QUIBRON-T- theophylline, anhydrous tablet
Monarch Pharmaceuticals, Inc.
Theophylline is structurally classified as a methylxanthine. It occurs as a white, odorless, crystalline powder with a bitter taste. Anhydrous theophylline has the chemical name 1HPurine- 2,6-dione, 3,7-dihydro-1,3-dimethyl-, and is represented by the following structural formula:
The molecular formula of anhydrous theophylline is C7 H8 N4 O2 with a molecular weight of 180.17.
Quibron® -T is available as tablets intended for oral administration, containing 300 mg of anhydrous theophylline per tablet. Quibron® -T is an oral bronchodilator in an immediate-release formulation in the ACCUDOSE® Tablet design. With functional trisects and bisects, Quibron® -T Tablets can be accurately divided into 100-, 150-, and 200-mg segments to provide a variety of dosing increments, as required.
|One-third tablet||= 100 mg|
|One-half tablet||= 150 mg|
|Two-thirds tablet||= 200 mg|
|One tablet||= 300 mg|
Inactive Ingredients: microcrystalline cellulose, yellow ferric oxide, hydroxypropyl methylcellulose 2910, lactose monohydrate, magnesium stearate, colloidal silicon dioxide, and sodium starch glycolate.
Theophylline has two distinct actions in the airways of patients with reversible obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects).
While the mechanisms of action of theophylline are not known with certainty, studies in animals suggest that bronchodilatation is mediated by the inhibition of two isozymes of phosphodiesterase (PDE III and, to a lesser extent, PDE IV) while non-bronchodilator prophylactic actions are probably mediated through one or more different molecular mechanisms, that do not involve inhibition of PDE III or antagonism of adenosine receptors. Some of the adverse effects associated with theophylline appear to be mediated by inhibition of PDE III (e.g., hypotension, tachycardia, headache, and emesis) and adenosine receptor antagonism (e.g., alterations in cerebral blood flow).
Theophylline increases the force of contraction of diaphragmatic muscles. This action appears to be due to enhancement of calcium uptake through an adenosine-mediated channel.
Bronchodilation occurs over the serum theophylline concentration range of 5-20 mcg/mL. Clinically important improvement in symptom control has been found in most studies to require peak serum theophylline concentrations >10 mcg/mL, but patients with mild disease may benefit from lower concentrations. At serum theophylline concentrations >20 mcg/mL, both the frequency and severity of adverse reactions increase. In general, maintaining peak serum theophylline concentrations between 10 and 15 mcg/mL will achieve most of the drug’s potential therapeutic benefit while minimizing the risk of serious adverse events.
Overview Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form. Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver.
The pharmacokinetics of theophylline vary widely among similar patients and cannot be predicted by age, sex, body weight or other demographic characteristics. In addition, certain concurrent illnesses and alterations in normal physiology (see Table I) and co-administration of other drugs (see Table II) can significantly alter the pharmacokinetic characteristics of theophylline. Within-subject variability in metabolism has also been reported in some studies, especially in acutely ill patients. It is, therefore, recommended that serum theophylline concentrations be measured frequently in acutely ill patients (e.g., at 24-hr intervals) and periodically in patients receiving long-term therapy, e.g., at 6-12 month intervals. More frequent measurements should be made in the presence of any condition that may significantly alter theophylline clearance (see PRECAUTIONS, Laboratory Tests).
|Population characteristics|| Total body clearance* |
| Half-life |
|Premature neonates |
postnatal age 3-15 days
postnatal age 25-57 days
|0.29 (0.09-0.49) |
|30 (17-43) |
|Term infants |
postnatal age 1-2 days
postnatal age 3-30 weeks
|1.7 (0.5-2.9) |
|3.4 (1.2-5.6) |
|Adults (16-60 years) |
otherwise healthy non-smoking asthmatics
|0.65 (0.27-1.03)||8.7 (6.1-12.8)|
|Elderly (>60 years) |
non-smokers with normal cardiac, liver, and renal function
|0.41 (0.21-0.61)||9.8 (1.6-18)|
|Concurrent illness or altered physiological state|
|Acute pulmonary edema||0.33** (0.07-2.45)||19** (3.1-82)|
|COPD >60 years, stable non-smoker >1 year||0.54 (0.44-0.64)||11 (9.4-12.6)|
|COPD with cor pulmonale||0.48 (0.08-0.88)||NR†|
|Cystic fibrosis (14-28 years)||1.25 (0.31-2.2)||6.0 (1.8-10.2)|
|Fever associated with acute viral respiratory illness (children 9-15 years)||NR†||7.0 (1.0-13)|
|Liver disease — cirrhosis |
|0.31** (0.1-0.7) |
|32** (10-56) |
|Pregnancy — 1st trimester |
|8.5 (3.1-13.9) |
|Sepsis with multi- organ failure||0.47 (0.19-1.9)||18.8 (6.3-24.1)|
|Thyroid disease — hypothyroid |
|0.38 (0.13-0.57) |
|11.6 (8.2-25) |
|¶ For various North American patient populations from literature reports. Different rates of elimination and consequent dosage requirements have been observed among other peoples.|
|* Clearance represents the volume of blood completely cleared of theophylline by the liver in one minute. Values listed were generally determined at serum theophylline concentrations <20 mcg/mL; clearance may decrease and half-life may increase at higher serum concentrations due to non-linear pharmacokinetics.|
|†† Reported range or estimated range (mean ± 2 SD) where actual range not reported.|
|† NR = not reported or not reported in a comparable format.|
Note: In addition to the factors listed above, theophylline clearance is increased and half-life decreased by low carbohydrate/high protein diets, parenteral nutrition, and daily consumption of charcoal-broiled beef. A high carbohydrate/low protein diet can decrease the clearance and prolong the half-life of theophylline.
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