Drug/Small Molecule:
theophylline

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.



Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
VIP No VIP available No VIP available CYP1A2 *1C N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs2031920 (-1053)C>T (Rsa 1 c1>c2), -1055C>T, 135339845C>T, 3979C>T, 6573776C>T, CYP2E1(-1055)C>T, Rsa1
C > T
5' Flanking
No VIP available No Clinical Annotations available VA
rs2069514 (-2964)G>A, 28338G>A, 3860G>A, 45828777G>A, 75038220G>A, CYP1A2*1C
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs35694136 -1635delT, 29731delT, 45830170delT, 75039613delT
T > -
5' Flanking
No VIP available No Clinical Annotations available VA
rs3813867 -1295G>C, 135339605G>C, 3739G>C, 6573536G>C, CYP2E1(-1295)C>G
G > C
5' Flanking
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Dimethylxanthine
  • Pseudotheophylline
  • Theophyline
  • Theophyllin
  • Theophylline Anhydrous
  • Theophylline aminoacetate
Trade Names
  • Accurbron
  • Acet-Theocin
  • Aerobin
  • Aerolate
  • Aerolate III
  • Aerolate SR
  • Afonilm
  • Afonilum
  • Aquaphyllin
  • Armophylline
  • Asbron
  • Asmalix
  • Asmax
  • Austyn
  • Bilordyl
  • Bronchoretard
  • Bronkodyl
  • Bronkodyl SR
  • Cetraphylline
  • Choledyl SA
  • Chronophyllin
  • Constant T
  • Diffumal
  • Diphyllin
  • Doraphyllin
  • Duraphyl
  • Duraphyllin
  • Dyspne-Inhal
  • Egifilin
  • Elan
  • Elixex
  • Elixicon
  • Elixomin
  • Elixophyllin
  • Elixophyllin SR
  • Elixophylline
  • Etheophyl
  • Euphyllin
  • Euphylline
  • Euphylong
  • Labid
  • Lanophyllin
  • Lasma
  • Liquophylline
  • Liquorice
  • Maphylline
  • Medaphyllin
  • Nuelin
  • Optiphyllin
  • Parkophyllin
  • Physpan
  • Pro-Vent
  • Pulmidur
  • Pulmo-Timelets
  • Quibron
  • Quibron T
  • Quibron T/SR
  • Quibron-T
  • Quibron-T/SR
  • Respbid
  • Respicur
  • Respid
  • Slo-Bid
  • Slo-Phyllin
  • Solosin
  • Somophyllin CRT
  • Somophyllin T
  • Somophyllin-CRT
  • Somophyllin-DF
  • Somophyllin-T
  • Spophyllin Retard
  • Sustaire
  • Synophylate
  • Synophylate-L.A. Cenules
  • T-Phyl
  • Talotren
  • Tefamin
  • Telb-DS
  • Telbans Dry Syrup
  • Teocen 200
  • Teofilina
  • Teofyllamin
  • Teolair
  • Teonova
  • Teosona
  • Tesona
  • Theacitin
  • Theal Tablets
  • Theo 24
  • Theo-11
  • Theo-24
  • Theo-DS
  • Theo-Dur
  • Theo-Nite
  • Theo-Sav
  • Theobid
  • Theobid Duracap
  • Theobid Jr.
  • Theochron
  • Theocin
  • Theoclair-SR
  • Theoclear
  • Theoclear 80
  • Theoclear L.A.-130
  • Theoclear LA
  • Theoclear-200
  • Theoclear-80
  • Theocontin
  • Theodel
  • Theodrip
  • Theodur Dry Syrup
  • Theofol
  • Theograd
  • Theolair
  • Theolair-SR
  • Theolix
  • Theolixir
  • Theon
  • Theona P
  • Theopek
  • Theophyl
  • Theophyl-225
  • Theophyl-SR
  • Theophylline-SR
  • Theoplus
  • Theospan
  • Theostat
  • Theostat 80
  • Theotard
  • Theovent
  • Uni-Dur
  • Unifyl
  • Unilong
  • Uniphyl
  • Uniphyllin
  • Xanthium
  • Xantivent
Brand Mixture Names
  • Bronchyl Syrup (alcohol anhydrous + beechwood creosote + cocillana + eucalyptus + guaiacol oleate + ipecac + lobelia inflata + menthol + myroxylon balsamum + theophylline + white pine)
  • Choledyl Expectorant Elixir (guaifenesin + oxtriphylline)
  • Diuerb tab (oil of fleabane + theophylline + urea)
  • IDM Expectorant tab (guaifenesin + potassium iodide + pyrilamine maleate + theophylline)
  • IDM tab (potassium iodide + pyrilamine maleate + theophylline)
  • PMS-Oxtriphylline Elixir (alcohol anhydrous + oxtriphylline)
  • Pulmo Septol Sirop (beechwood creosote + cocillana + eucalyptus oil + guaiacol + ipecac + lobelia inflata + myroxylon balsamum + theophylline + white pine)
  • Ratio-theo-bronc (guaifenesin + potassium iodide + pyrilamine maleate + theophylline)
  • Tedral tab (l-ephedrine hydrochloride + phenobarbital + theophylline)
  • Theophylline 0.8mg and 5% dextrose inj (dextrose + theophylline)
  • Theophylline 0.8mg/ml in 5% dextrose inj (dextrose + theophylline)
  • Theophylline 1.6mg and 5% dextrose inj (dextrose + theophylline)
  • Theophylline 4mg and 5% dextrose inj (dextrose + theophylline)
  • Theophylline rougier elixir (alcohol anhydrous + theophylline)

