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Drug Description

THEOPHYLLINE IN DEXTROSE
(theophylline anhydrous) Injection, Solution
USP in Plastic Container
VIAFLEX Plus Container

DESCRIPTION

Theophylline in 5% Dextrose Injection, USP is a sterile, nonpyrogenic solution of Theophylline, Anhydrous, USP in 5% Dextrose Injection. It contains no antimicrobial agents. 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 1H-Purine-2,6-dione,3,7-dihydro-1,3-dimethyl-, and is represented by the following structural formula:

Theophylline Structural Formula Illustration

The molecular formula of anhydrous theophylline is C7H8N4O2 with a molecular weight of 180.17. Dextrose Hydrous, USP has the chemical name D-Glucose monohydrate and is represented by the following structural formula:

Dextrose Hydrous Structural Formula Illustration

Theophylline in 5% Dextrose Injection, USP is intended for intravenous administration. Composition, osmolarity, pH and caloric content are shown in Table I.

Table I.

  Size (mL) Composition Osmolarity* (mOsmol/L) (calc) pH Caloric Content (kcal/L)
Theophylline Anhydrous, USP (mg/container) Dextrose Hydrous, USP(g/L)
200 mg Theophyllinein
5% Dextrose Injection, USP
50 200 50 275 4.5(3.5 to 6.5) 170
100 200 50 263 4.5(3.5 to 6.5) 170
400 mg Theophylline in 5% Dextrose Injection, USP 100 400 50 275 4.5 (3.5 to 6.5) 170
250 400 50 261 4.5 (3.5 to 6.5) 170
500 400 50 257 4.5 (3.5 to 6.5) 170
1000 400 50 255 4.5 (3.5 to 6.5) 170
800 mg Theophylline in 5% Dextrose Injection, USP 250 800 50 270 4.5 (3.5 to 6.5) 170
500 800 50 261 4.5 (3.5 to 6.5) 170
1000 800 50 257 4.5 (3.5 to 6.5) 170
*Normal physiologic osmolarity range is approximately 280 to 310 mOsmol/L. Administration of substantially hypertonic solutions ( ≥ 600 mOsmol/L) may cause vein damage.

This VIAFLEX Plus plastic container is fabricated from a specially formulated polyvinyl chloride (PL 146 Plastic). VIAFLEX Plus on the container indicates the presence of a drug additive in a drug vehicle. The VIAFLEX Plus plastic container system utilizes the same container as the VIAFLEX plastic container system. The amount of water that can permeate from inside the container into the overwrap is insufficient to affect the solution significantly. Solutions in contact with the plastic container can leach out certain of its chemical components in very small amounts within the expiration period, e.g., di-2-ethylhexyl phthalate (DEHP), up to 5 parts per million. However, the safety of the plastic has been confirmed in tests in animals according to USP biological tests for plastic containers as well as by tissue culture toxicity studies.

Indications & Dosage

INDICATIONS

Intravenous theophylline is indicated as an adjunct to inhaled beta-2 selective agonists and systemically administered corticosteroids for the treatment of acute exacerbations of the symptoms and reversible airflow obstruction associated with asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.

DOSAGE AND ADMINISTRATION

General Considerations

The steady-state peak serum theophylline concentration is a function of the infusion rate and the rate of theophylline clearance in the individual patient. Because of marked individual differences in the rate of theophylline clearance, the dose required to achieve a serum theophylline concentration in the 10-20 mcg/mL range varies fourfold among otherwise similar patients in the absence of factors known to alter theophylline clearance. For a given population there is no single theophylline dose that will provide both safe and effective serum concentrations for all patients. Administration of the median theophylline dose required to achieve a therapeutic serum theophylline concentration in a given population may result in either sub-therapeutic or potentially toxic serum theophylline concentrations in individual patients. The dose of theophylline must be individualized on the basis of peak serum theophylline concentration measurements in order to achieve a dose that will provide maximum potential benefit with minimal risk of adverse effects.

When theophylline is used as an acute bronchodilator, the goal of obtaining a therapeutic serum concentration is best accomplished with an intravenous loading dose. Because of rapid distribution into body fluids, the serum concentration (C) obtained from an initial loading dose (LD) is related primarily to the volume of distribution (V), the apparent space into which the drug diffuses:

C = LD/V

If a mean volume of distribution of about 0.5 L/kg is assumed (actual range is 0.3 to 0.7 L/kg), each mg/kg (ideal body weight) of theophylline administered as a loading dose over 30 minutes results in an average 2 mcg/mL increase in serum theophylline concentration. Therefore, in a patient who has received no theophylline in the previous 24 hours, a loading dose of intravenous theophylline of 4.6 mg/kg, calculated on the basis of ideal body weight and administered over 30 minutes, on average, will produce a maximum post-distribution serum concentration of 10 mcg/mL with a range of 6-16 mcg/mL. When a loading dose becomes necessary in the patient who has already received theophylline, estimation of the serum concentration based upon the history is unreliable, and an immediate serum level determination is indicated. The loading dose can then be determined as follows:

D = (Desired C - Measured C)(V)

where D is the loading dose, C is the serum theophylline concentration, and V is the volume of distribution. The mean volume of distribution can be assumed to be 0.5 L/kg and the desired serum concentration should be conservative (e.g., 10 mcg/mL) to allow for the variability in the volume of distribution. A loading dose should not be given before obtaining a serum theophylline concentration if the patient has received any theophylline in the previous 24 hours.

