Pharmacological properties of the drug Salbutamol
Salbutamol is a selective β2-adrenergic receptor agonist. Stimulates mainly β2-adrenergic receptors localized in the bronchi, myometrium, and blood vessels. When administered by inhalation, it acts mainly on β2-adrenergic receptors of the bronchi, with little effect on β2-adrenergic receptors of other localizations. Has a pronounced bronchodilator effect. By causing dilation of the bronchi, it relieves and prevents bronchospasm. Has virtually no effect on β1-adrenergic receptors of the heart. Prevents the release of allergy and inflammatory mediators (histamine, SRSA) from mast cells. Improves mucociliary clearance. The effect of the drug develops quickly and lasts 3–4 hours. After inhalation, approximately 10–20% of the active substance reaches the small bronchi, the rest settles in the upper respiratory tract. Plasma protein binding is 10%. Salbutamol is metabolized in the liver. It is excreted mainly in the urine unchanged and as an inactive metabolite. Most of the dose of salbutamol administered by inhalation or taken orally is eliminated within 72 hours.
Salbutamol 100 mcg/dose 200 doses 10 ml aerosol doses.
APPROVED by the Order of the Chairman of the Committee for Control of Medical and Pharmaceutical Activities of the Ministry of Health and Social Development of the Republic of Kazakhstan dated "____" ___________20, No. _________ Instructions for the medical use of the drug Salbutamol Trade name Salbutamol International nonproprietary name Salbutamol Dosage form Aerosol for inhalation, dosed, 100 mcg/ dose, 200 doses Composition One dose contains the active substance - salbutamol sulfate 120.5 mcg (equivalent to salbutamol 100 mcg), excipient - 1,1,1,2-tetrafluoroethane (HFA-134a propellant), ozone-safe. Description Homogeneous suspension of white or almost white color. Pharmacotherapeutic group Drugs for the treatment of obstructive respiratory diseases. Inhalation sympathomimetics. Beta2-agonists are selective. Salbutamol. ATX code R03AC02 Pharmacological properties Pharmacokinetics When using an aerosol, 10 to 20% of the dose taken reaches the lower respiratory tract, where it is adsorbed by the lung tissue and penetrates the pulmonary vessels, but is not metabolized here. The remaining part remains in the delivery device or settles in the oropharynx with further ingestion of the drug. Maximum plasma concentrations are reached after 2-4 hours. Plasma protein binding is 10%. When thresholds are reached by the circulatory system, salbutamol is metabolized through the hepatic mechanism and is excreted primarily in the urine as unchanged product and phenol sulfate. Salbutamol is metabolized during the first passage through the liver and, due to the ingestion of small quantities during inhalation, in the intestinal wall; the main metabolite is an inactive sulfate conjugate, which is excreted in the urine. T½ of salbutamol when administered intravenously is 4-6 hours. Salbutamol is rapidly excreted in the urine as an inactive metabolite 4'-O-sulfate and unchanged substance; excreted in small quantities in feces. Most of the salbutamol taken is eliminated from the body within 72 hours. Salbutamol does not cross the blood-brain barrier. Pharmacodynamics Salbutamol is a selective β2-adrenergic receptor agonist. In therapeutic doses, it stimulates β2-adrenergic receptors of the bronchial muscles, providing a bronchodilator effect. Salbutamol has a short duration of action (4 to 6 hours) and a rapid onset of action (about 5 minutes from the moment of application). In recommended therapeutic doses, it does not have a negative effect on the cardiovascular system and does not cause an increase in blood pressure. Children: Clinical studies conducted in children under 4 years of age have demonstrated a similar safety profile compared to older children, adolescents and adults. Indications for use: relief and prevention of the development of bronchospasm in patients with reversible airway obstruction (asthma, chronic bronchitis, emphysema) - to relieve the symptoms of an attack of bronchial asthma or to prevent them before contact with a known trigger (allergen). Bronchodilators should not be the only or main component of asthma therapy. If a patient with asthma does not respond to salbutamol therapy, inhaled corticosteroids are recommended to achieve and maintain symptom control. Insufficient response to salbutamol therapy may be a signal for urgent medical intervention/therapy. Method of administration and dose Salbutamol in the form of an aerosol is used only for inhalation by inhaling the aerosol through the mouth. An increased need for β2-agonists may indicate a worsening of asthma. In such cases, it is recommended to re-evaluate the therapy