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theophylline (Rx)Brand and Other Names:Theo 24, Theochron, more...Elixophyllin, aminophylline, Uniphyl

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule, extended-release (24 hours)

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

tablet, extended release (12 hours)

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

tablet, extended-release (24 hours)

  • 400mg
  • 600mg

oral elixir

  • 80mg/15mL

intravenous solution

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

Acute Bronchospasm

Loading

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

Maintenance

  • 0.4-0.6 mg/kg/hr IV or 4.8-7.2 mg/kg PO (extended release) q12hr to maintain levels 10-15 mg/L  
  • Smokers: 0.79 mg/kg/hr IV for next 12 hours after loading dose, then 0.63 mg/kg/hr or 5 mg/kg PO (extended release) q8hr
  • Coadmininstration with drugs that decrease theophylline clearance (eg, cimetidine, ciprofloxacin, and erythromycin and other macrolides): 0.2-0.3 mg/kg/hr IV or PO (extended release) q12-24hr
  • Congestive heart failure: 0.39 mg/kg/hr IV for next 12 hours after loading dose, then 0.08-0.16 mg/kg/hr
  • Aminophylline: 3.125 mg/kg PO q6hr

Dosing Considerations

If administering aminophylline, increase dose by 25% (aminophylline is approximately 79-86% theophylline;)

For PO 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/hr IV for next 12 hours, then 0.08-0.16 mg/kg/hr  

Dosage Forms & Strengths

capsule, extended-release (24 hours)

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

tablet, extended-release (12 hours)

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

tablet, extended-release (24 hours)

  • 400mg
  • 600mg

oral elixir

  • 80mg/15mL

intravenous solution

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

Bronchospasm

Loading

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

Maintenance

  • 1.5-6 months: 0.5 mg/kg/hr IV or 10 mg/kg/day PO in divided doses  
  • 6-12 months: 0.6-0.7 mg/kg/hr IV or 12-18 mg/kg/day PO in divided doses
  • 1-9 years: 1 mg/kg/hr IV or 8 mg/kg PO (extended release) q8hr
  • 9-12 years: 0.8-0.9 mg/kg/hr IV or 6.4 mg/kg PO (extended release) q8hr
  • 12-16 years: 0.7 mg/kg/hr IV or 5.6 mg/kg PO (extended release) q8hr

Neonatal Apnea

Loading: 4-5 mg/kg PO/IV once  

Maintenance: 3-6 mg/kg/day PO/IV divided q8hr

Dosing Considerations

If administering aminophylline, increase dose by 20-25% (aminophylline is approximately 79-86% theophylline)

Use ideal body weight to calculate dose

1 mg/kg results in 2 mg/L (34.4 mmol/L) increase in serum theophylline

Acute Bronchospasm

After loading dose, 0.47 mg/kg/hr IV for next 12 hours, then 0.24 mg/kg/hr  

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Interactions

Interaction Checker

theophylline and

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     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Peak serum concentration <20 mcg/mL

            • Central nervous system excitement, headache, insomnia, irritability, restlessness, seizure
            • Diarrhea, nausea, vomiting
            • Diuresis (transient)
            • Exfoliative dermatitis
            • Skeletal muscle tremors
            • Tachycardia, flutter
            • Hypercalcemia (with concomitant hyperthyroid disease)
            • Difficulty urinating (elderly males with prostatism)

            Peak serum concentration >30 mcg/mL

            • Acute myocardial infarction
            • Seizures (resistant to anticonvulsants)
            • Urinary retention
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            Warnings

            Contraindications

            Hypersensitivity

            Cautions

            Patients, who develop CNS abnormalities, reported (rarely) to experience nonconvulsive status epilepticus

            Theophylline clearance may decrease in patients with congestive heart failure, acute pulmonary edema, hepatic disease, cor pulmonale, acute hepatitis, hypothyroidism, cirrhosis, fever, or sepsis with multiorgan failure and shock

            Use with caution in patients with hyperthyroidism, seizure disorder, peptic ulcer, or cardiovascular disease

            Some dosage forms may contain propylene glycol; use caution; seizures, hyperosmolality, lactic acidosis, and respiratory depression reported associated with use of large amounts of propylene glycol

            Measure serum levels and withhold subsequent doses if patient develops signs and symptoms of theophylline toxicity

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Theophylline is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing human infants; serious adverse effects in infant are unlikely unless mother has toxic serum theophylline concentration

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            Theophylline relaxes smooth muscles of respiratory tract and suppresses the response of the airways to stimuli

            May increase tissue concentration of cyclic adenine monophosphate (cAMP) by inhibiting 2 isoenzymes of phosphodiesterase (PDE III and, to a lesser extent, PDE IV), which ultimately induces release of epinephrine from the adrenal medulla cells

            Absorption

            Onset: Variable

            Duration: Variable

            Peak plasma time: 1-2 hr

            Peak plasma concentration: 10 mcg/mL

            Distribution

            Protein bound: 40-55%

            Vd: 0.3-0.7 L/kg

            Metabolism

            Metabolized in liver by CYP1A2 and CYP3A4

            Metabolites: 1,3-Dimethyluric acid, 1-methyluric acid, 3-methylxanthine

            Elimination

            Half-life: Nonsmoker, 8 hr; smoker, 4-5 hr

            Clearance: 1.45 mL/min/kg

            Excretion: Urine

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            Administration

            IV Incompatibilities

            Additive: Clindamycin, dobutamine, epinephrine, erythromycin, meperdine, morphine, norepinephrine, vancomycin, vitamins B and C

            Y-site: Amiodarone, dobutamine, fenoldopam

            Not specified: Carbenicillin, tetracycline

            IV Compatibilities

            Additive: Calcium gluconate, dopamine, esmolol, heparin, hydrocortisone, hydroxyzine, lidocaine, nitroglycerin, pentobarbital, potassium chloride, sodium bicarbonate, verapamil

            Syringe: Heparin, pentobarbital

            Y-site: Ampicillin, cefazolin, esmolol, heparin, potassium chloride, vitamins B and C

            Not specified: Diazepam

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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