The drug Theophylline is a medication that is capable of providing antispasmodic, bronchodilator, antiasthmatic, vasodilating, cardiotonic, and diuretic effects.
Description Theophylline
There is information about the substance Theophylline as an alkaloid found in coffee and tea leaves. To manufacture the drug, it is possible to obtain it synthetically.
Theophylline release form
The drug is produced in the form of powder and suppositories, as well as capsules and tablets. In addition, in pharmacies you can also purchase an oral solution called an elixir.
Theophylline formula
Theophylline by chemical composition, which we can talk about as methylxanthine, a purine derivative, a heterocyclic alkaloid of plant origin.
Theophylline mechanism of action
Pharmacology
Being an effective bronchodilator, Theophylline in terms of pharmacology exhibits the following mechanisms of action:
- The drug is capable of inhibiting phosphodiesterase and increasing the accumulation of Camp, as well as acting as a blocker of purine receptors;
- Thanks to the action of Teofilin, the ability of calcium ions to flow through the tubules of cell membranes is significantly reduced, the contractile activity exhibited by smooth muscles is reduced, and the muscles located in the bronchi and blood vessels (brain, skin, kidneys) relax;
- The drug is capable of providing a peripheral vasodilating effect;
- Theophylline can influence membrane stabilization mast cells and do not allow the mediators of the allergic reaction to be released through powerful inhibition;
- The drug helps to increase mucociliary clearance and stimulate contractions of the diaphragm, as well as improve the function of both respiratory and intercostal muscles. In addition, due to the effect of the drug, the respiratory center is stimulated;
- Since the respiratory function is normalized under the influence of the drug, the blood is better saturated with oxygen and the concentration of carbon dioxide decreases;
- When conditions of hypokalemia develop in the body, taking the drug helps to increase ventilation of the lungs;
- Also, due to the effects of Theophylline, cardiac activity is stimulated and the heart rate increases, as well as their strength. In addition, the speed of coronary blood flow increases and the need of the heart muscle for oxygen increases;
- Taking the drug helps reduce the tone of blood vessels;
- The drug's action allows you to reduce vascular resistance pulmonary and lower circulatory pressure in its pulmonary circle;
- Thanks to the drug, renal blood flow increases and a moderate diuretic effect is provided;
- Under the influence of Theophylline, the extrahepatic bile ducts expand;
- Also thanks to the action medicine platelet aggregation is inhibited and the resistance of red blood cells to deformation increases, therefore the risk of blood clots is reduced and microcirculation is normalized.
The therapeutic therapeutic level of Theophylline is achieved in the blood approximately five hours after taking the tablet, since the active substance from the drug is released slowly. The effect can last half a day, therefore, when taking the drug twice a day, the concentration of theophylline will be necessary to provide therapeutic effects blood level.
Pharmacokinetics
The drug has a rapid period of complete absorption into the blood from gastrointestinal tract, in whatever form it may be taken. It is bound by plasma protein predominantly by albumin by 40 percent. Theophylline metabolism by methylation and oxidation occurs mainly in the liver. The half-life in an adult patient is approximately eight hours. Plasma concentration can be achieved within two hours. Once its concentration in the blood serum is achieved, the effect of bronchial expansion will be ensured.
Theophylline is eliminated from the body through urine, and about ten percent of the drug leaves the body unchanged.
Theophylline instructions
Regardless of the form in which the drug is released, each package contains instructions that describe in detail the drug itself and recommendations for its use, as well as all other information that is important to study before starting treatment.
Theophylline indications
The use of the drug Theophylline is indicated for broncho-obstructive syndrome that has developed for one reason or another. For example, due to bronchial asthma, and if it is asthma of physical exertion, then Theophylline will act as the main drug in treatment, and in other forms of the disease as an auxiliary one. Other causes of broncho-obstructive syndrome may include:
- Development of chronic obstructive bronchitis;
- With emphysema;
- With pulmonary heart;
- For pulmonary hypertension;
- For edema syndrome associated with kidney disease; the drug is used as part of complex treatment;
- For sleep apnea (a sleep disorder that causes sudden stops in breathing).
Theophylline contraindications
The drug also has enough contraindications, which it would be useful to familiarize yourself with, even if the drug was prescribed for treatment by a doctor.
