Theophylline

Теофиллин Drug photo

The description is actual on 16.01.2015

  • Latin name: Theophylline
  • ATH code: R03DA04
  • Active ingredient: Theophylline (Theophylline)
  • Producer: JSC Valenta Farmatsevtika, Russia

Structure

One tablet of drug as active ingredient can include 100, 200 or 300 mg of theophylline. Packaging contains 20, 30 or 50 tablets.

Release form

Valent Farmatsevtik's company the drug Theophylline is issued in the form of tablets of the prolonged action.

Pharmacological action

Bronkhodilatiruyushchy.

Pharmacodynamics and pharmacokinetics

Derivative purine theophylline is broncholitic means. Drug oppresses phosphodiesterase, thereby increases accumulation in tsAMF fabrics, promotes blocking of purine receptors, lowers transportation of calcium ions through channels of membranes of cells, reduces sokratitelny ability of smooth muscles. By means of a relaxation of muscles of bronchial tubes and vessels of circulatory system (in particular vessels of kidneys, integuments and a brain) shows vazodilatiruyushchy peripheral influence, strengthens a blood stream in kidneys, has diuretic effects of moderate character. Is the stabilizer of membranes of mast cells, and also suppresses release of mediators of allergic manifestations.

Strengthens mukotsiliarny clearance, improves diafragmentalny breath, increases functionality of intercostal and respiratory muscles, stimulates the center of breath. In blood lowers the content of carbonic acid and normalizes oxygen inflow. In the conditions of a hypopotassemia strengthens ventilation of the lungs.

Increases a coronary blood stream, stimulates activity of a cardiac muscle, increases force and frequency of its reductions, lowers oxygen requirement. Reduces the vascular resistance of lungs and pressure in a small circle of blood circulation. Expands bilious ways (extrahepatic). Interferes with aggregation of thrombocytes, by means of suppression of process of activation of E2 alpha prostaglandin and thrombocytes. Increases erythrocyte resistance to deformation, well influencing rheological indicators of blood. Slows down processes of formation of blood clots, and also normalizes microcirculation.

Thanks to the slowed-down release of active ingredient, plasma therapeutic concentration of theophylline is observed in 3-5 hours and remains for 10-12 hours, thereby, at administration of drug twice a day, providing its constant effective concentration in blood.

About 88-100% possess rather good absorption from a gastrointestinal tract and bioavailability. Communication with plasma proteins about 60%. TCmax varies at the level of 6 hours. Gets through a placental barrier and is defined in milk of the nursing mother.

90% of drug are exposed to a metabolism in a liver at participation of some enzymes of P450 cytochrome (the most significant CYP1A2), with allocation of the main metabolites 3 methylxanthines and 1,3-dimethyl uric acid.

Drug metabolites, and also 7-13% (at children's age to 50%) not changed substance, are removed by kidneys. At newborns, because of an incomplete metabolism, the most part drug is removed in the form of caffeine.

At non-smoking patients of T1/2 makes 6-12 hours whereas at nicotinodependent people goes down till 4-5 o'clock. At alcoholism, pathologies of a liver and kidneys of T1/2 it is extended. At HSN, a respiratory and liver failure, heavy fever, viral infections, and also aged about 12 months is also more senior than 55 years, the general clearance is lowered.

Indications to use

The Bronkhoobstruktivny syndrome which developed for various reasons:

  • bronchial asthma (at asthma of physical tension as choice drug, and also at other forms of asthma as additional drug);
  • obstructive bronchitis of a chronic current;
  • emphysema of lungs;
  • pulmonary heart;
  • pulmonary hypertensia;
  • edematous syndrome on an etiology of kidneys (in complex treatment);
  • night apnoea.

Contraindications

  • gastritis (at a hyperoxemia);
  • periods of an aggravation of a peptic ulcer of a gastrointestinal tract;
  • gastrointestinal tract bleedings;
  • epilepsy;
  • arterial hypo - or a hypertension of a heavy current;
  • hemorrhagic stroke;
  • heavy tachyarrhythmias;
  • eye retinal apoplexy;
  • age till 12 years (for not prolonged forms till 3 years);
  • hypersensitivity to theophylline, and also other derivatives of xanthine (theobromine, pentoksifillin, caffeine).

With care:

Side effects

TSNS:

Cardiovascular system:

Digestive organs:

  • gastralgia;
  • diarrhea;
  • heartburn;
  • nausea;
  • gastroesophageal reflux;
  • vomiting;
  • aggravations of a peptic ulcer;
  • loss of appetite (in case of prolonged use).

Allergic manifestations:

Others:

  • tachypnea;
  • stethalgias;
  • inflow to the person;
  • hamaturia;
  • albuminuria;
  • hypoglycemia;
  • the increased sweating;
  • diuresis strengthening.

