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APO-THEO ER is a brand name for Theophylline, supplied as a tablet (extended-release). The medicine, its uses, side effects and dosage are the same regardless of brand.
Verbatim from this product's HC label. Tap a section to expand.
1 Dosing Considerations Monitoring of plasma theophylline concentrations may be required when: higher doses are prescribed patients have co-morbidities resulting in impaired clearance (see WARNINGS AND PRECAUTIONS, Patients with Special Diseases and Conditions) theophylline is co-administered with medication that reduces theophylline clearance (see DRUG INTERACTIONS) Elderly patients are at a greater risk of experiencing serious toxic effects from theophylline than younger patients.
Careful attention to dose reduction and monitoring of serum theophylline concentrations are required in elderly patients due to pharmacokinetic a nd pharmacodynamic changes associated with aging, including the potential for decreased theophylline clearance.
APO-THEO ER is not recommended for use in patients under 12 years of age. 2 Recommended Dose and Dosage Adjustment Page 5 of 33 Administration and dosing of theophylline should be individualized in respect of the patient’s clinical response and serum theophylline levels.
There is considerable patient -to-patient variation in the daily theophylline dose required to achieve therapeutic and safe levels. Ide ally, all patients should have serum or plasma theophylline levels measured which would enable doses and dosing regimens to be tailored in order to maintain therapeutic levels, ensure optimal clinical response and avoid toxicity.
5 mcmol/L). Theophylline distributes poorly into body fat, therefore, mg/kg doses should be calculated on the basis of lean body mass (ideal body weight). 5 mcmol/L) represents the lower level of clinical effectiveness. Whereas the serum level of 20 mcg/mL (110 mcmol/L) is an important reference point in terms of toxicity (see WARNINGS AND PRECAUTIONS).
Initial Adult Dose:
For patients not currently receiving oral theophylline, the recommended initial dose is 400-600 mg once daily. In patients currently controlled on oral theophylline, APO-THEO ER (theophylline sustained release tablets) therapy should start at the same daily theophylline dosage (mg for mg basis), provided by the previous formulation.
For example, a patient receiving 400 mg twice daily (800 mg daily dosage), would be given two 400 mg APO-THEO ER tablets once daily. A minimum of 12 hours should elapse between a patient's last dose of the previou s oral theophylline formulation and the first dose of APO-THEO ER .
It is recommended that once-daily APO-THEO ER be taken in the evening. Studies have demonstrated that while the bioavailability and the pharmacokinetics of theophylline tablets were not significantly different between morning and evening dosing, a better clinical response was obtained with evening dosing.
Subsequent studies indicate that the clinical advantages of evening dosing are likely a result of the maximum theophylline levels occurring in the early morning hours, a time of greatest bronchoconstriction and symptoms for many asthmatics.
1 Adverse Reaction Overview The most common adverse reactions are gastric irritation, nausea, vomiting, epigastric pain, and tremor. These are usually early signs of toxicity, however with high doses ventricular arrhythmias or seizures may be the first signs to appear.
Adverse reactions classified by body system include:
Gastrointestinal: Abdominal pain, anorexia, diarrhea, epigastric pain, gastroesophageal reflux, hematemesis, intestinal bleeding, nausea, reactivation of peptic ulcer and vomiting.
Central Nervous System:
Convulsions, dizziness, headache, irritability, reflex hyperexcitability, restlessness, twitching and tremors.
Cardiovascular:
Atrial tachycardia, circulatory failure, extrasystoles, flushing, hypotension, palpitations, sinus tachycardia and ventricular arrhythmias.
Skin and Subcutaneous:
Pruritus and rash.
Page 11 of 33 Immune:
Anaphylactic reaction, anaphylactoid reaction and hypersensitivity. Metabolic and Nutritional:Hyperuricemia and hyperglycemia.
Psychiatric:
Agitation, anxiety, insomnia and sleep disorder.
Renal:
Albuminuria, diuresis, hematuria and urinary retention (see WARNINGS AND PRECAUTIONS, Patients with Special Diseases and Conditions).
Others:
Tachypnea and inappropriate ADH syndrome.
General In clinical situations where immediate bronchodilation is required, such as status asthmaticus, APO-THEO ER is not appropriate. Theophylline has a narrow therapeutic index, the margin of safety above therapeutic doses is small.
Whenever signs of intolerance to theophylline develop, the therapy should be reassessed. Theophylline clearance can be affected by various disease states, the age of the patient, concomitant use of other medication and lifestyle habits.
A dosage schedule in the pediatric population has not been established. Use of APO-THEO ER tablets in children under 12 years of age is not recommended. There is a marked variation in serum levels achieved in different patients given the same dose of theophylline.
Therefore, high serum levels may occur in some patients receiving doses considered to be conventional. The possibility of theophylline overdose should always be considered. The variability in serum levels is primarily due to differences in the rate of meta bolism.
Therefore, it is advisable to individualize the dosage regimen. Ideally, all patients should have serum theophylline levels measured which would enable doses and dosing regimens to be tailored for each patient in order to maintain therapeutic levels, ensure optimal clinical response and avoid toxicity.
5 mcmol/L) and levels above 20 mcg/mL (110 mcmol/L) are usually quite toxic in most adults. Page 9 of 33 Although theophylline tablets have pharmacokinetic properties similar to other sustained release theophylline formulations, it is not possible to ensure interchangeability between different formulations.
