Use:
1, which is used to treat bronchospasm caused by asthmatic bronchitis, bronchial asthma and emphysema, is prepared by chloromethylation, esterification, bromination, amination, hydrolysis, neutralization and hydrogenation of p-hydroxyacetophenone.
2. It is used as lean meat in modern pork breeding to improve the lean meat rate of pigs. Since 2002, it has been listed as a banned drug in aquaculture and may not be added in livestock and poultry breeding.
3. Clinically, obstetrics and gynecology are traditionally used to treat premature delivery, but it is not recorded in the drug instructions.
4, drug interaction:
1 combined with other adrenergic receptor agonists may increase its effects and aggravate its adverse reactions.
2. When theophylline is used together, it can increase the effect of relaxing bronchial smooth muscle. It may also increase adverse reactions.
3. The bronchodilatory effect of this product can be antagonized by propranolol, a β -receptor blocker, so it is not suitable to be used with propranolol.
The correct statement of salbutamol is that salbutamol is a short-acting β2 adrenergic receptor agonist. Used as an antiasthmatic drug, it can effectively inhibit the release of allergic substances such as histamine and prevent bronchospasm. Adding a small amount of salbutamol to livestock feed can increase lean meat and meat exchange rate and reduce fat, and its toxicity is much higher than that of ractopamine with the same function.
Introduction catalogue of salbutamol
1 pinyin 2 English reference 3 national essential drugs 4 overview 5 salbutamol pharmacopoeia standard
5. 1 name
5. 1. 1 Chinese name 5. 1.2 Chinese Pinyin 5. 1.3 English name
5.2 structural formula 5.3 molecular formula and molecular weight 5.4 source (name) and content (valence) 5.5 characters
5.5. 1 melting point 5.5.2 optical rotation
5.6 Identification 5.7 Inspection
5.7. Color of1ethanol solution 5.7.2 Salbutamol 5.7.3 Related substances 5.7.4 loss on drying 5.7.5 residue on ignition 5.7.6 Boron.
5.8 Content Determination 5.9 Category 5. 10 Storage 5. 1 1 Preparation 5. 12 Version.
6 salbutamol instructions
6. 1 drug name 6.2 English name 6.3 alias of salbutamol 6.4 classification 6.5 dosage form 6.6 pharmacological action of salbutamol 6.7 pharmacokinetics 6.8 indications of salbutamol 6.9 contraindications of salbutamol 6. 10 Precautions 6.1kloc-0/adverse reactions of salbutamol 6.65444
7 salbutamol poisoning
7. 1 clinical manifestations 7.2 diagnosis 7.3 treatment
Eight references are attached:
* Other versions of the drug instructions related to salbutamol.
1 Pinyin
When spring is blooming.
2 English reference
Salbutamol [Xiangya Medical Dictionary]
Salbutamol, Provence, Vantorin [Landau Chinese-English Dictionary]
3 National essential drugs
National retail guidance price information of salbutamol-related essential drugs
Essential drug serial number
DirectoryNo. Drug name, dosage form and specification Retail unit refers to
Price Category Description 754 107 Salbutamol Aerosol 140ug*200 (Solution Type) Branch 7 Chemicals and Biological Products * 755 107 Salbutamol Aerosol 100ug*200 (Suspension Type) Branch 23.8 Chemicals and Biological Products.
note:
1, and those marked with "*" in the remarks column in the table are representative products.
2. If "△" is marked in the remarks column for the specifications representing dosage forms in the table, the prices representing dosage forms and related specifications with a clear price difference are tentative prices.
4 Overview
Salbutamol is a β2 adrenergic receptor agonist with white crystalline powder. Odorless, almost tasteless. Its bronchodilating effect is equivalent to isoproterenol, and its effect lasts for a long time. The effect of increasing heart rate is only110 of isoproterenol. Can be used for treating bronchospasm of patients with bronchial asthma, asthmatic bronchitis and emphysema, and can be administered by oral administration or atomized inhalation.
