Duraphyl
Duraphyl Uses, Dosage, Side Effects, Food Interaction and all others data.
Duraphyl is a bronchodilator, structurally classified as a Methylxanthine. Duraphyl has two distinct actions in the airways of patients with reversible obstruction; smooth muscle relaxation and suppression of the response of the airways to stimuli. Duraphyl also increases the force of contraction of diaphragmatic muscles. The half-life of Duraphyl is influenced by a number of known variables. In adult nonsmokers with uncomplicated asthma the half-life ranges from 3 to 9 hours
Duraphyl, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Duraphyl 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).
Trade Name | Duraphyl |
Availability | Prescription only |
Generic | Theophylline |
Theophylline Other Names | Teofilina, Theophyllin |
Related Drugs | Dupixent, Xolair, ProAir Digihaler, albuterol, dexamethasone, methylprednisolone, Symbicort, Breo Ellipta, Ventolin, Xopenex |
Type | |
Formula | C7H8N4O2 |
Weight | Average: 180.164 Monoisotopic: 180.06472552 |
Protein binding | 40%, primarily to albumin. |
Groups | Approved |
Therapeutic Class | Theophylline & related drugs |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
This is used for the symptomatic treatment of reversible bronchoconstriction associated with bronchial asthma, chronic obstructive pulmonary emphysema, chronic bronchitis and related bronchospastic disorders.
Duraphyl is also used to associated treatment for these conditions: Asthma, Bronchitis, Bronchoconstriction, Bronchospasm, Chronic Obstructive Pulmonary Disease (COPD), Chronic bronchial inflammation, Airway secretion clearance therapy, Bronchodilation
How Duraphyl works
Duraphyl relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Duraphyl 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. Duraphyl 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.
Dosage
Duraphyl dosage
Dosages are adjusted to maintain serum theophylline concentrations that provide optimal relief of symptoms with minimal side effects. Most of the controlled release preparations may be administered every 12 hours in adults while administration every 8 hours may be necessary in some children with markedly rapid hepatic metabolism of theophylline. The recommended dosages for achieving serum theophylline concentrations within the accepted therapeutic range is as follow:
- 1-6 months: 10mg/Kg/day
- 6 months-1 year: 15mg/Kg/day
- 1-9 years: 24mg/Kg/day
- 10-16 years: 18mg/Kg/day
- Adults: 10-15mg/Kg/day
Side Effects
The following side effects have been observed:
Gastrointestinal: Nausea, vomiting, epigastric pain and diarrhoea.
Central nervous system: Headache, irritability, restlessness, insomnia, muscles twitching.
Cardiovascular: Palpitation, tachycardia, hypotension. circulatory failure.
Respiratory: Tachypnoea.Renal: Potentiation of diuresis.
Others: Alopecia, hyperglycemia, rash etc.
Toxicity
Symptoms of overdose include seizures, arrhythmias, and GI effects.
Precaution
Careful consideration is needed for various interacting drugs and physiologic conditions that can alter Duraphyl clearance. Dosage adjustment is required prior to initiation of Duraphyl therapy, prior to increases in Duraphyl dose, and during follow up. The dose of Duraphyl selected for initiation of therapy should be low and, if tolerated, increased slowly over a period of time.
Interaction
Allopurinol, cimetidine, norfloxacin, ciprofloxacin, erythromycin, oral contraceptives and propranolol increase serum theophylline levels. Phenytoin, methotrexate and rifampicin lead to decreased serum theophylline levels
Food Interaction
- 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.
[Moderate] GENERALLY AVOID: Coadministration with caffeine may increase the serum concentrations of theophylline.
The proposed mechanism involves competitive inhibition of theophylline metabolism via CYP450 1A2, as well as metabolic conversion of caffeine to theophylline in vivo and saturation of theophylline metabolism at higher serum concentrations.
In six healthy male volunteers (all smokers), serum concentrations of theophylline (administered as aminophylline 400 mg single oral dose) were significantly higher following consumption of caffeine (2 to 7 cups of instant coffee over 24 hours, equivalent to approximately 120 to 630 mg of caffeine) than after caffeine deprivation for 48 hours.
