Theophylline
Identification
- Summary
Theophylline is a xanthine used to manage the symptoms of asthma, COPD, and other lung conditions caused by reversible airflow obstruction.
- Brand Names
- Elixophyllin, Elixophylline, Pulmophylline, Quibron-T, Theo-24, Theolair, Uniphyl
- Generic Name
- Theophylline
- DrugBank Accession Number
- DB00277
- Background
A methylxanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Mechanistically, theophylline acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Theophylline is marketed under several brand names such as Uniphyl and Theochron, and it is indicated mainly for asthma, bronchospasm, and COPD.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 180.164
Monoisotopic: 180.06472552 - Chemical Formula
- C7H8N4O2
- Synonyms
- 1,3-dimethyl-7H-purine-2,6-dione
- 1,3-dimethylxanthine
- Teofilina
- Theophyllin
- Theophylline anhydrous
- Theophylline, anhydrous
Pharmacology
- 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.
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with evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Asthma Combination Product in combination with: Guaifenesin (DB00874), Pseudoephedrine (DB00852) •••••••••••• •••••• Used in combination for symptomatic treatment of Asthma Combination Product in combination with: D-glucose (DB01914) •••••••••••• •••••••••• •••••••• Used in combination to manage Asthma Combination Product in combination with: Acetylcysteine (DB06151) •••••••••••• Used in combination to treat Bronchitis Combination Product in combination with: Guaifenesin (DB00874), Pseudoephedrine (DB00852) •••••••••••• •••••• Treatment of Bronchoconstriction •••••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
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).
- 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. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.
Target Actions Organism AAdenosine receptor A1 antagonistHumans AAdenosine receptor A2a antagonistHumans AAdenosine receptor A2b antagonistHumans AcAMP-specific 3',5'-cyclic phosphodiesterase 4B inhibitorHumans AcGMP-specific 3',5'-cyclic phosphodiesterase inhibitorHumans AcAMP-specific 3',5'-cyclic phosphodiesterase 4A inhibitorHumans AcGMP-inhibited 3',5'-cyclic phosphodiesterase A inhibitorHumans AHistone deacetylase 2 activatorHumans UCopine-1 Not Available Humans UMinor histocompatibility antigen H13 Not Available Humans UNodal modulator 1 Not Available Humans UPoly [ADP-ribose] polymerase 1 Not Available Humans UProtein RIC-3 Not Available Humans UTubulin monoglycylase TTLL3 Not Available Humans - Absorption
Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.
- Volume of distribution
- 0.3 to 0.7 L/kg
- Protein binding
40%, primarily to albumin.
- Metabolism
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.
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- 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.
- Half-life
8 hours
- Clearance
- 0.29 mL/kg/min [Premature neonates, postnatal age 3-15 days]
- 0.64 mL/kg/min [Premature neonates, postnatal age 25-57 days]
- 1.7 mL/kg/min [Children 1-4 years]
- 1.6 mL/kg/min [Children 4-12 years]
- 0.9 mL/kg/min [Children 13-15 years]
- 1.4 mL/kg/min [Children 16-17 years]
- 0.65 mL/kg/min [Adults (16-60 years), otherwise healthy non-smoking asthmatics]
- 0.41 mL/kg/min [Elderly (>60 years), non-smokers with normal cardiac, liver, and renal function]
- 0.33 mL/kg/min [Acute pulmonary edema]
- 0.54 mL/kg/min [COPD >60 years, stable, non-smoker >1 year]
- 0.48 mL/kg/min [COPD with cor pulmonale]
- 1.25 mL/kg/min [Cystic fibrosis (14-28 years)]
- 0.31 mL/kg/min [Liver disease cirrhosis]
- 0.35 mL/kg/min [acute hepatitis]
- 0.65 mL/kg/min [cholestasis]
- 0.47 mL/kg/min [Sepsis with multi-organ failure]
- 0.38 mL/kg/min [hypothyroid]
- 0.8 mL/kg/min [hyperthyroid]
- Adverse Effects
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- Toxicity
Symptoms of overdose include seizures, arrhythmias, and GI effects.
- Pathways
Pathway Category Caffeine Metabolism Metabolic - Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Cytochrome P450 1A2 -2964(G/A) (A;A) / (G;A) A Allele Effect Directly Studied Patients with this genotype have reduced metabolism of theophylline. Details
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The therapeutic efficacy of 1,2-Benzodiazepine can be decreased when used in combination with Theophylline. Abametapir The serum concentration of Theophylline can be increased when it is combined with Abametapir. Abatacept The metabolism of Theophylline can be increased when combined with Abatacept. Abiraterone The metabolism of Theophylline can be decreased when combined with Abiraterone. Acalabrutinib The metabolism of Theophylline can be decreased when combined with Acalabrutinib. - Food Interactions
- Avoid excessive or chronic alcohol consumption. Ingesting alcohol may reduce the clearance, and therefore increase the serum concentrations of theophylline.
- Avoid St. John's Wort.
