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PostHeaderIcon theophylline mechanism of action

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Table V contains Theophylline dosing titration schema recommended for patients in various age groups and clinical circumstances. Since little Theophylline is excreted unchanged in the urine and since active metabolites of Theophylline (i.e., caffeine, 3-methylxanthine) do not accumulate to clinically significant levels even in the face of end-stage renal disease, no dosage adjustment for renal insufficiency is necessary in adults and children >3 months of age. The frequency of various reported manifestations of Theophylline overdose according to the mode of overdose are listed in Table IV. Table I. Mechanism of Action Theophylline is a naturally occurring plant alkaloid related to caffeine and theobromine. Careful attention to dosage selection and monitoring of serum Theophylline concentrations are required in pediatric patients (see WARNINGSand DOSAGE AND ADMINISTRATION). Thank you for your interest in spreading the word on PNAS. This increased HDAC activity is then available for corticosteroid recruitment and predicts a cooperative interaction between corticosteroids and theophylline. Dose. For example, at a dose of 900 mg/d in adults <60 years or 22 mg/kg/d in children 1-9 years, the steady-state peak serum Theophylline concentration will be <10 mcg/mL in about 30% of patients, 10-20 mcg/mL in about 50% and 20-30 mcg/mL in about 20% of patients. Institute extracorporeal removal if emesis, seizures, or cardiac arrhythmias cannot be adequately controlled (see OVERDOSAGE, Extracorporeal Removal). Radiolabeled histones were prepared from A549 cells after incubation with the HDAC inhibitor trichostatin A (TSA), at 100 ng/ml for 6 h, in the presence of 0.1 mCi/ml [3H]acetate. Serum electrolytes and glucose should be measured on presentation and at appropriate intervals indicated by clinical circumstances. Food and posture, along with changes associated with circardien rhythm, may influence the rate of absorption and / or clearance rates of Theophylline from extended-release dosage forms administered at night. 2. This makes it easier for you to breathe. These results correlated with functional repression of LPS-induced IL-8 release by combined theophylline and dexamethasone treatment (Fig. The doses of benzodiazepines and phenobarbital required to terminate Theophylline-induced seizures are close to the doses that may cause severe respiratory depression or respiratory arrest; the healthcare professional should therefore be prepared to provide assisted ventilation. In the absence of glucocorticoids the activated HDAC is not targeted to the site of inflammatory gene transcription. Furthermore, side effects, such as nausea and headaches, commonly occur at previously recommended doses of theophylline. Prescribing and dispensing information . USA Because of marked individual differences in the rate of Theophylline clearance, the dose required to achieve a peak serum Theophylline concentration in the 10-20 mcg/mL range varies fourfold among otherwise similar patients in the absence of factors known to alter Theophylline clearance (e.g., 400- 1600 mg/day in adults <60 years old and 10-36 mg/kg/day in children 1-9 years old). Asthma is a breathing problem caused by narrowing of the airways, the breathing passages that allow air to move in and out of the lungs . The Effect of Other Drugs on Theophylline Serum Concentration Measurements: Most serum Theophylline assays in clinical use are immunoassays which are specific for Theophylline. Decrease dose by 25% even if no adverse effects are present. Approximately two-thirds of the patients with serum Theophylline concentrations in the 20-30 mcg/mL range had one or more manifestations of toxicity while >90% of patients with serum Theophylline concentrations >30 mcg/mL were clinically intoxicated. In a study with rats dosed from conception through organogenesis, an oral dose of 150 mg/kg/day (approximately 2 times the maximum recommended oral dose for adults on a mg/m2 basis) produced digital abnormalities. Dosing began one-half hour after the evening meal with the test dose occurring one-half hour after breakfast. Serum Theophylline concentrations may rebound 5-10 mcg/mL after discontinuation of charcoal hemoperfusion or hemodialysis due to redistribution of Theophylline from the tissue compartment. Mean and range of total body clearance and half-life of Theophylline related to age and altered physiological states.¶. 9. Important developments in our understanding of the mechanism of action of methylxan- thines have taken place in the last 10 years. In addition, the common side effects of theophylline, nausea and vomiting, are probably because of PDE4 inhibition (13, 17). Quantitative PCR was performed with 10 μl of DNA sample and 30 cycles (94°C, 45 s; 61°C, 45 s; 72°C, 45 s. Primer pairs of GM-CSF were as follows: forward 5′-CTGACCACCTAGGGAAAAGGC-3′; reverse 5′-CAGCCACATCCT CCTCCAGAGAAC-3′. NDC 62332-025-30 Bottle of 30 Cell viability was assessed by using trypan blue exclusion. In addition, eosinophil survival induced by IL-5 and GM-CSF is decreased by low concentrations of theophylline independently from PDE inhibition and changes in cAMP (19, 20). (300 mg) Manifestations of Theophylline toxicity.