Estivin Ii
Estivin Ii Uses, Dosage, Side Effects, Food Interaction and all others data.
Estivin Ii is a rapid acting imidazoline sympathomimetic vasoconstrictor of ocular or nasal artierioles. It acts to decrease congestion and is found in many over the counter (OTC) eye drops and nasal preparations.
Estivin Ii was first developed in 1942 as a nasal formulation for congestion.
Estivin Ii is a sympathomimetic alpha adrenergic agonist that acts to vasoconstrict nasal or ocular arterioles, resulting in reduced congestion at the site of administration.
| Trade Name | Estivin Ii |
| Availability | Rx and/or OTC |
| Generic | Naphazoline |
| Naphazoline Other Names | Nafazolin, Nafazolina, Naphazoline |
| Related Drugs | phenylephrine ophthalmic, brimonidine ophthalmic, oxymetazoline ophthalmic, fluorometholone ophthalmic, tetrahydrozoline ophthalmic |
| Weight | 0.012%, 0.012%, 0.012%glycerin, 0.1% |
| Type | Ophthalmic gel forming solution, ophthalmic solution |
| Formula | C14H14N2 |
| Weight | Average: 210.2744 Monoisotopic: 210.115698458 |
| Protein binding | Protein binding data for naphazoline is unavailable. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Estivin Ii is a sympathomimetic vasoconstrictor used for the symptomatic relief of redness and itching of the eye, and nasal congestion.
Estivin Ii is indicated for use as OTC eyedrops for ocular vasoconstriction or as a nasal preparation for nasal congestion.
Estivin Ii is also used to associated treatment for these conditions: Bacterial Conjunctivitis, Blepharoconjunctivitis, Conjunctivitis, Conjunctivitis allergic, Dacryocystitis, Dacryostenosis, Dermatitis, Eczematous of the Eyelid, Eye Pain, Eye redness, Iritis, Lacrimation, Nasal Allergies, Nasal Congestion, Noninfective conjunctivitis, Otitis Media (OM), Photophobia, Foreign body sensation in eye, Ocular bacterial infections, Ocular vasoconstriction
How Estivin Ii works
Estivin Ii is a vasoconstrictor that functions by stimulating alpha adrenergic receptors in arterioles leading to decreased congestion at the site of administration.
Estivin Ii causes the release of norepinephrine in sympathetic nerves. Norepinephrine binds to alpha adrenergic receptors and causes vasoconstriction. Estivin Ii is also a mild beta adrenergic receptor agonist, which can cause rebound vasodilation after the alpha adrenergic stimulation has ended. Estivin Ii's release of norepinephrine also triggers a negative feedback loop which decreases production of norepinephrine, which can lead to rhinitis medicamentosa after long term use when naphazoline is stopped.
Toxicity
In high doses or when ingested, naphazoline can lead to central nervous system depression (which can progress to coma and death), hypothermia, bradycardia, and death. This effect is especially pronounced in children under 6 years.
Long term use of naphazoline can lead to rhinitis medicamentosa once naphazoline is stopped. This condition is a result of norepinephrine release by naphazoline triggering a negative feedback loop.
Safety and effectiveness in children under 12 has not been established. Studies in elderly patients have yet to be performed. Risk in pregnancy, breast feeding, and on overall fertility have not been established, though pregnant and breast feeding patients should consider the risk and benefit before starting naphazoline treatment.
Food Interaction
No interactions found.Estivin Ii Disease Interaction
Volume of Distribution
Distribution data for naphazoline are scarce but imidazoline compounds are distributed throughout the body, and can cross the blood-brain barrier.
Elimination Route
Absorption data for naphazoline are scarce but imidazoline compounds in general are weakly basic and lipophilic, with high bioavailability from the gastrointestinal tract.
Half Life
Half life has not been determined but effects last for 4 to 8 hours. Other imidazoline compounds have half lives varying from 2 to 12 hours.
Clearance
Clearance data for naphazoline is unavailable.
Elimination Route
Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urine. Urinary excretion is higher with more acidic urine.
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