and consider the possibility of additional administration of GCS. Due to the risk of adverse reactions if recommended doses are exceeded, the frequency of administration and doses used should be increased only as directed by a doctor. The duration of action of the drug Salbutamol in most patients is 4-6 hours. Persons who have difficulty coordinating inhalation and release of the drug from the inhaler can use the drug Salbutamol using a device in the form of a spacer. The need to take the drug should not exceed 4 times a day (800 mg). A sudden increase in the need for the drug indicates a worsening of asthma. For children under 4 years of age, Salbutamol is administered through a spacer. Relief of an acute attack of bronchospasm Adults: from 100 mcg to 200 mcg of Salbutamol once. Children: 100 mcg once. If necessary, the dose can be increased to 200 mcg. Prevention of exercise-induced bronchospasm or allergic etiology Adults: 200 mcg before exercise or expected allergen exposure Children: 100 mcg before exercise or expected allergen exposure. If necessary, the dose can be increased to 200 mcg. Long-term maintenance therapy Adults and children 100-200 mcg of the drug 4 times a day. The duration of treatment is determined by the attending physician. Instructions for using the inhaler The effect of the drug may be weakened if the inhaler is cold. When the canister cools, it is recommended to remove it from the plastic case and warm it with your hands for a few minutes. The can cannot be disassembled, pierced or thrown into fire, even if it is empty. Checking the serviceability of the inhaler Before using the inhaler for the first time, you must carefully remove the cap from the mouthpiece, shake the inhaler vigorously and spray two doses of the drug into the air to make sure that the device is working properly. If the inhaler has not been used for 5 days or more, it should be shaken well and two doses of the drug sprayed into the air to ensure that it is working properly. Using the inhaler 1. Remove the protective cap from the mouthpiece of the inhaler. Check the inside and outside of the inhaler, including the mouthpiece, for cleanliness and dryness, and for any loose parts of the device. 2. Shake the inhaler vigorously to evenly mix the contents of the inhaler and to remove any loose parts from the surface of the device. 3. Place the inhaler vertically between your thumb and forefinger, placing your thumb on the base, below the mouthpiece. 4. Exhale deeply (as far as possible). Then place the mouthpiece between your teeth (without biting it) and wrap your lips tightly around it. 5. Take a deep breath through your mouth. While continuing to take a deep breath, press the top of the inhaler. 6. Hold your breath, remove the inhaler from your mouth and remove your index finger from the top of the inhaler. Continue to hold your breath as much as possible. 7. If you need to continue inhalation, you should wait approximately half a minute, holding the inhaler vertically, and then repeat steps 2 to 6. 8. After inhalation, carefully place the dust cap on the mouthpiece. Attention Take your time when performing the actions indicated in paragraphs 4, 5 and 6. It is important that the inhaler is pressed at the beginning of a calm, deep breath. To be sure that the inhalation is performed correctly, you must first control the method of taking the medicine in front of a mirror. A “haze” appearing from the inhaler, lips or nose during inhalation indicates an incorrect inhalation technique and it is necessary to practice using the inhaler again, starting from point 2. If your doctor has given you any other recommendations for using the drug, follow your doctor's recommendations. Tell your doctor about any difficulties you have with taking the drug. Cleaning the inhaler The inhaler should be cleaned at least once a week. 1. Remove the metal container from the plastic body of the inhaler and remove the mouthpiece cover. 2. Rinse the sprayer with warm running water. 3. Dry the sprayer thoroughly inside and out. 4. Place the container and mouthpiece cover back into place. DO NOT IMMERSE THE METAL CONTAINER INTO WATER. Side effects Very often (>1/10), often (>1/100, <1/10), infrequently (>1/1,000, <1/100), rarely (>1/10,000, <1/1,000), very rare (<1/10,000). Often - tremor, headache - tachycardia Uncommon - irritation of the mucous membrane of the mouth and pharynx - palpitations - muscle cramps Rarely - hypokalemia (therapy with β2-agonists can lead to severe hypokalemia) - dilation of peripheral vessels Very rarely - hypersensitivity reactions, including urticaria, angioedema, bronchospasm, hypotension, collapse - paradoxical bronchospasm - lactic acidosis (in patients receiving salbutamol by intravenous injection