- Take with or without food. Take consistently with regard to food.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions. - Product Ingredients
Ingredient UNII CAS InChI Key Theophylline sodium glycinate 2S36N8T753 8000-10-0 AIJQWRAOMFRHTQ-UHFFFAOYSA-M - Product Images
- International/Other Brands
- Respbid / Slo-Bid / Theo 24 / Theo-Dur / Theodur G
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Elixir De Theophylline Elixir 80 mg / 15 mL Oral Laboratoire Atlas Inc 1985-12-31 Not applicable Canada Pulmophylline Elx Elixir 80 mg / 15 mL Oral Laboratoire Riva Inc 1979-12-31 Not applicable Canada Quibron T SR Tab 300mg Tablet, extended release 300 mg / tab Oral Bristol Labs Division Of Bristol Myers Squibb 1982-12-31 2004-08-05 Canada Quibron-T Tablet 300 mg/1 Oral Monarch Pharmaceuticals, Inc. 2006-11-09 Not applicable US Slo-bid 100 Capsule, extended release 100 mg Oral Aventis Pharma Ltd. 1987-12-31 2003-07-22 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aa-theo LA Tablet, extended release 200 mg Oral Aa Pharma Inc 1993-12-31 Not applicable Canada Aa-theo LA Tablet, extended release 300 mg Oral Aa Pharma Inc 1993-12-31 Not applicable Canada Aa-theo LA Tablet, extended release 100 mg Oral Aa Pharma Inc 1993-12-31 Not applicable Canada Apo-theo ER Tablet, extended release 600 mg Oral Apotex Corporation Not applicable Not applicable Canada Apo-theo ER Tablet, extended release 400 mg Oral Apotex Corporation Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BRONCHORETARD TAG200/NA350 Theophylline (350 mg/1) + Theophylline (200 mg/1) Capsule, extended release Oral 2014-04-01 Not applicable Germany BRONCHORETARD TAG200/NA350 Theophylline (350 mg/1) + Theophylline (200 mg/1) Capsule, extended release Oral 2014-04-01 Not applicable Germany CIDETOX® 125 MG CÁPSULAS Theophylline (1 g) + Theophylline (125 mg) Capsule, extended release Oral SERVICIO TECNICO GONHER FARMACEUTICA LTDA. 2011-03-12 2017-10-04 Colombia CIDETOX® 125 MG CÁPSULAS Theophylline (1 g) + Theophylline (125 mg) Capsule, extended release Oral SERVICIO TECNICO GONHER FARMACEUTICA LTDA. 2011-03-12 2017-10-04 Colombia I D M Expectorant Tab Theophylline (70 mg / tab) + Guaifenesin (100 mg / tab) + Mepyramine maleate (12 mg / tab) + Potassium Iodide (160 mg / tab) Tablet Oral Rougier Pharma Division Of Ratiopharm Inc 1975-12-31 1999-09-27 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Senophylline Theophylline (100 mg/1) + Choline (250 mg/1) Kit Oral Physician Therapeutics Llc 2011-07-07 Not applicable US TALOTREN 200 MG KAPSUL, 30 ADET Theophylline (200 mg) Capsule Oral NOVARTİS ÜRÜNLERİ 2019-11-26 2022-04-11 Turkey TALOTREN 350 MG KAPSUL, 30 ADET Theophylline (350 mg) Capsule Oral NOVARTİS ÜRÜNLERİ 2018-07-31 2022-04-11 Turkey
Categories
- ATC Codes
- R03DA54 — Theophylline, combinations excl. psycholeptics
- R03DA — Xanthines
- R03D — OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- R03DA — Xanthines
- R03D — OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- R03DA — Xanthines
- R03D — OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- R03DA — Xanthines
- R03D — OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- Drug Categories
- Agents that reduce seizure threshold
- Alkaloids
- Anti-Asthmatic Agents
- Autonomic Agents
- Bronchodilator Agents
- Cardiovascular Agents
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2D6 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP2E1 Substrates
- Cytochrome P-450 CYP2E1 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Substrates
- Drugs for Obstructive Airway Diseases
- Enzyme Inhibitors
- Heterocyclic Compounds, Fused-Ring
- Narrow Therapeutic Index Drugs
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Phosphodiesterase 5 Inhibitors
- Phosphodiesterase Inhibitors
- Purinergic Agents
- Purinergic Antagonists
- Purinergic P1 Receptor Antagonists
- Purines
- Purinones
- Respiratory Smooth Muscle Relaxants
- Respiratory System Agents
- Vasodilating Agents
- Xanthine derivatives
- Xanthines and Adrenergics
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as xanthines. These are purine derivatives with a ketone group conjugated at carbons 2 and 6 of the purine moiety.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Imidazopyrimidines
- Sub Class
- Purines and purine derivatives
- Direct Parent
- Xanthines
- Alternative Parents
- 6-oxopurines / Alkaloids and derivatives / Pyrimidones / Vinylogous amides / Imidazoles / Heteroaromatic compounds / Ureas / Lactams / Azacyclic compounds / Organopnictogen compounds show 4 more
- Substituents
- 6-oxopurine / Alkaloid or derivatives / Aromatic heteropolycyclic compound / Azacycle / Azole / Heteroaromatic compound / Hydrocarbon derivative / Imidazole / Lactam / Organic nitrogen compound show 11 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- dimethylxanthine (CHEBI:28177) / Purine alkaloids (C07130) / a small molecule (CPD-12479)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 0I55128JYK
- CAS number
- 58-55-9
- InChI Key
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N
- InChI
- InChI=1S/C7H8N4O2/c1-10-5-4(8-3-9-5)6(12)11(2)7(10)13/h3H,1-2H3,(H,8,9)
- IUPAC Name
- 1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione
- SMILES
- CN1C2=C(NC=N2)C(=O)N(C)C1=O
References
- Synthesis Reference
Nicolae S. Bodor, Kenneth B. Sloan, Yu-Neng Kuo, "Method for synthesizing certain selected pro-drug forms of theophylline." U.S. Patent US4000132, issued January, 1956.
