Theophylline

Registered South African indications:

• Asthma
• Chronic obstructive pulmonary disease

Contraindications

• Hypersensitivity to the active ingredient and any of its excipients
• Acute porphyria
• Children (tablet)
• Coadministration with ephedrine in children

Cautions

• Pregnancy
• Breastfeeding
• Hepatic impairment
• Elderly
• Cardiac arrhythmias
• Acute myocardial infarction
• Congestive cardiac failure
• Peptic ulcer disease
• Hyperthyroidism
• Severe hypertension
• Chronic alcoholism
• Chronic lung disease
• Acute febrile illnesses

Forms avail. in SA and covered in this monograph: tab; SR tab, syr

Asthma
Chronic obstructive pulmonary disease

• Oral (tab): 100-300mg, 6hrly; Max: 600mg/24hrs
• Oral (SR tab): 200-500mg, 12hrly; Max: 600mg/24hrs
• Oral (syr): 80-160mg, 8hrly

---

Tablets may be halved but not crushed or chewed

Paed. forms avail. in SA and covered in this monograph: syr

Apnoea of prematurity 

• Oral (syr): Maintenance: 1.5-2mg/kg, 6-8hrly

---

Drug levels should be measured at 0.5–1hr after each IV dose and every 1-2hrs after each oral dose

---

Asthma

Between 2-6 years

• Oral (syr): 13-53mg, 8hrly

Between 7-12 years

• Oral (syr): 53-80mg, 8hrly

Older than 12 years

• See adult dosage

Pregnancy

• Caution
• There are no adequate data from well-controlled studies of the use of theophylline in pregnant women. Theophylline has been reported to give rise to teratogenic effects in mice, rats and rabbits. The potential risk for humans is unknown. Theophylline should not be administered during pregnancy unless clearly necessary

Breastfeeding

• Caution
• Theophylline is secreted in breast milk and may be associated with irritability in the infant, therefore it should only be given to breastfeeding women when the anticipated benefits outweigh the risk to the child

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• Caution; dose adjustment recommended
  Max: 400mg/24hrs

Elderly

• Caution, dose adjustment recommended
  Max: 400mg/24hrs

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Confusion
• Restlessness
• Hyperventilation
• Vertigo
• Tremor
• Seizures
• Anxiety
• Insomnia
• Mania
• Delirium

Cardiovascular Disorders

• Palpitations
• Tachycardia
• Cardiac arrhythmias
• Hypotension

Gastrointestinal Disorders

• Nausea and vomiting
• Abdominal pain
• Diarrhoea
• Gastro-oesophageal reflux
• Gastrointestinal bleeding

Endocrine and Metabolic Disorders

• Hypokalaemia
• Hypophosphataemia
• Hyponatraemia 
• Extreme thirst 
• Hyperthermia

Skin and Subcutaneous Tissue Disorders

• Maculopapular rash
• Erythema
• Pruritus
• Urticaria
• Exfoliative dermatitis

Sensory Disorders

• Visual disturbances

• Xanthine derivatives
• Beta-2 agonists
• Steroids
• Diuretics
• Allopurinol
• Cimetidine
• Influenza vaccine
• Propranolol
• Macrolide antibiotics
• Lithium
• St John's wort
• Ketamine
• Beta blockers  
• Doxapram
• CYP450 inducers

None routine. Specific cases may require

• Theophylline levels (*see additional prescribing points)

Tablet 200mg - EML (Primary)

Tablet 300mg - EML (Non-EML) 

---

Check theophylline levels if patient has any symptoms suggestive of theophylline toxicity e.g. tachycardia and gastrointestinal disturbances.

Levels should also be checked if medications known to reduce clearance of theophylline are commenced.

Theophylline is a phosphodiesterase inhibitor which results in smooth muscle relaxation, diuresis, cardiac stimulation, cerebral stimulation and skeletal muscle stimulation. Through its ability to bring about smooth muscle relaxation, theophylline acts predominantly as a bronchodilator and vasodilator.

Tablet 100mg

• Norstan-Theophylline and Ethylenediamine (Pharmacare)

Tablet 200mg

• Norstan-Theophylline and Ethylenediamine (Pharmacare)
• Sandoz Theophylline Anhydrous 200 (Sandoz)

Tablet 250mg

• Nuelin SA (iNova) originator

Tablet 300mg

• Sandoz Theophylline Anhydrous 300 (Sandoz)

Tablet srt 200mg

• Theoplus (Takeda) originator

Tablet srt 225mg

• Phyllocontin (Pharmafrica)

Tablet srt 250mg

• Euphyllin Retard (Takeda) originator

Tablet srt 300mg

• Theoplus (Takeda) originator
• Adco Pulmophyllin Sr 300 (Adcock)

Tablet srt 400mg

• Uniphyl 400mg (Mundipharma)

Tablet srt 600mg

• Uniphyl 600mg (Mundipharma)

Capsule 100mg

• Genasma (Alliance) originator

Syrup (per 5ml) 26.667mg

• Alcophyllin (Adcock) originator

Syrup (per 5ml) 25mg

• Nuelin Liquid (iNova) originator

Syrup (per 10ml) 25.2mg

• Diphenamill (Dezzo) originator

Also available in injection.

COMBINATION PREPARATIONS

Theophylline/ Ammonium chloride/ Diphenylpyraline hydrochloride/ B-Hydroxyethyl theophylline

Syrup (per 5ml) 50mg/360mg/4mg/5mg

• Theophen Compound Elixir (Pharmacare)

Theophylline/ Hydroxyethyl theophylline/ Diphenhydramine hcl/ Ammonium chloride/ Sodium chloride

Syrup (per 5ml) 16.667mg/1.667mg/6.667mg/120mg/50mg

• Alcophyllex (Adcock) originator

Theophylline/ Etofylline nicotinate

Syrup (per 15ml) 80mg/10mg

• Theophen (Pharmacare)
• Solphyllin (Adcock) originator

Ammonium chloride/ Diphenhydramine hcl/ Menthol/ Sodium citrate/ Theophylline

Syrup (per 10ml) 273.86mg/28.15mg/2.28mg/113.85mg/56.31mg

• Diatussin Syrup (Adcock) originator

Ammonium chloride/ Diphenhydramine hcl/ Etofylline/ Theophylline

Syrup (per 15ml) 360mg/4mg/2.28mg/113.85mg/50mg

• Dynalex Elixir (Pharmacare)

Ammonium chloride/ Diphenhydramine hcl/ Etofylline/ Sodium citrate/ Theophylline

Syrup (per 30ml) 720mg/8mg/10mg/300mg/100mg

• Actophlem Cough syrup (Adcock)
• Solphyllex (Adcock) originator

Codeine/ Mepyramine/ Theophylline

Syrup (per 15ml) 8.45mg/15.84mg/52.8mg

• Adco-Metaxol (Adcock) originator