When did they start? Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances. Theophylline is a bronchodilator that is used to treat symptoms of asthma, bronchitis, emphysema, and other breathing problems. We comply with the HONcode standard for trustworthy health information. Saliva theophylline concentrations are not reliable for dose adjustments without special techniques. Guidelines on the management of asthma. Mean maximal increase (95% CI) in the FEV1 was 7.8% (2.4, 13.2), 17.1% (10.0, 24.2), 16.6% (11.2, 22.0), and 1.0% (1.1, 3.1) during infusion of aminophylline, olprinone, aminophylline and olprinone, and saline, respectively (anova P < 0.01). Theophylline (dimethylxanthine) has been used to treat airway diseases for more than 80 years. Bronchoscopic lung volume reduction with endobronchial Zephyr Valves for severe emphysema: A systematic review and meta-analysis. These are beta 2 agonists (salbutamol, bambuterol and terbutaline) and methylxanthines (theophylline and aminophylline). Accessibility May make these conditions worse. There are no additive or synergistic effects of administration of olprinone and aminophylline at the same time. Often, two sets of ears are better than one when you're learning about a complicated medical problem, such as COPD. This oral solution works by relaxing the muscles around your airways to help you breathe easier. If your primary care provider suspects that you have COPD, you'll likely be referred to a pulmonologist a doctor who specializes in lung disorders. Revised 2002 Jan 12; Accepted 2002 Oct 7. aminophylline, asthma, bronchodilatation, olprinone, phosphodiesterase 3 inhibitors. In: Harrison's Principles of Internal Medicine. Anosmia, whichis currently under investigation. Reduce dose carefully and monitor frequently. Foster RW, Rakshi K, Carpenter JR, Small RC. Others use oxygen all the time. With the availability of better and safer bronchodilators, the use of theophylline should not be routine. It was originally used as a bronchodilator but the relatively high doses required are associated with frequent side effects, so its use declined as inhaled 2-agonists became more widely used.More recently it has been shown to have anti-inflammatory effects in asthma and COPD at lower concentrations. You might need regular blood tests to make sure you're getting the correct . Your doctor may ask some of the following questions: Your doctor will ask additional questions based on your responses, symptoms and needs. https://goldcopd.org/. https://www.nhlbi.nih.gov/health-topics/copd. Theophylline is a bronchodilator, which means that it relaxes the muscles in your airways so that air passes through easier. National and international guidelines recommend the use of theophylline as second-line or, in most cases, third-line treatment for patients whose symptoms are not adequately controlled with corticosteroids and 2-adrenoceptor agonists [1-3].Indeed, theophylline is less effective as a bronchodilator than the inhalation of 2-agonists [], and is less effective as an anti . However, there is no evidence demonstrating the clinical usefulness of PDE inhibitors in the treatment of asthma. Accessed June 26, 2019. Those who are not currentlytaking theophylline should be given a loading dose of 5 to 7 mg/kg intravenously, followed by a maintenance dose of0.4 to 0.6 mg/kg per hour intravenously to maintain serum concentrations at 10 to 15 mg/L. Patient Education Dosage Forms Excipient information presented when available (limited, particularly for generics); consult specific product labeling. These observations suggest that PDE3 inhibitors may be effective as bronchodilators in asthmatics. If you are a Mayo Clinic patient, this could Medically reviewed by Drugs.com. Olprinone alone or in combination with aminophylline lowered diastolic blood pressure, and increased heart rate. CNS symptoms (irritability, lightheadedness, and dizziness) can also occur in patients. and transmitted securely. health information, we will treat all of that information as protected health In patients 1, 3, 7, 9 and 12, the effect of aminophylline was similar to placebo. Theophylline clearance is decreased 50% or more in hepatic insufficiency (e.g. Although theophylline isn't used much anymore, it can be helpful for nighttime asthma symptoms. The patient's electrolyte concentrations, fluid balance, and acid-base balance require monitoring during prolonged IV therapy. Theophylline: mechanism of action and use in asthma and chronic obstructive pulmonary disease. Worsening of the current illness, an occurrenceof a new illness, or any change in the patient's treatment protocol that may alter theophylline clearance should also promptthe physician to check serum concentrations of theophylline. Management of airway mucus hypersecretion on chronic airway inflammatory disease: Chinese expert consensus. Historically, theophylline has had two primary indications: as a bronchodilator for patients with asthma or chronic obstructive pulmonary disease and as an agent to treat apnea and bradycardia in premature newborns. 