Drug Indication

Drug 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.
from DrugBank
FDA Label
from DrugBank
LiverTox Summary
Theophylline is a xanthine derivative that induces relaxation of smooth muscle in the

bronchial tree causing bronchodilation. Theophylline is widely used in therapy of asthma
and is not believed to cause liver injury.
from LiverTox
Drug Classes
Antiasthmatic Agents
from LiverTox
FDA Orange Book
Prescription Drug Products
Prescription Drug Products: 1 of 10 (RX Drug Ingredient)
Drug Ingredient THEOPHYLLINE
Proprietary Name THEO-24
Applicant
ACTIENT PHARMS (Application Number: A087942)
AUXILIUM PHARMS INC (Application Number: A081034)
AUXILIUM PHARMS LLC (Application Number: A087943)
AUXILIUM PHARMS LLC (Application Number: A087944)
from FDA Orange Book

Proprietary Name THEOPHYLLINE 0.08% AND DEXTROSE 5% IN PLASTIC
CONTAINER
Applicant B BRAUN (Application Number: N019826)
Proprietary Name THEOCHRON
Applicant NOSTRUM PHARMS LLC (Application Number: A087400)
View All 10 Prescription Drug Products
Discontinued Drug Products
Discontinued Drug Products: 1 of 54 (DISCN Drug Ingredient)
Drug Ingredient THEOPHYLLINE SODIUM GLYCINATE
Proprietary Name SYNOPHYLATE
Applicant CENT PHARMS (Application Number: N006333)
Proprietary Name AEROLATE
Applicant FLEMING PHARMS (Application Number: A089141)
Proprietary Name BRONKODYL
Applicant SANOFI AVENTIS US (Application Number: A085264)
View All 54 Discontinued Drug Products

Drug Labels for Ingredients
Drug Labels for Ingredients: 1 of 1 (Label Title)
Label Information Total 53 labels
NDC Code(s)
NDC Code(s)
0121-0820-04, 0121-0820-16, 0121-4794-15, 0121-4820-15, 0121-4820-40, 0258-3625-

01, 0258-3634-01, 0258-3638-01, 0264-9554-10, 0280-8030-24 ... total 122.
Packagers AX Pharmaceutical Corp; Actavis Mid Atlantic LLC; Alembic

Pharmaceuticals Inc.; Alembic Pharmaceuticals Limited; American Health Packaging;
Atlantic Biologicals Corps; Attix Pharmaceuticals Inc; AvKARE, Inc.; Avera McKennan
Hospital; B. Braun Medical Inc. ... total 41.
from DailyMed
Drugs at PubMed Health
Drugs at PubMed Health: 1 of 11 (PubMed Health Drug Name)
Drug Name Uniphyl
Notes See Theophylline
from PubMed Health
Drug Name Uniphyl
Notes See Theophylline (By mouth)
from PubMed Health
Drug Name Theophylline (Intravenous route)
Description Theophylline injection is used together with other medicines to treat the
acute symptoms of asthma, bronchitis, emphysema, and other lung diseases in a
hospital setting.
Drug Classes Bronchodilator, Methylxanthine
from PubMed Health

View All 11 Drugs at PubMed Health
Clinical Trials
Download
1 to 5 of 35View More
Record ID Title Status Phase
NCT03115294 Digital Image Correlation in Right Ventricular Evaluation Recruiting
NCT03029429 Theophylline Treatment for Pseudohypoparathyroidism Not yet

recruiting 2
NCT03015090 Association Study Between CYP1A2 Gene Polymorphisms and

Metabolism of Theophylline Recruiting
NCT02537691 Longitudinal Cohort Study in Participants With Severe Asthma to Assess

Biomarkers Completed 4
NCT02479451 Helping Olfaction and Nutrition On Renal Replacement Recruiting

2
from ClinicalTrials.gov
Therapeutic Uses
Bronchodilator Agents; Phosphodiesterase Inhibitors; Purinergic P1 Receptor

