Naphazoline Hydrochloride

Levmetamfetamine/Naphazoline 1565

Metizoline Hydrochloride (BANM, USAN, rINNM) ⊗ Naphazoline Hydrochloride (BANM, rINNM) ⊗ Uses and Administration EX-10-781; Hidrocloruro de metizolina; Métizoline, Chlorhy- Hidrocloruro de nafazolina; Nafatsoliinihydrokloridi; Nafazolin Naphazoline is a sympathomimetic (p.1408) with drate de; Metizolini Hydrochloridum; Metyzoline Hydrochloride; Hidroklorür; Nafazolin-hidroklorid; Nafazolin-hydrochlorid; Na- marked alpha-adrenergic activity. It is a vasoconstric- RMI-10482A. 2-(2-Methylbenzo[b]thienylmethyl)-2-imidazoline fazolinhydroklorid; Nafazolino hidrochloridas; Naphazoline, chlo- tor with a rapid and prolonged action in reducing swell- hydrochloride. rhydrate de; Naphazolini hydrochloridum. ing and congestion when applied to mucous mem- Метизолина Гидрохлорид Нафазолина Гидрохлорид branes. C H N S,HCl = 266.8. 13 14 2 C14H14N2,HCl = 246.7. Naphazoline and its salts are used for the symptomatic CAS — 17692-22-7 (metizoline); 5090-37-9 (metizoline CAS — 550-99-2. hydrochloride). relief of nasal congestion (p.1548). Solutions contain- ATC — R01AA08; R01AB02; S01GA01. ing 0.05 to 0.1% of the hydrochloride or the nitrate ATC — R01AA10. ATC Vet — QR01AA08; QR01AB02; QS01GA01. ATC Vet — QR01AA10. may be applied topically as nasal drops or a spray usu- Pharmacopoeias. In Chin., Eur. (see p.vii), Jpn, and US. ally up to once every 6 hours. Children aged 7 years Ph. Eur. 6.2 (Naphazoline Hydrochloride). A white or almost white, crystalline powder. Freely soluble in water; soluble in al- and over have used a preparation containing 0.05%. S CH3 cohol. Protect from light. Solutions containing up to 0.1% of naphazoline hydro- N USP 31 (Naphazoline Hydrochloride). A white, odourless, crys- chloride have been instilled into the eye as a conjuncti- talline powder. Freely soluble in water and in alcohol; very slightly soluble in chloroform; practically insoluble in ether. pH val decongestant (see Conjunctivitis, p.564). N of a 1% solution in water is between 5.0 and 6.6. Store in airtight H Naphazoline has been used as a vasoconstrictor with containers. Protect from light. local anaesthetics. (metizoline) Naphazoline Nitrate (BANM, rINNM) ⊗ Naphazoline acetate has also been used in nasal preparations. NOTE. The name benazoline has been used as a synonym for meti- Nafatsoliininitraatti; Nafazolin Nitrat; Nafazolinnitrat; Nafazolin- zoline. Care should be taken to distinguish it from benazolin (4- nitrát; Nafazolino nitratas; Nafazoliny azotan; Naphazoline, ni- Preparations chloro-2,3-dihydro-2-oxo-1,3-benzothiazol-3-ylacetic acid, trate de; Naphazolini nitras; Naphazolinium Nitricum; Naph- C9H6ClNO3S = 243.7), which is a herbicide. Also do not confuse thizinum; Nitrato de nafazolina. USP 31: Naphazoline Hydrochloride and Pheniramine Maleate Ophthal- with benzazoline (see Tolazoline, p.1415), which is a vasodilator. mic Solution; Naphazoline Hydrochloride Nasal Solution; Naphazoline Hy- Нафазолина Нитрат Profile drochloride Ophthalmic Solution. Metizoline hydrochloride is a sympathomimetic with