INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo AMINOPHYLLIN® 500 SUPPOSICONES
AMINOPHYLLlN® 250 mg/l0 mL INJECTION
AMINOPHYLLIN® 500 mg/2 mL INJECTION
SCHEDULING STATUS:
Ampoules S4
Supposicones S1

PROPRIETARY NAME
(and dosage form):

AMINOPHYLLIN® 500 SUPPOSICONES
AMINOPHYLLlN® 250 mg/l0 mL INJECTION
AMINOPHYLLIN® 500 mg/2 mL INJECTION

COMPOSITION:
AMINOPHYLLIN 500 SUPPOSICONES contain 500 mg aminophylline with 60 mg benzocaine
AMINOPHYLLIN 250 mg/10 mL INJECTION contains 250 mg aminophylline dihydrate in 10 mL
AMINOPHYLLIN 500 mg/2 mL INJECTION contains 500 mg aminophylline dihydrate in 2 mL. Contains 2% benzyl alcohol.

PHARMACOLOGICAL CLASSIFICATION:
A 10.2 Bronchodilators

PHARMACOLOGICAL ACTION :
Aminophylline is a soluble complex containing approximately 85% theophylline and 15% ethylenediamine. Aminophylline directly relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels, thus acting mainly as a bronchodilator, pulmonary vasodilator and smooth muscle relaxant.

INDICATIONS:
AMINOPHYLLIN is indicated for relief of acute bronchial asthma and reversible bronchospasm associated with chronic bronchitis and emphysema, and in status asthmaticus; congestive heart failure; Cheyne-Stokes respiration; reduction of coughing, expectoration and exertional dyspnoea in emphysema patients, and for cardiac paroxysmal dyspnoea.

AMINOPHYLLIN SUPPOSICONES are intended for use in conditions requiring less urgent and more prolonged administration. AMINOPHYLLIN INJECTIONS are primarily for use in emergency situations.

CONTRA-INDICATIONS:
AMINOPHYLLIN should not be given to patients with active peptic ulcers, since it may increase the volume and acidity of gastric secretions. Patients with a history of hypersensitivity to aminophylline or theophylline should not be treated with AMINOPHYLLIN. Do not administer AMINOPHYLLIN with other xanthine preparations. Safe use of AMINOPHYLLIN in pregnancy has not been established.

DOSAGE AND DIRECTIONS FOR USE:
Supposicones:
Adults: One 500 mg supposicone once or twice daily.
Children: Use of the 500 mg supposicone is not recommended.
Supposicones must be removed from Rotoplast shells before use.

Ampoules:
250 mg/10 mL (Intravenous):
For intravenous administration, AMINOPHYLLIN is supplied in ampoules of 10 mL (250 mg) in aqueous solution.
Adults: 250 mg or 500 mg as required.
Children: The dose is proportionally smaller and is based upon the child’s age and body weight.

Note: AMINOPHYLLIN should be injected slowly, at a rate of 1 mL per minute. Too-rapid intravenous administration may have transient hypotensive effects.

500 mg/2 mL (intramuscular):
For intramuscular administration, AMINOPHYLLIN is supplied in ampoules of 2 mL (500 mg) in aqueous solution with 2% of benzyl alcohol.
Adults: 500 mg as required.
Children: The dose is proportionally smaller and is based upon the child’s age and body weight.

Note: The intramuscular administration of AMINOPHYLLIN is painful. The pain may last for several hours.

Therapeutic serum levels are considered to be between 10 mcg/mL and 20 mcg/mL. Levels above 20 mcg/mL may produce toxic effects.
Do not exceed the recommended dosage.

SIDE EFFECTS AND SPECIAL PRECAUTIONS:
Precautions:
Some children may be unusually sensitive to AMINOPHYLLIN.
Administration of ephedrine or other sympathomimetic drugs to patients already on treatment with AMINOPHYLLIN may result in toxic synergism.
Use with caution in patients with severe cardiac disease, hypertension, hyperthyroidism, acute myocardial injury, cor pulmonale, severe hypoxemia, hepatic impairment, or alcoholism, and in the elderly (especially males) and in neonates. Particular caution in dose administration must be exercised in patients with a history of peptic ulcer since the condition may be exacerbated. Caution should be used in giving aminophylline to patients in congestive heart failure. Serum levels in such patients may persist for long periods following discontinuation of the medicine. Theophylline half-life is shorter in smokers than non-smokers; therefore, smokers may require larger or more frequent doses.

