DOCSLIB.ORG

Review of H1 Antihistamines in the Treatment of Chronic Idiopathic Urticaria

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Review of H1 Antihistamines in the Treatment of Chronic Idiopathic Urticaria CONTINUING MEDICAL EDUCATION Review of H1 Antihistamines in the Treatment of Chronic Idiopathic Urticaria Eugene Monroe, MD GOAL To understand chronic idiopathic urticaria (CIU) to better manage patients with the condition OBJECTIVES Upon completion of this activity, dermatologists and general practitioners should be able to: 1. Describe the effect of CIU on patient quality of life. 2. Discuss antihistamine use in the treatment of CIU. 3. Explain the anti-inflammatory properties of antihistamines. CME Test on page 104. This article has been peer reviewed and is accredited by the ACCME to provide continuing approved by Michael Fisher, MD, Professor of medical education for physicians. Medicine, Albert Einstein College of Medicine. Albert Einstein College of Medicine designates Review date: July 2005. this educational activity for a maximum of 1 This activity has been planned and implemented category 1 credit toward the AMA Physician’s in accordance with the Essential Areas and Policies Recognition Award. Each physician should of the Accreditation Council for Continuing Medical claim only that credit that he/she actually spent Education through the joint sponsorship of Albert in the activity. Einstein College of Medicine and Quadrant This activity has been planned and produced in HealthCom, Inc. Albert Einstein College of Medicine accordance with ACCME Essentials. Dr. Monroe is in the speakers program and has been a clinical investigator for Sanofi-Aventis and Schering- Plough Corporation. The author discusses off-label use for antihistamines, antileukotrienes, corticosteroids, cyclosporine, doxepin, and tricyclic antidepressants. Dr. Fisher reports no conflict of interest. Chronic idiopathic urticaria (CIU) can have a to the individual. Oral H1 antihistamines are the profound effect on patient quality of life (QOL). mainstay of therapy for CIU, but agents within Ideally, any therapy used to treat CIU should be this class diverge in their individual therapeutic effective across a wide range of doses without indices. The literature was reviewed to compare causing unwanted side effects; a wide therapeu- the currently available oral H1 antihistamines tic window allows the physician to tailor treatment regarding their efficacy and safety at a wide range of doses. If sedation and cognitive impair- ment are considered relevant to treatment selec- Accepted for publication April 12, 2005. tion due to their effect on QOL and safety, then Dr. Monroe is President, Department of Dermatology, Advanced newer-generation agents should be selected Healthcare, Milwaukee, Wisconsin. over older-generation antihistamines. There are Reprints: Eugene Monroe, MD, Department of Dermatology, Advanced Healthcare, Milwaukee, WI 53209-4590 few well-controlled clinical studies in which (e-mail: [email protected]). newer-generation agents have been directly 118 CUTIS® Antihistamines for CIU compared. Moreover, there are no evidence- the effect of a disease or its treatment. This based data demonstrating statistical superiority parameter is particularly pertinent to CIU, as of one newer-generation agent over another in evidenced by O’Donnell et al9 whose analysis of a the treatment of CIU. However, of the newer disease-specific, purpose-designed questionnaire agents, those that are labelled nonsedating at and the Nottingham Health Profile demonstrated recommended doses (fexofenadine, loratadine, that patients with chronic urticaria experienced and desloratadine) should be selected over considerable disability, handicap, and reduced cetirizine. In cases where the physician judges QOL. Part 1 of the health profile showed that that a higher-than-recommended dose should be patients were restricted in areas of mobility, prescribed, or when the patient is likely to take a sleep, and energy and experienced pain, social higher dose, the relative safety profile of these isolation, and altered emotional reactions. Part 2 agents demands detailed consideration. showed that patients experienced problems in Cutis. 