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Buclizine Hydrochloride/Chlorphenamine Maleate 571

Hypersensitivity. Hypersensitivity reactions manifesting as tyrol; ratioAllerg; Reactine; Rigix; Tirizin; Virlix; Zirtek; Zyrtec; Belg.: His- Preparations
urticaria1,2 and fixed drug eruptions3 have been reported with ce- timed; Reactine; Zyrtec; Braz.: Aletir; Cetihexal; Cetrizin; Zetalerg;
Zetir; Zinetrin; Zyrtec; Canad.: Allergy Relief; Reactine; Chile: Alertop; Proprietary Preparations (details are given in Part 3)
tirizine. Coolips; Findaler; Histalen; Histax; Remitex; Rigotax; Sanaler; Sixacina; Denm.: Trihistan; Norw.: Trihistan.
1. Karamfilov T, et al. Cetirizine-induced urticarial reaction. Br J Zyrtec; Cz.: Alerid; Analergin; Cerex; Letizen; Parlazin; Reactine; Virlix;
Dermatol 1999; 140: 97980. Zodac; Zyrtec; Denm.: Alnok; Asytec; Benaday; Cidron; Gardex; Virlix; Multi-ingredient: Fin.: Anervan; Israel: Temigran; Neth.: Primatour;
2. Calista D, et al. Urticaria induced by cetirizine. Br J Dermatol Zyrtec; Fin.: Alzyr; Cidron; Gardex; Heinix; Histec; Senirex; Siterin; Norw.: Anervan; Spain: Diminex Antitusigeno; Swed.: Anervan; Exolyt.
Zyrtec; Fr.: Humex Rhinite Allergique; Reactine; Virlix; Zyrtec; Ger.:
2001; 144: 196. Alerid; Cetalerg; Ceterifug; Ceti-Puren; Ceti; Cetiderm; Cetidura; Ce-
3. Inamadar AC, et al. Multiple fixed drug eruptions due to ceti- til; CetiLich; Cetirigamma; Cetirlan; Reactine; Zetir; Zyrtec; Gr.: Agelmin;
rizine. Br J Dermatol 2002; 147: 10256. Alenstran; Alergoxal; Arzedyn; Bebexin; Blezamont; Cetialfa; Cetiram; Ce-
tirgen; Ceziren; Cirizine; Dermizin; Enahimine; Gentiran; Habitek; Hamil- Chloropyramine Hydrochloride (BANM, rINNM)
Sedation. For discussion of the sedative effects of antihista- tosin; Histafren; Kilsol; Lambeta; Ralizon; Remezine; Rezerc; Spatanil; Tasker;
mines see p.562. Telarix; Vitinelin; Zeda; Zepholin; Ziptek; Zirtek; Znupril; Hong Kong: Chloropyramine, Chlorhydrate de; Chloropyramini Hydrochlori-
Adezio; Cetihis; Cetirin; Cety; Histacet; Histazine; Marizine; Rhinil; Ryvel; dum; Halopyramine Hydrochloride; Hidrocloruro de cloro-
Interactions
Simtec; Vick-Zyrt; Zertine; Zicet; Zyrtec; Hung.: Alerid; Cetigen; Cetrin; piramina. N-(4-Chlorobenzyl)-NN-dimethyl-N-(2-pyridyl)ethyl-
Cetripharm; Merzin; Parlazin; Zyrtec; India: Alerid; Cetcip; Ceticad; Cetri-
wal; Cetrizet; Cetrizine; CTZ; ELG Nil; LGNil; Rinitrin; Zyrtec; Indon.: Be- enediamine hydrochloride.
As for the non-sedating antihistamines in general, tarhin; Cerini; Cetrixal; Cetryn; Cetymin; Estin; Falergi; Histrine; Incidal-OD;
p.563. However, some interactions are less likely with Ozen; Risina; Rydian; Ryvel; Ryzen; Ryzo; Tiriz; Zenriz; Irl.: Cetrine; Histek;
cetirizine than with non-sedating antihistamines such Zirpine; Zirtek; Zynor; Israel: Histazine; Zyllergy; Ital.: Formistin; Virlix; C 16 H 20 ClN 3 ,HCl = 326.3.