PharmGKB Accession Id:
PA451647

Description

A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP thus potentiates the actions of agents that act through adenylate cyclase and cyclic AMP.

Source: Drug Bank

Indication

For the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, such as emphysema and chronic bronchitis.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction.

Source: Drug Bank

Pharmacology

Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Theophylline has two distinct actions in the airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects).

Source: Drug Bank

Food Interaction

Avoid alcohol.|Avoid excessive quantities of coffee or tea (Caffeine).|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Biotransformation takes place through demethylation to 1-methylxanthine and 3-methylxanthine and hydroxylation to 1,3-dimethyluric acid. 1-methylxanthine is further hydroxylated, by xanthine oxidase, to 1-methyluric acid. About 6% of a theophylline dose is N-methylated to caffeine. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacologic activity.

Source: Drug Bank

Protein Binding

40%, primarily to albumin.

Source: Drug Bank

Absorption

Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.

Source: Drug Bank

Half-Life

8 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include seizures, arrhythmias, and GI effects.

Source: Drug Bank

Route of Elimination

Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver. Renal excretion of unchanged theophylline in neonates amounts to about 50% of the dose, compared to about 10% in children older than three months and in adults.

Source: Drug Bank

Volume of Distribution

  • 0.3 to 0.7 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C7H8N4O2

Source: Drug Bank

Isomeric SMILES

Cn1c2c(c(=O)n(c1=O)C)[nH]cn2

Source: OpenEye

Canonical SMILES

CN1C2=C(NC=N2)C(=O)N(C)C1=O

Source: Drug Bank

Average Molecular Weight

180.164

Source: Drug Bank

Monoisotopic Molecular Weight

180.06472552

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Caffeine Pathway, Pharmacokinetics
    Stylized liver cell showing candidate genes involved in the metabolism of caffeine.
  1. Theophylline Pathway, Pharmacokinetics
    Schematic representation of theophylline metabolism in human liver.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
CYP1A2
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available PW
CYP2E1
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available PW
CYP3A4
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available PW
XDH

Drug Targets

Gene Description
ADORA1 (source: Drug Bank)
ADORA2A (source: Drug Bank)
ADORA2B (source: Drug Bank)
PDE3A (source: Drug Bank)
PDE4A (source: Drug Bank)
PDE4B (source: Drug Bank)
PDE5A (source: Drug Bank)

