Naphazoline
Chemical compound
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Trade names | Clear Eyes, Cleari, Naphcon-A , Rohto |
AHFS / Drugs.com | Monograph |
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Ophthalmic drug administration , nasal administration |
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ECHA InfoCard | 100.011.492 |
Chemical and physical data | |
Formula | C 14 H 14 N 2 |
Molar mass | 210.274 g·mol −1 |
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Naphazoline is a medicine used as a decongestant , and a vasoconstrictor added to eye drops to relieve red eye . It has a rapid action in reducing swelling when applied to mucous membranes . It is a sympathomimetic agent with marked alpha adrenergic activity that acts on alpha-receptors in the arterioles of the conjunctiva to produce constriction, resulting in decreased congestion.
It was patented in 1934 and came into medical use in 1942. [1]
Medical uses
Nasal administration
Nasal decongestant . [2]
Ophthalmic drug administration
Eye drops (brand names Clear Eyes, and Cleari) narrowing swollen blood vessels ( ophthalmic arteries , and ophthalmic veins ) to relieve red eye . [2]
Temporary red eye can safely be treated when the cause of the redness is established (eg cannabis induces corneal vasodilation [3] )[Insufficient Bibliography]. However, continuous use is not recommended without knowing an underlying condition.
Side effects
A few warnings and contraindications that apply to all naphazoline-containing substances intended for medicinal use are:
- Hypersensitivity to naphazoline
- Use in infants and children can result in central nervous system depression, leading to coma and marked reduction in body temperature
- Should be used with caution in patients with severe cardiovascular disease including cardiac arrhythmia and in patients with diabetes , especially those with a tendency toward diabetic ketoacidosis
- A possible association with stroke has been suggested. [4]
Nasal administration
- Extended use may cause rhinitis medicamentosa , a condition of rebound nasal congestion .
Ophthalmic drug administration
- Stinging
- Discomfort
- Irritation
- Increased red eyes
- Blurred vision
- Mydriasis
- Punctate keratitis
- Lacrimation (tears)
- Increased intraocular pressure
Contraindications
- Patients taking MAO inhibitors can experience a severe hypertensive crisis if given a sympathomimetic drug such as naphazoline HCl
- Drug interactions can occur with anaesthetics that sensitize the myocardium to sympathomimetics (e.g. cyclopropane or halothane cautiously)
- Exercise caution when applying prior to use of phenylephrine .
Pharmacology
Naphazoline is a mixed α 1 - and α 2 -adrenergic receptor agonist . [2]
Chemistry
The non-hydrochloride form of Naphazoline has the molecular formula C 14 H 14 N 2 and a molar mass of 210.28 g/mol. The HCl salt form has a molar mass of 246.73 g/mol.
Society and culture
It is an active ingredient in several over-the-counter eye drop formulations including Clear Eyes, Rohto , Eucool, and Naphcon-A . [7]
Illicit use
The nasal or ophthalmic form of naphazoline has been abused by heroine or cocaine drug addicts . [8] [9] It's used as CNS stimulant and vasoconstrictor to enhance primary drug effects. [9]
References
- ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery . John Wiley & Sons. p. 552. ISBN 9783527607495 .
- 1 2 3 Hosten LO, Snyder C (2020). "Over-the-Counter Ocular Decongestants in the United States - Mechanisms of Action and Clinical Utility for Management of Ocular Redness" . Clinical Optometry . 12 : 95–105. doi : 10.2147/OPTO.S259398 . PMC 7399465 . PMID 32801982 .
- ↑ Yazulla S (September 2008). "Endocannabinoids in the retina: from marijuana to neuroprotection" . Progress in Retinal and Eye Research . 27 (5): 501–526. doi : 10.1016/j.preteyeres.2008.07.002 . PMC 2584875 . PMID 18725316 .
- ↑ Zavala JA, Pereira ER, Zétola VH, Teive HA, Nóvak EM, Werneck LC (September 2004). "Hemorrhagic stroke after naphazoline exposition: case report" . Arquivos de Neuro-Psiquiatria . 62 (3B): 889–891. doi : 10.1590/S0004-282X2004000500030 . PMID 15476091 .
- ↑ "Naphazoline - FDA prescribing information, side effects and uses" . Drugs.com .
- ↑ "naphazoline ophthalmic (eye): Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD" . www.webmd.com .
- ↑ Green SM (2008). "Ophthalmology: Naphazoline". Tarascon Pocket Pharmacopoeia 2009 . Jones and Bartlett. ISBN 978-0-7637-6572-9 .
- ↑ van Montfrans GA, van Steenwijk RP, Vyth A, Borst C (1981). "Intravenous naphazoline intoxication". Acta Medica Scandinavica . 209 (5): 429–430. doi : 10.1111/j.0954-6820.1981.tb11622.x . PMID 7246278 .
- 1 2 "Naphazoline abuse" . Reactions Weekly . 1815 (1): 251. 2020-08-01. doi : 10.1007/s40278-020-81577-1 . ISSN 1179-2051 . S2CID 195174995 .
Decongestants
and other nasal preparations (
R01
)
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Systemic use:
Sympathomimetics |
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