2005;76:118–126. relation to work, home management, social life, relationships, sex life, hobbies, and holidays. Interestingly, patients in this survey had almost ow idiopathic is chronic idiopathic urticaria identical scores for part 1 of the health profile as (CIU)? With the fast pace of scientific and did patients with coronary artery disease; both H medical discovery, it is anomalous that dis- groups experienced lack of energy, feelings of eases with no known cause remain. However, social isolation, and emotional upset.9 despite the fact that CIU is less well understood Perhaps because skin diseases are so visible and than many other diseases, recent findings have thus potentially stigmatizing, dermatology patients partially illuminated this condition’s etiology. can be impacted significantly in terms of QOL; At least 2 subgroups of patients with CIU exist. however, the effect of CIU appears to be particu- One group is composed of 30% to 50% of patients larly acute. Using the validated Dermatology Life with CIU with autoimmune chronic urticaria Quality Index (DLQI), a survey of 170 consecutive caused by autoantibodies against either the high- patients had results that showed that patients with affinity immunoglobulin E (IgE) receptor Fc⑀RI or, CIU experienced greater QOL impairment than less commonly, IgE.1,2 Patients in this subgroup outpatients with either psoriasis, acne, or vitiligo have an increased likelihood of thyroid autoimmu- and experienced a comparable level of impairment nity; thyroid autoantibodies, Hashimoto thyroidi- to patients with severe atopic dermatitis.10 Because tis, and Graves disease are recognized as being of CIU’s devastating effect on health-related QOL associated with CIU.3 Indeed, 27% of patients and the discomfort of CIU, appropriate treatment with CIU have high-titre antithyroglobulin, selection is crucial. The ideal treatment for CIU antithyroid peroxidase autoantibodies, or both, would not only rid the patient of the wheals, and 19% have abnormal thyroid function.3 How- edema, and pruritus that characterize the condition ever, the remaining 50% to 70% of patients with but also improve QOL. This review outlines the CIU are truly idiopathic, because there is no treatment options available, focusing on oral H1 known cause for the disease.1 antihistamines, and offers a means of differentiating In keeping with the illusive nature of CIU, the this class of agent. prevalence of the disease has not been firmly estab- lished.4 Most recent estimates suggest that 15% to Antihistamines in the Treatment of CIU 20% of the US population experience at least one It is well established that elevated tissue levels of episode of urticaria in their lifetime, and up to 3% histamine are found in the skin of patients with of the population are diagnosed with CIU.5,6 Inter- different forms of chronic urticaria.11-13 Although estingly, middle-aged women are more likely to more subclasses of histamine receptors have been 7 experience the condition than other groups ; also, identified, those initially isolated—H1 and H2— women are approximately 3 times more likely than are involved in the cutaneous responses seen in men to acquire any autoimmune disease during urticaria. Specifically, the binding of histamine to 8 their lifetime, supporting the notion that CIU is the H1 receptor causes erythema (by vasodilation), often an autoimmune disease. edema (by increasing vascular permeability), and itching. The same responses, with the exception of Quality of Life itching, are caused by histamine binding to the H2 The impact of a disease extends beyond physical signs receptor. In 30% to 50% of patients diagnosed with and symptoms; health-related quality of life (QOL) CIU, histamine release from mast cells leads to also should play a pivotal role in the evaluation of wheal formation because of an autoimmune process. VOLUME 76, AUGUST 2005 119 Antihistamines for CIU In contrast, patients with CIU without this auto- following overdose of older-generation antihista- immune response experience the same effects of mines because of the drug’s lack of selectivity.22-25 mast cell degranulation and subsequent release of Because older-generation antihistamines can histamine by a process yet to be elucidated. bind to H1 receptors in the brain and histamine in The sentinel involvement of histamine in CIU the brain plays a role in central nervous system is, therefore, unequivocal; irrespective of etiology, arousal and alertness, these agents also are associated the appropriate use of H1 antihistamines—which with sedation and cognitive impairment (eg, stabilize an active conformation of the H1 receptor impaired sensorimotor coordination and decreases in and thus prevent activation by histamine—remains attention span, memory function, ability to process the basis of treatment.14 However, for