As a rule, when lowering doses of Theophylline of manifestation of side effects decrease.

Theophylline, application instruction

The application instruction of Theophylline of the prolonged action assumes individual selection of doses of drug.

On average the initial peroral daily dose equals 400 mg. In case of good tolerance the patient of this dose, it can be increased disposable approximately by 25%. Each 2-3 days to achievement of the best medical effect recommend to carry out increase in doses.

Without monitoring procedure over the content of theophylline in blood reception of its maximum daily doses, components is possible: 18 mg/kg for age of 12-16 years and 13 mg/kg for age after 16 flyings.

In a case when use of the above-stated doses is ineffective (demands increase of a dosage) or causes toxic symptoms, further therapy has to be carried out under a constant control of content of theophylline to blood. Doses at the level of 10-20 mkg/ml are considered as optimum therapeutic doses. Smaller content of theophylline is ineffective, and bigger does not lead to significant strengthening of its action whereas the risk of manifestations of side effects considerably increases.

Overdose

At overdose by Theophylline observed: loss of appetite, diarrhea, a gastralgia, the nausea passing into vomiting (it is possible with blood), gastrointestinal tract bleedings. Ventricular arrhythmias, hyperemia of the person, tachypnea, tachycardia. Sleeplessness, uneasiness, motive excitement, tremor, photophobia, spasms. In case of heavy overdose development of epileptoidny attacks (in particular at children's age), hypoxias, confusion of consciousness, a hyperglycemia, a metabolic acidosis, a hypopotassemia, a necrosis of skeletal muscles, lowering of the ABP, insufficiency of kidneys with a myoglobinuria is possible.

The recommended treatment consists in drug withdrawal, a gastric lavage, reception of purgatives, absorbent carbon, an enteroclysis with use of electrolytes and polyethyleneglycol. The artificial diuresis, a plazmosorbtion, hemosorption, perhaps is also shown, but it is ineffective, carrying out a hemodialysis, purpose of symptomatic therapy. In case of severe nausea and vomiting intravenous administration of an ondansetron  or Metoclopramidum. At spasms it is necessary to provide and watch passability of respiratory tracts, also to carry out an oxygenotherapy. The attack is stopped intravenous administration of 0,1-0,3 mg/kg of Diazepam, but by no more than 10 mg.

Interaction

The clearance of theophylline decreases at the combined reception with macroleads, Allopyrinolum, oral contraceptives, Cimetidinum, Lincomycin and Izoprenalin, Propranolol.

Parallel reception of beta adrenoblockers, in particular non-selective, can lead to narrowing of bronchial tubes that will lower bronkhodilatiruyushchy effect of theophylline, and also it is possible also efficiency of beta adrenoblockers.

Effects of Theophylline strengthen stimulators β2-адренорецепторов, Furosemide and Caffeine.

Aminoglutetimid increases theophylline removal that can lower its efficiency.

The concomitant use of the Acyclovir or Disulfiramum increases the content in theophylline blood, thereby strengthening possible side effects.

The combined use with Felodipin, Diltiazem, Verapamil, Nifedipine, as a rule, moderately or slightly change the content of theophylline in blood, but do not influence broncholitic action (cases of strengthening of side effects at a concomitant use of Nifedipine or Verapamil were described).

Parallel use of Theophylline and salts of lithium can lead to decrease in their efficiency.

The combined reception of Phenytoinum and Theophylline is lowered by concentration and efficiency of both drugs.

Therapeutic effect of Theophylline decreases at reception of Phenobarbital, the Isoniazid, Rifampicin, Sulfinpyrazonum and Carbamazepine.

Significant increase in content of theophylline in blood causes parallel reception of Enoksatsin or other ftorkhinolon.

Terms of sale

Medicine Theophylline falls according to the recipe.

Storage conditions

Temperature of storage of Theophylline should not be higher 25ºС.

Period of validity

Tablets of the prolonged action can be stored for 3 years.

Special instructions

During treatment patients should not abuse kofeinsoderzhashchy drinks or products.

Review of dosages is necessary for: patients of children's and advanced age; at pathologies of a liver and kidneys, cardiovascular system; the smoking patients.

The prolonged tablets are not applied at medical emergencies, and also demand control of content in blood of active ingredient.

Analogs

Coincidence on the ATH code of the 4th level:

Analogs of Theophylline are provided by the following medicines:

Section: For cough
in more detail

Education: Graduated from the Vinnytsia national medical university of N. I. Pirogov, pharmaceutical faculty, the higher pharmaceutical education – the specialty "Pharmacist".

Experience: Work in Koneks and Bios-Media pharmacy chains as "Druggist". Work as "Pharmacist" in Avicenna pharmacy chain of the city of Vinnytsia.

PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Theophylline surely consult with the attending physician.