CHOLINE THIEOPHYLLINATE

Absorption

After ingestion, theophylline is released from oxytriphylline in the acidic environment of the stomach.

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).

Originator

Sabidal ,S.R. Zyma, UK ,1983

The Uses of CHOLINE THIEOPHYLLINATE

Bronchodilator.

The Uses of CHOLINE THIEOPHYLLINATE

Oxytrimethylline is used in the treatment for chronic asthma.

Background

Oxtriphylline 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.

Indications

Used to treat the symptoms of asthma, bronchitis, COPD, and emphysema.

Manufacturing Process

18 parts by weight of theophylline are added to 37.8 parts by weight of aqueous choline bicarbonate (47% assay) and the mixture stirred and heated at 80°C to 90°C until the evolution of carbon dioxide has ceased and complete solution effected. Water is separated from the reaction mixture by distillation under a vacuum sufficient to keep the still temperature between 50°C and 55 C. After about 95 parts by weight of water have been separated, about 80 parts by weight of isopropyl alcohol are added and the mixture subjected to further distillation under a vacuum sufficient to keep the mixture boiling at about 40°C. The distillation removes some of the water as an azeotrope with the isopropyl alcohol. During the removal of the water-isopropyl alcohol azeotrope a crystalline precipitate forms. The mixture is further cooled slowly to 5°C and the crystalline precipitate filtered off. The choline theophyllinate crystals are then washed with isopropyl alcohol and dried under vacuum at about 70°C. A second crop of the product may be obtained from the mother liquor by further reduction in volume and cooling. A yield of 90.5% of theory of choline theophyllinate is obtained completely free of inorganic salts.

brand name

Choledyl(Parke-Davis).

Therapeutic Function

Smooth muscle relaxant

Pharmacokinetics

Oxtriphylline is a bronchodilator. Oxtriphylline 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.

Metabolism

Theophylline undergoes hepatic metabolism to 1,3-dimethyluric acid, 1-methyluric acid, and 3-methylxanthine.