aminophylline

aminophylline /am·i·noph·yl·line/ (am″ĭ-nof´ĭ-lin) a salt of theophylline, used as a bronchodilator and as an antidote to dipyridamole toxicity.

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am·i·noph·yl·line (m-nf-ln)

n.

A theophylline derivative, used as a bronchodilator in the treatment of bronchial asthma, emphysema, and bronchitis.

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aminophylline

[am′ənōfil′in, əmē′nō-]

a bronchodilator.

indication It is prescribed in the treatment of bronchospasm associated with asthma, emphysema, and bronchitis.

contraindications Known hypersensitivity to this drug or other xanthine medication prohibits its use. It is used with caution in patients who have peptic ulcers and those in whom cardiac stimulation would be harmful.

adverse effects Among the more serious adverse reactions are GI disturbances, central nervous system stimulation, palpitations, tachycardia, nervousness, and seizures.

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aminophylline (theophylline ethylenediamine),

n brand names: Phyl-locontin;
drug class: xanthine;
action: relaxes smooth muscle of the respiratory system;
uses: bronchial asthma, bronchospasm, Cheyne-Stokes respirations.

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aminophylline

a mixture of theophylline and ethylenediamine; used as a respiratory stimulant, smooth muscle relaxant, myocardial stimulant and diuretic. Administration of the drug may be by mouth, intramuscularly, intravenously or rectally.

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aminophylline (theophylline, ethylenediamine)

Amnivent (UK), Phyllocontin (CA) (UK)

Pharmacologic class: Xanthine

Therapeutic class: Bronchodilator

Pregnancy risk category C

Action

Unclear. Thought to directly relax smooth muscle of bronchial airways and increase pulmonary blood flow by inhibiting phosphodiesterase.

Availability

Injection: 250 mg/10 ml

Oral liquid: 105 mg/5 ml

Suppositories: 250 mg, 500 mg

Tablets: 100 mg, 200 mg

⊘Indications and dosages

➣ Symptomatic relief of bronchospasm in patients with acute symptoms who require rapid theophyllinization

Adults (nonsmokers): 0.7 mg/kg/hour I.V. for first 12 hours. Maintenance dosage is 0.5 mg/kg/hour I.V.

Children ages 9 to 16: 1 mg/kg/hour I.V. for first 12 hours. Maintenance dosage is 0.8 mg/kg/hour I.V.

Children ages 6 months to 9 years: 1.2 mg/kg/hour I.V. for first 12 hours. Maintenance dosage is 1 mg/kg/hour I.V.

➣ Chronic bronchial asthma

Adults and children: Dosage is highly individualized. Common initial dosage is 16 mg/kg/24 hours I.V. or 400 mg/24 hours I.V. in divided doses at 6- or 8-hour intervals. If needed, dosage may be increased 25% at 3-day intervals.

Dosage adjustment

• Heart failure
• Hepatic disease
• Elderly patients
• Smokers

Off-label uses

• Dyspnea in patients with chronic obstructive pulmonary disease (COPD)

Contraindications

• Hypersensitivity to xanthine compounds or ethylenediamine
• GI disease
• Seizure disorders

Precautions

Use cautiously in:
• COPD, diabetes mellitus, glaucoma, renal or hepatic disease, heart failure or other cardiac or circulatory impairment, hypertension, hyperthyroidism, peptic ulcer, severe hypoxemia
• elderly patients
• neonates, infants, and young children.

Administration

• For I.V. use, dilute according to label directions and infuse at a rate no faster than 25 mg/minute.
• Don't give in I.V. solutions containing invert sugar, fructose, or fat emulsions.
• Give oral form at meals with 8 oz of water.

Route	Onset	Peak	Duration
P.O. (extended)	Variable	Variable	Variable
P.O. (liquid)	15-60 min	1-7 hr	Variable
I.V.	Immediate	Immediate	6-8 hr
P.R.	Unknown	Unknown	Unknown

Adverse reactions

CNS: irritability, dizziness, nervousness, restlessness, headache, insomnia, stammering speech, abnormal behavior, mutism, unresponsiveness alternating with hyperactivity, seizures

CV: palpitations, sinus tachycardia, extrasystoles, marked hypotension, arrhythmias, circulatory failure

GI: nausea, vomiting, diarrhea, epigastric pain, hematemesis, gastroesophageal reflux, anorexia

GU: urine retention (in men with enlarged prostate), diuresis, increased excretion of renal tubular cells and red blood cells, proteinuria

Metabolic: hyperglycemia

Musculoskeletal: muscle twitching

Respiratory: tachypnea, respiratory arrest

Skin: flushing

Other: fever, hypersensitivity reactions (including exfoliative dermatitis and urticaria)

Interactions

Drug-drug. Adenosine: decreased antiarrhythmic effect of adenosine

Barbiturates, nicotine, phenytoin, rifampin: decreased aminophylline blood level

Beta-adrenergic blockers: antagonism of aminophylline effects

Calcium channel blockers, cimetidine, ciprofloxacin, disulfiram, erythromycin, hormonal contraceptives, influenza vaccine, interferon, methotrexate: elevated aminophylline blood level

Carbamazepine, isoniazid, loop diuretics (such as furosemide): increased or decreased aminophylline blood level

Ephedrine, other sympathomimetics: toxicity, arrhythmias

Lithium: increased lithium excretion

Drug-diagnostic tests. Aspartate aminotransferase, glucose: increased levels

Drug-herbs. Cayenne: increased risk of aminophylline toxicity

Drug-behaviors. Smoking: increased aminophylline elimination

Patient monitoring

☞ Monitor aminophylline blood level. Adjust dosage if patient has signs or symptoms of toxicity (tachycardia, headache, anorexia, nausea, vomiting, diarrhea, restlessness, and irritability).
• Assess for arrhythmias, especially after giving loading dose.
• Check vital signs and fluid intake and output.
• Monitor patient's response to drug, and assess pulmonary function test results.

Patient teaching

• Advise patient to take oral doses at meals with 8 oz of water.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
• Advise patient to establish effective bedtime routine to minimize insomnia.
• Caution patient not to change aminophylline brands.
• If patient smokes, tell him to notify prescriber if he stops smoking; dosage may need to be adjusted.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

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aminophylline

Therapeutics The ethylenediamine salt of theophylline, administered IV to Pts with acute asthma Sx Mechanism Inhibits cAMP phosphodiesterase Action Relaxes upper airway and pulmonary vessel smooth muscle, resulting in broncho- and vasodilation; it is also diuretic, coronary vasodilator, cardiac and cerebral stimulant Adverse effects GI irritation–anorexia, N&V, epigastric pain, restlessness, insominia, headache Contraindications Peptic ulcers, seizures, hypersensitivity to ethylenediamine. See Theophylline.