Antagonists; Vasodilator Agents
National Library of Medicine's Medical Subject Headings. Theophylline. Online file

(MeSH, 2016). Available from, as of June 24, 2016:
https://www.nlm.nih.gov/mesh/2016/mesh_browser/MBrowser.html
from HSDB
/CLINICAL TRIALS/ ClinicalTrials.gov is a registry and results database of publicly and

privately supported clinical studies of human participants conducted around the world.
The Web site is maintained by the National Library of Medicine (NLM) and the National
Institutes of Health (NIH). Each ClinicalTrials.gov record presents summary information
about a study protocol and includes the following: Disease or condition; Intervention
(for example, the medical product, behavior, or procedure being studied); Title,
description, and design of the study; Requirements for participation (eligibility criteria);
Locations where the study is being conducted; Contact information for the study
locations; and Links to relevant information on other health Web sites, such as NLM's
MedlinePlus for patient health information and PubMed for citations and abstracts for
scholarly articles in the field of medicine. Theophylline is included in the database.
NIH/NLM; ClinicalTrials.Gov. Available from, as of July 6, 2016:
https://clinicaltrials.gov/search/intervention=theophylline
from HSDB
Limited evidence suggests that an IV xanthine derivative (e.g., theophylline,

aminophylline) could be beneficial as add-on therapy in children who are admitted to an
intensive care unit (ICU) for severe exacerbations of asthma not controlled by inhaled
and IV beta2-adrenergic agonists, ipratropium bromide, and IV corticosteroids; however,
the efficacy of such add-on IV theophylline therapy has not been established in adults.
American Society of Health-System Pharmacists 2016; Drug Information 2016. Bethesda,

MD. 2016, p. 3602
from HSDB
Theophylline is 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. /Included in US product labeling/
NIH; DailyMed. Current Medication Information for Theophylline (Anhydrous) Tablet,

Extended Release (Updated: November 2014). Available from, as of July 21, 2016:
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=038c2b07-8028-4dc4-847c-
adafe1b0e81a
from HSDB
IV theophylline (often as aminophylline) has been used to relieve the periodic apnea and
increase arterial blood pH in patients with Cheyne-Stokes respiration. /NOT included in
US product labeling/

