Fumarate 631

agitation 50 to IOOmg is injected intramuscularly initially, ling reasons and precautions should be taken in all (BANM, USAN, r!NNM} and the dose may be repeated every four to six hours as patients.1 Ketotifen Fumarate tlc!:WsJ:J;.\kei:otrfuhli required. For other indications when oral dosage is not 1. The Drug Database for Acute Porphyria. Available at: http://www. Fumarato de k&t{)iifijllio;. ketoitfeer.i: practical, the intramuscular dose is 2 5 to I 00 mg. drugs-porphyria.org {accessed 07/I0/11) vetyft,omaraatt:i; ·'k-etot\!eri l'umara�e; Ketotife e, .1 h!�EI1\Il9€j�• � Hydroxyzine should not be given by intravenous injection Fumarate dE;; hiPrcig�oofumarate de: Ketotifen­ since haemolysis may result. Interactions fumarat; Ketc,tifeK�t{ltlfe:liiiih&Orqg(\n-tUmari!t; Ketotifenhyctrogenfu­ For doses in children, see below. Dosage should be � .. As for the sedating antihistamines in general, p. 614.3. marat; Ketot ireni um�ras; .K�totifeoi reduced in patients with hepatic or renal impairment, see � • Ketotifeno,, fum?raro Ketotiferio-vander;ifiohydrCJ9<>n�fvrt)a furhaiatras:.as; below. · Cimetidine. A pharmacokinetic study iu 16 patients noted Ketot.tfeilvatefu maiat; Kerotk1de; (ile�:;lilP!lT· 4,S . .lcytloh(;lpt�:. hydroxyzine. 1 The combination generally produced a children to treat pruritus in the following oral doses ! l;2CI;Jt:hiophen-HJ(9!-I)-On�. hydm'qen fumarate. greater suppression of the cutaneous response to hist­ c1,t-h;NoS,c,H.a,Pfi5 5 expressed as the hydrochloride: •. · •· ·· ·. . . · · amine than hydroxyzine alone, but the difference was not children aged 6 months to 6 years: initially 5 to 15 mg . . .. • significant. RoiJ!,X17; . daily increased if necessary to 50 rng daily in divided C4S -..,- 34� /3-7:· (kero tif.eQ)J 34$8.0- 14:8 (ketotifen. film arate).. doses I. Simons FER, et al. Effect of the Hrantagonist cimetidine on the . ATC -'-Vet C!ROMXS01I7/'Gx0&QSO/GXQB ; pharmacokinetics and pharmacodynamics of the H1-antagonists :c- those 6 to 12 years of age: initially 15 to 25mg daily • hydroxyzine and cetirizine in patients with chronic urticaria. J Allergy � increased if necessary to 50 to 100 mg daily in divided Clin Immunol 1995; 95: 685-93. HBDSOJ WQRO: . . . doses Alternatively, I mg/kg daily may be given in divided doses, Pharmacokinetics Ph. Eur. 8: (Ketotifen Hydrogen Fumarate; Ketotifen to a maximum of 2.5 rng/kg daily in children aged I to 6 Fumarate BP 2014). A white to brownish-yellow, fine years or to a maximum of 2 mg/kg daily in those aged over 6 Hydroxyzine is rapidly absorbed from the gastrointestinal crystalliue powder. Sparingly soluble in water; very slightly years. tract and is metabolised. Metabolites include cetirizine soluble in acetonitrile; slightly soluble in methyl alcohol. The pre- or postoperative sedative dose in children is (p. 619.2), which has antihistaminic activity. An elimina­ 600 micrograms/kg orally; alternatively, a dose of 1.1 mg/kg tion half-life of about 20 hours has been reported. Uses and Administration has been given by intramuscular injection. References. Ketotifen is a sedating antihistamine (p. 610.2) that also has Children and adolescents aged 12 years and over may be I. Paton DM, Webster DR. Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet 1985; 10: 477-97. a stabilising action on mast cells analogous to that of sodium given usual adult doses, see p. 630.3. cromoglicate (p. 1226.1). It is used in the treatment of Administration in hepatic or renal impairment. In Liver disorders. For reference to a prolonged half-life of allergic conditions such as rhinitis (p. 612.1) and patients with hepatic impairment, UK licensed product hydroxyzine in patients with primary biliary cirrhosis, see conjunctivitis (p. 611.1). Ketotifen has also been used in under Adverse Effects and Precautions, above. the prophylactic management of asthma, when it may take information recommends a 33% reduction in the total 1 oral daily dose of hydroxyzine. In patients with moderate several weeks to exert its full effect; it should not be used to P epa a ons treat acute asthma attacks. or severe renal impairment, a dose reduction of 50% is ..r ...... r.....ti .. . Ketotifen is given as the fumarate, but doses are recommended. (details are given in Volume B) Proprietary...... Preparations .. expressed in terms of the base; ketotifen fumarate 1.38 rngis Anxiety disorders. Although hydroxyzine is used in the Single-ingredient Preparations. Arg.: Ataraxone; Hyderax; Aus­ equivalent to about I mg of ketotifen. management of anxiety, there is little evidence to support tria: Atarax; Belg.: Atarax; Braz.: Drotizin; Hidroxine; Hixilerg; Ketotifen fumarate is taken in oral doses equivalent to Hixizine; Pruri-Gran; Prurizin; Atarax; Dalun; its efficacy in anxious patients, 1 and the BNF considers Canad.: Chile: I mg of ketotifen twice daily with food, increased if Fasarax; Cz. : Atarax; Denm.: Atarax; Fin.: Atarax; Fr. : Atarax; that use of antihistamines solely for their sedative effect in necessary to 2 rng twice daily; 0.5 to I rng at night may be 3 Ger.: AH N; Atarax; Gr.: Atarax; Ictinal; Iremofar; Hong preferable for the first few days of treatment if drowsiness is anxiety is not appropriate. Kong: Atarax; Qualidrozine; Vataraxt; Hung.: Atarax; India: Ballenger JC, et al. Consensus statement on generalized anxiety disorder likely to be a problem. l. Atarax; H-Rax; Rozen; Hydil; Hydroze; Krust; Nizod; Indon.: from the International Consensus Group on Depression and Anxiety. J Ketotifen fumarate has also been applied topically, as eye Bestalin; Iterax; IrL Ucerax; Israel: Otarex; Ital.: Atarax; Clin Psychiatry 2001; 62 (suppl 11): 53-8. Available at: http:/lwww. Malaysia: Atarax; Mex. : Atarax; Neth.: Ataraxt; Norw.: Atarax; drops equivalent to 0.025% ketotifen, used twice daily. psychiatrist.com/private/supplenet/v62sll/v62sll08.p df (accessed For children's doses, see below. 15/08/08) NZ: Seredd; Philipp.: Iterax; Pol.: Atarax; Port.: Atarax; Cora­ phenet; Rus.: Atarax (AmpaKc); S.Afr. : Aterax; Neuraxt; Sin­ gapore: Atarax; Hizin; Phymorax; Spain: Atarax; Swed.: Atarax; Action. It has been suggested that the anti-allergic action Adverse Effects and Precautions Switz.: Atarax; Thai.: Abacus; Actadon; Allerax; Antipru; Anti­ of ketotifen was independent of its antihistaminic proper­ As for the sedating antihistarniues in general, p. 613.1 and zine; Atalog; Atano; Atarax; Cerax; Dormirax; Drazine; Hadar­ ties.' This might be due to its effect on responses to plate­ p. 613.3, respectively. ax; Histan; Hiszine; Hizin; Honsa; Hydrox; Hyzine; Katrax; Poli­ let-activating factor (PAF).2 However, the significance of Intramuscular injection of hydroxyzine has been zine; R-Rax; Taraxin; Trandrozine; Unaminet; Xyzine; Turk.: PAF in the pathogenesis of asthma has been questioned. Atarax; Validol; Vistaril; UK: Atarax; Ucerax; Ukr.: Atarax 1. Greenwood C. The pharmacology of ketotifen. Chest 1982; 82 (suppl): reported to cause marked local discomfort. Intravenous (ATapaKc); use has been associated with haemolysis. USA1 Vistaril. 455-85. 