patients information, and psychomotor performance16,26,27). unresponsive to conventional H1-antihistamine The binding of first-generation antihistamines to monotherapy, adjunctive treatments often are pre- cerebral H1 receptors has been demonstrated in scribed including a combination of H1 antihistamines many studies employing objective psychometric tests (either 2 different newer-generation agents con- and also by the relatively new technique of positron currently or a newer-generation agent plus a first- emission tomographic imaging.28-30 generation agent at night), H2 antihistamines, tricyclic antidepressants (principally doxepin), Newer-Generation Antihistamines antileukotriene therapy,
Load more

Recommended publications
  • 22-556Orig1s000
    CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 22-556Orig1s000 MEDICAL REVIEW(S) MEDICAL OFFICER REVIEW Division Of Pulmonary, Allergy, and Rheumatology Products, HFD-570 APPLICATION: NDA 22-556 TRADE NAME: Karbinal ER™ APPLICANT/SPONSOR: Tris Pharma USAN NAME: Carbinoxamine Extended-Release MEDICAL OFFICER: Peter Starke, MD Oral Suspension TEAM LEADER: Theresa Michele, MD CATEGORY: Antihistamine DATE: February 25, 2013 ROUTE: Oral SUBMISSIONS REVIEWED IN THIS DOCUMENT Document Date Submission Date Application/Doc Comments October 4, 2012 October 5, 2012 SD-17 Complete Response submission January 8, 2013 January 9, 2013 SD-20 Response to labeling (formatting) IR RELATED APPLICATIONS Date Application Comments REVIEW SUMMARY: This is clinical review of a Complete Response (CR) to a CR action taken by the Agency on October 7, 2011, for a 505(b)(2) application from Tris Pharma for Carbinoxamine Extended-Release (ER) Oral Suspension, equivalent to 4 mg of carbinoxamine maleate (CM) per 5 mL. The formulation is a sustained release formulation of carbinoxamine maleate suspended in a drug-polistirex resin complex. The proposed Trade Name is Karbinal ER. The application references both the currently available generic immediate-release Carbinoxamine Maleate 4 mg tablets (ANDA 40-442) and oral solution 4 mg/5 mL(ANDA 40-458), marketed under the brand name Palgic and manufactured by Milkart, Inc., and the no-longer-marketed immediate-release innovator products, Clistin 4 mg tablets (NDA 08-915) and 4 mg/5 mL elixir (NDA 08-955), previously marketed by McNeil. McNeil discontinued marketing the Clistin products in the 1990s, and the Orange Book makes the notation that the Clistin products were not discontinued or withdrawn for safety or efficacy reasons.
    [Show full text]
  • Prescribing Trends of Antihistamines in the Outpatient Setting in Al-Kharj
    Prescribing Trends of Antihistamines in the Outpatient Setting in Al-Kharj Nehad J. Ahmed1*, Menshawy A. Menshawy2 1Department of Clinical Pharmacy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj, Saudi Arabia, 2Department of Medicinal chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj, Saudi Arabia Abstract Aim: This study aims to illustrate the prescribing trends of antihistamines in the outpatient setting in Al-Kharj. Materials and Methods: This is a retrospective study that included the evaluation of antihistamines in the outpatient setting in a public hospital in Al-Kharj. The data were collected from the pharmacy-based computer system. Results: The total number of prescriptions that included antihistamines was 799. Most of the prescribed ORIGINAL ARTICLE ARTICLE ORIGINAL antihistamines were first-generation sedating antihistamines (chlorphenamine and diphenhydramine) (66.33%). About 63.20% of the prescribed antihistamines included chlorpheniramine followed by cetirizine (19.27%) and loratadine (14.39%). Conclusion: Antihistamines were prescribed commonly in the outpatient setting mainly first-generation sedating antihistamines. It is recommended to increase the awareness of health- care providers about the efficacy and the side effects of antihistamines and to encourage them to use these agents wisely. Key words: Antihistamines, outpatient, prescribing, trends INTRODUCTION In addition, antihistamines have been classified as sedating antihistamines (first-generation antihistamines) and non- ntihistamines are used in the sedating antihistamines (second-generation antihistamines).[4] management of allergic conditions. Sedating antihistamines include chlorphenamine, clemastine, They are useful for treating the itching hydroxyzine, alimemazine, cyproheptadine, promethazine, A [1] and ketotifen.[4] Non-sedating antihistamines include that results from the release of histamine.
