Salbutamol

The drug considered in this article is classified as a synthetic drug developed to provide emergency medical care. Salbutamol is a drug with anti-inflammatory properties and belongs to a group of clinical pharmacological agents with bronchodilator and mucolytic properties. Salbutamol is a drug classified as a beta 2-adrenomimetic.

Any disease affects our quality of life to a greater or lesser extent. Therefore, in order not to aggravate the clinical picture, at the first attacks of bronchial asthma with manifestations of bronchospasm, it is necessary to immediately consult a specialist. Without knowing the pharmacodynamics of the drug and the features of its interaction with other drugs, you should not self-medicate. Such an attitude to therapy can result in serious complications that worsen the patient's condition. Only a qualified specialist, based on the clinical picture and health condition and anamnesis of the patient, can prescribe a truly effective and minimally safe protocol for therapeutic therapy. Salbutamol is a high-quality drug with bronchodilating and mucolytic properties, which effectively stops or prevents attacks of spasm of the tissue structure of the bronchi. It will improve the patient's condition, returning him to normal life, but you should not deviate from the recommendations given by the attending physician.

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Indications Salbutamol

Before starting to develop any drug, it is necessary to understand what the indications for the use of Salbutamol should be, and, accordingly, what pharmacological characteristics it should have.

Therefore, having the necessary chemical and biological characteristics, Salbutamol can be used in the treatment of such pathological diseases:

1. Prevention of the occurrence of spasms of bronchial asthma in any form of its course.
2. Direct relief of suffocating attacks.
3. Improving the patient's condition in the presence of obstructive processes in the patient's body, which is characterized by narrowing or complete blockage of the passage section of the lumens in the bronchi. Therapy is effective if the obstruction process is reversible.
4. Prevention of possible complications of bronchitis.
5. Broncho-obstructive syndrome in young patients.
6. Emphysema of the lungs is increased airiness of the lung tissue.
7. Premature obstetrics, which is associated with a high tone of contractile activity of the uterus. This pathological failure during pregnancy poses a threat to the viability of the fetus. This pathology is especially dangerous if the woman's pregnancy is less than 37 weeks.
8. Decreased heart rate in a newborn during obstetrics at different stages of the birth process.
9. Low tone of functional activity of the cervix. Isthmic-cervical insufficiency.
10. Preventive measures that are carried out immediately before a surgical intervention affecting the uterus of a woman who is currently carrying her baby.

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Release form

Mainly Salbutamol, the active active chemical-pharmacological compound of which is salbutamol, as well as other drugs developed on the basis of this chemical substance, are presented in aerosols. This form of release is one of the most "in demand", as it is very convenient and easy to use. The aerosol form contains, in addition to the main active chemical compound, also fluorotrichloromethane and difluorodichloromethane, as well as ethanol and oleic acid.

Salbutamol is produced by the manufacturer in the form of an aluminum bottle, equipped with a protective cap, which simultaneously functions as a dosing device. To spray the medicinal drug into the oral cavity and throat, you just need to press the dispenser and it will “give out” the amount of medicine, which is equal to 0.1 mg. That is, 0.1 mg is one press - this is one dose.

Another form of the drug in which this medication is released is a tablet, which can be found on pharmacy shelves in two dosages of the active substance: 2 mg or 4 mg per unit of medication. The packaging form for a dosage of 2 mg is a blister of 15 pieces, which are packed in a cardboard box with two blisters. The packaging form for a dosage of 4 mg is a glass bottle.

Much less frequently, but still, Salbutamol is also used in the form of an injection solution, which is used for intravenous drip infusions.

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Pharmacodynamics

With the correct dosage, Salbutamol effectively activates the work of beta 2 - adrenergic receptors located on the surface layer of the bronchial lining. There are such receptors in the muscle tissues of the uterus, and they also serve the blood vessels.
Pharmacodynamics Salbutamol helps block the release of active chemical compounds from mast cells, which occurs over a long period of time.

The action of the drug makes it possible to increase the vital capacity of the lungs. This parameter is measured if, with a deep breath, the volume of air exhaled without much effort is measured.

Salbutamol helps prevent bronchial spasm, and if such an attack occurs, it actively stops it in a matter of minutes. The active substance reduces the resistance of the airways, blocking bronchial reactivity.