Caffeine consumption also increased the apparent elimination half-life of theophylline by an average of 32% and reduced its total body clearance by 23%.
In another study, steady-state concentration and area under the concentration-time curve of theophylline (1200 mg intravenously over 24 hours) increased by 23% and 40%, respectively, in eight healthy volunteers following administration of caffeine (300 mg orally three times a day).
MANAGEMENT: Given the narrow therapeutic index of theophylline, patients should limit or avoid significant fluctuations in their intake of pharmacologic as well as dietary caffeine.
ADJUST DOSING INTERVAL: Administration of theophylline with continuous enteral nutrition may reduce the serum levels or the rate of absorption of theophylline.
The mechanism has not been reported.
In one case, theophylline levels decreased by 53% in a patient receiving continuous nasogastric tube feedings and occurred with both theophylline tablet and liquid formulations, but not with intravenous aminophylline.
MANAGEMENT: When administered to patients receiving continuous enteral nutrition , some experts recommend that the tube feeding should be interrupted for at least 1 hour before and 1 hour after the dose of theophylline is given; rapid-release formulations are preferable, and theophylline levels should be monitored.
Duraphyl Hypertension interaction
[Moderate] The use of theophyllines is associated with an increase in heart rate which may progress to supraventricular tachycardia or ventricular arrhythmia at high serum drug concentrations.
Appearance of cardiac adverse effects is generally an indication of theophylline toxicity, although patients with a history of tachyarrhythmias may be more susceptible to the chronotropic effect of these drugs.
Therapy with theophyllines should be administered cautiously in such patients.
Caution is also advised in patients with hypertension, hyperthyroidism, angina pectoris, or recent myocardial infarction, since high dosages of the drugs are associated with positive inotropic as well as chronotropic effects.
Clinical monitoring of serum drug concentrations is recommended to prevent toxicity.
Duraphyl Drug Interaction
Moderate: fluticasone / salmeterol, albuterol / ipratropium, albuterol / ipratropium, esomeprazole, albuterol, budesonide / formoterol, albuterolMinor: furosemide, alprazolam, cetirizineUnknown: aspirin, duloxetine, pregabalin, guaifenesin, acetaminophen, clopidogrel, montelukast, tiotropium, cyanocobalamin, cholecalciferol
Duraphyl Disease Interaction
Major: PUD, renal dysfunction, seizure disordersModerate: GERD, hemodialysis, reduced clearance, tachyarrhythmias
Volume of Distribution
- 0.3 to 0.7 L/kg
Elimination Route
Duraphyl is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.
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]
Elimination Route
Duraphyl 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.
Pregnancy & Breastfeeding use
Pregnancy: It is not known whether Duraphyl can cause foetal harm when administered to pregnant woman.Xanthines should be given to a pregnant woman only if clearly needed.
Nursing mother: Duraphyl is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing human infants. Serious adverse effects in the infant are unlikely unless the mother has toxic serum Duraphyl concentrations.
Contraindication
Hypersensitivity to xanthine derivatives. It is also contraindicated in patients with active peptic ulcer disease and in individuals with underlying seizure disorders (unless receiving appropriate anti-convulsing medication).
Duraphyl should not be administered concurrently with other xanthine. Use with caution in patients with hypoxemia, hypertension, or those with history of peptic ulcer. Do not attempt to maintain any dose that is not tolerated.
Acute Overdose
Symptoms may include nausea, vomiting, gastrointestinal irritation, cramps, convulsions, tachycardia & hypotension. The stomach contents should be emptied & supportive measures employed to maintain circulation, respiration & fluid & electrolyte balance. Electrocardiographic monitoring should be carried out & in severe poisoning charcoal haemoperfusion should be used.
Storage Condition
Store in a cool and dry place, protect from light and moisture. Keep out of the reach of children
Innovators Monograph
You find simplified version here Duraphyl
Duraphyl contains Theophylline see full prescribing information from innovator Duraphyl Monograph, Duraphyl MSDS, Duraphyl FDA label
FAQ
What is Duraphyl used for?
