amber force field in 500 ns. The quantum mechanics calculations and molecular structure of these molecules investigated using B3LYP level of theory with 6-31 G (d) as a basis set. Theoretical computations were performed to study thermodynamic parameters and frequency analysis. Electronic, thermal, zero point and gibs free energy and enthalpy were estimated in frequency analysis. Semi empirical computations were summarized to pm3 method and different energy parameters (total energy, Binding Energy, Isolated Atomic Energy, Electronic Energy, Core–Core Interaction and Heat of Formation.
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Gelfand, Erwin W. "Pediatric Allergic Rhinitis: Factors Affecting Treatment Choice." Ear, Nose & Throat Journal 84, no. 3 (March 2005): 163–68. http://dx.doi.org/10.1177/014556130508400314.
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Allergic rhinitis is the most prevalent chronic allergic disease in children. Although it is not life-threatening, it can have a significantly detrimental effect on a child's quality of life, and it may exacerbate a number of common comorbidities, including asthma and sinusitis. The Allergic Rhinitis and its Impact on Asthma guidelines, an evidence-based algorithm for the treatment of allergic rhinitis, advocate the use of antihistamines for the treatment of the broad spectrum of the disease. However, first-generation antihistamines are associated with a number of adverse events, including central nervous system impairment and anticholinergic and cardiovascular effects. Moreover, these agents have not been rigorously tested in the pediatric population. Nevertheless, first-generation antihistamines remain the most frequently prescribed agents in this class of drugs. This is despite the fact that the second-generation antihistamines are largely free of the undesirable side effects associated with their predecessors and the fact that they have been shown to be effective in relieving allergic rhinitis symptoms in children in a number of large-scale clinical trials. Therefore, when selecting an antihistamine for a child, it would be prudent to consider the full range of antihistamines and to base the selection of a particular drug on its efficacy, onset and duration of action, and safety profile.
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Krivopalov, A. A., S. A. Rebrova, and P. A. Shamkina. "Features of the modern antihistamines use in the treatment of allergic rhinitis." Meditsinskiy sovet = Medical Council, no. 12 (September 19, 2021): 101–8. http://dx.doi.org/10.21518/2079-701x-2021-12-101-108.
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Allergic rhinitis remains one of the most relevant problems of modern otorhinolaryngology. The widespread prevalence, late diagnosis, underestimation of the possible risks of disease progression, the development of complications (including asthma) prompts the development and improvement of new treatment options for allergic rhinitis. Allergic rhinitis is a heterogeneous disease that presents with various clinical phenotypes, and therefore the severity of nasal symptoms can vary from mild malaise to severe disease.. Today, pharmacotherapy remains the most frequently used treatment tactic for patients with allergic rhinitis. While prescribing therapy the doctor develops an individual treatment plan based on the principles of personalized medicine, considering: the dominant symptoms, anamnesis data on previous therapy and the effect of treatment, the type of inflammation (Th2-type, mixed inflammation), concomitant diseases (conjunctivitis, asthma, etc.) etc.) and patient preferences. The tissue effects of the histamine mediator lead to the development of symptoms during the course of the disease, which determines the wide-spread use of antihistamines in the treatment of rhinitis. Antihistamines of the second generation are devoid of sedative effects, have a long-lasting effect and a good safety profile. One of the modern II generation antihistamines is bilastine. The research results proved the high antihistaminic activity of bilastine 20 mg in vitro and in vivo, the absence of cardiac and sedative side effects on the central nervous system, the ability to eliminate the nasal and ocular symptoms of disease and improve the quality of life of patients with allergic rhinitis. Thus, bilastine fully complies with current EAACI / WAO ARIA requirements for drugs used to treat AR. The paper presents a clinical case of a patient with chronic persistent allergic rhinitis, household sensitization with a slight uncontrolled course. The oral antihistamine bilastine was added to intranasal glucocorticosteroids, which help to relieve symptoms of the disease, stabilize the condition and prepare the patient for subsequent allergen-specific immunotherapy.