Careful clinical monitoring is required when changing from one formulation to another. The equivalent content of anhydrous theophylline is the active ingredient that determines the blood concentration and clinical response. If a change in theophylline product is made and it involves a change in anhydrous theophylline e quivalence, the dose should be adjusted accordingly.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Other brands of Theophylline in Canada.
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Brand names are compiled from public regulatory records for active-ingredient mapping only. Drugvu is not affiliated with any manufacturer. This is not medical advice.
It is advisable that theophylline tablets be taken with food, or within 1-2 hours of mealtime, as studies have suggested that absorption may be incomplete if taken under conditions of prolonged fasting. Overall, therefore, it is recommended that most patients should take once- daily APO-THEO ER with, or shortly following, the evening meal.
Dose Titration:
Dosage adjustments should be based on the patient's clinical response and/or serum theophylline levels, with increases of ½ tablet per day at 3 to 4 day intervals. Individual requirements vary considerably, therefore, the physician should be prepared to adjust each patient's dose.
Do not attempt to maintain any dosage that is poorly tolerated. It is not possible to ensure interchangeability between different sustained release theophylline products. Once titrated to an effective dose, patients should not be changed from theophylline product to another sustained release xanthine preparation without re-titration and careful clinical monitoring.
APO-THEO ER tablets must be swallowed whole and should not be broken, chewed, dissolved or crushed as this may lead to a rapid release of theophylline with the pote ntial for toxicity. Tablets may be halved. 5 Missed Dose Monitoring serum theophylline levels is important, especially during initiation of therapy and dosage adjustment.
For serum levels to be most useful, it is important that the patient not have Page 6 of 33 missed or added any doses during the previous 3 days and that the dose intervals remained relatively constant. At steady-state, theophylline sustained release tablets produce peak theophylline levels between 8 and 12 hours post-dose, and trough levels almost always occur at the time of dosing.
During once-daily dosing, the mean fluctuation between peak and trough theophylline levels is 130% (See ACTION AND CLINICAL PHARMACOLOGY for further information on the time of peak theophylline levels, and the relationship b etween a single level obtained 12 hours post-dose and the actual peak level).
5 mcmol/L), although some patients obtain a very good bronchodilator effect from serum levels les s than 10 mcg/mL (55 mcmol/L). In cases where it is not possible to monitor theophylline levels, patients should be closely observed for signs of toxicity and dosages greater than 13 mg/kg/day (or 900 mg/day, whichever is less) should not be given.
Use with caution in patients with severe cardiac disease, severe hypoxemia, hypertension, hyperthyroidism, acute myocardial injury, cor pulmonale, congestive heart failure, liver disease, porphyria, in elderly males with pre-existing partial urinary tract obstruction, such as prostatic enlargement, due to risk of urinary retention.
Patients with Special Diseases and Conditions Due to potential decreased theophylline clearance, which may result in increa sed serum levels and significant adverse drug reactions in patients, dose reduction and monitoring of serum theophylline concentrations may be required in elderly patients and in patients: with impaired liver or kidney function over 55 years of age, particularly males and those with chronic lung disease with cardiac disease with active influenza or other viral disease or after influenza immunization with a high carbohydrate, low protein diet with hypothyroidism (and when starting acute treatment for hypothyroidism) with a sustained high fever Cardiovascular Theophylline may cause arrhythmia and/or worsen pre-existing arrhythmia.
Any significant change in rate and/or rhythm warrants monitoring and further investigation. Many patients who require theophylline may exhibit tachycardia due to their underlying disease process so that the cause/effect relationship to elevated serum theophylline concentrations may not be appreciated.
Endocrine and Metabolism Due to potential increased theophylline clearance, dose increase and monitoring of serum theophylline concentrations may be required in patients with hyperthyroidism (and when starting acute hyperthyroidism treatment) and cystic fibrosis.
Patients who are rapid metabolizers of theophylline, peak to trough fluct uations in theophylline levels may be greater than desirable or result in side-effects at the time of maximum level and/or the recurrence of symptoms towards the end of the 24-hour dose interval when levels are lowest.
In such patients, dividing the total daily theophylline dose into two equal doses may be indicated. I. irritant. Therefore, the drug should only be used with caution in patients with a history of peptic ulcer disease. Neurologic Theophylline may exacerbate frequency and duration of seizures and therefore caution should be exercised in patients with history of seizures.
Page 10 of 33 Respiratory Particular care is advised in patients suffering from severe asthma who require acute theophylline administration. It is recommended that serum theophylline concentrations are monitored in such situations. 1 Pregnant Women Theophylline crosses the placental barrier, where concentrations are similar to plasma levels.
Safe use in pregnancy has not been established relative to possible adverse effects on fetal development. APO-THEO ER should not be administered during pregnancy unless considered essential by the physician. Theophylline should be given to pregnant women only when the anticipated benefits outweigh the risk to the child.
2 Breast-feeding Theophylline passes freely into breast milk, where concentrations are similar to plasma levels. Theophylline should be given to nursing mothers only when the anticipated benefits outweigh the risk to the child. 3 Pediatrics Pediatrics (<12 years of age): APO-THEO ER is not recommended for use in children under 12 years of age.
4 Geriatrics Geriatrics (>65 years of age): Dose reduction may be required in elderly patients (see WARNINGS AND PRECAUTIONS, Patients with Special Diseases and Conditions section).