What Is Terbutaline?

Drugs used to treat bronchial asthma, asthmatic bronchitis, emphysema, etc. 2-receptor stimulant with bronchodilator effect. It is highly selective for bronchial smooth muscle, has little excitatory effect on the heart, and has no central effect. For bronchial asthma, wheezing bronchitis, obstructive emphysema, and other lung diseases with bronchospasm. Especially suitable for asthma patients with hypertension, coronary heart disease and other cardiovascular diseases.

Chinese name: Terbutaline
Foreign name: Terbutaline

Product name: Boricone
Used for: Treatment of bronchial asthma

Terbutaline Basic Information

Chinese name: terbutaline

Chinese alias: 5- (1-hydroxy-2-tert-butylaminoethyl) benzene-1,3-diphenol

English name: terbutaline

English alias: SNGP-003-04H08; TelMisartan API; 1- (3,5-dihydroxyphenyl) -2- (tert-butylamino) -ethanol; TU-199; 4 '-[(2-n-Propyl-4-methyl -6- (1-methylbenzimidazol-2-yl) -benzimidazol-1-yl) -methyl] -2-carboxy-biphenyl;

CAS number: 23031-25-6

Molecular formula: C12H19NO3

Molecular weight: 225.28400

Exact mass: 225.13600

PSA: 72.72000

LogP: 1.91020

Terbutaline physical and chemical properties

Density: 1.171 g / cm3

Melting point: 204-208ºC

Boiling point: 419.2ºC at 760 mmHg

Flash point: 165.3ºC

Vapor pressure: 3.42E-07mmHg at 25 ° C ^[1]

Terbutaline molecular structure data

1. Molar refractive index: 63.19

2. Molar volume (cm3 / mol): 192.2

3. Isotonic specific volume (90.2K): 511.4

4. Surface tension (dyne / cm): 50.0

5. Polarizability (10-24cm3): 25.05

Terbutaline Computational Chemistry Data

1. Hydrophobic parameter calculation reference value (XlogP): None

2.Number of hydrogen-bonded donors: 4

3.Number of hydrogen bond acceptors: 4

4.Number of rotatable chemical bonds: 4

5.Number of tautomers: 5

6. Topological molecular polar surface area 72.7

7.Number of heavy atoms: 16

8.Surface charge: 0

9.Complexity: 205

10.Number of isotope atoms: 0

11. Determine the number of atomic stereocenters: 0

12. Uncertain number of atomic stereocenters: 1

13. Determine the number of chemical bond stereocenters: 0

14. Uncertain number of chemical bond stereocenters: 0

15.Number of covalent bond units: 1

Terbutaline Synthesis

3,5-dihydroxybenzoic acid and ethanol are reacted at reflux under sulfuric acid catalysis to obtain ethyl 3,5-dihydroxybenzoate. Ethyl 3,5-dihydroxybenzoate and benzyl chloride in the presence of potassium carbonate, refluxed for 20 h, hydrolyzed with 5 ml / L of hydrochloric acid or potassium hydroxide to the free acid, and refluxed with sulfoxide for 1 h, and chlorinated to The acid chloride reacted with azomethane to form azoacetyl, and reacted with hydrogen bromide to form bromoacetyl, and then refluxed with tert-butylamine for 20h. Terbutaline was finally obtained by catalytic hydrogenation in the presence of acetic acid. ^[2]

Terbutaline Related Drug Instructions

Terbutaline Classification Name

Primary classification: Respiratory drugs Secondary classification: Antiasthmatic drugs Third classification: Airway dilatation drugs

Terbutaline Drug English Name

Terbutaline

Terbutaline drug alias

Boliconi, m-Hydroxybutanin, M-Hydroxybutanin, T-Hydroxybutanine, M-Hydroxybutanine, Raleigh Corning, Teptalene, M-Hydroxybenzidine, Chuankangsu, Belikang Soner, Respirol, Brethine, Bricanyl, Bristurin

Terbutaline

1. Tablet: 2.5mg, 5mg; 2. Inhalant: 50mg, 0.25mg per spray, 200 times per bottle. 3. Aerosol: 50mg, 100mg, 0.25mg per tincture, 200 times and 400 times per bottle.

Terbutaline pharmacological effects

This product has high selectivity for airway 2 receptors, and its bronchodilator effect is similar to that of albuterol. The effect on the heart is only 1/100 of isoproterenol. This product replaces the catechol ring with a m-hydroxyphenol ring, and the hydrogen atom of the amino group is replaced by a tert-butyl group on the side chain of ethanolamine. This structural change makes it difficult to be inactivated by COMT, monoamine oxidase or sulfate kinase, and the action time is significantly prolonged, which has become its most significant feature. This product can also excite the 2 receptors in the myometrium and inhibit spontaneous uterine contraction or uterine contraction caused by oxytocin.