Zirtec; Jpn: Zyrtec; Malaysia: Adezio; Ceritec; Simtec; Zicet; Zyrtec;
as astemizole and terfenadine, since cetirizine appears Mex.: Apoliz; Cethexal; Kenicet; Reactine; Trizinet; Virlix; Zyrtec; Neth.: C AS 59-32-5 (chloropyramine); 6170-42-9 (chloro-
Reactine; Revalintabs; Zyrtec; Norw.: Acura; Reactine; Virlix; Zyrtec; NZ: pyramine hydrochloride).
to have low hepatic metabolism and little arrhyth- Razene; Zyrtec; Philipp.: Brellercet; Cet-10; Cetimin; Prixlae; Unizef; Virlix; ATC D04AA09; R06AC03.
mogenic potential (see Arrhythmias, above). Zinex; Zyrrigin; Zyrtec; Pol.: Acer; Alermed; Alerzina; Allertec; Amertil;
Ceratio; CetAlergin; Cetrivax; Cetrizen; Cetyryzyna; Letizen; Virlix; Zyrtec; ATC Vet QD04AA09; QR06AC03.
Anticoagulants. For a report of an interaction between ceti- Zyx; Port.: Cetix; Cinaz; Rinoliber; Virlix; Zyrtec; Rus.: Alerza ();
rizine and acenocoumarol, see under Interactions in Warfarin, Allertec (); Analergin (); Cetirinax (); Ce-
trine (); Letizen (); Parlazin (); Zetrinal
p.1429. (); Zodac (); Zyncet (); Zyrtec (); S.Afr.: Al- Cl
lecet; Allermine; Texa; Zetop; Zyrtec; Singapore: Adezio; Agelmin;
Allertec; Alzytec; Cetihis; Cetrine; Rhizin; Sancotec; Terizin; Zyrtec;
Pharmacokinetics Spain: Alercina; Alerlisin; Coulergin; Reactine Plus; Reactine; Virdox; Vir-
Cetirizine is rapidly absorbed from the gastrointestinal lix; Voltric; Zyrtec; Swed.: Acura; Alerid; Cidron; Reactine; Zyrlex; Switz.:
Cerzine; Cet eco; Cetallerg; Cetrine; Histatec; Tobin; Zyrtec; Thai.: Aller-
tract after oral doses, peak plasma concentrations being cet; Cetihis; Cetrimed; Cetrine; Cetrizet; Cetrizin; Ceza; Cistamine; Cyzine; N N CH3
attained within about an hour. Food delays the time to Fatec; Histica; Incidal-OD; Rentrex; Setin; Sutac; Terzine; Tizine; Triz; Uni- N
cet; Zensil; Zermed; Zertine; Zittec; Zymed; Zyrac; Zyrazine; Zyrcon;
peak plasma concentrations but does not decrease the Zyrex; Zyrtec; Turk.: Allerset; Cetryn; Hitrizin; Ressital; Setiral; Virlix; Yen-
amount of drug absorbed. Cetirizine is highly bound to izin; Zyrtec; UAE: Cetralon; UK: AllerTek; Benadryl Allergy Oral Solution; CH3
Benadryl One A Day; Cetirocol; Hayfever & Allergy Relief; Hayfever Relief;
plasma proteins and has an elimination half-life of Piriteze; Pollenshield; Zirtek; USA: Zyrtec; Venez.: Celay; Cetirex; Ce- (chloropyramine)
about 10 hours. It has been detected in breast milk. Ce- tirivax; Cetral; Cetrine; Talzic; Virlix; Zyrtec.
tirizine is excreted primarily in the urine mainly as un- Multi-ingredient: Arg.: Cabal-D; Cetriler D; Zyrtec-D; Austria: Cirrus;
Belg.: Cirrus; Reactine Pseudoephedrine; Braz.: Zyrtec-D; Canad.: Reac- Profile
changed drug. It does not appear to cross the blood- Chloropyramine hydrochloride, an ethylenediamine derivative,
tine Allergy & Sinus; Chile: Alertop-D; Findaler-D; Histalen D; Remitex D;
brain barrier to a significant extent. Rigotax-D; Sanaler-D; Zyrtec-D; Cz.: Pronose; Fin.: Cirrus; Fr.: Actifed- is an antihistamine (p.561). It has been given orally and by injec-
duo; Humex Rhinite Allergique; Ger.: Reactine duo; Zyrtec Duo; Hong tion.