5 Salbutamol Pharmacopoeia Standard 5. 1 Name 5. 1. 1 Chinese Name
Shuchuanning
5. 1.2 Chinese Pinyin
Sha Ding An Chun
5. 1.3 English name
Shuchuanning
5.2 structural formula
5.3 Molecular Formula and Molecular Weight
c 13h 2 1no 3 239.3 1
5.4 Source (Name) and Content (Titration)
This product is 1(4 hydroxy 3 hydroxymethylphenyl) 2 (tert-butylamino) ethanol. The content of C 13H2 1NO3 should be no less than 98.5% in terms of dry products.
5.5 characteristics
This product is white crystalline powder; Odorless, almost tasteless.
This product is soluble in ethanol, slightly soluble in water and insoluble in ether.
5.5. 1 melting point
The melting point of this product (appendix ⅵ C of Pharmacopoeia II of 20 10 version) is 154 ~ 158℃, and it decomposes at the same time when melting.
Optical rotation
Take about 0.50g of this product, weigh it accurately, put it in a 25ml volumetric flask, add methanol to dissolve and dilute it to scale, shake it evenly, and determine it according to law (Appendix VI E of Pharmacopoeia II, 20 10 Edition). Optical rotation should be 0. 10 to +0. 10.
5.6 Identification
(1) Take about 20mg of this product, add 2ml of water to dissolve it, add 2 drops of ferric chloride test solution, shake well until the solution turns purple, and add sodium bicarbonate test solution until the solution turns orange-red.
(2) Take this product, add 0. 1mol/L hydrochloric acid solution to make a solution containing about 0.08mg per 1ml, and determine it by UV-Vis spectrophotometry (Appendix IV A of Pharmacopoeia Part II, 20 10), and it has the maximum absorption at the wavelength of 276nm.
(3) The infrared absorption spectrum of this product should be consistent with the reference substance (Appendix Ⅳ c of Pharmacopoeia II, 20 10).
5.7 Check the color of 5.7. 1 ethanol solution.
Take 0.40g of this product, add 10ml anhydrous ethanol, and heat it in a warm water bath to dissolve it. If the color development is compared with the colorimetric solution with the same volume (take 0.5ml of yellow stock solution and add 10 ml of absolute ethanol) (the first method in appendix ⅸ A of Pharmacopoeia II, 20 10 edition), it shall not be deeper.
salbutamol
Take 50.0mg of this product, weigh it accurately, put it in a 25ml volumetric flask, add 0.0 1mol/L hydrochloric acid solution to dissolve and dilute it to scale, shake it evenly, and measure the absorbance at the wavelength of 3 10nm according to ultraviolet-visible spectrophotometry (Appendix IV A of Pharmacopoeia Part II, 20 10), which shall not be greater than 0.
Related substances
Take an appropriate amount of this product, add mobile phase to dissolve and dilute it, and make a solution containing about 2mg per 1ml as the test solution; Accurately measure 1ml, put it in a 100ml volumetric flask, dilute it to scale with mobile phase, and shake it evenly as a control solution. In addition, a proper amount of terbutaline sulfate reference substance and salbutamol reference substance were added to the mobile phase for dissolution and dilution, and the solution containing about 0.2mg each in 1ml was prepared as the system adaptability test solution. According to the test of high performance liquid chromatography (Pharmacopoeia 20 10, Appendix V D), octyl silane bonded silica gel was used as filler. Sodium heptane sulfonate solution [2.87g sodium heptane sulfonate and 2.5g potassium dihydrogen phosphate are dissolved and diluted to 1000ml with water, and the pH value is adjusted to 3.65 with phosphoric acid solution (1→2)]-acetonitrile (78: 22) as the mobile phase; The detection wavelength is 220 nm. The resolution of salbutamol peak and terbutaline sulfate peak should meet the requirements. Take 20μl of control solution, inject it into the liquid chromatograph, and adjust the detection sensitivity so that the peak height of the chromatographic peak of the principal component is about 25% of the full scale. Accurately measure 20μl of test solution and reference solution (injected within 12 hours after preparation), and inject them into the liquid chromatograph respectively, and record the chromatogram until the retention time of the principal component peak reaches 25 times. If there are impurity peaks in the chromatogram of the test sample, the area of a single impurity peak shall not be greater than 0.3 times (0.3%) of the main peak area of the reference sample, and the sum of impurity peak areas shall not be greater than the main peak area of the reference sample (1.0%). Any peak less than 0.05 times the main peak area of the control solution in the chromatogram of the test solution will be ignored.
