Drug reference

Aminophylline

BNF 80 (2020–2021)

Source: BNF 80 (2020–2021)
PDF pages: 309, 310

Review source pages for extracted sections and age labels. BNF dose snippets show only their first line.

Overview

Indications And Dose

Severe acute asthma in patients not previously treated with theophylline ▶BY SLOW INTRAVENOUS INJECTION ▶Child: 5 mg/kg (max. per dose 500 mg), to be followed by intravenous infusion ▶Adult: 250–500 mg (max. per dose 5 mg/kg), to be followed by intravenous infusion Severe acute asthma ▶BY INTRAVENOUS INFUSION ▶Child 1 month–11 years: 1 mg/kg/hour, adjusted according to plasma-theophylline concentration ▶Child 12–17 years: 500–700 micrograms/kg/hour, adjusted according to plasma-theophylline concentration ▶Adult: 500–700 micrograms/kg/hour, adjusted according to plasma-theophylline concentration ▶Elderly: 300 micrograms/kg/hour, adjusted according to plasma-theophylline concentration Severe acute exacerbation of chronic obstructive pulmonary disease in patients not previously treated with theophylline ▶BY SLOW INTRAVENOUS INJECTION ▶Adult: 250–500 mg (max. per dose 5 mg/kg), to be Respiratory system followed by intravenous infusion Severe acute exacerbation of chronic obstructive pulmonary disease ▶BY INTRAVENOUS INFUSION ▶Adult: 500–700 micrograms/kg/hour, adjusted according to plasma-theophylline concentration ▶Elderly: 300 micrograms/kg/hour, adjusted according to plasma-theophylline concentration Chronic asthma ▶BY MOUTH USING MODIFIED-RELEASE MEDICINES ▶Child (body-weight 40 kg and above): Initially 225 mg twice daily for 1 week, then increased if necessary to 450 mg twice daily, adjusted according to plasma- theophylline concentration Reversible airway obstruction ▶BY MOUTH USING MODIFIED-RELEASE MEDICINES ▶Adult (body-weight 40 kg and above): Initially 225 mg twice daily for 1 week, then increased if necessary to 450 mg twice daily, adjusted according to plasma- theophylline concentration

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Dose Adjustments

DUE TO INTERACTIONS ▶Dose adjustment may be necessary if smoking started or stopped during treatment. DOSES AT EXTREMES OF BODY-WEIGHT ▶To avoid excessive dosage in obese patients, dose should be calculated on the basis of ideal weight for height.

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Pharmacokinetics

▶Aminophylline is a stable mixture or combination of theophylline and ethylenediamine; the ethylenediamine confers greater solubility in water. ▶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 aminophylline are important because the toxic dose is close to the therapeutic dose. PHYLLOCONTIN CONTINUS ® FORTE Reversible airways obstruction ▶BY MOUTH USING MODIFIED-RELEASE MEDICINES ▶Adult: Initially 350 mg twice daily for 1 week, then increased if necessary to 700 mg twice daily, increase dose according to plasma-theophylline concentration l UNLICENSED USE ▶In children Aminophylline injection not licensed for use in children under 6 months.

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Cautions

Arrhythmias following rapid intravenous injection. cardiac arrhythmias or other cardiac disease. elderly (increased plasma-theophylline concentration). epilepsy. fever. hypertension. peptic ulcer. risk of hypokalaemia. thyroid disorder

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Allergy And Cross Sensitivity

Allergy to ethylenediamine can cause urticaria, erythema, and exfoliative dermatitis.

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Prescribing And Dispensing Information

Patients taking oral theophylline or aminophylline should not normally receive a loading dose of intravenous aminophylline. Consider intravenous aminophylline for treatment of severe and life-threatening acute asthma only after consultation with senior medical staff. Modified release The rate of absorption from modiﬁed- release preparations can vary between brands. If a prescription for a modiﬁed-release oral aminophylline 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. PHYLLOCONTIN CONTINUS ® FORTE ▶With oral use Phyllocontin Continus ® Forte tablets are for smokers and other patients where theophylline half-life is shorter.

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Safety

Interactions

→Appendix 1: aminophylline

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Side Effects

GENERAL SIDE-EFFECTS Headache. nausea. palpitations. seizure (more common when given too rapidly by intravenous injection) SPECIFIC SIDE-EFFECTS ▶With intravenous use Abdominal pain. anxiety. arrhythmia (more common when given too rapidly by intravenous injection). confusion. delirium. diarrhoea. dizziness. electrolyte imbalance. gastrointestinal haemorrhage. gastrooesophageal reﬂux disease. hyperthermia. hyperventilation. hypotension (more common when given too rapidly by intravenous injection). insomnia. mania. metabolic disorder. pain. skin reactions. tachycardia (more common when given too rapidly by intravenous injection). thirst. tremor. vertigo. visual impairment. vomiting Respiratory system ▶With oral use Arrhythmias. central nervous system stimulation. epigastric discomfort SIDE-EFFECTS, FURTHER INFORMATION Potentially serious hypokalaemia may result from beta2-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. Overdose Theophylline and related drugs are often prescribed as modiﬁed-release formulations and toxicity can therefore be delayed. They 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 speciﬁc details on the management of poisoning, see Theophylline, under Emergency treatment of poisoning p. 1430.