2018; doi:10.1016/j.mayocp.2018.05.026. In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. Accessed March 10, 2020. 1998 May:44(5):1124-8 [PubMed PMID: 9590396], Mouni J, Richard L, Ribon B, Hersant J, Sarmini H, Houin G. Methods of theophylline assay and therapeutic monitoring of this drug. Some patients have also experienced adverse effects at low plasma concentrations. We thank Eisai Co., Ltd. (Tokyo, Japan) for measuring the olprinone concentration. Only increase dose if the current dose is well tolerated. Epub [PubMed PMID: 25894641], Hendeles L, Weinberger M. Avoidance of adverse effects during chronic therapy with theophylline. Morgan Ltd, Gillingham, Dorset, UK). A clinical study in 2008 reported that theophylline could potentially improve the sense of smell in those with anosmia. Theophylline is a drug derived from methylxanthine (a purine derivative) and has smooth muscle relaxant, bronchial dilation, diuretic, cardiac and central nervous system (CNS) stimulant activities. We compared the bronchodilator effects of intravenously administered olprinone, a selective PDE3 inhibitor, and aminophylline, a nonselective PDE inhibitor, both alone and concomitantly. All rights reserved. It is also anonselective adenosine receptor antagonist. Calculate dose based on this formula: Concentration = loading dose / volume of distribution, Each mg/kg ideal body weight theophylline administered over 30 minutes increases serum theophylline approximately 2 mcg/mL (assuming volume of distribution of 0.5 L/kg). It may not cover all possible information. The present study compared the cardiopulmonary effects of olprinone and aminophylline alone and in combination in a double-blind crossover fashion over a total period of 150 min. Oral theophylline has been used as a bronchodilator . Exacerbations may be caused by a respiratory infection, air pollution or other triggers of inflammation. Mean maximal increase in FEV1 was calculated based on the highest value of FEV1 among 30, 60, 90 and 120 min after the start of each infusion. You may have to give up some activities you previously enjoyed. This activity will highlight the mechanism of action, adverse event profile . Theophylline is a medication used to treat asthma and chronic obstructive pulmonary disease as a second-line drug. Stomach ulcerUse with caution. BMJ (Clinical research ed.). Spirometry was performed and evaluated with ATS criteria for acceptability and reproducibility [14]. And you may benefit from counseling or medication if you feel depressed or overwhelmed. Theophylline as a Bronchodilator in COPD and Its Combination with Inhaled -Adrenergic Drugs The bronchodilating action of theophylline in COPD has been examined, with emphasis on its combined use with inhaled 2 agonists. tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over the affected area, confusion about identity, place, and time, dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position, fast, pounding, or irregular heartbeat or pulse, numbness or tingling in the hands, feet, or lips, pain or discomfort in the arms, jaw, back, or neck, shakiness in the legs, arms, hands, or feet, vomiting of blood or material that looks like coffee grounds. Your family and friends may have difficulty adjusting to some of the changes. This activity reviews the indications, action, and contraindications for theophylline as a potential agent in treating asthma and chronic obstructive pulmonary disease. Nevertheless, theophylline remains an important drug: Before Jameson JL, et al., eds. Bethesda, MD 20894, Web Policies Theo-24, Theo-Dur, Quibron-T/SR, Elixophyllin, +6 more. For patients taking oral treatment, monitor serum concentrations at 6-month intervals for rapidly developing children and at annual intervals for all other patients (if their symptoms are well controlled). In conclusion, intravenous PDE3 inhibitors exhibit bronchodilatory effect. 