Drying loss
Take this product and dry it at 105℃ to constant weight, and the weight loss shall not exceed 0.5% (Appendix VIII L of Pharmacopoeia II, 20 10).
Ignition residue
It shall not exceed 0. 1% (Appendix VIII N of Pharmacopoeia II, 20 10).
boron
Take 50mg of this product, add 5ml of carbonate solution (dissolve anhydrous sodium carbonate1.3g and potassium carbonate1.7g in water to make100ml), evaporate in water bath, dry at 120℃, and then quickly ignite for organic destruction. After the destruction, let them cool, and add 0.5 ml of water and 0.655 ml of newly made water. Dissolve the residue at low temperature, cool, add 3 ml of sulfuric acid-glacial acetic acid solution (1: 1), mix well, let stand for 30 minutes, transfer to 100ml volumetric flask, dilute with ethanol to scale, shake well, filter, take filtrate, and use ultraviolet-visible spectrophotometry (2065433). Take a proper amount of boric acid, dissolve it in water, dilute it quantitatively, and make a solution containing 5.72 micrograms per 1 ml, and accurately measure 2.5 ml, starting with "5 ml carbonate solution", and do the same operation. The absorbance of the test solution shall not be greater than that of the control solution (50 parts per million).
5.8 Content Determination
Take about 0.2g of this product, accurately weigh it, add 25ml glacial acetic acid to dissolve it, add 1 drop crystal violet indicator, titrate with perchloric acid titration solution (0. 1mol/L) until the solution is blue, and correct the titration result with blank test. Every 1ml perchloric acid titration solution (0. 1mol/L) is equivalent to 23.93mg c 13h 2 1no 3.
5.9 categories
β2 adrenergic receptor agonist.
5. 10 storage
Shading, sealing and storage.
5. 1 1 Prepare
Salbutamol aerosol
Version 5. 12
People's Republic of China (PRC) Pharmacopoeia 20 10 Edition
6 salbutamol instruction 6. 1 drug name
Shuchuanning
6.2 English name
Shuchuanning
6.3 Alias of salbutamol
Chuan Lening; Liu Ding ammonia alcohol; Hydroxymethyl tert-butyl epinephrine; Shu Chuanling; Cough must be done well; Sobamin; Elsa; Ai Naling; Quantization; Sam; Pingchuanling; Hydroxymethyl isobutyrate kidney; Salbutamol; Proventil saltanol; Shuchuanling
6.4 classification
Circulatory drugs, antiarrhythmic drugs, bradyarrhythmia drugs.
6.5 dosage form
1. The total weight of each bottle 18g, containing 20mg of salbutamol, can be sprayed for 200 times, with each spray of 0.1mg; ;
2. elsa aerosol: each aerosol contains 20mg of salbutamol. It can be sprayed for 200 times, with 0. 1mg each time. ;
3. Ainaline, sustained-release capsules: each capsule contains 4mg and 8 mg of salbutamol;
4. Salbutamol, aerosol: 0. 14%, each containing 28mg of salbutamol;
5. Quantining, controlled release tablets: each tablet contains 4mg and 8 mg of salbutamol sulfate;
6. Sam, pills: 2 mg, 4 mg each.
6.6 pharmacological action of salbutamol
It has high selectivity to β2 receptor of airway smooth muscle, enhanced resistance to catechol oxymethyltransferase and monoamine oxidase, prolonged action time and less excitability to heart. In vitro experiments, the drug selectivity index was obtained by comparing the required isointensity concentration of airway smooth muscle and myocardium. The highest value of salbutamol was 250, terbutaline was 138 and isoproterenol was 1.4. Through the observation of patients, the changes of forced expiratory volume (FEV 1) and heart rate between intravenous salbutamol and isoproterenol were compared. It was found that the low dose of salbutamol per minute of 0. 1μg/kg could significantly increase FEV 1, and the heart rate could be accelerated with the increase of dose, indicating that the selectivity was higher, while isoproterenol was superior.