    [Show full text]
  • FEXOFENADINE HYDROCHLORIDE 180 MG FILM-COATED TABLETS Fexofenadine Hydrochloride
    ID1089 MRP _ UK Version: 07 Review Date: 19/02/2020 PACKAGE LEAFLET: INFORMATION FOR THE USER FEXOFENADINE HYDROCHLORIDE 120 MG FILM-COATED TABLETS FEXOFENADINE HYDROCHLORIDE 180 MG FILM-COATED TABLETS Fexofenadine hydrochloride Read all of this leaflet carefully before you start using this medicine because it contains important information for you. - Keep this leaflet. You may need to read it again. - If you have any further questions, ask your doctor or pharmacist. - This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours. - If you get any of the side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet, (see section 4). In this leaflet: 1. What Fexofenadine hydrochloride is and what it is used for 2. What you need to know before you take Fexofenadine hydrochloride 3. How to take Fexofenadine hydrochloride 4. Possible side effects of Fexofenadine hydrochloride 5. How to store Fexofenadine hydrochloride 6. Contents of the pack and other information 1. WHAT FEXOFENADINE HYDROCHLORIDE IS AND WHAT IT IS USED FOR FEXOFENADINE HYDROCHLORIDE Contains fexofenadine hydrochloride which is an antihistamine. Only Fexofenadine hydrochloride 120 mg tablets is used in adults and adolescents of 12 years and older to relieve the symptoms that occur with hay fever (seasonal allergic rhinitis) such as sneezing, itchy, running or blocked nose and itchy, red and watery eye). Fexofenadine hydrochloride 180 mg tablets is used in adults and adolescents of 12 years and older to relieve the symptoms that occur with long term allergic skin reactions( chronic idiopathic urticaria) such as itching, swelling and rashes 2.
    [Show full text]
  • Cetirizine) – New Drug Approval
    Quzyttir™ (cetirizine) – New drug approval • On October 4, 2019, the FDA approved TerSera Therapeutics’ Quzyttir (cetirizine) injection, for the treatment of acute urticaria in adults and children 6 months of age and older. — Quzyttir is not recommended in pediatric patients less than 6 years of age with impaired renal or hepatic function. • Quzyttir is the first FDA approved intravenous (IV) formulation of cetirizine. Oral formulations of cetirizine are available generically as prescription as well as well over-the-counter (OTC) (eg, Zyrtec®). — Prescription oral cetirizine is approved for perennial allergic rhinitis and chronic urticaria. — Zyrtec and other OTC products are approved for use to temporarily relieve symptoms due to hay fever or other upper respiratory allergies: runny nose, sneezing, itchy and watery eyes, and itching of the nose or throat. • The efficacy of Quzyttir was established in a randomized, active-controlled, double-blind, single-dose study in 262 adult patients with acute urticaria. Patients were treated with Quzyttir or diphenhydramine injection. The primary efficacy endpoint was the change from baseline in patient-rated pruritus score assessed 2 hours post treatment. The study was non-inferiority design with the pre-specified non- inferiority margin of 0.50 for the difference between treatment groups. — The effectiveness of Quzyttir was demonstrated to be non-inferior to the effectiveness of diphenhydramine. The mean change from baseline in patient-rated pruritus score was -1.61 and -1.50 for Quzyttir and diphenhydramine, respectively (adjusted difference: 0.06; 95% CI: - 0.28, 0.40). • The efficacy of Quzyttir for the treatment of acute urticaria down to 6 months of age is based on extrapolation of the efficacy of Quzyttir in adults with acute urticaria and supported by pharmacokinetic data with oral cetirizine hydrochloride in patients 6 months to 17 years of age.