So, the drug Theophylline should not be used to treat the following conditions and diseases:
- For gastritis with high acidity;
- During the period of exacerbation of gastrointestinal ulcerative diseases;
- For gastrointestinal bleeding;
- For epilepsy;
- In the presence of arterial hypertension or hypotension if its course is regarded as severe;
- For hemorrhagic stroke;
- For severe tachyarrhythmia;
- For hemorrhages in the retina of the eyes;
- Until twelve summer age;
- In case of hypersensitivity to the active substance of the drug.
In addition to the fact that the drug has a whole list of contraindications, there is also a list that prescribes its use for treatment with caution.
- In severe manifestations of coronary insufficiency, where angina pectoris and myocardial infarction occur in the acute phase;
- For obstructive hypertrophic cardiomyopathy;
- For vascular atherosclerosis;
- For chronic heart failure;
- With frequent ventricular extrasystole;
- With increased convulsive readiness;
- In case of liver or kidney failure;
- With gastrointestinal ulcer, even if it was diagnosed earlier;
- With existing or recent gastrointestinal bleeding;
- With prolonged hyperthermia;
- For thyrotoxicosis and hypothyroidism;
- For gastroesophageal reflux;
- For prostate adenoma;
- During lactation and pregnancy;
- In childhood and old age.
Theophylline use
Dosing of the drug Theophylline is established with individual approach. Based on an initial dose of 400 milligrams per day, which can be gradually increased to 25 percent every three days until the maximum is reached therapeutic effect. This can be allowed provided that the drug is well tolerated.
The maximum dosage that can be allowed without monitoring the concentration of Theophylline in the blood plasma:
- Children from 3 to 9 years old - 24 milligrams per kilogram of body weight per day;
- Children from 9 to 12 years old - 20 milligrams per kilogram of body weight per day;
- Adolescents from 12 to 16 years old - 18 milligrams per kilogram of body weight per day;
- Patients over 16 years of age - 13 milligrams per kilogram of body weight per day or 900 milligrams.
If, with the use of the indicated doses of the drug, the severity of toxic symptoms or the need to further increase the dosage when the therapeutic effect is insufficient, it should be recommended to monitor the concentration of Theophylline in the blood plasma.
The optimal therapeutic concentration is no more than 20 micrograms per milliliter. When its indicator is less, it means the effect therapeutic action the drug is weakly expressed. If the reading exceeds the norm, it means that with a slight increase in the effect of the drug, the possibility of the occurrence of side effects.
Also, regarding the frequency of taking the drug, you can follow the instructions, depending on the type of its dosage form.
Theophylline tablets during pregnancy
The use of the drug during pregnancy and breastfeeding may be permitted only in cases of extreme necessity, where it should be taken into account that Theophylline has the ability to be released into breast milk.
Side effects
- Central nervous system: Dizziness and headaches may be noted. Conditions of insomnia, anxiety, agitation, irritability, and tremor may also occur.
- Cardiovascular system: the heart rate may increase and blood pressure may decrease. An increase in attacks of tachycardia, cardialgia, and angina pectoris is observed. Arrhythmia appears.
- Digestive system: after long-term use, a decrease in appetite and nausea, vomiting, heartburn and diarrhea may occur. Gastroesophageal reflux and exacerbation of ulcers may also occur.
- Allergies: appearance skin rash, itching, fever.
- Others: facial flushing, increased sweating and chest pain.
By reducing the dose of the drug, side effects may be eliminated or reduced.
special instructions
During treatment, caution should be exercised when consuming foods and drinks containing caffeine.
It should be taken into account that smoking people the effect of theophylline may be reduced.
Drug interactions
The drug actively interacts with other drugs, where the effect of Theophylline can significantly increase or, on the contrary, its effectiveness decreases. Usually drug interactions the doctor takes into account when prescribing treatment, but all this information is described in detail in the instructions.
Theophylline analogues
The drug has at least twenty-three analogues, among which Teopek tablets, Spofillin Retard 100, Spophylline Retard 250 stand out.
Theophylline price
The drug, due to its serious nature, is relatively inexpensive; its estimated price is just over one hundred rubles.
One tablet of the drug as an active ingredient may contain 100, 200 or 300 mg theophylline . The package contains 20, 30 or 50 tablets.
Release form
by the company Valenta Pharmaceuticals Theophylline is available in the form of extended-release tablets.
pharmachologic effect
Bronchodilator.