Terbutaline pharmacokinetics

Orally affected by the first-pass effect of the liver, the bioavailability is only 15% ± 6%, the asthma effect occurs in about 30 minutes, the effective plasma concentration is 3 g / ml, the plasma protein binding rate is 25%, and the steady-state distribution volume is 1.6L / kg, pediatric (1.57 ± 0.19) L / kg. The peak time of plasma drug concentration is 2 to 4 hours, and the effect lasts 4 to 7 hours. Subcutaneous injection takes effect from 5 to 15 minutes, and the effect reaches a peak from 0.5 to 1 hour, lasting 1.5 to 4 hours. Aerosol inhalation takes effect after 5 15min, the maximum effect is achieved within 0.5 1h, and the effect lasts for 4h. The concentration of this drug in each tissue varies depending on the route of administration. Because of its hydrophilic nature, the concentration of tissues and organs after intravenous injection or oral administration is slightly lower than the plasma concentration, and the plasma protein binding rate is 25%. After aerosol inhalation, the lung concentration is higher and the maintenance time is longer. After diffused into the blood stream, the lung / plasma concentration ratio is about the same. After 4 hours of intravenous injection, the heart / plasma concentration ratio was approximately the same. After intravenous injection for 5 minutes, the urine concentration can exceed the blood concentration. The drug does not easily penetrate the blood-cerebrospinal fluid barrier and hardly affects the central nervous system. The drug can pass through the placenta and into the breast. The drug concentration was higher in the muscle, with a muscle / plasma drug concentration ratio of 4.6. In the body, part is metabolized in the liver, and the rest is excreted in the original form by the urine. Excretion is 30% within 12 hours and 40% within 72 hours. More than 90% of the urine is excreted after parenteral administration, of which 66% is the original drug. The average human clearance is 3.0ml / kg per minute. The average plasma half-life was 12 hours. The plasma half-life of asthma patients was (3.6 ± 0.3) hours.

Terbutaline indication

It is used for bronchospasm in bronchial asthma, asthma-like bronchitis and chronic obstructive pulmonary disease to prevent premature birth.

Terbutaline contraindications

Those who are allergic to this product are prohibited.

Terbutaline notes

1. Use with caution in patients with hypertension, coronary heart disease, and hyperthyroidism. 2. Diabetic women should pay attention to adjusting insulin dosage when using this product. 3. In cases where pregnancy must be terminated, such as stillbirth, intrauterine infection, severe pregnancy poisoning, this product must be discontinued.

Terbutaline adverse reactions

A few patients have hand tremor, headache, palpitations, and gastrointestinal disorders. When 5 mg orally, the incidence of hand tremor is 20% to 30%.

Terbutaline dosage

1. Oral: 2.5 to 5 mg per adult, 3 times a day. Children are reduced. 2. Aerosol inhalation: 0.2mg per adult, 3 to 4 times per day. 3. Subcutaneous injection: 0.25mg each time, if there is no obvious clinical improvement in 15-30 minutes, the injection can be repeated once, but the total amount in 4h cannot exceed 0.5mg.

Terbutaline drug interactions

1. The combination of this drug with other adrenergic receptor agonists can increase the efficacy, but the adverse reactions may also worsen. 2. Monoamine oxidase inhibitors, tricyclic antidepressants, antihistamines, levothyroxine, etc. can enhance the adverse reactions of this drug. 3. This medicine combined with succinylcholine can enhance the muscle relaxation of the latter. 4. This medicine can reduce the blood pressure-lowering effect of guanethidine. 5. This medicine can enhance the adverse reactions of non-potassium-preserving diuretics. 6. Epinephrine beta blockers (such as acebutolol, atenolol, labelol, metoprolol, naldolol, indolol, propranolol, timolol Seoul, etc.) can antagonize the effect of this drug and reduce the efficacy. 7. When this medicine is used in combination with insulin or oral hypoglycemic agents, the dosage of the latter must be adjusted. 8. When this medicine is combined with theophylline. Can reduce theophylline blood concentration.

Terbutaline Drug Evaluation

According to foreign reports, the clinical evaluation of 262 cases in general clinical trials has an effective rate of 64.80% (46/71) for adults with bronchial asthma; 68% (70/103) for children; 66.7 for adults with chronic bronchitis % (40/54); 74.1% (40/54) of children with asthmatic bronchitis; 88.9% (8/9) of patients with bronchiectasis; and 100% (4/4) of patients with emphysema. According to two reports in China, the total effective rate of improvement in pulmonary function expiratory volume per second (PEV1) of terbutaline aerosol for bronchial asthma was 64% and 82%, respectively. Another report evaluated the efficacy of terbutaline in the treatment of pediatric asthmatic diseases. Forty patients were divided into two groups of 20 patients each. The treatment group was orally administered with the product 0.05 to 0.06 mg / kg 3 times a day for 5 to 7 consecutive times. Days; the control group took aminophylline 4-6 mg / kg orally 3 times a day, the course of treatment was the same as that of other treatments and treatment groups. Results The disappearance time of lung asthma sounds in the treatment group was significantly faster than the latter, and the significant and total effective rates were also higher than the latter (P0.05). Terbutaline can promote the disappearance of pediatric pneumonia rales. Fifty children should take this product orally; control group should take anisodamine orally; both groups were treated with antibiotics to control infection. Results The total effective rates of the two groups were 87% and 63%, respectively. The disappearance time of lung rales was (3.95 + 1.47) days and (5.57 + 1.93) days (P <0.01). Terbutaline is about 70% effective in treating asthma, can effectively improve the symptoms of asthma patients, and is one of the main drugs for treating asthma. Terbutaline sulfate injection can effectively improve the pulmonary ventilation function of patients with bronchial asthma and chronic asthmatic bronchitis, effectively reduce respiratory resistance, and significantly improve FEV1, FVC, PEF, and other indicators. It can be used as a preferred drug for treating bronchial asthma One, the effective rate is 88.4%. The efficacy of terbutaline aerosol is higher than that of tablets. The complete remission rate of pediatric asthma treated with nebulized solution was 91.4%. The medicine is inhaled with a compression inhaler. The medicine can reach the airway surface uniformly. The performance is stable and the child is easy to accept. It is suitable for all age groups, especially infants. There were a few cases of adverse reactions, including palpitations, tremors, stomach upset, and fatigue. The incidence of adverse reactions was 13.3%. The adverse reactions were mildly tolerable and did not affect continued treatment. ^[3]