and nebulizer for the treatment of exacerbations of bronchial asthma) - hyperactivity - arrhythmia, including atrial fibrillation, supraventricular tachycardia and extrasystole Providing data on suspected side effects reactions of the drug is a very important point, allowing for continuous monitoring of the risk/benefit ratio of the drug. Health care professionals should provide information about any suspected adverse reactions to the contacts listed at the end of the prescribing information and through the national reporting system. Contraindications - hypersensitivity to any component of the drug - premature labor - threatened abortion Forms of salbutamol not intended for intravenous administration should not be used to terminate premature labor and threatened miscarriage. Drug interactions It is not recommended to simultaneously use the drug Salbutamol and non-selective beta-adrenergic receptor blockers, such as propranolol. Salbutamol is not contraindicated in patients receiving monoamine oxidase inhibitors (MAOIs). Special instructions For children under 4 years of age, Salbutamol is administered through a spacer. Treatment of asthma is usually done in stages, with the patient's response monitored clinically and with pulmonary function tests. An increased need for β2-agonists may indicate worsening asthma control. In such cases, the patient's treatment plan should be reconsidered. A sudden and progressive deterioration of bronchial asthma can pose a threat to the patient's life, so in such situations it is necessary to urgently decide on the issue of prescribing or increasing the dose of glucocorticosteroids. In such patients, daily monitoring of peak expiratory flow is recommended. The drug should be used with caution in patients with thyrotoxicosis, heart failure, myocardial ischemia, tachyarrhythmia, hypertrophic cardiomyopathy. Patients with cardiovascular diseases, including a history of, for example, coronary heart disease, arrhythmia or severe heart failure, when prescribed salbutamol, should be warned that they must consult a doctor in the event of chest pain or other symptoms of exacerbation of cardiovascular disease. vascular disease. Symptoms such as shortness of breath and chest pain should be carefully assessed as they may be due to both cardiovascular and bronchopulmonary dysfunction. Therapy with β2-adrenergic agonists, especially when administered parenterally or via nebulizer, can lead to hypokalemia. Particular caution is recommended when treating severe attacks of bronchial asthma, since in these cases hypokalemia may increase as a result of the simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics, as well as due to hypoxia. In such situations, it is necessary to monitor the level of potassium in the blood serum. As is the case with the use of other inhaled drugs, the development of paradoxical bronchospasm is possible as a result of the occurrence of a spasm immediately after dosing. If paradoxical bronchospasm occurs, immediate relief is required using an alternative drug or a fast-acting inhaled bronchodilator from a different pharmacological group. You should immediately stop treatment with this form of Salbutamol, and, if necessary, prescribe other fast-acting bronchodilators for further use. If the effect of the usual dose of Salbutamol becomes less effective or shorter lasting (the effect of the drug should last at least 3 hours), the patient should consult a doctor. The physician must ensure that the patient is using the inhaler correctly and that there is timing between actuation and inhalation for optimal delivery of the drug to the lungs. Salbutamol should be used with caution in patients who have already taken high doses of other sympathomimetics. Like other beta-adrenergic agonists, salbutamol can cause reversible metabolic changes, such as an increase in blood glucose concentrations. Patients with diabetes may develop decompensation, and in some cases, the development of ketoacidosis. Concomitant use of glucocorticosteroids may enhance this effect. When used intravenously, as well as when using a nebulizer solution of short-acting beta-agonists, very rare cases of lactic acidosis associated with high therapeutic doses in patients with exacerbation of bronchial asthma have been described. Increased lactate levels lead to shortness of breath and compensatory hyperventilation, which can be misinterpreted as symptoms of improperly treated asthma. This may lead to erroneous increases in doses of short-acting beta-agonists, so monitoring for increased serum lactate and therefore metabolic acidosis is recommended. Fertility There is no data on the effect of the drug on fertility in humans. The drug does not have a negative effect on the fertility of