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H1 antagonist

January 01, 1970

H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines.[citation needed]

In common use, the term "antihistamine" refers only to H1-antihistamines. Virtually all H1-antihistamines function as inverse agonists at the histamine H1-receptor, as opposed to neutral antagonists, as was previously believed.[1][2][3]

Medical uses edit

H1-antihistamines are clinically used in the treatment of histamine-mediated allergic conditions. These indications may include:[4]

H1-antihistamines can be administered topically (through the skin, nose, or eyes) or systemically, based on the nature of the allergic condition.

The authors of the American College of Chest Physicians Updates on Cough Guidelines (2006) recommend that, for cough associated with the common cold, first-generation antihistamine-decongestants are more effective than newer, non-sedating antihistamines. First-generation antihistamines include diphenhydramine (Benadryl), carbinoxamine (Clistin), clemastine (Tavist), chlorpheniramine (Chlor-Trimeton), and brompheniramine (Dimetane). However, a 1955 study of "antihistaminic drugs for colds," carried out by the U.S. Army Medical Corps, reported that "there was no significant difference in the proportion of cures reported by patients receiving oral antihistaminic drugs and those receiving oral placebos. Furthermore, essentially the same proportion of patients reported no benefit from either type of treatment."[5]

Side effects edit

Adverse drug reactions are most commonly associated with the first-generation H1-antihistamines. This is due to their relative lack of selectivity for the H1-receptor and their ability to cross the blood–brain barrier.

The most common adverse effect is sedation; this "side-effect" is utilized in many OTC sleeping-aid preparations. Other common adverse effects in first-generation H1-antihistamines include dizziness, tinnitus, blurred vision, euphoria, incoordination, anxiety, increased appetite leading to weight gain, insomnia, tremor, nausea and vomiting, constipation, diarrhea, dry mouth, and dry cough. Infrequent adverse effects include urinary retention, palpitations, hypotension, headache, hallucination, psychosis and erectile dysfunction.[4][6][7]

The newer, second-generation H1-antihistamines are far more selective for peripheral histamine H1-receptors and have a better tolerability profile compared to the first-generation agents. The most common adverse effects noted for second-generation agents include drowsiness, fatigue, headache, nausea and dry mouth.[4]

Continuous and/or cumulative use of anticholinergic medications, including first-generation antihistamines, is associated with higher risk for cognitive decline and dementia in older people.[8][9]

Pharmacology edit

In type I hypersensitivity allergic reactions, an allergen (a type of antigen) interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the allergen cross-links Immunoglobulin E, tyrosine kinases rapidly signal into the cell, leading to cell degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, the histamine can react with local or widespread tissues through histamine receptors.[citation needed]

Histamine, acting on H1-receptors, produces pruritus, vasodilation, hypotension, flushing, headache, bradycardia, bronchoconstriction, increase in vascular permeability and potentiation of pain.[2]

While H1-antihistamines help against these effects, they work only if taken before contact with the allergen. In severe allergies, such as anaphylaxis or angioedema, these effects may be of life-threatening severity. Additional administration of epinephrine, often in the form of an autoinjector, is required by people with such hypersensitivities.[citation needed]

Comparison of selected sedating antihistamines
Antihistamine Dosea Time to peak Half-lifeb Metabolism Anticholinergic
Diphenhydramine 50 mg 2–3 hours 2–9 hours CYP2D6, others Yes
Doxylamine 25 mg 2–3 hours 10–12 hours CYP2D6, others Yes
Hydroxyzine 25–100 mg 2 hours 20 hours ADH, CYP3A4, others No
Doxepin 3–6 mg 2–3 hours 17 hoursc CYP2D6, others No (at low doses)
Mirtazapine 7.5–15 mg 2 hours 20–40 hours CYP2D6, others No
Quetiapinee 25–200 mg 1.5 hours 7 hoursd CYP3A4 No (at low doses)
Footnotes: a = For sleep/sedation. b = In adults. c Active metabolite nordoxepin half-life is 31 hours. d Active metabolite norquetiapine half-life is 9–12 hours. e Not recommended per literature reviews. Sources: See individual articles for references. See also selected reviews.[10][11][12]

First-generation (unselective) edit

These are the oldest H1-antihistaminergic drugs and are relatively inexpensive and widely available. They are effective in the relief of allergic symptoms, but are typically moderately to highly potent muscarinic acetylcholine receptor (anticholinergic) antagonists as well. These agents also commonly have action at α-adrenergic receptors and/or 5-HT receptors. This lack of receptor selectivity is the basis of the poor tolerability profile of some of these agents, especially when compared with the second-generation H1-antihistamines. Patient response and occurrence of adverse drug reactions vary greatly between classes and between agents within classes.