Drug Interactions

Drug Description
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Acyclovir increases the effect and toxicity of theophylline. (source: Drug Bank)
theophylline This xanthine decreases the effect of adenosine (source: Drug Bank)
theophylline This xanthine decreases the effect of adenosine (source: Drug Bank)
theophylline This xanthine decreases the effect of adenosine (source: Drug Bank)
theophylline Theophylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if theophylline is initiated, discontinued or dose changed. (source: Drug Bank)
theophylline Increases or decreases the effect of theophylline (source: Drug Bank)
theophylline Increases or decreases the effect of theophylline (source: Drug Bank)
theophylline Increases or decreases the effect of theophylline (source: Drug Bank)
theophylline Increases the effect of theophylline (source: Drug Bank)
theophylline Increases the effect of theophylline (source: Drug Bank)
theophylline The quinolone increases the effect of theophylline (source: Drug Bank)
theophylline The quinolone increases the effect of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline The macrolide increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline The macrolide, erythromycin, may increase the effect and toxicity of theophylline. (source: Drug Bank)
theophylline The contraceptive increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline The contraceptive increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Decreased effect of both products (source: Drug Bank)
theophylline The quinolone increases the effect of theophylline (source: Drug Bank)
theophylline The quinolone increases the effect of theophylline (source: Drug Bank)
theophylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Theophylline decreases serum levels of lithium (source: Drug Bank)
theophylline Theophylline decreases serum levels of lithium (source: Drug Bank)
theophylline Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline The quinolone increases the effect of theophylline (source: Drug Bank)
theophylline The quinolone increases the effect of theophylline (source: Drug Bank)
theophylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Interferon increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Pentoxifylline increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Pentoxifylline increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline The barbiturate decreases the effect of theophylline (source: Drug Bank)
theophylline The barbiturate, phenobarbital, decreases the effect of theophylline. (source: Drug Bank)
theophylline Decreased effect of both products (source: Drug Bank)
theophylline Decreased effect of both products (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline The barbiturate decreases the effect of theophylline (source: Drug Bank)
theophylline The barbiturate, primidone, decreases the effect of theophylline. (source: Drug Bank)
theophylline Propafenone increases the effect of theophylline (source: Drug Bank)
theophylline Propafenone increases the effect of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline Rifampin decreases the effect of theophylline (source: Drug Bank)
theophylline Rifampin decreases the effect of theophylline (source: Drug Bank)
theophylline Tacrine may reduce the elimination rate of Theophylline. Monitor for changes in the therapeutic and toxic effects of theophylline if Tacrine is initiated, discontinued or if the dose is changed. (source: Drug Bank)
theophylline Telithromycin may reduce clearance of Theophylline. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Theophylline if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
theophylline Theophylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Theophylline is initiated, discontinued or dose changed. (source: Drug Bank)
theophylline Terbinafine increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Terbinafine increases the effect and toxicity of theophylline (source: Drug Bank)
aciclovir Aciclovir increases the effect and toxicity of theophylline (source: Drug Bank)
aciclovir Aciclovir increases the effect and toxicity of theophylline (source: Drug Bank)
adenosine The xanthine decreases the effect of adenosine (source: Drug Bank)
adenosine The xanthine decreases the effect of adenosine (source: Drug Bank)
amobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
amobarbital The barbiturate, amobarbital, decreases the effect of theophylline. (source: Drug Bank)
aprobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
aprobarbital The barbiturate, aprobarbital, decreases the effect of theophylline. (source: Drug Bank)
atracurium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
atracurium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
butabarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
butabarbital The barbiturate, butabarbital, decreases the effect of theophylline. (source: Drug Bank)
butalbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
butalbital The barbiturate, butalbital, decreases the effect of theophylline. (source: Drug Bank)
butethal The barbiturate decreases the effect of theophylline (source: Drug Bank)
butethal The barbiturate, butethal, decreases the effect of theophylline. (source: Drug Bank)
carbamazepine Carbamazepine increases or decreases the effect of theophylline (source: Drug Bank)
carbamazepine Carbamazepine increases or decreases the effect of theophylline (source: Drug Bank)
carteolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
carteolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
cimetidine Cimetidine increases the effect of theophylline (source: Drug Bank)
cimetidine Cimetidine increases the effect of theophylline (source: Drug Bank)
ciprofloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
ciprofloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
clarithromycin Clarithromycin increases the effect and toxicity of theophylline (source: Drug Bank)
clarithromycin Clarithromycin increases the effect and toxicity of theophylline (source: Drug Bank)
disulfiram Disulfiram increases the effect and toxicity of theophylline (source: Drug Bank)
disulfiram Disulfiram increases the effect and toxicity of theophylline (source: Drug Bank)
doxacurium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
doxacurium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
enoxacin The quinolone increases the effect of theophylline (source: Drug Bank)
enoxacin The quinolone increases the effect of theophylline (source: Drug Bank)
erythromycin The macrolide increases the effect and toxicity of theophylline (source: Drug Bank)
erythromycin The macrolide, erythromycin, may increase the effect and toxicity of theophylline. (source: Drug Bank)
estradiol The contraceptive increases the effect and toxicity of theophylline (source: Drug Bank)
ethinyl estradiol The contraceptive increases the effect and toxicity of theophylline (source: Drug Bank)
ethotoin Decreased effect of both products (source: Drug Bank)
ethotoin Decreased effect of both products (source: Drug Bank)
fluvoxamine Fluvoxamine increases the effect and toxicity of theophylline (source: Drug Bank)
fluvoxamine Fluvoxamine increases the effect and toxicity of theophylline (source: Drug Bank)
fosphenytoin Decreased effect of both products (source: Drug Bank)
fosphenytoin Decreased effect of both products (source: Drug Bank)
gallamine triethiodide Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
gallamine triethiodide Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
grepafloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
grepafloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
halothane Increased risk of cardiac arrhythmia (source: Drug Bank)
halothane Increased risk of cardiac arrhythmia (source: Drug Bank)
heptabarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
heptabarbital The barbiturate, heptabarbital, decreases the effect of theophylline. (source: Drug Bank)
hexobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
hexobarbital The barbiturate, hexobarbital, decreases the effect of theophylline. (source: Drug Bank)
isoniazid Isoniazid increases the effect and toxicity of theophylline (source: Drug Bank)
isoniazid Isoniazid increases the effect and toxicity of theophylline (source: Drug Bank)
josamycin The macrolide increases the effect and toxicity of theophylline (source: Drug Bank)
josamycin The macrolide, josamycin, may increase the effect and toxicity of theophylline. (source: Drug Bank)
lithium Theophylline decreases serum levels of lithium (source: Drug Bank)
lithium Theophylline decreases serum levels of lithium (source: Drug Bank)
mephenytoin Decreased effect of both products (source: Drug Bank)
mephenytoin Decreased effect of both products (source: Drug Bank)
mestranol The contraceptive increases the effect and toxicity of theophylline (source: Drug Bank)
mestranol The contraceptive increases the effect and toxicity of theophylline (source: Drug Bank)
methohexital The barbiturate decreases the effect of theophylline (source: Drug Bank)
methohexital The barbiturate, methohexital, decreases the effect of theophylline. (source: Drug Bank)
methylphenobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
methylphenobarbital The barbiturate, methylphenobarbital, decreases the effect of theophylline. (source: Drug Bank)
metocurine Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
metocurine Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
mexiletine Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank)
mexiletine Mexiletine increases the effect and toxicity of theophylline (source: Drug Bank)
mivacurium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
mivacurium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
nadolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
nadolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
norfloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
norfloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
pancuronium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
pancuronium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
pefloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
pefloxacin The quinolone increases the effect of theophylline (source: Drug Bank)
penbutolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
penbutolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of theophylline. (source: Drug Bank)
pentoxifylline Pentoxifylline increases the effect and toxicity of theophylline (source: Drug Bank)
pentoxifylline Pentoxifylline increases the effect and toxicity of theophylline (source: Drug Bank)
phenobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
phenobarbital The barbiturate, phenobarbital, decreases the effect of theophylline. (source: Drug Bank)
phenytoin Decreased effect of both products (source: Drug Bank)
phenytoin Decreased effect of both products (source: Drug Bank)
pindolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
pindolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
primidone The barbiturate decreases the effect of theophylline (source: Drug Bank)
primidone The barbiturate, primidone, decreases the effect of theophylline. (source: Drug Bank)
propafenone Propafenone increases the effect of theophylline (source: Drug Bank)
propafenone Propafenone increases the effect of theophylline (source: Drug Bank)
propranolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
propranolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
quinidine The barbiturate decreases the effect of theophylline (source: Drug Bank)
quinidine The barbiturate, quinidine barbiturate, decreases the effect of theophylline. (source: Drug Bank)
rifampin Rifampin decreases the effect of theophylline (source: Drug Bank)
rifampin Rifampin decreases the effect of theophylline (source: Drug Bank)
ritonavir Ritonavir decreases the effect of theophylline (source: Drug Bank)
ritonavir Ritonavir decreases the effect of theophylline (source: Drug Bank)
rofecoxib Rofecoxib increases the effect and toxicity of theophylline (source: Drug Bank)
rofecoxib Rofecoxib increases the effect and toxicity of theophylline (source: Drug Bank)
secobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
secobarbital The barbiturate, secobarbital, decreases the effect of theophylline. (source: Drug Bank)
sotalol Antagonism of action and increased effect of theophylline (source: Drug Bank)
sotalol Antagonism of action and increased effect of theophylline (source: Drug Bank)
tacrine Tacrine increases the effect and toxicity of theophylline (source: Drug Bank)
tacrine Tacrine increases the effect and toxicity of theophylline (source: Drug Bank)
talbutal The barbiturate decreases the effect of theophylline (source: Drug Bank)
talbutal The barbiturate, talbutal, decreases the effect of theophylline. (source: Drug Bank)
terbinafine Terbinafine increases the effect and toxicity of theophylline (source: Drug Bank)
terbinafine Terbinafine increases the effect and toxicity of theophylline (source: Drug Bank)
thiabendazole Thiabendazole increases the effect and toxicity of theophylline (source: Drug Bank)
thiabendazole Thiabendazole increases the effect and toxicity of theophylline (source: Drug Bank)
ticlopidine Ticlopidine increases the effect and toxicity of theophylline (source: Drug Bank)
ticlopidine Ticlopidine increases the effect and toxicity of theophylline (source: Drug Bank)
timolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
timolol Antagonism of action and increased effect of theophylline (source: Drug Bank)
troleandomycin The macrolide increases the effect and toxicity of theophylline (source: Drug Bank)
troleandomycin The macrolide, troleandomycin, may increase the effect and toxicity of theophylline. (source: Drug Bank)
tubocurarine Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
tubocurarine Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
vecuronium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
vecuronium Theophylline decreases the effect of the muscle relaxant (source: Drug Bank)
verapamil Verapamil increases the effect of theophylline (source: Drug Bank)
verapamil Verapamil increases the effect of theophylline (source: Drug Bank)
zileuton Zileuton increases the effect and toxicity of theophylline (source: Drug Bank)
zileuton Zileuton increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Theophylline by decreasing Theophylline metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Theophylline if Thiabendazole is initiated, discontinued or dose changed. (source: Drug Bank)
theophylline Ticlopidine increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Ticlopidine increases the effect and toxicity of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline Antagonism of action and increased effect of theophylline (source: Drug Bank)
theophylline Tipranavir, co-administered with Ritonavir, may decrease the concentration of Theophylline. (source: Drug Bank)
theophylline Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of theophylline by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of theophylline if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)
theophylline Zafirlukast serum concentrations may be decreased by Theophylline. (source: Drug Bank)
theophylline Zileuton may increase the therapeutic and adverse effects of theophylline by increasing its serum concentration. Monitor for changes in the therapeutic and adverse effects of theophylline if zileuton is initiated, discontinued or dose changed. Dose alterations should be considered. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to theophylline: 14

