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Antihistamines, Decongestants, and Expectorants during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Naphazoline, oxymetazoline, and xylometazoline are sympathomimetic agents with decongestant in long-acting nasal sprays (Afrin, Allerest, Dristan, 4-Way). Birth defects were not increased in frequency among more than 250 infants born to women who used oxymetazoline during the first trimester (Aselton et al., 1985; Jick et al., 1981). The Swedish registry reported no increased frequency of birth defects (3.3 percent) among 3521 infants whose were exposed to oxymetazoline during organogenesis (Kallen, 2019). Likewise, the frequency of birth defects was not increased in 432 infants exposed to xylometazoline during embryogenesis (Aselton et al., 1985; Jick et al., 1981). The Swedish registry reported the frequency of birth defects was not increased among 1168 infants born to women who used xylometazoline during the first trimester (Kallen, 2019). An incidental observation is that xylometazoline was significantly protective against congenital anomalies in the analysis. No studies have been published regarding naphazoline monotherapy use during pregnancy. However, the combination antazoline—naphazoline ophthalmologic preparation was used during the first trimester among 3061 infants, and the rate of birth defects was not increased above background (3.0 percent) or compared to controls (3.5 percent) (Thomseth et al., 2019).
Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Naphazoline is an imidazole derivative and a direct-acting sympathomimetic amine with vasoconstrictive properties. Upon ocular administration, it acts on α-adrenergic receptors in the arterioles of the conjunctiva to produce vasoconstriction, resulting in decreased conjunctival congestion and diminished itching, irritation and redness. It has similar effect when applied to the nasal mucosa. Naphazoline is indicated for use as over-the-counter eye drops for ocular vasoconstriction and as a nasal preparation for nasal congestion. In pharmaceutical products, naphazoline is employed as naphazoline hydrochloride (CAS number 550-99-2, EC number 208-989-2, molecular formula C14H15ClN2) (1).
Sympathomimetic Amines: Actions and Uses
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Sympathomimetic amine decongestants should be used with care in hypertensive, diabetic and hyperthyroid subjects and men with prostatic enlargement. They are contraindicated in patients being treated for depression with MAO inhibitors (see Chapter 2). Oral administration is more likely to induce systemic complications but the risks of rebound congestion are reduced. Sympathomimetic amines are often combined with antihistamines and anticholinergics in decongestant formulations and with analgesics in OTC cough and cold remedies. The most popular are phenylpropanolamine, pseudoephedrine and ephedrine as general purpose decongestants, while oxymetazoline and xylometazoline are used for rhinitis. Naphazoline is no longer recommended. Table 4.4 shows those sympathomimetic amines in common use.
Low‐dose brimonidine for relief of ocular redness: integrated analysis of four clinical trials
Published in Clinical and Experimental Optometry, 2019
Stacey L Ackerman, Gail L Torkildsen, Eugene Mclaurin, Jason L Vittitow
Ocular redness, which commonly results from inflammation of the conjunctiva and associated dilation of the conjunctival vessels, has a number of potential aetiologic factors including allergy, infection, dry eye, exposure to environmental irritants, and contact lens wear.2010 Treatment should, whenever possible, be specific to the underlying cause (for example, antihistamines and mast cell stabilisers for allergic conjunctivitis and topical antibiotics for bacterial conjunctivitis).2010 For ocular redness with no apparent underlying pathology, over‐the‐counter ocular vasoconstrictors (decongestants) may provide relief.2010 These agents produce vasoconstriction via agonist activity at α‐adrenergic receptors, but vary in their receptor binding profiles.2018 Phenylephrine and tetrahydrozoline exhibit relatively selective affinity for α1‐adrenergic receptors (selective α1‐receptor agonists) whereas naphazoline and oxymetazoline bind to both α1‐ and α2‐adrenergic receptors (mixed α1/α2‐receptor agonists).
Evaluation of Efficacy and Safety of Brimonidine Tartrate Ophthalmic Solution, 0.025% for Treatment of Ocular Redness
Published in Current Eye Research, 2018
Gail L. Torkildsen, Christine M. Sanfilippo, Heleen H. DeCory, Paul J. Gomes
Ocular redness, or hyperemia, is a common ophthalmic condition typically caused by inflammation of the conjunctiva due to allergy, exposure to environmental irritants, or as a reaction to infectious agents (e.g., bacteria, virus). Preferred treatment depends on the cause of redness.1,2 For instance, current agents used to treat allergic conjunctivitis include antihistamines and mast cell stabilizers. Topical vasoconstrictor agents (i.e. ocular decongestants) are commonly used to treat ocular redness, particularly non-allergic and non-infectious redness caused by minor eye irritations.1,2 Current over-the-counter (OTC) vasoconstrictors are α-adrenergic receptor (α-AR) agonists. These agents induce smooth muscle contraction and differ in their affinity for the α1- and α2- AR subtypes. Phenylephrine and tetrahydrozoline are considered selective α1-AR agonists,3 while naphazoline and oxymetazoline are considered mixed α1/α2- AR agonists.4
Understanding ocular comfort differences between 0.7% olopatadine and 0.3% pheniramine maleate/0.025% naphazoline hydrochloride eye drops
Published in Clinical and Experimental Optometry, 2023
Chris Lievens, Andrew D. Pucker, Gerald McGwin, Amy Logan, Quentin Franklin, Randy Brafford, Catherine Hogan, Laurel R Kelley, Mike Christensen
Fortunately, numerous topical options are available for allergic conjunctivitis relief. When prescribing therapy, considerations should include initial comfort upon instillation as poor topical drop comfort has the potential to negatively impact compliance as patients are unlikely to maintain consistent use of a drop that causes bothersome symptoms. Top current pharmacologic options indicated for allergic conjunctivitis include medications such as olopatadine (antihistamine with mast-cell stabiliser properties) and pheniramine maleate (antihistamine) paired with naphazoline hydrochloride (ocular decongestant). These topical medications provide more immediate relief than systemic medications, in part due to the drop flushing the ocular surface of allergens and by supplementing the tear film to minimise exposure.4 Naphazoline hydrochloride is an alpha adrenergic vasoconstrictor that results in decreased conjunctival hyperaemia.5 When combined with pheniramine maleate, a H1-histamine antagonist, a dual action antihistamine and redness-reliever is constructed.5 Olopatadine is a dual action anti-histamine and mast cell stabiliser with high H1 receptor affinity for improved anti-itch relief and effective reduction in mast cell degranulation.4,6 The prolonged duration of action is due to the subsequent decrease in release of other cellular mediators that upregulate the inflammatory response. While olopatadine may provide immediate relief, the optimal performance is when used consistently prior to allergen exposure.5,7 Although olopatadine at 0.1% and 0.2% concentrations have been in the market for a while, 0.7% olopatadine (Pataday Once Daily Relief Extra Strength; Alcon, Fort Worth, TX, USA) is a relatively new treatment that has been introduced in select markets.