2. Morley J, et al. Effects of ketotifen upon responses to platelet activating Multi�ingredient Preparations. Braz.: Marax; India: Marax; S. factor: a basis for asthma prophylaxis. Ann Allergy 1986; 56: 335-40. Arrhythmias. ECG abnormalities, particularly alterations Afr_ : Geratart; Spain: Calmoplext; Dolodenst; Ukr.: Distonin in T -waves, were associated with anxiolytic doses of (,UIICTOHHH)t; USA: Hydrophed; Marax; Theomax DF. Administration in children. Ketotifen fumarate can be hydroxyzine hydrochloride and were similar to those pro­ given to children for the treatment of allergic conditions duced by thioridazine and tricyclic antidepressants.1 PharmacopoeialPreparations BP 2014: such as rhinitis (p. 612.1) or conjunctivitis (p. 611.1), and 1 Hydroxyzine Oral Solution; Hydroxyzine Tablets; I. Hollister LE. Hydroxyzine hydrochloride: possible adverse cardiac USP 36: Hydroxyzine Hydrochloride Injection; Hydroxyzine has been used in the prophylactic management of asthma. interactions. Psychophannacol Comm 1975; 1: 61-5. Hydrochloride Syrup; Hydroxyzine Hydrochloride Tablets; Oral doses equivalent to I mg of ketotifen twice daily with Hydroxyzine Pamoate Capsules; Hydroxyzine Pamoate Oral food may be used from 3 years of age. A dose equivalent Effects on sexual function. A 32-year-old man had pro­ Suspension. to 500 micrograms ketotifen twice daily has been given to longed penile erections (priapism) after taking two sepa­ children aged between 6 months and 3 years. rate doses of hydroxyzine for a skin rash 1 It was suggested Ketotifen fumarate has also been applied topically twice that the effect might be due to a hydroxyzine metabolite lsothipendyl Hydrochloride (BANM, r!NNM} daily, as eye drops equivalent to 0.025% ketotifen, in that was found to be structurally similar to a metabolite of children from 3 years of age. trazodone, a drug known to induce penile erections. Hidrodoruro isotlpendll; tsothiPl'ndy!, Chlorhydrate I. Thavundayil JX. et a!. Prolonged penile erections induced by lsothiperx;lylide. HydrochlorlduQil; lsotipendii, hidrod\)ruro de;q'; Asthma.Results of studies on the efficacy of ketotifen in hydroxyzine: possible mechanism of action. Neuropsychobiology 1994; vhort-tneHAvma t-tApoxn

. • hydrochloride for restlessness developed a fixed drug erup­ . anti-asthmatic drugs, 2.4 others have reported no significant tion of the penis.1 All recovered on drug withdrawal and C,6H,�N:;S,HCI"'321.9 benefits, 5•6 and UK guidelines on the management of subsequently had positive rechallenges. C4S - 482-15-5 (isothipemJyl); asthma consider ketotifen to be ineffective.' A systematic

I. Cohen et al. Fixed drug eruption of the penis due to hydroxyzine review8 found that it was of benefit in improving control , hydrochloD04M:?iR06AD09.ride). hydrochloride.HA Ann Pharmacother 1997; 31: 327-9. ATC :..__ of asthma and wheezing in children with mild to moder­ . ate disease, but noted that the high prevalence of atopy in ATCV.:C.ei 99i{- Af!1LBVIJQD04AA22;, (}R06AD09 Intra-arterial injection. Accidental intra-arterial injection UN/I several of the studies reviewed meant that the results of hydroxyzine has led to necrosis of the extremity requir­ might not be generalisable to children with asthma in gen­ ing amputation of the digits of the affected lirnb.1 Profile era!. A study in children described as 'preasthmatic' (that 1. Hardesty Inadvertent intra-arterial injection. lAMA I 970; 213: 872. . Isothipendyl hydrochloride, an azaphenothiazine deriva­ is, being at high risk of developing asthma) suggested that WH tive, is an antihistamine (p. 610.1) that has been applied long-term therapy with ketotifen decreased the risk of It has been suggested1 that hydroxyzine Liver disorders. topically for hypersensitivity and pruritic skin disorders asthma onset.9 should only be given once daily for the relief of pruritus in although as with any antihistamine there is a risk of I. Paterson