Naphazoline

Naphazoline

Drug Nomenclature

Date of monograph revision: 30-Sep-1997; 25-Jun-1998; 12-Apr-2000; 01-Nov-2001; 01-Jul-2004; 05-Jul-2006; (last modified: 24-Jul-2006)
Synonyms: Nafatsoliini; Nafazolin; Nafazolina; Naphazolinum
BAN: Naphazoline
INN: Naphazoline [rINN (en)]
INN: Nafazolina [rINN (es)]
INN: Naphazoline [rINN (fr)]
INN: Naphazolinum [rINN (la)]
INN: Нафазолин [rINN (ru)]
Chemical name: 2-(1-Naphthylmethyl)-2-imidazoline
Molecular formula: C14H14N2 =210.3
CAS: 835-31-4
ATC code: R01AA08; R01AB02; S01GA01
Read code: y03zK
Chemical Structure of Naphazoline

Chemical Structure of Naphazoline

Naphazoline Hydrochloride

Drug Nomenclature

Date of monograph revision: 30-Sep-1997; 25-Jun-1998; 12-Apr-2000; 01-Nov-2001; 01-Jul-2004; 05-Jul-2006; (last modified: 24-Jul-2006)
Synonyms: Nafatsoliinihydrokloridi; Nafazolin-hidroklorid; Nafazolin-hydrochlorid; Nafazolina, hidrocloruro de; Nafazolinhydroklorid; Nafazolino hidrochloridas; Naphazolini Hydrochloridum
BAN: Naphazoline Hydrochloride [BANM]
INN: Naphazoline Hydrochloride [rINNM (en)]
INN: Hidrocloruro de nafazolina [rINNM (es)]
INN: Naphazoline, Chlorhydrate de [rINNM (fr)]
INN: Naphazolini Hydrochloridum [rINNM (la)]
INN: Нафазолина Гидрохлорид [rINNM (ru)]
Molecular formula: C14H14N2,HCl =246.7
CAS: 550-99-2
ATC code: R01AA08; R01AB02; S01GA01
Read code: y03mz
Pharmacopoeias:

In Chin., Eur. (see Go to European Pharmacopoeia Convention Signatories), Jpn, and US.

Ph. Eur. 5.5 (Naphazoline Hydrochloride). A white or almost white, crystalline powder. Freely soluble in water; soluble in alcohol. Protect from light.

USP 29 (Naphazoline Hydrochloride). A white, odourless, crystalline powder. Freely soluble in water and in alcohol; very slightly soluble in chloroform; practically insoluble in ether. pH of a 1% solution in water is between 5.0 and 6.6. Store in airtight containers. Protect from light.

Naphazoline Nitrate

Drug Nomenclature

Date of monograph revision: 30-Sep-1997; 25-Jun-1998; 12-Apr-2000; 01-Nov-2001; 01-Jul-2004; 05-Jul-2006; (last modified: 24-Jul-2006)
Synonyms: Nafatsoliininitraatti; Nafazolin-nitrát; Nafazolina, nitrato de; Nafazolinnitrat; Nafazolino nitratas; Naphazolini Nitras; Naphazolinium Nitricum; Naphthizinum
BAN: Naphazoline Nitrate [BANM]
INN: Naphazoline Nitrate [rINNM (en)]
INN: Nitrato de nafazolina [rINNM (es)]
INN: Naphazoline, Nitrate de [rINNM (fr)]
INN: Naphazolini Nitras [rINNM (la)]
INN: Нафазолина Нитрат [rINNM (ru)]
Molecular formula: C14H14N2,HNO3 =273.3
CAS: 5144-52-5
ATC code: R01AA08; R01AB02; S01GA01
Pharmacopoeias:

In Eur. (see Go to European Pharmacopoeia Convention Signatories), Jpn, Pol., and Viet.

Ph. Eur. 5.5 (Naphazoline Nitrate). A white or almost white, crystalline powder. Sparingly soluble in water; soluble in alcohol. A 1% solution in water has a pH of 5.0 to 6.5. Protect from light.

Adverse Effects, Treatment, and Precautions

As for Sympathomimetics, Go to Adverse Effects, Go to Treatment of Adverse Effects, and Go to Precautions; naphazoline has mainly alpha-agonist effects. After local use, transient irritation may occur. Rebound congestion may occur after frequent or prolonged use. Systemic effects, including nausea, headache, and dizziness have occurred after topical use. Overdosage or accidental dosage by mouth may cause CNS depression with marked reduction of body temperature and bradycardia, sweating, drowsiness, and coma, particularly in children; it should be used with great caution, if at all, in infants and young children. Use of naphazoline in the eye may liberate pigment granules from the iris, especially when given in high doses to elderly patients. Hypertension may be followed by rebound hypotension. Treatment of adverse effects is symptomatic.