Classes edit

The first H1-antihistamine discovered was piperoxan, by Ernest Fourneau and Daniel Bovet (1933) in their efforts to develop a guinea pig animal model for anaphylaxis at the Pasteur Institute in Paris.[13] Bovet went on to win the 1957 Nobel Prize in Physiology or Medicine for his contribution. Following their discovery, the first-generation H1-antihistamines were developed in the following decades. They can be classified on the basis of chemical structure, and agents within these groups have similar properties.

Class Description Examples
Ethylenediamines Ethylenediamines were the first group of clinically effective H1-antihistamines developed.
Ethanolamines Diphenhydramine was the prototypical agent in this group. Significant anticholinergic adverse effects, as well as sedation, are observed in this group but the incidence of gastrointestinal adverse effects is relatively low.[4][14]
Alkylamines The isomerism is a significant factor in the activity of the agents in this group. E-triprolidine, for example, is 1000-fold more potent than Z-triprolidine. This difference relates to the positioning and fit of the molecules in the histamine H1-receptor binding site.[14] Alkylamines are considered to have relatively fewer sedative and gastrointestinal adverse effects, but relatively greater incidence of paradoxical central nervous system (CNS) stimulation.[4]
Piperazines These compounds are structurally related to the ethylenediamines and the ethanolamines, and produce significant anticholinergic adverse effects with the exception of hydroxyzine, which has low to no affinity for muscarinic acetylcholine receptors and therefore produces negligible anticholinergic side-effects.[15] Compounds from this group are often used for motion sickness, vertigo, nausea, and vomiting. The second-generation H1-antihistamine cetirizine also belongs to this chemical group.[14]
Tricyclics and Tetracyclics These compounds differ from the phenothiazine antipsychotics in the ring-substitution and chain characteristics.[14] They are also structurally related to the tricyclic antidepressants (and tetracyclics), explaining the H1-antihistaminergic adverse effects of those three drug classes and also the poor tolerability profile of tricyclic H1-antihistamines. The second-generation H1-antihistamine loratadine was derived from compounds in this group.

Common structural features edit

  • Two aromatic rings, connected to a central carbon, nitrogen or CO
  • Spacer between the central X and the amine, usually 2–3 carbons in length, linear, ring, branched, saturated or unsaturated
  • Amine is substituted with small alkyl groups, e.g., CH3

 
X = N, R1 = R2 = small alkyl groups
X = C
X = CO

  • Chirality at X can increase both the potency and selectivity for H1-receptors
  • For maximum potency, the two aromatic rings should be orientated in different planes
    • for example, tricyclic ring system is slightly puckered and the two aromatic rings lie in different geometrical planes, giving the drug a very high potency.

Second-generation edit

Second-generation H1-antihistamines are newer drugs that are much more selective for peripheral H1 receptors as opposed to the central nervous system H1 receptors and cholinergic receptors. This selectivity significantly reduces the occurrence of adverse drug reactions, such as sedation, while still providing effective relief of allergic conditions. The reason for their peripheral selectivity is that most of these compounds are zwitterionic at physiological pH (around pH 7.4). As such, they are very polar, meaning that they are less likely to cross the blood–brain barrier and act mainly outside the central nervous system.

Examples of systemic second-generation antihistamines include:

Examples of topical second-generation antihistamines include:

Regulation edit

Over-the-counter edit

H1 receptor antagonists that are approved for over-the-counter sale, at least in the United States, include the following.[29]

First-generation edit

Common/marketed:

Uncommon/discontinued:

