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Theophylline
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DRUG INFO Theophylline
Drug Name:
Theophylline
Indication: For the treatment of bronchospasm (due to asthma) and chronic bronchitis.
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).
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.
Drug Category: Vasodilator Agents; Bronchodilator Agents; Respiratory Smooth Muscle Relaxants; ATC:R03DA04
Brand Names/Synonyms: Accurbron; Acet-Theocin; Aerobin; Aerolate; Aerolate Iii; Aerolate Sr; Afonilm; Afonilum; Aminophylline; Aquaphyllin; Armophylline; Asbron; Asmalix; Asmax; Austyn; Bilordyl; Bronchoretard; Bronkodyl; Bronkodyl Sr; Cetraphylline; Choledyl Sa; Chronophyllin; Constant T; Diffumal; Dimethylxanthine; Diphyllin; Doraphyllin; Duraphyl; Duraphyllin; Dyspne-Inhal; Egifilin; Elan; Elixex; Elixicon; Elixomin; Elixophyllin; Elixophyllin Sr; Elixophylline; Etheophyl; Euphyllin; Euphylline; Euphylong; GS 2591A; Labid; Lanophyllin; Lasma; Liquophylline; Liquorice; Maphylline; Medaphyllin; NSC 2066; Nuelin; Optiphyllin; Parkophyllin; Physpan; Pro-Vent; Pseudotheophylline; 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 Tabl.; 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; Theophyline; Theophyllin; Theophylline; Theophylline Anhydrous; Theophylline, Anhydrous; Theophylline-Sr; Theoplus; Theospan; Theostat; Theostat 80; Theotard; Theovent; Uni-Dur; Unifyl; Unilong; Uniphyl; Uniphyllin; X 115; Xanthium; Xantivent
Dosage Forms: Immediate-Release Oral Forms; Tablet and suspension; Sustained Action Capsules
Absorption: Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.
Interactions:
DrugBank: Interactions for Theophylline
Interactions for Theophylline:
Theophylline interacts with a wide variety of drugs. The interaction may be pharmacodynamic, i.e., alterations in
the therapeutic response to theophylline or another drug or occurrence of adverse effects without a change in serum
theophylline concentration. More frequently, however, the interaction is pharmacokinetic, i.e., the rate of
theophylline clearance is altered by another drug resulting in increased or decreased serum theophylline
concentrations. Theophylline only rarely alters the pharmacokinetics of other drugs.
The drugs listed in TABLES 2A and 2B have the potential to produce clinically significant pharmacodynamic or
pharmacokinetic interactions with theophylline. The information in the "Effect" column of TABLES 2A and 2B assumes
that the interacting drug is being added to a steady-state theophylline regimen. If theophylline is being initiated
in a patient who is already taking a drug that inhibits theophylline clearance (e.g., cimetidine,
erythromycin), the dose of theophylline required to achieve a therapeutic serum theophylline concentration will be
smaller. Conversely, if theophylline is being initiated in a patient who is already taking a drug that enhances
theophylline clearance (e.g., rifampin), the dose of theophylline required to achieve a therapeutic serum
theophylline concentration will be larger. Discontinuation of a concomitant drug that increases theophylline
clearance will result in accumulation of theophylline to potentially toxic levels, unless the theophylline dose is
appropriately reduced. Discontinuation of a concomitant drug that inhibits theophylline clearance will result in
decreased serum theophylline concentrations, unless the theophylline dose is appropriately increased.
The listing of drugs in TABLES 2A and 2B is current as of April 3, 1995. New interactions are continuously being
reported for theophylline, especially with new chemical entities. The clinician should not assume that a drug does
not interact with theophylline if it is not listed in TABLES 2A and 2B.Before addition of a newly available drug
in a patient receiving theophylline, the package insert of the new drug and/or the medical literature should be
consulted to determine if an interaction between the new drug and theophylline has been reported.