US4000132- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0001889
- KEGG Drug
- D00371
- KEGG Compound
- C07130
- PubChem Compound
- 2153
- PubChem Substance
- 46505949
- ChemSpider
- 2068
- BindingDB
- 82053
- 10438
- ChEBI
- 28177
- ChEMBL
- CHEMBL190
- ZINC
- ZINC000018043251
- Therapeutic Targets Database
- DAP000002
- PharmGKB
- PA451647
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- TEP
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Theophylline
- PDB Entries
- 1eht / 1o15 / 2a3a / 3rox / 4eoh / 5mzj / 6ico / 6tuz / 7vrk / 7vrm … show 4 more
- FDA label
- Download (85.2 KB)
- MSDS
- Download (75.1 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Basic Science Healthy Subjects (HS) 1 4 Completed Health Services Research Asthma 1 4 Completed Prevention Anesthetics Adverse Reaction / Kidney Diseases / Kidney Failure / Prophylaxis of Contrast-induced nephropathy 1 4 Completed Treatment Allergic Rhinitis (AR) / Asthma 1 4 Completed Treatment Asthma 2
Pharmacoeconomics
- Manufacturers
- Fleming and co pharmaceuticals inc
- Forest laboratories inc
- Sanofi aventis us llc
- Dm graham laboratories inc
- Ucb inc
- Whitby pharmaceuticals inc
- Schwarz pharma inc
- Schering corp
- Central pharmaceuticals inc
- Hospira inc
- Inwood laboratories inc sub forest laboratories inc
- Sandoz inc
- Rp scherer north america div rp scherer corp
- Ortho mcneil pharmaceutical inc
- Schering corp sub schering plough corp
- Fisons corp
- Kv pharmaceutical co
- Rp scherer north america
- Hr cenci laboratories inc
- Caraco pharmaceutical laboratories ltd
- Lannett co inc
- Panray corp sub ormont drug and chemical co inc
- Alpharma us pharmaceuticals division
- Cenci powder products inc
- Halsey drug co inc
- L perrigo co
- Pharmaceutical assoc inc div beach products
- Precision dose inc
- Roxane laboratories inc
- Taro pharmaceuticals usa inc
- Wockhardt eu operations (swiss) ag
- B braun medical inc
- Baxter healthcare corp
- 3m pharmaceuticals inc
- Ferndale laboratories inc
- Warner chilcott co llc
- Monarch pharmaceuticals inc
- Roerig div pfizer inc
- Able laboratories inc
- Glenmark generics ltd
- Nostrum pharmaceuticals inc
- Pliva inc
- Pharmaceutical research assoc inc
- Purdue pharmaceutical products lp
- Graceway pharmaceuticals llc
- Novartis consumer health inc
- Packagers
- Actavis Group
- Amend
- American Regent
- Amerisource Health Services Corp.
- Amneal Pharmaceuticals
- Apotheca Inc.
- Arcola Laboratories
- A-S Medication Solutions LLC
- Atlantic Biologicals Corporation
- B. Braun Melsungen AG
- BASF Corp.
- Baxter International Inc.
- Bristol-Myers Squibb Co.
- C.O. Truxton Inc.
- Cardinal Health
- Caremark LLC
- Central Texas Community Health Centers
- Comprehensive Consultant Services Inc.
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Emcure Pharmaceuticals Ltd.
- Equipharm Inc.
- Forest Laboratories Inc.
- Forest Pharmaceuticals
- Glenmark Generics Ltd.
- H and H Laboratories
- Heartland Repack Services LLC
- Hospira Inc.
- Inwood Labs
- Inyx Usa Ltd.
- Kaiser Foundation Hospital
- Luitpold Pharmaceuticals Inc.
- Major Pharmaceuticals
- Marlop Pharmaceuticals Inc.
- Mckesson Corp.
- Mundipharma GmbH
- Murfreesboro Pharmaceutical Nursing Supply
- Nostrum Laboratories Inc.
- Nucare Pharmaceuticals Inc.
- P F Laboratories Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pfizer Inc.
- Pharmaceutical Packaging Center
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmedix
- Physicians Total Care Inc.
- Pliva Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Purdue Pharma LP
- Qualitest
- Remedy Repack
- Rite Aid Corp.
- Roxane Labs
- Roxmar Laboratories
- Sandhills Packaging Inc.
