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aminophylline (theophylline ethylenediamine)

(am in off' i lin)


Pregnancy Category C

Drug classes

Therapeutic actions
Relaxes bronchial smooth muscle, causing bronchodilation and increasing vital capacity, which
has been impaired by bronchospasm and air trapping; in higher concentrations, it also inhibits the
release oI slow-reacting substance oI anaphylaxis (SRS-A) and histamine.

O Symptomatic relieI or prevention oI bronchial asthma and reversible bronchospasm
associated with chronic bronchitis and emphysema
O Unlabeled uses: Respiratory stimulant in Cheyne-Stokes respiration; treatment oI
apnea and bradycardia in premature babies

Contraindications and cautions
O Contraindicated with hypersensitivity to any xanthine or to ethylenediamine, peptic
ulcer, active gastritis; rectal or colonic irritation or inIection (use rectal preparations).
O Use cautiously with cardiac arrhythmias, acute myocardial injury, CHF, cor
pulmonale, severe hypertension, severe hypoxemia, renal or hepatic disease,
hyperthyroidism, alcoholism, labor, lactation, pregnancy.

Available Iorms
Tablets100, 200 mg; liquid105 mg/5 mL; injection250 mg/10 mL; suppositories250,
500 mg

Individualize dosage: Base adjustments on clinical responses; monitor serum theophylline levels;
maintain therapeutic range oI 1020 mcg/mL; base dosage on lean body mass; 127 mg
aminophylline dihydrate 100 mg theophylline anhydrous.
O Acute symptoms requiring rapid theophyllini:ation in patients not receiving
theophylline. An initial loading dose is required, as indicated below:

Patient Group Loading Followed by Maintenance
Young adult
6 mg/kg 3 mg/kg q 4 hr
3 doses
3 mg/kg q 6 hr
Adult nonsmokers
who are otherwise
6 mg/kg 3 mg/kg q 6 hr
2 doses
3 mg/kg q 8 hr

O ong-term therapy. Usual range is 6001,600 mg/day PO in three to Iour divided
500 mg q 68 hr by rectal suppository or retention enema.
Children are very sensitive to CNS stimulant action oI theophylline; use caution in younger
children who cannot complain oI minor side eIIects.
O 6 mo. Not recommended.
O 6 yr. Use oI timed-release products not recommended.
O Acute therapy. For acute symptoms requiring rapid theophyllinization in patients not
receiving theophylline, a loading dose is required. Dosage recommendations are as

Patient Group Loading Followed by Maintenance
Children 6 mo9 yr 6 mg/kg 4 mg/kg q 4 hr
3 doses
4 mg/kg q 6 hr
Children 916 yr 6 mg/kg 3 mg/kg q 4 hr
3 doses
3 mg/kg q 6 hr

O ong-term therapy. 12 mg/kg per 24 hr PO; slow clinical adjustment oI the oral
preparations is preIerred; monitor clinical response and serum theophylline levels. In the
absence oI serum levels, adjust up to the maximum dosage shown below, providing the
dosage is tolerated.

Age Maximum Daily
9 yr 30.4 mg/kg/day
912 yr 25.3 mg/kg/day
1216 yr 22.8 mg/kg/day
~ 16 yr 16.5 mg/kg/day or
1,100 mg,
whichever is less

Use caution, especially in elderly men and in patients with cor pulmonale, CHF, liver disease
(halI-liIe oI aminophylline may be markedly prolonged in CHF, liver disease).
O Acute therapy. For acute symptoms requiring rapid theophyllinization in patients not
receiving theophylline, a loading dose is necessary as Iollows:

Patient Group Loading Followed by Maintenance
Older patients and cor
6 mg/kg 2 mg/kg q 6 hr
2 doses
2 mg/kg q 8 hr
CHF 6 mg/kg 2 mg/kg q 8 hr
2 doses
12 mg/kg q 12