1. Very large overdoses, such as those during suicide attempts, could potentially be lethal because of the development of arrhythmias and convulsions. If it is safe to put it in the trash, pour the medication out of the container. 2001 Nov:108(5):671-80 [PubMed PMID: 11692087], Weinberger M, Hendeles L. Theophylline in asthma. Accessed May 28, 2018. Blood pressure and heart rate also were recorded prior to the pulmonary function tests. The currentlyrecommended loading dose is 6 to 7 mg/kg administered intravenously over 20 to 30 minutes. This activity will highlight the mechanism of action, adverse event profile, pharmacokinetics, and drug interactions pertinent for members of the interprofessional team in the treatment of patients with asthma and chronic obstructive pulmonary disease. Trials of the bronchodilator activity of the isoenzyme-selective phosphodiesterase inhibitor AH 21-132 in healthy volunteers during a methacholine challenge test. Theophylline doses should not exceed 400 mg/d. Available for Android and iOS devices. Initial dose: No adjustment recommended in patients over 3 months of age. Therefore, the lower concentration of aminophylline would be a possible reason why the bronchodilator effect of intravenous aminophylline was observed in only a proportion of the patients. Careers. Depending on the severity of your disease, you may need a short-acting bronchodilator before activities, a long-acting bronchodilator that you use every day or both. Inhalation of salbutamol at a dose of 300 g was performed 120 min after the start of each infusion. Hansel TT, Tennant RC, Tan AJ, Higgins LA, Neighbour H, Erin EM, Barnes PJ. It works by opening the airways of the lungs, making it easier to breathe. Journal of the American Medical Association. However, long-term use of these medications can have serious side effects, such as weight gain, diabetes, osteoporosis, cataracts and an increased risk of infection. Dose adjustments should be guided by serum theophylline concentrations. Bronchodilators are medicines that relax the muscles in the bronchial tubes (air passages) of the lungs. This site needs JavaScript to work properly. Even for more advanced stages of disease, effective therapy is available that can control symptoms, slow progression, reduce your risk of complications and exacerbations, and improve your ability to lead an active life. 2014:10(4):297-303 [PubMed PMID: 25594527], Essayan DM. The maximum increase in FEV1 produced by olprinone was significantly (P < 0.01) greater than that produced by aminophylline, and was equal to that achieved by salbutamol during aminophylline infusion; in addition, the onset of action of olprinone was rapid. We compared the acute cardiopulmonary effects of intravenously administered olprinone and aminophylline both alone and concomitantly. Pacifici GM. privacy practices. In: StatPearls [Internet]. Extended release tablets may pass an intact tablet matrix in the stool or colostomy bag which has little or no theophylline remaining. Ogawa T, Ohhara H, Tsunoda H, Kuroki J, Shoji T. Cardiovascular effects of the new cardiotonic agent 1,2-dihydro-6-methyl-2-oxo-5-(imidazo[1,2-a]pyridin-6-yl)-3-pyridine carbonitrile hydrochloride monohydrate. Brand names of this medication are Elixophyllin and Slo-Phyllin. Dosing must be based on peak serum concentrations for maximum benefit with minimum risk. Drugs.com provides accurate and independent information on more than 24,000 prescription drugs, over-the-counter medicines and natural products. Weight over 45 kg or age 16 years and older: Peak and trough serum levels may vary from the previous regimen. 8600 Rockville Pike Chronic obstructive pulmonary disease. Medically reviewed by Drugs.com. Aminophylline and olprinone, either alone or in combination, produced more bronchodilatation than saline (Figure 1). It is a bronchodilator. 1990:48(5):287-93 [PubMed PMID: 2195925], Aronson JK, Hardman M, Reynolds DJ. Once symptoms improve, your doctor can talk with you about measures to prevent future exacerbations, such as quitting smoking; taking inhaled steroids, long-acting bronchodilators or other medications; getting your annual flu vaccine; and avoiding air pollution whenever possible. Tell your care team if your symptoms do not improve or if they get worse. It acts on A1, A2, and A3 receptors with almost the same affinity, which possibly explains theophylline's cardiac effects. European journal of respiratory diseases. Administering by inhalation is both irritating and ineffective. Bronchodilator effect of inhaled olprinone, a phosphodiesterase 3 inhibitor, in asthmatic patients. National Asthma Project. Theophylline belongs to a group of medicines known as bronchodilators. These patients could be regarded as nonresponders to aminophylline. In 12 patients with mild stable asthma, we compared the acute bronchodilator effects of the following two drugs, alone and together using a double-blind crossover design: intravenous administration of olprinone, 30 g min1; aminophylline, 2.25 mg min1; and olprinone plus aminophylline over a total period of 150 min. Do you or have you ever smoked cigarettes? Theophylline Oral Solution - Clinical Pharmacology. 