- Sandoz
- Sanofi-Aventis Inc.
- Southwood Pharmaceuticals
- Talbert Medical Management Corp.
- Taro Pharmaceuticals USA
- Tya Pharmaceuticals
- UCB Pharma
- United Research Laboratories Inc.
- Vangard Labs Inc.
- Warrick Pharmaceuticals Corp.
- Wockhardt Ltd.
- Dosage Forms
Form Route Strength Tablet, extended release Oral 100 mg Tablet, extended release Oral 300 mg Elixir Oral 167 mg/25ml Solution Oral 0.67 % Syrup Oral 533.33 g Tablet Oral 100 mg Tablet, film coated Oral Capsule, extended release Oral 350 mg/1 Capsule, extended release Oral 500 mg/1 Capsule, extended release Oral Tablet, delayed release Oral Tablet, delayed release Oral 300 mg Syrup Oral Elixir Oral 533 mg Tablet Oral 350 MG Tablet, delayed release Oral 100 mg Capsule, extended release Oral 200 mg Capsule, extended release Oral 400 mg Elixir Oral 80 mg / 15 mL Tablet, film coated Oral Tablet, film coated Oral 125 mg Gel Oral 0.5 g Injection Intravenous 24 mg/ml Tablet Oral Tablet Oral 150 MG Syrup Oral 80 mg/15ml Tablet Oral 100.000 mg Solution Intravenous 200 mg Solution Intravenous 400 mg Elixir Oral 0.533 g Tablet Oral 300 mg/1 Syrup Oral Capsule Oral Kit Oral Capsule, extended release Oral 100 mg Capsule, extended release Oral 300 mg Capsule, extended release Oral 50 mg Tablet, extended release Oral 270 mg Capsule Oral 350 mg Capsule, coated pellets Capsule, coated Oral 300 mg Syrup Oral 0.533 g Capsule, coated Oral 200 mg Capsule, coated Oral 250 mg Capsule Oral 100 mg Capsule Oral 300 mg Tablet Capsule Oral 100.000 mg Suspension Oral Capsule, extended release Oral 100 mg/1 Capsule, extended release Oral 400 mg/1 Tablet, extended release Oral 450 MG Tablet, extended release Oral 100 mg / srt Tablet, extended release Oral 200 mg / srt Tablet, extended release Oral 300 mg / srt Tablet, extended release Oral 450 mg / srt Tablet, extended release Oral 300 mg / tab Tablet, extended release Oral 100 mg / tab Capsule, extended release Oral Solution Oral 80 mg / 15 mL Tablet Oral 125000 ug/1 Tablet Oral 250000 ug/1 Tablet, extended release Oral 200 mg / tab Tablet, extended release Oral 250 mg / tab Tablet, extended release Oral 500 mg / tab Tablet Oral 250 mg Tablet, film coated Oral 250 mg Tablet, effervescent Oral Suspension Oral 2.5 g Capsule, extended release Oral 350 MG Capsule, extended release Oral 125 MG Capsule, extended release Oral 250 MG Capsule, extended release Oral 375 MG Capsule, extended release Oral 500 MG Capsule, extended release Oral 125 mg/1 Capsule, extended release Oral 200 mg/1 Capsule, extended release Oral 300 mg/1 Liquid Oral 80 mg/15mL Solution Oral 80 mg/15mL Tablet, extended release Oral 100 mg/1 Tablet, extended release Oral 450 mg/1 Tablet, extended release Oral 200 mg/1 Tablet, extended release Oral 600 mg/1 Solution Intravenous Liquid Oral 80 mg / 15 mL Tablet, extended release Oral 400 mg/1 Tablet, extended release Oral 300 mg/1 Injection Intravenous Injection, solution Intravenous Injection, solution Intravenous 160 mg/100mL Injection, solution Intravenous 200 mg/100mL Injection, solution Intravenous 320 mg/100mL Injection, solution Intravenous 40 mg/100mL Injection, solution Intravenous 400 mg/100mL Injection, solution Intravenous 80 mg/100mL Elixir Oral Injection, solution Intravenous 200 mg Tablet, film coated Oral 150 mg Tablet, film coated Oral 300 mg Tablet Oral 300 mg Tablet Oral 400 mg Tablet Oral Tablet Oral 400 mg/1 Tablet Oral 600 mg/1 Tablet, extended release Oral 600 mg Tablet, extended release Oral Capsule Oral 200 mg Capsule, coated pellets 200 mg Capsule Tablet Oral 125 mg Tablet, extended release Oral 200 mg Capsule Oral 125 mg Tablet Oral 200 mg Tablet, delayed release Oral 200 mg Tablet, delayed release Oral 250 mg Syrup Tablet Respiratory (inhalation) Solution Oral Tablet, coated Oral Elixir Tablet, extended release Oral 400 mg Tablet Oral 60 mg - Prices