TABLE 2A - Clinically significant drug interactions with theophylline*
| Drug |
Type of Interaction |
Effect** |
| Adenosine |
Theophylline blocks adenosine receptors. |
Higher doses of adenosine may be required to achieve desired effect. |
| Alcohol |
A single large dose of alcohol (3 ml/kg of whiskey) decreases theophylline clearance for up to
24 hours. |
30% increase |
| Allopurinol |
Decreases theophylline clearance at allopurinol doses ³600
mg/day. |
25% increase |
| Aminoglutethimide |
Increases theophylline clearance by induction of microsomal enzyme activity. |
25% decrease |
| Carbamazepine |
Similar to aminoglutethimide. |
30% decrease |
| Cimetidine |
Decreases theophylline clearance by inhibiting cytochrome P450 1A2. |
70% increase |
| Ciprofloxacin |
Similar to cimetidine. |
40% increase |
| Clarithromycin |
Similar to erythromycin. |
25% increase |
| Diazepam |
Benzodiazepines increase CNS concentrations of adenosine, a potent CNS depressant, while
theophylline blocks adenosine receptors. |
Larger diazepam doses may be required to produce desired level of sedation. |
| Discontinuation of theophylline without reduction of diazepam dose may result in
respiratory depression. |
| Disulfiram |
Decreases theophylline clearance by inhibiting hydroxylation and demethylation. |
50% increase |
| Enoxacin |
Similar to cimetidine. |
300% increase |
| Ephedrine |
Synergistic CNS effects |
Increased frequency of nausea, nervousness, and insomnia. |
| Erythromycin |
Erythromycin metabolite decreases theophylline clearance by inhibiting cytochrome P450
3A3. |
35% increase. |
| Erythromycin steady-state serum concentrations decreased by a similar amount. |
| Estrogen |
Estrogen containing oral contraceptives decrease theophylline clearance in a dose-dependent
fashion. The effect of progesterone on theophylline clearance is unknown. |
30% increase |
| Flurazepam |
Similar to diazepam. |
Similar to diazepam. |
| Fluvoxamine |
Similar to cimetidine myocardium to catecholamines, theophylline increases release of
endogenous catecholamines. |
Similar to cimetidine ventricular arrhythmias. |
| Interferon, human recombinant alpha-A |
Decreases theophylline clearance. |
100% increase |
| Isoproterenol (IV) |
Increases theophylline clearance. |
20% decrease |
| Ketamine |
Pharmacologic |
May lower theophylline seizure threshold. |
| Lithium |
Theophylline increases renal lithium clearance. |
Lithium dose required to achieve a therapeutic serum concentration increased an average of
60%. |
| Lorazepam |
Similar to diazepam. |
Similar to diazepam. |
TABLE 2B - Clinically significant drug interactions with theophylline*
| Drug |
Type of Interaction |
Effect** |
| Methotrexate (MTX) |
Decreases theophylline clearance. |
20% increase after low dose MTX, higher dose MTX may have a greater effect. |
| Mexiletine |
Similar to disulfiram. |
80% increase |
| Midazolam |
Similar to diazepam. |
Similar to diazepam. |
| Moricizine |
Increases theophylline clearance. |
25% decrease |
| Pancuronium |
Theophylline may antagonize non-depolarizing neuromuscular blocking effects; possibly due to
phosphodiesterase inhibition. |
Larger dose of pancuronium may be required to achieve neuromuscular blockade. |
| Pentoxifylline |
Decreases theophylline clearance. |
30% increase |
| Phenobarbital (PB) |
Similar to aminoglutethimide. |
25% decrease after two weeks of concurrent PB. |
| Phenytoin |
Phenytoin increases theophylline clearance by increasing microsomal enzyme activity.