6.7 Pharmacokinetics of Salbutamol
Salbutamol is not easily destroyed by sulfatase in digestive tract and catechol O-methyltransferase in tissue, so it is effective and lasts for a long time orally. Oral bioavailability is 30%, and it takes effect 15 ~ 30 min after administration. The peak time of blood drug concentration is 2 ~ 4 hours, and the action lasts for more than 6 hours. The elimination half-life is 2.7 ~ 5 hours. Healthy volunteers took salbutamol 8mg controlled-release tablets for many times, and 90% of the drugs were released at a stable rate of 0.8 mg/h, and the drugs were released continuously, thus avoiding the fluctuation of blood drug concentration. The drug release rate is not affected by acidity, gastrointestinal peristalsis and food quantity. When inhaling aerosol, most of the inhaled dose is swallowed and then absorbed by gastrointestinal tract. The bioavailability of aerosol is 10%, and it takes effect at 1 ~ 5 min after inhalation, and reaches the peak at1h. Most of salbutamol is metabolized in intestinal wall and liver, and less than 20% of the original drug enters the blood circulation. After oral administration or inhalation, 80% of salbutamol is excreted in urine within 3 days.
6.8 Indications of salbutamol
Used for various types of bronchial asthma and various bronchial and pulmonary diseases accompanied by bronchospasm; Obstetrics is used to prevent premature delivery, relieve placental vasospasm and increase placental blood flow. Used for bradyarrhythmia and heart failure, such as sinus bradycardia, sinus arrest, sinus atrial block and atrioventricular block.
6.9 Taboos of Salbutamol
People who are allergic to salbutamol are prohibited.
6. 10 preventive measures
1. Use with caution in patients with cardiovascular insufficiency, hypertension and hyperthyroidism and pregnant women; Sensitive person, a β -receptor stimulant, should be used with caution for the elderly.
2. When using, you should start with a small dose and gradually increase the dose.
3. Long-term use can produce tolerance.
4. Can't be used with beta receptor antagonists.
6. Adverse reactions of11salbutamol
The common adverse reaction is muscle tremor, which mainly occurs in the skeletal muscles of limbs, face and neck. Light people feel uncomfortable, and heavy people will affect their lives and work. Some patients have obvious muscle tremor at the beginning of medication, but it can be gradually reduced or disappeared with the extension of medication time. The reason of muscle tremor is that salbutamol stimulates the β2 receptor on the slow-contracting fibers of skeletal muscle, making them contract faster and stronger, and destroying the fusion between fast-contracting fibers and slow-contracting fibers. About 30% patients always have different degrees of muscle tremor when taking salbutamol orally. There are few adverse cardiac reactions during medication. 40 cases of oral salbutamol, the dose is several times to dozens of times the therapeutic dose. The only adverse cardiac reaction was ventricular tachycardia, no arrhythmia and no poisoning death. It can be seen that the safety of salbutamol is far greater than that of isoproterenol and ammonia tea. There is no need to monitor the blood drug concentration during medication. A few people can see nausea, headache, flushing and palpitation, which can also cause the increase of blood lactic acid, pyruvate and ketone body. Diabetic patients should pay attention to the possibility of ketosis or lactic acid poisoning when using it Excessive use or combination with glucocorticoid may cause hypokalemia, which may lead to arrhythmia. Potassium salt should be supplemented when necessary.
6. Usage and dosage of12 salbutamol
1. Acute or intermittent medication: 65438+ 0 ~ 2 sprays per inhalation; Maintenance or preventive medication: 2 sprays each time, 3 ~ 4 times a day; Prevention of exercise-induced asthma: Inhale 2 sprays before exercise. Children's dose is halved.
2. Asthma aerosol: the usage and dosage are the same as above.
3. Chuanlening tablets: 2 ~ 4 mg for adults, 3 ~ 4 times a day. Children aged 2 ~ 6 years, each time1~ 2 mg; 6 ~ 12 years old, 2mg each time, 3 ~ 4 times a day; /kloc-People over 0/2 years old are adults.
4. Long-acting Chuanlening (Chuantening): 8mg each time, every 12 hours 1 time.
5. Chuanlening injection: subcutaneous or intramuscular injection for adults: 500μ g each time; Intravenous injection: 250μg slow injection, used for asthma status quo.
