Naphazoline hydrochloride

246.74

246.092

3716843

208-989-2

MZ1131787D

757110|35711

DTXSID7045788

C47632

WHITE CRYSTALLINE POWDER

29339900

24.4

2.95040

White Crystalline Powder

1.15 g/cm3

255-260 °C

440.5°C at 760 mmHg

220.2ºC

H2O: 170 g/L (20 ºC)

Naphazoline hydrochloride ophthalmic solutions should be protected from light and should be stored in tight, light-resistant containers. The drug is degraded in the presence of aluminum and, therefore, should not be stored in aluminum containers. ... Fixed combinations containing naphazoline hydrochloride and antazoline phosphate should be stored at temperatures less than 25 deg C.

LD50 s.c. in rats: 385 mg/kg (Gylfe)

ODORLESS

Bitter

A 1% aqueous solution has a pH of about 6.2

pKa = 10.35 (25 °C); pKa = 10.13 (35 °C); pKa = 9.92 (45 °C)

148.5 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

DECOMP @ 253-258 °C

III

6.1

UN 2811 6.1/PG 2

3

25-23/24/25-20/21/22

45-36/37/39-24/25

NJ4375000

T,Xn

NAPHAZOLINE HYDROCHLORIDE WAS STABLE FOR 2 MO @ 5 & 15 DEG C.

P264, P270, P301+P310, P301+P312, P321, P330, P405, P501

H300

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Nasal decongestant active ingredients. The active ingredient of the product consists of any of the following when used within the dosage limits and in the dosage forms established for each ingredient: ... Topical nasal decongestants: naphazoline hydrochloride.|Ophthalmic vasoconstrictors. The active ingredient of the product consists of one of the following, within the established concentration for each ingredient: ... Naphazoline hydrochloride, 0.01 to 0.03 percent.|The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription and over-the-counter drug products, incl naphazoline hydrochloride, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act.

|Danger|H300 (87.76%): Fatal if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|Aggregated GHS information provided by 49 companies from 6 notifications to the ECHA C&L Inventory.

/GUIDE 154: SUBSTANCES - TOXIC AND/OR CORROSIVE (NON-COMBUSTIBLE)/ Health: TOXIC; inhalation, ingestion, or skin contact with material may cause severe injury or death. Contact with molten substance may cause severe burns to skin and eyes. Avoid any skin contact. Effects of contact or inhalation may be delayed. Fire may produce irritating, corrosive and/or toxic gases. Runoff from fire control or dilution water may be corrosive and/or toxic and cause pollution. /Poisonous solid, organic, NOS; Toxic solid, organic, NOS (Naphazoline hydrochloride)/|/GUIDE 154: SUBSTANCES - TOXIC AND/OR CORROSIVE (NON-COMBUSTIBLE)/ Fire or Explosion: Non-combustible, substance itself does not burn but may decompose upon heating to produce corrosive and/or toxic fumes. Some are oxidizers and may ignite combustibles (wood, paper, oil, clothing, etc.). Contact with metals may evolve flammable hydrogen gas. Containers may explode when heated. /Poisonous solid, organic, NOS; Toxic solid, organic, NOS (Naphazoline hydrochloride)/|/GUIDE 154: SUBSTANCES - TOXIC AND/OR CORROSIVE (NON-COMBUSTIBLE)/ Public Safety: CALL Emergency Response Telephone Number ... . As an immediate precautionary measure, isolate spill or leak area in all directions for at least 50 meters (150 feet) for liquids and at least 25 meters (75 feet) for solids. Keep unauthorized personnel away. Stay upwind. Keep out of low areas. Ventilate enclosed areas. /Poisonous solid, organic, NOS; Toxic solid, organic, NOS (Naphazoline hydrochloride)/|/GUIDE 154: SUBSTANCES - TOXIC AND/OR CORROSIVE (NON-COMBUSTIBLE)/ Protective Clothing: Wear positive pressure self-contained breathing apparatus (SCBA). Wear chemical protective clothing that is specifically recommended by the manufacturer. It may provide little or no thermal protection. Structural firefighters' protective clothing provides limited protection in fire situations ONLY; it is not effective in spill situations where direct contact with the substance is possible. /Poisonous solid, organic, NOS; Toxic solid, organic, NOS (Naphazoline hydrochloride)/|For more DOT Emergency Guidelines (Complete) data for NAPHAZOLINE HYDROCHLORIDE (8 total), please visit the HSDB record page.