    [Show full text]
  • Histamine and Antihistamines
    ACTA FACULTATIS MEDICAE NAISSENSIS UDC: 615.218 DOI: 10.1515/afmnai-2015-0001 Review article Histamine and Antihistamines Nikola Stojković1, Snežana Cekić2, Milica Ristov3, Marko Ristić1, Davor Đukić1, Maša Binić1, Dragan Virijević1 1University of Niš, Faculty of Medicine, PhD student, Serbia 2Institute of Physiology, University of Niš, Faculty of Medicine , Serbia 3Doctor of Medicine SUMMARY In recent years, there has been a steady increase in the prevalence of allergic diseases. Allergic immune response represents a complex network of cellular events involving numerous immune cells and mediators. It represents the interaction of innate and acquired immune response. The key role in the immune cascade is taken by histamine, a natural component of the body, which in the allergic inflammatory response is releasesd by the mast cells and basophils. The aim of this study was to highlight the role of histamine in allergic immunological events, their effect on Th1 and Th2 subpopulation of lymphocytes and the production of the corresponding cytokines, as well as the role of histamine blockers in the treatment of these conditions. Histamine achieves its effect by binding to the four types of its receptors, which are widely distributed in the body. Histamine blockers block a numerous effects of histamine by binding to these receptors. As a highly selective second-generation antihistamine, cetirizine not only achieves its effects by binding to H1 receptors, but also attenuates numerous events during the inflammatory process. Knowledge of the effects
    [Show full text]
  • Cetirizine Hydrochloride) Tablets and Syrup for Oral Use
    70-4573-00-5 ZYRTEC® (cetirizine hydrochloride) Tablets and Syrup For Oral Use DESCRIPTION Cetirizine hydrochloride, the active component of ZYRTEC® tablets and syrup, is an orally active and selective H1-receptor antagonist. The chemical name is (±) - [2- [4- [ (4- chlorophenyl)phenylmethyl] -1- piperazinyl] ethoxy]acetic acid, dihydrochloride. Cetirizine hydrochloride is a racemic compound with an empirical formula of C21H25ClN2O3•2HCl. The molecular weight is 461.82 and the chemical structure is shown below: Cl • CH - N N - CH2 - CH2 - O - CH2 - COOH 2HCl Cetirizine hydrochloride is a white, crystalline powder and is water soluble. ZYRTEC tablets are formulated as white, film-coated, rounded-off rectangular shaped tablets for oral administration and are available in 5 and 10 mg strengths. Inactive ingredients are: lactose; magnesium stearate; povidone; titanium dioxide; hydroxypropyl methylcellulose; polyethylene glycol; and corn starch. ZYRTEC syrup is a colorless to slightly yellow syrup containing cetirizine hydrochloride at a concentration of 1 mg/mL (5 mg/5 mL) for oral administration. The pH is between 4 and 5. The inactive ingredients of the syrup are: banana flavor; glacial acetic acid; glycerin; grape flavor; methylparaben; propylene glycol; propylparaben; sodium acetate; sugar syrup; and water. CLINICAL PHARMACOLOGY Mechanism of Actions: Cetirizine, a human metabolite of hydroxyzine, is an antihistamine; its principal effects are mediated via selective inhibition of peripheral H1 receptors. The antihistaminic activity of cetirizine has been clearly documented in a variety of animal and human models. In vivo and ex vivo animal models have shown negligible anticholinergic and antiserotonergic activity. In clinical studies, however, dry mouth was more common with cetirizine than with placebo.
    [Show full text]
  • Download Large Text CMI (PDF)
    Children's Paedamin Antihistamine Oral Liquid Decongestant and Antihistamine Children 6-12 years Consumer Medicine Information What is in this leaflet? • Itchy, watery eyes Before you give • Nasal congestion Children's Paedamin This leaflet answers some common Children's Paedamin Decongestant Decongestant and questions about Children's and Antihistamine contains Antihistamine Paedamin® Decongestant and Diphenhydramine Hydrochloride Antihistamine. and Phenylephrine Hydrochloride. When you must not give it It does not contain all the available Diphenhydramine Hydrochloride Do not use Children's Paedamin information. It does not take the belongs to a group of medicines Decongestant and Antihistamine if place of talking to your doctor or called 'antihistamines'. you/ your child have an allergy to: pharmacist. Antihistamines help reduce allergic All medicines have risks and symptoms, such as sneezing, runny • any medicine containing benefits. Your doctor or pharmacist nose or itchy, watery eyes, by Diphenhydramine has weighed the risks of you/your preventing the effects of a substance Hydrochloride or other child taking Children's Paedamin called histamine. Histamine is antihistamines Decongestant and Antihistamine produced by the body in response to • any medicine containing against the benefits they expect it foreign substances that the body is Phenylephrine Hydrochloride will have for you. allergic to. • any of the ingredients listed at If you have any concerns about Phenylephrine Hydrochloride the end of this leaflet taking this medicine, ask your belongs to a group of medicines Some of the symptoms of an doctor or pharmacist. called decongestants. allergic reaction may include: Keep this leaflet with the It works by reducing congestion in • shortness of breath medicine.
