Neofilin - description of the drug, instructions for use, reviews

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Manufacturers: DARNITSA (Pharmaceutical company)

Active ingredients

• Theophylline

Disease class

• Not indicated. See instructions

Clinical and pharmacological group

• Not indicated. See instructions

Pharmacological action

• Not indicated. See instructions

Pharmacological group

• Not indicated. See instructions

Pharmacodynamics and pharmacokinetics

purine derivative , theophylline, is a bronchodilator. The drug inhibits phosphodiesterase , thereby increasing the accumulation of cAMP , helping to block purine receptors , reducing the transport of calcium ions through cell membrane channels, and reducing the contractility of smooth muscles . By relaxing the muscles of the bronchi and blood vessels of the circulatory system (especially the vessels of the kidneys, skin and brain), it exhibits a vasodilating peripheral effect, increases blood flow in the kidneys, and has moderate diuretic It is a stabilizer of mast cell membranes and also inhibits the release of mediators of allergic manifestations .

Strengthens mucociliary clearance , improves diaphragmatic breathing , increases the functionality of the intercostal and respiratory muscles, and stimulates the respiratory center. It lowers the carbon dioxide content in the blood and normalizes the flow of oxygen. In conditions of hypokalemia, it enhances ventilation of the lungs.

Increases coronary blood flow , stimulates the activity of the heart muscle , increases the strength and frequency of its contractions, and reduces the need for oxygen. Reduces vascular resistance of the lungs and pressure in the pulmonary circulation . Expands the bile ducts (extrahepatic). Prevents platelet aggregation by suppressing the process of activation of prostaglandin E2-alpha and platelets . Increases erythrocyte resistance to deformation, having a beneficial effect on blood rheological parameters . Inhibits the process of blood clot and also normalizes microcirculation .

Due to the delayed release of the active ingredient, the plasma therapeutic concentration of theophylline is 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 the blood.

It has fairly good absorption from the gastrointestinal tract and bioavailability of about 88-100%. Communication with plasma proteins is approximately 60%. TCmax varies at 6 hours. Penetrates the placental barrier and is detected in the milk of a nursing mother.

90% of the drug is metabolized in the liver with the participation of certain 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 of caffeine .

In non-smoking patients, T1/2 is 6-12 hours, while in nicotine-dependent people it decreases to 4-5 hours. With alcoholism , pathologies of the liver and kidneys, T1/2 lengthens. With CHF , respiratory and liver failure, severe fever , viral infections , as well as under the age of 12 months and over 55 years, the total clearance is reduced.

Pharmacological properties of the drug Neophyllin

Theophylline (1,3-dimethylxanthine) is a natural compound, an alkaloid. The mechanism of its action is primarily due to blocking of adenosine receptors, inhibition of phosphodiesterases, an increase in the content of intracellular cAMP, and a decrease in the intracellular concentration of calcium ions. As a result, the smooth muscles of the bronchi, gastrointestinal tract, biliary tract, uterus, coronary, cerebral and pulmonary vessels relax, the coronary arteries dilate, and peripheral vascular resistance decreases. The drug increases the tone of the respiratory muscles (intercostal muscles and diaphragm), reduces pulmonary vascular resistance and improves blood oxygenation, activates the respiratory center of the medulla oblongata, increases its sensitivity to carbon dioxide, improves alveolar ventilation, which leads to a decrease in the severity and frequency of apnea episodes. Theophylline eliminates vasospasm, increases collateral blood flow and oxygen saturation, reduces perifocal and general cerebral edema, reduces cerebrospinal fluid and, accordingly, intracranial pressure. Improves the rheological properties of blood, reduces thrombus formation, inhibits platelet aggregation (inhibiting platelet activating factor and prostaglandin F2-α), normalizes microcirculation. It has an antiallergic effect, suppressing mast cell degranulation and reducing the level of allergy mediators (serotonin, histamine, leukotrienes). It increases renal blood flow, has a diuretic effect due to a decrease in tubular reabsorption, increases the excretion of water, chlorine ions, sodium, etc. The effect of the drug fully develops after 3-4 days from the start of treatment. When taken orally, theophylline is completely absorbed from the gastrointestinal tract, bioavailability is about 90%. When taking theophylline in the form of extended-release tablets, the maximum concentration is achieved after 6 hours. Plasma protein binding is about 60% in healthy adults and 35% in patients with cirrhosis. Penetrates through histohematic barriers, distributed in tissues. About 90% of theophylline is metabolized in the liver with the participation of several cytochrome P450 isoenzymes to inactive metabolites - 1,3-dimethyluric acid, 1-methyluric acid and 3-methylxanthine. Excreted mainly by the kidneys in the form of metabolites; up to 13% of the drug is excreted unchanged in adults, and up to 50% of the drug in children. Partially excreted in breast milk. The half-life of theophylline depends on age and the presence of concomitant diseases and is 6–12 hours in adult patients with asthma, 3–4 hours in children over 6 months, 4–5 hours in smokers, 4–5 hours in elderly patients and with cardiac disease. failure, impaired liver function, pulmonary edema, COPD and bronchitis - more than 24 hours, which requires appropriate adjustment of the interval between doses of the drug. The therapeutic concentration of theophylline in the blood to achieve a bronchodilator effect is 10-20 mcg/ml, for a stimulating effect on the respiratory center - 5-10 mcg/ml. Toxic concentration is above 20 mcg/ml.