Theophylline decreases phenytoin absorption. |
Serum theophylline and phenytoin concentrations decrease about 40%. |
| Propafenone |
Decreases theophylline clearance and pharmacologic interaction. |
40% increase. Beta-2 blocking effect may decrease efficacy of theophylline. |
| Propranolol |
Similar to cimetidine and pharmacologic interaction. |
100% increase. Beta-2 blocking effect may decrease efficacy of theophylline. |
| Rifampin |
Increases theophylline clearance by increasing cytochrome P450 1A2 and 3A3 activity. |
20-40% decrease |
| Sulfinpyrazone |
Increases theophylline clearance by increasing demethylation and hydroxylation. |
20% decrease |
| Decreases renal clearance of theophylline. |
| Tacrine |
Similar to cimetidine, also increases renal clearance of theophylline. |
90% increase |
| Thiabendazole |
Decreases theophylline clearance. |
190% increase |
| Ticlopidine |
Decreases theophylline clearance. |
60% increase |
| Troleandomycin |
Similar to erythromycin. |
33-100% increase depending on troleandomycin dose. |
| Verapamil |
Similar to disulfiram. |
20% increase |
|
* Refer to
DRUG INTERACTIONSfor further information regarding table.
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** Average effect on steady state theophylline concentration or other clinical effect for pharmacologic
interactions. Individual patients may experience larger changes in serum theophylline concentration than the
value listed.
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The Effect of Other Drugs on Theophylline Serum Concentration Measurements: Most serum theophylline assays in
clinical use are immunoassays which are specific for theophylline. Other xanthines such as caffeine, dyphylline, and
pentoxifylline are not detected by these assays. Some drugs (e.g., cefazolin, cephalothin), however, may
interfere with certain HPLC techniques. Caffeine and xanthine metabolites in neonates or patients with renal
dysfunction may cause the reading from some dry reagent office methods to be higher than the actual serum
theophylline concentration.
Chemical IUPAC Name: 1,3-dimethyl-3,7-dihydropurine-2,6-dione
Chemical Formula: C7H8N4O2
Half Life: 8 hours
Drug Type: Approved Drug
# Accession No: APRD00082
CAS Registry Number: 58-55-9
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Theophylline News (When available)
Guardians of children's safety Jan 13, 2006 Appleton Post Crescent, Fourth-grader Austyn Maynard, 10, said Rammer always is paying attention at the right moments. "I tell her what's new because she always asks me," Austyn said. ...
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Belleayre Shows Its Appreciation Jan 12, 2006 OnTheSnow.com, Consumer demo days are Saturday and Sunday, with reps from Atomic, Blizzard, Elan and Dynastar on hand to hypnotize you with their latest gear. ...
Elan to Present at Healthcare Conferences in January 2006 Dec 22, 2005 PharmaLive.com (press release), DUBLIN, Ireland--(BUSINESS WIRE)--Dec 22, 2005 - Elan Corporation, plc announces that it will present at two healthcare conferences in January 2006. ...
Elan to Present at Healthcare Conferences in January 2006 Dec 22, 2005 Genetic Engineering News, On January 5, 2006, Elan will present at the Morgan Stanley Pharmaceutical CEO's Unplugged Conference in New York at 8:00 am Eastern Standard Time (EST), 1 ...
XM-R3 Triple Satellite Audio Receiver From ELAN Home Systems Now ... Dec 14, 2005 eHomeUpgrade, ELAN® Home Systems, a leading manufacturer of award-winning Multi-Room audio/video and home control systems, announced today that the company has begun ...
UPDATE 1-Wyeth plans trials of 3 Alzheimer drugs in 2006 Jan 13, 2006 Reuters The two other Wyeth medicines already in human trials are being developed under a 50/50 partnership with Irish drugmaker Elan Corp. ...
Winemakers begin to take advantage of court ruling Jan 12, 2006 Bothell Herald, For a small winery such as Elan, which makes about 1,000 cases a year, being able to ship is crucial, said owner Linda Elliott-Smith, who has had 15 cases of ...
Former National City, KeyCorp execs form new manager Jan 11, 2006 Pensions & Investments, Giesen. Mr. Giesen will be joined by former National City colleagues Mitchell Krahe and Ori Elan. Mr ... Messrs. Giesen and Elan. The ...
News In Brief Jan 11, 2006 Unison.ie, ELAN has entered into a licensing agreement in which EntreMed will use its nanocrystal technology to develop its oncology drug Panzem. ...
What's your winter wonderland? Jan 10, 2006 ic Wales, The usual suspects of Snowdon, Gower and the Elan Valley featured strongly but it was Tenby that was declared the surprise winner in terms of votes cast. ...
