Aminophylline (theophylline ethylenediamine) (Truphylline)

Category:

  • Respiratory

Description:

  • Antiasthmatic, bronchodilator, COPD agent

Indications:

  • Asthma, reversible bronchospasm associated with COPD

  • Pulmonary edema

Contraindications:

  • Hypersensitivity to xanthines or ethylenediamine, underlying seizure disorder (not on anticonvulsant therapy)

  • Suppositories contraindicated in presence of infection or irritation of lower bowel or rectum

Precautions:

  • Pregnancy category C

  • Elderly, CHF, corpulmonale, hepatic disease

  • Hypertension, infants <1 year, hypoxemia, sustained high fever, history of peptic ulcer

  • Alcoholism

Adverse Reactions (Side Effects):

  • CNS: anxiety, dizziness, headache, insomnia, lightheadiness, muscle twitching, reflex hyperexcitability, restlessness, seizures

  • CV: circulatory failure, flushing, hypotension, flushing, ventricular arrhythmias

  • GI: anorexia, bitter taste, black stools, diarrhea, dyspepsia, epigastric pain, esophageal reflux, hematemesis, nausea, vomiting

  • GU: proteinuria, urinary frequency

  • MISC: urticaria, alopecia, tachypnea, hyperglycemia

Dosage:

Administered orally, rectally, intravenously

Adult and Child:  

  • PO acute therapy (patient not currently receiving theophylline products): 

    • Following a 6.3 mg/kg loading dose, maintenance dose follows:

      • children age 1-9 years, 5.1 mg/kg every 6 hours 

      • children 9-16 years and smokers, 3.8 mg/kg every 6 hours

      • otherwise healthy non-smoking adults, 3.8 mg/kg every 8 hours

      • older patients/ patients with CHF, corpulmonale, 2.5 mg/kg every 8 hours

  • PO acute therapy (patients currently receiving theophylline products): 

    • Defer loading dose if serum theophylline concentration can be rapidly obtained

    • base loading dose on the principle that each 0.63 mg/kg of aminophylline will increase serum theophylline concentration by 1 mcg/ml 

    • if this is not possible and sufficient respiratory distress is present (without signs of theophylline toxicity), 

      • use 3.1 mg/kg of a rapidly available form of aminophylline

      • will likely increase serum theophylline concentration 5 mcg/ml 

    • maintenance dosage as previously described

  • PO chronic therapy:

    • Initial dose 20.3 mg/kg/24 hours or 500 mg/24 hours (whichever is less) divided by 6-8 hours; 

    • increase every 3 days by 25% as tolerated until clinical response or maximum dose is reached (below); 

    • monitor serum theophylline concentrations; 

    • do not exceed the following (or 1140mg, whichever is less without serum monitoring): 

      • Age 1-9 years, 30.4 mg/kg/day; 

      • age 9-12 years, 25.3 mg/kg/day; 

      • age 12-16 years22.8 mg/kg/day; 

      • age 16 years and older, 16.5 mg/kg/day

  • IV (patients not currently receiving theophylline products): 

    • Following a 6.3 mg/kg IV loading dose, maintenance dose follows: 

      • children age 1-9 years, 1 mg/kg/hr; 

      • children age 9-16 years and smokers, 0.8 mg/kg/hour;  

      • otherwise healthy non-smoking adults, 0.5 mg/kg/hour; 

      • older patients/patients with cor pulmonale 0.3 mg/kg/hour; 

      • patients with CHF, 0.1-0.2 mg/kg/hour

  • IV (patients currently receiving theophylline products): 

    • Defer loading dose if serum theophylline concentration can be rapidly obtained.  

    • Base loading dose on the principle that each 0.63 mg/kg of aminophylline will increase serum theophylline concentration by 1 mcg/ml

    • if this is not possible and sufficient respiratory distress is present:

      • use 3.1 mg/kg aminophylline

      • will likely increase serum theophylline concentration 5 mcg/ml

      • administer only if theophylline toxicity is not present

    • maintenance dosage as described above.

 
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