Teofilina

Teofilina Uses, Dosage, Side Effects, Food Interaction and all others data.

Teofilina is a bronchodilator, structurally classified as a Methylxanthine. Teofilina 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. Teofilina also increases the force of contraction of diaphragmatic muscles. The half-life of Teofilina is influenced by a number of known variables. In adult nonsmokers with uncomplicated asthma the half-life ranges from 3 to 9 hours

Teofilina, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Teofilina 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 Teofilina
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
Last Updated: September 19, 2023 at 7:00 am
Teofilina
Teofilina

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.

Teofilina 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 Teofilina works

Teofilina relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Teofilina 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. Teofilina 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

Teofilina 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 Teofilina clearance. Dosage adjustment is required prior to initiation of Teofilina therapy, prior to increases in Teofilina dose, and during follow up. The dose of Teofilina 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.

Teofilina 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.

Volume of Distribution

  • 0.3 to 0.7 L/kg

Elimination Route

Teofilina 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

Teofilina 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 Teofilina can cause foetal harm when administered to pregnant woman.Xanthines should be given to a pregnant woman only if clearly needed.

Nursing mother: Teofilina 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 Teofilina 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).

Teofilina 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 Teofilina

Teofilina contains Theophylline see full prescribing information from innovator Teofilina Monograph, Teofilina MSDS, Teofilina FDA label

FAQ

What is Teofilina used for?

Teofilina 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 Teofilina?

Teofilina may safe if you usuing properly.Many people using this medication do not have serious side effects.

What are the common side effects of Teofilina?

The common side effects of Teofilina are include:

Nausea/vomiting, stomach/abdominal pain, headache, trouble sleeping, diarrhea, irritability, restlessness, nervousness, shaking, or increased urination may occur.

Can Teofilina be taken long-term?

Teofilina 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 Teofilina?

You should not Teofilina if you have kidney disease in infants younger than 3 months of age.

Is Teofilina safe during pregnancy?

Teofilina has been used for many years during pregnancy without any apparent complications, suggesting that it is safe during pregnancy.

Is Teofilina safe during breastfeeding?

Teofilina 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 Teofilina is not suggested.

Can I drink alcohol while taking Teofilina?

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 Teofilina work?

This Teofilina works within 30 minutes.

What foods should I avoid while taking Teofilina?

Drinking or eating foods high in caffeine, like coffee, tea, cocoa, and chocolate, may increase the side effects caused by Teofilina. Avoid large amounts of these substances while you are taking Teofilina.

Is Teofilina used for Covid 19?

Teofilina 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 Teofilina?

If you overdose on Teofilina is metabolic disturbances (hypokalemia, hyperglycemia, and metabolic acidosis), nausea, vomiting, and, in severe cases, seizures, cardiac arrhythmias, and death.

Is Teofilina an anti inflammatory?

Teofilina did have anti-inflammatory effects on cytokines primarily produced by mononuclear phagocytic cells.

Does Teofilina cause drowsiness?

Teofilina oral tablet doesn't cause drowsiness but it can cause other side effects.

Can I take Teofilina at night?

Once daily Teofilina 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 Teofilina cause seizures?

Teofilina can cause seizures in patients without known underlying epilepsy.

Is Teofilina short or long acting?

Teofilina is only available in a long-acting form.

How long does Teofilina stay in system?

Teofilina stay in your system eight hours in non-smoking adults.

Is Teofilina still used for asthma?

Teofilina is still one of the most widely prescribed drugs for the treatment of asthma.

What foods increase Teofilina?

High-carbohydrate, low-protein diets can increase Teofilina activity and side effects.

Can take Teofilina on an empty stomach?

This medicine works best 30 minutes to 1 hour before meals or 2 hours after meals.

What is Teofilina toxicity?

Teofilina toxicity occurs when serum Teofilina levels surpass the levels in the therapeutic range.

Does Teofilina raise blood sugar?

During the most active phase of glucose counterregulation, the rate of increase of plasma glucose was larger with Teofilina.

Why Teofilina is not recommended?

Teofilina tablets are rapidly absorbed, but plasma concentrations show wide fluctuations and are therefore not currently recommended.

Can I drive after taking Teofilina?

Avoid driving or hazardous activity until you know how Teofilina will affect you.

Can Teofilina be stopped abruptly?

Even tyleno Teofilina and few others like paracetamol also exhibit withdrawal symptoms if stopped abruptly.

*** Taking medicines without doctor's advice can cause long-term problems.
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