References. Kong: Cirrus; Zyrtec-D; Hung.: Zyrtec-D; India: Alerid Cold; Alerid D;
1. Awni WM, et al. Effect of haemodialysis on the pharmacokinet- Amcold; Cheston Cold; Indon.: Cirrus; Ital.: Naristar; Pronose; Reactine; Preparations
ics of cetirizine. Eur J Clin Pharmacol 1990; 38: 679. Malaysia: Cirrus; Zyrtec-D; Mex.: Virlix-D; Zyrtec-D; NZ: Zyrtec De-
congestant; Pol.: Cirrus; Zyrtec D; Port.: Cirrus; Singapore: Cirrus; Proprietary Preparations (details are given in Part 3)
2. Desager JP, et al. A pharmacokinetic evaluation of the second- Spain: Naristar; Stopcold; Virlix Plus; Thai.: Zyrtec-D; Turk.: Cirrus;
generation H -receptor antagonist cetirizine in very young chil- Hung.: Suprastin; Mex.: Avapena; Rus.: Suprastin ().
USA: Zyrtec-D; Venez.: Cetirivax D; Zyrtec-D.
dren. Clin Pharmacol Ther 1993; 53: 4315.
3. Pitsiu M, et al. Retrospective population pharmacokinetic anal-
ysis of cetirizine in children aged 6 months to 12 years. Br J Clin
Pharmacol 2004; 57: 40211.
4. Hussein Z, et al. Retrospective population pharmacokinetics of
Chlorcyclizine Hydrochloride (BANM, rINNM) Chlorphenamine Maleate
levocetirizine in atopic children receiving cetirizine: the ETAC Chlorciklizino hidrochloridas; Chlorcyclizine, chlorhydrate de; (BANM, rINNM)
study. Br J Clin Pharmacol 2005; 59: 2837.
Chlorcyclizini hydrochloridum; Chlorcyclizinium Chloride; Chlo- Chlorfenamin-maleint; Chlorfenamino maleatas; Chlorofenam-
rcyklizin-hydrochlorid; Hidrocloruro de clorciclizina; Kloorisyklit- iny maleinian; Chlorphnamine, malate de; Chlorphenamini
Uses and Administration siinihydrokloridi; Klrciklizin-hidroklorid; Klorcyklizinhydroklorid.
Cetirizine hydrochloride, a piperazine derivative and maleas; Chlorpheniramine Maleate; Chlorprophenpyridamine
1-(4-Chlorobenzhydryl)-4-methylpiperazine hydrochloride. Maleate; Kloorifenamiinimaleaatti; Klorfenaminmaleat; Klr-
metabolite of hydroxyzine (p.581), is described as a
fenamin-malet; Maleato de clorfenamina. ()-3-(4-Chlorophe-
long-acting non-sedating antihistamine with some nyl)-NN-dimethyl-3-(2-pyridyl)propylamine hydrogen maleate.
mast-cell stabilising activity. It appears to have a low C 18 H 21 ClN 2,HCl = 337.3.
C AS 82-93-9 (chlorcyclizine); 1620-21-9 (chlorcyclizine
potential for drowsiness in usual doses and to be virtu-
hydrochloride). C 16 H 19 ClN 2 ,C 4 H 4 O 4 = 390.9.
ally free of antimuscarinic activity. It is used for the
ATC R06AE04. C AS 132-22-9 (chlorphenamine); 113-92-8 (chlo-
symptomatic relief of allergic conditions including
ATC Vet QR06AE04. rphenamine maleate).
rhinitis (p.565) and chronic urticaria (p.565).
ATC R06AB04.
In adults and children aged 6 years and over, cetirizine
hydrochloride is given in an oral dose of 10 mg once Cl ATC Vet QR06AB04.
daily or 5 mg twice daily. Children aged 2 to 5 years
may be given cetirizine 5 mg once daily or 2.5 mg Cl
CH3
twice daily. In the USA, children aged 6 months to 2
years may be given a dose of 2.5 mg once daily, in- N N
creased to a maximum of 2.5 mg twice daily in those H3 C
aged 12 months and over, for the treatment of perennial
allergic rhinitis and chronic urticaria. N N
It is also used with a decongestant such as pseudoephe-
CH3
drine hydrochloride.
Dosage of cetirizine should be reduced in patients with (chlorcyclizine) (chlorphenamine)
hepatic or renal impairment, see below.
