Instructions Aerofilin tablets 400 mg No. 20
Composition
active ingredient: doxophylline;
1 tablet contains doxofylline 400 mg;
Excipients: sodium carboxymethylcellulose-microcrystalline cellulose; pregelatinized starch; lactose monohydrate; talc; povidone K-30; colloidal silicon dioxide aqueous; magnesium stearate; colloidal silicon dioxide anhydrous.
Dosage form
Pills.
Main physicochemical properties: round tablets with a biconvex surface, white in color, with a score on one side.
Pharmacotherapeutic group
Other agents for systemic use in obstructive airway diseases. Xanthines. Doxophylline. ATX code R03D A11.
Pharmacological properties
Pharmacodynamics
Doxofylline acts directly on bronchial smooth muscle and pulmonary vessels, resulting in bronchodilation. It acts primarily as a bronchodilator, pulmonary vasodilator, and bronchial muscle relaxant. The activity of doxofylline may be mediated, at least in part, by inhibition of the enzyme phosphodiesterase, which is accompanied by an increase in intracellular cAMP (cyclic adenosine monophosphate), which causes a decrease in the contractile activity of smooth muscle. Doxofylline at higher concentrations may slow the release of histamine from cells.
Pharmacokinetics
The biological half-life of doxofylline is more than 6 hours, which ensures effective constant plasma levels of the drug when administered three times a day. After taking the tablet dosage form, the maximum plasma level of the drug is reached after 60 minutes.
Absolute bioavailability is approximately 62.6%; at pH 7.4, the amount of plasma protein binding is approximately 48%.
When administered orally, less than 4% of the drug is excreted unchanged in the urine.
Indication
Bronchial asthma.
Lung disease with a bronchial spastic component.
Contraindication
Aerofilin® is contraindicated in patients with hypersensitivity to doxofylline or other xanthine derivatives. It is also contraindicated in patients with acute myocardial infarction, arterial hypotension.
Interaction with other medicinal products and other types of interactions
Aerofilin® should not be used together with other xanthine derivatives. It is recommended to limit the intake of foods and drinks containing caffeine.
Caution should be exercised when using Aerofilin® with ephedrine and other sympathomimetics.
When doxofylline is used simultaneously with other drugs such as erythromycin, troleandomycin, lincomycin, clindamycin, allopurinol, cimetidine, influenza vaccine and propranolol, as well as when xanthines interact with disulfiram, fluvoxamine, interferon α, oral contraceptives, the elimination of xanthine derivatives may be slowed down with an increase in the level of the drug in the blood plasma. In such cases, the dose of the drug should be reduced.
As with other xanthines, concomitant administration of ranitidine may reduce the hepatic clearance of doxophylline, leading to increased blood levels. In such cases, the dose should be reduced. No relationship has been established between serum doxophylline concentrations and toxicity.
Concomitant use of doxofylline with phenytoin, other anticonvulsants, use of doxofylline in patients who smoke, as well as the interaction of xanthines with rifampicin, ritonavir, sulfinpyrazone, may accelerate the elimination of xanthine derivatives with a subsequent decrease in plasma half-life. In these cases, the dose of the drug should be increased.
Xanthines have a risk of toxic synergy with ephedrine or halothane and ketamine. They may interfere with the action of adenosine and other neuromuscular blocking agents.
Lithium elimination may be increased with subsequent loss of effect. Xanthines may potentiate hypokalemia caused by hypoxia or associated with the use of β2-adrenergic agonists (β2-adrenergic agonists), corticosteroids, and diuretics. Concomitant use of xanthines and β-blockers should be avoided because β-blockers may cause bronchospasm.
Application features
Several factors may contribute to a decrease in hepatic clearance of xanthine derivatives, which will increase the drug's plasma levels. These include: age, congestive heart failure, chronic obstructive pulmonary disease, severe liver disease, concomitant infections, concomitant use of multiple drugs such as erythromycin, lincomycin, troleandomycin, clindamycin, allopurinol, cimetidine, influenza vaccine, propranolol. In these cases, the dose of the drug should be reduced.
In situations that may affect the excretion of xanthine derivatives, laboratory monitoring of doxofylline plasma concentrations is recommended to control the therapeutic range.
The drug should be used with extreme caution in patients with elevated body temperature, cardiac arrhythmias, and alcoholism.
Aerofilin® should be used with caution in patients with heart disease, patients with arterial hypertension, elderly patients, and patients with severe hypoxemia, hyperthyroidism, chronic right ventricular failure, congestive heart failure, liver disease, peptic ulcer, and patients with impaired renal function.
Particular caution should be exercised when treating patients with congestive heart failure, as in such patients the elimination of the drug from the blood is significantly slowed with prolonged high plasma levels after discontinuation.
Doxofylline is not habit-forming or addictive.
Aerofilin® contains lactose, so if the patient has been diagnosed with an intolerance to some sugars, they should consult a doctor before taking it.
Use during pregnancy or breastfeeding
Pregnancy: Animal studies have shown that the active substance doxofylline does not harm prenatal and postnatal development.
Since experience with doxofylline during pregnancy is limited, this medicine should be used in pregnant women only if clearly needed, taking into account the benefit/risk ratio.
Breastfeeding. Doxofylline is contraindicated in women who are breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
The drug does not affect the reaction speed when driving vehicles or other mechanisms.
But in case of adverse reactions from the nervous system (tremor, dizziness), it is necessary to limit driving or working with other mechanisms.
Method of administration and doses
The dose is set by the doctor individually depending on the age, body weight and metabolic characteristics of the patient. The average daily dose for adults and children over 12 years old is 800–1200 mg (1 tablet 2–3 times a day). Children aged 6 to 12 years old – ½ tablet 2–3 times a day (12–18 mg/kg per day).
Children
The drug should be used in children over 6 years of age.
Overdose
In case of overdose, the patient may experience severe cardiac arrhythmia, tonic-clonic convulsions, agitation, increased diuresis, and increased manifestations of adverse reactions. These symptoms may be the first sign of intoxication.
Since there is no specific antidote, in case of overdose, symptomatic therapy for heart failure and anticonvulsant therapy should be used.
Adverse reactions
On the part of the digestive tract: nausea, vomiting, epigastric pain, gastroesophageal reflux, rarely - diarrhea, dyspepsia.
From the nervous system: irritability, headache, insomnia, dizziness, tremor, convulsions.
From the cardiovascular system: extrasystole, palpitations, tachycardia, arrhythmia.
From the respiratory system: tachypnea.
From the blood system: in rare cases - hyperglycemia, albuminuria.
Allergic reactions: rarely - hypersensitivity reactions, including anaphylactic shock, angioedema.
Expiration date
5 years.
Storage conditions
Store at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister; 2 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
A. B. C. PHARMACY S.P.A.
Location of the manufacturer and address of its place of business
VIA CANTONE MORETTI, 29 (loc. LOCALITA SAN BERNARDO) - 10015 IVREA (TO), Italy.
Applicant
A. B. C. PHARMACY S.P.A.
Applicant's location
CORSO VITTORIO EMANUELE II, 72 10121 - TURIN (TO), Italy.