animals. Pregnancy and lactation The use of the drug during pregnancy and lactation is justified only if the expected benefit to the mother outweighs the risk to the fetus/infant. Salbutamol is likely excreted in breast milk. In some studies, polydactyly and cleft palate were identified in children when mothers took drugs during pregnancy, including salbutamol (a clear causal relationship between their occurrence and drug use has not been established), and therefore the risk is estimated at 2-3%. Experimental studies revealed the presence of a teratogenic effect of salbutamol: in mice with subcutaneous administration (doses 11.5-115 times higher than the maximum recommended in humans for inhalation administration), the development of a “cleft palate” was noted; in rabbits when administered orally (doses 2315 times higher than the maximum for inhalation administration) – non-fusion of the skull bones. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms Considering the possible side effects, care must be taken when driving a vehicle and potentially dangerous mechanisms. Overdose Symptoms: Most symptoms of salbutamol overdose are transient adverse reactions of beta-agonists. In case of overdose, hypokalemia may develop, and therefore monitoring of potassium levels in the blood serum is necessary. When using high therapeutic doses and overdose with short-acting beta-agonists, the development of lactic acidosis was detected. Treatment: the use of large doses of salbutamol can cause hypokalemia, therefore, if overdose is suspected, serum potassium levels should be monitored. Monitoring of lactate levels and the subsequent development of metabolic acidosis is necessary (especially in the presence or worsening of tachypnea despite the elimination of bronchospasm). Release form and packaging Aerosol for inhalation, dosed, 100 mcg/dose, 200 doses. 200 doses are placed in an aluminum container equipped with a dosing valve, a spray nozzle and a protective cap. 1 cylinder, along with instructions for medical use in the state and Russian languages, is placed in a cardboard pack. Storage conditions Store at a temperature not exceeding 30 ºС. Protect from light and hypothermia. Keep out of the reach of children! Shelf life: 2 years Do not use after expiration date. Conditions for dispensing from pharmacies By prescription Manufacturer Glaxo Wellcome Production, France Zone Idustrelle n`2, 23 rue Lavoisier, 27000 EVREUX Packer Glaxo Wellcome Production, France Zone Idustrelle n`2, 23 rue Lavoisier, 27000 EVREUX Registration certificate holder Laboratories GlaxoSmithKline, France 100 , rout de Versailles 78163 MARLY-LE-ROI Cedex Address of the organization that accepts claims from consumers on the quality of products (products) in the territory of the Republic of Kazakhstan Representative office of GlaxoSmithKline Export Ltd. in Kazakhstan 050059, Almaty, Furmanov St., 273 Telephone number, Number Fax: + Email address
Indications for use of the drug Salbutamol
BA (prevention and relief of attacks), chronic obstructive bronchitis, emphysema and other diseases that occur with bronchospasm. As a tocolytic agent, it is indicated for the threat of premature birth, isthmic-cervical insufficiency, a decrease in the fetal pulse depending on uterine contractions during periods of cervical dilatation and expulsion, for prophylactic purposes - during operations on the pregnant uterus (application of a circular suture for insufficiency of the internal uterine pharynx) .
Use of the drug Salbutamol
Inhalation - adults and children over 4 years of age are prescribed 0.1 mg of salbutamol for inhalation to eliminate bronchial obstruction. If the attack does not stop within 5–10 minutes after the first inhalation, inhalation can be repeated. For preventive purposes, 0.1 mg of salbutamol is also recommended to be administered by inhalation 10–15 minutes before possible contact with the suspected allergen. With long-term use of salbutamol, use 1-2 inhalations (0.1 mg) 3-4 times a day with an interval of at least 3 hours. Long-term use of salbutamol for COPD or asthma is carried out only against the background of basic therapy. Do not use more than 10 doses (1 mg of salbutamol) per day. Orally, adults are usually prescribed 0.002 g 3-4 times a day. As a tocolytic agent to eliminate the threat of premature birth, as well as after operations on the pregnant uterus, it is administered intravenously in a dose of 5 mg in 400–500 ml of isotonic solution or 5% glucose solution at a rate of 15–20 drops (starting from 5 drops) per minute. The infusion rate is adjusted taking into account the intensity of uterine contractions and tolerance (heart rate and other hemodynamic indicators are monitored). Duration of administration: 6–12 hours.