Pharmacodynamics and pharmacokinetics
Derivative purina – theophylline is a bronchodilator. The drug is depressing phosphodiesterase , thereby increasing accumulation in tissues cAMP , promotes blocking purine receptors , reduces transportation calcium ions through the channels of cell membranes, reduces contractility smooth muscle . By relaxing the muscles of the bronchi and blood vessels circulatory system(especially the vessels of the kidneys, skin and brain) exhibits vasodilating peripheral effect, increases blood flow in the kidneys, has diuretic moderate effects. Is mast cell membrane stabilizer , and also suppresses release mediators of allergic manifestations .
Strengthens mucociliary clearance , improves diaphragmatic breath , increases the functionality of intercostal and respiratory muscles, stimulates the breathing center. It lowers the carbon dioxide content in the blood and normalizes the flow of oxygen. In conditions hypokalemia enhances lung ventilation.
Increases coronary blood flow , stimulates activity heart muscle , increases the strength and frequency of its contractions, and reduces the need for oxygen. Reduces vascular resistance lungs and blood pressure pulmonary circulation . Expands the bile ducts (extrahepatic). Prevents aggregation , by suppressing the activation process E2-alpha And platelets . Increases resistance to deformation, having a beneficial effect on rheological blood parameters . Inhibits the processes of education and also normalizes microcirculation .
Due to the delayed release of the active ingredient, the plasma therapeutic concentration theophylline observed after 3-5 hours and persists for 10-12 hours, thereby, when taking the drug twice a day, ensuring its constant effective concentration in blood.
Has quite good absorption from the gastrointestinal tract and bioavailability about 88-100%. Communication with plasma proteins is approximately 60%. TCmax varies at 6 hours. Penetrates through placental barrier And detected in milk nursing mother.
90% of the drug is exposed metabolism in the liver with the participation of some cytochrome P450 enzymes (the most significant CYP1A2), with the release of the main metabolites 3-methylxanthine and 1,3-dimethyluric acid.
Metabolites of the drug, as well as 7-13% (in childhood up to 50%) of unchanged substance are excreted by the kidneys. In newborns, due to incomplete metabolism, most of the drug is excreted in the form caffeine .
In non-smoking patients, T1/2 is 6-12 hours, while in nicotine-dependent people it decreases to 4-5 hours. At , pathologies of the liver and kidneys T1/2 lengthens. At CHF , respiratory and liver failure, severe , viral infections , as well as under the age of 12 months and over 55 years, general ground clearance downgraded
Indications for use
Broncho-obstructive syndrome , developed by various reasons:
- (for exercise asthma as a drug of choice, as well as for other forms of asthma as an additional drug);
- obstructive chronic course;
- emphysema ;
- cor pulmonale ;
- pulmonary hypertension ;
- edema syndrome due to kidney disease (in complex treatment);
Contraindications
- (with increased acidity);
- periods of exacerbation Gastrointestinal tract ;
- gastrointestinal bleeding;
- arterial hypo- or severe course;
- hemorrhagic ;
- heavy tachyarrhythmias ;
- hemorrhage into the retina of the eye;
- age up to 12 years (for non-extended forms up to 3 years);
- hypersensitivity to theophylline , as well as other derivatives xanthine ( , pentoxifylline, caffeine).
Carefully:
- severe manifestations coronary insufficiency , including and acute phase;
- obstructive hypertrophic cardiomyopathy ;
- vessels;
- chronic heart failure ;
- frequent ventricular extrasystole ;
- increased convulsive readiness ;
- or liver ;
- peptic ulcer Gastrointestinal tract (diagnosed in the past);
- recent gastrointestinal bleeding;
- long-term hyperthermia ;
- or ;
- gastroesophageal reflux ;
- periods of breastfeeding and pregnancy;
- elderly or children's age.
Side effects
- excitation;
- anxiety;
- irritability;
The cardiovascular system:
- (also observed in the fetus when using Theophylline in the third trimester);
- heartbeat;
- cardialgia ;
- decreased blood pressure ;
- more frequent attacks.
Digestive organs:
- gastralgia ;
- nausea;
- gastroesophageal reflux ;
- vomit;
- exacerbation of peptic ulcer disease;
- loss of appetite (in case of long-term use).
Allergic manifestations:
- And skin.
Parallel reception beta blockers , especially non-selective ones, can lead to narrowing of the bronchi , which will reduce the bronchodilator effect theophylline , and also possibly the effectiveness of the beta blockers .
Theophylline – medicinal product, which has a bronchodilator effect; adenosine receptor blocker, phosphodiesterase inhibitor.