MD. 2016, p. 3602
from HSDB
Theophylline oral liquids are used in the treatment of idiopathic apnea in neonates,
characterized by cessation of respiration that lasts 20 seconds or longer. ... Theophylline
should be considered in addition to administration of oxygen, sensory stimulation, or
low pressure nasal continuous positive airway pressure. /NOT included in US product
labeling/
Thomson.Micromedex. Drug Information for the Health Care Professional. 25th ed.
Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial
Convention, Inc. Greenwood Village, CO. 2005., p. 650
from HSDB
(VET): Theophylline is administered for inflammatory airway disease in cats, dogs, and
horses. Use in animals has been primarily derived from empirical use, some
experimental models, and experience in humans. There are no well-contolled clinical
studies or efficacy trials to document clinical effectiveness. It has been used to control
clinical signs of reversible airway constriction, such as seen with feline asthma. In dogs,
the uses include collapsing trachea, bronchitis, and other airway diseases. In horses, it
will relieve signs of recurrent airway obstruction (heaves), but the IV dose may cause
adverse effects in horses.
Papich, M.G. Saunders Handbook of Veterinary Drugs Small and Large Animal. 3rd ed. St.
Louis, MO: Elsevier Saunders, 2011, p. 742
from HSDB
/EXPL THER/ Cisplatin is a potent antineoplastic agent used and its major limiting side
effect is nephrotoxicity. The aims of the study are early detection of acute kidney injury
(AKI) with biomarkers and investigation of the potential nephron-protective effects of
theophylline. Glomerular filtration rates (GFR), neutrophil gelatinase-associated lipocalin
(NGAL), cystatin C were measured at 5th day of treatment in all of the patients. In
addition, these parameters were measured repeatedly after the administration of
cisplatin, at 2nd hour, 5th and 20th days. PATIENTS: Sixty patients who are planned to
receive cisplatin for the first time were included in the study. Patients were divided into
two groups as Group 1 (n=30) (standard treatment arm) and Group II (n=30)
(theophylline arm). In both groups after the administration of cisplatin, GFR showed a
significant decrease within time (p=0.006). Urine NGAL levels were significantly high
after 2 hr of cisplatin administration (p<0.001), no significant difference was observed
between groups. However, when the time*group effects were considered together,
higher NGAL levels were detected in the group not receiving theophylline (p=0.025).
After 5 days of cisplatin administration, urine protein levels were significantly higher in
both groups (p<0.001). Results showed that urine NGAL level is a superior biomarker
compared to serum creatinine and serum cystatin C in the detection of early AKI.
Theophylline was found not to bring a complete protection for the kidneys, but less
nephrotoxicity was developed when compared to the group not receiving theophylline.
Abstract: PubMed
Karademir LD et al; Ren Fail 38 (5): 806-14 (2016)
from HSDB
/EXPL THER/ When managing therapy for the post-lumbar puncture headaches (PLPHs),
an efficacious, fast-acting, practical and safe method is preferred. Invasive methods
have known complications and oral medications might be problematic when nausea and
vomiting occurs with severe headaches. The aim of this study was to highlight the brief
initial time for a remarkable decrease of PLPH pain levels after the administration of IV
theophylline infusion. We observed that IV theophylline infusion has a rapid and marked
effect on decreasing pain in PLPHs. At 30 min of theophylline infusion, mean VAS levels
were decreased by 47.1 % and at 60 min of infusion, the decrease of pain was 61.9 %.
We conclude that IV theophylline infusion is a rapidly effective, noninvasive, practical
and low-cost way to treat PLPHs. ...[Ergun U et al; Acta Neurol Belg. 2015 Nov 12.
Abstract: PubMed
Epub ahead of print]
from HSDB
/EXPL THER/ Cervical spinal contusion injuries are the most common form of spinal cord
injury (>50%) observed in humans. These injuries can result in the impaired ability to
breathe. In this study we examine the role of theophylline in the rescue of breathing
behavior after a cervical spinal contusion. Previous research in the C2 hemisection
model has shown that acute administration of theophylline can rescue phrenic nerve
activity and diaphragmatic EMG on the side ipsilateral to injury. However, this effect is
dependent on intact and uninjured pathways. In this study we utilized a cervical
contusion injury model that more closely mimics the human condition. This injury model
can determine the effectiveness of therapeutic interventions, in this case theophylline,
on the isolated contused pathways of the spinal cord. Three weeks after a 150 kD C3/4
unilateral contusion subjects received a 15 mg/kg dose of theophylline prior to a
contralateral C2 hemisection. Subjects that received theophylline were able to
effectively utilize damaged pathways to breathe for up to 2 min, while subjects treated
with saline were unable to support ventilation. Through these experiments, we
demonstrate that theophylline can make injured pathways that mediate breathing more
effective and therefore, suggest a potential therapeutic role in the critical time points
immediately after injury.
Abstract: PubMed
Hoy KC Jr, Alilain WJ; Exp Neurol 271: 72-6 (2015)
from HSDB
Drug Warning
When administered rectally as suppositories (dosage form no longer commercially

available in the US), theophyllines have caused rectal irritation and inflammation.
/Theophyllines/

MD. 2016, p. 3605
from HSDB
Theophyllines may also produce transiently increased urinary frequency, dehydration,
twitching of fingers and hands, tachypnea, and elevated serum AST (SGOT)
concentrations. Hypersensitivity reactions characterized by urticaria, generalized
pruritus, and angioedema have been reported with aminophylline administration. A
contact-type dermatitis, caused by hypersensitivity to the ethylenediamine component
of aminophylline, has also been reported. Bone marrow suppression, leukopenia,
thrombocytopenia, and hemorrhagic diathesis have also been reported, but their
association with theophylline therapy is questionable. Other adverse effects of
theophyllines include albuminuria, increased urinary excretion of renal tubular cells and
erythrocytes, hyperglycemia, and syndrome of inappropriate secretion of antidiuretic
hormone (SIADH). /Theophyllines/

