Thonzylamine Hydrochloride/Tritoqualine 593 Adverse Effects and Precautions and rhinitis (p.565), and in pruritic skin disorders Med-Actigen†; Medofed; Milafed; Nanafed†; Nasolin†; Nostrilet; Policol; Policold; Polyfed; Pondactil; Profed; Prophedin; Sinusaid; Sufed; Trifed; Tri- As for the sedating antihistamines in general, p.561. (p.565). It is often used in combination with pseu- ofed; Tripo; Triprodrine; Vefed†; Vesprolid-HCL; Turk.: A-ferin; Actidem; UK product information for acrivastine has warned doephedrine hydrochloride for rhinitis and in other Actifed; UAE: Sedofan; Sedofan DM; UK: Benylin Childrens Coughs & Colds; Multi-Action Actifed; Multi-Action Actifed Chesty Coughs Expecto- that acrivastine should not be used in patients hyper- compound preparations for the symptomatic treatment rant; Multi-Action Actifed Dry Coughs; Sudafed Plus; USA: Actagen; Acta- sensitive to triprolidine. of coughs and the common cold (p.564). gen-C Cough; Actifed; Actifed Cold & Allergy; Actifed Cold & Sinus; Actifed Plus; Allercon; Allerfrim; Allerfrim with Codeine; Allerphed; Aprodine; Breast feeding. No adverse effects have been seen in breast- It is given orally, the usual dose for adults being 2.5 mg Aprodine with Codeine; Bayer Select Night Time Cold; Cenafed Plus; fed infants whose mothers were receiving triprolidine, and the up to four times daily. Genac; Silafed; Trifed-C Cough; Triofed; Tripohist D; Triposed; Zymine HC; 1 Zymine-D; Venez.: Actifed†. American Academy of Pediatrics considers that it is therefore Triprolidine tannate has been used similarly. usually compatible with breast feeding. In a study2 in 3 women of the excretion of triprolidine and pseu- Triprolidine hydrochloride has also been applied topi- doephedrine, taken orally in a combined preparation, triprolidine cally to the skin although, as with other antihistamines, Tritoqualine (rINN) was found to reach concentrations in breast milk similar to those there is a risk of sensitisation. L-554; Tritocualina; Tritoqualinum. 7-Amino-4,5,6-triethoxy-3- found in plasma in one subject, and slightly lower than in plasma (5,6,7,8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]iso- in the others. It was calculated that 0.06 to 0.2% of the ingested Preparations quinolin-5-yl)phthalide. dose was distributed into breast milk over 24 hours. Concentra- BP 2008: Triprolidine Tablets; tions of pseudoephedrine in breast milk exceeded those in plas- USP 31: Triprolidine and Pseudoephedrine Hydrochlorides Syrup; Tripro- Тритоквалин ma in all 3 women. lidine and Pseudoephedrine Hydrochlorides Tablets; Triprolidine Hydro- chloride Syrup; Triprolidine Hydrochloride Tablets. C26H32N2O8 = 500.5. 1. American Academy of Pediatrics. The transfer of drugs and oth- CAS — 14504-73-5. Proprietary Preparations (details are given in Part 3) er chemicals into human milk. Pediatrics 2001; 108: 776–89. ATC — R06AX21. Correction. ibid.; 1029. Also available at: Israel: Pro-Actidil†; Ital.: Actidil†; Spain: Pro-Actidil†; UAE: Sedofan T; http://aappolicy.aappublications.org/cgi/content/full/ USA: Zymine. ATC Vet — QR06AX21. pediatrics%3b108/3/776 (accessed 30/01/04) Multi-ingredient: Arg.: Actifedrin; Austral.: Actifed; Actifed CC Junior; 2. Findlay JWA, et al. Pseudoephedrine and triprolidine in plasma Codral Original Day & Night Cold & Flu; Sudafed Sinus Day & Night Relief; and breast milk of nursing mothers. Br J Clin Pharmacol 1984; Sudafed Sinus Pain & Allergy Relief; Belg.: Actifed; Braz.: Actifedrin; Trife- 18: 901–6. drin; Canad.: Actifed; Actifed Plus; CoActifed; Covan†; ratio-Cotridin; ra- H3C tio-Cotridin Expectorant; Chile: Actifedrin; Actifedrin Antitusivo; Cz.: CH3 Trifed Expectorant†; Trifed†; Fr.: Actifed; Actifed Toux Seche†; Ger.: Rhi- N Interactions nopront Kombi; Hong Kong: Actifed; Actifed Compound; Actifed DM†; O As for the sedating antihistamines in general, p.563. Actihist-Co†; Antifort; Cough-EN†; Fedac; Fedac Compound; Prolifed; Set- CH3 prodine†; Syncofit; Uni-Fedra Compound; Vidalidine; India: Actifed DM†; O O Actifed Plus†; Actifed†; Actiflu; Actiflu Plus; Ascoril-D+; Deletus; Deletus D; Pharmacokinetics Nocold Plus; Indon.: Actifed; Actifed DM; Actifed Expectorant; Actigesic; Alerfed; Crofed; Eflin; Flutrop; Lapifed; Lapifed DM; Lapifed Expectorant; O O After absorption from the gastrointestinal tract, tripro- O O Nasafed; Nasafed Plus; Nichofed; Nostel; Protifed; Stop Cold; Tremenza; H C lidine is metabolised; a carboxylated derivative ac- Trifed; Trifedrin; Valved; Valved DM; Irl.: Actifed; Actifed Chesty†; Actifed 3 Compound†; Benylin Childrens Cough and Cold; Benylin Dual Action Dry; NH CH counts for about half the dose excreted in the urine. Re- Israel: Actifed Compound†; Actifed DM†; Actifed