Drug Targeting to the Lung: Chemical and Biochemical Considerations
Anthony J. Hickey, Sandro R.P. da Rocha in Pharmaceutical Inhalation Aerosol Technology, 2019
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
Donald Rudikoff, Steven R. Cohen, Noah Scheinfeld in Atopic Dermatitis and Eczematous Disorders, 2014
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).
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
Using miniature brain implants in rodents for novel drug discovery
Published in Expert Opinion on Drug Discovery, 2019
Ben Waldau
The artificial blood-brain barrier could be evaluated with compounds with known behavior across the blood-brain barrier. Drugs with known penetration of the blood-brain barrier, for example, are propranolol, caffeine, antipyrine, carbamazepine, and trazadone. In mice, propranolol could be administered i.p. at a dose of 1.5 mg/kg to 6 mg/kg [95], caffeine at a dose of 6.25 mg/kg to 100 mg/kg i.p. [96], antipyrine at 20 mg/kg i.v. [97], carbamazepine at 20 mg/kg to 40 mg/kg i.p. [98] and trazadone at 5 mg/kg to 10 mg/kg i.p. [99]. Drugs with known poor penetration of the blood-brain barrier are sulpiride [100], epinastine [101], cimetidine [102], quinidine [103], and prazosin [104]. Sulpiride could be administered at a dose of 3 to 10 mg/kg i.p. [105], epinastin at 1 mg/kg s.c. [106], cimetidine at 50 mg/kg i.p. [107], quinidine at 100 mg/kg i.p. [108] and prazosin at 0.5 to 1 mg/kg i.p. [109]. A concentric microdialysis probe placed directly into the center of the transplanted organoid perfused at a rate of less than 3 microliter/minute could obtain serial samples of the concentration of drugs in the CNS interstitial space. At the same time, plasma concentrations could be determined by venous blood sampling from the central line inserted into the jugular vein.
An anaphylactic reaction after simultaneous injection of hyaluronic acid fillers and human collagen
Published in Journal of Cosmetic and Laser Therapy, 2022
Kiyoko Kato, Eiko Inoue
The patient received two doses of the Pfizer COVID-19 vaccine at 3-week intervals starting around 2.5 months after the initial procedure. Swelling of the lower eyelid flared up temporarily 2 weeks later but resolved in 3 days with oral epinastine hydrochloride 10 mg/day.
Related Knowledge Centers
- Allergic Conjunctivitis
- Mast Cell Stabilizer
- Antihistamine
- Eye Drop
- Binding Selectivity
- Blood–Brain Barrier