Instruction for use: Choline theophyllinate

Trade name of the drug – Apo-Oxtriphylline

The Latin name of the substance Choline theophyllinate

Cholini theophyllinas (genus. Cholini theophyllinatis)

Chemical name

(2-Hydroxyethyl) trimethylammonium theophylline salt (1: 1)

Gross Formula

C₁₂H₂₁N₅O₃

Pharmacological group:

Adenosinergic agents

The nosological classification (ICD-10)

J43 Emphysema: Interstitial emphysema; Emphysema of the lungs; Chronic lung diseases; Chronic Obstructive Pulmonary Diseases; Obstructive emphysema of the lungs; Chronic emphysema of the lungs; Chronic obstructive pulmonary emphysema

J45 Asthma: Asthma of physical effort; Asthmatic conditions; Bronchial asthma; Bronchial asthma of light course; Bronchial asthma with difficulty in sputum discharge; Bronchial asthma of severe course; Bronchial asthma physical effort; Hypersecretory asthma; The hormone-dependent form of bronchial asthma; Curbing asthma attacks with bronchial asthma; Non-allergic bronchial asthma; Night Asthma; Exacerbation of bronchial asthma; Attack of bronchial asthma; Endogenous forms of asthma; Night attacks of asthma; Cough with bronchial asthma

J98.8.0 * Bronchospasm: Bronchospasm with bronchial asthma; Bronchospasm when exposed to an allergen; Bronchospastic reactions; Bronchospastic conditions; Bronchospastic syndrome; Diseases accompanied by bronchospastic syndrome; Reversible bronchospasm; Spasmodic cough

CAS Code

4499-40-5

Pharmacology

Pharmacological action - Antispasmodic.

It inhibits phosphodiesterase, promotes the accumulation of cAMP in the tissues, inhibits the myosin connection with actin, reduces the contractile activity of smooth muscles, in particular, relaxes the bronchi. Inhibits the transport of calcium ions through the slow channels of cell membranes, blocks adenosine receptors, has a cholinolytic effect. After oral administration, it is quickly absorbed, distributed in the extracellular fluid and evenly - in all tissues. The therapeutic concentration in the blood is 8-20 μg / ml. For most patients, the serum concentration of the drug in excess of 20 μg / ml is toxic. 55-65% is bound by plasma proteins. T1 / 2 on the average is 4.5 hours. 10% of the ingested dose is excreted in the urine. The equilibrium concentration in the blood is established within 1-2 days. In the Cl patients, the drug is increased by stimulating the liver enzymes involved in its metabolism. Relaxes smooth muscles (including bronchi), has a stimulating effect on the central nervous system, increases contractility of the myocardium and skeletal muscles, increases diuresis, gastric secretion. Promotes an increase in the level of prothrombin and fibrinogen in the blood (shortens prothrombin time).

Application of the substance Choline theophyllinate

Prevention of bronchospasm in bronchial asthma and other chronic obstructive pulmonary diseases, pulmonary hypertension, incl. With emphysema of the lungs.

Contraindications

Hypersensitivity, peptic ulcer of the stomach and duodenum in the phase of exacerbation, ischemic heart disease.

Restrictions

Severe pulmonary and cardiovascular diseases.

Side effects of Choline theophyllinate

Nausea, vomiting, diarrhea, epigastric pain, exacerbation of erosive and ulcerative gastrointestinal lesions, headache, sleep disturbances, tachycardia, lowering blood pressure down to collapse, leukopenia, thrombocytopenia, contact dermatitis, urticaria, skin itching.

Interaction

Erythromycin raises the level in the blood plasma to toxic. Strengthens the cardiac effects of cardiac glycosides and the diuretic effect of thiazides, is an antagonist of coumarin anticoagulants, reduces the uricosuric activity of probenecid and pyrazolone derivatives. Drugs acidifying urine, weaken, and alkalizing, - increase the effect.

Routes of administration

Inside.

Precautions for the substance Choline theophyllinate

It should not be administered with other xanthines and sympathomimetic amines.