2017; doi:10.1183/13993003.00791-2016. Wedzicha JA, et al. Also, avoid secondhand smoke exposure whenever possible. Theophylline is an orally administered xanthine derivative that induces relaxation of smooth muscle in the bronchial tree causing bronchodilation. March 11, 2020. or 95% confidence intervals (CI). Other contraindications include hypersensitivity to xanthine derivatives and patients with coronary artery disease (where the cardiac stimulation effect of theophylline might prove harmful). You'll work with a variety of specialists, who can tailor your rehabilitation program to meet your needs. COPD lifestyle changes. Foster and colleagues [12] reported that intravenous AH 21-132, a dual inhibitor of PDE3 and PDE4, exhibits weak and short-lived bronchodilatation in healthy volunteers. Theophylline causes the endogenous release of . National Academy of Clinical Biochemistry. A clinical practice guideline update from the American College of Physicians, American College of Chest Physicians, American Thoracic Society, and European Respiratory Society. These medications are useful for people with frequent exacerbations of COPD. https://www.lung.org/lung-health-and-diseases/lung-disease-lookup/copd/living-with-copd/copd-lifestyle-changes.html. Before Do not alter the dose, timing, or frequency of administration without consulting a healthcare provider. Notify health care professional immediately if these occur. However, the present study does not provide any information on the use of intravenous aminophylline or olprinone during a severe acute asthma attack. 2011; doi:10.7326/0003-4819-155-3-201108020-00008. It is a bronchodilator. Have started or stopped taking another medicine in the last few weeks. Last updated on Sep 6, 2022. Polson JB, Krzanowski JJ, Goldman AL, Szentivanyi A. Inhibition of human pulmonary phosphodiesterase activity by therapeutic levels of theophylline. Side effects may include bruising, oral infections and hoarseness. Sign up for free and stay up to date on research advancements, health tips, current health topics, and expertise on managing health. Side effects are dose related and may include nausea, headache, fast heartbeat and tremor, so tests are used to monitor . This creates extra space in your chest cavity so that the remaining healthier lung tissue can expand and the diaphragm can work more efficiently. Outline the importance of collaboration and coordination among the interprofessional team to enhance patient care when dosing and monitoring theophylline therapy. FVC and FEV1 were measured on a dry wedge spirometer (Transfer Test; P.K. Pharmacists can verify dosing and perform medication reconciliation, and nurses can counsel on dosing and adverse effects. Shen Y, et al. 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Have changed your diet in the last few weeks. INDICATIONS AND USAGE Your doctor may decide not to treat you with this medication or change some of the other medicines you take. Furthermore, in patients 1, 3, 7, and 9, who did not have bronchodilator response to aminophylline, aminophylline concentration was low. This content does not have an English version. One proposed mechanism is that theophylline, through nonselective phosphodiesterase (PDE) inhibition, raises the intracellular cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) concentrations, resulting in relaxation of airway smooth muscle, although a total therapeutic concentration of theophylline inhibits PDE activity in human lung extract by only 510% [6]. On A1, A2, and increased heart rate the clinical usefulness of PDE inhibitors the. A severe acute asthma attack in is theophylline a bronchodilator levitra professional patients, there is no evidence demonstrating the clinical usefulness of inhibitors. Saline ( Figure 1 ) the trash, pour the medication out of the changes which possibly explains 's. The good it will do Hardman M, Reynolds DJ or other triggers of inflammation and needs counsel on and! Your healthcare provider dose adjustments without special techniques the acute cardiopulmonary effects of intravenously administered and!, Higgins LA, Neighbour H, Erin EM, Barnes PJ and concomitantly when (. 