JW, et al. Evaluation of ketotifen (HC20-511) in bronchial patients with primary biliary cirrhosis. The mean serum 25: 1 sensitisation. It has also been given orally and by the rectal asthma. Eur J Clin Phannaco/ 1983; 187-93. elimination half-lives of hydroxyzine and its metabolite 2. Tinkelman DG, et a!. A multicenter trial of the prophylactic effect of route. cetirizine in 8 patients with primary biliary cirrhosis were ketotifen, theophylline, and placebo in atopic asthma. J Allergy Clin Immunol 1985; 76: 487-97. prolonged at 36.6 and 25.0 hours, respectively. 3. Miraglia Del Giudice M, et al. Study of the efficacy of ketotifen treatment Simons FER, et al. The pharmacokinetics and pharmacodynamics of l. in asthmatic children under 3 years of age. Curr Ther Res 1986; 40: 685- hydroxyzine in patients with primary biliary cirrhosis. J Clin Phannacol ProprietaryPreparations (details are given in Volume B) 93. 1989; 29: 809-1 5. 4. Rackham A, et al. A Canadian multicenter study with Zaditen {ketotifen) Arg. : Actapront; Braz.: Andantol; in the treatment of bronchial asthma in children aged 5 17 years. J Single�ingredient Preparations. 10 Porphyria. The Drug Database for Acute Porphyria, corn­ Fr. : Apaisylt; Apaisylgel; Histapaisyl; Sedermyl; Indon.: Andan­ Allergy ClinImmunol 1989; 84: 286-96. 5. White et al. Ketotifen in the young asthmatic-a double-blind piled by the Norwegian Porphyria Centre (NAPOS) and tol; Israel: Thiodantol; Ital.: Calmogel; Mex. : Andantol. , placebo-controlledMP trial. J Int Med Res 1988; 16: 107-13. the Porphyria Centre Sweden, classifies hydroxyziue as Multi-ingredient Preparations.Ind on.1 Nipe; Transpulmin. 6. Volovitz B, et al. Efficacy and safety of ketotifen in young children with porphyrinogenic; it should be prescribed only for compel- asthma. J Allergy Clin lmmuno/ 1988; 81: 526-30.

The symbol t denotes a preparation no longer actively marketed 632 Antihistamines

7. Scottish Intercollegiate Guidelines Network/British Thoracic Society. Firmapol; Frenasma; Isocaren; K-Drops; Kathricol; Klevistamin; necessary. It is recommended that treatment should be British guideline on the management of asthma: a national clinical Labelphen; Lavoptik; Meni-drops; Nostimex; Noxtor; Orpidix; stopped if there is no improvement within 3 days. guideline (issued May 2008, revised June 2009). Available at: http:// Pellexeme; Sudaved; Urpem; Zaditen; Zeoklamin; Zethrinal; www.sign.ac.uk/pdf/signlOl.pdf (accessed 06/08/09) References. Zidofen; Hong Kong: Amitone; Asmafen; Astifen; Dhatifen; 1 I. Noble McTavish D. Levocabastine: an update of its pharmacology, 8. Bassler D, et al. Ketotifen alone or as additional medication for long-term 5, control of asthma and wheeze in children. Available in The Cochrane Ketifent; Vidatifent; Zaditen; Hung.: Zaditen; India: Airyfen; clinically efficacy and tolerability in the topical treatment of allergic Database of Systematic Reviews; Issue l. Chichester: John Wiley; 2004 Albalon; Asthafen; Azofen; Ketasma; Ketorid; Ketotif; Mastifen; rhinitis and conjunctivitis. Drugs 1995; 50: I032-49. (accessed 14/04/08). Indon.: Astifent; lntifen; Nortifen; Prevast; Profilas; Scanditen; 2. Doughty MJ. Levocabastinc, a topical ocular antihistamine available as a 9. Bustos GJ, et a!. Prevention of asthma with ketotifen preasthmatic pharmacy medicine - a literature review. Pharm 2002; 268: 367-70. in Zaditen; Irl. : Zaditen; Israel: Profiten; Zaditen; Ital. : Allealt; .l 25: children: a three-year foUow-up study. Clin ExpAller gy 1995; 568-73. Allerket; Bentifen; Chetofen; Chetotifene; Ketoftil; Sosefen; Stamifent; Zaditen; Jpn: Zaditen; Malaysia: Asmafen; Asmaten; Administration in children. For dosage in children, see Conjunctivitis. References. Asumalife; Denerel; Dhatifen; Ketifen; Licoften; Zaditen; Mex.: above. 1. Martfn AP, et al. The effect of ketotifen on inflammatory markers in allergic conjunctivitis: an open, uncontrolled study. BMC Ophthalmol AsmaralMK; Biotifen; Cantelt; Kasmal; Kedrop; Keraffler; 2003; 3: 2. Available at: http://www.biomedcentral.com/content/pdf/ Nemodine; Nomotec; Osaten; Pretifen; Saluket-H1; Ventisol; Adverse Effects and Precautions 1471-2415-3-2.pdf (accessed 17/08110) Zaditen; Neth.: Altriabak; Bentifent; Zaditen; Norw.: Zaditen; 2. Kidd M, et at. Efficacy and safety of ketotifen eye drops in the treatment NZ: Asmafent; Zaditen; Philipp.: Azimef; Zadec; Zaditen; Pol.: As·for the antihistamines in general. p. 613.1 and p. 613.3, of seasonal allergic conjunc1ivitis. Br J Ophthalmol 2003; 87: 1206-ll. Zaditen; Port.: Bentifen; Cipanfeno; Zabak; Zaditen; Rus.: respectively. The most common adverse effects reported 3. Ganz M, et al. Ketotifen fumarate and olopatadine hydrochloride in the Zaditen (3MHTeH); Zetifen (3eTnljleH)t; S.Afr. : Adco·Zetofen; with Ievocabastine eye drops are transient stinging and treatment of allergic conjunctivitis: a real-world comparison of efficacy burning of the eyes, urticaria, dyspnoea, drowsiness, and and ocular comfort. Adv Therapy 2003; 20: 79-91. Ketohexalt; Zaditen; Singapore: Amitone; Asmafen; Asmaten; 4. Abelson MB, et al. Efficacy and safety of single-and multiple-dose Asumalife; Beatifen; Denerel; Dhatifen; Erliten; Licoften; SP­ headache. With nasal use headache, nasal irritation, ketotifen fumarate 0.025% ophLhalmic solution in a pediatric Totifen; Suntotifen; Tofen; Zaditen; Spain: Bentifen; Okeye; somnolence, and fatigue have been noted. The use of population. Pediatr Allergy Immunol 2004; 15: 551-7. Zaditen; Zasten; Swed. : Zaditen; Switz.: Zabak; Zaditen; Thai.: levocabastine nasal spray is not recommended in those with Ibis; Katifen; Kenefen; Keten; Ketifent; Keto; Ketofen; Medko­ significant renal impairment. Adverse Effects and Precautions fent; Politifen; Sukafen; Sykofen; TM Fen; Zadino; Zaditen; Zetofen; Zytofen; Turk.: Astafen; Fumast; Mitofen; Zaditen; Porphyria. The Drug Database for Acute Porphyria, com· As for the antihistamines in general, p. 613.1 and p. 613.3, UAB: Asmafort; UK: Zaditen; Ukr.: Zaditen (3a;:uneH); USA: piled by the Norwegian Porphyria Centre (NAPOS) and respectively; drowsiness may be a problem, and dry mouth Alaway; Claritin Eye; Itchy Eye Dropst; Visine All Day Eye Itch the Porphyria Centre Sweden, classifies levocabastine as and dizziness may occur at the beginning of treatment but Relief; Zaditor; Zyrtec Itchy Eye Drops; Venez. : Cosolve; Ketop­ probably not porphyrinogenic when given intra-nasally; it tic; Ketotisin; Zaditen. usually resolve with continued use. Weight gain and CNS may be used as a drug of first choice and no precautions stimulation have been reported. Isolated cases of severe skin are needed. When given ophthalmically it has been classi Multi-ingredient Preparations. Arg.: Hyalcrom NF; China: Xu · reactions, cystitis, and hepatitis have been reported. Hong (it!!.*); India: Azofen-T; Mastifen-C; Mastifen-S; Mex. : fied as not porphyrinogenic.1 Irritation, pain, and punctate keratitis are commonly Hyalcrom NF. l. The Drug Database for Acute Porphyria. Available at: http:/!www. reported after topical application to the eye. drugs-porphyria.org (accessed 07/ l 0/ ll) Sin1ilar precautions to those for sodium cromoglicate (p. 1227.2) should be observed in asthmatic patients. latrepirdine (USAN. r/NN) Ketotifen may take several weeks to exert its full effect; Pharmacokinetics existing anti -asthma treatment should not be abruptly Dlmebpl; Dirnebolio; Dimeboffne; Levocabastine is absorbed after both nasal and ocular use. mebane; a !.atrepirdine:· ir n Systemic availability has been estimated at 60 to 80% after withdrawn after starting ketotifen therapy. It should not be DSfiN·0622-'\78;r L;;� tr pirdin ; Latrep iDimebon;um; PF" used for the treatment of acute asthma attacks. e L\HMe6om1H. d nasal doses and 30 to 60% after ocular use. However absolute peak plasma concentrations are low. Plasma 1. 