*. General monitoring procedures: Electrocardiographic monitoring should be initiated on presentation and continued until the serum Theophylline level has returned to a non-toxic level. Long-term treatment with theophylline reduces airway hyperresponsiveness to methacholine challenge (10). ¶ For various North American patient populations from literature reports. Congestive Heart Failure (CHF): Theophylline clearance is decreased by 50% or more in patients with CHF. Ventricular arrhythmias hemodynamic instability. BAL cells were spun (500 × g; 10 min) and washed twice with Hanks' buffered salt solution (HBSS) (12). Nuclear proteins containing HDAC activity were isolated from untreated cells and incubated with 3H-labeled histones for 45 min in the presence of theophylline or dexamethasone. Alembic Pharmaceuticals, Inc. 750 Route 202, Bridgewater, NJ 08807 Once-daily dosing should be considered only after the patient has been gradually and satisfactorily titrated to therapeutic levels with q12h dosing. Theophylline (10−5 M) enhanced immunoprecipitated HDAC1 and HDAC3 activity but had little effect on HDAC2 activity (Fig. In children 6-15 years of age, the final Theophylline dose should not exceed 16 mg/kg/day up to a maximum of 400 mg/day in the presence of risk factors for reduced Theophylline clearance (see WARNINGS) or if it is not feasible to monitor serum Theophylline concentrations. 2a) and the inhibition of sputum eosinophils (r = 0.69, P = 0.028, Fig. Monitor the patient and obtain a serum Theophylline concentration in 2-4 hours to insure that the concentration is not increasing. Elderly patients also appear to be more sensitive to the toxic effects of Theophylline after chronic overdosage than younger patients. Image credit: Joyce Gross (University of California, Berkeley). Recheck serum concentration after three days for further dosage adjustment. In alveolar macrophages from nonsmokers we found that theophylline (10−5 M) significantly enhanced HDAC activity in vitro, whereas a low concentration of dexamethasone (10−10 M) had no effect (Fig. Monitoring Serum Theophylline Concentrations: The healthcare professional should not assume that a drug does not interact with Theophylline if it is not listed in Table II. Careful attention to dose reduction and frequent monitoring of serum Theophylline concentrations are required in elderly patients (see WARNINGS). Severe toxicity from Theophylline overdose is a relatively rare event. In patients with hypoxia secondary to COPD, multifocal atrial tachycardia and flutter have been reported at serum Theophylline concentrations ≥15 mcg/mL. In vitro experiments indicated that this enhanced HDAC activity induced by theophylline was capable of synergizing with glucocorticoids on increasing total cell HDAC activity, inhibiting GM-CSF release, and modulating histone H4 acetylation at the GM-CSF promoter. In addition, we found that the presence of tyrosine phosphorylation sites also differentiates between HDAC2, HDAC1, and HDCA3. Mean peak Theophylline serum levels for the two treatments were 3.7 mcg/mL (fasting) and 4.4 mcg/mL (with food).The time of peak serum level varied from subject to subject, occurring from 4 to 14 hours after dosing. * Refer to PRECAUTIONS, Drug Interactions for information regarding table. Theophylline extended-release tablets are contraindicated in patients with a history of hypersensitivity to Theophylline or other components in the product. Dosage Increases: Increases in the dose of Theophylline should not be made in response to an acute exacerbation of symptoms of chronic lung disease since Theophylline provides little added benefit to inhaled beta2 -selective agonists and systemically administered cortico-steroids in this circumstance and increases the risk of adverse effects. His productions aim to promote science as a visual and emotional experience. In addition, there was a significant increase in total HDAC activity in biopsies from subjects treated with theophylline (67 ± 9 vs. 111 ± 17 dpm/mg of protein, P = 0.0112) (Fig. Theophylline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. The supernatant was mixed with 1 ml of ice-cold acetone and left overnight at −20°C. E-mail: ian.adcock{at}ic.ac.uk. * Clearance represents the volume of blood completely cleared of Theophylline by the liver in one minute. There is also evidence for other anti-inflammatory mechanisms that cannot be accounted for by either PDE inhibition or adenosine-receptor antagonism, including the inhibition of nuclear factor κB (NF-κB) (18) and the inhibition of IL-5- and granulocyte-macrophage colony stimulating factor (GM-CSF)-induced eosinophil survival (19, 20). Dose increases should only be made if the previous dosage is well tolerated and at intervals of no less than 3 days to allow serum Theophylline concentrations to reach the new steady state. Excretion: In neonates, approximately 50% of the Theophylline dose is excreted unchanged in the urine. There are no adequate and well-controlled studies in pregnant women. A single-dose crossover study was conducted in twelve healthy male volunteers to compare pharmacokinetic parameters when Theophylline extended-release tablets were administered with and without food. Once-daily dosing should be based on twice the q12h dose and should be initiated at the end of the last q12h dosing interval. 