Release form and composition
Theophylline is available in the form of long-acting tablets: flat-cylindrical, white with a yellowish tint, with a bevel (dose of 100 mg) or with a bevel and a score (dose of 200 mg and 300 mg) (10 pieces each in blister packs, in a cardboard pack of 2, 3 or 5 packs; 20, 30 or 50 pieces in polymer cans, 1 can in a cardboard pack).
Composition per 1 tablet:
- active ingredient: theophylline – 100, 200 or 300 mg;
- auxiliary components: sodium lauryl sulfate, microcrystalline cellulose, polyvinyl acetate, calcium stearate, povidone, silicon dioxide.
Indications for use
- chronic obstructive diseases (for example, emphysema and chronic obstructive bronchitis);
- bronchial asthma (Theophylline is the drug of choice in patients with exercise-induced asthma; in other forms of asthma it is used as an additional remedy);
- "pulmonary" heart;
- sleep apnea;
- pulmonary hypertension;
- edematous syndrome of renal etiology (in complex treatment).
Contraindications
Absolute:
- severe tachyarrhythmias;
- retinal hemorrhage;
- bleeding from the gastrointestinal tract;
- peptic ulcer duodenum and stomach;
- hemorrhagic stroke;
- gastritis with high acidity;
- epilepsy;
- severe arterial hypotension or hypertension;
- children under 12 years of age;
- hypersensitivity to the components of the drug and other xanthine derivatives.
Relative (Theophylline is used with caution):
- chronic heart failure;
- renal failure;
- liver failure;
- prolonged hyperthermia;
- severe coronary insufficiency;
- hypertrophic obstructive cardiomyopathy;
- increased convulsive readiness;
- widespread vascular atherosclerosis;
- frequent ventricular extrasystole;
- uncontrolled hypothyroidism;
- gastroesophageal reflux;
- peptic ulcer of the duodenum and stomach (indications in the anamnesis);
- uncontrolled thyrotoxicosis;
- prostatic hypertrophy;
- recent bleeding from the gastrointestinal tract;
- period of pregnancy and breastfeeding;
- elderly age.
Directions for use and dosage
Theophylline tablets are taken orally.
The average recommended dose for adult patients and children over 12 years of age is 300 mg twice a day (10-15 mg/kg body weight in two doses with an interval of 12 hours between them). If necessary, prescribe 300 mg three times a day or 500 mg once, in the evening, before bedtime (if attacks are predominantly nocturnal or morning).
For non-smoking patients weighing 60 kg or more, theophylline is prescribed at an initial dose of 200 mg (in the evening), which is then increased to 200 mg twice a day.
For patients weighing less than 60 kg, the initial dose is 100 mg (at bedtime), and then 100 mg twice a day.
Treatment with the drug begins with smaller doses, gradually increasing them until the maximum therapeutic effect is achieved. The dose is increased by 100-200 mg per day with an interval of 1-2 days. If theophylline is poorly tolerated, the dose should be reduced.
The dose of the drug depends on parameters such as the patient’s age and body weight, as well as the nature of the disease.
If there is a need to take large doses, then during treatment it is necessary to monitor the concentration of theophylline in plasma: at a value of 20-25 mcg/ml daily dose should be reduced by 10%; at 25-30 mcg/ml – reduce the daily dose by 25%; above 30 mcg/ml – reduce it by half. After three days it is necessary to carry out a control measurement. If the concentration of theophylline is reduced, the daily dose should be increased by 25% at intervals of 3 days. When the patient's condition has stabilized while using the drug in high doses, monitoring is carried out every six months or a year.
Maintenance daily doses:
- non-smoking adult patients weighing 60 kg or more – 600 mg;
- non-smoking adult patients weighing less than 60 kg – 400 mg;
- smoking patients weighing 60 kg or more - 900 mg (300 mg in the morning and 600 mg in the evening);
- smoking patients weighing less than 60 kg - 600 mg (200 mg in the morning and 400 mg in the evening).
For liver dysfunction and diseases of cardio-vascular system Dose adjustment is required: patients weighing more than 60 kg are prescribed 400 mg of theophylline per day, those weighing less than 60 kg are prescribed 200 mg per day.
The daily dose of the drug is also reduced in case of severe damage to the liver and heart, infections of viral origin and in elderly patients.
