Theophylline

What is Theophylline?

• Theophylline is a xanthine derivative, a phosphodiesterase inhibiting drug used to prevent and treat wheezing, shortness of breath, and chest tightness caused by asthma, chronic bronchitis, emphysema, and other lung diseases.

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Theophylline

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Theophylline 3D ball

What are the uses of this medicine?

• Theophylline is used for the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.

How does this medicine work?

• Theophylline (thee of' i lin) is an effective bronchodilator and is widely used in treatment of acute attacks of asthma and in chronic management of bronchospasm in patients with asthma and chronic obstructive pulmonary disease.
• 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).
• Bronchodilation 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.
• 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.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• a history of hypersensitivity to theophylline or other components in the product.

What drug interactions can this medicine cause?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Be sure to mention any of the following:

• allopurinol (Zyloprim)
• azithromycin (Zithromax)
• carbamazepine (Tegretol)
• cimetidine (Tagamet)
• ciprofloxacin (Cipro)
• clarithromycin (Biaxin)
• diuretics ('water pills')
• erythromycin
• lithium (Eskalith, Lithobid)
• oral contraceptives
• phenytoin (Dilantin)
• prednisone (Deltasone)
• propranolol (Inderal)
• rifampin (Rifadin)
• tetracycline (Sumycin)
• other medications for infections or heart disease.

Is this medicine FDA approved?

• Theophylline was approved for use in the United States in 1982 and is available in multiple generic forms for oral and intravenous use.

How should this medicine be used?

Recommended dosage:

• Typical dose regimens are 100 to 300 mg three to four times daily.
• Dosage is highly individualized.

1 Starting Dosage:

• In Children < 45 kg:12-14 mg/kg/day up to a maximum(300 mg/day divided Q8-12 hrs*)

Children > 45 kg and adults:

• 300 mg/day divided Q8-12 hrs*

Administration:

• Theophylline comes as an extended-release (long-acting) tablet, extended-release capsule, and a solution (liquid) to take by mouth.
• It usually is taken every 6, 8, 12, or 24 hours.
• Take this medication with a full glass of water on an empty stomach, at least 1 hour before or 2 hours after a meal.
• Extended-release capsules (e.g., Theo-Dur Sprinkles) may be swallowed whole or opened and the contents mixed with soft food and swallowed without chewing.
• Swallow the extended-release tablets whole; do not chew or crush them.
• Theophylline controls symptoms of asthma and other lung diseases but does not cure them.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Theophylline comes as an extended-release (long-acting) tablet, extended-release capsule, and a solution (liquid)

This medicine is available in fallowing brand namesː

• Theophylline is marketed under multiple brand names including Asmalix, Elixophyllin, Quibron-T, Respbid, Theobid, Duracaps, and Uniphyl.

What side effects can this medication cause?

The most common side effects of this medicine include:

• Vomiting
• Abdominal Pain
• Diarrhea
• Hematemesis
• Hypokalemia
• Hyperglycemia
• Acid/base disturbance
• Rhabdomyolysis
• Sinus tachycardia
• tachycardias
• Ventricular premature beats
• Atrial fibrillation or flutter
• Multifocal atrial tachycardia
• Ventricular arrhythmias wit hemodynamic instability
• Hypotension/shock

What special precautions should I follow?

• The patient (or parent/care giver) should be instructed to seek medical advice whenever nausea, vomiting, persistent headache, insomnia or rapid heart beat occurs during treatment with theophylline, even if another cause is suspected.
• Patients should be instructed to not alter the dose, timing of the dose, or frequency of administration without first consulting their clinician. If a dose is missed, the patient should be instructed to take the next dose at the usually scheduled time and to not attempt to make up for the missed dose.
• Theophylline should be used with extreme caution in patients with the following clinical conditions due to the increased risk of exacerbation of the concurrent condition: Active peptic ulcer disease; Seizure disorders; Cardiac arrhythmias (not including bradyarrhythmias)
• Increases in the dose of theophylline should not be made in response to an acute exacerbation of symptoms of chronic lung disease since theophylline provides little added benefit to inhaled beta2-selective agonists and systemically administered corticosteroids in this circumstance and increases the risk of adverse effects.
• The dose of theophylline selected for initiation of therapy should be low and, if tolerated, increased slowly over a period of a week or longer with the final dose guided by monitoring serum theophylline concentrations and the patient's clinical response.
• Theophylline is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing human infants.
• Theophylline is widely used in therapy of asthma and is not believed to cause liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• seizures
• cardiac arrhythmias
• increases in serum calcium
• creatine kinase
• myoglobin and leukocyte count
• decreases in serum phosphate and magnesium
• acute myocardial infarction
• urinary retention

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• CATEGORY C.
• There are no adequate and well controlled studies in pregnant women.

Can this medicine be used in children?

• Theophylline is safe and effective for the approved indications in pediatric patients.

What are the active and inactive ingredients in this medicine?

Active ingredients:

• Theophylline, anhydrous

Inactive Ingredients:

• black iron oxide
• butylparaben
• castor oil
• edetate calcium disodium
• ethylcellulose
• gelatin
• methylparaben
• pharmaceutical glaze
• povidone
• propylparaben
• sodium lauryl sulfate
• sodium propionate
• starch
• sugar spheres
• talc

Who manufactures and distributes this medicine?

• Inwood Laboratories, Inc.
• Subsidiary of FOREST LABORATORIES, INC.
• Inwood, New York

What should I know about storage and disposal of this medication?

• Store at controlled room temperature 15° - 30°C (59°- 86°F).

• Dailymed label info on Theophylline
• FDA Theophylline

Beta-2 Adrenergic Agonists

Albuterol, Bitolterol, Formoterol, Metaproterenol, Pirbuterol, Salbutamol, Salmeterol, Terbutaline

Leukotriene Receptor Antagonists

Montelukast, Zafirlukast

Monoclonal Antibodies

Benralizumab, Mepolizumab, Omalizumab, Reslizumab

Xanthine Derivatives

Theophylline Zileuton

• Dailymed label info on Theophylline
• FDA Theophylline