Theophylline
lINDICATIONS AND DOSE
NUELIN SA®175MG TABLETS
Chronic asthma
▶BY MOUTH USING MODIFIED-RELEASE MEDICINES
▶Child 6–11 years: 175 mg every 12 hours
▶Child 12–17 years: 175 – 350 mg every 12 hours
NUELIN SA®250 TABLETS
Chronic asthma
▶BY MOUTH USING MODIFIED-RELEASE MEDICINES
▶Child 6–11 years: 125 – 250 mg every 12 hours
▶Child 12–17 years: 250 – 500 mg every 12 hours
SLO-PHYLLIN®
Chronic asthma
▶BY MOUTH USING MODIFIED-RELEASE MEDICINES
▶Child 6 months–1 year: 12 mg/kg every 12 hours (max.
per dose 120 mg)
▶Child 2–5 years: 60 – 120 mg every 12 hours
▶Child 6–11 years: 125 – 250 mg every 12 hours
▶Child 12–17 years: 250 – 500 mg every 12 hours
UNIPHYLLIN CONTINUS®
Chronic asthma
▶BY MOUTH USING MODIFIED-RELEASE MEDICINES
▶Child 2–11 years: 9 mg/kg every 12 hours (max. per dose
200 mg), dose may be increased in some children with
chronic asthma; increased to 10 – 16 mg/kg every
12 hours (max. per dose 400 mg), may be appropriate to
give larger evening or morning dose to achieve
optimum therapeutic effect when symptoms most
severe; in patients whose night or daytime symptoms
persist despite other therapy, who are not currently
receiving theophylline, total daily requirement may be
added as single evening or morning dose
▶Child 12–17 years: 200 mg every 12 hours, adjusted
according to response to 400 mg every 12 hours, may
be appropriate to give larger evening or morning dose
to achieve optimum therapeutic effect when symptoms
most severe; in patients whose night or daytime
symptoms persist despite other therapy, who are not
currently receiving theophylline, total daily
requirement may be added as single evening or
morning dose
DOSE ADJUSTMENTS DUE TO INTERACTIONS
▶Dose adjustment may be necessary if smoking started
or stopped during treatment.
PHARMACOKINETICS
▶Theophylline is metabolised in the liver. The plasma-
theophylline concentration is increased in heart
failure, hepatic impairment, and in viral infections.
The plasma-theophylline concentration is decreased in
smokers, and by alcohol consumption. Differences in
the half-life of theophylline are important because the
toxic dose is close to the therapeutic dose.lUNLICENSED USESlo-phyllin®capsules not licensed for
use in children under 2 years.
lCAUTIONSCardiac arrhythmias or other cardiac disease.
epilepsy.fever.hypertension.hyperthyroidism.peptic
ulcer.risk of hypokalaemia
lINTERACTIONS→Appendix 1 : theophylline
lSIDE-EFFECTSAnxiety.arrhythmias.diarrhoea.dizziness
.gastrointestinal discomfort.gastrooesophageal reflux
disease.headache.hyperuricaemia.nausea.palpitations.
seizure.skin reactions.sleep disorders.tremor.urinary
disorders.vomiting
SIDE-EFFECTS, FURTHER INFORMATIONPotentially serious
hypokalaemia may result from beta 2 -agonist therapy.
Particular caution is required in severe asthma, because
this effect may be potentiated by concomitant treatment
with theophylline and its derivatives, corticosteroids, and
diuretics, and by hypoxia. Plasma-potassium
concentration should therefore be monitored in severe
asthma.
OverdoseTheophylline in overdose can cause vomiting
(which may be severe and intractable), agitation,
restlessness, dilated pupils, sinus tachycardia, and
hyperglycaemia. More serious effects are haematemesis,
convulsions, and supraventricular and ventricular
arrhythmias. Severe hypokalaemia may develop rapidly.
For details on the management of poisoning, see
Theophylline, under Emergency treatment of poisoning
p. 832.
lPREGNANCYNeonatal irritability and apnoea have been
reported. Theophylline can be taken as normal during
pregnancy as it is particularly important that asthma
should be well controlled during pregnancy.
lBREAST FEEDINGPresent in milk—irritability in infant
reported; modified-release preparations preferable.
Theophylline can be taken as normal during breast-
feeding.
lHEPATIC IMPAIRMENT
Dose adjustmentsReduce dose.
lMONITORING REQUIREMENTS
▶In most individuals, a plasma-theophylline concentration
of 10 – 20 mg/litre ( 55 – 110 micromol/litre) is required for
satisfactory bronchodilation, although a lower plasma-
theophylline concentration of 5 – 15 mg/litre may be
effective. Adverse effects can occur within the range
10 – 20 mg/litre and both the frequency and severity
increase at concentrations above 20 mg/litre.
▶Plasma-theophylline concentration is measured 5 days
after starting oral treatment and at least 3 days after any
dose adjustment. A blood sample should usually be taken
4 – 6 hours after an oral dose of a modified-release
preparation (sampling times may vary—consult local
guidelines).
lDIRECTIONS FOR ADMINISTRATION
SLO-PHYLLIN®Contents of the capsule (enteric-coated
granules) may be sprinkled on to a spoonful of soft food
(e.g. yoghurt) and swallowed without chewing.
lPRESCRIBING AND DISPENSING INFORMATIONThe rate of
absorption from modified-release preparations can vary
between brands. If a prescription for a modified-release
oral theophylline preparation does not specify a brand
name, the pharmacist should contact the prescriber and
agree the brand to be dispensed. Additionally, it is
essential that a patient discharged from hospital should be
maintained on the brand on which that patient was
stabilised as an in-patient.
lPATIENT AND CARER ADVICE
SLO-PHYLLIN®Patient or carer should be given advice on
how to administer theophylline modified release capsules.lMEDICINAL FORMS
There can be variation in the licensing of different medicines
containing the same drug.
Modified-release tablet
CAUTIONARY AND ADVISORY LABELS21, 25
▶Nuelin SA(Meda Pharmaceuticals Ltd)
Theophylline 175 mgNuelin SA 175 mg tablets| 60 tabletp£ 6. 38
DT = £ 6. 38
Theophylline 250 mgNuelin SA 250 tablets| 60 tabletp£ 8. 92 DT
=£ 8. 92
▶Uniphyllin Continus(Napp Pharmaceuticals Ltd)
Theophylline 200 mgUniphyllin Continus 200 mg tablets|
56 tabletp£ 2. 96 DT = £ 2. 96
Theophylline 300 mgUniphyllin Continus 300 mg tablets|
56 tabletp£ 4. 77 DT = £ 4. 77
Theophylline 400 mgUniphyllin Continus 400 mg tablets|
56 tabletp£ 5. 65 DT = £ 5. 65BNFC 2018 – 2019 Airways disease, obstructive 169
Respiratory system3