pharmacopeia
GET
/api/v1/drug/theophylline
2D structure
1,3-dimethyl-7H-purine-2,6-dione
SMILES CN1C2=C(C(=O)N(C1=O)C)NC=N2
InChIKey ZFXYFBGIUFBOJW-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action class: Phosphodiesterase Inhibitors.

Phosphodiesterase

Indications

Sourced from openFDA
  • Theophylline extended-release tablets are indicated 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.ICD-10: J20.9, J45.909

Contraindications

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

Dosage & administration

Sourced from openFDA

Taking theophylline extended-release tablets immediately after a high-fat content meal may result in a somewhat higher C max and delayed T max and somewhat greater extent of absorption. However, the differences are usually not great and this product may normally be administered without regard to meals (see CLINICAL PHARMACOLOGY, Drug interactions, Drug-Food Interactions ). Theophylline extended-release tablets are recommended for chronic or long-term management and prevention of symptoms, and not for use in treating acute symptoms of asthma and reversible bronchospasm. General considerations: The steady-state peak serum theophylline concentration is a function of the dose, the dosing interval, and the rate of theophylline absorption and clearance in the individual patient. Because of marked individual differences in the rate of theophylline clearance, the dose required to achieve a peak serum theophylline concentration in the 10-20 mcg/mL range varies fourfold among otherwise similar patients in the absence of factors known to alter theophylline clearance (e.g., 400- 1600 mg/day in adults <60 years old and 10-36 mg/kg/day in children 1-9 years old). For a given population there is no single theophylline dose that will provide both safe and effective serum concentrations for all patients. Administration of the median theophylline dose required to achieve a therapeutic serum theophylline concentration in a given population may result in either sub-therapeutic or potentially toxic serum theophylline concentrations in individual patients.

Warnings & precautions

Sourced from openFDA

Concurrent Illness: 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) Conditions that Reduce Theophylline Clearance: There are several readily identifiable causes of reduced theophylline clearance. If the total daily dose is not appropriately reduced in the presence of these risk factors, severe and potentially fatal theophylline toxicity can occur. Careful consideration must be given to the benefits and risks of theophylline use and the need for more intensive monitoring of serum theophylline concentrations in patients with the following risk factors: Age: Neonates (term and premature), Children <1 year, Elderly (>60 years) Concurrent Diseases: Acute pulmonary edema, congestive heart failure, cor-pulmonale, fever (≥102° for 24 hours or more; or lesser temperature elevations for longer periods), reduced renal function in infants <3 months of age, sepsis with multi-organ failure and shock. Cessation of Smoking Drug Interactions: Adding a drug that inhibits theophylline metabolism (e.g., cimetidine, erythromycin, tacrine) or stopping a concurrently administered drug that enhances theophylline metabolism (e.g., carbamazepine, rifampin). (see PRECAUTIONS, Drug Interactions, Table II ).

Adverse reactions

Sourced from openFDA

Adverse reactions associated with theophylline are generally mild when peak serum theophylline concentrations are <20 mcg/mL and mainly consist of transient caffeine-like adverse effects such as nausea, vomiting, headache, and insomnia. When peak serum theophylline concentrations exceed 20 mcg/mL, however, theophylline produces a wide range of adverse reactions including persistent vomiting, cardiac arrhythmias, and intractable seizures which can be lethal (see OVERDOSAGE ). The transient caffeine-like adverse reactions occur in about 50% of patients when theophylline therapy is initiated at doses higher than recommended initial doses (e.g.,>300 mg/day in adults and >12 mg/kg/day in children beyond 1 year of age). During the initiation of theophylline therapy, caffeine-like adverse effects may transiently alter patient behavior, especially in school age children, but this response rarely persists. Initiation of theophylline therapy at a low dose with subsequent slow titration to a predetermined age-related maximum dose will significantly reduce the frequency of these transient adverse effects (see DOSAGE AND ADMINISTRATION, Table V ). In a small percentage of patients (<3% of children and <10% of adults) the caffeine-like adverse effects persist during maintenance therapy, even at peak serum theophylline concentrations within the therapeutic range (i.e., 10-20 mcg/mL).

