Theophylline

Theophylline is a prescription medication used to treat chronic (ongoing) lung diseases such as asthma, and chronic obstructive pulmonary disease (COPD) which includes emphysema, and chronic bronchitis.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Do not take theophylline in larger or smaller amounts or for longer than recommended. Theophylline overdose can occur if you accidentally take too much at one time, or if your daily doses are too high. To be sure you are using the correct dose, your blood will need to be tested often.

Do not start or stop smoking without first talking to your doctor. Smoking changes the way your body uses theophylline, and you may need to use a different dose.

Sometimes it is not safe to use certain drugs at the same time. Many drugs can interact with theophylline. Tell your doctor about all other medicines you use. Also tell your doctor if you start or stop using any of your other medications.

Stop using theophylline and call your doctor at once if you have severe or continued vomiting, rapid heartbeats, confusion, tremors, or seizure.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using theophylline and call your doctor at once if you have a serious side effect such as:

• severe or continued vomiting;

• rapid or uneven heartbeats;

• seizure (convulsions);

• confusion, tremors or shaking;

• nausea and vomiting, severe headache, rapid heart rate;

• low potassium (confusion, uneven heart rate, extreme thirst, increased urination, leg discomfort, muscle weakness or limp feeling); or

• high blood sugar (increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss).

Less serious side effects may include:

• stomach pain, diarrhea, upset stomach;

• headache;

• sweating;

• sleep problems (insomnia); or

• feeling restless, nervous, or irritable;

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Theophylline extended-release tablets are contraindicated in patients with a history of hypersensitivity to Theophylline or other components in the product.

Theophylline Extended-Release Tablets 300 mg (30 Tablets in 1 Bottle)
Each uncoated extended-release tablet contains: Theophylline (Anhydrous) USP 300 mg
62332-025-30

• Phosphodiesterase Enzyme Inhibitor, Nonselective

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: Rapid and complete with up to 100% absorption depending upon the formulation used

Distribution

0.45 L/kg (range: 0.3 to 0.7 L/kg) based on ideal body weight; distributes poorly into body fat; Vd may increase in premature neonates, patients with hepatic cirrhosis, acidemia (uncorrected), the elderly

Metabolism

Hepatic via demethylation (CYP 1A2) and hydroxylation (CYP 2E1 and 3A4); theophylline is metabolized to active metabolites, caffeine and 3-methylxanthine; in neonates this theophylline-derived caffeine accumulates due to decreased hepatic metabolism and significant concentrations of caffeine may occur; a substantial decrease in serum caffeine concentrations occurs after 40 weeks postmenstrual age

Excretion

Urine:

Neonates: 50% as unchanged theophylline

Children >3 months and Adults: ~10% as unchanged theophylline

Clearance: Note: Maturation of clearance in premature infants and term infants is most closely related to postconceptional age (PCA); adult clearance values are reached at approximately 55 weeks PCA and higher pediatric values at approximately 60 weeks PCA (Kraus1993).

Premature infants, postnatal age 3 to 15 days: 0.29 mL/kg/minute

Premature infants, postnatal age 25 to 27 days: 0.64 mL/kg/minute

Children 1 to 4 years: 1.7 mL/kg/minute

Children 4 to 12 years: 1.6 mL/kg/minute

Children 13 to 15 years: 0.9 mL/kg/minute

Children 16 to 17 years: 1.4 mL/kg/minute

Adults ≥18 years to ≤ 60 years (nonsmoking, asthmatic): 0.65 mL/kg/minute

Adults >60 years (nonsmoking, healthy): 0.41mL/kg/minute

Acute pulmonary edema: 0.33 mL/kg/minute

Cystic fibrosis (14 to 28 years): 1.25 mL/kg/minute

Acute hepatitis: 0.35 mL/kg/minute

Cholestasis: 0.65 mL/kg/minute

Cirrhosis: 0.31 mL/kg/minute

Sepsis with multiorgan failure: 0.46 mL/kg/minute

Hypothyroid: 0.38 mL/kg/minute

Hyperthyroid: 0.8 mL/kg/minute

Oral: IV:

Infants 1 to 3 months: Consider dose reduction and frequent monitoring of serum theophylline concentrations.

Infants >3 months, Children, Adolescents, and Adults: No dosage adjustment necessary.

Oral: Infants, Children, Adolescents, and Adults: No dosage adjustment provided in manufacturer’s labeling. However, dose reduction and frequent monitoring of serum theophylline concentration are required in patients with decreased hepatic function (eg, cirrhosis, acute hepatitis, cholestasis). Maximum dose: 400 mg daily

IV: Infants, Children, Adolescents, and Adults: Initial: 0.2 mg/kg/hour; maximum daily dose: 400 mg daily unless serum concentrations indicate need for larger dose. Use with caution and monitor serum theophylline concentrations frequently.

IV: Administer loading dose over 30 minutes; follow with a continuous infusion as appropriate

Oral: Long-acting preparations should be taken with a full glass of water, swallowed whole, or cut in half if scored. Do not crush. Extended release capsule forms may be opened and the contents sprinkled on soft foods; do not chew beads.