Second-generation edit

See also edit

References edit

  1. ^ Leurs R, Church MK, Taglialatela M (April 2002). "H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects". Clinical and Experimental Allergy. 32 (4): 489–98. doi:10.1046/j.0954-7894.2002.01314.x. PMID 11972592. S2CID 11849647.
  2. ^ a b Simons FE (November 2004). "Advances in H1-antihistamines". The New England Journal of Medicine. 351 (21): 2203–17. doi:10.1056/NEJMra033121. PMID 15548781.
  3. ^ Khilnani G, Khilnani AK (September 2011). "Inverse agonism and its therapeutic significance". Indian Journal of Pharmacology. 43 (5): 492–501. doi:10.4103/0253-7613.84947. PMC 3195115. PMID 22021988.
  4. ^ a b c d e Rossi S (Ed.) (2004). Australian Medicines Handbook 2004. Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2 [page needed]
  5. ^ Hoagland RJ, Deitz EN, Myers PW, Cosand HC (May 1950). "Antihistaminic drugs for colds; evaluation based on a controlled study". Journal of the American Medical Association. 143 (2): 157–60. doi:10.1001/jama.1950.02910370007003. PMID 15415236.
  6. ^ "8 Substances That May be Killing Your Erection". 26 August 2015.
  7. ^ "Drugs That Can Cause Erectile Dysfunction".
  8. ^ Gray SL, Anderson ML, Dublin S, Hanlon JT, Hubbard R, Walker R, et al. (March 2015). "Cumulative use of strong anticholinergics and incident dementia: a prospective cohort study". JAMA Internal Medicine. 175 (3): 401–407. doi:10.1001/jamainternmed.2014.7663. PMC 4358759. PMID 25621434.
  9. ^ Carrière, I; Fourrier-Reglat, A; Dartigues, J-F; Rouaud, O; Pasquier, F; Ritchie, K; Ancelin, M-L (July 2009). "Drugs with anticholinergic properties, cognitive decline, and dementia in an elderly general population: the 3-city study". Archives of Internal Medicine. 169 (14): 1317–1324. doi:10.1001/archinternmed.2009.229. PMC 2933398. PMID 19636034.
  10. ^ Vande Griend JP, Anderson SL (2012). "Histamine-1 receptor antagonism for treatment of insomnia". J Am Pharm Assoc (2003). 52 (6): e210–9. doi:10.1331/JAPhA.2012.12051. PMID 23229983.
  11. ^ Matheson E, Hainer BL (July 2017). "Insomnia: Pharmacologic Therapy". Am Fam Physician. 96 (1): 29–35. PMID 28671376.
  12. ^ Lie JD, Tu KN, Shen DD, Wong BM (November 2015). "Pharmacological Treatment of Insomnia". P T. 40 (11): 759–71. PMC 4634348. PMID 26609210.
  13. ^ Fourneau, Ernest; Daniel Bovet (1933). "Recherches sur l'action sympathicolytique d'un nouveau dérivé du dioxane". Archives Internationales de Pharmacodynamie et de Thérapie. 46: 178–91. ISSN 0003-9780.
  14. ^ a b c d Nelson, Wendel L. (2007). "Antihistamines and Related Antiallergic and Antiulcer Agents". In William O. Foye; Thomas L. Lemke; David A. Williams (eds.). Foye's Principles of Medicinal Chemistry. Hagerstown, Maryland: Lippincott Williams & Wilkins. pp. 1004–1027. ISBN 978-0-7817-6879-5. OCLC 149596645.
  15. ^ Kubo, Nobuo; Shirakawa, Osamu; Kuno, Takayoshi; Tanaka, Chikako (1987). "Antimuscarinic Effects of Antihistamines: Quantitative Evaluation by Receptor-Binding Assay". The Japanese Journal of Pharmacology. 43 (3): 277–282. doi:10.1254/jjp.43.277. PMID 2884340.
  16. ^ "Bepotastine Monograph for Professionals".
  17. ^ "Cetirizine Monograph for Professionals".
  18. ^ Howell G, West L, Jenkins C, Lineberry B, Yokum D, Rockhold R (August 2005). "In vivo antimuscarinic actions of the third generation antihistaminergic agent, desloratadine". BMC Pharmacology. 5: 13. doi:10.1186/1471-2210-5-13. PMC 1192807. PMID 16109168.
  19. ^ "Desloratadine Monograph for Professionals".
  20. ^ Vena GA, Cassano N, Filieri M, Filotico R, D'Argento V, Coviello C (September 2002). "Fexofenadine in chronic idiopathic urticaria: a clinical and immunohistochemical evaluation". International Journal of Immunopathology and Pharmacology. 15 (3): 217–224. doi:10.1177/039463200201500308. PMID 12575922. S2CID 23060714.
  21. ^ "Fexofenadine Monograph for Professionals".
  22. ^ "Ketotifen Monograph for Professionals".
  23. ^ Nettis E, Colanardi MC, Barra L, Ferrannini A, Vacca A, Tursi A (March 2006). "Levocetirizine in the treatment of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study". The British Journal of Dermatology. 154 (3): 533–8. doi:10.1111/j.1365-2133.2005.07049.x. PMID 16445787. S2CID 35041518.
  24. ^ "Levocetirizine Monograph for Professionals".
  25. ^ "Loratadine Monograph for Professionals".
  26. ^ "Azelastine Monograph for Professionals".
  27. ^ Al-Ahmad, Mona; Hassab, Mohammed; Al Ansari, Ali (21 December 2020). "Allergic and Non-allergic Rhinitis". Textbook of Clinical Otolaryngology. Cham: Springer International Publishing. pp. 241–252. doi:10.1007/978-3-030-54088-3_22. ISBN 978-3-030-54087-6. S2CID 234142758. Intranasal H1 antihistamines such as azelastine are effective for controlling nasal symptoms. They need to be applied twice daily.
  28. ^ "Olopatadine Monograph for Professionals".
  29. ^ "OTC Active Ingredients" (PDF). United States Food and Drug Administration. 7 April 2010.