Salbutamol Sopharma syrup 2mg/5ml 125ml No.1
Name
Salbutamol.
Description
Salbutamol Sopharma syrup is a drug from the group of so-called bronchodilators. It provides short-term (4-6 hours) bronchodilation, relaxing the smooth muscles of the bronchi, and promotes the expansion of the airways, relieving tension in the chest, wheezing, and facilitating breathing. Used to ease breathing and prevent asthma and other lung diseases; is acceptable for use in children and adults who are unable to use inhalants.
Contraindications
- if you are allergic (hypersensitivity) to the active substance or to any of the excipients of Salbutamol Sopharma;
- Salbutamol Sopharma syrup should not be used to stop uncomplicated premature labor or in cases of threatened miscarriage.
Precautionary measures
The drug Salbutamol Sopharma is not used alone or as a primary treatment for the treatment of severe or unstable asthma; not used to relieve asthmatic attacks. Tell your doctor if you have:
- disease of the thyroid gland associated with an increase in its function;
- heart disease, and especially those associated with heart rhythm disturbances or angina pectoris (chest pain);
- treatment with other sympathomimetics;
- diabetes.
Salbutamol Sopharma contains ethanol, sucrose, methyl and propyl parahydroxybenzoate. This medicine contains 3.84 vol. % ethanol, i.e. up to 0.155 g of alcohol in a dose of 5 ml, which is equivalent to 3.84 ml of beer and 1.6 ml of wine. The use of the drug in pregnant and breastfeeding women, children and risk groups such as patients with liver disease, epilepsy and alcoholism should be taken into account. The medicine contains 37.5 g of sucrose. Each 5 ml dose delivers up to 1.5 g of sucrose. If you have been told by your doctor that you have an intolerance to certain sugars, consult your doctor before using this medicine. The syrup contains methyl and propyl parahydroxybenzoate, which may cause allergic reactions (possibly delayed).
Interaction with other drugs
Tell your doctor or pharmacist if you are taking, have recently taken or may take any other medicines, including those taken without a prescription. Tell your doctor if you are taking beta blockers (such as propranolol).
Pregnancy and breastfeeding
If you are pregnant or breastfeeding, think you may be pregnant, or are planning to become pregnant, ask your doctor or pharmacist for advice before using this medicine. The use of Salbutamol Sopharma in pregnant women is not recommended due to the lack of sufficient data on the safe use of the drug in this category of patients. If you are breastfeeding and treatment with the drug is required, breastfeeding should be discontinued.
Directions for use and doses
Always take Salbutamol Sopharma exactly as prescribed by your doctor. If you are unsure about anything, ask your doctor or pharmacist. The syrup is taken orally regardless of meals. The usual dose is: Adults: 5-10 ml syrup (2-4 mg salbutamol) 3-4 times a day. If necessary, the dose can be increased to 20 ml (8 mg) 4 times a day (maximum daily dose 32 mg). Elderly patients: it is recommended to start treatment with lower doses - 5 ml of syrup (2 mg) 3-4 times a day. Use in children and adolescents Children from 2 to 6 years of age: initial dose – 2.5 ml of syrup (1 mg) 3 times a day. If necessary, the dose can be increased to 5 ml of syrup (2 mg) 3-4 times a day. Children 6-12 years of age: the minimum initial dose is 2 mg (5 ml syrup) 3 times a day. If necessary, the frequency of taking the drug can be increased up to 4 times. Children over 12 years of age: 5-10 ml of syrup (2-4 mg of salbutamol) 3-4 times a day. Children under 2 years of age: The safety, effectiveness and dosage of the drug in children under 2 years of age have not been established. If during treatment you do not feel the effect of drug treatment or there is a need for more frequent use, you should immediately contact your doctor. He will assess your condition and possibly reconsider your treatment. You should not change the dosage of the drug yourself without consulting your doctor! If you take a dose that exceeds the required dose, you may experience trembling of the limbs, increased heart rate, hyperactivity, nausea, vomiting, increased blood sugar, especially in children, decreased amount of potassium in the blood , rapid breathing. Seek advice from your healthcare professional immediately. If you miss a dose of Salbutamol Sopharma If you miss one dose, take it as soon as possible. If it is almost time for your next dose, take it as usual, skipping the forgotten dose. Do not take a double dose to make up for a missed dose. If you have any additional questions about using this medicine, ask your doctor or pharmacist.