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Nucera, Eleonora, Riccardo Inchingolo, Rosario Nicotra, Manuela Ferraironi, Anna Giulia Ricci, Giuseppe Parrinello, Marilena La Sorda, Maurizio Sanguinetti, Antonio Gasbarrini, and Angela Rizzi. "Influence of Antihistamines on Basophil Activation Test in Food Allergy to Milk and Egg." Diagnostics 11, no. 1 (December 30, 2020): 44. http://dx.doi.org/10.3390/diagnostics11010044.
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Background: The basophil activation test (BAT) is used to improve the accuracy of food allergy diagnosis. To date, the influence of antiallergic drugs on BAT reactivity is poorly investigated. The aim of the study was to investigate if BAT results were influenced by antihistamine intake for 3 months in a cohort of patients with IgE-mediated food allergy to milk or egg. Methods: A retrospective, single-center, observational study was performed. We enrolled subjects with history of hypersensitivity reaction after specific food ingestion, positive skin prick tests and specific IgEs, concomitant allergic rhinitis, and, contraindication to the double-blind, placebo-controlled food challenge due to personal history of systemic reactions related to the ingestion of culprit food. Validated allergens (α-lactoalbumin, β-lactoglobulin, casein, egg white, and yolk) for BAT were used. Results: Thirty-nine patients with well-documented food symptoms and positive allergological workup were included in the study. BAT was positive in 29 patients. The mean percentages of CD63+ expression to specific culprit allergen did not change after the administration of drugs. Conclusions: This was the first study assessing the effects of oral antihistamines on basophil reactivity in cow’s milk and egg food allergy. Antihistamines do not interfere with BAT results.
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Källén, B. "Use of antihistamine drugs in early pregnancy and delivery outcome." Journal of Maternal-Fetal & Neonatal Medicine 11, no. 3 (January 2002): 146–52. http://dx.doi.org/10.1080/jmf.11.3.146.152.
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BROOKS, C., and K. KARL. "Hay fever treatment with combined antihistamine and cyclooxygenase-inhibiting drugs." Journal of Allergy and Clinical Immunology 81, no. 6 (June 1988): 1110–17. http://dx.doi.org/10.1016/0091-6749(88)90877-9.
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Murashkin, N. N., M. I. Gluzmin, A. I. Materikin, N. N. Murashkin, M. I. Gluzmin, and A. I. Materi kin. "Assessment of the efficacy of antihistamine drugs in complex treatment of chronic itchingdermatoses." Vestnik dermatologii i venerologii 87, no. 4 (August 15, 2011): 84–87. http://dx.doi.org/10.25208/vdv1050.
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The authors give a review of current concepts of mechanisms of skin itching development for different types of chronic dermatoses. The authors also present the results of a study aimed at assessing the efficacy of different 2nd generation antihistamine drugs used for complex treatment of 83 patients aged 14-73 suffering from different chronic itching dermatoses (atopic dermatitis, eczema, pruritus, chronic urticaria, progressing psoriasis, lichen acuminatus, contact allergic dermatitis). The authors conclude that Glencet (levocetirizine) used in a complex therapy of dermatoses accompanied with itching can efficiently arrest both subjective itching sensations and objective clinical symptoms of the diseases as well as reliably (р < 0.001) reduce the term of inpatient care by 4.8 ± 2.3 on average. Glencet (levocetirizine) is a drug of choice among the 2nd generation antihistamine drugs used for treatment of chronic skin diseases accompanied with itching.
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Luss, L. V. "Fenkarol - the first nonsedative antihistamine for parenteral administration." Russian Journal of Allergy 12, no. 1 (December 15, 2015): 54–59. http://dx.doi.org/10.36691/rja491.
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In the pathogenesis of various diseases histamine performs an important role relating to one of the most important mediators involved in the regulation of vital functions in the body. Histamine plays a key role in the development of allergic diseases and pseudoallergic reactions. Therefore, in clinical practice, of particular interest are drugs that block the effects of histamine - antihistamines. The lecture highlights mechanisms of action of histamine and indications for antihistamines. Particular attention is given to parenteral forms of antihistamines and benefits of a new form of antihistamines for parenteral use without sedation - fenkarol one of quinuclidine derivatives. Features and advantages of antihistamines - quinuclidine derivatives, first developed in Laboratory of academician M.D. Mashkovsky are presented.