A serum concentration obtained 30 minutes after an intravenous loading dose, when distribution is complete, can be used to assess the need for and size of subsequent loading doses, if clinically indicated, and for guidance of continuing therapy. Once a serum concentration of 10 to 15 mcg/mL has been achieved with the use of a loading dose(s), a constant intravenous infusion is started. The rate of administration is based upon mean pharmacokinetic parameters for the population and calculated to achieve a target serum concentration of 10 mcg/mL (see Table VI). For example, in nonsmoking adults, initiation of a constant intravenous theophylline infusion of 0.4 mg/kg/hr at the completion of the loading dose, on average, will result in a steady-state concentration of 10 mcg/ mL with a range of 7-26 mcg/mL. The mean and range of steady-state serum concentrations are similar when the average child (age 1 to 9 years) is given a loading dose of 4.6 mg/kg theophylline followed by a constant intravenous infusion of 0.8 mg/kg/ hr. Since there is large interpatient variability in theophylline clearance, serum concentration will rise or fall when the patient's clearance is significantly different from the mean population value used to calculate the initial infusion rate. Therefore, a second serum concentration should be obtained one expected half-life after starting the constant infusion (e.g., approximately 4 hours for children age 1 to 9 and 8 hours for nonsmoking adults; See Table II for the expected half-life in additional patient populations) to determine if the concentration is accumulating or declining from the post loading dose level. If the level is declining as a result of a higher than average clearance, an additional loading dose can be administered and/or the infusion rate increased. In contrast, if the second sample demonstrates a higher level, accumulation of the drug can be assumed, and the infusion rate should be decreased before the concentration exceeds 20 mcg/mL. An additional sample is obtained 12 to 24 hours later to determine if further adjustments are required and then at 24-hour intervals to adjust for changes, if they occur. This empiric method, based upon mean pharmacokinetic parameters, will prevent large fluctuations in serum concentration during the most critical period of the patient's course.

In patients with cor pulmonale, cardiac decompensation, or liver dysfunction, or in those taking drugs that markedly reduce theophylline clearance (e.g., cimetidine), the initial theophylline infusion rate should not exceed 17 mg/hr unless serum concentrations can be monitored at 24-hour intervals. In these patients, 5 days may be required before steady-state is reached.

Theophylline distributes poorly into body fat, therefore, mg/kg dose should be calculated on the basis of ideal body weight. Table VI contains initial theophylline infusion rates following an appropriate loading dose recommended for patients in various age groups and clinical circumstances. Table VII contains recommendations for final theophylline dosage adjustment based upon serum theophylline concentrations. Application of these general dosing recommendations to individual patients must take into account the unique clinical characteristics of each patient. In general, these recommendations should serve as the upper limit for dosage adjustments in order to decrease the risk of potentially serious adverse events associated with unexpected large increases in serum theophylline concentration.

Table VI : Initial theophylline infusion rates following an appropriate loading dose.

Patient population Age Theophylline infusion rate (mg/kg/hr)*†
Neonates Postnatal age up to 24 days 1 mg/kg q12h/‡
Postnatal age beyond 24 days 1.5 mg/kg q 12h/‡
Infants 6-52 weeks old mg/kg/hr = (0.008) (age in weeks) + 0.21
Young children 1-9 years 0.8
Older children 9-12 years 0.7
Adolescents (cigarette or marijuana smokers) 12-16 years 0.7
Adolescents (nonsmokers) 12-16 years 0.5§
Adults (otherwise healthy nonsmokers) 16-60 years 0.4§
Elderly >60 years 0.3¶
Cardiac decompensation, cor pulmonale, liver dysfunction, sepsis with multi-organ failure, or shock   0.2¶
* To achieve a target concentration of 10 mcg/mL. Use ideal body weight for obese patients.
† Lower initial dosage may be required for patients receiving other drugs that decrease theophylline clearance (e.g., cimetidine).
‡ To achieve a target concentration of 7.5 mcg/mL for neonatal apnea.
§ Not to exceed 900 mg/day, unless serum levels indicate the need for a larger dose.
¶ Not to exceed 400 mg/day, unless serum levels indicate the need for a larger dose.

Table VII : Final dosage adjustment guided by serum theophylline concentration.

Peak Serum Concentration Dosage Adjustment


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