    [Show full text]
  • Your Child's Emergency Allergy Pack with Antihistamine
    Your Child’s Emergency Allergy Pack with Antihistamine Patient information Paediatric Department Watford General Hospital Hemel Hempstead Hospital If you need this leaflet in another language, large print, Braille or audio version, please call 01923 217 187 or email [email protected] Author Dr Ashley Reece Department Paediatrics Ratified Date / Review Date Feb 2021 / Feb 2024 Version Number / ID Number 40-1104-V1 Why does my child I need an Allergy Action Pack? An allergy action pan is a kit contianing evrything you need in case of an allergic reaction. Is my/ my child’s allergy severe? There is no such thing as a mild or severe allergy as reactions are always unpredicatble. However we do classify reactions as mild, moderate or severe. While it follows that a severe reaction makes the anxiety about the severity of the next reaction high, we cannot predict the severity of subsequent reactions. However there are some foods and some allergies which are assessed as having very low risk of a significant reaction. The way to manage your child with their allergy is to ensure you have the best possible safety net in case of an unforeseen reaction. Your doctor will give you a specific allergy plan (like the one to the right) which you should also give to your child’s school. Generally allergy is mananged by: You MUST avoid any foods which you know your child is allergic to. Avoidance Take care with labels and risk assess any new foods and when eating out in a restaurant or from a take-away.
    [Show full text]
  • Complete Dissertation
    VU Research Portal Histamine H-receptor agonists and antagonists ter Laak, A.M. 1995 document version Publisher's PDF, also known as Version of record Link to publication in VU Research Portal citation for published version (APA) ter Laak, A. M. (1995). Histamine H-receptor agonists and antagonists: molecular modeling and drug design. General rights Copyright and moral rights for the publications made accessible in the public portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognise and abide by the legal requirements associated with these rights. • Users may download and print one copy of any publication from the public portal for the purpose of private study or research. • You may not further distribute the material or use it for any profit-making activity or commercial gain • You may freely distribute the URL identifying the publication in the public portal ? Take down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. E-mail address: [email protected] Download date: 06. Oct. 2021 Histamine H1~receptor Agonists and Antagonists Molecular Modeling and Drug Design , Ton tel' Laak Histamine HI-receptor Agonists and Antagonists Molecular Modeling and Drug Design VRIJE UNIVERSlTEIT Histamine HI-receptor Agonists and Antagonists Molecular Modeling and Drug Design ACADEMISCH PROEFSCHRIFT ter verkrijging van de graad van doctor aan de Vrije Universiteit te Amsterdam, op gezag van de rector magnificus prof.dr E. Boeker, in het openbaar te verdedigen ten overstaan van de promotiecommissie van de faculteit der scheikunde op maandag 16 oktober 1995 te 13.45 uur in het hoofdgebouw van de universiteit, De Boelelaan 1105 door Antonius Marinus ter Laak geboren te Delft Promotor prof.dr H.