External links edit

January 01, 1970
antagonist, antagonists, also, called, blockers, class, medications, that, block, action, histamine, receptor, helping, relieve, allergic, reactions, agents, where, main, therapeutic, effect, mediated, negative, modulation, histamine, receptors, termed, antihi. H1 antagonists also called H1 blockers are a class of medications that block the action of histamine at the H1 receptor helping to relieve allergic reactions Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines other agents may have antihistaminergic action but are not true antihistamines citation needed In common use the term antihistamine refers only to H1 antihistamines Virtually all H1 antihistamines function as inverse agonists at the histamine H1 receptor as opposed to neutral antagonists as was previously believed 1 2 3 Contents 1 Medical uses 2 Side effects 3 Pharmacology 4 First generation unselective 4 1 Classes 4 2 Common structural features 5 Second generation 6 Regulation 6 1 Over the counter 6 1 1 First generation 6 1 2 Second generation 7 See also 8 References 9 External linksMedical uses editH1 antihistamines are clinically used in the treatment of histamine mediated allergic conditions These indications may include 4 Allergic rhinitis Allergic conjunctivitis Allergic dermatological conditions contact dermatitis Rhinorrhea runny nose Urticaria Angioedema Diarrhea Pruritus atopic dermatitis insect bites Anaphylactic or anaphylactoid reactions adjunct only Nausea and vomiting Sedation first generation H1 antihistamines H1 antihistamines can be administered topically through the skin nose or eyes or systemically based on the nature of the allergic condition The authors of the American College of Chest Physicians Updates on Cough Guidelines 2006 recommend that for cough associated with the common cold first generation antihistamine decongestants are more effective than newer non sedating antihistamines First generation antihistamines include diphenhydramine Benadryl carbinoxamine Clistin clemastine Tavist chlorpheniramine Chlor Trimeton and brompheniramine Dimetane However a 1955 study of antihistaminic drugs for colds carried out by the U S Army Medical Corps reported that there was no significant difference in the proportion of cures reported by patients receiving oral antihistaminic drugs and those receiving oral placebos Furthermore essentially the same proportion of patients reported no benefit from either type of treatment 5 Side effects editAdverse drug reactions are most commonly associated with the first generation H1 antihistamines This is due to their relative lack of selectivity for the H1 receptor and their ability to cross the blood brain barrier The most common adverse effect is sedation this side effect is utilized in many OTC sleeping aid preparations Other common adverse effects in first generation H1 antihistamines include dizziness tinnitus blurred vision euphoria incoordination anxiety increased appetite leading to weight gain insomnia tremor nausea and vomiting constipation diarrhea dry mouth and dry cough Infrequent adverse effects include urinary retention palpitations hypotension headache hallucination psychosis and erectile dysfunction 4 6 7 The newer second generation H1 antihistamines are far more selective for peripheral histamine H1 receptors and have a better tolerability profile compared to the first generation agents The most common adverse effects noted for second generation agents include drowsiness fatigue headache nausea and dry mouth 4 Continuous and or cumulative use of anticholinergic medications including first generation antihistamines is associated with higher risk for cognitive decline and dementia in older people 8 9 Pharmacology editIn type I hypersensitivity allergic reactions an allergen a type of antigen interacts with and cross links surface IgE antibodies on mast cells and basophils Once the allergen cross links Immunoglobulin E tyrosine kinases rapidly signal into the cell leading to cell degranulation and the release of histamine and other chemical mediators from the mast