Biogen: FDA to rule on Tysabri Jan 10, 2006 MarketWatch Biogen and partner Elan Pharmaceuticals voluntarily pulled Tysabri from the market in February 2005 after three cases of PML were reported. ...
European Stocks Fall in Week; Stoxx 600 Snaps 11-Week Advance Jan 14, 2006 Bloomberg Standard & Poor's raised its outlook on the company's debt to stable from negative on better earnings prospects. Elan Corp. surged 13 percent to 13.14 euros. ...
Volunteer Opportunities Jan 13, 2006 Boston Globe, ...and Brockton. Please contact Elan Babchuck at 617-457-8669 or ebabchuck@jcrcboston.org. MATCH-UP Interfaith Volunteers Inc. needs ...
Injury time looms on Big Brother Jan 14, 2006 Telegraph.co.uk, ...nightmares. No Englishman would have survived them, and I hope his dignity and elan continue to put us to shame for years to come.
Where does the other half live? Jan 14, 2006 Unison.ie, ...addresses. Kelly Martin, the former Merrill Lynch investment banker who runs Elan, gives his address as 1040 Fifth Avenue, New York. ...
Top tournament in North Wales Jan 14, 2006 Wrexham Evening Leader, Ruthin have four players with Sioned Roberts and Elan Iorwerth in the under 16s and Llyr Iorwerth and Sarah Delonger in the 18s. ...
Hate the old kitchen? Love the new one Jan 14, 2006 DesMoinesRegister.com, Davis suggested the heavy, comfortable bar chairs from Elan Contemporary Furnishings in Omaha that surround the eating part of the kitchen island. ...
ISEQ breaches 7500 threshold Jan 9, 2006 Ireland Online, AIB rose 4c to €18.49 and Bank of Ireland rose 1c to €13.83. Pharmaceutical company Elan also recorded heavy gains, finishing up 36c to €12.02. ...
ISEQ falls just short of 7500 mark Jan 11, 2006 Ireland Online, The Dublin market closed up 71.41 points at 7494.37 as Elan led the charge, up 69c, almost 6%, to €12.55. It was a mostly positive day for the financials. ...
10.45am Markets Update Jan 10, 2006 RTE.ie, Shares in Ryanair were down 11 cent to €7.98 after a broker downgrade, while Elan shares lost 12 cent to stand at €11.90 after it announced a new ...
Schaeffer's Top and Bottom Ranked Stocks (CEPH, ELN, HSY) Jan 9, 2006 Schaeffers Research, ...trading opportunities. The stocks appearing on today's list of top and bottom ranked stocks are Cephalon, Elan, and Hershey. Not ...
Live at MacWorld: EVDO to Upgrade for MacBook Pro Jan 11, 2006 Gizmodo.com, ...updated as news comes in. The EVDOinfo forum reports a USB 2.0 dongle sold by Elan Digital Systems. EVDOinfo’s ExpressCard page ...
New drugs use saliva to help relieve pain Jan 10, 2006 Auburn Citizen, ...about. Recently, new drugs have been added to the market, exenatides (Byetta/Amylin Lilly) and ziconotides (Prialt/Elan). These ...
Irish stock exchange on course to be European favourite Dec 31, 2005 The Sunday Times, The main laggards were: Elan, where concerns over Tysabri affected investor sentiment; Waterford Wedgwood, which was dogged by weak sales in America; and Iona ...
2005 Gave Nanotech Investors Plenty to Chew On Jan 6, 2006 Motley Fool American Pharmaceutical's success was closely followed by an announcement that Roche had signed a deal with Elan (NYSE: ELN) to apply Elan's nanocrystal ...
Sharewatch: Desmond piles up the chips on Amarin’s march to ... Dec 31, 2005 The Sunday Times, The drug development company spun out of Elan raised $26.4m (€22.3m) just days before Christmas to fund what it hopes will be the final phase of trials for ...
CES Day Two: Must-Haves For Homebodies Jan 6, 2006 KLAS-TV, ...all into one system.". Elan's home systems aren't just for the rich and famous building a brand new custom home. "About 50-percent ...