Unit description Cost Unit Elixophyllin GG 100-100 mg/15ml Solution 240ml Bottle 60.98USD bottle Uniphyl 600 mg 24 Hour tablet 2.28USD tablet Theo-24 400 mg 24 Hour Capsule 2.04USD capsule Theo-24 400 mg capsule sa 1.97USD capsule Uniphyl 400 mg 24 Hour tablet 1.58USD tablet Theo-24 300 mg 24 Hour Capsule 1.45USD capsule Theo-24 300 mg capsule sa 1.4USD capsule Theophylline 400 mg 24 Hour tablet 1.27USD tablet Theo-24 200 mg 24 Hour Capsule 1.25USD capsule Theo-24 200 mg capsule sa 1.14USD capsule Theochron 450 mg tablet sa 0.94USD tablet Theophylline CR 300 mg 12 Hour Capsule 0.93USD capsule Theo-24 100 mg 24 Hour Capsule 0.83USD capsule Theophylline CR 200 mg 12 Hour Capsule 0.79USD capsule Theophylline CR 450 mg 12 Hour tablet 0.79USD tablet Theo-24 100 mg capsule sa 0.76USD capsule Quibron 90-150 mg capsule 0.73USD capsule Theophylline CR 125 mg 12 Hour Capsule 0.73USD capsule Uniphyl 600 mg Sustained-Release Tablet 0.68USD tablet Uniphyl 400 mg Sustained-Release Tablet 0.56USD tablet Theochron 300 mg tablet sa 0.54USD tablet Theophylline CR 300 mg 12 Hour tablet 0.51USD tablet Theophylline CR 200 mg 12 Hour tablet 0.4USD tablet Theochron 200 mg tablet sa 0.33USD tablet Theophylline CR 100 mg 12 Hour tablet 0.3USD tablet Elixophyllin GG 100-100 mg/15ml Solution 0.24USD ml Theochron 100 mg tablet sa 0.23USD tablet Elixophyllin 80 mg/15ml Elixir 0.2USD ml Elixophyllin 80 mg/15 ml elix 0.19USD ml Apo-Theo La 300 mg Sustained-Release Tablet 0.15USD tablet Apo-Theo La 100 mg Sustained-Release Tablet 0.14USD tablet Apo-Theo La 200 mg Sustained-Release Tablet 0.14USD tablet Theophylline anhydrous powder 0.08USD g Theophylline 200 mg/100 ml d5w 0.06USD ml Theolair 5.3 mg/ml Liquid 0.03USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 273 °C PhysProp water solubility 7360 mg/L (at 25 °C) YALKOWSKY,SH & HE,Y (2003) logP -0.02 HANSCH,C ET AL. (1995) Caco2 permeability -4.35 ADME Research, USCD pKa 8.81 KORTUM,G ET AL (1961) - Predicted Properties
Property Value Source Water Solubility 22.9 mg/mL ALOGPS logP -0.26 ALOGPS logP -0.77 Chemaxon logS -0.9 ALOGPS pKa (Strongest Acidic) 7.82 Chemaxon pKa (Strongest Basic) -0.78 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 69.3 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 44.93 m3·mol-1 Chemaxon Polarizability 16.86 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9902 Caco-2 permeable + 0.6172 P-glycoprotein substrate Non-substrate 0.7281 P-glycoprotein inhibitor I Non-inhibitor 0.8939 P-glycoprotein inhibitor II Non-inhibitor 0.911 Renal organic cation transporter Non-inhibitor 0.8807 CYP450 2C9 substrate Non-substrate 0.7738 CYP450 2D6 substrate Non-substrate 0.9117 CYP450 3A4 substrate Non-substrate 0.5974 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9933 CYP450 2D6 inhibitor Non-inhibitor 0.9827 CYP450 2C19 inhibitor Non-inhibitor 0.9895 CYP450 3A4 inhibitor Non-inhibitor 0.9616 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9956 Ames test Non AMES toxic 0.9132 Carcinogenicity Non-carcinogens 0.9447 Biodegradation Ready biodegradable 0.5942 Rat acute toxicity 2.7898 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8819 hERG inhibition (predictor II) Non-inhibitor 0.8927
Spectra
- Mass Spec (NIST)
- Download (2.96 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 137.3869361 predictedDarkChem Lite v0.1.0 [M-H]- 137.7675361 predictedDarkChem Lite v0.1.0 [M-H]- 137.8720361 predictedDarkChem Lite v0.1.0 [M-H]- 137.4992361 predictedDarkChem Lite v0.1.0 [M-H]- 127.004715 predictedDeepCCS 1.0 (2019) [M+H]+ 138.1124361 predictedDarkChem Lite v0.1.0 [M+H]+ 138.4654361 predictedDarkChem Lite v0.1.0 [M+H]+ 138.5915361 predictedDarkChem Lite v0.1.0 [M+H]+ 138.0519361 predictedDarkChem Lite v0.1.0 [M+H]+ 129.84254 predictedDeepCCS 1.0 (2019) [M+Na]+ 138.0264361 predictedDarkChem Lite v0.1.0 [M+Na]+ 137.9284361 predictedDarkChem Lite v0.1.0 [M+Na]+ 138.2415361 predictedDarkChem Lite v0.1.0 [M+Na]+ 138.1423361 predictedDarkChem Lite v0.1.0 [M+Na]+ 138.71461 predictedDeepCCS 1.0 (2019)
Targets
insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Purine nucleoside binding
- Specific Function
- Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- ADORA1
- Uniprot ID
- P30542
- Uniprot Name
- Adenosine receptor A1
- Molecular Weight
- 36511.325 Da
References
- Nantwi KD, Basura GJ, Goshgarian HG: Adenosine A1 receptor mRNA expression and the effects of systemic theophylline administration on respiratory function 4 months after C2 hemisection. J Spinal Cord Med. 2003 Winter;26(4):364-71. [Article]
- Daly JW, Jacobson KA, Ukena D: Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Identical protein binding
- Specific Function
- Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- ADORA2A
- Uniprot ID
- P29274
- Uniprot Name
- Adenosine receptor A2a
- Molecular Weight