Effects on the eyes.

For mention of conjunctivitis induced by ophthalmic decongestant preparations containing naphazoline, see under Phenylephrine, Go to Effects on the eyes..

Intraoperative use.

A report1 of 2 cases of toxicity associated with intraoperative use of a naphazoline-soaked sponge to control excessive bleeding after adenoidectomy. Both patients experienced hypertension and reflex bradycardia, which evolved in one case into marked hypotension. There was evidence of CNS depression with a reduced respiration rate and prolonged recovery from anaesthesia.

  1. 1. Wenzel S, et al. Course and therapy of intoxication with imidazoline derivate naphazoline. Int J Pediatr Otorhinolaryngol 2004; 68: 979–83. PubMed

Interactions

Since naphazoline is absorbed through the nasal mucosa interactions may follow topical application. The BNF considers that all sympathomimetic nasal decongestants may cause a hypertensive crisis if used during treatment with an MAOI. For the interactions of sympathomimetics in general, see Go to Interactions.

Pharmacokinetics

Systemic absorption has been reported following topical application of solutions of naphazoline. It is not used systemically, but it is readily absorbed from the gastrointestinal tract.

Uses and Administration

Naphazoline is a sympathomimetic (Go to Actions and Uses) with marked alpha-adrenergic activity. It is a vasoconstrictor with a rapid and prolonged action in reducing swelling and congestion when applied to mucous membranes.

Naphazoline and its salts are used for the symptomatic relief of nasal congestion (Go to Nasal congestion). Solutions containing 0.05 to 0.1% of the hydrochloride or the nitrate may be applied topically as nasal drops or a spray usually up to once every 6 hours. Children aged 7 years and over have used a preparation containing 0.05%.

Solutions containing up to 0.1% of naphazoline hydrochloride have been instilled into the eye as a conjunctival decongestant (see Conjunctivitis, Go to Conjunctivitis).

Naphazoline has been used as a vasoconstrictor with local anaesthetics.

Naphazoline acetate has also been used in nasal preparations.

Preparations

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Argentina: Bactio Rhin; Bano Ocular Agrand; Dazolin; Disel; Gotabiotic D; Gotinal; Mirasan; Mirus-S; Nasalex; Privina; Rhinal; Australia: Albalon; Clear Eyes¤; Naphcon; Optazine; Austria: Aconex; Coldan; Isoftal; Mertan; Privin; Rhinon; Rhinoperd; Belgium: Albalon¤; Deltarhinol-Mono; Naphcon¤; Neusinol; Priciasol; Vasocedine; Brazil: Clarivit; Claroft; Multisoro; Narial; Naridex¤; Narix; Nazicol; Neosoro; Privina; Rino Resfenol; Rinoklin¤; Rinos-A; Rinox Adulto¤; Canada: Ak-Con; Albalon; Allergy Drops; Clear Eyes; Degest 2¤; Diopticon; Naphcon Forte; Opcon¤; Privine¤; Red Away¤; Rhino-Mex-N¤; RO-Naphz¤; Vasocon; Chile: Albasol¤; Clarimir; Red Off; Vi-Claro¤; Czech Republic: Proculin; Sanorin; Germany: Idril N sine; Piniol Nasenspray¤; Piniol¤; Privin; Proculin; Rhinex¤; Tele-Stulln; Vistalbalon¤; Greece: Coldan; Naphcon; Hong Kong: Albalon; All Clear; Hungary: Naphcon; Proculin; India: Clearine; Ocustress; Ireland: Albalon¤; Israel: Naphasal; Naphcon Forte; Italy: Alfa¤; Collirio Alfa; Desamin Same; Imidazyl; Imizol¤; Iridina Due; Lucisan¤; Naftazolina; Pupilla; Ran¤; Rinazina; Rino Naftazolina; Rinoftal¤; Transpulmina Rino¤; Video-Mill; Virginiana Gocce Verdi; Malaysia: Albalon; Mexico: Afazol; Alphadinal; Celunaf; Gotinal; Nazil; Oftazil¤; Netherlands: Albalon; New Zealand: Albalon¤; Clear Eyes; Naphcon; Portugal: Murine¤; Russia: Naphthyzin (Нафтизина); Sanorin (Санорин); South Africa: Albalon¤; Murine Clear Eyes¤; Safyr Bleu; Singapore: Antistin-Privin; Spain: Alfa; Euboral; Miraclar; Privina¤; Vasoconstrictor Pensa; Sweden: Rimidol; Switzerland: Albalon; Minha¤; Thailand: Albalon; Naphcon; United Kingdom: Murine; United States: Ak-Con; Albalon; All Clear; Allerest; Allergy Drops; Allersol¤; Clear Eyes Plus Redness Relief; Clear Eyes; Comfort Eye Drops; Degest; Nafazair; Napha Forte; Naphcon; Privine; Vasocon; Venezuela: Clarasol; Clearize; Fanasal; Fazonil; Nafin; Naphcon; Niazol; Ninazo;