Side effects
- cardiovascular system: decrease blood pressure, pain in the heart area, tachycardia, increased frequency of angina attacks, palpitations, arrhythmias;
- digestive system: exacerbation of duodenal and gastric ulcers, nausea, heartburn, gastroesophageal reflux, vomiting, diarrhea, gastralgia; with long-term therapy – decreased appetite;
- allergic reactions: fever, itchy skin, skin rash;
- nervous system: anxiety, headache, tremor, agitation, dizziness, insomnia, irritability;
- other: hematuria, albuminuria, increased sweating, increased diuresis, tachypnea, hypoglycemia, flushing, chest pain.
Probability of development side effects decreases with decreasing dose of Theophylline.
special instructions
The drug passes into breast milk, so if it is necessary to use it during lactation, it is recommended to stop breastfeeding. If Theophylline is used at the end of pregnancy, then tachycardia can be observed not only in the pregnant woman, but also in the fetus.
Theophylline is not intended for the relief of acute attacks.
During treatment, caution should be exercised when consuming large quantities of drinks or foods containing caffeine.
Drug interactions
Theophylline increases the likelihood of side effects of drugs for general anesthesia, gluco- and mineralocorticosteroids, as well as drugs that stimulate the central nervous system.
When used simultaneously with carbamazepine, moracizine, phenytoin, rifampicin, sulfinpyrazone, phenobarbital, aminoglutethimide, isoniazid and oral estrogen-containing contraceptives, an increase in theophylline dose may be required.
Absorption of the drug is reduced when combined with enterosorbents and antidiarrheals.
The therapeutic effect of Theophylline can be increased when taken simultaneously with isoprenaline, lincomycin, mexiletine, thiabendazole, verapamil, macrolide antibiotics, allopurinol, fluoroquinolones, enoxacin, methotrexate, propafenone, ticlopidine, cimetidine, recombinant interferon alpha, disulfiram, and also with influenza vaccination, so a dose reduction may be required.
Theophylline enhances the effects of diuretics and beta-agonists, and reduces the effects of beta-blockers and lithium preparations.
Theophylline can be used with antispasmodics; it is prescribed with caution with anticoagulants. The drug should not be taken simultaneously with other xanthine derivatives.
Terms and conditions of storage
Store in a dry place, protected from light, at a temperature not exceeding 25 °C. Keep away from children.
Shelf life – 3 years.
Theophylline (Theophyllinum lat.) is a purine derivative, an alkaloid, an adenosinergic agent, known as a central nervous system stimulant, with antispasmodic, bronchodilator, antiasthmatic, cardiotonic and pronounced diuretic properties.
This purine derivative is produced in well-packaged containers that protect the main active ingredient - Theophylline - from direct impact Sveta.
Theophylline release forms:
- oral tablets Theophylline anhydrous – (100 mg, 200 mg); depot (200 mg, 300 mg); retard (100 mg, 250 mg);
- powder in capsules – (50 mg, 75 mg, 100 mg, 125 mg, 200 mg, 300 mg);
- rectal suppositories 0.2 g;
- syrup (Elixir) (15 ml - 80 mg).
Theophylline tablets
Theophylline anhydrous tablets (flat-cylindrical with a chamfer) are coated with a soluble coating, or can be produced without it. Packaged in blisters (cell packaging) and in plastic container jars.
The active substance in one tablet is from 100 to 300 mg.
“Depot” and “retard” are not the names of tablets! This is a compressed form of Theophylline powder containing the main medicinal substance Theophylline. It dissolves in the stomach layer by layer, allowing the medicine to enter the body gradually, in doses - a prolonged form of obtaining the medicine. Depono (lat.) – to postpone, retardo (lat.) – to slow down.
This form is most attractive to the patient, as it provides stable concentration medicinal substance in the body, eases the load on the gastrointestinal tract and significantly reduces Negative consequences, if the drug was not taken on time or was completely forgotten.
Capsule and powder form of the drug
Anhydrous Theophylline capsules are a drug of modified action, that is, combining the speed of onset therapeutic effect and duration of exposure.
Theophylline powder is packaged in a hard gelatin shell with 3 colors for easy determination of drug quantity. So:
- white-pink capsule (white or colorless body and pink cap) – 100 mg;
- white-blue capsule – 200 mg;
- capsule No. 1 white-green – 300 mg.
Theophylline suppositories
Theophylline rectal suppositories are suppositories containing 0.2 g of theophylline, the rest is a fat base in which the drug is distributed evenly.
Such bases melt under the influence of body temperature, ensuring maximum availability of the medicinal substance through the mucous membrane, having the ability to easily pass from solid state into a liquid, bypassing the “ominous” state.