cell or basophil Once released the histamine can react with local or widespread tissues through histamine receptors citation needed Histamine acting on H1 receptors produces pruritus vasodilation hypotension flushing headache bradycardia bronchoconstriction increase in vascular permeability and potentiation of pain 2 While H1 antihistamines help against these effects they work only if taken before contact with the allergen In severe allergies such as anaphylaxis or angioedema these effects may be of life threatening severity Additional administration of epinephrine often in the form of an autoinjector is required by people with such hypersensitivities citation needed Comparison of selected sedating antihistamines Antihistamine Dosea Time to peak Half lifeb Metabolism Anticholinergic Diphenhydramine 50 mg 2 3 hours 2 9 hours CYP2D6 others Yes Doxylamine 25 mg 2 3 hours 10 12 hours CYP2D6 others Yes Hydroxyzine 25 100 mg 2 hours 20 hours ADH CYP3A4 others No Doxepin 3 6 mg 2 3 hours 17 hoursc CYP2D6 others No at low doses Mirtazapine 7 5 15 mg 2 hours 20 40 hours CYP2D6 others No Quetiapinee 25 200 mg 1 5 hours 7 hoursd CYP3A4 No at low doses Footnotes a For sleep sedation b In adults c Active metabolite nordoxepin half life is 31 hours d Active metabolite norquetiapine half life is 9 12 hours e Not recommended per literature reviews Sources See individual articles for references See also selected reviews 10 11 12 First generation unselective editThese are the oldest H1 antihistaminergic drugs and are relatively inexpensive and widely available They are effective in the relief of allergic symptoms but are typically moderately to highly potent muscarinic acetylcholine receptor anticholinergic antagonists as well These agents also commonly have action at a adrenergic receptors and or 5 HT receptors This lack of receptor selectivity is the basis of the poor tolerability profile of some of these agents especially when compared with the second generation H1 antihistamines Patient response and occurrence of adverse drug reactions vary greatly between classes and between agents within classes Classes edit The first H1 antihistamine discovered was piperoxan by Ernest Fourneau and Daniel Bovet 1933 in their efforts to develop a guinea pig animal model for anaphylaxis at the Pasteur Institute in Paris 13 Bovet went on to win the 1957 Nobel Prize in Physiology or Medicine for his contribution Following their discovery the first generation H1 antihistamines were developed in the following decades They can be classified on the basis of chemical structure and agents within these groups have similar properties Class Description Examples Ethylenediamines Ethylenediamines were the first group of clinically effective H1 antihistamines developed Mepyramine pyrilamine Chloropyramine Antazoline Tripelennamine Ethanolamines Diphenhydramine was the prototypical agent in this group Significant anticholinergic adverse effects as well as sedation are observed in this group but the incidence of gastrointestinal adverse effects is relatively low 4 14 Diphenhydramine Carbinoxamine Doxylamine Orphenadrine Bromazine Clemastine Dimenhydrinate Alkylamines The isomerism is a significant factor in the activity of the agents in this group E triprolidine for example is 1000 fold more potent than Z triprolidine This difference relates to the positioning and fit of the molecules in the histamine H1 receptor binding site 14 Alkylamines are considered to have relatively fewer sedative and gastrointestinal adverse effects but relatively greater incidence of paradoxical central nervous system CNS stimulation 4 Pheniramine Chlorphenamine chlorpheniramine Dexchlorpheniramine Dexbrompheniramine Brompheniramine Triprolidine Dimetindene Piperazines These compounds are structurally related to the ethylenediamines and the ethanolamines and produce significant anticholinergic adverse effects with the exception of hydroxyzine which has low to no affinity for muscarinic acetylcholine receptors and therefore produces negligible anticholinergic side effects 15 Compounds from this group are often