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Aminophylline

PHYLLOCONTIN

Aminophylline ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Aminophylline ballicule
Aminophylline PHYLLOCONTIN mascot mnemonic cartoon
Visual mnemonic: Aminophylline mascot
“A mean old Feline”
intravenous
tree → related to “tree-o-phylline” (also a CYP1A2 substrate)

What it isWater-soluble theophylline salt; acute bronchospasm.

Why this oneIt can be given intravenously when inhaled therapy is failing.

What limits itA narrow therapeutic index with levels required, and CYP1A2 makes it interaction-prone. Largely displaced by inhaled therapy.

Aminophylline molecular structure (skeletal formula)
Molecular structure: Aminophylline

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Acute bronchodilation (asthma/COPD)Adult, non-smokingLoading 5.7 mg/kg IV over 30 min (ideal body weight)Maintenance infusion 0.5 mg/kg/hrTitrate to serum theophylline 10–20 mcg/mL
Acute bronchodilationPeds 1–9 yrLoading 5.7 mg/kg IVInfusion 1.0 mg/kg/hrSerum theophylline 10–20 mcg/mL

Renal Undefined

Hepatic In liver dysfunction (also cor pulmonale, cardiac decompensation, or clearance-reducing drugs), keep initial infusion ≤21 mg/hr (as aminophylline) unless serum levels are monitored.

Each 1 mg/kg (IBW) of theophylline raises serum concentration ~2 mcg/mL; aminophylline = theophylline / 0.8.

Instructions

Available strengths

Cautions

Adverse reactions

Pregnancy Undefined

Lactation Undefined

Cost

Aminophylline (PHYLLOCONTIN)
Strength#/mogeneric $/unitCostPlus
25 mg/mLinjper unitnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Aminophylline is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskA narrow therapeutic index with levels required, and CYP1A2 makes it interaction-prone

Classes and tags

Clinical profile

Therapeutic safety burden4 / 4
Overdose danger3 / 4
Sedation liability0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

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Memory aids: interaction avatars

Aminophylline CYP1A2 substrate avatar mnemonic
CYP1A2 substrate

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