Side effect
Like all medicines, Salbutamol Sopharma can cause side effects, although not everyone gets them. Very common (affects more than 1 in 10 patients): tremor (trembling of the limbs). Common (occurs in less than 1 in 10 patients): headache, increased heart rate, palpitations, muscle cramps. Rare (affects less than 1 in 1,000 patients): irregular heart rhythm, dilation of blood vessels in the extremities, decreased amount of potassium in the blood. Very rare (affects less than 1 in 10,000 patients): allergic reactions such as hives, angioedema (swelling of the face, lips, mouth, tongue or throat, which can make swallowing and breathing difficult), airway spasms, decreased blood pressure and collapse, hyperactivity, feeling of muscle tension. With unknown frequency (no estimate can be made from existing data). Although it is not known to what extent or how often it occurs, some patients may experience chest pain (due to cardiac problems). Notify your doctor if you experience any of the symptoms described during treatment with Salbutamol Sopharma, but do not stop using the medicine without the direction and recommendation of your doctor. If any of the side effects become serious or you notice other side effects not described in this leaflet, notify your doctor or pharmacist.
Storage conditions
Store in original packaging at a temperature not exceeding 25 °C. Keep out of the reach of children. The syrup can be used up to 1 month after opening the bottle.
Best before date
2 years. Do not use Salbutamol Sopharma after the expiration date stated on the package. The expiration date corresponds to the last day of the specified month. Medicines should not be disposed of in a sewer or household waste container. Ask your pharmacist how to dispose of your unused medications. These measures will contribute to environmental protection.
Conditions for dispensing from a pharmacy chain
On prescription.
Compound
5 ml of syrup contains: Active substance: 2 mg of salbutamol (in the form of salbutamol sulfate). Excipients: ethanol, sucrose, methyl parahydroxybenzoate (E218), propyl parahydroxybenzoate (E216), sodium citrate dihydrate, citric acid monohydrate, liquid essence “Lemon”, purified water.
Package
Transparent viscous liquid from colorless to yellow with a specific lemon odor. 125 ml of syrup in dark brown glass bottles with polyethylene caps or in dark brown polyethylene terephthalate (PET) bottles with polyethylene caps; 1 (one) bottle in a cardboard box along with a measuring cup and a leaflet.
Buy Salbutamol Sopharma syrup 2 mg/5 ml in bottle 125 ml in pack No. 1 in the pharmacy
Price for Salbutamol Sopharma syrup 2 mg/5 ml in bottle 125 ml in pack No. 1
Instructions for use for Salbutamol Sopharma syrup 2mg/5ml in bottle 125ml in pack No. 1
Special instructions for the use of the drug Salbutamol
Use with extreme caution in case of hypersensitivity to sympathomimetics, severe heart disease (chronic ischemic heart disease, acute myocardial infarction, hypertrophic obstructive cardiomyopathy, rhythm disturbances), hyperthyroidism, unstable diabetes mellitus, pheochromocytoma. During pregnancy, it can be used only for health reasons. Since salbutamol passes into breast milk, its use during breastfeeding is possible only if the expected therapeutic effect for the mother outweighs the potential risk for the child. The use of salbutamol in high doses may worsen the reaction when driving a car or operating machinery. This effect is enhanced by simultaneous use of alcohol and tranquilizers.