used for motion sickness vertigo nausea and vomiting The second generation H1 antihistamine cetirizine also belongs to this chemical group 14 Cyclizine Chlorcyclizine Hydroxyzine Meclizine Tricyclics and Tetracyclics These compounds differ from the phenothiazine antipsychotics in the ring substitution and chain characteristics 14 They are also structurally related to the tricyclic antidepressants and tetracyclics explaining the H1 antihistaminergic adverse effects of those three drug classes and also the poor tolerability profile of tricyclic H1 antihistamines The second generation H1 antihistamine loratadine was derived from compounds in this group Promethazine Alimemazine trimeprazine Cyproheptadine Common structural features edit Two aromatic rings connected to a central carbon nitrogen or CO Spacer between the central X and the amine usually 2 3 carbons in length linear ring branched saturated or unsaturated Amine is substituted with small alkyl groups e g CH3 nbsp X N R1 R2 small alkyl groups X C X CO Chirality at X can increase both the potency and selectivity for H1 receptors For maximum potency the two aromatic rings should be orientated in different planes for example tricyclic ring system is slightly puckered and the two aromatic rings lie in different geometrical planes giving the drug a very high potency Second generation editSecond generation H1 antihistamines are newer drugs that are much more selective for peripheral H1 receptors as opposed to the central nervous system H1 receptors and cholinergic receptors This selectivity significantly reduces the occurrence of adverse drug reactions such as sedation while still providing effective relief of allergic conditions The reason for their peripheral selectivity is that most of these compounds are zwitterionic at physiological pH around pH 7 4 As such they are very polar meaning that they are less likely to cross the blood brain barrier and act mainly outside the central nervous system Examples of systemic second generation antihistamines include Acrivastine Benadryl Allergy Relief UK Semprex D US Astemizole Hismanal withdrawn Bepotastine Talion Bepreve 16 Bilastine Blexten Fortecal Lendin Cetirizine Zyrtec Benadryl Allergy One a Day Relief UK 17 Desloratadine Aerius 18 19 Ebastine Evastin Kestine Ebastel Aleva Ebatrol Fexofenadine Allegra 20 21 Ketotifen Zaditor also mast cell stabilizer 22 sometimes classified as a first generation antihistamine see Ketotifen Classification Levocetirizine Xyzal 23 24 Loratadine Claritin 25 Mizolastine Mizollen Quifenadine Phencarol Fenkarol Rupatadine Rupafin Terfenadine Seldane US Triludan UK and Teldane Australia withdrawn Examples of topical second generation antihistamines include Azelastine 26 27 Levocabastine Olopatadine 28 Regulation editOver the counter edit H1 receptor antagonists that are approved for over the counter sale at least in the United States include the following 29 First generation edit Common marketed Brompheniramine Dimetapp Dimetane Chlorpheniramine Chlor Trimeton Dimenhydrinate Dramamine Gravol combination of diphenhydramine and 8 chlorotheophylline Diphenhydramine Benadryl Doxylamine Unisom Uncommon discontinued Chlorcyclizine Dexbrompheniramine Dexchlorpheniramine Methapyrilene Phenindamine Pheniramine Phenyltoloxamine Pyrilamine Thenyldiamine Thonzylamine Triprolidine Second generation edit Cetirizine Zyrtec Fexofenadine Allegra Levocetirizine Xyzal Loratadine Alavert Claritin See also editH2 receptor antagonist H3 receptor antagonistReferences edit Leurs R Church MK Taglialatela M April 2002 H1 antihistamines inverse agonism anti inflammatory actions and cardiac effects Clinical and Experimental Allergy 32 4 489 98 doi 10 1046 j 0954 7894 2002 01314 x PMID 11972592 S2CID 11849647 a b Simons FE November 2004 Advances in H1 antihistamines The New England Journal of Medicine 351 21 2203 17 doi 10 1056 NEJMra033121 PMID 15548781 Khilnani G Khilnani AK September 2011 Inverse agonism and its therapeutic significance Indian Journal of Pharmacology 43 5 492 501 doi 10 4103 0253 7613 84947 PMC 3195115 PMID 22021988 a b