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
PDE4: A Novel Target in the Treatment of Chronic Obstructive Pulmonary Disease. Clinical pharmacology and therapeutics. 2011. Michalski J M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP1A2. Pharmacogenetics and genomics. 2011. Thorn Caroline F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The effect of CYP1A2 gene polymorphisms on Theophylline metabolism and chronic obstructive pulmonary disease in Turkish patients. BMB reports. 2010. Uslu Ahmet, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The relative contribution of human cytochrome P450 isoforms to the four caffeine oxidation pathways: an in vitro comparative study with cDNA-expressed P450s including CYP2C isoforms. Biochemical pharmacology. 2008. Kot Marta, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Prediction of pharmacokinetic drug-drug interactions using human hepatocyte suspension in plasma and cytochrome P450 phenotypic data. II. In vitro-in vivo correlation with ketoconazole. Drug metabolism and disposition: the biological fate of chemicals. 2008. Lu Chuang, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Variation in CYP1A2 activity and its clinical implications: influence of environmental factors and genetic polymorphisms. Pharmacogenomics. 2008. Gunes Arzu, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In vivo evaluation of CYP1A2, CYP2A6, NAT-2 and xanthine oxidase activities in a Greek population sample by the RP-HPLC monitoring of caffeine metabolic ratios. Biomedical chromatography : BMC. 2007. Begas E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Associations between CYP2E1 promoter polymorphisms and plasma 1,3-dimethyluric acid/theophylline ratios. European journal of clinical pharmacology. 2006. Yoon Yeomin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Time response of cytochrome P450 1A2 activity on cessation of heavy smoking. Clinical pharmacology and therapeutics. 2004. Faber Mirko S, et al. PubMed
Polymorphisms in the CYP1A2 gene and theophylline metabolism in patients with asthma. Clinical pharmacology and therapeutics. 2003. Obase Yasushi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Reversal of the antiinflammatory effects of methotrexate by the nonselective adenosine receptor antagonists theophylline and caffeine: evidence that the antiinflammatory effects of methotrexate are mediated via multiple adenosine receptors in rat adjuvant arthritis. Arthritis and rheumatism. 2000. Montesinos M C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Metabolism of theophylline by cDNA-expressed human cytochromes P-450. British journal of clinical pharmacology. 1995. Ha H R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Biotransformation of caffeine, paraxanthine, theobromine and theophylline by cDNA-expressed human CYP1A2 and CYP2E1. Pharmacogenetics. 1992. Gu L, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0089-0342-10
DrugBank:
DB00277
PDB:
TEP
ChEBI:
28177
KEGG Compound:
C07130
KEGG Drug:
D00371
PubChem Compound:
2153
PubChem Substance:
46505949
7847437
IUPHAR Ligand:
413
Drugs Product Database (DPD):
627410
BindingDB:
10847
ChemSpider:
2068
HET:
TEP
Therapeutic Targets Database:
DAP000002
FDA Drug Label at DailyMed:
3829d74e-b3ab-46df-a08b-f0327b63304e

Clinical Trials

These are trials that mention theophylline and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.