Theophylline/ Hydroxyethyl Theophylline/ Diphenhydramine/ Ammonium Chloride/ Sodium Citrate

Registered South African indications:

• Bronchospasm associated with bronchial congestion

South African registered contraindications

• Hypersensitivity to the active ingredient or any of the excipients in this combination product
• Premature infants or neonates
• During acute attacks of asthma
• Patients with metabolic or respiratory alkalosis, hypocalcaemia, or hypochlorhydria
• Impaired renal function
• Impaired hepatic function
• Epilepsy
• Not recommended for children under 2 years of age

South African recommendations

• Pregnancy
• Breastfeeding
• Intake of alcohol or other central nervous system depressants
• Fructose intolerance
• Glucose-galactose malabsorption
• Diabetes mellitus (due to sucrose content)
• Peptic ulceration (for theophylline)
• Hyperthyroidism (for theophylline)
• Hypertension (for theophylline)
• Cardiac arrhythmias (for theophylline)
• Cardiovascular disease (for theophylline)
• Congestive heart failure (for theophylline)
• Chronic alcoholism (for theophylline)
• Acute febrile illness (for theophylline)
• Severe hypoxia (for theophylline)
• Cor pulmonale (for theophylline)
• Acute pulmonary oedema (for theophylline)
• Chronic lung disease (for theophylline)
• Neonates and the elderly (for theophylline)
• Narrow angle glaucoma (for diphenhydramine)
• Urinary retention (for diphenhydramine)
• Prostatic hypertrophy (for diphenhydramine)
• Patients receiving corticosteroids (for sodium citrate)
• Congestive heart failure (for sodium citrate)
• Cirrhosis of the liver (for sodium citrate)
• When conducting positive skin tests
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: liq

South African registered indications and dosages

Bronchospasm associated with bronchial congestion
- Bronchial asthma
- Paroxysmal dyspnoea
- Colds
- Bronchitis
- Tracheitis

Theophylline/ Hydroxyethyl Theophylline/ Diphenhydramine/ Ammonium Chloride/ Sodium Citrate
16.667/1.667/6.667/120/50 (mg)

• Oral (liq): 10-15ml, 4hrly

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

South African registered indications and dosages

Bronchospasm associated bronchial congestion
- Bronchial asthma
- Paroxysmal dyspnoea
- Colds
- Bronchitis
- Tracheitis

Theophylline/ Hydroxyethyl Theophylline/ Diphenhydramine/ Ammonium Chloride/ Sodium Citrate
16.667/1.667/6.667/120/50 (mg)

• Younger than 2 years: Contraindicated
• Between 2-6 years: 2.5-5ml, 4hrly
• Between 7-12 years: 5-10ml, 4hrly
• Older than 12 years: See adult dosage

Pregnancy

South African recommendations

• Caution
• Safety and/or efficacy has not been established

Breastfeeding

South African recommendations

• Caution
• Safety and/or efficacy has not been established

South African recommendations

• Contraindicated

South African recommendations

• Contraindicated

South African recommendations

• Caution; no dose adjustment recommended

Combination products may have additional pharmacological effects not accounted for by the action of the individual ingredients

Diphenhydramine Hydrochloride

Central Nervous System

• Sedation, from slight drowsiness to deep sleep
• Lassitude
• Dizziness
• Incoordination
• Paradoxical CNS stimulation, including insomnia, nervousness, tachycardia, tremors, and convulsions (particularly in children)
• Epileptiform seizures (in patients with focal lesions of the cerebral cortex)
• Muscular weakness
• Tinnitus
• Euphoria
• Headache

Gastrointestinal System

• Nausea
• Vomiting
• Diarrhoea
• Constipation
• Anorexia
• Increased appetite
• Epigastric pain

Antimuscarinic Effects

• Blurred vision
• Difficulty in micturition
• Dysuria
• Dryness of the mouth
• Tightness of the chest

Other Systems

• Hypotension
• Thrombocytopenia

Ammonium Chloride

Gastrointestinal System

• Nausea
• Vomiting

• Other xanthines
• Allopurinol
• Cimetidine
• Influenza vaccine
• Propranolol
• Erythromycin
• Macrolides
• Phenytoin
• Anticonvulsants
• Monoamine oxidase inhibitors
• Other antihistamines
• Other anti-muscarinic agents
• Central nervous system depressants
• Alcohol
• Barbiturates
• Hypnotics
• Narcotic analgesics
• Sedatives
• Tranquillisers
• Atropine
• Tricyclic antidepressants
• Drugs causing cross-sensitivity reactions

Other interactions

• Cigarette smoking

None routine

Theophylline 
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 predominently as a bronchodilator and vasodilator

Hydroxyethyl theophylline
Hydroxyethyl theophylline is a N-7 substituted theophylline derivative which acts similar to other xanthines. The bronchodilating action of xanthines is thought to result from the competitive inhibition of phosphodiesterase, which is the enzyme responsible for the breakdown cyclic AMP in smooth muscle cells

Diphenhydramine
Diphenhydramine is a histamine H1- receptor antagonist that competes with free histamine for binding at histamine receptors. In addition to its usual anti-allergy actions, it also has significant sedative and antimuscarinic properties

Ammonium chloride
Ammonium chloride is used as an expectorant. It causes irritation of the bronchial mucosa, which results in the production of excess respiratory tract fluid. This allows for easier mucus expulsion due to its decreased viscosity

Sodium citrate 
Sodium citrate is metabolized to sodium bicarbonate and acts as a systemic alkalizer  

COMBINATION PREPARATIONS

Theophylline/ Hydroxyethyl Theophylline/ Diphenhydramine/ Ammonium Chloride/ Sodium Citrate

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

• Alcophyllex (Adcock Ingram) originator