Route Onset Peak Duration
Oral 16 hr 46 hr 68 hr
IV Immediate 30 min 48 hr

09,-olism: Hepatic; T
: 315 hr
Dis97i-:9ion: Crosses placenta; enters breast milk
Exc709ion: Urine

IV Iacts
P705,7,9ion: May be inIused in 100200 mL oI 5 dextrose injection or 0.9 sodium chloride
Inf:sion: Do not exceed 25 mg/min inIusion rate. Substitute oral therapy or IV therapy as soon
as possible; administer maintenance inIusions in a large volume to deliver the desired amount oI
drug each hour.
Ad:l9: 6 mg/kg. For acute symptoms requiring rapid theophyllinization in patients receiving
theophylline: a loading dose is required. Each 0.6 mg/kg IV administered as a loading dose will
result in about a 1 mcg/mL increase in serum theophylline. Ideally, deIer loading dose until
serum theophylline determination is made; otherwise, base loading dose on clinical judgment
and the knowledge that 3.2 mg/kg aminophylline will increase serum theophylline levels by
about 5 mcg/mL and is unlikely to cause dangerous adverse eIIects iI the patient is not
experiencing theophylline toxicity beIore this dose. Aminophylline IV maintenance inIusion
rates (mg/kg/hr) are given below:

Patient Group First 12 hr Beyond 12 hr
Young adult
1 0.8
Adult nonsmokers
who are otherwise
0.7 0.5

P0di,97ic: AIter an IV loading dose, these maintenance rates (mg/kg/hr) are recommended:

Patient Group First 12 hr Beyond 12 hr
Children 6 mo9 yr 1.2 1
Children 916 yr 1 0.8

07i,97ic: AIter a loading dose, these maintenance inIusion rates (mg/kg/hr) are recommended:

Patient Group First 12 hr Beyond 12 hr
Other patients, cor
0.6 0.3
CHF, liver disease 0.5 0.10.2

Com5,9i-ili9: Aminophylline is compatible with most IV solutions, but do not mix in solution
with other drugs, including vitamins.
Y-si90 incom5,9i-ili9: Dobutamine, hydralazine, ondansetron.

Adverse eIIects
O $07:m 90o5llin0 l0;0ls < 20 mcg/mL: Adverse eIIects uncommon
O $07:m 90o5llin0 l0;0ls > 20-25 mcg/mL: Nausea, vomiting, diarrhea, headache,
insomnia, irritability (75 oI patients)
O $07:m 90o5llin0 l0;0ls > 30-35 mcg/mL: Hyperglycemia, hypotension, cardiac
arrhythmias, tachycardia (~ 10 mcg/mL in premature newborns); s0iz:70s, -7,in
O CN$: Irritability (especially children); restlessness, dizziness, muscle twitching,
seizures, severe depression, stammering speech; abnormal behavior characterized by
withdrawal, mutism, and unresponsiveness alternating with hyperactive periods
O CV: Palpitations, sinus tachycardia, ventricular tachycardia, liIe-threatening
ventricular arrhythmias, circulatory Iailure
O I: Loss oI appetite, hematemesis, epigastric pain, gastroesophageal reIlux during
sleep, increased AST
O &: Proteinuria, increased excretion oI renal tubular cells and RBCs; diuresis
(dehydration), urinary retention in men with prostate enlargement
O #0s5i7,9o7: Tachypnea, respiratory arrest
O 907: Fever, Ilushing, hyperglycemia, SIADH, rash