c d e Rossi S Ed 2004 Australian Medicines Handbook 2004 Adelaide Australian Medicines Handbook ISBN 0 9578521 4 2 page needed Hoagland RJ Deitz EN Myers PW Cosand HC May 1950 Antihistaminic drugs for colds evaluation based on a controlled study Journal of the American Medical Association 143 2 157 60 doi 10 1001 jama 1950 02910370007003 PMID 15415236 8 Substances That May be Killing Your Erection 26 August 2015 Drugs That Can Cause Erectile Dysfunction Gray SL Anderson ML Dublin S Hanlon JT Hubbard R Walker R et al March 2015 Cumulative use of strong anticholinergics and incident dementia a prospective cohort study JAMA Internal Medicine 175 3 401 407 doi 10 1001 jamainternmed 2014 7663 PMC 4358759 PMID 25621434 Carriere I Fourrier Reglat A Dartigues J F Rouaud O Pasquier F Ritchie K Ancelin M L July 2009 Drugs with anticholinergic properties cognitive decline and dementia in an elderly general population the 3 city study Archives of Internal Medicine 169 14 1317 1324 doi 10 1001 archinternmed 2009 229 PMC 2933398 PMID 19636034 Vande Griend JP Anderson SL 2012 Histamine 1 receptor antagonism for treatment of insomnia J Am Pharm Assoc 2003 52 6 e210 9 doi 10 1331 JAPhA 2012 12051 PMID 23229983 Matheson E Hainer BL July 2017 Insomnia Pharmacologic Therapy Am Fam Physician 96 1 29 35 PMID 28671376 Lie JD Tu KN Shen DD Wong BM November 2015 Pharmacological Treatment of Insomnia P T 40 11 759 71 PMC 4634348 PMID 26609210 Fourneau Ernest Daniel Bovet 1933 Recherches sur l action sympathicolytique d un nouveau derive du dioxane Archives Internationales de Pharmacodynamie et de Therapie 46 178 91 ISSN 0003 9780 a b c d Nelson Wendel L 2007 Antihistamines and Related Antiallergic and Antiulcer Agents In William O Foye Thomas L Lemke David A Williams eds Foye s Principles of Medicinal Chemistry Hagerstown Maryland Lippincott Williams amp Wilkins pp 1004 1027 ISBN 978 0 7817 6879 5 OCLC 149596645 Kubo Nobuo Shirakawa Osamu Kuno Takayoshi Tanaka Chikako 1987 Antimuscarinic Effects of Antihistamines Quantitative Evaluation by Receptor Binding Assay The Japanese Journal of Pharmacology 43 3 277 282 doi 10 1254 jjp 43 277 PMID 2884340 Bepotastine Monograph for Professionals Cetirizine Monograph for Professionals Howell G West L Jenkins C Lineberry B Yokum D Rockhold R August 2005 In vivo antimuscarinic actions of the third generation antihistaminergic agent desloratadine BMC Pharmacology 5 13 doi 10 1186 1471 2210 5 13 PMC 1192807 PMID 16109168 Desloratadine Monograph for Professionals Vena GA Cassano N Filieri M Filotico R D Argento V Coviello C September 2002 Fexofenadine in chronic idiopathic urticaria a clinical and immunohistochemical evaluation International Journal of Immunopathology and Pharmacology 15 3 217 224 doi 10 1177 039463200201500308 PMID 12575922 S2CID 23060714 Fexofenadine Monograph for Professionals Ketotifen Monograph for Professionals Nettis E Colanardi MC Barra L Ferrannini A Vacca A Tursi A March 2006 Levocetirizine in the treatment of chronic idiopathic urticaria a randomized double blind placebo controlled study The British Journal of Dermatology 154 3 533 8 doi 10 1111 j 1365 2133 2005 07049 x PMID 16445787 S2CID 35041518 Levocetirizine Monograph for Professionals Loratadine Monograph for Professionals Azelastine Monograph for Professionals Al Ahmad Mona Hassab Mohammed Al Ansari Ali 21 December 2020 Allergic and Non allergic Rhinitis Textbook of Clinical Otolaryngology Cham Springer International Publishing pp 241 252 doi 10 1007 978 3 030 54088 3 22 ISBN 978 3 030 54087 6 S2CID 234142758 Intranasal H1 antihistamines such as azelastine are effective for controlling nasal symptoms They need to be applied twice daily Olopatadine Monograph for Professionals OTC Active Ingredients PDF United States Food and Drug Administration 7 April 2010 External links editAntihistaminics H1 at the U S National Library of Medicine Medical Subject Headings MeSH Retrieved from https en wikipedia org w index php title H1 antagonist amp oldid 1212799197, wikipedia, wiki, book, books, library,

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