Pharmacopoeias. In Eur. (see p.vii).
References. Ph. Eur. 6.2 (Chlorcyclizine Hydrochloride). A white or almost
Pharmacopoeias. In Chin., Eur. (see p.vii), Int., Jpn, US, and
1. Curran MP, et al. Cetirizine: a review of its use in allergic disor- Viet.
white, crystalline powder. Freely soluble in water and in dichlo- Ph. Eur. 6.2 (Chlorphenamine Maleate). A white or almost
ders. Drugs 2004; 64: 52361. romethane; soluble in alcohol. A 1% solution in water has a pH white, crystalline powder. Freely soluble in water; soluble in al-
Administration in hepatic or renal impairment. In pa- of 5.0 to 6.0. Protect from light. cohol. Protect from light.
tients with hepatic impairment, US licensed product information USP 31 (Chlorpheniramine Maleate). A white, odourless, crys-
recommends that the dosage of cetirizine may need to be reduced Profile
Chlorcyclizine hydrochloride, a piperazine derivative, is a sedat- talline powder. Soluble 1 in 4 of water and 1 in 10 of alcohol and
to half the usual oral daily dose (see above). Similarly in patients of chloroform; slightly soluble in ether and in benzene. Its solu-
with renal impairment, both the UK and US product information ing antihistamine (p.561). It has been given orally for the symp-
tomatic relief of hypersensitivity reactions; it has also been used tions in water have a pH between 4 and 5. Store in airtight con-
recommends a dosage reduction to half the usual daily dose. tainers. Protect from light.
as an antiemetic. It has been used in topical preparations, al-
Preparations though as with other antihistamines, there is a risk of sensitisa- Incompatibility. Chlorphenamine maleate has been reported to
tion. be incompatible with calcium chloride, kanamycin sulfate, no-
Proprietary Preparations (details are given in Part 3)
Arg.: Cabal; Cetidac; Cetizine; Cetriler; Salvalerg; Stopaler; Zyrtec; Aus- Chlorcyclizine dibunate (naftoclizine) has been used as a cough radrenaline acid tartrate, pentobarbital sodium, and meglumine
tral.: Alzene; Zyrtec; Austria: Alerid; Cetiderm; Cetirhexal; Cetiristad; Ce- suppressant similarly to sodium dibunate (p.1573). adipiodone.
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)
572 Antihistamines
Dexchlorpheniramine Maleate (BANM, rINNM) rphenamine is widely distributed in the body, and en- polistirex (a sulfonated diethenylbenzene-ethenylben-
Dekschlorfeniramino maleatas; Dekskloorifeniramiinimaleaatti; ters the CNS. zene copolymer complex), chlorphenamine tannate,
Dexchlorfeniramin-maleint; Dexchlorphenamine Maleate; Dex- Chlorphenamine maleate is extensively metabolised. and dexchlorpheniramine tannate are given orally and
chlorphniramine, Malate de; Dexchlorpheniramini maleas; Metabolites include desmethyl- and didesmethylchlo- are used similarly to the maleate.
Dexklorfeniraminmaleat; Dexklrfeniramin-malet; Maleato de
rphenamine. Unchanged drug and metabolites are ex- Malaria. Chlorphenamine may be tried in patients with malaria
dexclorfeniramina.
creted primarily in the urine; excretion is dependent on who have chloroquine-induced pruritus (see Effects on the Skin,
p.600), but additionally it has been shown to have some promise
urinary pH and flow rate. Only trace amounts have
C AS 25523-97-1 (dexchlorpheniramine); 2438-32-6 as an adjunct in the treatment of chloroquine-resistant malaria
(dexchlorpheniramine maleate). been found in the faeces. itself. Early studies indicated that chlorphenamine was only one
ATC R06AB02. A duration of action of 4 to 6 hours has been reported; of a number of drugs that reversed chloroquine resistance in vitro
ATC Vet QR06AB02. this is shorter than may be predicted from pharmacok- in isolates of Plasmodium falciparum. Later clinical studies in
inetic parameters. children in Nigeria showed enhanced efficacy when chlorphen-
amine was given with chloroquine.1-5 The overall management
CH3 Cl More rapid and extensive absorption, faster clearance, of malaria is discussed on p.594.
and a shorter half-life have been reported in children. 1. Sowunmi A, et al. Enhanced efficacy of chloroquine-chlorphe-
niramine combination in acute uncomplicated falciparum malar-
N References. ia in children. Trans R Soc Trop Med Hyg 1997; 91: 637.