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Amina Mumtaz, Amina Mumtaz, and Sajjad ul Hassan and Shafaq Mubarak Sajjad ul Hassan and Shafaq Mubarak. "Development and Optimization of Green Method for Antihistamine Using Ecofriendly Reagent in Pure and Pharmaceutical Formulations by Microwave Assisted Spectrophotometry." Journal of the chemical society of pakistan 41, no. 6 (2019): 1028. http://dx.doi.org/10.52568/000810/jcsp/41.06.2019.
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Synthetic substances and solvents utilized in investigation of drugs crumble the earth as well as human health. So attempts should be made to minimize or eliminate the utilization of obnoxious chemicals and solvents. The objective of study is to develop the green spectroscopic method using new ecofriendly chromogenic reagent for the evaluation of antihistamine i.e. desloratadine in pure and commercial dosage forms. Both heating systems (conventional and microwave assisted procedures) are used for the development of color. The method is based on formation of stable blue coloured complex with ammonium molybdate in the presence of acid having λmax at 732nm respectively. All the reaction conditions and different statistic parameters for the proposed methods have been studied. The method is found to be rapid, precise and accurate and can be successfully used for the determination of antihistamines in bulk and commercial tablet formulations.
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Oh, Ki-Kwang, Md Adnan, and Dong-Ha Cho. "Network Pharmacology Study to Elucidate the Key Targets of Underlying Antihistamines against COVID-19." Current Issues in Molecular Biology 44, no. 4 (April 8, 2022): 1597–609. http://dx.doi.org/10.3390/cimb44040109.
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Antihistamines have potent efficacy to alleviate COVID-19 (Coronavirus disease 2019) symptoms such as anti-inflammation and as a pain reliever. However, the pharmacological mechanism(s), key target(s), and drug(s) are not documented well against COVID-19. Thus, we investigated to decipher the most significant components and how its research methodology was utilized by network pharmacology. The list of 32 common antihistamines on the market were retrieved via drug browsing databases. The targets associated with the selected antihistamines and the targets that responded to COVID-19 infection were identified by the Similarity Ensemble Approach (SEA), SwissTargetPrediction (STP), and PubChem, respectively. We described bubble charts, the Pathways-Targets-Antihistamines (PTA) network, and the protein–protein interaction (PPI) network on the RPackage via STRING database. Furthermore, we utilized the AutoDock Tools software to perform molecular docking tests (MDT) on the key targets and drugs to evaluate the network pharmacological perspective. The final 15 targets were identified as core targets, indicating that Neuroactive ligand–receptor interaction might be the hub-signaling pathway of antihistamines on COVID-19 via bubble chart. The PTA network was constructed by the RPackage, which identified 7 pathways, 11 targets, and 30 drugs. In addition, GRIN2B, a key target, was identified via topological analysis of the PPI network. Finally, we observed that the GRIN2B-Loratidine complex was the most stable docking score with −7.3 kcal/mol through molecular docking test. Our results showed that Loratadine might exert as an antagonist on GRIN2B via the neuroactive ligand–receptor interaction pathway. To sum up, we elucidated the most potential antihistamine, a key target, and a key pharmacological pathway as alleviating components against COVID-19, supporting scientific evidence for further research.
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Muñoz-Cano, Rosa M., Rocio Casas-Saucedo, Antonio Valero Santiago, Irina Bobolea, Paula Ribó, and Joaquim Mullol. "Platelet-Activating Factor (PAF) in Allergic Rhinitis: Clinical and Therapeutic Implications." Journal of Clinical Medicine 8, no. 9 (August 29, 2019): 1338. http://dx.doi.org/10.3390/jcm8091338.
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Platelet-activating factor (PAF) is a lipid mediator involved in several allergic reactions. It is released from multiple cells of the immune system, such as eosinophils, neutrophils, and mast cells, and also exerts its effect on most of them upon specific binding to its receptor, becoming a pleiotropic mediator. PAF is considered a potential relevant mediator in allergic rhinitis, with a key role in nasal congestion and rhinorrhoea due to its effect on vascular permeability. Interestingly, despite its potential relevance as a therapeutic target, no specific PAF inhibitors have been studied in humans. However, rupatadine, a second-generation antihistamine with dual antihistamine and anti-PAF effects has shown promising results by both blocking nasal symptoms and inhibiting mast cell activation induced by PAF, in comparison to antihistamine receptor drugs. In conclusion, the inhibition of PAF may be an interesting approach in the treatment of allergic rhinitis as part of a global strategy directed at blocking as many relevant inflammatory mediators as possible.
