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should be alert to the development of eosinophilia,

vasculitic rash, worsening pulmonary symptoms, cardiac complications, or periphe


ral neuropathy.
Pregnancy There is limited evidence for the safe use
of leukotriene receptor antagonists during pregnancy;
however, they can be taken as normal in females who
have shown a significant improvement in asthma not
achievable with other drugs before becoming pregnant,
see also p. 131.
MONTELUKAST
Cautions interactions: Appendix 1 (leukotriene
receptor antagonists)
Pregnancy manufacturer advises avoid unless essential; see also notes above
Breast-feeding manufacturer advises avoid unless
essential
Side-effects abdominal pain, thirst, headache,
hyperkinesia (in young children); less commonly dry
mouth, dyspepsia, oedema, dizziness, drowsiness,
malaise, sleep disturbances, sleep-walking, abnormal
dreams, anxiety, agitation (including aggressive
behaviour or hostility), depression, psychomotor
hyperactivity (including irritability and restlessness),
paraesthesia, hypoaesthesia, seizures, arthralgia,
myalgia (including muscle cramps), epistaxis, bruising; rarely palpitation, trem
or, disturbance in attention, memory impairment, increased bleeding tendency; ve
ry rarely hepatic eosinophilic infiltration,
hepatic disorders, hallucinations, suicidal thoughts
and behaviour, disorientation, Churg-Strauss
syndrome (see notes above), erythema nodosum,
erythema multiforme
Indications and dose
Prophylaxis of asthma see notes above and Management of Chronic Asthma table, p.
133
. By mouth
Child 6 months 6 years 4 mg once daily in the
evening
Child 6 15 years 5 mg once daily in the evening
Child 15 18 years 10 mg once daily in the evening
Symptomatic relief of seasonal allergic rhinitis in
children with asthma
. By mouth
Child 15 18 years 10 mg once daily in the evening
Montelukast (Non-proprietary) A
Chewable tablets, montelukast (as sodium salt)
4 mg, net price 28-tab pack = 1.96; 5 mg, 28-tab
pack = 2.35. Label: 23, 24
Excipients include aspartame (section 9.4.1)
Granules, montelukast (as sodium salt) 4 mg, net
price 28-sachet pack = 4.01. Counselling, administration
Counselling Granules may be swallowed whole or mixed
with cold, soft food (not liquid) and taken immediately
Tablets, montelukast (as sodium salt) 10 mg, net
price 28-tab pack = 2.33
Singulair (MSD) A
Chewable tablets, pink, cherry-flavoured, montelukast (as sodium salt) 4 mg, net
price 28-tab pack =
25.69; 5 mg, 28-tab pack = 25.69. Label: 23, 24
Excipients include aspartame equivalent to phenylalanine
674 micrograms/4-mg tablet and 842 micrograms/5-mg
tablet (section 9.4.1)

Granules, montelukast (as sodium salt) 4 mg, net


price 28-sachet pack = 25.69. Counselling, administration
Counselling Granules may be swallowed whole or mixed
with cold, soft food (not liquid) and taken immediately
Tablets, beige, f/c, montelukast (as sodium salt)
10 mg, net price 28-tab pack = 26.97
Note The Scottish Medicines Consortium has advised (June
2007) that Singulair chewable tablets and granules are
restricted for use as an alternative to low-dose inhaled
corticosteroids for children 2 14 years with mild persistent
asthma who have not recently had serious asthma attacks
that required oral corticosteroid use, and who are not
capable of using inhaled corticosteroids; Singulair chewable
tablets and granules should be initiated by a specialist in
paediatric asthma
ZAFIRLUKAST
Cautions interactions: Appendix 1 (leukotriene
receptor antagonists)
Hepatic disorders Children or their carers should be told
how to recognise development of liver disorder and advised
to seek medical attention if symptoms or signs such as
persistent nausea, vomiting, malaise or jaundice develop
Hepatic impairment manufacturer advises avoid
Renal impairment manufacturer advises caution
Pregnancy manufacturer advises use only if potential
benefit outweighs risk; see also notes above
Breast-feeding present in milk manufacturer
advises avoid
Side-effects gastro-intestinal disturbances; headache;
rarely bleeding disorders, hypersensitivity reactions
including angioedema and skin reactions, arthralgia,
myalgia, hepatitis, hyperbilirubinaemia, thrombocytopenia; very rarely Churg-Str
auss syndrome (see
notes above), agranulocytosis
Indications and dose
Prophylaxis of asthma see notes above and Management of Chronic Asthma, p. 133
. By mouth
Child 12 18 years 20 mg twice daily
Accolate (AstraZeneca) A
Tablets, f/c, zafirlukast 20 mg, net price 56-tab pack
= 17.75. Label: 23
3.4 Antihistamines,
immunotherapy, and
allergic emergencies
3.4.1 Antihistamines
3.4.2 Allergen immunotherapy
3.4.3 Allergic emergencies
3.4.1 Antihistamines
Antihistamines (histamine H1-receptor antagonists) are
classified as sedating or non-sedating, according to their
relative potential for CNS depression. Antihistamines
differ in their duration of action, incidence of drowsiness, and antimuscarinic
effects; the response to an
antihistamine may vary from child to child (see Sideeffects, p. 152). Either a s
edating or a non-sedating
antihistamine may be used to treat an acute allergic
reaction; for conditions with more persistent symptoms
which require regular treatment, a non-sedating antiBNFC 2014 2015 3.4 Antihistami
nes, immunotherapy, and allergic emergencies 151
3Respiratory system

histamine should be used to minimise the risk of sedation and psychomotor impair
ment associated with
sedating antihistamines.
Oral antihistamines are used in the treatment of nasal
allergies, particularly seasonal allergic rhinitis (hay
fever), and may be of some value in vasomotor rhinitis;
rhinorrhoea and sneezing is reduced, but antihistamines
are usually less effective for nasal congestion. Antihistamines are used topical
ly to treat allergic reactions in
the eye (section 11.4.2) and in the nose (section 12.2.1).
Topical application of antihistamines to the skin is not
recommended (section 13.3).
An oral antihistamine may be used to prevent urticaria,
and for the treatment of acute urticarial rashes, pruritus,
insect bites, and stings. Antihistamines are also used in
the management of nausea and vomiting (section 4.6),
of migraine (section 4.7.4.1), and the adjunctive management of anaphylaxis and
angioedema (section 3.4.3).
The non-sedating antihistamine cetirizine is safe and
effective in children. Other non-sedating antihistamines
that are used include acrivastine, bilastine, desloratadine (an active metabolit
e of loratadine), fexofenadine
(an active metabolite of terfenadine), levocetirizine (an
isomer of cetirizine), loratadine, mizolastine, and
rupatadine. Most non-sedating antihistamines are
long-acting (usually 12 24 hours). There is little evidence that desloratadine or
levocetirizine confer any
additional benefit they should be reserved for children
who cannot tolerate other therapies.
Sedating antihistamines are occasionally useful when
insomnia is associated with urticaria and pruritus (section 4.1.1). Most of the
sedating antihistamines are
relatively short-acting, but promethazine may be effective for up to 12 hours. A
limemazine and promethazine have a more sedative effect than chlorphenamine and
cyclizine (section 4.6). Chlorphenamine is
used as an adjunct to adrenaline (epinephrine) in the
emergency treatment of anaphylaxis and angioedema
(section 3.4.3).
Cautions and contra-indications Antihistamines
should be used with caution in children with epilepsy.
Most antihistamines should be avoided in acute porphyria, but some are thought t
o be safe (see section
9.8.2). Sedating antihistamines have significant antimuscarinic activity they shou
ld not be used in neonates and should be used with caution in children with
urinary retention, glaucoma, or pyloroduodenal
obstruction. Phenothiazine sedating antihistamines,
such as alimemazine and promethazine, should not be
given to children under 2 years, except on specialist
advice, because the safety of such use has not been
established. See also MHRA/CHM advice, p. 166. Interactions: see Appendix 1 (ant
ihistamines).
Hepatic impairme nt Sedating antihistamines
should be avoided in children with severe liver disease increased risk of coma.
Pregnancy Most manufacturers of antihistamines
advise avoiding their use during pregnancy; however
there is no evidence of teratogenicity, except for
hydroxyzine where toxicity has been reported with
high doses in animal studies. The use of sedating antihistamines in the latter p
art of the third trimester may
cause adverse effects in neonates such as irritability,

paradoxical excitability, and tremor.


Breast-feeding Most antihistamines are present in
breast milk in varying amounts; although not known to
be harmful, most manufacturers advise avoiding their
use in mothers who are breast-feeding.
Side-effects Drowsiness is a significant side-effect
with most of the older antihistamines although paradoxical stimulation may occur
rarely in children, especially with high doses. Drowsiness may diminish after a
few days of treatment and is considerably less of a
problem with the newer antihistamines (see also notes
above). Side-effects that are more common with the
older antihistamines include headache, psychomotor
impairment, and antimuscarinic effects such as urinary
retention, dry mouth, blurred vision, and gastro-intestinal disturbances. Other
rare side-effects of antihistamines include hypotension, palpitation, arrhythmia
s,
extrapyramidal effects, dizziness, confusion, depression,
sleep disturbances, tremor, convulsions, hypersensitivity reactions (including b
ronchospasm, angioedema,
anaphylaxis, rashes, and photosensitivity reactions),
blood disorders, and liver dysfunction.
Non-sedating antihistamines
Skilled tasks Although drowsiness is rare, children
and their carers should be advised that it can occur and
may affect performance of skilled tasks (e.g. cycling or
driving); alcohol should be avoided.
ACRIVASTINE
Cautions see notes above
Contra-indications see notes above; also hypersensitivity to triprolidine
Renal impairment avoid in severe impairment
Pregnancy see notes above
Breast-feeding see notes above
Side-effects see notes above
Indications and dose
Symptomatic relief of allergy such as hay fever,
chronic idiopathic urticaria
. By mouth
Child 12 18 years 8 mg 3 times daily
Acrivastine (Non-proprietary)
Capsules, acrivastine 8 mg, net price 12-cap pack =
2.75, 24-cap pack = 4.76. Counselling, skilled
tasks
Brands include Benadryl Allergy Relief
BILASTINE
Cautions see notes above
Contra-indications see notes above
Pregnancy avoid limited information available; see
also notes above
Breast-feeding avoid no information available; see
also notes above
Side-effects headache, malaise; less commonly abdominal pain, diarrhoea, increas
ed appetite, weight gain,
thirst, gastritis, prolongation of the QT interval, dyspnoea, anxiety, insomnia,
vertigo, dizziness, pyrexia,
oral herpes, tinnitus
152 3.4.1 Antihistamines BNFC 2014 2015
3Respiratory syste

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