O Increased eIIects with cimetidine, erythromycin, troleandomycin, clindamycin,
lincomycin, inIluenza virus vaccine, Iluoroquinolones, hormonal contraceptives
O Possibly increased eIIects with thiabendazole, riIampin, allopurinol
O Increased cardiac toxicity with halothane; increased likelihood oI seizures when
given with ketamine; increased likelihood oI adverse GI eIIects when given with
O Increased or decreased eIIects with Iurosemide, levothyroxine, liothyronine, liotrix,
thyroglobulin, thyroid hormones
O Decreased eIIects in patients who are cigarette smokers (12 packs per day);
theophylline dosage may need to be increased 50100
O Decreased eIIects with phenobarbital, aminoglutethimide
O Increased eIIects, toxicity oI sympathomimetics (especially ephedrine) with
theophylline preparations
O Decreased eIIects oI phenytoin and theophylline preparations when given
O Decreased eIIects oI lithium carbonate, nondepolarizing neuromuscular blockers
given with theophylline preparations
O Mutually antagonistic eIIects oI beta-blockers and theophylline preparations
O Elimination is increased by a low-carbohydrate, high-protein diet and by charcoal-
broiled beeI
O Elimination is decreased by a high-carbohydrate, low-protein diet
O Food may alter bioavailability and absorption oI timed-release theophylline
preparations, causing toxicity; these Iorms should be taken on an empty stomach
Drug-lab test
O InterIerence with spectrophotometric determinations oI serum theophylline levels by
Iurosemide, phenylbutazone, probenecid, theobromine; coIIee, tea, cola beverages,
chocolate, acetaminophen cause Ialsely high values
O Alteration in assays oI uric acid, urinary catecholamines, plasma Iree Iatty acids by
theophylline preparations

Nursing considerations
O is9o7: Hypersensitivity to any xanthine or to ethylenediamine, peptic ulcer, active
gastritis, cardiac arrhythmias, acute myocardial injury, CHF, cor pulmonale, severe
hypertension, severe hypoxemia, renal or hepatic disease, hyperthyroidism, alcoholism,
labor, lactation, rectal or colonic irritation or inIection (aminophylline rectal preparations)
O Psic,l: Bowel sounds, normal output; P, auscultation, BP, perIusion, ECG; R,
adventitious sounds; Irequency oI urination, voiding, normal output pattern, urinalysis,
LFTs, renal Iunction tests; liver palpation; thyroid Iunction tests; skin color, texture,
lesions; reIlexes, bilateral grip strength, aIIect, EEG

O Administer to pregnant patients only when clearly neededneonatal tachycardia,
jitteriness, and withdrawal apnea observed when mothers received xanthines up until
O Caution patient not to chew or crush enteric-coated timed-release Iorms.
O Give immediate-release, liquid dosage Iorms with Iood iI GI eIIects occur.
O Do not give timed-release Iorms with Iood; these should be given on an empty
stomach 1 hr beIore or 2 hr aIter meals.
O Maintain adequate hydration.
O Monitor results oI serum theophylline levels careIully, and arrange Ior reduced
dosage iI serum levels exceed therapeutic range oI 1020 mcg/mL.
O Take serum samples to determine peak theophylline concentration drawn 1530 min
aIter an IV loading dose.
O Monitor Ior clinical signs oI adverse eIIects, particularly iI serum theophylline levels
are not available.
O Ensure that diazepam is readily available to treat seizures.

Teaching points
O Take this drug exactly as prescribed; iI a timed-release product is prescribed, take
this drug on an empty stomach, 1 hour beIore or 2 hours aIter meals.
O Do not to chew or crush timed-release preparations.
O Administer rectal solution or suppositories aIter emptying the rectum.
O It may be necessary to take this drug around-the-clock Ior adequate control oI asthma
O Avoid excessive intake oI coIIee, tea, cocoa, cola beverages, and chocolate.
O Smoking cigarettes or other tobacco products impacts the drug's eIIectiveness. Try
not to smoke. NotiIy your health care provider iI smoking habits change while taking this
O Frequent blood tests may be necessary to monitor the eIIect oI this drug and to ensure
saIe and eIIective dosage; keep all appointments Ior blood tests and other monitoring.
O You may experience these side eIIects: Nausea, loss oI appetite (taking this drug with
Iood may help iI taking the immediate-release or liquid dosage Iorms); diIIiculty
sleeping, depression, emotional lability (reversible).
O Report nausea, vomiting, severe GI pain, restlessness, seizures, irregular heartbeat.

Adverse eIIects in talic are most common; those in old are liIe-threatening.