Astmopent

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Non-selective stimulator of b-adrenergic receptors . Stimulates β1- and β2-adrenergic receptors . It has a bronchodilator effect and an effect on the myocardium.

Its chemical structure is similar to isadrin , but in comparison with it, the selectivity of the action on the receptors of the bronchial system is more pronounced, and the bronchodilator effect is longer lasting. By acting on adenylate cyclase , it inhibits the entry of calcium into the cell. A decrease in intracellular calcium and a simultaneous increase in intracellular cAMP causes relaxation of the smooth muscle fibers of the bronchial system . of histamine , leukotrienes , and serotonin from mast cells is also inhibited The drug is used for the prevention and relief of bronchospasm .

The effect develops after 10 minutes, complete relief of the attack is noted after 1 hour, the duration of action is 3-5 hours. The drug increases the force of myocardial contractions, and has a beneficial effect in case of conduction disorders. Side effects include tachycardia and tremor .

Pharmacokinetics

The half-life from the blood is up to 2.5 hours. It is excreted mostly by the kidneys.

Astmopent (Alupent) - complete instructions

The chemical name of Astmopent in international format is orciprenaline.

Compound

The main component of the suspension drug is orciprenaline sulfate in an amount of 750 micrograms.

The following additional ingredients were used: natural soy lecithin, sorbitol span 85, fluorotrichloromethane (Freon 11) and difluorotrichloromethane (Freon 12).

Release form

Inhalation metered spray. Alupent (asthmopent) is an inhalation drug against asthma.

Useful information on inhalations:

Pharmacology

The pharmacodynamic effect is that orciprenaline sulfate suppresses the focus of inflammation in the bronchi, localizes spasms in the bronchi, and activates β2-adrenergic receptors.

Pharmacokinetics show that after 10–15 minutes. after the inhalation procedure, the product begins to act, reaches its maximum effect after an hour and a half, and retains it for another three to six hours.

The drug is half-removed from the blood plasma, combined with sulfuric acid, mainly by the kidneys for about 2-3 hours.

Astmopent indications for use

Suppression of attacks of shortness of breath, which are caused by spasms of smooth bronchial muscles in asthmatic conditions and chronic pulmonary diseases (obstructive bronchitis, pulmonary emphysema).

Asthmopent dosage

It is recommended to prescribe an initial dose of Astmopent to adults and children over 12 years of age in 1–2 doses. If there is a need to repeat the dosage, this can be done about half an hour after the first use. The next dose is recommended after 4 hours. You cannot use the product more than 12 times a day.

With one-time use, the medicine can also be used in the treatment of children from three years of age.

Side effect

Sometimes there is a feeling of excitement and fatigue. Unpleasant symptoms such as nausea, vomiting, and an unpleasant taste sensation may occur. In rare cases, headaches and dizziness occur, blood pressure rises, sweating increases, muscles tremble, various types of arrhythmias appear, in particular tachycardia, and the concentration of potassium in the blood decreases.

Patients who are too sensitive to all components of the spray sometimes experience allergic reactions. In some cases, orciprenaline sulfate causes coughing, and even less often, it causes bronchospasms and increases shortness of breath.

The drug is contraindicated for patients with hypersensitivity to the components of the aerosol, suffering from arrhythmia and should not be used during the lactation period.

At the first signs of overdose, you should stop taking the drug and eliminate the symptoms of overdose.

Special instructions for the use of asmopent

With great caution, the drug is prescribed to patients with coronary artery disease (coronary artery disease), hypertension, hyperthyroidism, diabetics and epileptics. When the dose is increased, the patient’s condition does not improve; the heart rhythm may only be disturbed

When the dose is increased, the patient's condition does not improve; the heart rhythm may only be disturbed.

There is very little information about the effect of the drug on the fetus during pregnancy. Consequently, it is prescribed to pregnant women only when the benefits for the mother are significantly higher than the consequences for the fetus.

Astmopent does not in any way affect the ability to drive vehicles.

How to use the product

To achieve an effective treatment result, the main thing is to use the inhaler correctly. Children should only use the medicine under adult supervision.