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Martínez-Algaba, C., J. M. Bermúdez-Saldaña, R. M. Villanueva-Camañas, S. Sagrado, and M. J. Medina-Hernández. "Analysis of pharmaceutical preparations containing antihistamine drugs by micellar liquid chromatography." Journal of Pharmaceutical and Biomedical Analysis 40, no. 2 (February 2006): 312–21. http://dx.doi.org/10.1016/j.jpba.2005.07.037.
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Sadykov, B. G. "Experience of using citral in combination with nonspecific drugs for Rh and ABO incompatible pregnancies." Kazan medical journal 43, no. 4 (November 16, 2021): 47–49. http://dx.doi.org/10.17816/kazmj87207.
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To prevent hemolytic disease of the newborn (HDN) in Rh and ABO incompatible pregnancies, effective desensitizing treatment is required. For this purpose, various means and methods have been proposed and tested. Among them are antihistamine drugs, namely antistin, citral (L. Girshfeld, T. G. Solovyova, I. A. Vasilyeva).
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Kast, Richard E., Marc-Eric Halatsch, and Rafael Rosell. "OPALS: A New Osimertinib Adjunctive Treatment of Lung Adenocarcinoma or Glioblastoma Using Five Repurposed Drugs." Cells 10, no. 5 (May 10, 2021): 1148. http://dx.doi.org/10.3390/cells10051148.
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Background: Pharmacological targeting aberrant activation of epidermal growth factor receptor tyrosine kinase signaling is an established approach to treating lung adenocarcinoma. Osimertinib is a tyrosine kinase approved and effective in treating lung adenocarcinomas that have one of several common activating mutations in epidermal growth factor receptor. The emergence of resistance to osimertinib after a year or two is the rule. We developed a five-drug adjuvant regimen designed to increase osimertinib’s growth inhibition and thereby delay the development of resistance. Areas of Uncertainty: Although the assembled preclinical data is strong, preclinical data and the following clinical trial results can be discrepant. The safety of OPALS drugs when used individually is excellent. We have no data from humans on their tolerability when used as an ensemble. That there is no data from the individual drugs to suspect problematic interaction does not exclude the possibility. Data Sources: All relevant PubMed.org articles on the OPALS drugs and corresponding pathophysiology of lung adenocarcinoma and glioblastoma were reviewed. Therapeutic Opinion: The five drugs of OPALS are in wide use in general medicine for non-oncology indications. OPALS uses the anti-protozoal drug pyrimethamine, the antihistamine cyproheptadine, the antibiotic azithromycin, the antihistamine loratadine, and the potassium sparing diuretic spironolactone. We show how these inexpensive and generically available drugs intersect with and inhibit lung adenocarcinoma growth drive. We also review data showing that both OPALS adjuvant drugs and osimertinib have data showing they may be active in suppressing glioblastoma growth.
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Kovalevskaya, M. A., and L. A. Filina. "Clinical forms of allergic eye manifestations: prospects of therapy." Russian Ophthalmological Journal 13, no. 1 (March 15, 2020): 94–101. http://dx.doi.org/10.21516/2072-0076-2020-13-1-94-101.
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The review presents the main clinical forms of eye allergy. The modern classification of conjunctival allergic diseases (CAD) divides them into several types according to the presence or absence of proliferative changes complicated by atopic dermatitis or mechanical artifactual irritation. These include: 1) allergic conjunctivitis (AC) without proliferative changes, including seasonal allergic conjunctivitis and chronic allergic conjunctivitis, in which the symptoms persist the whole year; 2) atopic keratoconjunctivitis, a chronic allergic conjunctival disease affecting patients with atopic dermatitis, 3) spring keratoconjunctivitis with conjunctival and proliferative changes — papillary conjunctival hyperplasia with the involvement of the cornea (superficial punctate keratitis, erosion, persistent epithelial defect, sterile corneal ulceration), 4) giant papillary conjunctivitis (GPC) accompanied by proliferative changes in the upper lid and the arch of the conjunctiva of the eyeball, caused by mechanical irritation factors (contact lenses, eye prostheses, or surgical sutures). To treat these conditions, the following groups of medications are used: artificial tears; topical antihistamine drugs; mast cell membrane stabilizers; dualaction drugs, preferably without preservatives, nonsteroid anti-inflammatory medications and vasoconstrictors having side effects. Olopatadin 1 mg/1 ml, preservative free (Olofadin -ECO), has certain advantages due to the fact that it combines antihistamine and membrane stabilizing action. Due to the presence of an antihistamine component in the composition, an acute reaction is stopped, while the effect of the drug is accumulated due to the presence of a membrane-stabilizing component. It is safe for long-term therapy.