Aminophylline may lower the seizure threshold.

Elevated serum levels of theophylline may occur in patients treated concomitantly with aminophylline and cimetidine, troleandomycin, erythromycin, allopurinol, or oral contraceptive steroids. Co-medication with phenobarbitone, phenytoin, or rifampicin may increase theophylline clearance and an increase of the aminophylline dose may be required. The excretion of lithium carbonate is increased in patients receiving aminophylline.

Consumption of coffee, tea, cola beverages, chocolate, or paracetamol contributes to falsely high serum theophylline levels when theophylline is measured spectrophotometrically without previous isolation by chromatography.

SIDE-EFFECTS:
The most consistent adverse reactions observed with therapeutic amounts of aminophylline are:
1. Gastrointestinal: nausea, vomiting, anorexia, bitter aftertaste, dyspepsia, heavy feeling in the stomach, and gastrointestinal distress.
2. Central nervous system: dizziness, vertigo, light-headedness, headache, nervousness, insomnia, and agitation.
3. Cardiovascular: palpitation, tachycardia, flushing, extrasystoles and cardiac rhythm disturbances.
4. Respiratory: increase in respiratory rate.
5. Dermatologic: urticaria.
Proctitis may follow the repeated administration of aminophylline suppositories. The benzocaine in the suppositories may cause local irritation.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
The most consistent reactions observed with toxic overdoses of aminophylline are:
1. Gastrointestinal: nausea, vomiting, epigastric pain, haematemesis and diarrhoea.
2. Central nervous system: in addition to those cited above, the patient may exhibit hyperreflexia, fasciculations, and clonic and tonic convulsions. These are especially prone to occur in cases of overdosage in infants and small children.
3. Cardiovascular: in addition to those outlined above, marked hypotension and circulatory failure may be manifest.
4. Respiratory: tachypnoea and respiratory arrest may occur.
5. Renal: Increased excretion of renal tubular cells has been observed.
Management of Toxic Symptoms:
1. Discontinue drug immediately.
2. There is no known specific antidote.
3. Gastric lavage.
4. Emetic medication may be of value.
5. Avoid administration of sympathomimetic drugs.
6. Intravenous fluids, oxygen, and other supportive measures to prevent hypotension and overcome dehydration.
7. Central nervous system stimulation and seizures may respond to short-acting barbiturates.
8. Monitor serum levels until below 20 mcg/mL.

IDENTIFICATION:
AMINOPHYLLIN 500 SUPPOSICONES: white opaque wax suppositories.
AMINOPHYLLIN 250 mg/10 mL INJECTION: clear glass ampoules containing a clear, colourless to slightly yellow liquid.
AMINOPHYLLIN 500 mg/2 mL INJECTION: clear glass ampoules containing a clear colourless to slightly yellow liquid.

PRESENTATION:
AMINOPHYLLIN 500 SUPPOSICONES: boxes containing 10 suppositories
AMINOPHYLLIN 250 mg/10 mL INJECTION: boxes containing 5 ampoules
AMINOPHYLLIN 500 mg/2 mL INJECTION: boxes containing 6 ampoules

STORAGE INSTRUCTIONS:
Store in a cool dry place (below 25°C) away from light.
Keep out of reach of children.

REFERENCE NUMBERS:
AMINOPHYLLIN 500 SUPPOSICONES: G1275 (Act l01/1965)
AMINOPHYLLIN 250 mg/10 mL INJECTION: G1271 (Act 101/1965)
AMINOPHYLLIN 500 mg/2 mL INJECTION: G1270 (Act 101/1965)

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
G.D. Searle (South Africa) (Pty) Ltd
14 Mandy Road
Reuven
Johannesburg

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
1 July 1974

® 1994, G.D. Searle (South Africa) (Pty) Ltd

Rosside 22133
Code 4045 (IMA-7888 (R4))-8-9/94

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