    [Show full text]
  • Fexofenadine Hydrochloride) Tablets
    Rev. September 2005 ALLEGRA® (fexofenadine hydrochloride) Tablets DESCRIPTION Fexofenadine hydrochloride, the active ingredient of ALLEGRA, is a histamine H1-receptor antagonist with the chemical name (±)-4-[1 hydroxy-4-[4-(hydroxydiphenylmethyl)-1- piperidinyl]-butyl]-α, α-dimethyl benzeneacetic acid hydrochloride. It has the following chemical structure: The molecular weight is 538.13 and the empirical formula is C32H39NO4•HCl. Fexofenadine hydrochloride is a white to off-white crystalline powder. It is freely soluble in methanol and ethanol, slightly soluble in chloroform and water, and insoluble in hexane. Fexofenadine hydrochloride is a racemate and exists as a zwitterion in aqueous media at physiological pH. ALLEGRA is formulated as a tablet for oral administration. Each tablet contains 30, 60, or 180 mg fexofenadine hydrochloride (depending on the dosage strength) and the following excipients: croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and pregelatinized starch. The aqueous tablet film coating is made from hypromellose, iron oxide blends, polyethylene glycol, povidone, silicone dioxide, and titanium dioxide. CLINICAL PHARMACOLOGY Mechanism of Action Fexofenadine hydrochloride, the major active metabolite of terfenadine, is an antihistamine with selective peripheral H1-receptor antagonist activity. Both enantiomers of fexofenadine hydrochloride displayed approximately equipotent antihistaminic effects. Fexofenadine hydrochloride inhibited antigen-induced bronchospasm in sensitized guinea pigs and histamine
    [Show full text]
  • Paediatric Drug Development: an Opportunity for Academia to Close the Gap
    Paediatric drug development: an opportunity for academia to close the gap Pauline De Bruyne Promotor: Prof. dr. J. Vande Walle Copromotor: Prof. dr. M. Van Winckel Ghent University Faculty of Medicine and Health Sciences Department of Paediatrics and Medical Genetics Paediatric drug development: an opportunity for academia to close the gap Pauline De Bruyne This thesis is submitted as fulfillment of the requirements for the degree of Doctor in Health Sciences. Academic year 2015 – 2016 Promotors: Prof. dr. Johan Vande Walle Prof. dr. Myriam Van Winckel Promotors: Prof. dr. Johan Vande Walle Prof. dr. Myriam Van Winckel Members of the Supervisory Board: Prof. dr. Dirk Matthys dr. Lieve Nuytinck Prof. dr. Luc Van Bortel Members of the Examination Committee: Prof. dr. Johan Van de Voorde (chair) Prof. dr. Karel Allegaert Prof. dr. ir. Sofie Bekaert Prof. dr. Daniel Brasseur Prof. dr. Sylvie Rottey Prof. dr. Jan Van Bocxlaer Prof. dr. John van den Anker The research reported in this thesis was supported by a doctoral grant for Strategic Basic Research (IWT SB-111279) awarded to Pauline De Bruyne, and a grant for Strategic Basic Research (IWT SBO-130033) awarded to the SAFE-PEDRUG project; both of the Agency for Innovation by Science and Technology in Flanders. Voor Sara, Emile en Julie Table of contents TABLE OF CONTENTS Table of contents ............................................................................................................ 1 List of abbreviations ......................................................................................................
    [Show full text]
  • Prescribing Information for High-Dose Fexofenadine in the Management of Urticaria in Adults
    1 Prescribing information for high-dose fexofenadine in the management of urticaria in adults This prescribing information document outlines the prescribing responsibilities between the specialist and GP. GPs are invited to participate. If the GP feels that such prescribing is outside their area of expertise or have clinical concerns about the safe management of the drug in primary care, then he or she is under no obligation to do so. In such an event, clinical responsibility for the patient’s health remains with the specialist. If a specialist asks the GP to prescribe, the GP should reply to this request as soon as practicable. Consultant details GP details Patient details Name: Name: Name: Address: Address: NHS Number: Email: Email: Date of birth: Contact number: Contact number: Contact: Introduction Fexofenadine is a second generation non-sedating H1-antihistamine used in the treatment of allergic disorders. Fexofenadine is a pharmacologically active metabolite of terfenadine. Licensed indication: In adults and children 12 years and older, the licensed dose is 180mg daily for the relief of symptoms associated with chronic idiopathic urticaria. Unlicensed indication (the focus of this document): As advised by Europeani and British Association of Dermatologistsii guidelines, doses of antihistamines up to four times the recommended daily dose may be used in the treatment of urticaria. Adult dosage and administration The licensed maximum recommended daily dose is 180mg once daily taken before a meal. Doses of up to four times the daily recommended dose have been used in the treatment of severe urticaria (unlicensed indication)i Available as: 30mg, 120mg and 180mg tablets Specialist responsibilities Provide patient/carer with relevant written information on the unlicensed use of high-dose fexofenadine and possible side-effects.
    [Show full text]