Aminophylline IV Injection 125 mg/5 ml

Description

Indications
Aminophylline is indicated for the treatment and prophylaxis of bronchospasm associated with asthma, emphysema, and chronic bronchitis. It is also indicated for adults in the treatment of cardiac asthma and left ventricular or congestive cardiac failure.
Use only as directed by a registered healthcare professional.

Pharmacology
Aminophylline is a combination of theophylline and ethylenediamine. Ethylenediamine is inactive and serves to increase the solubility of theophylline in water. Theophylline works by relaxing bronchial smooth muscle. Suggested mechanisms for its therapeutic effect include:

• Increase in intracellular cyclic AMP (cAMP) through inhibition of phosphodiesterase
• Adenosine receptor antagonism
• Prostaglandin antagonism
• Effects on intracellular calcium

Dosage & Administration

• Oral (Chronic bronchospasm):
  • Adults: As hydrate, initially 225-450 mg twice daily, increased if necessary.
  • Children (over 3 years): As modified-release hydrate, 12 mg/kg daily, increased to 24 mg/kg daily in two divided doses after one week.
• Intravenous (Acute severe bronchospasm):
  • Adults: Loading dose: 5 mg/kg (ideal body weight) or 250-500 mg (25 mg/ml) by slow injection or infusion over 20-30 minutes. Maintenance infusion dose: 0.5 mg/kg/hr. Max rate: 25 mg/min.
  • Children: Same loading dose as adults. Maintenance dose:
    • 6 months-9 years: 1 mg/kg/hr
    • 10-16 years: 0.8 mg/kg/hr
• Elderly: Dose reduction may be necessary.
• Hepatic impairment: Dose reduction may be necessary.
  Use only as directed by a registered healthcare professional.

Administration
Aminophylline tablets should be swallowed whole and not chewed due to the structure of the tablet.
Use only as directed by a registered healthcare professional.

Contraindications
Aminophylline should not be administered to patients with:

• Hypersensitivity to xanthines or ethylenediamine
• Active peptic ulcer, as it may increase the volume and acidity of gastric secretions

Side Effects
The most common adverse effects include:

• Gastric irritation
• Nausea, vomiting, diarrhea
• Hematemesis (vomiting blood), epigastric pain, and tremor (early signs of toxicity)
  With high doses, more severe symptoms may develop, such as:
• Ventricular arrhythmias, seizures
• Reactivation of peptic ulcer
• Headache, irritability, restlessness, insomnia, twitching, convulsions, and reflex hyperexcitability
• Palpitations, tachycardia, hypotension, circulatory failure
• Flushing, albuminuria (protein in urine), diuresis (increased urine output), hematuria (blood in urine)
• Inappropriate ADH (antidiuretic hormone) syndrome

Pregnancy & Lactation

• Pregnancy: The use of Aminophylline in pregnant women should be carefully considered, balancing the risk of uncontrolled disease with potential risks to the fetus.
• Lactation: Aminophylline is excreted in breast milk, and its use during breastfeeding should be evaluated based on the benefits of breastfeeding and the clinical need for the medication in the mother.

Precautions & Warnings
Aminophylline should be used with caution in the following conditions:

• Peptic ulceration
• Hyperthyroidism
• Hypertension
• Cardiac arrhythmias or other cardiovascular diseases
• Epilepsy
• Heart failure, hepatic dysfunction, chronic alcoholism, acute febrile illness
• Neonates and elderly patients, as theophylline clearance may be decreased in these populations, leading to increased serum theophylline concentrations and serum half-life.

Also, exercise caution in patients with impaired liver function, severe acute illnesses, or conditions requiring close monitoring.

Therapeutic Class

• Bronchodilator
• Methylxanthine derivatives
• Respiratory stimulants (analeptics)
• Theophylline & related drugs