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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-
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
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-
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
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