Salbutamol somewhat liquefies the sputum accumulated in the bronchi, facilitating its removal. It allows stimulating the functioning of the cellular structures of the ciliated epithelium, which prevents the provocation of the development of bronchial spasm caused by an allergic reaction of the patient's body to an external irritant. Under certain factors, the drug is able to affect the synthesis of insulin in the blood (growth in glucose levels) and the breakdown of glycogen (namely lipids), which is very important for patients with diabetes. There are situations where the clinical picture against the background of therapy, the protocol of which includes Salbutamol, shows a decrease in the amount of potassium in the patient's blood plasma.

Beta-adrenergic agonists, to which the drug in question belongs, have a targeted effect on β ₂ -adrenergic receptors.

Compared with other drugs in this group, Salbutamol does not have a significant effect on the components of the cardiovascular system. This applies to both inotropic and chronotropic effects. When treated with this drug, no pathological changes in blood pressure values are observed. Under the influence of this medication, in some cases, a slight increase in the diameter of the coronary vessels of the heart is observed.

The drug in question effectively works to reduce the tone and intensity of myometrium contraction, acting on this organ of the female reproductive system tocolytically.

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Pharmacokinetics

The high efficiency of the pharmacokinetics of Salbutamol is demonstrated by the fact that the therapeutic result, in the case of aerosol administration, begins to be observed already during the first minutes of the drug's action. The maximum efficiency is achieved after half an hour to an hour from the moment of drug administration. This indicator directly depends on the individual characteristics of each specific patient's body. The effect of the drug used in the form of an aerosol is observed for another three hours.

If the form of administration is tablets, such administration is more prolonged, and the effectiveness of the clinical picture of the disease can last from six to eight hours. But when taking tablets, there are also disadvantages, compared to an aerosol - the medicinal effect occurs only half an hour after their intake.

In the case of prescribing an aerosol form of administration, the administered substance is absorbed into the blood fairly quickly, but in this case, the concentrations of Salbutamol in the patient's blood that are determined during the study are not observed or are found in very small doses.

The active substance of the drug in question shows a low percentage (only 10%) of binding to blood proteins. Salbutamol metabolism processes occur in the liver during its primary passage. The main metabolite of the basic chemical compound of the drug is an inactive sulfate conjugate.

The main way of drug elimination is the utilization of metabolites to a greater extent and unchanged substance to a lesser extent through the kidneys, together with urine. A small amount of them leaves the patient's body together with bile or feces.

The half-life (T _1/2 ) of this drug is from two to seven hours. This indicator significantly depends on the health characteristics of the patient's body at the time of therapy.

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Dosing and administration

If the patient's medical history shows the need to add the drug Salbutamol to the treatment, the attending physician, depending on the treatment picture and the patient's condition, chooses the most effective method of administration and dose of the drug.

When prescribing a medicine in the form of an aerosol, it is allowed to take one or two doses of the medicine, which corresponds to one or two presses on the cap - the dispenser of the aerosol can, respectively. To remove bronchospasm - this is quite enough. If after ten minutes there is no improvement in the patient's condition, then another dose of the medicine is allowed in the same dosage. Then it is necessary to maintain an interval in inhalations of at least four to six hours (it is better, if possible, to maintain six). The number of inhalations during the day should not exceed six procedures.

When prescribing the drug in tablet form as a bronchodilator to adults and adolescents who are already 12 years old, the recommended dose is 2-4 mg (one tablet, taking into account the concentration of the active substance), administered orally three to four times a day.

If therapeutically necessary, the amount of the drug can be increased to 8 mg (4 tablets of 2 mg or 2 tablets of 4 mg), administered four times a day. Hence, the maximum daily amount of the drug that a patient can take in one day is 32 mg.

For small patients aged between six and 12 years, it is recommended to take 2 mg (one tablet) three to four times a day, for children aged between two and six - 1 to 2 mg three times a day.

As a tocolytic agent, Salbutamol is used intravenously by drip in a dosage of 1–2 mg.

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Use Salbutamol during pregnancy

If a woman has a period of pregnancy burdened with bronchial asthma, the use of Salbutamol during pregnancy is entirely acceptable, but the medication should be taken with careful adherence to prescribed therapeutic dosages. In this case, the pregnant woman should be under the constant supervision of a doctor - gynecologist, who leads her pregnancy.