UK Stocks Climb, Paced by Royal Bank of Scotland; P&O Surges Jan 11, 2006 Bloomberg Ireland's ISEQ Overall Index gained 0.8 percent to 7481.25, buoyed by shares of Elan Corp. ... Shares of Elan increased 3.7 percent to 12.3 euros in Dublin. ...
Joshi, Dhruv in title clash Jan 13, 2006 Rediff, In the semi-finals, Maharashtra's Joshi, potting with elan, displayed silken touch to wallop Rupesh Shah of Gujarat 1498-832, while promising Dhruv halted the ...
Brockton girls are doubles trouble Jan 12, 2006 Boston Globe, Bay Independent: With 10 seconds left in regulation, junior Elan Ziff (15 points) made two free throws to give Gann (3-4) a 56-54 victory over BU Academy. ...
Basketball: UNT men, women aiming for third conference victory 16 Jan 2006 Dallas Morning News (subscription), ...back on track. Lasma Jekabsone, a 6-3 center, comes into the game averaging 13.5 points and 9.5 rebounds a game. The junior from ...
Freshman leads women in second Sun Belt win Jan 12, 2006 Beacon Newspaper (subscription), ...rebounds. "She had a really good shooting night and she was the leader on the floor in the game," said junior center Lasma Jekabsone. ...
Thornton scores 37, but FSU men fall Jan 15, 2006 Miami Herald, Denver 50, Florida International 45: Lasma Jekabsone had 10 points and 12 rebounds in a losing effort as the Golden Panthers (9-6, 3-1 Sun Belt) fell to ...
Denver Downs Florida International, 50-45 Jan 14, 2006 DenverPioneers.com, With one minute remaining, the Panthers cut the Pioneer lead to two off back-to-back baskets by FIU leading scorer Lasma Jekabsone. ...
ODU women fall as layups, foul shots fail to drop Dec 21, 2005 Virginian Pilot, Panthers in a Wednesday matinee at Florida International’s Pharmed Arena, the Monarchs succumbed to poor second-half shooting and center Lasma Jekabsone in ...
Coach Russo prepares for tough second half of season Jan 9, 2006 Beacon Newspaper (subscription), ...lies ahead. Lasma Jekabsone is averaging nearly 15 points, 10 rebounds and is shooting just about 50 percent from the field. Wasn ...
Injuries alter NSU guard's view Jan 10, 2006 Sun-Sentinel.com, FIU: Lasma Jekabsone, Sun Belt player of the week, leads the conference in blocked shots with an average of 3. Her total of 110 is fourth on the school's all ...
Golden Panthers stifle Trojans Jan 6, 2006 Miami Herald, Sun Belt Conference opener. FIU's Lasma Jekabsone and Marquita Adley each snagged 10 rebounds in the victory. FIU's bench players ...
FIU women rally, topple N. Illinois Dec 30, 2005 Miami Herald, Freshman guard Iva Ciglar's 13 points gave FIU a much-needed spark off the bench to complement leading scorer Lasma Jekabsone, who scored 22 points. ...
Thornton powers Seminoles past Hokies Jan 8, 2006 Sun-Sentinel.com, Miami· Faeza Bouderra and Lasma Jekabsone combined to hit all six free throws in the final 26 seconds to help FIU defeat Arkansas State 54-51. ...
FAU baseball gets recognition Jan 7, 2006 Miami Herald, Junior basketball player Lasma Jekabsone was named the Sun Belt Conference's Player of the Week for the first time in her career. ...
FIU rallies to victory Dec 31, 2005 Miami Herald, Tournament MVP Lasma Jekabsone began the Golden Panthers' run by hitting two free throws at the 9:45 mark to cut the lead to 15.
Kansas women top FIU, remains unbeaten Dec 18, 2005 Miami Herald, Eva Makela had 16 points on six of 15 shooting to lead Florida International (4-4). Iva Ciglar and Lasma Jekabson each had 14 points, LaQuetta Ferguson had 12 ...
Game Preview: Florida International at Kansas Dec 18, 2005 Kansas City Star, | |