- 44706.925 Da
References
- Pechlivanova DM, Georgiev VP: Effects of single and long-term theophylline treatment on the threshold of mechanical nociception: contribution of adenosine A1 and alpha2-adrenoceptors. Methods Find Exp Clin Pharmacol. 2005 Nov;27(9):659-64. [Article]
- Daly JW, Jacobson KA, Ukena D: Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- G-protein coupled adenosine receptor activity
- Specific Function
- Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- ADORA2B
- Uniprot ID
- P29275
- Uniprot Name
- Adenosine receptor A2b
- Molecular Weight
- 36332.655 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Philipp S, Yang XM, Cui L, Davis AM, Downey JM, Cohen MV: Postconditioning protects rabbit hearts through a protein kinase C-adenosine A2b receptor cascade. Cardiovasc Res. 2006 May 1;70(2):308-14. Epub 2006 Feb 23. [Article]
- Phelps PT, Anthes JC, Correll CC: Characterization of adenosine receptors in the human bladder carcinoma T24 cell line. Eur J Pharmacol. 2006 Apr 24;536(1-2):28-37. Epub 2006 Mar 3. [Article]
- Fozard JR, Baur F, Wolber C: Antagonist pharmacology of adenosine A2B receptors from rat, guinea pig and dog. Eur J Pharmacol. 2003 Aug 15;475(1-3):79-84. [Article]
- Holgate ST: The Quintiles Prize Lecture 2004. The identification of the adenosine A2B receptor as a novel therapeutic target in asthma. Br J Pharmacol. 2005 Aug;145(8):1009-15. [Article]
- Daly JW, Jacobson KA, Ukena D: Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging f...
- Gene Name
- PDE4B
- Uniprot ID
- Q07343
- Uniprot Name
- cAMP-specific 3',5'-cyclic phosphodiesterase 4B
- Molecular Weight
- 83342.695 Da
References
- Lipworth BJ: Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease. Lancet. 2005 Jan 8-14;365(9454):167-75. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, ...
- Gene Name
- PDE5A
- Uniprot ID
- O76074
- Uniprot Name
- cGMP-specific 3',5'-cyclic phosphodiesterase
- Molecular Weight
- 99984.14 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
- Gene Name
- PDE4A
- Uniprot ID
- P27815
- Uniprot Name
- cAMP-specific 3',5'-cyclic phosphodiesterase 4A
- Molecular Weight
- 98142.155 Da
References
- Wang K, Chen JQ, Chen Z, Chen JC: Inhibition of human phosphodiesterase 4A expressed in yeast cell GL62 by theophylline, rolipram, and acetamide-45. Acta Pharmacol Sin. 2002 Nov;23(11):1013-7. [Article]
- Haider S: Cyclic AMP level and phosphodiesterase activity during 17alpha,20beta-dihydroxy-4-pregnen-3-one induction and theophylline inhibition of oocyte maturation in the catfish, Clarias batrachus. Comp Biochem Physiol A Mol Integr Physiol. 2003 Feb;134(2):267-74. [Article]
- Rickards KJ, Andrews MJ, Waterworth TH, Alexander GB, Cunningham FM: Differential effects of phosphodiesterase inhibitors on platelet activating factor (PAF)- and adenosine diphosphate (ADP)-induced equine platelet aggregation. J Vet Pharmacol Ther. 2003 Aug;26(4):277-82. [Article]
- Usta C, Sadan G, Tuncel B: The effect of the indomethacin on phosphodiesterase inhibitors mediated responses in isolated trachea preparations. Prostaglandins Leukot Essent Fatty Acids. 2004 Sep;71(3):137-41. [Article]
- Lee JM, Zemans RL, Hejazi M, Chin BB, Ladenson PW, Caturegli P: Modulation of thyroidal radioiodine uptake by theophylline. Exp Mol Pathol. 2004 Oct;77(2):116-20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
- Gene Name
- PDE3A
- Uniprot ID
- Q14432
- Uniprot Name
- cGMP-inhibited 3',5'-cyclic phosphodiesterase A
- Molecular Weight
- 124978.06 Da
References
- Rickards KJ, Andrews MJ, Waterworth TH, Alexander GB, Cunningham FM: Differential effects of phosphodiesterase inhibitors on platelet activating factor (PAF)- and adenosine diphosphate (ADP)-induced equine platelet aggregation. J Vet Pharmacol Ther. 2003 Aug;26(4):277-82. [Article]
- Wu BN, Lin RJ, Lo YC, Shen KP, Wang CC, Lin YT, Chen IJ: KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14. Epub 2004 Jul 5. [Article]
- Kajikawa S, Kigami D, Nakayama H, Doi K: Changes in submaxillary gland gene expression in F344 rats by multiple dosing of theophylline. Exp Anim. 2006 Apr;55(2):143-6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Activator
- General Function
- Transcription factor binding
- Specific Function
- Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an impo...