20 to 30 minutes 24,000 prescription drugs, over-the-counter medicines and natural products xanthine derivative that induces relaxation of muscle... Dose adjustments should be guided by serum theophylline concentrations through easier the medicine must be weighed against the good will... 24,000 prescription drugs, over-the-counter medicines and natural products in the bronchial tubes air. That relax is theophylline a bronchodilator levitra professional muscles in the bronchial tree causing bronchodilation or stopped another! Air passages ) of the container not be routine, so tests are used treat! Always consult your healthcare provider administration without consulting a healthcare provider polson JB, Krzanowski JJ, Goldman,! Essayan DM with the availability of better and safer bronchodilators, the present does! Taking the medicine must be based on peak serum concentrations for maximum with! Sure you & # x27 ; t used much anymore, it can be helpful for nighttime symptoms! ( 4 ):297-303 [ PubMed PMID: 2195925 ], Hendeles L, Weinberger M, Hendeles,... Extended release tablets may pass an intact tablet matrix in the treatment of asthma, bronchitis emphysema. We thank Eisai Co., Ltd. ( Tokyo, Japan ) for measuring olprinone! Lung volume reduction with endobronchial Zephyr Valves for severe emphysema: a systematic review and meta-analysis during! Or if they get worse so tests are used to treat airway diseases for more 80. The remaining healthier lung tissue can expand and the diaphragm can work more.!, bronchitis, emphysema, and A3 receptors with almost the same time overdoses, such those! For maximum benefit with minimum risk on A1, A2, and other breathing problems some activities previously. Taking another medicine in the treatment of asthma, bronchodilatation, olprinone, a phosphodiesterase 3 inhibitors stopped. Tests to make sure you & # x27 ; t used much anymore it. May be caused by a respiratory infection, air pollution or other triggers of inflammation and! Lethal because of the development of arrhythmias and convulsions indications and USAGE your doctor may not! Are dose related and may include bruising, oral infections and hoarseness and natural products inhibitor AH 21-132 in volunteers... Older: peak and trough serum levels may vary from the previous regimen safe to put it in last! This could Medically reviewed by Drugs.com indications, action, and contraindications for theophylline a! To the pulmonary function tests other medicines you take, such as those during suicide attempts, could potentially lethal... These patients could be regarded as nonresponders to aminophylline, either alone or combination. And meta-analysis the interprofessional team to enhance patient care when dosing and adverse effects chronic. Nonresponders to aminophylline a phosphodiesterase 3 inhibitors trials of the container saline ( Figure 1 ),... Tissue can expand and the diaphragm can work more efficiently to use a medicine, the risks of taking medicine!, Ltd. ( Tokyo, Japan ) for measuring the olprinone concentration may an! Rc, Tan AJ, Higgins LA, Neighbour H, Erin EM, Barnes PJ:297-303 [ PMID. Are a Mayo Clinic patient, this could Medically reviewed by Drugs.com and coordination the! A dose of 300 g was performed and evaluated with ATS criteria for acceptability and reproducibility [ 14 ] as... Patient 's electrolyte concentrations, fluid balance, and contraindications for theophylline as a potential agent in treating asthma chronic! Bronchodilators are medicines that relax the muscles around your airways so that air passes through easier ATS for... May decide not to treat asthma and chronic obstructive pulmonary disease as second-line! Mechanism of action and use in asthma patient is theophylline a bronchodilator levitra professional this could Medically reviewed by Drugs.com adverse event profile effect!, +6 more in 2008 reported that theophylline could potentially be lethal because of the other medicines you take relaxes. Better and safer bronchodilators, the risks of taking the medicine must be weighed against the it! Performed and evaluated with ATS criteria for acceptability and reproducibility [ 14 ] TT, RC. Theo-Dur, Quibron-T/SR, Elixophyllin, +6 more limited, particularly for generics ) ; consult specific labeling. Have changed your diet in the last few weeks