Patients being treated with monoamine oxidase (MAO) inhibitors may experience a severe hypertensive reaction if administered with a sympathomimetic drug. Although this reaction has not specifically been reported with naphazoline, the possibility of such an interaction should be considered.|Concurrent use of maprotiline or tricyclic antidepressants with naphazoline hydrochloride may potentiate the pressor effects of naphazoline.|PENTOBARBITONE APPEARS TO ENHANCE HYPOTENSIVE ACTION OF ALPHA-SYMPATHOMIMETIC DRUGS, INCL NAPHAZOLINE HYDROCHLORIDE.

LD50 Rat sc 385 mg/kg

Patients with glaucoma should be advised not to use naphazoline hydrochloride ophthalmic solutions except under the advice and supervision of a physician. Ophthalmic solutions of the drug should not be used in patients with angle-closure glaucoma.|One manufacturer states that 0.1% naphazoline hydrochloride ophthalmic solution is contraindicated in infants and children, since CNS depression possibly progressing to coma and hypothermia may occur in children, especially infants.|Naphazoline hydrochloride ophthalmic solution should be used with caution in patients with hypertension, cardiovascular abnormalities, diabetes mellitus, hyperthyroidism, ... .

Adrenergic alpha-Agonists; Nasal Decongestants|Naphazoline is applied topically to the conjunctiva to temporarily relieve congestion, itching, and minor irritation. Ocular decongestants are ineffective in the treatment of delayed hypersensitivity reactions such as contact dermatoconjunctivitis. The vasoconstrictor effects of naphazoline may be used during some ocular diagnostic procedures, but some clinicians prefer phenylephrine to naphazoline for this use.|Ophthalmic solutions containing naphazoline in combination with antihistamines such as antazoline phosphate or pheniramine maleate and/or astringents such as zinc sulfate are commercially available. In the concentrations usually employed, zinc sulfate is a relatively ineffective antiseptic and may promote vasodilation.|Adrenergic (vasoconstrictor); decongestant.|Naphazoline hydrochloride (0.1%), an imidazole derivative with preferential alpha-2 activity, /was instilled/ in 17 eyes of 12 patients with myopathic ptosis due to involvement of the levator palpebrae superioris, in the attempt to selectively stimulate Muller's smooth muscle. Naphazoline significantly widened the palpebral fissure with little change in pupillary diameter and no significant change in ocular pressure, visual acuity and near point determination. However, a reduction of the effect, probably due to tachyphylaxis, was noticed when using naphazoline regularly several times a day for few weeks. In conclusion naphazoline has powerful cosmetical and functional effects in mild to moderate myopathic ptosis above all if taken occasionally.

Ophthalmic use of naphazoline may occasionally cause systemic sympathomimetic effects such as headache, hypertension, cardiac irregularities, nervousness, nausea, dizziness, weakness, and sweating.|Use of naphazoline in the eye may cause blurred vision, mild transient stinging and/or irritation, mydriasis, and increased or decreased intraocular pressure. Conjunctival application of naphazoline, especially when high concentrations are used in geriatric patients, may liberate pigment granules, presumably from the iris. Rebound congestion, characterized by reactive hyperemia frequently occurs with prolonged use and may result in overuse of the drug. Prolonged use of the drug should be avoided for these reasons.|The incidence of serious adverse effects is low in patients receiving therapeutic dosages of ophthalmic solutions of naphazoline hydrochloride. When naphazoline hydrochloride is used in combination preparations, the cautions applicable to each ingredient in the formulation must be observed. Excessive dosage and/or prolonged or too frequent use may irritate the conjunctiva and, especially in children, cause adverse systemic effects.|Naphazoline hydrochloride ophthalmic solution should be used with caution in patients with hypertension, cardiovascular abnormalities, diabetes mellitus, hyperthyroidism, infection, or injury.|For more Drug Warnings (Complete) data for NAPHAZOLINE HYDROCHLORIDE (14 total), please visit the HSDB record page.

