Choline Theophyllinate
Choline Theophyllinate Uses, Dosage, Side Effects, Food Interaction and all others data.
Choline Theophyllinate is the choline salt form of theophylline. Once in the body, theophylline is released and acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Its main physiological reponse is to dilate the bronchioles. As such, oxytriphylline is indicated mainly for asthma, bronchospasm, and COPD (i.e. all the same indications as the other theophyllines). It is marketed under the name Choledyl SA, and several forms of oxytriphylline have been discontinued. In the US, oxtriphylline is no longer available.
Choline Theophyllinate is a bronchodilator. Choline Theophyllinate works in several ways: it relaxes muscles in your lungs and chest to allow more air in, decreases the sensitivity of your lungs to allergens and other substances that cause inflammation, and increases the contractions of your diaphragm to draw more air into the lungs.
Trade Name | Choline Theophyllinate |
Availability | Discontinued |
Generic | Oxtriphylline |
Oxtriphylline Other Names | Choline theophyllinate, Choline theophylline, Cholini theophyllinas, Oxtriphylline, Teofilinato de colina, Theocolin, Theophyllinate de choline |
Related Drugs | Dupixent, Xolair, Trelegy Ellipta, ProAir Digihaler, prednisone, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA |
Type | |
Formula | C12H21N5O3 |
Weight | Average: 283.3268 Monoisotopic: 283.164439563 |
Protein binding | With a serum concentrations of 17 mcg/mL, adults and children have about 56% theophylline bound to plasma protein, and premature infants have about 36%. |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Choline Theophyllinate is a bronchodilator used for the treatment of asthma, bronchitis, COPD, and emphysema.
Used to treat the symptoms of asthma, bronchitis, COPD, and emphysema.
Choline Theophyllinate is also used to associated treatment for these conditions: Bronchoconstriction
How Choline Theophyllinate works
Choline Theophyllinate is a choline salt of theophylline. After ingestion, theophylline is released from oxytriphylline, and 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. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.
Toxicity
Symptoms of toxicity include abdominal pain (continuing or severe), confusion or change in behavior, convulsions (seizures), dark or bloody vomit, diarrhea, dizziness or lightheadedness, fast and/or irregular heartbeat, nervousness or restlessness (continuing), and trembling (continuing).
Food Interaction
- Limit caffeine intake.
- Take with food. Food reduces irritation.
Choline Theophyllinate 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.
Choline Theophyllinate Disease Interaction
Major: PUD, renal dysfunction, seizure disordersModerate: GERD, hemodialysis, reduced clearance, tachyarrhythmias
Volume of Distribution
Theophylline has an apparent volume of distribution of 0.3–0.7 L/kg in children and adults, and the Vd is about twice that of an adult in premature infants.
Elimination Route
After ingestion, theophylline is released from oxytriphylline in the acidic environment of the stomach.
Half Life
The serum half life varies greatly between patients and in age. The half life range for a healthy, nonsmoking adult is 3-12.8 hours, for children is 1.5–9.5 hours, and for for premature infants is 15–58 hours.
Clearance
Theophylline has an average clearance in children (over 6 months) of 1.45 mL/kg per minute, and in healthy, nonsmoking adults of 0.65 mL/kg per hour.
Elimination Route
The kidneys are the main route of elimination for both theophylline and its metabolites, but some unchanged theophylline is eliminated in the feces.
Innovators Monograph
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