effects C14H14N2,HNO3 = 273.3. Proprietary Preparations (details are given in Part 3) similar to those of naphazoline (p.1565) that has been used for its CAS — 5144-52-5. Arg.: Actifedrin Nasal; Bactio Rhin; Bano Ocular Agrand; Dazolin; Disel; vasoconstrictor activity in the treatment of nasal congestion. ATC — R01AA08; R01AB02; S01GA01. Gotabiotic D; Gotinal; Let-Nasal; Mirasan; Mirus-S; Nafazolex; Nasalex; ATC Vet — QR01AA08; QR01AB02; QS01GA01. Privina; Rhinal; Austral.: Albalon; Clear Eyes†; Naphcon; Optazine†; Aus- tria: Aconex; Coldan; Isoftal; Mertan; Privin; Rhinon; Rhinoperd; Belg.: Al- Pharmacopoeias. In Eur. (see p.vii), Jpn, and Viet. balon†; Deltarhinol-Mono; Naphcon; Neusinol; Priciasol; Vasocedine; Ph. Eur. 6.2 (Naphazoline Nitrate). A white or almost white, Braz.: Clarivit†; Claroft; Multisoro; Narial†; Narix; Nazicol; Neosoro; Privi- Morclofone (rINN) na; Rino Resfenol†; Rinos-A; Canad.: Ak-Con; Albalon; Allergy Drops; crystalline powder. Sparingly soluble in water; soluble in alco- Clear Eyes; Diopticon; Naphcon Forte; Red Away†; Vasocon†; Chile: Al- Dimeclofenone; Morclofona; Morclofonum; Morclophon. 4′- hol. A 1% solution in water has a pH of 5.0 to 6.5. Protect from basol†; Clarimir; Red Off; Vi-Claro†; Cz.: Proculin†; Sanorin; Ger.: Idril N Chloro-3,5-dimethoxy-4-(2-morpholinoethoxy)benzophenone. light. sine†; Piniol Nasenspray†; Privin; Proculin; Rhinex mit Naphazolin; Tele- Stulln; Gr.: Coldan; Naphcon; Hong Kong: Albalon; All Clear; Hung.: Морклофон Naphcon†; Proculin†; India: Clearine; Ocustress; Indon.: Optrine; Israel: C H ClNO = 405.9. Adverse Effects, Treatment, and Precau- Naphasal; Naphcon Forte; Ital.: Collirio Alfa; Desamin Same; Imidazyl; Iridi- 21 24 5 na Due; Naftazolina; Pupilla; Rinazina; Rino Naftazolina; Video-Mill; Virgin- CAS — 31848-01-8 (morclofone); 31848-02-9 (mor- tions iana Gocce Verdi†; Malaysia: Albalon; Mex.: Afazol; Alphadinal; Celunaf; clofone hydrochloride). As for Sympathomimetics, p.1407; naphazoline has Fazolin; Gotinal; Nazil; Neth.: Albalon; NZ: Albalon†; Clear Eyes; Naphcon; ATC — R05DB25. mainly alpha-agonist effects. After local use, transient Philipp.: Cosooth; Pol.: Rhinazin; Rus.: Naphthyzin (Нафтизина)†; Sa- ATC Vet — QR05DB25. norin (Санорин); S.Afr.: Murine Clear Eyes†; Safyr Bleu; Spain: Alfa; Eub- irritation may occur. Rebound congestion may occur oral; Miraclar; Vasoconstrictor Pensa; Swed.: Rimidol†; Switz.: Albalon; Minha†; Thai.: Albalon; Naphcon; Turk.: Deltarhinol; Enflucide; UK: after frequent or prolonged use. Systemic effects, in- Murine; USA: Ak-Con; Albalon; All Clear; Allerest†; Allergy Drops†; Clear H C cluding nausea, headache, and dizziness have occurred Eyes; Clear Eyes Plus Redness Relief; Comfort Eye Drops†; Degest†; Na- 3 after topical use. Overdosage or accidental dosage by fazair†; Napha Forte; Naphcon; Privine; Vasocon†; Venez.: Clarasol; Clear- O ize; Fanasal†; Fazolan; Fazonil†; Gotinal; Nafin†; Naphcon; Nas; Niazol; Nina- mouth may cause CNS depression with marked reduc- zo. O tion of body temperature and bradycardia, sweating, Multi-ingredient: Arg.: Alercortil†; Alvo Nasal†; Antibiocort†; Bactio O drowsiness, and coma, particularly in children; it Rhin Prednisolona; Bideon; Biotaer Nasal; Dexafurazon†; Dexalergin; Disel Hidrocortisona; Drynisan; Factioneye; Fadanasal; Gramicortil†; Hyalcrom; should be used with great caution, if at all, in infants Mira Klonal; Mirus; Nasojol†; Nasomicina; Neo-Currino; Neodexa Plus; and young children. Use of naphazoline in the eye may Neoefodil†; Neosona; Nexadron Compuesto; Nexadron Plus; Panoptic; O N Provacsin Nasal; Refenax Colirio; Refenax Gotas Nasales; Rinofilax AG M; liberate pigment granules from the iris, especially Rinogel; Suavithiol; Vistacloran†; Austral.: Albalon-A; Antistine-Privine; In A H3C when given in high doses to elderly patients. Hyperten- Wink†; Naphcon-A; Optrex; Visine Allergy with Antihistamine; Austria: Coldistan; Coldophthal; Histophtal; Luuf-Nasenspray; Ophtaguttal; Rhino- Cl O sion may be followed by rebound hypotension. Treat- drin; Rhinon; Rhinoperd comp; Belg.: Diphenhydramine Constrictor†; Min- ment of adverse effects is symptomatic. havez; Naphcon-A; Neofenox; Sofraline; Sofrasolone; Zincfrin Antihistamin- Profile icum†; Braz.: Alergotox Nasal†; Claril; Colirio Legrand; Colirio Moura Effects on the eyes. For mention of conjunctivitis induced by Brasil; Colirio Teuto; Conidrin; Fluo-Vaso; Hemodotti; Hidrocin; Inhadrina†; Morclofone is a centrally acting cough suppressant used for non- Lerin; Maxibell; Mentodrin†; Naridrin; Nariflux; Naso-Josp†; Nazobel†; Na- productive cough (p.1547); it is given orally in usual doses of ophthalmic decongestant preparations containing naphazoline, zobio†; Neo Quimica Colirio; Nitrileno; Novo Rino; Rhinosept; Rinisone; 150 mg four or five times daily. It has also been given as the hy- see under Phenylephrine, p.1568. Rinosite†; Sinustrat Vasoconstritor; Sorine Adulto; Stilux; Visazul; Visiplex; drochloride. Visolon; Visual†; Zincolok; Canad.: Albalon-A; Clear Eyes Allergy; Collyre Intraoperative use. A report1 of 2 cases of toxicity associated Bleu†; Diopticon A; Naphcon-A; Onrectal; Opcon-A; Vasocon-A†; Visine Preparations with intraoperative use of a naphazoline-soaked sponge to con- Advance Allergy; Zincfrin-A; Chile: Albasol A†; Clarimir F; Dessolets; Miral; trol excessive bleeding after adenoidectomy. Both patients expe- Mirus†; Naphcon-A; Naphtears; Nico Drops; Novo-Tears; Oculosan; Ofta- Proprietary Preparations (details are given in Part 3) rienced hypertension and reflex bradycardia, which evolved in lirio; Red Off Aqua; Red Off Plus; Cz.: Sanorin-Analergin; Denm.: Ansal; Ital.: Plausitin; Switz.: Nitux. Antistina-Privin; Sesal; Fin.: Antistin-Privin†; Zincfrin-A†; Fr.: Collyre Bleu; one case into marked hypotension. There was evidence of CNS Derinox; Ger.: Antistin-Privin; Diabenyl-Rhinex†; duraultra; Konjunktival depression with a reduced respiration rate and prolonged recov- Thilo†; Oculosan N; Rhinoguttae Dexamethasoni cum Naphazolino†; Rhi- ery from anaesthesia. nosovil†; Siozwo; Stipo†; Gr.: Neo-Priphen; Oculosan; Septobore; Za- bysept; Hong Kong: Clear Blue; Frazoline; Konjunktival†; Naphcon-A; Na- (BAN, rINN) 1. Wenzel S, et al. Course and therapy of intoxication with imida- zin; Oculosan; Opcon-A; Hung.: Coldistan†; India: Andre; Andre-I-Kul; Naphazoline ⊗ zoline derivate naphazoline. Int J Pediatr Otorhinolaryngol Betnesol-N Nasal; Efcorlin; Fenox; Ocurest; Ocurest-AH; Ocurest-Z; Pro- 2004; 68: 979–83. to-Boric; Indon.: Flamergi; Indofrin-A; Isotic Azora; Naphcon-A; Oculosan; Nafatsoliini; Nafazolin; Nafazolina; Naphazolinum. 