Drugs designed to treat inflammation of the nasal passages, generally the result of an infection (more often than not the common cold) or an allergy related condition, e.g., hay fever. The inflammation involves swelling of the mucous membrane that lines the nasal passages and results in inordinate mucus production. The primary class of nasal decongestants are vasoconstrictor agents. (From PharmAssist, The Family Guide to Health and Medicine, 1993) (See all compounds classified as Nasal Decongestants.)|Drugs that selectively bind to and activate alpha adrenergic receptors. (See all compounds classified as Adrenergic alpha-Agonists.)

Following topical application of naphazoline hydrochloride solutions to the conjunctiva, local vasoconstriction usually occurs within 10 minutes and may persist for 2-6 hours. Occasionally, enough naphazoline may be absorbed to produce systemic effects. Information on the distribution and elimination of the drug in humans is not available

Naphazoline constricts the vascular system of the conjunctiva. It is presumed that this effect is due to direct stimulation action of the drug upon the alpha-adrenergic receptors in the arterioles of the conjunctiva, resulting in decreased conjunctival congestion.|The mechanism of action of naphazoline has not been conclusively determined. Most pharmacologists believe that the drug directly stimulates alpha-adrenergic receptors of the sympathetic nervous system and exerts little or no effect on beta-adrenergic receptors. Following topical application of naphazoline to the conjunctiva, small arterioles are constricted and conjunctival congestion is temporarily relieved, but reactive hyperemia may occur. The drug also may produce mydriasis when applied to the conjunctiva, but this effect is usually minimal with the concentrations used as ocular decongestants.

/VET:/ Decontamination may not be practical due to the rapid absorption and onset of clinical signs. Heart rate and rhythm and blood pressure should be assessed, and an ECG obtained if needed. IV fluids should be given, along with atropine at 0.02 mg/kg, IV, if bradycardia is present. Diazepam (0.25-0.5 mg/kg, IV) can be given if CNS signs (eg, apprehension, shaking) are present. Serum electrolytes (ie, potassium, sodium, chloride) should be assessed and corrected as needed. Yohimbine, which is a specific a2-adrenergic antagonist, can also be used at 0.1 mg/kg, IV, and repeated in 2-3 hr if needed. /Imidazoline decongestants/|No specific antidote is available but a symptomatic drug therapy with intravenous administration of phentolamine, an alpha-adrenoceptor antagonist acts against the vasoconstrictive side effects. Because of the serious side effects and the narrow therapeutic to toxic window of naphazoline a strict observance of guidelines and contradictions, such as maximum dose, is necessary.