MD. 2016, p. 3605
from HSDB
Adverse cardiovascular effects of theophyllines include palpitation, sinus tachycardia,

extrasystoles, and increased pulse rate. These adverse cardiovascular effects are usually
mild and transient. Flushing, hypotension, circulatory failure, and ventricular
arrhythmias may also occur. /Theophyllines/

MD. 2016, p. 3605
from HSDB
Theophyllines produce GI irritation and CNS stimulation following administration by any

route. Theophyllines are all somewhat irritating to gastric mucosa; the importance of
reported differences among the individual agents is doubtful. The most common
adverse GI effects (both locally and centrally mediated) include nausea, vomiting,
epigastric pain, abdominal cramps, anorexia, and, rarely, diarrhea. Hematemesis has
also occurred. Adverse CNS effects, which are often more severe in children than in
adults, include headache, irritability, restlessness, nervousness, insomnia, dizziness,
reflex hyperexcitability, and seizures. Reduction of theophylline dosage usually reduces
the incidence and severity of adverse gastric and CNS effects; however, if these adverse
effects persist, the drug may have to be withdrawn. The drugs may be administered
orally before or after meals, with a full glass of liquid, or with antacids to minimize
locally mediated GI irritation. /Theophyllines/

MD. 2016, p. 3605
from HSDB
Theophyllines are contraindicated in patients who are allergic to any of the
theophyllines, caffeine, or theobromine ... . At least one manufacturer states that
theophyllines also are contraindicated in patients with active peptic ulcer disease and in
those with underlying seizure disorders, unless the latter patients are receiving
adequate anticonvulsant therapy.

MD. 2016, p. 3606
from HSDB
Some commercially available formulations of theophyllines contain sulfites that may

cause allergic-type reactions, including anaphylaxis and life-threatening or less severe
asthmatic episodes, in certain susceptible individuals. The overall prevalence of sulfite
sensitivity in the general population is unknown but probably low; such sensitivity
appears to occur more frequently in asthmatic than in nonasthmatic individuals.
/Theophyllines/

MD. 2016, p. 3606
from HSDB
The drugs should be used with caution in patients with peptic ulcer, hyperthyroidism,
glaucoma, diabetes mellitus, severe hypoxemia, hypertension, or in patients with
compromised cardiac or circulatory function. Theophylline preparations should be used
cautiously in patients with angina pectoris or acute myocardial injury when myocardial
stimulation would be harmful. Since theophylline may cause dysrhythmia and/or worsen
preexisting arrhythmias, any substantial change in rate and/or rhythm warrants
electrocardiographic (ECG) monitoring and further investigation. /Theophyllines/

MD. 2016, p. 3606
from HSDB
VET: Adverse effects include nausea, vomiting, and diarrhea. With high doses,
tachycardia, excitement, tremors, and seizures are possible. cardiovascular and CNS
adverse effects appear to be less frequent in dogs than people. Overdoses can cause
hypokalemia.
Papich, M.G. Saunders Handbook of Veterinary Drugs Small and Large Animal. 3rd ed. St.
Louis, MO: Elsevier Saunders, 2011, p. 743
from HSDB
The clearance of theophylline is decreased by an average of 30% in healthy elderly
adults (>60 yrs) compared to healthy young adults. Careful attention to dose reduction
and frequent monitoring of serum theophylline concentrations are required in elderly
patients.

adafe1b0e81a
from HSDB
The clearance of theophylline is very low in neonates. Theophylline clearance reaches

maximal values by one year of age, remains relatively constant until about 9 years of age
and then slowly decreases by approximately 50% to adult values at about age 16. 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. Careful
attention to dosage selection and monitoring of serum theophylline concentrations are
required in pediatric patients.