During the first use, shake the can vigorously and spray one or two times into the air.

When performing inhalation, do the following:

1. Remove the safety cap.
2. Shake the substance vigorously by shaking the container.
3. Exhale deeply through your mouth.
4. Turn the canister upside down and squeeze the inhaler tube with your lips. Make sure that the guides on the sticker and can are facing up.
5. Take a deep breath of air flow into your lungs and at the same time press the bottom of the container. Then hold your breath for a couple of seconds, remove the tube from your mouth and exhale.
6. Close the bottle with the cap.
7. The inhalation tube (mouthpiece) must be constantly cleaned with heated water.

There is no need to violate storage conditions. Temperature – 15-25 degrees. Places that are inaccessible to children. Do not allow overheating to exceed 50°C. The can should not be disassembled.

Astmopent analogues

It is recommended to replace asthmapent with bronchodilators, in particular albuterol or terbutaline. However, they must be prescribed after testing.

Other products of this type:

Indications for use

• bronchospasm in obstructive bronchitis , bronchial asthma , emphysema and pneumosclerosis ;
• prevention of bronchospasm during bronchoscopy , after operations on the chest organs;
• Morgagni-Adams-Stokes syndrome;
• heart block;
• bradycardia while taking glycosides;
• heart failure.

Astmopent's analogs

Salbutamol

OJSC "Moskhimfarmpreparaty", Russia
The average cost is 120 rubles per package.

Salbutamol is one of the most famous drugs for relieving and preventing asthmatic attacks. With the help of the drug, you can successfully fight this disease; this drug is also on the list of potent substances that are prohibited for use by the Anti-Doping Agency. Salbutamol helps not only from narrowing the lumens of the bronchi, but also supports the health of patients suffering from emphysema, chronic bronchitis, and asthmatic bronchitis. Less commonly, salbutamol can be given to improve labor if the expectant mother has no contraindications to use.

Pros:

• An effective and inexpensive remedy
• Helps quickly.

Minuses:

• Has side effects
• Negatively affects the heart.

Berotek

Boehringer Ingelheim, Germany
The average cost in Russia is 450 rubles per package.

Berotec is an inhalation drug based on fenoterol hydrobromide. The drug is a selective beta-2 receptor stimulant, which in theory makes it safer to use. Despite its selectivity, it still has a sufficient list of side effects.

Pros:

• Efficiency and speed
• Imported good analogue.

Minuses:

• Expensive product
• There are side effects.

Contraindications

• increased sensitivity;
• age up to 12 years;
• tachyarrhythmia;
• ventricular fibrillation;
• hyperthyroidism;
• pronounced tachycardia .

Prescribed with caution for arterial hypertension , diabetes mellitus in the stage of decompensation, coronary artery disease , epilepsy . It is not recommended to take it with MAO inhibitors and non-selective beta-blockers .

Drug interactions

In the case of simultaneous use, methylxanthines, anticholinergics, sympathomimetics and beta-adrenergic agonists enhance the effect of Asthmopent, resulting in headache, anxiety, palpitations, dizziness and hypokalemia.

The drug is not recommended for use simultaneously with non-selective beta-blockers, sympathomimetics and beta-agonists.

Monoamine oxidase inhibitors and tricyclic antidepressants enhance the effect of orciprenaline on vascular smooth muscle.

Side effects

• anxiety, dizziness , weakness, headache , muscle tremors , convulsions;
• nausea, taste in mouth, vomiting;
• increased blood pressure , tachycardia , cardiac arrhythmia, palpitations, chest pressure;
• allergic reactions;
• sweating , cough;
• hypokalemia;
• paradoxical bronchospasm (very rare).

Asthmopent

Packaging Aerosol for inhalation

Pharmacological action Stimulates beta2-adrenergic receptors.

List of analogues of "asthmopent"

— Alupent

* — the list and cost are formed without taking into account the forms of release of the drug

Indications for use

Relief of asthma attacks in bronchial asthma, chronic obstructive pulmonary diseases (chronic bronchitis, emphysema).

