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Theophylline

Medical and Pharmacy Editor:

Brand Name: Theo 24, Theochron, Elixophyllin, aminophylline, Uniphyl

Generic Name: Theophylline

Drug Class: Xanthine Derivatives; Phosphodiesterase Enzyme Inhibitors, Nonselective

What Is Theophylline and How Does It Work?

Theophylline is used to treat lung diseases such as asthma and COPD (bronchitis, emphysema). It must be used regularly to prevent wheezing and shortness of breath. This medication belongs to a class of drugs known as xanthines. It works in the airways by relaxing muscles, opening breathing passages, and decreasing the lungs' response to irritants. Controlling symptoms of breathing problems can decrease time lost from work or school.

Theophylline must be used regularly to be effective. It does not work right away and should not be used to relieve sudden breathing problems. If sudden shortness of breath occurs, use your quick-relief inhaler as prescribed.

Theophylline is available under the following different brand names: Theo 24, Theochron, Elixophyllin, aminophylline, and Uniphyl.

Dosages of Theophylline

Dosage Forms and Strengths

Capsule, extended-release (24 hours)

  • 100 mg
  • 200 mg
  • 300 mg
  • 400 mg

Tablet, extended release (12 hours)

  • 100 mg
  • 200 mg
  • 300 mg
  • 450 mg

Tablet, extended-release (24 hours)

  • 400 mg
  • 600 mg

Oral elixir

  • 80 mg/15mL

Intravenous solution

  • 400 mg/250mL D5W
  • 400 mg/500mL D5W
  • 800 mg/500mL D5W

Dosage Considerations – Should be Given as Follows:

Acute Bronchospasm

Adult:

Load

  • Patients not currently taking theophylline: 5-7 mg/kg intravenously/orally; not to exceed 25 mg/min intravenously (IV)
  • Aminophylline: 6-7 mg/kg intravenously/orally; IV infused over 20 minutes

Maintenance

  • 0.4-0.6 mg/kg/hour intravenously (IV) or 4.8-7.2 mg/kg orally (extended release) every 12 hours to maintain levels 10-15 mg/L
  • Smokers: 0.79 mg/kg/hour IV for next 12 hours after loading dose, then 0.63 mg/kg/hour or 5 mg/kg orally (extended release) every 8 hours
  • Coadmininstration with drugs that decrease theophylline clearance (e.g., cimetidine, ciprofloxacin, and erythromycin and other macrolides): 0.2-0.3 mg/kg/hour IV or orally (extended release) every 12-24 hours
  • Congestive heart failure: 0.39 mg/kg/hour IV for next 12 hours after loading dose, then 0.08-0.16 mg/kg/hour
  • Aminophylline: 3.125 mg/kg orally every 6 hours

Pediatric:

Load

  • No theophylline administered in previous 24 hours: 5-7 mg/kg intravenously/orally; IV infused over 20-30 minutes

Maintenance

  • 1.5-6 months: 0.5 mg/kg/ hour intravenously (IV) or 10 mg/kg/day orally in divided doses
  • 6-12 months: 0.6-0.7 mg/kg/ hour IV or 12-18 mg/kg/day orally in divided doses
  • 1-9 years: 1 mg/kg/ hour IV or 8 mg/kg orally (extended release) every 8 hours
  • 9-12 years: 0.8-0.9 mg/kg/ hour IV or 6.4 mg/kg orally (extended release) every 8 hours
  • 12-16 years: 0.7 mg/kg/ hour IV or 5.6 mg/kg orally (extended release) every 8 hours

Neonatal Apnea

  • Loading: 4-5 mg/kg orally/intravenously (IV) once
  • Maintenance: 3-6 mg/kg/day orally/IV divided every 8 hours
  • Dosing Considerations
  • If administering aminophylline, increase dose by 25% (aminophylline is approximately 79-86% theophylline)
  • For oral loading, use immediate-release theophylline or aminophylline
  • If patient is already taking theophylline, give smaller loading dose
  • Use ideal body weight to calculate dose
  • 1 mg/kg results in 2 mg/L (34.4 mmol/L) increase in serum theophylline
  • Therapeutic range: 10-20 mg/L (172-344 mmol/L)

Dosing Modifications

  • Hepatic impairment: After loading dose, 0.39 mg/kg/hour intravenously (IV) for next 12 hours, then 0.08-0.16 mg/kg/hour

What Are Side Effects Associated with Using Theophylline?

Side effects of theophylline at peak serum concentration less than 20 mcg/mL include:

Side effects of theophylline at peak serum greater than 20 mcg/mL include:

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

What Other Drugs Interact with Theophylline?

If your doctor has directed you to use this medication for your condition, your doctor or pharmacist may already be aware of any possible drug interactions or side effects and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any medicine before getting further information from your doctor, healthcare provider or pharmacist first.

Severe Interactions of theophylline include:

  • dipyridamole
  • febuxostat
  • riociguat

Theophylline has serious interactions with at least 23 different drugs.

Theophylline has moderate interactions with at least 145 different drugs.

Theophylline has mild interactions with at least 26 different drugs.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

What Are Warnings and Precautions for Theophylline?

Warnings

This medication contains theophylline. Do not take Theo 24, Theochron, Elixophyllin, aminophylline, or Uniphyl if you are allergic to theophylline or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

  • Hypersensitivity

Effects of Drug Abuse

  • No information available

Short-Term Effects

  • See "What Are Side Effects Associated with Using Theophylline?"

Long-Term Effects

  • See "What Are Side Effects Associated with Using Theophylline?"

Cautions

Pregnancy and Lactation

  • Use theophylline with caution during pregnancy if benefits outweigh risks. Animal studies show risk and human studies are not available or neither animal nor human studies were done.
  • It is not known if theophylline is excreted in breast milk; its effect on nursing infants is not known. Consult your doctor before breastfeeding.
Reviewed on 1/10/2018


Medscape. Theophylline.
https://reference.medscape.com/drug/theo-24-theochron-theophylline-343447

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