adafe1b0e81a
from HSDB
Gender differences in theophylline clearance are relatively small and unlikely to be of

clinical significance. Significant reduction in theophylline clearance, however, has been
reported in women on the 20th day of the menstrual cycle and during the third
trimester of pregnancy.

adafe1b0e81a
from HSDB
Fever, regardless of its underlying cause, can decrease the clearance of theophylline.
The magnitude and duration of the fever appear to be directly correlated to the degree
of decrease of theophylline clearance. Precise data are lacking, but a temperature of 39
deg C (102 deg F) for at least 24 hours is probably required to produce a clinically
significant increase in serum theophylline concentrations. Children with rapid rates of
theophylline clearance (i.e., those who require a dose that is substantially larger than
average [e.g., >22 mg/kg/day] to achieve a therapeutic peak serum theophylline
concentration when afebrile) may be at greater risk of toxic effects from decreased
clearance during sustained fever. Careful attention to dose reduction and frequent
monitoring of serum theophylline concentrations are required in patients with sustained
fever.

adafe1b0e81a
from HSDB
Tobacco and marijuana smoking appears to increase the clearance of theophylline by

induction of metabolic pathways. Theophylline clearance has been shown to increase by
approximately 50% in young adult tobacco smokers and by approximately 80% in elderly
tobacco smokers compared to non-smoking subjects. Passive smoke exposure has also
been shown to increase theophylline clearance by up to 50%. Abstinence from tobacco
smoking for one week causes a reduction of approximately 40% in theophylline
clearance. Careful attention to dose reduction and frequent monitoring of serum
theophylline concentrations are required in patients who stop smoking. Use of nicotine
gum has been shown to have no effect on theophylline clearance.

adafe1b0e81a
from HSDB
Theophylline clearance is decreased by 50% or more in patients with hepatic

insufficiency (e.g., cirrhosis, acute hepatitis, cholestasis). Careful attention to dose
reduction and frequent monitoring of serum theophylline concentrations are required in
patients with reduced hepatic function.

adafe1b0e81a
from HSDB
Theophylline clearance is decreased by 50% or more in patients with congestive heart

failure (CHF). The extent of reduction in theophylline clearance in patients with CHF
appears to be directly correlated to the severity of the cardiac disease. Since
theophylline clearance is independent of liver blood flow, the reduction in clearance
appears to be due to impaired hepatocyte function rather than reduced perfusion.
Careful attention to dose reduction and frequent monitoring of serum theophylline
concentrations are required in patients with CHF.

adafe1b0e81a
from HSDB
Theophylline is safe and effective for the approved indications in pediatric patients. The
maintenance dose of theophylline must be selected with caution in pediatric patients
since the rate of theophylline clearance is highly variable across the pediatric age range.

adafe1b0e81a
from HSDB
There are no adequate and well-controlled studies in pregnant women. Theophylline

should be used during pregnancy only if the potential benefit justifies the potential risk
to the fetus.

adafe1b0e81a
from HSDB
FDA Pregnancy Risk Category: C /RISK CANNOT BE RULED OUT. Adequate, well
controlled human studies are lacking, and animal studies have shown risk to the fetus or
are lacking as well. There is a chance of fetal harm if the drug is given during pregnancy;
but the potential benefits may outweigh the potential risk./

adafe1b0e81a
from HSDB
Elderly patients are at a significantly greater risk of experiencing serious toxicity from
theophylline than younger patients due to pharmacokinetic and pharmacodynamic
changes associated with aging. The clearance of theophylline is decreased by an average
of 30% in healthy elderly adults (>60 yrs) compared to healthy young adults.
Theophylline clearance may be further reduced by concomitant diseases prevalent in
the elderly, which further impair clearance of this drug and have the potential to
increase serum levels and potential toxicity. These conditions include impaired renal
function, chronic obstructive pulmonary disease, congestive heart failure, hepatic
disease and an increased prevalence of use of certain medications with the potential for
pharmacokinetic and pharmacodynamic interaction. Protein binding may be decreased
in the elderly resulting in an increased proportion of the total serum theophylline
concentration in the pharmacologically active unbound form. Elderly patients also
appear to be more sensitive to the toxic effects of theophylline after chronic overdosage
than younger patients. Careful attention to dose reduction and frequent monitoring of
serum theophylline concentrations are required in elderly patients.