Expectorant†; Actifed†; O 2 3 ported half-lives vary from 3 to 5 hours or more. Histafed; Histafed Comp; Histafed Expectorant; Sinufed Kid Night†; Ital.: Actifed; Actifed Composto; Actigrip; Malaysia: Actifed; Actifed DM; Ac- Triprolidine is distributed into breast milk. tifed Expectorant; Actihist; Actihist Expectorant; Actihist-Co; Axcel Tridine; Profile Beatafed; Beatafed Compound†; Cough-EN; Decol; Fedac; Pabron Cold & Tritoqualine is stated to inhibit histidine decarboxylase which ca- ◊ General references. Flu; Pabron Cough & Sinus; Pabron Cough-D; Peace; Pseudoephedrine T; talyses the conversion of histidine to histamine. It has no action 1. Paton DM, Webster DR. Clinical pharmacokinetics of H -recep- Rhynacol; Mex.: Actifed; Actifed DM; Giparlix; NZ: Actifed; Codral Day- on histamine H -receptors and at therapeutic doses has no seda- tor antagonists (the antihistamines). Clin Pharmacokinet 1985; time/Nightime; Sudafed Day/Nightime Relief; Sudafed Sinus Pain & Allergy 1 10: 477–97. Relief; Pol.: Actifed; Actitrin; Port.: Actifed; Dinaxil; S.Afr.: Actifed; Actifed tive or antimuscarinic effects. It has the uses of antihistamines 2. Miles MV, et al. Pharmacokinetics of oral and transdermal Cold & Fever; Actifed Dry Cough Regular; Actifed Dry Cough Sugar Free; (p.563) and has been given orally in usual doses of 200 to triprolidine. J Clin Pharmacol 1990; 30: 572–5. Acuflu P; Acugest; Acugest Co; Acugest DM; Acugest Expect; Acutussive; 600 mg daily in 2 or 3 divided doses for the symptomatic relief Adco-Flupain; Adco-Tussend; Betafed; Coff-Rest†; Coryx; Endcol Cough of hypersensitivity reactions including allergic rhinitis and urti- Linctus†; Endcol DM†; Endcol Expectorant†; Fludactil Co; Fludactil Expec- Uses and Administration torant†; Fludactil†; Linctifed; Medifed; Merck-Cough Linctus; Merck-Expec- caria. Triprolidine hydrochloride, an alkylamine derivative, torant; Merck-Fed; Neofed†; Sinuclear; Tixylix Flu; Trifen; Singapore: 3P†; Preparations Actifed; Actifed Compound; Actifed DM; Actifed Expectorant; Beactafed; is a sedating antihistamine with antimuscarinic and Beactafed Co; Cough-EN; Fedac; Fedac Compound; Peacef; Trodrine†; Proprietary Preparations (details are given in Part 3) mild sedative effects. It is used for the symptomatic re- Unitifed†; Spain: Iniston Antitusivo y Descongestivo; Iniston Desconges- Austria: Hypostamin; Fr.: Hypostamine; Ger.: Inhibostamin†. tivo; Iniston Expectorante y Descongestivo; Thai.: Actifed; Actifed Com- lief of allergic conditions including urticaria (p.565) pound†; Actifed DM; Actil; Actiplex; Clinikold; Cofed; Consudine; Hiscifed; 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) Antimalarials/Amodiaquine 597 en at intervals at least one month apart. For maximum ben- 14. Lengeler C. Insecticide-treated bed nets and curtains for pre- soning. However, large doses of amodiaquine have been report- efit 2 to 3 doses of IPT should be given. For further venting malaria. Available in The Cochrane Database of Sys- ed to produce syncope, spasticity, convulsions, and involuntary tematic Reviews; Issue 2. Chichester: John Wiley; 2004 (ac- 9 information on the use of pyrimethamine in pregnancy, see cessed 18/08/05). movements. under Precautions for Pyrimethamine, p.611. In areas of 15. CDC. Malaria. In: The Yellow Book: CDC Health Information 1. Anonymous. Amodiaquine and agranulocytosis. WHO Drug Inf for International Travel; 2008. Available at: 1987; 1: 5–6. low or unstable malaria transmission, where pregnant http://wwwn.cdc.gov/travel/yellowBookCh4-Malaria.aspx (ac- 2. Larrey D, et al. Amodiaquine-induced hepatitis. Ann Intern Med women have low immunity to malaria, use of insecticide- cessed 28/09/07) 1986; 104: 801–3. treated nets and prompt case management of pregnant 16. Chiodini P, et al. HPA Advisory Committee on Malaria Preven- 3. Phillips-Howard PA, West LJ. Serious adverse drug reactions to tion in UK Travellers. Guidelines for malaria prevention in trav- pyrimethamine–sulphadoxine, pyrimethamine–dapsone and to women with fever and malarial illness is recommended. In ellers from the United Kingdom (issued 01/07). Available at: amodiaquine in Britain. J R Soc Med 1990; 83: 82–5. addition, all pregnant women should take iron and folate http://www.hpa.org.uk/web/HPAwebFile/HPAweb_C/ 4. Anonymous. Development of recommendations for the protec- supplements. 1203496943523 (accessed 17/06/08) tion of short-stay travellers to malaria endemic areas: memoran- dum from two WHO meetings. Bull WHO 1988; 66: 177–96. Prophylaxis during breast feeding. It is generally ac- 5. Olliaro P, et al. Systematic review of amodiaquine treatment in cepted for most antimalarials that the amounts distributed uncomplicated malaria. Lancet 1996;