Previously, women who had a history of such a diagnosis, to become pregnant and bear a baby was strictly forbidden. Modern women with such problems got the opportunity to become mothers thanks to such a drug as Salbutamol. It effectively prevents the onset or arrest of an already started attack of bronchospasm.

Apply the medication in question and if the pregnant woman has a premature birth process. This is particularly true when the pregnancy is less than 37 weeks. Salbutamol also helps in the case when the doctor diagnoses a future mother with placental insufficiency.

But it should be clearly remembered that the medicament can be prescribed only by the attending physician and only in a situation where the therapeutic effect when taking it for a pregnant woman is significantly more significant than the harm that can threaten her unborn baby.

To date, there is no reliable data on the effect of salbutamol on fetal development in the early stages of pregnancy. Therefore, the obstetrician-gynecologist prefers to avoid prescribing this medication in the first trimester of pregnancy and with special caution goes to this during the second trimester. 

The active substance penetrates into the breast milk of a woman, so if the therapy is necessary for a woman at the time when she feeds her newborn baby with mother's milk, it is necessary to refuse breastfeeding and transfer the baby to artificial nutrition, because the modern food market offers a wide range of baby food .    

Contraindications

The drug in question is a synthetic chemical compound that has a chemically active substance, which has an effect on the patient's body. But it is impossible to completely exclude its effects on other organs and systems, especially when it comes to the tablet form of administration of the drug to the patient's body. Therefore, there are also
Contraindications to the use of Salbutamol, which are due to:

1. The patient's age. For example, a medicine in the form of an aerosol is not allowed to be administered to children under two years of age, while its tablet form and inhalation powder are prohibited for children under four years of age.
2. Premature detachment of the placenta in a pregnant woman.
3. Individual intolerance to the components of the drug.
4. The threat of miscarriage, which occurs in the first or second trimester of pregnancy.
5. Uterine bleeding in the third trimester of pregnancy.
6. Late toxicosis.

In other cases, during pregnancy, the use of this drug is carried out under the close supervision of the attending physician.

Salbutamol should be administered with special caution to people who suffer from tachyarrhythmia, as well as to those who have a history of serious heart problems (for example, aortic stenosis, acute heart failure, heart disease, myocarditis). Under the supervision of a doctor, the drug in question should also be taken if the patient suffers from diabetes, arterial hypertension, optic nerve damage (glaucoma), thyrotoxicosis (excess thyroid hormones in the body).

If there is a therapeutic need to reduce the interval between doses of the drug (such a step must be exceptional and clinically justified) or increase its dosage, these changes must be adjusted by a specialist. Taking the drug with a changed treatment protocol must be carried out under constant supervision of a doctor.

During Salbutamol therapy, there have been cases where hypokalemia has developed. Therefore, when treating bronchial asthma, the patient's blood calcium level should be regularly monitored. The probability of developing this pathological deviation is higher, the more pronounced the hypoxia.

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Side effects Salbutamol

Taking medication sometimes causes unpleasant side effects, which in some cases require immediate discontinuation of the medication and its replacement with another analogue. Or the dosage is adjusted or symptomatic treatment is performed.

The side effects of Salbutamol are varied.

The following may be encountered predominantly:

• Tremor of the upper (mainly) and lower extremities. This symptom is quite common in beta-adrenergic receptor drugs. It largely depends on the dosage of the drug taken.
• The patient may feel internal trembling.
• Increased heart rate.
• Problems with sleep.

Somewhat less frequently observed:

• Dizziness.
• Irritability.
• Pain symptoms affecting the head area.
• Nausea, and if particularly intense, the urge to vomit.
• Increase in the diameter of the cross-section of the peripheral vessels of the brain.
• Drowsiness.
• Hyperemia of the skin.

Quite rarely, but the following may occur:

• Angioedema.
• Hallucinations.
• A sharp drop in blood pressure, leading to fainting and collapse.
• An attack of bronchial spasm.
• Hypersensitivity and allergic reaction of the body: urticaria, itching, skin rash and others.
• Unstable psychological state.
• Ventricular fibrillation.
• Cardiovascular failure.
• Hypokalemia is a decrease in potassium in the patient’s blood.
• Increased hyperactivity in young patients.
• Irritation of the mucous membrane of the mouth and pharynx.
• Supraventricular extrasystole.
• Muscle cramps.

If the patient or his relatives begin to observe the appearance of one or more symptoms from this list, they should immediately notify their attending physician.