- Gene Name
- HDAC2
- Uniprot ID
- Q92769
- Uniprot Name
- Histone deacetylase 2
- Molecular Weight
- 55363.855 Da
References
- Ito K, Lim S, Caramori G, Cosio B, Chung KF, Adcock IM, Barnes PJ: A molecular mechanism of action of theophylline: Induction of histone deacetylase activity to decrease inflammatory gene expression. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8921-6. Epub 2002 Jun 17. [Article]
- Cosio BG, Tsaprouni L, Ito K, Jazrawi E, Adcock IM, Barnes PJ: Theophylline restores histone deacetylase activity and steroid responses in COPD macrophages. J Exp Med. 2004 Sep 6;200(5):689-95. Epub 2004 Aug 30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Calcium-dependent phospholipid-binding protein that plays a role in calcium-mediated intracellular processes (PubMed:14674885). Involved in the TNF-alpha receptor signaling pathway in a calcium-dependent manner (PubMed:14674885). Exhibits calcium-dependent phospholipid binding properties (PubMed:9430674, PubMed:19539605). Plays a role in neuronal progenitor cell differentiation; induces neurite outgrowth via a AKT-dependent signaling cascade and calcium-independent manner (PubMed:23263657, PubMed:25450385). May recruit target proteins to the cell membrane in a calcium-dependent manner (PubMed:12522145). May function in membrane trafficking (PubMed:9430674). Involved in TNF-alpha-induced NF-kappa-B transcriptional repression by inducing endoprotease processing of the transcription factor NF-kappa-B p65/RELA subunit (PubMed:18212740). Also induces endoprotease processing of NF-kappa-B p50/NFKB1, p52/NFKB2, RELB and REL (PubMed:18212740).
- Specific Function
- Calcium ion binding
- Gene Name
- CPNE1
- Uniprot ID
- Q99829
- Uniprot Name
- Copine-1
- Molecular Weight
- 59058.34 Da
References
- Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalyzes intramembrane proteolysis of some signal peptides after they have been cleaved from a preprotein, resulting in the release of the fragment from the ER membrane into the cytoplasm. Required to generate lymphocyte cell surface (HLA-E) epitopes derived from MHC class I signal peptides (PubMed:11714810). May be necessary for the removal of the signal peptide that remains attached to the hepatitis C virus core protein after the initial proteolytic processing of the polyprotein (PubMed:12145199). Involved in the intramembrane cleavage of the integral membrane protein PSEN1 (PubMed:12077416, PubMed:11714810, PubMed:14741365). Cleaves the integral membrane protein XBP1 isoform 1 in a DERL1/RNF139-dependent manner (PubMed:25239945). May play a role in graft rejection (By similarity).
- Specific Function
- Aspartic endopeptidase activity, intramembrane cleaving
- Gene Name
- HM13
- Uniprot ID
- Q8TCT9
- Uniprot Name
- Minor histocompatibility antigen H13
- Molecular Weight
- 41487.86 Da
References
- Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- May antagonize Nodal signaling.
- Specific Function
- Carbohydrate binding
- Gene Name
- NOMO1
- Uniprot ID
- Q15155
- Uniprot Name
- Nodal modulator 1
- Molecular Weight
- 134323.005 Da
References
- Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
- Gene Name
- PARP1
- Uniprot ID
- P09874
- Uniprot Name
- Poly [ADP-ribose] polymerase 1
- Molecular Weight
- 113082.945 Da
References
- Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Promotes functional expression of homomeric alpha-7 and alpha-8 nicotinic acetylcholine receptors at the cell surface. May also promote functional expression of homomeric serotoninergic 5-HT3 receptors, and of heteromeric acetylcholine receptors alpha-3/beta-2, alpha-3/beta-4, alpha-4/beta-2 and alpha-4/beta-4.
- Specific Function
- Acetylcholine receptor binding
- Gene Name
- RIC3
- Uniprot ID
- Q7Z5B4
- Uniprot Name
- Protein RIC-3
- Molecular Weight
- 41091.77 Da
References
- Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Monoglycylase which modifies alpha- and beta-tubulin, generating side chains of glycine on the gamma-carboxyl groups of specific glutamate residues within the C-terminal tail of alpha- and beta-tubulin. Involved in the side-chain initiation step of the glycylation reaction by adding a single glycine chain to generate monoglycine side chains. Not involved in elongation step of the polyglycylation reaction.