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Lee, Fu-Shing, Lois J. Matthews, John H. Mills, Judy R. Dubno, and Warren Y. Adkins. "Gender-Specific Effects of Medicinal Drugs on Hearing Levels of Older Persons." Otolaryngology–Head and Neck Surgery 118, no. 2 (February 1998): 221–27. http://dx.doi.org/10.1016/s0194-5998(98)80020-x.
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As part of a large-scale study of presbyacusis, responses to a medicinal drug questionnaire from 85 female and 126 male human subjects were analyzed. Medicinal drugs were divided into 35 categories based on their pharmacologic effects. Subjects' ages ranged from 60 to 82 years. At least 10% of subjects reported taking drugs in 14 of 35 categories. Results were significantly different between female and male subjects. In men, none of the 14 categories showed a statistically significant relation to the pure-tone average (PTA) of 500, 1000, 2000, and 4000 Hz. In women, 3 of the 14 categories showed a statistically significant relation to the PTA. First, the average PTA of female subjects taking β-adrenergic medication was 20 dB higher (poorer) than those not taking β-adrenergic medication. Second, women taking antihistamine/cold preparations had an average PTA 9 dB higher (poorer) than those not taking antihistamine/cold preparations. Third, the average PTA of women taking calcium-channel blockers (CCBs) was 12 dB lower (better) than those not taking CCBs. In men, however, these drugs produced effects on the PTA of less than 3 dB. Differences between women and men were not explainable by differences in age or hearing level.
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Skorokhodkina, O. V., and S. V. Klyucharyova. "Rationale for selecting antihistamine drugs for the therapy of chronic urticaria in terms of efficacy and safety." Vestnik dermatologii i venerologii 90, no. 2 (April 24, 2014): 64–71. http://dx.doi.org/10.25208/0042-4609-2014-90-2-64-71.
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Goal of the study. To compare the efficacy of antihistamine drugs for the therapy of chronic urticaria taking into consideration their effect on the patients’ cognitive functions. Materials and methods. The study involved 178 patients with chronic urticaria who were divided into six groups taking second generation antihistamine drugs: Cetirizine (n = 38), Levocetirizine (n = 27), Fexofenadine (n=26), Ebastine (n = 33), Loratadine (n = 26) and Desloratadine (n = 28). The patients recorded dynamic changes in clinical symptoms of the disease (number of urticarial components, skin itching intensity, availability or absence of urticarial derniographism, angioedema signs and signs of the shortness of breath and reduced blood pressure) in their individual diaries. Baseline signs of the patients’ cognitive condition and those recorded during the treatment were studied using the Kraepelin’s arithmetic test (modified by Schulte), I.M. Lushchikhina’s verbal and visual thinking assessment method and method for memorizing ten words. The control group comprised 31 subjects without chronic urticaria. Results of the study. Ebastine and Fexofenadine are the most efficient antihistamine drugs for the treatment of chronic urticaria. At the same time, they do not have any negative effect on the patients’ cognitive functions so they can be recommended for long-term treatment of chronic urticaria. In spite of its evident positive therapeutic effect, Cetirizine reduces mental alertness and deteriorates thinking in patients with chronic urticaria. Because of this, the drug must be prescribed with care for long-term administration to those patients whose professional activities demand increased attention concentration. Loratadine has a positive effect on the patients’ attention and thinking. However, taking into consideration its low efficacy, the drug can be prescribed as the basis therapy for the treatment of light forms of chronic urticaria.