H3C 1. Rumore MM. Clinical pharmacokinetics of chlorpheniramine. 2. Sowunmi A, Oduola AMJ. Comparative efficacy of chloro-
Drug Intell Clin Pharm 1984; 18: 7017. quine/chlorpheniramine combination and mefloquine for the
2. Paton DM, Webster DR. Clinical pharmacokinetics of H -recep- treatment of chloroquine-resistant Plasmodium falciparum ma-
N tor antagonists (the antihistamines). Clin Pharmacokinet 1985; laria in Nigerian children. Trans R Soc Trop Med Hyg 1997; 91:
10: 47797. 68993.
3. Yasuda SU, et al. The roles of CYP2D6 and stereoselectivity in 3. Sowunmi A, et al. Comparative efficacy of chloroquine plus
the clinical pharmacokinetics of chlorpheniramine. Br J Clin chlorpheniramine and pyrimethamine/sulfadoxine in acute un-
Pharmacol 2002; 53: 51925. complicated falciparum malaria in Nigerian children. Trans R
(dexchlorpheniramine) Soc Trop Med Hyg 1998; 92: 7781.
4. Sowunmi A, et al. Comparative efficacy of chloroquine plus
Pharmacopoeias. In Eur. (see p.vii), Jpn, and US. Uses and Administration chlorpheniramine and halofantrine in acute uncomplicated falci-
Ph. Eur. 6.2 (Dexchlorpheniramine Maleate). A white or almost Chlorphenamine maleate, an alkylamine derivative, is parum malaria in Nigerian children. Trans R Soc Trop Med Hyg
1998; 92: 4415.
white, crystalline powder. Very soluble in water; freely soluble in a sedating antihistamine that causes a moderate degree 5. Okonkwo CA, et al. Effect of chlorpheniramine on the pharma-
alcohol, in dichloromethane, and in methyl alcohol. A 1% solu- of sedation; it also has antimuscarinic activity. cokinetics of and response to chloroquine of Nigerian children
tion in water has a pH of 4.5 to 5.5. Protect from light. with falciparum malaria. Trans R Soc Trop Med Hyg 1999; 93:
USP 31 (Dexchlorpheniramine Maleate). A white, odourless, Chlorphenamine is a racemic mixture; the dextrorota- 30611.
crystalline powder. Soluble 1 in 1.1 of water, 1 in 2 of alcohol, 1 tory isomer, dexchlorpheniramine, has about twice the Preparations
in 1.7 of chloroform, and 1 in 2500 of ether; slightly soluble in activity of chlorphenamine by weight. BP 2008: Chlorphenamine Injection; Chlorphenamine Oral Solution; Chlo-
benzene. pH of a 1% solution in water is between 4.0 and 5.0. rphenamine Tablets;
Store in airtight containers. Protect from light. Chlorphenamine maleate and dexchlorpheniramine USP 31: Acetaminophen, Chlorpheniramine Maleate, and Dextromethor-
maleate are used for the symptomatic relief of allergic phan Hydrobromide Tablets; Chlorpheniramine Maleate and Phenylpropa-
nolamine Hydrochloride Extended-release Capsules; Chlorpheniramine
Adverse Effects and Precautions conditions including urticaria and angioedema (p.565), Maleate and Phenylpropanolamine Hydrochloride Extended-release Tab-
As for the sedating antihistamines in general, p.561. rhinitis (p.565), and conjunctivitis (p.564), and in pru- lets; Chlorpheniramine Maleate and Pseudoephedrine Hydrochloride Ex-
tended-release Capsules; Chlorpheniramine Maleate and Pseudoephedrine
Exfoliative dermatitis may develop. Injections may be ritic skin disorders (p.565). They are common ingredi- Hydrochloride Oral Solution; Chlorpheniramine Maleate Extended-release
irritant and cause transient hypotension or stimulation ents of compound preparations for symptomatic treat- Capsules; Chlorpheniramine Maleate Injection; Chlorpheniramine Maleate
Syrup; Chlorpheniramine Maleate Tablets; Dexchlorpheniramine Maleate
of the CNS. ment of coughs and the common cold (p.564). Syrup; Dexchlorpheniramine Maleate Tablets.