Indications for use

Broncho-obstructive syndrome developed for various reasons:

• bronchial asthma (for asthma of physical exertion as a drug of choice, as well as for other forms of asthma as an additional drug);
• chronic obstructive bronchitis
• emphysema;
• cor pulmonale;
• pulmonary hypertension;
• edema syndrome due to kidney disease (in complex treatment);
• sleep apnea.

Contraindications

• gastritis (with high acidity);
• periods of exacerbation of gastrointestinal ulcer ;
• gastrointestinal bleeding;
• epilepsy;
• arterial hypo- or severe hypertension;
• hemorrhagic stroke;
• severe tachyarrhythmias ;
• retinal hemorrhage
• age up to 12 years (for non-extended forms up to 3 years);
• hypersensitivity to theophylline , as well as other xanthine ( theobromine , pentoxifylline, caffeine).

Carefully:

• severe manifestations of coronary insufficiency , including angina pectoris and the acute phase of myocardial infarction ;
• obstructive hypertrophic cardiomyopathy ;
• atherosclerosis ;
• chronic heart failure;
• frequent ventricular extrasystole ;
• increased convulsive readiness ;
• kidney or liver failure;
• gastrointestinal ulcer (diagnosed in the past);
• recent gastrointestinal bleeding;
• prolonged hyperthermia ;
• thyrotoxicosis or hypothyroidism ;
• gastroesophageal reflux;
• BPH;
• periods of breastfeeding and pregnancy;
• elderly or children's age.

Side effects

CNS:

• excitation;
• dizziness;
• anxiety;
• headache;
• irritability;
• insomnia;
• tremor.

The cardiovascular system:

• tachycardia (also observed in the fetus when using Theophylline in the third trimester);
• heartbeat;
• arrhythmias;
• cardialgia;
• decreased blood pressure;
• more frequent attacks of angina .

Digestive organs:

• gastralgia;
• diarrhea;
• heartburn;
• nausea;
• gastroesophageal reflux;
• vomit;
• exacerbation of peptic ulcer disease;
• decreased appetite (in case of long-term use).

Allergic manifestations:

• fever;
• rash and itching of the skin.

Other:

• tachypnea;
• chest pain;
• hot flashes to the face;
• hematuria;
• albuminuria;
• hypoglycemia;
• increased sweating;
• increased diuresis.

As a rule, when theophylline doses are lowered, side effects decrease.

Theophylline, instructions for use

Instructions for use of long-acting theophylline involve individual selection of doses of the drug.

On average, the initial oral daily dose is 400 mg. If the patient tolerates this dose well, it can be increased one-time by approximately 25%. It is recommended to increase doses every 2-3 days until the best therapeutic effect is achieved.

Without monitoring the content of theophylline in the blood, it is possible to take its maximum daily doses, which are: 18 mg/kg for ages 12-16 years and 13 mg/kg for ages after 16 years.