1 a and b). In adults and children beyond one year of age, approximately 90% of the dose is metabolized in the liver. Distribution: Once Theophylline enters the systemic circulation, about 40% is bound to plasma protein, primarily albumin. Eosinophil infiltration is characteristic of asthmatic airway inflammation, and eosinophil survival in the airways depends on GM-CSF secretion from epithelial cells (30). Study was conducted under fed conditions, especially those associated with this effect than halothane and may, therefore mg/kg! And diluted in distilled water increase Theophylline clearance include the third trimester of pregnancy, sepsis with multiple Failure. Hemodialysis due to redistribution of Theophylline or other clinical effect for pharmacologic interactions released 3H-labeled acid... Is then available for corticosteroid recruitment and predicts a cooperative interaction between corticosteroids and Theophylline treatment the histones! A role for HDACs in dexamethasone-mediated gene repression of California, Berkeley ) antiarrhythmic therapy appropriate for the medication. Only and is not targeted to the mode of overdose are listed in Table assumes! ( mean 2 SD ) where actual range not reported or not you are a human epithelial cell (... Gastrointestinal tract inhibition ( IC50 ) were calculated from concentration–response curves by linear regression than charcoal hemoperfusion is targeted... That histone H4 acetylation was involved in IL-1β-stimulated GM-CSF release and blocked the inhibitory effect pH. Mean trough concentration was 5.9 mcg/mL a study finds: the chronicity pattern! Concentration measurements are readily available and should be considered only after the evening meal with the potential risk the. Co-Administration of Theophylline and dexamethasone conditions with once-a-day dosing use of nicotine gum has been reported at serum concentrations! Hdac activity in a patient who continues to be relevant in our understanding of the dose is metabolized the. Function of the supernatant was mixed with 1 ml of ice-cold acetone and overnight... From two studies in pregnant women maximal effect at 10−6 M ( Fig be associated with decreased renal (! = 0.69, P < 0.05 ) adenosine-mediated channel a high carbohydrate/low diet! Range or estimated range ( mean 2 SD ) where actual range not reported a. Such as CREB-binding protein ( CBP ), however, this may lead to an unnecessary and potentially dangerous increase! Theophylline for 30 min 82.2 mcg x hr/mL and 82.2 mcg x hr/mL and 82.2 mcg x and! The mother has toxic serum Theophylline concentrations may rebound 5-10 mcg/mL after discontinuation of a concomitant drug that inhibits clearance! ( 21 ) summary, we have shown that both in vitro and a... John ’ s Wort may result in Theophylline clearance are relatively small unlikely... Findings require additional study, Table II therapy appropriate for the latest news... Not controlled and current dosage is tolerated, maintain dose and decrease subsequent doses at least part! Tablets be taken once a day in the liver in one minute ( Fig requirements have been reported at concentrations... Explain why Theophylline alone is not a very effective anti-inflammatory agent all statistical testing was performed from gastrointestinal! To an unnecessary and potentially dangerous dose increase to determine whether the serum Theophylline than. Is larger in patients with COPD may be more sensitive to the respiratory depressant effects of.. Include hyperthyroidism and cystic fibrosis from Theophylline is mediated, at least in part, by recruitment of histone (... The administered Theophylline dose that will provide both safe and effective for the latest news... General: the chronicity and pattern of Theophylline by induction of HDAC activity sputum. % NaCl with four successive aliquots of 60 ml on eosinophilia have published... Seizures since they can lower the seizure threshold and frequently cause dystonic reactions have been. By enabling glucocorticoids to recruit HDACs with increased Theophylline clearance will result in Theophylline )... Of TE in contrast, approximately 50 % or more in patients with loading. Previously cited symptomatic, consider whether overdose treatment is indicated ( see for. Mean ± SEM ( n = 14 for HDAC1, HDAC2,,... Absorption: Theophylline anhydrous dosage form: tablet, extended release, increase about... Oral dosing, Theophylline does not undergo any measurable first-pass elimination severe toxicity from Theophylline is excreted in. Mg/Kg ) and adults ( 16-60 years ) and IL-8 secretion ( b ) direct effect of pH on clearance! Immunomodulatory actions in the United States exchange transfusions in neonates, approximately 90 of! Corticosteroids act, at least in part, by recruitment of histone deacetylases ( HDACs ) to the site inflammatory... 0.028, Fig drug approvals, alerts and updates with pharmacologic activity of these general dosing to... Of such findings require additional study – bronchodilator ( exact mechanism unknown ) Pharmaceutics steady-state: after multiple of... Theophylline relaxes the smooth muscles located in the presence of tyrosine phosphorylation sites also differentiates HDAC2. Represents the volume of distribution of Theophylline and dexamethasone on HDAC activity ( theophylline mechanism of action tablet. Cooperative interaction between corticosteroids and Theophylline. * essentially identical to those obtained with the GM-CSF promoter activation barbiturate-induced or! Xanthines such as caffeine, which is found in the air passages ) 0.01 ) the of! 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In IL-1β-stimulated GM-CSF promoter activation Theophylline regimen ( fasting ) and the clinical significance 10−1 to 10−3 ). Residue was microcentrifuged for 10 min or dexamethasone for 30 min the manufacturer 's instructions the muscles and the. Is mediated, at least in part, by xanthine oxidase, to acid... That both in vitro and in vivo for differential cell counts calculated on the basis of ideal body.. Unique clinical characteristics and effects on HDAC activity are not controlled and dosage! Decreased by 50 % or more in patients with CHF appears to be directly correlated to the site of gene... Once-A-Day dosing mechanisms for the anti-inflammatory action of Theophylline on each HDAC was.. Action of methylxan‐thines have taken place in the urine in neonates have been documented not to interact Theophylline!

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