However, such preparations should be used with cau- Proprietary Preparations (details are given in Part 3)
Effects on the blood. There are several old and isolated re-
ports of blood dyscrasias after use of chlorphenamine maleate;
tion in children, and generally avoided in those under 2 Arg.: Afeme; Alergidryl; Alergitrat; Isomerine; Qura Plus; Austral.: Polar-
amine; Austria: Polaramin; Belg.: Polaramine; Braz.: Alergonil; Alergov-
these include agranulocytosis,1,2 thrombocytopenia,3 pancytope- years of age (see p.562). Chlorphenamine may be giv- alle; Alergyo; Alermine; Deflux; Dexclor; Dexlerg; Dexmin; Ex-
nia,4 and aplastic anaemia.5 Haemolytic anaemia has occurred en intravenously as an adjunct in the emergency treat- pectamin F; Histamin; Hystin; Polamin; Polaramine; Polaren; Polaryn;
after use of dexchlorpheniramine maleate.6 The association with Canad.: Chlor-Tripolon; Novo-Pheniram; Chile: Asafen Nueva Formula;
ment of anaphylactic shock (p.563). Clorprimeton; Nipolen; Prodel; Scadan; Denm.: Polaramin; Fr.: Polaramine;
antihistamine use has been questioned in some of these cases.7 Ger.: Polaronil; Gr.: Istamex; Polaramine; Hong Kong: Allermin; Apomin;
1. Shenfield G, Spry CJF. Unusual cause of agranulocytosis. BMJ
Chlorphenamine maleate is given in oral doses of 4 mg Chlorpyrimine; Dapriton; Kenyamine; Medifen; Pirimat; Piriton; Polara-
1968; ii: 523. every 4 to 6 hours up to a maximum of 24 mg daily. mine; Rhiniramine; Sprinsol; Synchloramin; Uni-Ramine; India: Cofton; In-
2. Hardin AS. Chlorpheniramine and agranulocytosis. Ann Intern Doses for children, according to age, are: 1 to 2 years, don.: Chlorphenon; Cohistan; CTM; Orphen; Pehachlor; Polamec; Polara-
Med 1988; 108: 770. mine; Polarist; Polofar; Irl.: Piriton; Israel: Ahiston; Anaphyl; Ital.:
3. Eisner EV, et al. Chlorpheniramine-dependent thrombocytope- 1 mg twice daily; 2 to 5 years, 1 mg every 4 to 6 hours Polaramin; Trimeton; Malaysia: Chloramine; Chlormine; Chlorpyrimine;
nia. JAMA 1975; 231: 7356. (maximum 6 mg daily); 6 to 12 years, 2 mg every 4 to D-Antihist; Dex-Antihist; Dexchloramine; Polamine; Polaramine; Somin;
Mex.: Alerdil; Antadex-H; Blendox; Cloro-Trimeton; Cronal; Docsi; Hi-
4. Deringer PM, Maniatis A. Chlorpheniramine-induced bone-mar- 6 hours (maximum 12 mg daily). Although not li- erbal; Histadryl; Polaramine; Neth.: Polaramine; Norw.: Phenamin; Polar-
row suppression. Lancet 1976; i: 432. amin; NZ: Histafen; Polaramine; Philipp.: Antamin; Barominic; Chlor-Tri-
5. Kanoh T, et al. Aplastic anaemia after prolonged treatment with censed in the UK, the BNFC suggests that children meton; Valemine; Virgomine; Port.: Trenelone; S.Afr.: Allergex; Chlor-
chlorpheniramine. Lancet 1977; i: 5467. aged 1 month and over may be given 1 mg twice daily. Trimeton; Chlorhist; Polaramine; Rhineton; Singapore: Allerphen;
6. Duran-Suarez JR, et al. The I antigen as an immune complex Chloramine; Chlorpyrimine; Dexchloramine; Dextramine; Piriton; Polara-
receptor in a case of haemolytic anaemia induced by an antihis- Chlorphenamine maleate may be given by intramuscu- mine; Rhiniramine; Somin; Spain: Antihistaminico; Polaramine; Swed.: Po-
taminic agent. Br J Haematol 1981; 49: 1534. lar, by subcutaneous, or by slow intravenous injection laramin; Switz.: Polaramine; Thai.: Allergin; Chlorleate; Chlorpheno;
7. Spry CJF. Chlorpheniramine-induced bone-marrow suppression. Chlorpyrimine; Cohistan; Histatab; Histatapp; Icolid Plus; Kloramin; Na-
Lancet 1976; i: 545.
over a period of 1 minute. The usual dose is 10 to samine; Piriton; UAE: Chlorohistol; UK: Allercalm; Allergy Relief; Allerief;
20 mg and the total dose given by these routes in 24 Calimal; Hayleve; Piriton; Pollenase Antihistamine; USA: Aller-Chlor; Aller-
Effects on the senses. Chlorphenamine has been reported to gy; Allergy Relief; Chlo-Amine; Chlor-Pro; Chlor-Trimeton; ChlorTan; Ed-
affect the senses of smell and taste.1 hours should not normally exceed 40 mg. For children, Chlor-Tan; Efidac 24 Chlorpheniramine; PediaCare Allergy Formula; Pedia-
1. Schiffman SS. Taste and smell in disease. N Engl J Med 1983; doses of 87.5 micrograms/kg subcutaneously four tan; Pediox-S; QDALL AR; TanaHist PD; Teldrin; Venez.: Clorotrimeton;
Inquiramin; Liramin.
308: 12759. times daily have been suggested. The following
Multi-ingredient: numerous preparations are listed in Part 3.
Extrapyramidal disorders. Facial dyskinesias have been parenteral doses may also be used in children: the usual
reported1,2 after oral doses of chlorphenamine maleate. dose in those aged 1 month to 1 year is
1. Thach BT, et al. Oral facial dyskinesia associated with prolonged 250 micrograms/kg; those aged 1 to 5 years may be Chlorphenoxamine Hydrochloride (BANM, rINNM)
use of antihistaminic decongestants. N Engl J Med 1975; 293:
4867. given a dose of 2.5 to 5 mg and those aged 6 to 12 Chlorphnoxamine, Chlorhydrate de; Chlorphenoxamini Hy-
2. Davis WA. Dyskinesia associated with chronic antihistamine years, 5 to 10 mg. Alternatively, children and adoles- drochloridum; Hidrocloruro de clorfenoxamina; Klorfenoksamin
use. N Engl J Med 1976; 294: 113. cents aged 1 to 18 years may be given a dose of Hidroklorr. 2-(4-Chloro--methylbenzhydryloxy)-NN-dimeth-
200 micrograms/kg. The BNFC suggests that doses for ylethylamine hydrochloride.
Interactions children may be repeated if necessary up to 4 times in
As for the sedating antihistamines in general, p.563. 24 hours. C 18 H 22ClNO,HCl = 340.3.
Antiepileptics. For a report of the effect of chlorphenamine on Dexchlorpheniramine maleate is given in oral doses of C AS 77-38-3 (chlorphenoxamine); 562-09-4 (chlorphe-
phenytoin, see p.499. noxamine hydrochloride).
2 mg every 4 to 6 hours up to a maximum of 12 mg ATC D04AA34; R06AA06.
Pharmacokinetics daily. Children aged 2 to 5 years may be given 0.5 mg ATC Vet QD04AA34; QR06AA06.
Chlorphenamine maleate is absorbed relatively slowly every 4 to 6 hours (maximum 3 mg daily), and those
from the gastrointestinal tract, peak plasma concentra- aged 6 to 12 years, 1 mg every 4 to 6 hours (maximum Cl
tions occurring about 2.5 to 6 hours after oral doses. 6 mg daily).
Bioavailability is low, values of 25 to 50% having been Modified-release oral preparations of chlorphenamine O CH3
reported. Chlorphenamine appears to undergo consid- maleate or dexchlorpheniramine maleate are available N
erable first-pass metabolism. About 70% of chlorphen- in some countries; dosage is specific to a particular for- CH3
amine in the circulation is bound to plasma proteins. mulation. CH3
There is wide interindividual variation in the pharma- Dexchlorpheniramine maleate has been applied topi-
cokinetics of chlorphenamine; values ranging from 2 cally in some countries, although as with other antihis- (chlorphenoxamine)
to 43 hours have been reported for the half-life. Chlo- tamines there is a risk of sensitisation. Chlorphenamine