adafe1b0e81a
from HSDB
Pharmacology and Biochemistry
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).
from DrugBank
Theophylline is a natural alkaloid derivative of xanthine isolated from the plants

Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase
and prostaglandin production, regulate calcium flux and intracellular calcium
distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial
smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS,
stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may
also suppress inflammation and improve contractility of the diaphragm. (NCI04)

Drug Indication

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Drug Indication

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Drug Indication

Theophylline is a xanthine derivative that induces relaxation of smooth muscle in the

FDA Orange Book

Prescription Drug Products

Prescription Drug Products: 1 of 10 (RX Drug Ingredient)

Drug Ingredient THEOPHYLLINE

Proprietary Name THEO-24

ACTIENT PHARMS (Application Number: A087942)

AUXILIUM PHARMS INC (Application Number: A081034)

AUXILIUM PHARMS LLC (Application Number: A087943)

AUXILIUM PHARMS LLC (Application Number: A087944)

from FDA Orange Book

Prescription Drug Products: 2 of 10 (RX Drug Ingredient)

Drug Ingredient THEOPHYLLINE

Applicant B BRAUN (Application Number: N019826)

from FDA Orange Book

Prescription Drug Products: 3 of 10 (RX Drug Ingredient)

Drug Ingredient THEOPHYLLINE

Proprietary Name THEOCHRON

Applicant NOSTRUM PHARMS LLC (Application Number: A087400)

from FDA Orange Book

View All 10 Prescription Drug Products

Discontinued Drug Products

Discontinued Drug Products: 1 of 54 (DISCN Drug Ingredient)

Drug Ingredient THEOPHYLLINE SODIUM GLYCINATE

Proprietary Name SYNOPHYLATE

Applicant CENT PHARMS (Application Number: N006333)

from FDA Orange Book

Discontinued Drug Products: 2 of 54 (DISCN Drug Ingredient)

Drug Ingredient THEOPHYLLINE

Proprietary Name AEROLATE

Applicant FLEMING PHARMS (Application Number: A089141)

from FDA Orange Book

Discontinued Drug Products: 3 of 54 (DISCN Drug Ingredient)

Drug Ingredient THEOPHYLLINE

Proprietary Name BRONKODYL

Applicant SANOFI AVENTIS US (Application Number: A085264)

from FDA Orange Book

View All 54 Discontinued Drug Products

Drug Labels for Ingredients: 1 of 1 (Label Title)

Label Information Total 53 labels

Drug Ingredient THEOPHYLLINE

0121-0820-04, 0121-0820-16, 0121-4794-15, 0121-4820-15, 0121-4820-40, 0258-3625-

Packagers AX Pharmaceutical Corp; Actavis Mid Atlantic LLC; Alembic

Drugs at PubMed Health

Drugs at PubMed Health: 1 of 11 (PubMed Health Drug Name)

Drug Name Uniphyl

Notes See Theophylline

from PubMed Health

Drugs at PubMed Health: 2 of 11 (PubMed Health Drug Name)

Drug Name Uniphyl

Notes See Theophylline (By mouth)

from PubMed Health

Drugs at PubMed Health: 3 of 11 (PubMed Health Drug Name)

Drug Name Theophylline (Intravenous route)

Drug Classes Bronchodilator, Methylxanthine

from PubMed Health

Record ID Title Status Phase

NCT03115294 Digital Image Correlation in Right Ventricular Evaluation Recruiting

NCT03029429 Theophylline Treatment for Pseudohypoparathyroidism Not yet

NCT03015090 Association Study Between CYP1A2 Gene Polymorphisms and

NCT02537691 Longitudinal Cohort Study in Participants With Severe Asthma to Assess

NCT02479451 Helping Olfaction and Nutrition On Renal Replacement Recruiting