Release form

• aerosol dosed 0.75 mg/dose
• aerosol can (can) 20 ml with dispenser, box (box) 1

Pharmacodynamics of the drug Interacts (mainly) with beta2-adrenergic receptors of bronchial smooth muscle, activates adenylate cyclase, which increases the amount of cAMP, which leads to a decrease in the concentration of intracellular calcium and bronchodilation. Inhibits the release of biologically active substances from mast cells, improves mucociliary clearance; causes tachycardia and increases myocardial oxygen demand, improves AV conduction, dilates peripheral vessels and reduces blood pressure. It has tocolytic properties (activates beta2-adrenergic receptors in the smooth muscles of the uterus). Depending on the route of administration, from 3% (inhalation) to 10% (enteral) is absorbed. Metabolized in the liver.

Excreted in feces.

Pharmacokinetics of the drug: About 3% of the inhaled dose enters the systemic circulation unchanged from the bronchi. Cmax in serum is recorded after 2.5 hours. Metabolized in the liver; T1/2 - 2.5 hours; excreted in urine and feces.

Use during pregnancy is possible only after consultation with a doctor.

Contraindications for use

Hypersensitivity, tachyarrhythmia, hyperthyroidism.

Side effects From the nervous system and sensory organs: anxiety, weakness, dizziness, headache, convulsions or muscle tremors. From the gastrointestinal tract: nausea, vomiting, unpleasant taste in the mouth. From the cardiovascular system and blood (hematopoiesis, hemostasis): increased blood pressure, cardiac arrhythmia, tachycardia, palpitations, feeling of pressure in the chest. Other: allergic reactions, sweating, hypokalemia, cough; very rarely - paradoxical bronchospasm and increased asthma attack.

DosageInhalation. Adults and children over 12 years of age: 1-2 inhalations once, if necessary - again (not earlier than after 20-30 minutes). With regular use, the intervals between inhalations are 4 hours. The maximum daily dose is no more than 12 doses. Using an inhaler

When using for the first time, shake the inhaler and press the metering valve 1 or 2 times.

When inhaling it is necessary:

1.

3.

5.

After inhalation, the mouthpiece should be closed with a lid.

Interactions with other drugs Increases the effect of antidepressants; When used together with beta-blockers, idiosyncratic phenomena are possible.

Precautions when taking: Prescribe with caution for ischemic heart disease, arterial hypertension, decompensated diabetes mellitus, epilepsy, in combination with MAO inhibitors. Concomitant use with non-selective beta-blockers is not recommended.

Storage conditions: Protected from light, at a temperature not exceeding 25 °C.

Shelf life: 36 months.

pharmachologic effect

Antiasthmatic

Description The anti-asthmatic effect is associated with inhibition of the release of histamine and other mediators from mast cells, blocking histamine H1 receptors and inhibition of the PDE enzyme, resulting in an increase in the level of cAMP in mast cells.

Active ingredients

Orciprenaline

DescriptionWhite crystalline powder.

The data provided is for informational purposes only. Before use, please consult a specialist.

Astmopent, instructions for use (Method and dosage)

The Astmopent inhaler is intended for inhalation use by adults and children over 12 years of age. Prescribe 1-2 inhalations at a time. If necessary, repeat inhalation is carried out after 30 minutes. With regular use, an interval of 4 hours must be observed between inhalations. The daily dose should not exceed 12 doses.

When inhaling, you need to remove the cap from the mouthpiece and shake the inhaler. Holding it vertically, place your finger on the base of the can and insert the mouthpiece into your mouth, wrapping your lips around it. After a deep exhalation, begin inhaling and press the canister, continuing to take a deep breath. After this, the breath is held and the inhaler is removed from the mouth. The mouthpiece is covered with a lid. Once a week, wash the mouthpiece cover and the inhaler body with warm water and dry it.

Release form and composition

• tablets (10 pcs. in blisters, 2 blisters per package);
• dosed aerosol: suspension with a characteristic odor, from white to light yellow [in 20 ml cans (400 doses), 1 can in a cardboard pack];
• solution for injection (1 ml in ampoules, 10 ampoules per package).