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Pregnancy

Neonatal 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.

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Breast Feeding

Present in milk—irritability in infant reported; modiﬁed-release preparations preferable. Theophylline can be taken as normal during breast- feeding.

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Hepatic Impairment

Manufacturer advises caution (risk of reduced clearance). Dose adjustments ▶With oral use Manufacturer advises consider dose reduction. ▶With intravenous use Manufacturer advises maintenance dose reduction—consult product literature.

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Monitoring Requirements

▶Aminophylline is monitored therapeutically in terms of plasma-theophylline concentrations. ▶Measurement of plasma-theophylline concentration may be helpful and is essential if a loading dose of intravenous aminophylline is to be given to patients who are already taking theophylline, because serious side-effects such as convulsions and arrhythmias can occasionally precede other symptoms of toxicity. ▶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. ▶If aminophylline is given intravenously, a blood sample should be taken 4–6 hours after starting treatment. ▶With oral use 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).

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Dose and formulations

Directions For Administration

▶With intravenous use For intravenous injection, give very slowly over at least 20 minutes (with close monitoring). ▶With intravenous use in children For intravenous infusion, dilute to a concentration of 1 mg/mL with Glucose 5% or Sodium Chloride 0.9%. ▶With intravenous use in adults For intravenous infusion, give continuously in Glucose 5% or Sodium Chloride 0.9%. ▶With intramuscular use Aminophylline is too irritant for intramuscular use.

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Medicinal Forms

There can be variation in the licensing of different medicines containing the same drug. Forms available from special-order manufacturers include: solution for infusion Solution for injection ▶Aminophylline (Non-proprietary) Aminophylline 25 mg per 1 ml Aminophylline 250mg/10ml solution for injection ampoules | 10 ampoule P £8.50 DT = £8.50 Modified-release tablet CAUTIONARY AND ADVISORY LABELS 25 ▶Phyllocontin Continus (Napp Pharmaceuticals Ltd) Aminophylline hydrate 225 mg Phyllocontin Continus 225mg tablets | 56 tablet p £2.40 DT = £2.40 Aminophylline hydrate 350 mg Phyllocontin Forte Continus 350mg tablets | 56 tablet p £4.22 DT = £4.22

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Dose text by age group

Child

5 mg/kg (max. per dose 500 mg), to be followed

First-line fragment. Read the complete Indications and Dose section above.

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Child 1 month–11 years

1 mg/kg/hour, adjusted

First-line fragment. Read the complete Indications and Dose section above.

PDF page 309

Child 12–17 years

500–700 micrograms/kg/hour,

First-line fragment. Read the complete Indications and Dose section above.

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Child (body-weight 40 kg and above)

Initially 225 mg

First-line fragment. Read the complete Indications and Dose section above.

PDF page 309

Age labels are extracted for navigation. Check the complete source section and current local guidance before clinical use.

Drug reference

Aminophylline

BNF 80 (2020–2021)

Source: BNF 80 (2020–2021)
PDF pages: 309, 310

Review source pages for extracted sections and age labels. BNF dose snippets show only their first line.

Overview

Indications And Dose

PDF page 309

Dose Adjustments

PDF page 309

Pharmacokinetics

PDF page 309

Cautions

PDF page 309

Allergy And Cross Sensitivity

Allergy to ethylenediamine can cause urticaria, erythema, and exfoliative dermatitis.

PDF page 310

Prescribing And Dispensing Information

PDF page 310

Safety

Interactions

→Appendix 1: aminophylline

PDF page 309

Side Effects

PDF pages 309, 310

Pregnancy

Neonatal 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.

PDF page 310

Breast Feeding

Present in milk—irritability in infant reported; modiﬁed-release preparations preferable. Theophylline can be taken as normal during breast- feeding.

PDF page 310

Hepatic Impairment

PDF page 310

Monitoring Requirements

PDF page 310

Dose and formulations

Directions For Administration

PDF page 310

Medicinal Forms

PDF page 310

Dose text by age group

Child

5 mg/kg (max. per dose 500 mg), to be followed

First-line fragment. Read the complete Indications and Dose section above.

PDF page 309

Child 1 month–11 years

1 mg/kg/hour, adjusted

First-line fragment. Read the complete Indications and Dose section above.

PDF page 309

Child 12–17 years

500–700 micrograms/kg/hour,

First-line fragment. Read the complete Indications and Dose section above.

PDF page 309

Child (body-weight 40 kg and above)

Initially 225 mg

First-line fragment. Read the complete Indications and Dose section above.

PDF page 309

Age labels are extracted for navigation. Check the complete source section and current local guidance before clinical use.