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Canadian Brand Names
Bronchodilator in reversible airway obstruction due to asthma or COPD; increase diaphragmatic contractility
Pregnancy Risk Factor
Theophylline crosses the placenta; adverse effects may be seen in the newborn. Theophylline metabolism may change during pregnancy; monitor serum levels.
Enters breast milk/compatible (AAP rates "compatible")
Hypersensitivity to theophylline, ethylenediamine, or any component of the formulation
If a patient develops signs and symptoms of theophylline toxicity, a serum level should be measured and subsequent doses held. Due to potential saturation of theophylline clearance at serum levels within (or in some patients less than) the therapeutic range, dosage adjustment should be made in small increments (maximum: 25% reduction). Due to wide interpatient variability, theophylline serum level measurements must be used to optimize therapy and prevent serious toxicity. Use caution with peptic ulcer, hyperthyroidism, seizure disorder, hypertension, or tachyarrhythmias.
Uncommon at serum theophylline concentrations
1% to 10%:
Central nervous system: Nervousness, restlessness
Gastrointestinal: Nausea, vomiting
<1%: Insomnia, irritability, seizure, skin rash, gastric irritation, tremor, allergic reactions
of CYP1A2 (major), 2E1 (minor), 3A4 (minor)Substrate
CYP1A2 inducers: May decrease the levels/effects of aminophylline. Example inducers include aminoglutethimide, carbamazepine, phenobarbital, and rifampin.
CYP1A2 inhibitors: May increase the levels/effects of aminophylline. Example inhibitors include amiodarone, ciprofloxacin, fluvoxamine, ketoconazole, norfloxacin, ofloxacin, and rofecoxib.
Food: Food does not appreciably affect absorption. Avoid extremes of dietary protein and carbohydrate intake. Changes in diet may affect the elimination of theophylline; charcoal-broiled foods may increase elimination, reducing half-life by 50%.
Do not use solutions if discolored or if crystals are present
Stable in dextran 6% in D5W, dextran 6% in NS, D5LR, D5NS, D5/2NS, D5/4NS, D5W, D10W, D20W, LR, /2NS, NS; in fat emulsion 10%111variable stability (consult detailed reference)
Y-site administration: Compatible: Allopurinol, amifostine, amphotericin B cholesteryl sulfate complex, aztreonam, ceftazidime, cimetidine, cladribine, docetaxel, doxorubicin liposome, enalaprilat, esmolol, etoposide, famotidine, filgrastim, fluconazole, fludarabine, foscarnet, gatifloxacin, gemcitabine, granisetron, heparin with hydrocortisone sodium succinate, inamrinone, labetalol, levofloxacin, linezolid, melphalan, meropenem, morphine, paclitaxel, pancuronium, piperacillin/tazobactam, potassium chloride, propofol, ranitidine, remifentanil, sargramostim, tacrolimus, teniposide, thiotepa, tolazoline, vecuronium, vitamin B complex with C. Incompatible: Amiodarone, ciprofloxacin, clarithromycin, dobutamine, hydralazine, ondansetron, vinorelbine, warfarin. Variable (consult detailed reference): Cisatracurium, diltiazem
Compatibility in syringe: Compatible: Heparin, metoclopramide, pentobarbital, thiopental. Incompatible: Doxapram
Compatibility when admixed: Compatible: Amobarbital, bretylium, calcium gluconate, chloramphenicol, cimetidine, dexamethasone, diphenhydramine, dopamine, erythromycin lactobionate, esmolol, floxacillin, flumazenil, furosemide, heparin, hydrocortisone sodium succinate, lidocaine, mephentermine, meropenem, methyldopate, metronidazole with sodium bicarbonate, nitroglycerin, pentobarbital, phenobarbital, potassium chloride, ranitidine, sodium bicarbonate, terbutaline. Incompatible: Atracurium, bleomycin, cefepime, ceftazidime, ceftriaxone, chlorpromazine, ciprofloxacin, clindamycin, dobutamine, doxorubicin, epinephrine, hydralazine, hydrocortisone sodium succinate with cephalothin sodium, hydroxyzine, insulin (regular), isoproterenol, levorphanol, meperidine, morphine, norepinephrine, papaverine with trimecaine, penicillin G potassium, pentazocine, prochlorperazine edisylate, prochlorperazine mesylate, promazine, promethazine, vitamin B complex with C. Variable (consult detailed reference): Amikacin, ascorbic acid, corticotropin, dimenhydrinate, methylprednisolone sodium succinate, nafcillin, procaine, vancomycin, verapamil, zinc
Mechanism of Action
Causes bronchodilatation, diuresis, CNS and cardiac stimulation, and gastric acid secretion by blocking phosphodiesterase which increases tissue concentrations of cyclic adenine monophosphate (cAMP) which in turn promotes catecholamine stimulation of lipolysis, glycogenolysis, and gluconeogenesis and induces release of epinephrine from adrenal medulla cells
Absorption: Oral: Dosage form dependent
Distribution: 0.45 L/kg based on ideal body weight
Protein binding: 40%, primarily to albumin
Metabolism: Children >1 year and Adults: Hepatic; involves CYP1A2, 2E1 and 3A4; forms active metabolites (caffeine and 3-methylxanthine)
Half-life elimination: Highly variable and dependent upon age, liver function, cardiac function, lung disease, and smoking history
Time to peak, serum:
Oral: Immediate release: 1-2 hours
I.V.: Within 30 minutes
Excretion: Urine Children >3 months and Adults: 10% unchanged
Treatment of acute bronchospasm: I.V.:
Loading dose (in patients not currently receiving aminophylline or theophylline): 6 mg/kg (based on aminophylline) administered I.V. over 20-30 minutes; administration rate should not exceed 25 mg/minute (aminophylline)
Approximate I.V. maintenance dosages are based upon continuous infusions; bolus dosing (often used in children <6 months of age) may be determined by multiplying the hourly infusion rate by 24 hours and dividing by the desired number of doses/day
6 weeks to 6 months: 0.5 mg/kg/hour
6 months to 1 year: 0.6-0.7 mg/kg/hour
1-9 years: 1 mg/kg/hour
9-16 years and smokers: 0.8 mg/kg/hour
Adults, nonsmoking: 0.5 mg/kg/hour
Older patients and patients with cor pulmonale: 0.3 mg/kg/hour
Patients with congestive heart failure: 0.1-0.2 mg/kg/hour
Dosage should be adjusted according to serum level measurements during the first 12- to 24-hour period.