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Abbaali, Izra, Danny A. Truong, Shania D. Day, Nancy Haro-Ramirez, and Naomi S. Morrissette. "Systematic Analysis of Clemastine, a Candidate Apicomplexan Parasite-Selective Tubulin-Targeting Agent." International Journal of Molecular Sciences 23, no. 1 (December 22, 2021): 68. http://dx.doi.org/10.3390/ijms23010068.
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Apicomplexan parasites, such as Toxoplasma gondii, Plasmodium spp., Babesia spp., and Cryptosporidium spp., cause significant morbidity and mortality. Existing treatments are problematic due to toxicity and the emergence of drug-resistant parasites. Because protozoan tubulin can be selectively disrupted by small molecules to inhibit parasite growth, we assembled an in vitro testing cascade to fully delineate effects of candidate tubulin-targeting drugs on Toxoplasma gondii and vertebrate host cells. Using this analysis, we evaluated clemastine, an antihistamine that has been previously shown to inhibit Plasmodium growth by competitively binding to the CCT/TRiC tubulin chaperone as a proof-of-concept. We concurrently analyzed astemizole, a distinct antihistamine that blocks heme detoxification in Plasmodium. Both drugs have EC50 values of ~2 µM and do not demonstrate cytotoxicity or vertebrate microtubule disruption at this concentration. Parasite subpellicular microtubules are shortened by treatment with either clemastine or astemizole but not after treatment with pyrimethamine, indicating that this effect is not a general response to antiparasitic drugs. Immunoblot quantification indicates that the total α-tubulin concentration of 0.02 pg/tachyzoite does not change with clemastine treatment. In conclusion, the testing cascade allows profiling of small-molecule effects on both parasite and vertebrate cell viability and microtubule integrity.
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Guseva, A. L., and M. L. Derbeneva. "Antihistamines in the treatment of allergic rhinitis." Meditsinskiy sovet = Medical Council, no. 6 (May 27, 2020): 90–96. http://dx.doi.org/10.21518/2079-701x-2020-6-90-96.
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Allergic rhinitis is a common allergic disease that have a substantially negative impact on the patients’ quality of life. Pharmacotherapy is essential to the treatment of allergic rhinitis, including the use of antihistamines, leukotriene receptor antagonists, topical steroids, decongestants, cromones, anticholinergics and their various combinations. Antihistamines are commonly prescribed drugs to treat mild, moderate, and severe disease. The article discusses the mechanisms of action of first- and second-generation antihistamines and compares the potential side effects and drug interactions.First-generation antihistamines differ in their significant sedative and hypnotic effect, mainly due to their pronounced lipophilic properties and ability to transverse the blood–brain barrier and bind to H1-histamine receptors in the central nervous system. Due to low selectivity of the first-generation antihistamines, they may interact with other receptors and develop adverse side effects, including dry mouth, nasopharynx, more rarely pupillary dilation, increased intraocular pressure, tachycardia, and urine retention. Bilastine is a highly selective second-generation antihistamine that has a rapid onset and a prolonged action. This drug does not interact with the P450 cytochrome system or undergo significant metabolism in the human body, and therefore the drug has low potential for drug-drug interactions. Bilastine is excreted almost completely unchanged and therefore does not require dose adjustment in patients with renal or hepatic impairment. Bilastine demonstrated similar efficacy in seasonal allergic rhinitis compared to cetirizine and desloratadine, as well as similar efficacy and safety in long-term treatment of patients with perennial rhinitis compared to cetirizine. Bilastine is well tolerated both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity.
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Raikar, Prachi, Bannimath Gurupadayya, and Venkata Sairam Koganti. "Recent Advances in Chiral Separation of Antihistamine Drugs: Analytical and Bioanalytical Methods." Current Drug Delivery 15, no. 10 (October 22, 2018): 1393–410. http://dx.doi.org/10.2174/1567201815666180830100015.
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Pandey, Ajay Kumar, and Dharmendra Dwivedi. "TITRIMETRIC ASSAY OF SOME ANTIHISTAMINE DRUGS WITH PYRIDINIUM FLUORO CHROMATE (PFC) REAGENT." Journal of Drug Delivery and Therapeutics 8, no. 5 (September 11, 2018): 407–10. http://dx.doi.org/10.22270/jddt.v8i5.1947.