Use in specific populations

Sourced from openFDA

Pregnancy: Teratogenic Effects: In studies in which pregnant mice, rats and rabbits were dosed during the period of organogenesis, theophylline produced teratogenic effects. In studies with mice, a single intraperitoneal dose at and above 100 mg/kg (approximately equal to the maximum recommended oral dose for adults on a mg/m 2 basis) during organogenesis produced cleft palate and digital abnormalities. Micromelia, micrognathia, clubfoot, subcutaneous hematoma, open eyelids, and embryolethality were observed at doses that are approximately 2 times the maximum recommended oral dose for adults on a mg/m 2 basis. In a study with rats dosed from conception through organogenesis, an oral dose of 150 mg/kg/day (approximately 2 times the maximum recommended oral dose for adults on a mg/m 2 basis) produced digital abnormalities. Embryolethality was observed with a subcutaneous dose of 200 mg/kg/day (approximately 4 times the maximum recommended oral dose for adults on a mg/m 2 basis). In a study in which pregnant rabbits were dosed throughout organogenesis, an intravenous dose of 60 mg/kg/day (approximately 2 times the maximum recommended oral dose for adults on a mg/m 2 basis), which caused the death of one doe and clinical signs in others, produced cleft palate and was embryolethal.

Overdosage

Sourced from openFDA

General: The chronicity and pattern of theophylline overdosage significantly influences clinical manifestations of toxicity, management and outcome. There are two common presentations: (1) acute overdose , i.e., ingestion of a single large excessive dose (>10 mg/kg) as occurs in the context of an attempted suicide or isolated medication error, and (2) chronic overdosage , i.e., ingestion of repeated doses that are excessive for the patient's rate of theophylline clearance. The most common causes of chronic theophylline overdosage include patient or care giver error in dosing, healthcare professional prescribing of an excessive dose or a normal dose in the presence of factors known to decrease the rate of theophylline clearance, and increasing the dose in response to an exacerbation of symptoms without first measuring the serum theophylline concentration to determine whether a dose increase is safe. Severe toxicity from theophylline overdose is a relatively rare event. In one health maintenance organization, the frequency of hospital admissions for chronic overdosage of theophylline was about 1 per 1000 person-years exposure.

Approval history

Sourced from openFDA
  • Jan 11, 1983ANDAANDA087400Nostrum Pharms Llc
  • Aug 22, 1983ANDAANDA087943Endo Operations
  • Apr 30, 1990ANDAANDA089763Heritage Pharma Avet
  • Nov 9, 1992ANDAANDA081236Heritage Pharma Avet
  • Apr 21, 2006ANDAANDA040560Mpp Pharma
  • Jul 13, 2010ANDAANDA090355Glenmark Pharms Ltd
  • Oct 27, 2010ANDAANDA090430Alembic
  • Apr 13, 2011ANDAANDA091156Chartwell Molecular

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
12,166 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea2,37420%
  2. 2Asthma2,03517%
  3. 3Pneumonia1,40712%
  4. 4Wheezing1,36211%
  5. 5Vomiting1,1789.7%
  6. 6Cough1,0939.0%
  7. 7Drug Hypersensitivity8857.3%
  8. 8Malaise8026.6%
  9. 9Drug Ineffective7906.5%
  10. 10Pain7456.1%
  11. 11Oedema7215.9%
  12. 12Chest Pain6665.5%
  13. 13Nausea6585.4%
  14. 14Chronic Obstructive Pulmonary Disease6495.3%
  15. 15Fatigue4974.1%

Literature

View JSON

Recent PubMed references pinned to Theophylline as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 126 ClinicalTrials.gov registrations naming Theophylline as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Theophylline work?
Mechanism-of-action class: Phosphodiesterase Inhibitors.
What is Theophylline used for?
According to FDA labeling, Theophylline carries indications including: Theophylline extended-release tablets are indicated 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Theophylline?
Theophylline is classified as Xanthines, Phosphodiesterase Inhibitors, Bronchodilation, Inhibition Gastric Acid Secretion, Positive Chronotropy.
What are the brand names for Theophylline?
Theophylline is marketed under brand names including Elixophyllin, Theo-24.
What are the contraindications for Theophylline?
Theophylline labeling lists contraindications including: Theophylline extended-release tablets are contraindicated in patients with a history of hypersensitivity to theophylline or other components in the product.. Always consult the full prescribing information and a clinician.
Note. Data for theophylline is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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