Theophylline suppositories are the least toxic, practically do not cause allergies, and dissolve within an hour. One package contains 10 per rectum suppositories with theophylline.
Syrup
Theophylline syrup
Theophylline in elixir form is often called "syrup". Theophyllinum elixir has a trade name - Theophylline KI. The generic (international) name is complex - Theophylline/Potassium Iodine (Theophylline-potassium iodide). It is called syrup because of the high sugar content in the orange solution and the orange-citrus taste and smell pleasant for children.
This elixir has a significant advantage over other forms of Theophylline - it is available for use by children from 1 year old, while, like other forms, it is not earlier than 6 or 12 years.
Pharmacological action of Theophylline drugs
Since the drug theophylline is an alkaloid, its highest content is in tea leaves and coffee beans. It is known that the action of this substance is dilation of the coronary vessels of the heart, relaxation of the muscles of the bronchi, stimulation of the nervous system and a diuretic effect.
Nowadays, such a derivative of purine and xanthine is obtained synthetically, which has made Theophylline available to everyone.
Use of alkaloids in medicine:
- Improving coronary circulation in angina and chronic coronary insufficiency.
- At stagnation cardiac and renal circulation - edema.
Theophylline, in combination with other drugs, copes well with all these tasks. For example, it enhances the convergence of edema in combination with cardiac medications. The effect is higher than that of theobromine (cocoa bean alkaloid). And in combination with it is used for treatment bronchial asthma with bronchospasms.
By enhancing MCC (Mucociliary clearance) by stabilizing the mast cell membrane, Theophylline affects:
- on the functions of the respiratory and intercostal muscles, increasing contractions of the diaphragm;
- stimulating the respiratory center - normalizes breathing, increases the secretion of adrenaline by the adrenal glands.
This promotes oxygen saturation of the blood and other organs, reduces the concentration of carbon dioxide and increases ventilation of the lungs.
In turn, this action has a positive stimulating effect on the heart, increasing the strength and frequency of heart contractions, ensuring the supply of oxygen to the myocardium.
Effect of use:
- tone decreases blood vessels brain, kidneys (diuretic effect) and skin;
- pulmonary vascular resistance decreases;
- the contractile activity of bronchial smooth muscles decreases;
- the pressure in the pulmonary circulation decreases;
- the superficial function of the left and right heart ventricles improves.
Theophylline is used as the main drug (for broncho-obstructive syndrome), and as an adjuvant for other diseases (edematous syndrome of renal origin).
Indications for use of Theophylline
The main areas of use of tablets, capsules and suppositories of 1,3-Dimethylxanthine (chemical name Theophylline):
- Pulmonary heart and pulmonary hypertension.
- Edema syndrome of renal origin (in complex).
Indications for the use of Theophylline KI elixir for children under 3 years of age: ATC category - bronchodilator and (mucolytic, bronchodilators).
The packaging of the medicinal product of any release form contains instructions, with detailed description the drug itself and recommendations for its use, other helpful information, which is important to study before starting treatment.
Method of administration and dosage of the drug
Theophylline is dispensed from pharmacies with a doctor's prescription.
This is due to an individual approach for each patient in calculating the dose and the doctor’s confidence, after passing certain tests, in the tolerable tolerability of the drug.
Common doses of Theophyllinum are:
- the initial dose should not exceed 400 mg of 1,3-Dimethylxanthine per day;
- the dosage can be gradually increased by 25% over 3 days;
- When the therapeutic effect is achieved (4–5 days), it is advisable to stop the increase.
The doctor must decide whether to stop or continue use.
Theophylline dosage in blood plasma, which should not exceed mg/kg per day:
- from 20 to 25 kg – 24 mg/kg;
- from 24 to 32 kg – 20 mg/kg;
- from 50 to 70 kg – 18 mg/kg;
- from 70 – 13 mg/kg.
Intolerance to purine derivatives, stroke, heart attack, hemorrhage (including peptic ulcer), atherosclerosis coronary arteries, pregnancy and lactation.
Side effects of the medicine
Most often observed:
- impairment of consciousness and vision;
- anxiety;
- convulsions;
- attacks of angina pectoris, arrhythmias, tachycardia;
- sore throat;
- atony;
- allergic reactions.
Analogues and trade names of the drug:
- Afonilum;
- Spophylline retard;
- Teobiolong;
- Theodile;
- Ventax;
- Uni-dur;
- Uniler;
- Diffumal;
- Spophylline;
- Retafil.
