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Drug Targeting to the Lung: Chemical and Biochemical Considerations
Published in Anthony J. Hickey, Sandro R.P. da Rocha, Pharmaceutical Inhalation Aerosol Technology, 2019
Peter A. Crooks, Narsimha R. Penthala, Abeer M. Al-Ghananeem
Structural modification of the antihistamine azatadine (10a) by replacing the N-methyl group with various carbamate groups eliminates CNS activity (Villani et al. 1986). Loratidine (10b), the most potent compound in this series of carbamates, shows no sedation liability in experimental animals and binds selectively to peripheral histamine receptors (Ahn and Barnett 1986). Other non-sedatory H1 antihistamines are temelastine (11), tazifylline (12), cetrizine (13), levocabastine (14), and epinastine (15) (Brown et al. 1986, Nicholson and Stone 1986, deVos et al. 1986). Tazifylline is reported to have ten times the bronchodilator activity exhibited by either astemizole or terfenadine. The pre-clinical pharmacology of AHR-11325 (16) and PR 1036-654 (17) suggests that both these new compounds are potent, non-sedating, long-acting H1 antagonists (Nolan et al. 1989, Palmer et al. 1989). Ebastine (18a), a structural analogue of terfenadine, has been reported to be a potent, selective, long-lasting antihistamine devoid of sedation at an oral dose of 10 mg (Vincent et al. 1988). Its mode of action is thought to be due to metabolism to the active form (18b) (Vincent et al. 1988).
Pruritus in Atopic Dermatitis: Pathophysiology and Treatment Options
Published in Donald Rudikoff, Steven R. Cohen, Noah Scheinfeld, Atopic Dermatitis and Eczematous Disorders, 2014
Tejesh Surendra Patel, Gil Yosipovitch
Novel pharmacological agents that target these receptors (especially H4-receptor antagonists) may provide alternative and effective therapies to treat pruritus in skin diseases such as atopic dermatitis. A recent small study demonstrated that epinastine, an H1-receptor, antagonist that may have cross-reactivity with the H4-receptor was shown to decrease serum IL-31 levels and itching assessed by a visual analog scale (Otsuka et al. 2011).
Bullous pemphigoid in patients receiving peritoneal dialysis: a case series and a literature survey
Published in Renal Failure, 2021
Kohkichi Morimoto, Tadashi Yoshida, Naoki Washida, Kiyotaka Uchiyama, Takashin Nakayama, Hiroshi Itoh, Mototsugu Oya
A 79-year-old woman with ESRD of unknown cause initiated PD in October 2012 using 1.36% glucose solution for a daytime exchange and icodextrin solution for a night exchange. She had complained of moderate skin itchiness for several years around the induction of PD, and diphenhydramine ointment and skin moisturizer had been prescribed. In addition, we had instructed the patient and her family on the appropriate skincare. However, she presented with systemic pruritic eruptions in May 2017. Although betamethasone ointment and oral epinastine were prescribed, her skin symptoms worsened by scratching. Systemic diffuse blisters and erosive skin lesions developed in the following 2 months (Figure 1(B)). The laboratory data, PD condition, and PD prescriptions are shown in Table 1. The autoantibody for BP was positive (anti-BP180-NC16a antibody 45.8 U/mL), whereas the autoantibodies for pemphigus were negative (anti-Dsg1 antibody <3.0 U/mL and anti-Dsg3 antibody <3.0 U/mL). Skin biopsy revealed subepidermal blister formation and multiple eosinophil infiltration accompanied by the deposition of BP-specific autoantibody. She was diagnosed with BP and administered oral PSL 1 mg/kg (40 mg) daily for 2 weeks. She obtained clinical remission of BP with the disappearance of blister formation and erosion. PSL was tapered (−5 mg/week) without recurrence. In November 2017, she was transferred to a nursing home due to age-related mobility disability and stopped visiting our hospital.
Pharmacotherapeutic management of atopic keratoconjunctivitis
Published in Expert Opinion on Pharmacotherapy, 2020
Ibtesham T Hossain, Priyanka Sanghi, Bita Manzouri
Cromones, such as sodium cromoglycate, are the oldest therapeutic agent for the treatment of allergic eye disease. Due to their delayed onset of action, they are not useful in the acute phase of the disease and are therefore reserved for the prevention of symptoms [11]. Lodoxamide is approximately 2500 times more potent in the prevention of histamine release compared to sodium cromoglycate based on in-vitro assays [25]. Lodoxamide and is used for both the acute and chronic phases of the disease by acting on eosinophil chemotaxis in addition to preventing histamine release from mast cells [24]. If single agents fail to control symptoms then dual-acting agents (olopatadine, ketotifen, azelastine, epinastine, and bepotastine) can be effective. These agents exert multiple pharmacological effects such as stabilization of mast cell degranulation, histamine receptor antagonist action, and inhibition of eosinophil activation and infiltration [26,27]. Olopatadine is a selective H1 receptor antagonist and demonstrates significant effectiveness in comparison to placebo in clinical trials [28,29]. These agents are well tolerated and have minimal side effects, although they are seldom effective in isolation.
Efficacy and Tolerability of Ketotifen in the Treatment Of Seasonal Allergic Conjunctivitis: Comparison between Ketotifen 0.025% and 0.05% Eye Drops
Published in Ocular Immunology and Inflammation, 2019
Andrea Leonardi, Decio Capobianco, Nicola Benedetti, Antonio Capobianco, Fabiano Cavarzeran, Tania Scalora, Rocco Modugno, Oren Mark Feuerman
The last generation of anti-allergic ophthalmic compounds share the mast cell stabilization and the antihistaminic activity in the same molecule: azelastine hydrochloride 0.05%, epinastine hydrochloride 0.05%, ketotifen fumarate 0.025% and 0.05%, and olopatadine hydrochloride 0.1%. Olopatadine 0.2%, the first daily dosing ocular anti-allergic compound, bepotastine besilate 1.5%, and once daily dosing alcaftadine 0.25%, approved by FDA, are not available in the European countries. These agents combine the season-long prevention of allergy attacks by mast cell stability with the instant gratification afforded by the antihistamine, alleviating the immediate signs and symptoms of the patient. Because of their long duration of action, they are prescribed for twice daily dosing; these are considerable advantages over mast cell stabilizers. All topical antihistamines and mast cell stabilizers reduce symptoms and signs of seasonal allergic conjunctivitis when compared with placebo in the short term.5