Multi-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Argentina: Alercortil¤; Alvo Nasal; Antibiocort¤; Bactio Rhin Prednisolona; Biotaer Nasal; Dexafurazon; Dexalergin; Disel Hidrocortisona; Drynisan; Factioneye; Fadanasal; Gramicortil¤; Hyalcrom; Mira Klonal; Mirus; Nasojol¤; Nasomicina; Neo-Currino; Neodexa Plus; Neoefodil; Neosona; Nexadron Compuesto; Panoptic; Provacsin Nasal; Refenax Colirio; Refenax Gotas Nasales; Rinofilax AG M; Rinogel; Suavithiol; Vistacloran; Australia: Albalon-A; Antistine-Privine; In A Wink; Naphcon-A; Optazine A¤; Optrex; Visine Allergy with Antihistamine¤; Austria: Coldistan; Coldophthal; Histophtal¤; Luuf-Nasenspray; Ophtaguttal; Rectosan¤; Rhinodrin; Rhinon; Rhinoperd comp; Belgium: Deltarhinol¤; Diphenhydramine Constrictor; Naphcon-A¤; Neofenox; Sofraline; Sofrasolone; Zincfrin Antihistaminicum; Brazil: Adnax¤; Albassol¤; Alergotox Nasal; Borato de Sodio¤; Claril; Colirio Blumen¤; Colirio Legrand; Colirio Moura Brasil¤; Colirio Teuto; Colirio Vima¤; Colyrazul¤; Conidrin; Dexa-Vastrictol¤; Fluo-Vaso; Hemodotti; Hermodotti¤; Hidrocin; Inhadrina; Lerin; Maxibell; Mentodrin; Naricin¤; Naridrin; Nariflux; Naso Instil¤; Naso-Josp; Nasopan¤; Nazobel; Nazobio; Nazotiran¤; Neo Quimica Colirio; Nitrileno; Nitronasal¤; Novo Rino; Oftazul¤; Penetran¤; Rhinodex¤; Rhinosept; Rinatrol¤; Rinisone; Rinocron¤; Rinosite; Rinozin¤; Sinus¤; Sinustrat Vasoconstritor; Solucao Nasal de Nafazolina¤; Sorine Adulto; Stilux; Vastrictol¤; Visiplex; Visolon¤; Visual; Zincolok; Canada: Albalon-A; Antistin-Privin¤; Blue Collyrium¤; Collyre Bleu¤; Cooper AR¤; Diopticon A; Naphcon-A; Onrectal; Opcon-A; Rhino-Mex¤; Vasocon-A; Zincfrin-A; Chile: Albasol A¤; Clarimir F; Dessolets; Miral; Mirus; Naphcon-A; Naphtears; Nico Drops; Novo-Tears; Oculosan; Oftalirio; Red Off Plus; Czech Republic: Sanorin-Analergin; Denmark: Ansal; Antistina-Privin; Sesal; Finland: Antistin-Privin; Zincfrin-A¤; France: Alcolene¤; Collyre Bleu; Derinox; Frazoline¤; Scarlene¤; Soframycine Naphazoline¤; Germany: Alformin¤; Antistin-Privin; Aquapred¤; Bisrenin¤; Boro-Hexamin¤; Borocarpin-N¤; Borocarpin¤; Combiamid¤; Diabenyl-Rhinex¤; Diabenyl¤; duraforte¤; duraultra forte¤; duraultra; Konjunktival Thilo; Lensch¤; Oculosan N; Ophtalmin¤; Ophtomydrol¤; Ophtopur-N¤; Proculens N¤; Prothanon¤; Rhinoguttae Dexamethasoni cum Naphazolino¤; Rhinosovil¤; Salvizol¤; Siozwo¤; Siozwo; Solupen-D¤; Solupen¤; Stipo¤; Zincfrin-A¤; Greece: Neo-Priphen; Oculosan; Septobore; Zabysept; Hong Kong: Frazoline; Konjunktival¤; Naphcon-A; Oculosan¤; Hungary: Coldistan; India: Andre-I-Kul; Andre; Betnesol-N