Theophylline has a number of generics - this is how medications are usually called for which the official patent period (patent protection) has expired.
Generics are famous for their lower price compared to patented drugs, but the price of Theophylline is already low (about 200-300 rubles per pack).
If a person suffers from airway obstruction, this may indicate the presence of this disease. This disease is quite common. This pathology often occurs in smokers. Also, the development of this disease is caused by infection or some kind of damage to the lungs. When a person's airways become narrowed, it is difficult for them to exhale air.
As a result, the main symptoms of this disease are shortness of breath, cough, and sputum production. This is important to know. The most common is the development of certain types of COPD. This is the occurrence of asthma, chronic bronchitis, emphysema, bronchiectasis. A drug such as Theophylline will help in the treatment of these and many other diseases. Instructions for using the medicine will be discussed in this text. More on this later.
Description
"Theophylline", the composition of which will be described below, is a white crystalline powder. It is slightly soluble in cold water(in a ratio of 1:180), but easily dissolves in hot water (in a ratio of 1:85). It also dissolves in alkalis and acids.
Compound
In this drug the main active substance is theophylline. This also includes certain auxiliary components. Namely - lactose monohydrate, talc, methacrylic acid.
Release form
In this regard, there are several types. "Theophylline" is produced in the form of prolonged-release tablets (0.1 g, 0.25 g), capsules (0.125 g, 0.5 g) and suppositories (0.2 g).
Pharmacological actions
The functionality of this drug is multifaceted. "Theophylline", reviews of which are positive, relaxes the muscles of the bronchi and has a stimulating and vasodilating effect. This drug ensures the normal functioning of the respiratory center. Eliminate pain syndrome in the diaphragm and improve the functioning of the intercostal muscles, “Theophylline” also helps. Using it regularly reduces the likelihood of reactions allergic type in organs respiratory system. This drug may have a diuretic effect. The presence of active substances in this medicine helps to normalize respiratory function, reducing carbon dioxide levels and increasing ventilation.
"Theophylline" effectively enhances coronary blood circulation. It also helps to reduce the tone of blood vessels in the brain, kidneys and heart. When implementing long-term treatment expansion occurs biliary tract, normalization of microcirculation, and also increases the resistance of red blood cells to deformation. Patients suffering from hypotension may experience a decrease in blood pressure.
Taking a drug such as Theophylline along with beta-blockers and antibiotics leads to an increased risk of side effects.
Indications for use
This medicine is prescribed when bronchial status or obstructive bronchitis occurs. It is also used as an adjuvant in newborns with apnea. Theophylline is used mainly as a bronchodilator.
It is also used as a moderate cardiotonic (increasing the force of heart contractions) and diuretic (diuretic) drug for congestive manifestations of renal and cardiac origin. Sometimes it is prescribed together with other antispasmodics and bronchodilators.
Detailed description of the spectrum of action of the specified drug
Initially when COPD treatment bronchodilators are prescribed. They open the airways. One of these medications, as mentioned above, is a drug such as Theophylline. The instructions for use characterize this medicine as a bronchodilator that blocks the so-called purine receptors. The presence of such a mechanism of action ensures the relief of spasms in the smooth muscles of the bronchi, the elimination pain in the diaphragm, activating the flow of oxygen into the lungs, improving the functioning of the intercostal muscles. As a result Airways open, a person can breathe easier.
"Theophylline" has a certain advantage. Instructions for use indicate that this medicine can have a positive effect not only on the respiratory tract, but also on other body systems. This drug promotes the expansion of coronary and peripheral blood vessels, prevents the process of platelet adhesion, and has a moderate diuretic effect. This stimulates the contractile activity of the heart muscle (myocardium), lowers blood pressure, and also has a beneficial effect on the central nervous system. As a result, this drug is able to act in many ways, simultaneously possessing antiasthmatic, bronchodilator, diuretic, antispasmodic, vasodilating and cardiotonic properties.
"Theophylline": instructions for use
There are many criteria for determining the dosage. "Theophylline", according to the instructions, should be taken by children from 14 years of age and adults 300 mg per day 2-3 times. In this case, this medicine should be taken with plenty of water. If necessary, the dosage can be increased to 500 mg 2 times a day if recommended by the attending physician. If the patient has a body weight of less than 60 kg, then the dosage should be 100 mg 2 times a day. IN in this case is prescribed in the morning and evening reception a drug such as Theophylline. The instructions state that the treatment course should begin with small doses, and then gradually increase them.