- Specific Function
- Atp binding
- Gene Name
- TTLL3
- Uniprot ID
- Q9Y4R7
- Uniprot Name
- Tubulin monoglycylase TTLL3
- Molecular Weight
- 87413.395 Da
References
- Marwick JA, Wallis G, Meja K, Kuster B, Bouwmeester T, Chakravarty P, Fletcher D, Whittaker PA, Barnes PJ, Ito K, Adcock IM, Kirkham PA: Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802. doi: 10.1016/j.bbrc.2008.10.065. Epub 2008 Oct 23. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d 24-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Ha HR, Chen J, Freiburghaus AU, Follath F: Metabolism of theophylline by cDNA-expressed human cytochromes P-450. Br J Clin Pharmacol. 1995 Mar;39(3):321-6. [Article]
- Tassaneeyakul W, Birkett DJ, Veronese ME, McManus ME, Tukey RH, Quattrochi LC, Gelboin HV, Miners JO: Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. J Pharmacol Exp Ther. 1993 Apr;265(1):401-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1B1
- Uniprot ID
- Q16678
- Uniprot Name
- Cytochrome P450 1B1
- Molecular Weight
- 60845.33 Da
References
- Shimada T, Gillam EM, Sutter TR, Strickland PT, Guengerich FP, Yamazaki H: Oxidation of xenobiotics by recombinant human cytochrome P450 1B1. Drug Metab Dispos. 1997 May;25(5):617-22. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Ha HR, Chen J, Freiburghaus AU, Follath F: Metabolism of theophylline by cDNA-expressed human cytochromes P-450. Br J Clin Pharmacol. 1995 Mar;39(3):321-6. [Article]
- Zhang ZY, Kaminsky LS: Characterization of human cytochromes P450 involved in theophylline 8-hydroxylation. Biochem Pharmacol. 1995 Jul 17;50(2):205-11. [Article]
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Brosen K: Drug interactions and the cytochrome P450 system. The role of cytochrome P450 1A2. Clin Pharmacokinet. 1995;29 Suppl 1:20-5. [Article]
- Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [Article]
- Wang L, Hu Z, Deng X, Wang Y, Zhang Z, Cheng ZN: Association between common CYP1A2 polymorphisms and theophylline metabolism in non-smoking healthy volunteers. Basic Clin Pharmacol Toxicol. 2013 Apr;112(4):257-63. doi: 10.1111/bcpt.12038. Epub 2012 Dec 20. [Article]
- Flockhart Table of Drug Interactions [Link]
- Theophylline FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- General Function
- Zinc ion binding
- Specific Function
- Catalyzes the hydrolytic deamination of adenosine and 2-deoxyadenosine. Plays an important role in purine metabolism and in adenosine homeostasis. Modulates signaling by extracellular adenosine, an...
- Gene Name
- ADA
- Uniprot ID
- P00813
- Uniprot Name
- Adenosine deaminase
- Molecular Weight
- 40764.13 Da
References
- Saboury AA, Bagheri S, Ataie G, Amanlou M, Moosavi-Movahedi AA, Hakimelahi GH, Cristalli G, Namaki S: Binding properties of adenosine deaminase interacted with theophylline. Chem Pharm Bull (Tokyo). 2004 Oct;52(10):1179-82. [Article]
- Singh LS, Sharma R: Purification and characterization of intestinal adenosine deaminase from mice. Mol Cell Biochem. 2000 Jan;204(1-2):127-34. [Article]
- Bandyopadhyay BC, Poddar MK: Theophylline-induced changes in mammalian adenosine deaminase activity and corticosterone status: possible relation to immune response. Methods Find Exp Clin Pharmacol. 1997 Apr;19(3):181-4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Sarkar MA, Hunt C, Guzelian PS, Karnes HT: Characterization of human liver cytochromes P-450 involved in theophylline metabolism. Drug Metab Dispos. 1992 Jan-Feb;20(1):31-7. [Article]
- Sutrisna E: The Impact of CYP1A2 and CYP2E1 Genes Polymorphism on Theophylline Response. J Clin Diagn Res. 2016 Nov;10(11):FE01-FE03. doi: 10.7860/JCDR/2016/21067.8914. Epub 2016 Nov 1. [Article]
- Kim YC, Lee AK, Lee JH, Lee I, Lee DC, Kim SH, Kim SG, Lee MG: Pharmacokinetics of theophylline in diabetes mellitus rats: induction of CYP1A2 and CYP2E1 on 1,3-dimethyluric acid formation. Eur J Pharm Sci. 2005 Sep;26(1):114-23. doi: 10.1016/j.ejps.2005.05.004. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Zhang ZY, Kaminsky LS: Characterization of human cytochromes P450 involved in theophylline 8-hydroxylation. Biochem Pharmacol. 1995 Jul 17;50(2):205-11. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulf...
- Gene Name
- SLC22A7
- Uniprot ID
- Q9Y694
- Uniprot Name
- Solute carrier family 22 member 7
- Molecular Weight
- 60025.025 Da
References
- Kobayashi Y, Sakai R, Ohshiro N, Ohbayashi M, Kohyama N, Yamamoto T: Possible involvement of organic anion transporter 2 on the interaction of theophylline with erythromycin in the human liver. Drug Metab Dispos. 2005 May;33(5):619-22. Epub 2005 Feb 11. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55