Nasal; Efcorlin; Fenox; Ocurest-AH; Ocurest-Z; Ocurest; Proto-Boric; Israel: Alnase; Antistin-Privin; Diphenazol¤; Nazodin¤; Nodryl; Optryl; Phenyphrine-Azol; Proaf; Italy: Adrenosin Composto¤; Alfaflor; Antisettico Astringente Sedativo; Antistin-Privina; Citroftalmina VC¤; Collirio Alfa Antistaminico; Corizzina; Deltarinolo; Fenox¤; Fotofil; Genalfa; Idroneomicil; Imidazyl Antistaminico; Indaco; Iristamina; Nafcon A; Oftalmil; Oftalzina¤; Pupilla Antistaminico; Rinocidina; Rinofomentil¤; Rinospray¤; Rinovit Nube¤; Vapor Sol¤; Zinc-Imizol; Zincoimidazyl¤; Malaysia: Alergoftal; Naphcon-A; Oculosan; Mexico: Afazol Z; Biofrin; Biotarson O; Istasol; Mirus; Naphacel; Naphtears; Oftalirio¤; Opcon-A; Soltrictor con Lagrifilm; Solutina; Sulvi; Zincfrin-A; Norway: Antistin-Privin¤; New Zealand: Albalon-A¤; Betnesol Aqueous; Clear Eyes ACR¤; Degest 2¤; Naphcon-A; Optrex Red-Eye Relief; Visine Allergy; Portugal: Alergiftalmina; Colircusi Anestesico; Gramixina¤; Naso-Prieulina; Russia: Betadrin (Бетадрин); Sanorin (Санорин); Sanorin-Analergin (Санорин-аналергин); South Africa: Albalon-A; Antistin-Privin; Covomycin; Covosan; ENT; Fenox¤; Nasdro; Oculosan; Universal Nasal Drops; Wink¤; Zincfrin-A; Singapore: Alergoftal¤; Flucur¤; Naphcon-A; Spain: Alergoftal; Ant Sedan¤; Antib Sedante¤; Antibio Sedan¤; Antisep Sedant¤; Antisept Sed¤; Astringen¤; Astringente¤; Bao¤; Centilux; Clo Zinc¤; Cloran Zinc; Coliriocilina Adren Astr; Corilisina¤; Dexa Vasoc¤; Epistaxol; Fluo Vasoc¤; Kanafosal Predni; Kanafosal; Lagrimol¤; Lidrone¤; Nasal Rovi¤; Nebulizador Antihis Pens¤; Oftalmol Dexa¤; Oftalmol Ocular; Ojosbel Azul¤; Ojosbel; Polirino¤; Rinosular¤; Rinovel; Vasocon Ant¤; Vasoconstr¤; Vasoconstricto¤; Zolina; Sweden: Antasten-Privin; Switzerland: Antistin-Privin; Collyre Alpha; Collyre Bleu Laiter; Derinox¤; Gouttes nasales N¤; Napharzol¤; Oculosan; Optazine¤; Spray nasal comp pour adultes; Zincfrin-A¤; Thailand: Levoptin; Naphcon-A; Oculosan; United Kingdom: Eye Dew; Optrex Red Eyes; Vasocon-A¤; United States: 4-Way Fast Acting; Ak-Con-A¤; Antazoline-V; Clear Eyes Seasonal Relief; Estivin¤; Maximum Strength Allergy Drops; Muro's Opcon¤; Nafazair A; Naphazole-A¤; Naphazoline Plus; Naphcon-A; Naphoptic-A; Ocuhist; Opcon-A; VasoClear A; VasoClear; Vasocon-A; Visine-A; Venezuela: Fazolan; Fesanol; Soltin;

Adjuvant to Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

France: Xylocaine; Spain: Anest Compuesto¤; Anestesico;


  • Dr J Neethling  2013-01-30

    I am interested to obtain Naphazoline nitrate and am trying to source a supplier. Any contact details available??? J Neethling reply

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