Aminophylline Relaxes bronchial smooth muscle, causing bronchodilation. It also inhibits the release oI slow-reacting substance oI anaphylaxis (SRS-A) and histamine. It is contraindicated with hypersensitivity to any xanthine or to ethylenediamine, peptic ulcer, active gastritis, rectal or colon irritation or inIection.
Aminophylline Relaxes bronchial smooth muscle, causing bronchodilation. It also inhibits the release oI slow-reacting substance oI anaphylaxis (SRS-A) and histamine. It is contraindicated with hypersensitivity to any xanthine or to ethylenediamine, peptic ulcer, active gastritis, rectal or colon irritation or inIection.
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Aminophylline Relaxes bronchial smooth muscle, causing bronchodilation. It also inhibits the release oI slow-reacting substance oI anaphylaxis (SRS-A) and histamine. It is contraindicated with hypersensitivity to any xanthine or to ethylenediamine, peptic ulcer, active gastritis, rectal or colon irritation or inIection.
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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.
Indications 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.
Dosages 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. ADULTS Oral 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 smokers 6 mg/kg 3 mg/kg q 4 hr 3 doses 3 mg/kg q 6 hr Adult nonsmokers who are otherwise healthy 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 doses. Rectal 500 mg q 68 hr by rectal suppository or retention enema. PEDIATRIC PATIENTS 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. Oral O Acute therapy. For acute symptoms requiring rapid theophyllinization in patients not receiving theophylline, a loading dose is required. Dosage recommendations are as Iollows:
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 Dose 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
GERIATRIC PATIENTS OR IMPAIRED ADULTS 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). Oral 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 pulmonale 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 hr
Pharmacokinetics Route Onset Peak Duration Oral 16 hr 46 hr 68 hr IV Immediate 30 min 48 hr
09,-olism: Hepatic; T 1/2 : 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 injection. 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 smokers 1 0.8 Adult nonsmokers who are otherwise healthy 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 pulmonale 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 $07:m 90o5llin0 l0;0ls > 30-35 mcg/mL: Hyperglycemia, hypotension, cardiac arrhythmias, tachycardia (~ 10 mcg/mL in premature newborns); s0iz:70s, -7,in d,m,g0 O CN$: 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
Interactions Drug-drug 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 tetracyclines 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 concomitantly O Decreased eIIects oI lithium carbonate, nondepolarizing neuromuscular blockers given with theophylline preparations O Mutually antagonistic eIIects oI beta-blockers and theophylline preparations Drug-Iood 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 Assessment 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
Interventions O Administer to pregnant patients only when clearly neededneonatal tachycardia, jitteriness, and withdrawal apnea observed when mothers received xanthines up until delivery. 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 attacks. 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 drug. 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.