6. Chuanlening atomized solution: 0.5 ~2ml spray or intermittent positive pressure inhalation.
7. Shuchuanling tablets: 2.4 ~ 4.8 mg each time, 3 ~ 4 times a day. When used in obstetrics, it should be used alternately with other antispasmodic drugs. 1 week is 1 course of treatment, and can be used repeatedly at intervals of 1 week. Oral administration: 2.4mg each time, 3 ~ 4 times a day.
6. 13 drug interaction
Beta receptor antagonists such as propranolol can antagonize the bronchodilatory effect of salbutamol, so it is not suitable to use them together. When combined with glucocorticoid, it may cause hypokalemia, which may lead to arrhythmia. Potassium salt should be supplemented when necessary. When other adrenergic receptor agonists are used at the same time, their effects can be enhanced and the adverse reactions may be aggravated. The combination of tea and medicine can enhance the relaxation effect of salbutamol on bronchial smooth muscle, and the adverse reactions may also be enhanced.
6. 14 Expert opinion
Salbutamol is a β 1 receptor agonist, which has been used in clinic for a long time and its curative effect has been widely confirmed. Convenient administration, low local toxicity, good safety and definite curative effect. The compound preparation composed of salbutamol and tranilast can not only exert the rapid antiasthmatic effect of salbutamol, but also exert the antiallergic effect of tranilast, and can also prevent the drug resistance of salbutamol after long-term administration. The compound tranilast capsule composed of them is superior to salbutamol in the effective rate, improvement of symptoms and signs, improvement of lung function and antiallergic effect of asthma, with low adverse reaction rate and no adverse reaction to blood pressure, heart rate, hematopoietic function, liver and kidney function and heart. In addition, it can reduce the pressure of uterine muscles, relax the uterus, inhibit uterine contraction, and use pregnancy to prevent threatened abortion. It has obvious function of relaxing bronchial smooth muscle, and is commonly used in clinical treatment of bronchial asthma, chronic bronchitis and emphysema. It can also relax uterine smooth muscle by exciting β receptor, thus playing a role in protecting the fetus. In addition, the effect of β 1 receptor is weak, and the effect of increasing heart rate is only 1/2 of isoproterenol, so it is also used as an anti-bradycardia drug in clinic.
7 salbutamol poisoning
The bronchodilating effect of salbutamol (salbutamol, salbutamol, hydroxymethyl tert-butyl epinephrine) is similar to that of isoproterenol and lasts for a long time. The effect of increasing heart rate is only110 of isoproterenol. Can be used for treating bronchospasm of patients with bronchial asthma, asthmatic bronchitis and emphysema, and can be administered by oral administration or atomized inhalation. The oral bioavailability is about 30%, the onset time is 65 0.5 ~ 30 minutes, and the maintenance time is more than 6 hours. The bioavailability of atomized inhalation is about 10%, which takes effect in 1 ~ 5 minutes and lasts for 4 ~ 6 hours. [ 1]
7. Clinical manifestations of1
[ 1]
1. Common adverse reactions during treatment include finger tremor, nausea, headache, dizziness, increased heart rate or blood pressure fluctuation. Less common adverse reactions are dizziness, dizziness and dry mouth and throat.
2. Precursor manifestations of overdose: chest pain, dizziness, persistent severe headache, severe hypertension, persistent nausea and vomiting, sustained rapid heart rate or strong heartbeat, premature ventricular beats, and emotional irritability. It can cause hypokalemia, and the effect is the strongest 4 hours after taking it.
7.2 diagnosis
The diagnostic points of salbutamol poisoning are [1]:
There is a history of salbutamol application, and the above performance appears.
7.3 treatment
The treatment points of salbutamol poisoning are [1]:
1. When the dose is too large, tachycardia and blood pressure fluctuation occur, which can generally be recovered by reducing the dose. In severe cases, the drug should be stopped. When bronchospasm occurs due to repeated overuse, the drug should be stopped immediately.
2. When the curative effect of the drug is poor, it is not appropriate to increase the drug excessively, and other drugs that excite bronchial β2 receptors can be replaced as appropriate.