2-(1-Naph- Zincopto; Israel: Alnase; Antistin-Privin†; Nodryl†; Optryl; Phenyphrine- thylmethyl)-2-imidazoline. Interactions Azol†; Proaf; Ital.: Alfaflor; Antisettico Astringente Sedativo; Antistin-Privi- Нафазолин na; Collirio Alfa Antistaminico; Corizzina†; Deltarinolo; Fotofil; Genalfa; Id- Since naphazoline is absorbed through the nasal muco- roneomicil†; Imidazyl Antistaminico; Indaco; Iristamina; Nafcon A†; Oftalmil; C14H14N2 = 210.3. Pupilla Antistaminico; Rinocidina; Rinofomentil†; Zinc-Imizol; Malaysia: sa interactions may follow topical application. The Alergoftal; Napha A; Naphcon-A; Oculosan†; Mex.: Afazol Z; Biofrin; Bio- CAS — 835-31-4. BNF considers that all sympathomimetic nasal decon- tarson O; Eyrasil; Istasol; Midazol Ofteno; Mirus; Naphacel; Naphtears; ATC — R01AA08; R01AB02; S01GA01. Oftalirio†; Opcon-A; Soltrictor con Lagrifilm; Solutina; Sulvi; Zincfrin-A; NZ: gestants may cause a hypertensive crisis if used during Albalon-A†; Betnesol Aqueous; Clear Eyes ACR†; Degest 2†; Naphcon-A; ATC Vet — QR01AA08; QR01AB02; QS01GA01. treatment with an MAOI. For the interactions of sym- Optrex Red-Eye Relief; Visine Allergy; Philipp.: Decocon A; Moisturizing All Clear; Naphcon-A; Oculosan; Optaphen; Pol.: Betadrin; Cincol; Der- pathomimetics in general, see p.1407. mophenazol; Mibalin; Oculosan; Oftophenazol; Rhinophenazol; Sulfarinol; Port.: Alergiftalmina; Colircusi Anestesico; Naso-Prieulina†; Rus.: Betadrin N (Бетадрин); Polynadim (Полинадим); Sanorin (Санорин); Sanorin-Anal- Pharmacokinetics ergin (Санорин-аналергин); S.Afr.: Albalon-A†; Antistin-Privin; Covomy- Systemic absorption has been reported after topical use cin; Covosan; ENT; Nasdro; Oculosan; Universal Nasal Drops; Zincfrin-A; N Singapore: Antistin-Privin; Flucur†; Naphcon-A; Spain: Alergoftal; Cen- H of solutions of naphazoline. It is not given systemical- tilux; Cloram Zinc; Coliriocilina Adren Astr; Epistaxol; Kanafosal; Kanafosal ly, but it is readily absorbed from the gastrointestinal Predni; Oftalmol Ocular; Ojosbel; Rinovel; Zolina; Swed.: Antasten-Privin; Switz.: Antistin-Privin; Collyre Alpha†; Collyre Bleu Laiter; Gouttes nasales tract. Naphazoline instilled into the eye causes con- N†; Oculosan; Spray nasal comp pour adultes; Thai.: Levoptin; Naphcon- junctival vasoconstriction within 10 minutes and ef- A; Oculosan; Turk.: Alergoftal; Sulfarhin; UK: Eye Dew; Optrex Red Eyes; USA: 4-Way Fast Acting; Antazoline-V; Clear Eyes Seasonal Relief; Maxi- fects can last for up to 6 hours. mum Strength Allergy Drops; Nafazair A†; Naphazoline Plus; Naphcon-A; The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii)