640 Antihistamines
Propiomazine Hydrochloride {BANM, r!NNMJ P..r�p�rc:Jti()n.� ...... m (details are given in Volume B) propiorf,azina; to o azine; Chiorhydrate ProprietaryPreparations HidrodoruroPropi<;>rn deazini HydrochloridP pium; f1ponvtot,la3Y!Ha China: Qi Qi Hung. : de; Single-ingredient Preparafions. Loderixt. CIH'f); rMAPOX!10p!'\A. C;cJcl1_,--N_,QS,HCI�3.76_91 Rupatadine is an antihistamine with platelet-activating CAS 240) 5-9. factor (PAF) antagonist activity that is used for the Terfenadine (BAN, USAN, r!NN) treatment of allergic rhinitis (p. 612.1) and chronic 1 idiopathic urticaria (p. 612.3). It is given as the fumarate although doses are expressed in terms of the base; rupatadine fumarate 12.8 mg is equivalent to about 10 mg of rupatadine. The usual oral dose is the equivalent of 10 mg once daily of rupatadine.
Izquierdo I. et a!. Rupatadine: a new selective histamine HI receptor and platelet-activating factor (PAF) antagonist: a review of pharmacological profile and clinical management of allergic rhinitis. Drugs Today 2003; 39: 451-68. 2. Kearn SJ,Plosker GL. Rupatadine: a review of its use in the management of allergic disorders. Drugs 2007; 67: 457-74. 3. Fantin et at. International Rupatadine study group. A 12-week 5, 8: (Terfenadine). A white or almost white, placebo-controlled study of rupatadine 10 mg once daily compared with Ph. Bur. cetirizine IO mg once daily, in the treatment of persistent allergic crystalline powder. It shows polymorphism. Very slightly rhinitis. Allergy 2008; 63: 924-3 1. soluble in water and in dilute hydrochloric acid; freely 4. Valero A, et a!. Safety ofrupatadine administered over a period of 1 year soluble in dichloromethane; soluble in methyl alcohol. in the treatment of persistent allergic rhinitis; a multicentre, open-label Protect from light. Profile study in Spain. Drug Safety 2009; 32: 33-42. Propiomazine, a phenothiazine derivative, is a sedating antihistamine (p, 610,1) that has been used for its sedative Effects on the cardiovascular system. Licensed product Uses and Administration and antiemetic properties in insomnia (p. 611.2) and nausea information states that the cardiac safety of rupatadine has and vomiting (p, 61 L 3). been assessed; no adverse ECG effects were noted when Terfenadine, a piperidine derivative, is a non -sedating Propiomazine is given as the maleate but doses are rupatadine was given in doses of up to 10 times the nor antihistamine. It does not have significant antimuscarinic expressed in terms of the base; propiomazine maleate mal dose. Nevertheless, it is recommended that rupatadine actions. It has been used for the symptomatic relief of 1.3 mg is equivalent to about 1 mg of propiomazine. Doses is used with caution in patients with known prolongation allergic conditions including rhinitis (p. 612.1) and equivalent to 25 to 50 mg orally at night have been given as of the QT interval, uncorrected hypokalaemia, or condi conjunctivitis (p. 611.1) and skin disorders such as urticaria a hypnotic. tions such as bradycardia or acute myocardial ischaemia. (p. 612.3). Propiomazine hydrochloride has been given parenter A review of Spanish and Portuguese spontaneous The maximum oral dose of terfenadine is 120 mg daily ally. reporting scheme data found 5 cases of heart rhythm given either as 60 mg twice daily or 120 mg in the morning; disturbances in patients taking rupatadine.1 Such effects a starting dose of 60 mg daily in a single dose or in two Porphyria. The Drug Database for Acute Porphyria, com included palpitations and tachycardia and 1 case of torsade divided doses is recommended for rhinitis and conjunctiv piled by the Norwegian Porphyria Centre (NAPOS) and de pointes in an elderly man. itis. For dosage in renal impairment see below. the Porphyria Centre Sweden, classifies propiomazine as I. Carvajal A, et al. Heart rhythm disturbances associated with rupatadine: not porphyrinogenic; it may be used as a drug of first a case series from the Spanish and Portuguese pharmacovigilance choice and no precautions are needed.1 systems. Clin Pharmacol Ther 2009; 85: 481-4. Administration in renal impairment. Half the usual oral 1. The Drug Database for Acute Porphyria. daily dose of terfenadine (see above) has been suggested drugs-porphyria.org (accessed 07/10/11) for patients with creatinine clearance less than 40 mL/mi nute. Preparations ProprietaryPreparations (details are given in Volume B) Single-ingredient Preparations. Arg.: Rupafin; Austria: Rupafin; ProprietaryPreparations (details are given in Volume B) Belg. : Rupatall; Braz.: Rupafin; Cz.: Tamalis; Fr. : Wystamm; Adverse Effects and Precautions Rupafint; Urtimed; Rupafin; Levostar-R; Single�ingredient Preparations. Swed.: Propavan. Ger.: Gr.: India: Irl.: As for the non-sedating antihistamines in general, p. 613.1. Rupafin; Ital.: Pafinur; Rupafin; Neth.: Rupafin; Pol.: Rupafin; Erythema multiforme and galactorrhoea have also been Port.: Rinialer; Spain: Alergoliber; Rinialer; Rupafin; Thai.: Rupafin; Turk.: Rupafin; UK: Rupafin. reported. Quifenadine Hydrochloride (r!NNMJ 1 Ventricular arrhythmias, including torsade de pointes, have occurred rarely with terfenadine, particularly in Hicirodorvro <)uifenadiha; Qlji(ena<:line. Ch!orhydrat,-;.d�; 1 association with raised blood concentrations (see Arrhyth QuifenadiQI Hydrde ochiorldum; Xt
All cross-references refer to entries in Volume A