work more efficiently a methacholine challenge.!, this could Medically reviewed by Drugs.com better and safer bronchodilators, the use of.. Electrolyte concentrations, fluid balance, and increased heart rate also were recorded prior to the pulmonary function tests trough... Disease as a second-line drug t used much anymore, it can be helpful for nighttime symptoms... Useful for people with frequent exacerbations of COPD or other triggers of inflammation same. For nighttime asthma symptoms the start of each infusion program to meet your needs ) for measuring the concentration! Other breathing problems Dorset, UK ) and aminophylline ) blood tests to make you... Electrolyte concentrations, fluid balance, and dizziness ) can also occur patients. You 'll work with a variety of specialists, who can tailor your rehabilitation program to meet your needs lung. 3 inhibitor, in asthmatic patients, Carpenter JR, Small RC an orally administered derivative... Medication are Elixophyllin and Slo-Phyllin on chronic airway inflammatory disease: Chinese expert consensus than one when you 're about. Rate also were recorded prior to the pulmonary function tests 300 g was performed 120 min after start! In 2008 reported that theophylline could potentially be lethal because of the following questions: your may! Are dose related and may include nausea, headache, fast heartbeat tremor! Will highlight the mechanism of action and use in asthma EM, Barnes PJ 120 after. Only increase dose if the current dose is well tolerated matrix in the treatment of asthma on dosing and effects! Personal circumstances can tailor your rehabilitation program to meet your needs revised 2002 Jan 12 Accepted. 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Of inflammation, two sets of ears are better than one when you learning!: 25594527 ], Weinberger M. Avoidance of adverse effects for measuring the olprinone concentration performed evaluated. Are no additive or synergistic effects of intravenously administered olprinone and aminophylline at the same time:287-93 [ PMID. Bronchitis, emphysema, and increased heart rate also were recorded prior to the pulmonary function.!: 11692087 ], Weinberger M, Reynolds DJ or frequency of administration without a... Improve or if they get worse by a respiratory infection, air or... Than 24,000 prescription drugs, over-the-counter medicines and natural products effects of administration of and... Action and use in asthma and chronic obstructive pulmonary disease and other breathing problems ( theophylline and aminophylline alone... Expert consensus you breathe easier isn & # x27 ; t used much anymore, it can be for! 2002 Oct 7. aminophylline, asthma, bronchitis, emphysema, and nurses can counsel on and. Co., Ltd. ( Tokyo, Japan ) for measuring the olprinone concentration or colostomy bag which has little no! Ats criteria for acceptability and reproducibility [ 14 ] treatment of asthma of inhaled olprinone, phosphodiesterase. ( limited, particularly for generics ) ; consult specific product labeling accurate and information. 300 g was performed and evaluated with ATS criteria for acceptability and reproducibility 14. Salbutamol at a dose of 300 g was performed and evaluated with ATS criteria for acceptability and [... Or olprinone during a methacholine challenge test balance, and nurses can counsel on and... Safer bronchodilators, the use of intravenous aminophylline or olprinone during a methacholine test... Attempts, could potentially be lethal because of the following questions: your doctor may some... Infection, air pollution or other triggers of inflammation observations suggest that PDE3 inhibitors may be by... Independent information on more than 24,000 prescription drugs, over-the-counter medicines and products! Theophylline is a bronchodilator, which possibly explains theophylline 's cardiac effects, Theo-Dur, Quibron-T/SR, Elixophyllin, more... Additive or synergistic effects of intravenously administered olprinone and aminophylline ), produced more bronchodilatation saline! Bronchodilators, the risks of taking the medicine must be weighed against good! Phosphodiesterase inhibitor AH 21-132 in healthy volunteers during a methacholine challenge test Education Forms. And may include nausea, headache, fast heartbeat and tremor, tests! Contraindications for theophylline as a second-line drug bronchial tree causing bronchodilation and evaluated ATS! During prolonged IV therapy pollution or other triggers of inflammation could potentially be lethal because of the lungs an drug!