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- Volume 4, Issue 5, 2005
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents - Volume 4, Issue 5, 2005

Volume 4, Issue 5, 2005
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Editorial [Hot Topic: Antihistamines (Guest Editor: Esen Ozkaya)]
By Esen OzkayaAntihistamines are among the most commonly prescribed drugs in the world. They are widely used in the treatment of conditions such as urticaria and angioedema, seasonal and perennial rhinoconjunctivitis, and pruritic diseases occurring in children and adults. The first generation antihistamines are still widely available and in use today since their first introduction more than 50 years ago. As these drugs have consi Read More
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Development of New H1 Antihistamines: The Importance of Pharmacokinetics in the Evaluation of Safe and Therapeutically Effective Agents
Authors: Rhys Whomsley and Margherita S. BenedettiH1 antihistamines are widely used in the treatment of allergic disorders. The CNS depressant and antimuscarinic effects of the first generation compounds limited their use in allergic disorders, and the second generation compounds were developed to reduce or eliminate these effects. However, the use of the first second generation H1 antihistamines, terfenadine and astemizole, under certain circumstances, was associ Read More
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Action Mechanism of Antihistamines and the New Antihistamines
Authors: Neslihan Sendur and Meltem UsluAntihistamines have an important role in dermatology. In order to understand how antihistamines work, effects of histamine should be examined first. Histamine was first defined in 1920s and was shown to take part in the pathogenesis of diseases such as urticaria, anaphylaxis, asthma, and allergic rhinitis. The main goal in the treatment of urticaria and other diseases related to histamine is to keep this powerful mediator's ef Read More
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The Role of Antihistamines in the Management of Allergic Rhinitis
Authors: Murat Unal and Gunter HafizAllergic rhinitis is a common disease worldwide and antihistamines remain the mainstay of pharmacotherapy for allergic rhinitis. Histamine is one of main mediators involved in the disease pathophysiology. The primary mechanism of antihistamine action is believed to be competitive antagonism of histamine receptors, specifically the H1-receptors. These receptors are present on nerve endings, smooth muscles, and Read More
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Use of Antihistamines in Ocular Therapy
By Acun GezerApproximately 20% of the general population have allergic symptoms of various forms. One third of these people have also ocular symptoms. Some forms of ocular allergy can cause severe symptoms and result in significant ocular morbidity. Allergic ocular disease consists of allergic conjunctivitis (including seasonal hay fever and perennial allergic rhinoconjunctivitis and acute anaphylaxis), giant papillary conjunctivitis Read More
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Antihistamine Use in Dermatologic Disorders
By Emel FetilAntihistamines can be used in various disorders of dermatology. They are the mainstay of pharmacological therapy used in the management of urticaria and angioedema. They are also important in the management of atopic dermatitis, mastocytosis, eosinophilic disorders, contact dermatitis and flushing. Pruritus associated with other conditions such as lichen planus, pityriasis rosea, lichen simplex chronicus, derma Read More
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New Oral Antihistamines in Pediatrics and Safety of Antihistamines in Children
Authors: Ulker Ones and Zeynep TamayH1 antihistamines are first line drugs in the treatment of allergic rhinitis and chronic idiopathic urticaria and widely used in children as well as in adults. Although first-generation antihistamines are effective in relieving allergic symptoms, they are not preferred because of their sedative side effects. The earliest "second generation" antihistamines, terfenadine and astemizole, non-sedating alternatives to the first generation co Read More
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Adverse Systemic Reactions of Antihistamines: Highlights in Sedating Effects, Cardiotoxicity and Drug Interactions
Authors: Tulin Ergun and Sadiye KusAntihistamines are already among the most frequently used pharmaceutical compounds and with the predictable increase of the prevalence of atopic disease, even more patients are expected to use them in future. Though the common belief on their safety has existed since some decades, they, including the over the counter ones, might potentially bear serious side effects. Thus , the following article focuses on the adverse Read More
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Adverse Effects of Antihistamines on Skin Tests and Antihistamines in Pregnancy
Authors: Isil Kilinc and Sibel AlperAllergy skin tests are the best and most reliable method of diagnosing allergies. Medications may influence the interpretation of skin testing. Antihistamines interfere with prick and intradermal skin tests, while they do not suppress patch tests. Some other medications also have influence on allergy skin tests. It's important to know the suppression mechanism and the duration of the inhibitory effect of these drugs on the sk Read More
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Adverse Cutaneous Reactions of Systemic Antihistamines
By Esen OzkayaCutaneous adverse reactions to systemic antihistamines are rare but an important finding. The reaction may vary from an eczematous eruption as the most frequent type, to rare but severe reactions such as urticaria / angioedema, erythema multiforme / Stevens-Johnson syndrome or Lyell syndrome. This is a review of the reported types of cutaneous adverse reactions due to systemically administered old and new antihistamines.
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Implication for Thiazolidinediones (TZDs) as Novel Potential Anti- Inflammatory Drugs
Authors: H. Xu, D. Finas, F. Koster, G. Griesinger, M. Friedrich, K. Diedrich and D. HornungPPAR-γ (peroxisome proliferator activated receptor gamma) mediates ligand-dependent transcriptional activation and repression. PPAR-γ was shown to be directly activated by naturally occurring fatty acids and several synthetic compounds such as thiazolidinediones (TZDs), agonists of PPAR-γ. TZDs are used in the first place as orally active antidiabetic agents in the treatment of type 2 diabetes. Lately, it has been implic Read More
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Inhibition of DNA Polymerase λ Suppresses 12-O-Tetradecanoylphorbol- 13-Acetate-Induced Inflammation
Authors: Yoshiyuki Mizushina, Hiromi Yoshida and Kengo SakaguchiWe found that compounds, which can selectively inhibit the activity of mammalian DNA polymerase λ (pol λ) in vitro, show an anti-12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammatory effect in mice. Originally, we screened selective inhibitors for each of the mammalian DNA polymerases, and found two novel pol λ-inhibitors, phenolic compounds termed petasiphenol and curcumin (diferuloylmethane). Cu Read More
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