913�.39;et.narahydro-rpei11<1P2.ii)I-1H;l"dimethyi- 5:[2-\6:rnethyl-3-f)yridi Overdosage. Overdoses of ketotifen ranging from 0 to 2;3,4,'5-T1H:p yriqof4,3·b]iodoi<:>. nyil protein binding is about 55%. An elimination half-life of 35 120 mg were reported in 8 patients. 1 Symptoms includedI to 40 hours has been reported for all routes of delivery. etf:lyl]c · drowsiness, confusion, dyspnoea, bradycardia or tachy­ 97657-92·6 Elimination of levocabastine is mainly renal with 70% (]2,H>ONl=3195- 315 13-[ 3'8 cardia, disorientation, and convulsions. Gastric lavage was CAS (lo.rtepkdine� (la trepitdlne excreted as unchanged drug and 10% as an inactive . · performed in 6 patients. and all 8 recovered within 12 dihydroctrlorideJ; 14292-23'0 (lmrep!rdine x-hydrochlqride) . acetylglucuronide metabolite; the remaining 20% is hours after supportive treatment. excreted unchanged in the faeces. IJN/1 -'-- O[J923 1K)Z6: . In an overview of 21 cases of overdosage (including those Trace amounts of levocabastine have been found in reported above) the manufacturers stated that no serious Profile breast milk after ocular and nasal use. signs or symptoms had been reported with doses below Latrepirdine is an antihistamine that is reported to also have References. 20 mg, and there had been no fatalities 2 The most serious I. Heykants J, et al. The pharmacokinetic properties of topical neuroprotective effects. It is under investigation as the effects reported had included unconsciousness, convulsions, levocabastine: a review. Clin Pharmacokinet 1995; 29: 221-30. dihydrochloride in the treatment of Alzheimer's disease (see bradycardia and tachycardia, and a severe hypotensive Dementia, p. 388.1) and Huntington's disease. P epa a ons reaction. Management is essentially supportive and r r ti...... symptomatic. References. . . 1. Doody RS, et a!. Effect of dimebon on cognition, activities of daily living, Proprietary. Preparations (details are given in Volume B) I. Jefferys DB, Volans GN. Ketotifen overdose: surveillance of the toxicity behaviour, and global function in patients with mild-to-moderate 282: Arg.: Histimet; Austral. : Livostin; of a new drug. BMJ 1981; 1755-6. Alzheimer's disease: a randomiscd, double-blind, placebo-controlled Single�ingredient Preparations. 2. Le Blaye I, et at. Acute ketotifen overdosage: a review of present clinical study. Lancet 2008; 372: 207-15. Austria: Livostin; Belg. : Livostin; Braz.: Livostin; Canad.: Livos­ 7: experience. Drng Safety 1 992; 387-92. 2. Kicburtz �t a!. A randomized, placebo-controlled trial of latrepirdine tin; Chile: Livostint; China: Livostin Cz. : Livostin; K, in Huntington disease. Arch Neurol 2010; 67: 154-60. Denm.: Benaliv; Livostint; Fin.: Livostin;(V:1l1J); Fr. : Allergiflash; Porphyria. The Drug Database for Acute Porphyria, com­ Levofree; Levophta; Ger.: Livocab; Gr.: Livostin; Israel: LivosM piled by the Norwegian Porphyria Centre (NAPOS) and tin; Ital.: Levoreact; Levostab; Livocabt: Livostin; Jpn: Livostin; the Porphyria Centre Sweden, classifies ketotifen as not Levocabastine Hydrochloride Mex. : Livostin; Neth.: Livocab; Norw.: Livostin; NZ: Livostin; Port. : Livostin; S.A r.: Livostin; Sinumax Allergy; Spain: Bilina; porphyrinogenic when given by the ophthalmic route; it (BANM, USAN, r/NNM) f may be used as a drug of first choice and no precautions Livocabt; Reactine Levocabastina; Swed.: Livostin; Switz.: · Livostin; Livostint; Livostin. are needed. The safety of systemic formulations has not Hidrodowro · de Jevocaba�tint>; Levocabastina, hidrocloruro 1 Turk.: Venez.: yet been classified. 