This medicine should be taken at certain intervals. They should last 2-3 days. According to these instructions, during the treatment process it is necessary to carry out regular diagnostic procedures. Namely - performing a blood test, measuring blood pressure, x-ray, ECG, determining cholesterol and hemoglobin levels. Manifestation therapeutic effect the indicated remedy occurs after two days. This is important to know. At joint reception of this drug with antispasmodics there is an increase in effectiveness healing process. "Theophylline" helps reduce the effect of antidiarrheal drugs. During the treatment period, you should take caffeine-containing products and antidepressants with caution.
Taking this drug during breastfeeding and pregnancy
"Theophylline" acts on the fetus under category "C" by the FDA. This drug penetrates the placental barrier. Pregnant women can use this medicine only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. During the first trimester and the last weeks of pregnancy, you should take the drug, following strict indications. This is important to remember.
From many observations it follows that the clearance of theophylline during the third trimester of pregnancy is reduced. This may require more frequent definition concentration of this substance in the blood and possible dose reduction.
At breastfeeding Theophylline passes into milk and may cause irritability or other signs of toxicity in infants. This is important to know. The concentration of this substance in breast milk is approximately equivalent to its content in the mother. Also, this remedy slightly suppresses uterine contractions.
Contraindications
"Theophylline", the instructions for use of which are described above, is contraindicated if there is:
It is necessary to take this drug with caution in case of manifestation of peptic ulcer of the duodenum and stomach.
Special criteria
Smoking significantly affects the metabolism and excretion of substances such as theophylline. This should be remembered. Persons who smoke 1-2 packs of cigarettes per day have a reduced half-life. In patients with liver, heart or severe respiratory failure, as well as with viral infections and hyperthermia, elimination slows down active substance. Ingestion of alcoholic beverages and caffeine-containing products also has a significant effect on theophylline metabolism.
Interactions
The drug "Theophylline" helps potentiate the effect of β2-adrenergic agonists. It can also increase tremor, which is caused by sympathomimetic drugs and can inhibit the absorption of phenytoin. The elimination of this drug is slowed down when it interacts with Erythromycin and Phenobarbital. Theophylline increases renal excretion of lithium. In this case, the therapeutic balance is disrupted in patients who take the corresponding salts. The drug "Cimetidine" helps to increase the concentration of theophylline in the blood and also increases the time of its elimination. Medicines similar action will be listed below.
Presence of side effects
When taking this medicine, various negative symptoms. Namely:
- Manifestations may occur in the form of dizziness, insomnia, headache, fainting, anxiety, tremor, confusion, epilepsy.
- In the field of the cardiovascular system - arrhythmia, tachycardia, cardialgia, a sharp decline blood pressure, angina pectoris.
- From the outside digestive system- the occurrence of nausea, vomiting, heartburn, diarrhea, flatulence, colitis, gastritis.
- With long-term use of this drug, manifestations of some allergic reactions may occur in the form of itching, burning, urticaria, dermatitis, fever, increased sweating, and skin rashes.
Overdose
In this case, certain symptoms occur. These manifestations mean:
Agitation;
Confusion;
Convulsions;
Tachycardia;
Arrhythmia;
Hypotension;
Nausea;
Vomiting with blood;
Hyperglycemia;
Metabolic acidosis.
At indicated symptoms specific treatment is prescribed. Namely, they carry out:
- Reception of activated carbon.
- Irrigate the intestinal area with a combination of a solution of salts and polyethylene glycol.
- Intravenous administration of Metoclopramide or Ondansetron for severe symptoms nausea and vomiting.
- Taking Benzodiazepine, Phenobarbital (or peripheral muscle relaxants when seizures occur.
"Theophylline": analogues
There are several various medications similar type. In this case, the following medications are considered:
- "Theobilongum"
- "Spophillin retard"
- "Perfillon" ("PerphyUon").
- "Neo-Efrodal".
- "Franol"
Storage
Powders and tablets ("Theophylline") are stored in a dry place, protected from light. Their duration is five years. Candles must be stored in the refrigerator. However, they should not be frozen. Their shelf life is four years.
Bottom line
Having read the above, everyone will be able to imagine what a drug like “Theophylline” is, the price of which is reasonable (in the range of 70-160 rubles). This text also contains instructions for use. of this medicine, its interaction with other means.