In cases where the use of the above doses is ineffective (requires an increase in dosage) or causes toxic symptoms , further therapy should be carried out under constant monitoring of theophylline in the blood. Optimal therapeutic doses are considered to be doses at the level of 10-20 mcg/ml. theophylline content is ineffective, and more does not lead to a significant increase in its effect, while the risk of side effects increases significantly.

Use of the drug Neophyllin

The dose of the drug is selected individually depending on the severity of the disease, the patient’s body weight, age, and metabolic characteristics of smokers. In adults, the initial dose is usually 0.3 g once a day. After 3 days, in the absence of serious side effects, the dose can be increased to a maintenance dose - 0.6 g (0.3 g 2 times a day), in the case of predominantly night and morning attacks - 0.6 g once in the evening. In smoking patients, the initial dose is 0.3 g once a day, which, if well tolerated, is gradually increased every 2 days by 0.3 g to a maintenance dose of 0.9–1.2 g (0.6 g in the evening, 0.3 -0.6 g in the morning). For persons weighing less than 60 kg, the daily dose is 0.3 g (once a day or 0.2 g in the evening and 0.1 g in the morning); for body weight less than 40 kg, the initial dose is 0.2 g once a day, the maintenance dose is 0.4 g (0.2 g 2 times a day). In children aged 12–16 years with a body weight of 40–60 kg, the initial dose is 0.3 g 1 time per day. After 3 days, if well tolerated, the dose can be increased to a maintenance dose of 0.6 g (0.3 g 2 times a day). For children aged 6–12 years with a body weight of 20–40 kg, the initial dose is 0.2 g 1 time per day. After 3 days, if well tolerated, the dose can be increased to a maintenance dose of 0.4 g (0.2 g 2 times a day). The initial dose for children aged 3–6 years weighing up to 20 kg is 0.1 g 1 time per day. After 3 days, if well tolerated, the dose can be increased to a maintenance dose of 0.2 g (0.1 g 2 times a day).

Overdose

In case of an overdose of Theophylline, the following were observed: loss of appetite, diarrhea , gastralgia , nausea leading to vomiting (possibly with blood), gastrointestinal bleeding . Ventricular arrhythmias , facial hyperemia, tachypnea , tachycardia . Insomnia , anxiety, motor agitation, tremor , photophobia, convulsions . In case of severe overdose, the development of epileptoid seizures (especially in childhood), hypoxia , confusion hyperglycemia , metabolic acidosis, hypokalemia , necrosis of skeletal muscles, decreased blood pressure , renal failure with myoglobinuria is possible.

Recommended treatment consists of drug withdrawal, gastric lavage, laxatives, activated charcoal , and colon lavage using electrolytes and polyethylene glycol . Also indicated are forced diuresis , plasma sorption , hemosorption , possibly, but ineffectively, hemodialysis , and the prescription of symptomatic therapy. In case of severe nausea and vomiting, intravenous administration of ondansetron or metoclopramide . In case of convulsions, it is necessary to ensure and monitor the patency of the airways, and also administer oxygen therapy . The seizure is stopped by intravenous administration of 0.1-0.3 mg/kg Diazepam , but not more than 10 mg.

Neofilin oral tablets

Instructions for medical use of the drug

Description of pharmacological action

The drug increases the tone of the respiratory muscles (intercostal muscles and diaphragm), reduces pulmonary vascular resistance and improves blood oxygenation, activates the respiratory center of the medulla oblongata, increases its sensitivity to carbon dioxide, improves alveolar ventilation, which leads to a decrease in the severity and frequency of apnea episodes. Theophylline eliminates vasospasm, increases collateral blood flow and oxygen saturation, reduces perifocal and general cerebral edema, reduces cerebrospinal fluid and, accordingly, intracranial pressure. Improves the rheological properties of blood, reduces thrombus formation, and inhibits platelet aggregation.

Indications for use

Bronchial asthma, status asthmaticus, chronic obstructive bronchitis and lung diseases with symptoms of bronchial obstruction, pulmonary hypertension, sleep apnea.

Release form

extended-release tablets 100 mg No. 50

Use during pregnancy

Contraindicated.