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Overdose

If the recommended doses of the drug taken were violated, or due to the individual characteristics of the patient's body and his medical history, the administration of Salbutamol may lead to an overdose of the drug, manifested by its symptoms.

When taking the medication in tablet form, the following pathological manifestations can be expected:

1. The appearance of increased heart rate.
2. Heart rhythm disturbance.
3. Cramps.
4. Pathological change in blood pressure readings: both in the direction of a sharp increase and in the direction of a rapid decrease in these values.
5. Dizziness.
6. Insomnia.
7. Upper limb tremor.
8. Painful symptoms in the heart area.
9. There is a high risk of developing hypokalemia.

Excess of the active substance in the patient's body after taking the medication in aerosol form can cause excessive stimulation of b-adrenergic receptors, as well as symptoms similar to those described above.

Treatment therapy, when signs of overdose appear, consists of several points.

1. Discontinuation of the drug that caused the side effects.
2. Carrying out measures to provide first medical aid: gastric lavage, administration of adsorption materials (for example, activated carbon).
3. Prescribing appropriate symptomatic therapy. The victim is given an antidote - a drug belonging to the group of drugs cardioselective b-blockers. But all these drugs must be prescribed very carefully, especially if the patient's history includes such a pathology as bronchospasm.
4. If it is necessary to continue treatment of the underlying disease, another drug is prescribed that has bronchodilatory and mucolytic properties, but has slightly different characteristics. The dosage of the drug is also adjusted.
5. Since severe hypokalemia may develop while taking Salbutamol, regular monitoring of the quantitative component of potassium in the blood serum is necessary.
   

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Interactions with other drugs

Some people do not even think about it when, against the background of one treatment, they begin to take drugs of a different pharmacological orientation. For example, we treat bronchitis, the stomach has seized up, the person, without thinking, begins to independently drink drugs for gastric pathology. And then they begin to be surprised that other pathological symptoms appear or the therapeutic effectiveness is weak.

Therefore, before prescribing a specific drug, it is necessary to know the interactions of Salbutamol with other drugs in order to prevent the development of additional pathological symptoms.

Non-cardioselective beta-blockers, the pharmacodynamics of which are aimed at relieving angina, when taken in parallel with the drug in question act in a mutually suppressive manner, that is, when they are administered together, the expected therapeutic effectiveness in the treatment of either disease does not occur.

The simultaneous use of Salbutamol and theophylline leads to an increased likelihood of developing such negative manifestations as irregular heart rhythm and increased heart rate.

If glucocorticosteroids and Salbutamol are present in parallel in one treatment protocol, hypokalemia can be expected to develop. A similar result is obtained with the combined administration of the drug in question with diuretics, i.e. their combined use can lead to a sharp drop in the potassium level in the patient's blood.

Considering that the drug prescribed for the relief of bronchial spasm has an irritating effect on the sympathetic nervous system, patients whose medical history is burdened with epileptic seizures, damage to the optic nerve (glaucoma), pathological changes affecting the cardiovascular system, as well as hyperthyroidism (endocrinological syndrome caused by hyperfunction of the thyroid gland), against the background of the main treatment, should be especially careful when prescribing the method of administration and dosage of Salbutamol.

It should also be noted that if taking the drug in question does not bring the expected result or its effect lasts less than three hours, in such a situation it is necessary to inform your doctor.

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Storage conditions

When purchasing this medicine, it is necessary to pay attention to the storage conditions of Salbutamol, at home. After all, the quality of the preserved pharmacological properties, which must correspond to the properties attached to it throughout the therapeutic period, depends on how strictly the recommendations given in the instructions attached to the drug are followed.

There are several such recommendations:

1. The medicine must be stored in a cool place where the room temperature does not exceed +25 °C.
2. The room where Salbutamol is stored must be dry.
3. The storage location should not be exposed to direct sunlight.
4. Throughout the entire operational period, it is necessary to protect the aerosol can (for aerosol administration of the drug) from falling and from deformation of the packaging.
5. The drug should not be accessible to small children.

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Shelf life

After purchasing a medicinal product, you should definitely familiarize yourself with the production dates of the medicine and especially pay attention to the final effective use date, which must be reflected on the packaging of any product. If this date has expired, the medicine in question should not be used in the future. The shelf life of the Salbutamol in question, depending on the manufacturer who released this drug on the pharmaceutical market, can be from one and a half to four years.

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