Bronchodilator: Oral: Children
Dilute with I.V. fluid to a concentration of 1 mg/mL and infuse over 20-30 minutes; maximum concentration: 25 mg/mL; maximum rate of infusion: 0.36 mg/kg/minute, and no greater than 25 mg/minute. I.M. administration is not recommended. Oral and I.V. should be administered around-the-clock rather than 4 times/day, 3 times/day, etc (ie, 12-6-12-6, not 9-1-5-9) to promote less variation in peak and trough serum levels.
Do not drink or eat large quantities of caffeine-containing beverages or food (colas, coffee, chocolate).
Encourage patient to drink adequate fluids (2 L/day) to decrease mucous viscosity in airways; monitor vital signs, I & O, serum concentrations, and CNS effects (insomnia, irritability)
Aminophylline is a 2:1 complex of theophylline and ethylenediamine.
Theophylline results in significant tachycardia and, at higher doses, may impair ventricular rate control in patients with atrial fibrillation. This is particularly a concern since patients with underlying chronic obstructive lung disease often have coexisting atrial fibrillation. Aminophylline can be used to treat patients who have adverse hemodynamic responses to adenosine or dipyridamole, when used during cardiovascular stress testing.
Dental Health: Effects on Dental Treatment
Prescribe erythromycin products with caution to patients taking theophylline products. Erythromycin will delay the normal metabolic inactivation of theophyllines leading to increased blood levels; this has resulted in nausea, vomiting, and CNS restlessness.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause nervousness or restlessness
Mental Health: Effects on Psychiatric Treatment
Carbamazepine and barbiturates may decrease aminophylline levels; disulfiram and propranolol may increase aminophylline levels
[DSC] = Discontinued product
Injection, solution: 25 mg/mL (10 mL, 20 mL)
Liquid, oral [DSC]: 105 mg/5 mL (500 mL) [apricot flavor]
Tablet: 100 mg, 200 mg
"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,"Pediatrics, 2001, 108(3):776-89.
Cummins LH, et al, "Erythromycin's Effect on Theophylline Blood Levels. Correspondence,"Pediatrics, 1977, 59:144-5.
Delaforge M and Sartori E, "In Vivo Effects of Erythromycin, Oleandomycin, and Erythralosamine Derivatives on Hepatic Cytochrome P450,"Biochem Pharmacol, 1990, 40(2):223-8.
Ludden TM, "Pharmacokinetic Interactions of the Macrolide Antibiotics,"Clin Pharmacokinet, 1985, 10(1):63-79.
International Brand Names
Afonilum® [inj.] (DE); Aminocardol® (TR); Aminocont® (FI); Aminofilina® (AR, BR, CL, PL); Aminofilina Ariston® (EC); Aminofilina Biocrom® (AR); Aminofilina Bioquim® (AR); Aminofilina Czopki pediatryczne® (PL); Aminofilina Fabra® (AR); Aminofilina Inyectable® (CL); Aminofilina L.CH.® (CL); Aminofilina Northia® (AR); Aminofilina Rigo® (AR); Aminofilina (RO); Aminofilin® (RO, YU); Aminofillina Fisiopharma® (IT); Aminofillina® (IT); Aminoima® (BR); Aminomal® (BD, IT, RO); Aminophyllin® (DE, HR, NO, ZA); Aminophylline Atlantic® (SG, TH); Aminophylline® (AU, BD, GB, IL, NZ, RO, RU); Aminophylline DBL® (SG); Aminophyllinum® (CZ, HU, PL, RO, SI, YU); Aminophyllinum Retard® (PL, RO); Aminoslow® (LU); Amnivent® (GB); Amofilin® (RO); Asmafilin® (TR); Cardiomin® (CL); Cardirenal® (AR); Cardophyllin® (BD); Caréna® (TR); Carine® (AU); Clonofillin SR® (HU); Diaphyllin® (HU, RO); Diaphyllin Venosum® (HU); Drafilyn® (MX); Elixophyllin® (IL); Eufilina® (ES, RO); Eufilin® (BR); Euphyllin® (CZ, EG, HK, JO, KW, LB, LU, NL, RU); Fadafilina® (AR); Larjanfilina® (AR); Min-I-Jet Aminophylline® (GB); Miofilin® (RO); Mundiphyllin® (AT); N-Aminofilina® (RO); Neophyllin® (JP); Norphyllin® (GB); Novphyllin® (BG); Peterphyllin Injection® (ZA); Pharophyllin® (CZ); Phyllocontin®-350 (CA); Phyllocontin® (CA, IE, ZA); Phyllocontin Continus® (GB, ID, IE); Phyllotemp® (CH, DE); Q-Med Theophyllin® (ZA); Retafilin® (HR); Syntophyllin® (CZ); Tefamin® (IT); Teofyllamin Ipex® (SE); Theofylline FNA® (NL); Theophyllamin Jenapharm® (DE); Theophyllin EDA-ratiopharm® (DE)