Theophylline

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Generic Name of Theophylline - Learn More

Theophylline

Theophylline Precaution - What You Need to Know

Before starting Theophylline, patients should be aware of the following precautions:
- Renal and Hepatic Impairment: Theophylline is metabolized in the liver and excreted via the kidneys, so patients with liver disease or kidney dysfunction may require a dose adjustment or closer monitoring due to altered drug metabolism and elimination.
- Cardiac Conditions: Caution is advised for patients with arrhythmias, heart failure, or other cardiovascular diseases. Theophylline can cause tachycardia and arrhythmias, particularly at higher concentrations.
- Seizure Disorders: Theophylline can lower the seizure threshold, making seizures more likely in individuals with a history of epilepsy or other seizure disorders.
- Smoking: Smoking can increase the metabolism of theophylline, requiring higher doses to achieve therapeutic levels. Conversely, cessation of smoking can lead to increased theophylline levels and potential toxicity.
- Elderly Population: Older adults may have decreased renal and hepatic function, increasing the risk of toxicity from theophylline. Monitoring drug levels and adjusting the dose is necessary.
- Pregnancy and Breastfeeding: Theophylline should only be used during pregnancy if clearly needed, as it can cross the placenta. It is excreted in breast milk, so consult a healthcare provider before using theophylline while breastfeeding.

Theophylline Indication - Uses and Benefits

Theophylline is prescribed for the following indications:
- Asthma: It is used as an adjunct treatment for asthma, particularly in individuals who are not adequately controlled by inhaled corticosteroids and bronchodilators.
- Chronic Obstructive Pulmonary Disease (COPD): Theophylline helps manage COPD symptoms, improving breathing by dilating the airways and reducing inflammation.
- Apnea of Prematurity: In neonatal care, theophylline is used to treat apnea of prematurity, a condition where premature infants stop breathing for short periods.
- Acute Bronchospasm: Theophylline can be used in severe cases of bronchospasm (e.g., from an asthma attack), often as a second-line agent when other treatments do not provide adequate relief.
- Chronic Bronchitis and Emphysema: It may help in managing symptoms of chronic bronchitis and emphysema, as part of a broader treatment regimen to improve airflow.

Theophylline Contraindications - Important Warnings

Theophylline is contraindicated in the following scenarios:
- Allergy to Theophylline: Individuals who are hypersensitive to theophylline or any component of the formulation should avoid its use.
- Acute Peptic Ulcer Disease: Theophylline may exacerbate gastric irritation, so it is not recommended for patients with active peptic ulcers.
- Severe Arrhythmias: Theophylline can worsen arrhythmias and should not be used in patients with severe cardiac arrhythmias or conditions like ventricular fibrillation.
- Severe Liver Disease: Patients with severe liver dysfunction may experience reduced metabolism of theophylline, leading to higher levels and increased risk of toxicity.
- Uncontrolled Seizure Disorders: Due to the risk of seizures, it is contraindicated in patients with poorly controlled epilepsy or history of seizures.

Theophylline Side Effects - What to Expect

Common side effects of theophylline include:
- Gastrointestinal Symptoms: Nausea, vomiting, epigastric pain, and heartburn.
- Central Nervous System Effects: Headache, insomnia, nervousness, tremors, and seizures (at higher doses).
- Cardiovascular: Tachycardia, arrhythmias (e.g., atrial fibrillation or supraventricular tachycardia).
- Diuresis: Increased urine production and dehydration may occur.
- Hypokalemia: Low potassium levels in the blood may result from increased renal excretion of potassium.
- Severe Toxicity: Symptoms of theophylline toxicity include arrhythmias, severe nausea, vomiting, seizures, and hypotension. Immediate medical attention is required if toxicity is suspected.

Theophylline Pregnancy Category ID - Safety Information

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Theophylline Mode of Action - How It Works

Theophylline works by relaxing the smooth muscles of the airways, dilating the bronchi and bronchioles, which helps to improve airflow and decrease wheezing. Its mechanism of action includes:
- Inhibition of Phosphodiesterase (PDE): Theophylline inhibits the enzyme phosphodiesterase, leading to increased levels of cyclic AMP (cAMP), which helps to relax bronchial smooth muscles.
- Adenosine Receptor Antagonism: Theophylline also works by blocking adenosine receptors in the lungs, leading to bronchodilation and reduced inflammation.
- Anti-inflammatory Effects: It may also have mild anti-inflammatory effects, reducing swelling in the airways and improving breathing.
- Increased Respiratory Muscle Strength: Theophylline may help improve the function of respiratory muscles, enhancing the ability to breathe effectively in individuals with respiratory conditions.

Theophylline Drug Interactions - What to Avoid

Theophylline has several known interactions with other medications, food, and substances:
- CYP450 Enzyme Inhibitors: Medications that inhibit CYP1A2 or CYP3A4 enzymes, such as cimetidine, fluoroquinolone antibiotics, and macrolides (e.g., erythromycin), can increase the levels of theophylline in the blood, raising the risk of toxicity.
- CYP450 Enzyme Inducers: Rifampin, carbamazepine, and phenobarbital can increase the clearance of theophylline, reducing its effectiveness.
- Beta-blockers: The combination of theophylline with beta-blockers may increase the risk of arrhythmias.
- Alcohol: Chronic alcohol consumption can increase the metabolism of theophylline, whereas acute alcohol consumption may increase its side effects, including toxicity.
- Food: High-protein diets can increase the metabolism of theophylline, while high-fat meals can reduce its absorption.

Theophylline Adult Dose - Recommended Dosage

Theophylline dosing varies based on patient condition, serum drug levels, and individual response. Typical dosing guidelines include:
- For Asthma/COPD: The initial dose often ranges from 300 to 400 mg/day, divided into multiple doses, with adjustments made based on serum theophylline levels.
- For Acute Bronchospasm: An initial loading dose of 5 mg/kg may be given intravenously (if injectable form) or orally, followed by maintenance dosing based on serum concentration.
- Therapeutic Serum Concentration: The target therapeutic range is typically 10–20 mcg/mL. Adjust doses to maintain this range for optimal efficacy and to avoid toxicity.

Theophylline Child Dose - Dosage for Children

For pediatric patients, the dosing of theophylline is based on weight and clinical condition. The usual pediatric doses are:
- For Asthma or Chronic Bronchitis: The dose is typically 10–15 mg/kg/day, divided into two or three doses.
- For Premature Neonates with Apnea: The initial dose is typically 2–3 mg/kg every 24 hours, with adjustments based on clinical response and serum levels.
- Serum drug levels are especially important in children to avoid both under-dosing (ineffective treatment) and over-dosing (toxicity).

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Important Note:
Always consult a healthcare provider before starting Theophylline therapy, particularly for dosing adjustments and to ensure safe use in the presence of any comorbid conditions or drug interactions. Regular monitoring of serum theophylline levels is essential for preventing toxicity and ensuring therapeutic effectiveness.

Theophylline Renal Dose - Dosage for Kidney Conditions

For patients with renal impairment, theophylline metabolism may be affected, and the drug should be used with caution. Renal dose adjustments may be necessary:
- Mild to Moderate Renal Dysfunction: Monitor theophylline serum levels and adjust doses accordingly.
- Severe Renal Dysfunction: Dose reduction is recommended, and serum theophylline levels should be carefully monitored to avoid toxicity.