1 de; . Levocabastine, .: chiorhvdrate de; Lev()(abastinhvoro­ . 1. The Drug Database for Acute Porphyria. Available at: http:f/www. chlori.d; Hy rochlorid\ tn; �evocabastini d J ·. Levokabastilnihy-· drugs-porphyria.org (accessed 07110/11) drokl(?ridi; Levokqbastlo-hydrochiorid; -��vo kabqs\inhydrok­ lorid; . k vCJkabastino hidro�hloridas;. . � L�vokabaS4tin­ Interactions hldroRlorid; WS0$47; J)�aoKa6amn;a. As for the sedating antihistamines in general, p. 614.3. <+trf{nS' 1-[cis'4·Cyan(.\'4·(p·fluoroprMJ:lpOhenyl)cyclohexX110f)lr!!l. \llJ-3- A reversible fall in the platelet count has been seen in ·a meth}+4·phen�lisonipegooc acid hydmchlorlde. few patients receiving ketotifen with oral antidiabetics and (26HEFN:z02,HQ=457Q · it has been suggested that this combination should therefore � be avoided. CAS . 795 16-6�� (l� vocabasrine).' . l954/C78- 7 (levocabas.tinf! . iwdnxhlork;!e); 7944 9-98"-2 {cabestine). Pharmacokinetics ATC,..�R01AC02; SO I.GXO:?,QSOI GX02 ATCUN!J ·.Vet.�··124X...,- QRM.A01A6YEI.C02; Ketotifen fumarate is almost completely absorbed from the gastrointestinal tract after oral doses, but bioavailability is NOTE. Cabastine (riNN) is the racemate of levocabastine. reported to be only about 50% due to hepatic first-pass Pharmacopoeias. In Bur. (see p. vii) and US. metabolism. Peak plasma concentrations occur 2 to 4 hours Ph. Eur. 8: (Levocabastine Hydrochloride). A white or after an oral dose. It is mainly excreted in the urine as almost white powder. Practically insoluble in water; slightly inactive metabolites with a small amount of unchanged soluble in alcohol and in a 0.2% solution of sodium drug; the terminal elimination half-life is about 21 hours. hydroxide; sparingly soluble in methyl alcohol. Protect from P epa a ons light. r r ti USP 36: (Levocabastine Hydrochloride). Protect from light. Proprietary Preparations (details are given in Volume B) Single-ingredient Preparations. Arg.: Antilerg; Bilozen; Bio­ Uses and Administration mirat; Farmoftal; Ketocev; Respimex; Zaditen; Austral.: Levocabastine, a piperidine derivative, is a long-acting and Zaditen; Austria: Ketotisan; Zaditen; Belg.: Altriabak; Zaditen; potent antihistamine with a rapid onset of action. Braz.: Asdron; Asmalergin; Asmanon; Asmax; Asmen; Asmifen; Asmofen; Biatos; Octifen; Prurifen; Zaditen; Zetitec; Canad. : Levocabastine hydrochloride equivalent to 0.05% levoca� Zaditen; Zaditor; Chile: Farmoftal; Ketotisin; Oftaler; Zaditen; bastine is used topically twice daily as eye drops or as a nasal China: Bei Ka Ming (IJ1-FBJl);Rui Na TI Tong Fen spray in the treatment of allergic conjunctivitis (p. 611.1) Cz.: Ketof; Zabak; Zaditen; Denm.: (J1fflJlllZaditen;'!i'); Zalerg; Fi(iii]n.: and rhinitis (p. 612.1), respectively. in adults and children Levocetirizine is the R-enantiomer of cetirizine (p. 619.2) Zaditen;1r); Fr. : Zaditen; Zalerg; Ger.: Ketoft; Padiatifent; Zaditen; aged 9 years and over. The frequency of the dose in both and is used similarly, as the hydrochloride, for the Gr.: Cleroptic; Demetofrin; Dovidio; Ecradin; Eucycline; Fental; conditions may be increased to 3 or 4 times daily if symptomatic relief of allergic conditions including rhinitis

All cross-references refer to entries in Volume A