Active substance: orciprenaline (in the form of sulfate):

• 1 tablet – 20 mg;
• 1 dose of aerosol – 0.75 mg;
• 1 ml of solution – 0.5 mg.

Auxiliary components of the aerosol: purified soy lecithin, dichlorofluoromethane, trichlorofluoromethane, sorbitol trioleate.

Reviews about Astmopent

Almost all β-adrenergic agonists cause tremor , trembling of fingers, irritability, restlessness and anxiety. The occurrence of tremor usually coincides with the development of a bronchodilator effect. Adverse reactions occur much more often when taking non-selective or partially selective adrenergic agonists ( alupent , asthmapent ). If we compare Astmopent - Salbutamol , the latter is a selective β2-adrenergic agonist and is considered as a more promising and safe drug that does not cause adverse reactions. The bronchodilator effect occurs quickly - after 2-5 minutes and the maximum effect is achieved after 40-60 minutes. It lasts from 4 to 6 hours. In addition, it promotes the separation of sputum and is highly effective for expiratory shortness of breath, since it is able to expand small bronchi. However, this drug also has side effects when the dose is increased (selectivity disappears), or the frequency of use increases (the drug accumulates, which leads to the disappearance of selectivity). Therefore, all these drugs are taken strictly in doses and repeated doses are possible no earlier than after 3 hours.

Patient reviews note the effectiveness of Astmopent, which prevailed over adverse reactions. Some patients switched to other inhalers without pain.

• “... This is the only medicine that REALLY helped! The price suited everyone, but now it’s gone!!!”
• “... Stopped the attacks well. It’s bad that it’s not for sale now.”
• “...Berotek doesn’t help me after Astmopent.”
• “... I used Astmopent aerosol for many years, and after it disappeared from pharmacies I switched to other safer products. Personally, I didn’t feel any difference.”

Interaction

Astmopent should not be used in conjunction with drugs with adrenomimetic and sympathomimetic effects due to additive effects. The same applies to monoamine oxidase inhibitors (antidepressants, antiparkinsonian drugs). But beta blockers inhibit the activity of orciprenaline.

Astmopent is an effective drug for the relief and prevention of broncho-obstructive syndrome. It can be used in other situations, but is prescribed only by a doctor. After an appropriate examination, the specialist will determine the optimal dosage form, dosage and course of administration. And the patient must adhere to his recommendations.

Side effects

Astmopent, like its orciprenaline-based substitutes, in addition to the main therapeutic effects, has a number of side effects. Negative phenomena during treatment with the drug include:

1. Cardiovascular (tachycardia, hypotension, angina).
2. Neurological (hand tremors, headaches and dizziness, anxiety, insomnia, convulsions).
3. Dyspeptic (nausea and vomiting).
4. Allergic (itching and urticaria).
5. Respiratory (paradoxical bronchospasm, atrophy of the ciliated epithelium).
6. Other (addiction, increased sweating).

Such effects must be taken into account when prescribing the drug, and their pronounced intensity becomes a reason for its discontinuation.

Top 5 best inhalers

A detailed analysis revealed the best inhalers indicated for bronchial asthma:

1. Symbicor Turbuhaler is suitable for the treatment of severe disease, has a long-lasting effect, and prevents the occurrence of symptoms.
2. Seretide Multidisk relieves asthma attacks for a long time and improves the ventilation function of the lungs.
3. Berodual is recommended for daily use for mild asthma; it quickly relieves bronchospasm.
4. Berotek-N is prescribed for emergency relief of bronchoconstriction and inhibits the inflammatory process in the respiratory system.
5. Pulmicort Turbuhaler is an alternative for moderate cases of the process, it has an anti-inflammatory and antihistamine effect, and allows you to avoid the systemic use of hormonal drugs.

Thus, treating bronchial asthma with properly selected drugs will help prevent the progression of the disease, achieve stable remission and improve the quality of life.