Full textAbstract:
In the present paper, simple, convenient accurate, precise and cost effective titrimetric (Visual volumetric) method has been reported for the estimation of some antihistamine drugs e.g. Cyproheptadine hydrochloride (CPH), Fexofenadine hydrochloride (FFH), Promethazine hydrochloride (PMH) and Pheniramine maleate (PM) in pure form and in their pharmaceutical preparations such as Ciplactin (Tab), Allegra (Tab), Phenergan (Tab and Inj) and Avil (Tab and Inj) with Pyridinium fluoro chromate (PFC) reagent. The principle of this method is based on the fact, that each pharmaceutical drug consists of certain organic functional group which on oxidation by a known excess of potassium iodate in sulphuric acid medium followed by iodometric titration in presence of reagent Pyridinium fluoro chromate (PFC) establishes stoichiometric relationship between drug molecule and an oxidising reagent Pyridinium fluoro chromate (PFC).Different results obtained for each drug during experiment, has been validated by different statistical parameters such as percentage error, standard deviation (SD) and coefficient of variation (CV).Results obtained from these statistical parameters proves the accuracy and precision of adopted method.
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Mahjour, Marjan, and Arash Khoushabi. "An Herbal H2 Blocker in Melasma Treatment." Current Drug Discovery Technologies 17, no. 3 (July 15, 2020): 272–77. http://dx.doi.org/10.2174/1570163816666190121145653.
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Background: Melasma is a skin pigmentation disorder that remains resistant to available therapies. The exact cause of melasma is unknown. Histamine is an inflammatory factor. Its involvement in pigmentation is obscure. The aim of this study is to introduce an herbal antihistamine H2 receptor which is effective in these disorders. Methods: This is a review study by searching the electronic databases and also Persian Medicine books, from 2000 to 2018 by the keywords such as H2 antagonist, H2 blocker and melasma. Results: According to the researched studies, histamine can induce melanogenesis and melasma after a series of stages in the body. Also, Histamine, through receptors 2, triggers melasma. Therefore, it can be said that antihistamine H2 receptor can be effective in melasma. Considering chemical antihistamine, H2 receptors have side effects, such as digestive problems, H2 antagonists can be used in the treatment of diseases such as dyspepsia but they have multiple complications. On the other hand, there is an herbal H2 antagonist that can be useful for melasma due to having some special properties. Conclusion: Herbal H2 blockers should be noted in melasma treatment along with the topical drugs.
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Martina, Emanuela, Federico Diotallevi, Tommaso Bianchelli, Matteo Paolinelli, and Annamaria Offidani. "Novel Therapeutic Approaches and Targets for Treatment of Chronic Urticaria: New Insights and Promising Targets for a Challenging Disease." Current Pharmaceutical Biotechnology 22, no. 1 (December 31, 2020): 32–45. http://dx.doi.org/10.2174/1389201021666200630140137.
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Background: Chronic Spontaneous Urticaria (CSU) is a disease characterized by the onset of wheals and/or angioedema over 6 weeks. The pathophysiology for CSU is very complex, involving mast cells and basophils with a multitude of inflammatory mediators. For many years the treatment of CSU has been based on the use of antihistamines, steroids and immunosuppressive agents with inconstant and frustrating results. The introduction of omalizumab, the only licensed biologic for antihistamine- refractory CSU, has changed the management of the disease. Objective: The aim of this article is to review the current state of the art of CSU, the real-life experience with omalizumab and the promising drugs that are under development. Methods:: An electronic search was performed to identify studies, case reports, guidelines and reviews focused on the new targets for the treatment of chronic spontaneous urticaria, both approved or under investigation. The search was limited to articles published in peer-reviewed journals in the English Language in the PubMed database and trials registered in Clinicaltrials.gov. Results:: Since the advent of omalizumab, the search for new therapies for chronic spontaneous urticaria has had a new impulse. Anti-IgE drugs will probably still be the cornerstone of therapy, but new targets may prove effective in syndromic urticaria or refractory cases. Conclusion:: Although omalizumab has been a breakthrough in the treatment of CSU, many patients do not completely get benefit and even require more effective treatments. Novel drugs are under investigation with promising results.