Contraindications for use

Hypersensitivity to the components of the drug and xanthine derivatives (caffeine, pentoxifylline), epilepsy, peptic ulcer of the stomach or duodenum in the acute stage, glaucoma, simultaneous use of oleandomycin or erythromycin, hemorrhagic stroke, hemorrhage in the retina, acute myocardial infarction, severe atherosclerosis of the coronary arteries, previous internal bleeding, pregnancy, lactation, children under 3 years of age, severe arterial hypertension, tachyarrhythmia, hypertrophic obstructive cardiomyopathy, hyperthyroidism.

Side effects

From the central nervous system: headache, dizziness, agitation, tremor, anxiety, insomnia, convulsions. From the gastrointestinal tract: discomfort and pain in the epigastric region, vomiting, heartburn, exacerbation of cholecystitis, cholestatic hepatitis, increased concentrations of ALT, AST in the blood. From the cardiovascular system: tachycardia, arrhythmia, decreased blood pressure. Allergic reactions: skin rash, itching, flu-like syndrome, difficulty in nasal breathing.

Directions for use and doses

The dose of the drug is selected individually depending on the severity of the disease, the patient’s body weight, age, and metabolic characteristics of smokers. In adults, the initial dose is usually 0.3 g once a day. After 3 days, in the absence of serious side effects, the dose can be increased to a maintenance dose - 0.6 g (0.3 g 2 times a day), in the case of predominantly night and morning attacks - 0.6 g once in the evening. In smoking patients, the initial dose is 0.3 g once a day, which, if well tolerated, is gradually increased every 2 days by 0.3 g to a maintenance dose of 0.9-1.2 g (0.6 g in the evening, 0.3 -0.6 g in the morning). In persons weighing less than 60 kg: the daily dose is 0.3 g (1 time per day or dividing the dose: 0.2 g in the evening, 0.1 g in the morning); for body weight less than 40 kg: the initial dose is 0.2 g 1 time per day, maintenance dose is 0.4 g (0.2 g 2 times per day). In children 12-16 years old (with a body weight of 40-60 kg): the initial dose is 0.3 g 1 time per day. After 3 days, if well tolerated, the dose can be increased to a maintenance dose of 0.6 g (0.3 g 2 times a day). In children 6-12 years old (with a body weight of 20-40 kg): the initial dose is 0.2 g 1 time per day. After 3 days, if well tolerated, the dose can be increased to a maintenance dose of 0.4 g (0.2 g 2 times a day). In children 3-6 years old (with body weight up to 20 kg): the initial dose is 0.1 g 1 time per day. After 3 days, if well tolerated, the dose can be increased to a maintenance dose of 0.2 g (0.1 g 2 times a day).

Overdose

Symptoms in adults: convulsions, increased body temperature, cardiac disturbances (tachycardia, ventricular arrhythmias, hypotension). Symptoms in children: increased excitability, mental disorders, increased body temperature, nausea, convulsions, tachycardia, hypotension, dyspnea. Treatment. Stop taking the drug, gastric lavage, intestinal irrigation with a combination of polyethylene glycol and salts, taking activated charcoal, stimulating the removal of theophylline from the body (forced diuresis, hemosorption, plasma sorption, hemodialysis, peritoneal dialysis) and prescribing symptomatic drugs: for severe nausea and vomiting - metoclopramide or ondansetron , for convulsions - diazepam.

Interactions with other drugs

With the simultaneous use of theophylline preparations with sympathomimetics and diuretics, their action mutually enhances; with β-blockers and lithium preparations - their effect mutually decreases. The pharmacotherapeutic effects of theophylline may be reduced when used simultaneously with xanthines, carbamazepine, diphenine, rifampicin, isoniazid, terbutaline. Allopurinol, cimetidine, isoprenaline, cyclosporine A, macrolide antibiotics (erythromycin, oleandomycin), lincomycin, oral contraceptives (estrogens) and anti-influenza serum increase the risk of side effects of theophylline (due to a decrease in its clearance), which necessitates the need to adjust its dose. The risk of developing side effects of glucocorticoids, mineralocorticoids, anesthetics increases (the risk of ventricular arrhythmias increases), xanthines and drugs that excite the central nervous system (neurotoxicity increases), ephedrine and ephedrine-containing drugs, beta-adrenergic agonists.

Special instructions for use

In case of severe diseases of the cardiovascular system, liver, viral infection, or in the elderly, the dose of the drug should be reduced and used with caution. In smokers, the effectiveness of the drug may be reduced.

Storage conditions

Store in original packaging at a temperature not exceeding 25 °C. Keep out of the reach of children.

Best before date

24 months

Interaction

Theophylline clearance decreases when taken in combination with macrolides , Allopurinol , oral contraceptives , Cimetidine , Lincomycin and Isoprenaline , Propranolol .

Concurrent use of beta-blockers , especially non-selective ones, can lead to narrowing of the bronchi , which will reduce the bronchodilating effect of theophylline , as well as possibly the effectiveness of the beta-blockers .

The effects of Theophylline are enhanced by β2-adrenergic receptor stimulants, Furosemide and Caffeine .

Aminoglutethimide increases the elimination of theophylline , which may reduce its effectiveness.

Concomitant use of Acyclovir or Disulfiram increases the level of theophylline , thereby increasing possible side effects.

Combined use with Felodipine , Diltiazem , Verapamil , Nifedipine , as a rule, moderately or slightly changes the content of theophylline in the blood, but does not affect the bronchodilator effect (cases of increased side effects have been described when taking Nifedipine or Verapamil simultaneously).

Parallel use of Theophylline and lithium salts may lead to a decrease in their effectiveness.

The combined use of Phenytoin and Theophylline reduces the concentrations and effectiveness of both drugs.

The therapeutic effect of Theophylline is reduced when taking Phenobarbital , Isoniazid , Rifampicin , Sulfinpyrazone and Carbamazepine .

A significant increase in the content of theophylline in the blood is caused by parallel administration of Enoxacin or other fluoroquinolones.

Drug interactions Neophylline

With the simultaneous use of theophylline preparations with sympathomimetics and diuretics, their action mutually enhances; with β-adrenergic receptor blockers and lithium preparations, their effect is mutually reduced. The pharmacotherapeutic effects of theophylline may be reduced (due to an increase in its clearance through the induction of microsomal liver enzymes) when used simultaneously with xanthines, carbamazepine, diphenin, rifampicin, isoniazid, terbutaline. Allopurinol, cimetidine, isoprenaline, cyclosporine A, macrolide antibiotics (erythromycin, oleandomycin), lincomycin, oral contraceptives (estrogens) and anti-influenza serum increase the risk of side effects of theophylline (due to a decrease in its clearance), which necessitates the need to adjust its dose. The risk of developing side effects of corticosteroids, mineralocorticoids, anesthetics (increases the risk of ventricular arrhythmias), xanthines and central nervous system stimulants (increases neurotoxicity), ephedrine and ephedrine-containing drugs, β-adrenergic agonists increases.

Analogs

Level 4 ATC code matches:
Aerophyllin

Eufillin

Theotard

Teopek

Aminophylline

Neophylline

Theophylline analogues are represented by the following drugs:

• Eufillin;
• Teofedrine-N;
• Diprophylline;
• Theobromine;
• Neo-Theophedrine.

Reviews

Information about this substance can be viewed from two sides. Therefore, first you need to understand how theophylline , what it is and what effect it has on the human body. Theophylline originally discovered in tea leaves and is similar in chemical structure to caffeine , although, unlike it, it exhibits different effects. The beneficial effects of tea on diseases of the lungs , cardiovascular system and other painful conditions have been known for a long time, and although the amount of theophylline in tea is quite small, it is certainly one of the components of the positive effect of this drink on the human body.

theophylline appeared , that is, a chemical used in medicine. Reviews from doctors about this drug, although not excellent, are often positive, with mention of some side effects . The thing is that the advisability of prescribing Theophylline can only be assessed by a doctor who has not only knowledge, but also sufficient experience. For example, the long-acting tablets we are considering are not suitable for relieving attacks , whereas with long-term therapy they can show excellent treatment results. You should also take into account medical history , concomitant diseases, individual sensitivity , taking other medications and much more, which is impossible for a person to do without appropriate training. In this regard, a doctor should prescribe therapy, and then the drug Theophylline will show all its positive sides.

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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use Neofilin, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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** Attention! The information presented in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of the drug Neofilin is provided for informational purposes and is not intended for prescribing treatment without the participation of a doctor. Patients need to consult a specialist!

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