Duraphyl is used to prevent and treat wheezing, shortness of breath, and chest tightness caused by asthma, chronic bronchitis, emphysema, and other lung diseases.
How safe is Duraphyl?
Duraphyl may safe if you usuing properly.Many people using this medication do not have serious side effects.
What are the common side effects of Duraphyl?
The common side effects of Duraphyl are include:
Nausea/vomiting, stomach/abdominal pain, headache, trouble sleeping, diarrhea, irritability, restlessness, nervousness, shaking, or increased urination may occur.
Can Duraphyl be taken long-term?
Duraphyl is a long-term control medicine. This means it is used daily to maintain control of your lung disease. It is not one of the first medications used for long-term control of lung diseases.
When should I not use Duraphyl?
You should not Duraphyl if you have kidney disease in infants younger than 3 months of age.
Is Duraphyl safe during pregnancy?
Duraphyl has been used for many years during pregnancy without any apparent complications, suggesting that it is safe during pregnancy.
Is Duraphyl safe during breastfeeding?
Duraphyl passes from the mother to infant in breast milk. The drug is found in strong concentrations in breast milk and may cause infant irritability. Mild toxicity may occur, so breastfeeding while taking Duraphyl is not suggested.
Can I drink alcohol while taking Duraphyl?
Avoid drinking large amounts of beverages containing alcohol or caffeine (such as coffee, tea, colas), eating large amounts of chocolate, or taking nonprescription products that contain caffeine.
How quickly does Duraphyl work?
This Duraphyl works within 30 minutes.
What foods should I avoid while taking Duraphyl?
Drinking or eating foods high in caffeine, like coffee, tea, cocoa, and chocolate, may increase the side effects caused by Duraphyl. Avoid large amounts of these substances while you are taking Duraphyl.
Is Duraphyl used for Covid 19?
Duraphyl have anti-inflammatory properties that may make them useful in COVID-19 pneumonia. We conducted a retrospective review of hospitalized COVID-19 patients requiring oxygen who received these drugs.
Can I overdose on Duraphyl?
If you overdose on Duraphyl is metabolic disturbances (hypokalemia, hyperglycemia, and metabolic acidosis), nausea, vomiting, and, in severe cases, seizures, cardiac arrhythmias, and death.
Is Duraphyl an anti inflammatory?
Duraphyl did have anti-inflammatory effects on cytokines primarily produced by mononuclear phagocytic cells.
Does Duraphyl cause drowsiness?
Duraphyl oral tablet doesn't cause drowsiness but it can cause other side effects.
Can I take Duraphyl at night?
Once daily Duraphyl products are useful in reducing the number of times you take your medicine. They are often useful when given in the evening to people who have increased symptoms at night.
Can Duraphyl cause seizures?
Duraphyl can cause seizures in patients without known underlying epilepsy.
Is Duraphyl short or long acting?
Duraphyl is only available in a long-acting form.
How long does Duraphyl stay in system?
Duraphyl stay in your system eight hours in non-smoking adults.
Is Duraphyl still used for asthma?
Duraphyl is still one of the most widely prescribed drugs for the treatment of asthma.
What foods increase Duraphyl?
High-carbohydrate, low-protein diets can increase Duraphyl activity and side effects.
Can take Duraphyl on an empty stomach?
This medicine works best 30 minutes to 1 hour before meals or 2 hours after meals.
What is Duraphyl toxicity?
Duraphyl toxicity occurs when serum Duraphyl levels surpass the levels in the therapeutic range.
Does Duraphyl raise blood sugar?
During the most active phase of glucose counterregulation, the rate of increase of plasma glucose was larger with Duraphyl.
Why Duraphyl is not recommended?
Duraphyl tablets are rapidly absorbed, but plasma concentrations show wide fluctuations and are therefore not currently recommended.
Can I drive after taking Duraphyl?
Avoid driving or hazardous activity until you know how Duraphyl will affect you.
Can Duraphyl be stopped abruptly?
Even tyleno Duraphyl and few others like paracetamol also exhibit withdrawal symptoms if stopped abruptly.