/SIGNS AND SYMPTOMS/ Overdosage of the drug may produce drowsiness, decreased body temperature, bradycardia, shock-like hypotension, and coma.|/SIGNS AND SYMPTOMS/ Excessive dosage of topically applied naphazoline hydrochloride may cause marked sedation in children, and, if severe, symptomatic and supportive therapy should be initiated. One manufacturer states that 0.1% naphazoline hydrochloride ophthalmic solution is contraindicated in infants and children, since CNS depression possibly progressing to coma and hypothermia may occur in children, especially infants.|/SIGNS AND SYMPTOMS/ Naphazoline, a sympathomimetic and an imidazoline derivative, is used as 0.05-0.1% solution for local decongestion of the nasal and ocular mucosa. In excessive dosage, or if ingested by accident, may cause depression of the central nervous system (disturbances of consciousness progressing to coma), hypothermia, bradycardia and sweating. These naphazoline effects are particularly strongly pronounced in children. Anglo-Saxon pharmacotherapy excludes the application of naphazoline nasal drops in children younger than six years, whereas the Croatian pharmacotherapeutic literature (and practice) allows its use even in infancy. At the Kantrida Pediatric Clinic, Clinical Hospital Center in Rijeka, 11 children with signs of intoxication with naphazoline nasal drops were hospitalized from 1990 to 1992. The symptoms pertaining to the central nervous system i.e. disturbances of consciousness in the form of somnolence were clearly marked in all children. Some children developed skin pallor, bradycardia, bradypnoea and hypothermia. Resolution occurred within 24 hours and the findings returned to normal values. Clinical picture followed by rapid resolution and normal findings, with a personal history of drug taking, is a safe indication for diagnosis. There are several reasons to account for intoxication (drops difficult to use with children, containers inadequate for proper dosage), but the major factor is the age of the patient--all hospitalized children were younger than six years.|/SIGNS AND SYMPTOMS/ It is reported that many accidental poisonings in Japan are the result of ingestion of dermatologic preparations containing naphazoline hydrochloride; symptoms include somnolence, elevation of blood pressure, and bradycardia.|For more Human Toxicity Excerpts (Complete) data for NAPHAZOLINE HYDROCHLORIDE (11 total), please visit the HSDB record page.

Afazol Grin

Ophthalmic: Solution: 0.012% All Clear ( with benzalkonium chloride), (Bausch & Lomb), Clear Eyes ( with benzalkonium chloride and glycerin 0.2%), (Prestige Brands), Naphcon ( with benzalkonium chloride), (Alcon); 0.03% All Clear AR ( with benzalkonium chloride), (Bausch & Lomb); 0.1% AK-Con ( with benzalkonium chloride), (Akorn), Albalon ( with benzalkonium chloride), (Allergan), Naphazoline Hydrochloride Ophthalmic Solution, (Bausch & Lomb).|Ophthalmic: Solution: 0.012% with Zinc Sulfate 0.25% Clear Eyes ACR ( with benzalkonium chloride and glycerin 0.2%), (Prestige Brands); 0.025% with Pheniramine Maleate 0.3% Naphcon-A (with benzalkonium chloride), (Alcon) Visine A , (Pfizer); 0.027% with Pheniramine Maleate 0.315% Opcon A, (Bausch & Lomb); 0.05% with Antazoline Phosphate 0.5% Vasocon-A ( with benzalkonium chloride), (Novartis).|Trade names: Ak-Con (Akorn); Albalon (Allergan); Allerest Eye Drops (Pharmacraft); Allergy Drops (Bausch & Lomb); Clear Eyes (Ross); Clera (Person and Covey); Comfort Eye Drops, Degest 2 (Barnes-Hind); Imidazyl (Allergan); Naphcon (Alcon); I-Naphline (Americal); Opcon (Bausch & Lomb); Optazine (Lederle); Otrivin, Privin, Privina, Privine (Ciba); Vasocon Regular (IOLAB).

COLORIMETRIC DETERMINATION OF NAPHAZOLINE IN SOME PHARMACEUTICAL PREPARATIONS. MAX ABSORBANCE @ 550 NM.|THIN-LAYER CHROMATOGRAPHY. SUNSHINE, I, WW FIKE, & H LANDESMAN, J FORENSIC SCI 11, 428 (1966); GOENECHEA, S, DUNNSCHICHTCHROMATOGRAPHISCHER NACHWEIS VON VIER THERAPEUTISCH WICHTIGEN IMIDAZOLINDERIVATEN, J CHROMATOGR 36, 375 (1968).|Analyte: naphazoline hydrochloride; matrix: chemical identification; procedure: infrared absorption spectrophotometry with comparison to standards|Analyte: naphazoline hydrochloride; matrix: chemical identification; procedure: ultraviolet absorption spectrophotometry with comparison to standards|For more Analytic Laboratory Methods (Complete) data for NAPHAZOLINE HYDROCHLORIDE (18 total), please visit the HSDB record page.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients