page211
ZAFIRLUKAST
Indications
prophylaxis of asthma,
see notes above
and Management of Chronic Asthma table,
p.
172
Cautions
elderly;
interactions: Appendix 1 (leuko-
triene receptor antagonists)
Hepatic disorders
Patients 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 in
moderate to severe impairment
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,
respir-
atory infections,
headache,
insomnia, malaise;
rarely
bleeding disorders,
hypersensitivity reactions includ-
ing angioedema and skin reactions,
arthralgia,
myal-
gia,
hepatitis,
hyperbilirubinaemia,
thrombocytope-
nia;
very rarely
Churg-Strauss syndrome (see notes
above), agranulocytosis
Dose
.
ADULT
and
CHILD
over 12 years,
20 mg twice daily
Accolate
c
(AstraZeneca) A
Tablets
, f/c, zafirlukast 20 mg, net price 56-tab pack =
£17.75.
Label:
23
3.3.3
Phosphodiesterase type-
4 inhibitors
Roflumilast
is
a phosphodiesterase type-4 inhibitor
with anti-inflammatory properties;
it
is licensed as an
adjunct
to bronchodilators for the maintenance treat-
ment of patients with severe chronic obstructive pulm-
onary disease associated with chronic bronchitis and a
history of frequent exacerbations.
ROFLUMILAST
Indications
see notes above
Cautions
monitor body-weight;
latent infection (such
as tuberculosis,
viral hepatitis,
herpes infection);
moderate to severe cardiac failure;
history of psy-
chiatric illness,
or concomitant use of drugs likely to
cause psychiatric events;
interactions: Appendix 1
(roflumilast)
Contra-indications
severe immunological disease;
severe acute infectious disease;
cancer (except basal
cell carcinoma);
concomitant treatment with immu-
nosuppressive drugs (except short-term systemic
corticosteroids)
Hepatic impairment
caution in mild impairment;
avoid in moderate to severe impairment
Pregnancy
manufacturer advises avoid—toxicity in
animal
studies;
women of child-bearing age should
use effective contraception
Breast-feeding
manufacturer advises avoid—present
in milk in
animal
studies
Side-effects
diarrhoea,
nausea,
abdominal pain,
weight loss,
decreased appetite,
headache,
insomnia;
less commonly
gastritis, vomiting, gastro-oesophageal
reflux, dyspepsia, palpitation, anxiety, tremor, vertigo,
dizziness, malaise, muscle spasm, myalgia, back pain,
rash;
rarely
taste disturbances,
haematochezia,
con-
stipation,
respiratory tract infections,
depression,
nervousness, suicidal ideation, gynaecomastia, raised
creatine kinase,
urticaria
Dose
.
ADULT
over 18 years, 500 micrograms once daily
Daxas
c
(MSD) T A
Tablets
,
yellow,
f/c,
roflumilast 500 micrograms,
net
price 30-tab pack = £37.71,
90-tab pack = £113.14.
Counselling,
patient card
Counselling
Patients should be given a patient card before starting
treatment and advised to record body-weight at regular intervals
3.4
Antihistamines,
hyposensitisation, and
allergic emergencies
3.4.1 Antihistamines
3.4.2 Allergen Immunotherapy
3.4.3 Allergic emergencies
3.4.1
Antihistamines
All antihistamines are of potential value in the treatment
of
nasal
allergies,
particularly seasonal
allergic rhinitis
(hay fever), and they may be of some value in vasomotor
rhinitis.
They reduce rhinorrhoea and sneezing but are
usually less
effective for
nasal
congestion.
Antihist-
amines are used topically in the eye (section 11.4.2),
in the nose (section 12.2.1),
and on the skin (section
13.3).
Oral antihistamines are also of some value in preventing
urticaria and are used to treat urticarial rashes, pruritus,
and insect bites and stings;
they are also used in drug
allergies. Injections of chlorphenamine or promethazine
are used as an adjunct to adrenaline (epinephrine) in the
emergency treatment
of
anaphylaxis and angioedema
(section 3.4.3).
For the use of antihistamines (including
cinnarizine,
cyclizine,
and promethazine teoclate)
in
nausea
and vomiting,
see
section 4.6.
Buclizine
is
included as an anti-emetic in a preparation for migraine
(section 4.7.4.1).
For
reference to the use of
antihist-
amines for occasional insomnia, see section 4.1.1.
All
older antihistamines cause sedation but
alimema-
zine and promethazine may be more sedating whereas
chlorphenamine and cyclizine (section 4.6)
may be
less so.
This sedating activity is sometimes used to
manage the pruritus
associated with some allergies.
There is little evidence that any one of the older, ‘sedat-
ing’
antihistamines is superior to another and patients
vary widely in their response.
Non-sedating antihistamines such as acrivastine, cetir-
izine,
desloratadine (an active metabolite of
lorat-
adine),
fexofenadine (an active metabolite of
terfen-
adine),
levocetirizine
(an
isomer
of
cetirizine),
loratadine,
mizolastine,
and rupatadine cause less
sedation and psychomotor impairment
than the older
BNF 61
3.3.3 Phosphodiesterase type-4 inhibitors
191
3
Respiratory system