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Home > Encyclopedia > Terbutaline sulfate

Terbutaline sulfate

pharmaceutical raw materials
Terbutaline sulfate structure

Terbutaline sulfate 

structure
  • CAS No:

    23031-32-5

  • Formula:

    C12H19NO3.1/2H2O4S

  • Chemical Name:

    Terbutaline sulfate

  • Synonyms:

    1,3-Benzenediol,5-[2-[(1,1-dimethylethyl)amino]-1-hydroxyethyl]-,sulfate (2:1);Benzyl alcohol,α-[(tert-butylamino)methyl]-3,5-dihydroxy-,sulfate (2:1) (salt);1,3-Benzenediol,5-[2-[(1,1-dimethylethyl)amino]-1-hydroxyethyl]-,sulfate (2:1) (salt);Terbutaline sulfate;Terbutalin sulfate;2-(tert-Butylamino)-1-(3,5-dihydroxyphenyl)ethanol sulfate (2:1);Bricanyl;Brethine;Brithine;Benzyl alcohol,α-[(tert-butylamino)methyl]-3,5-dihydroxy-,sulfate (2:1) (salt),(±)-;(±)-Terbutaline sulfate;1,3-Benzenediol,5-[2-[(1,1-dimethylethyl)amino]-1-hydroxyethyl]-,(±)-,sulfate (2:1) (salt);dl-Terbutaline sulfate;Terbasmin;Terbul;Monovent;Butaliret;Brethaire;(±)-Terbutaline hemisulfate;Terbutaline hemisulphate;Terbutaline hemisulfate;98225-49-1;32550-09-7

  • Categories:

    Active Pharmaceutical Ingredients  >  Respiratory Drugs

Description

Terbutaline sulfate is a β2-adrenergic receptor agonist; a fast-acting bronchodilator and a tocolytic to delay premature labor.


Terbutaline sulfate is an ethanolamine sulfate salt. It derives from a terbutaline.|The beta-2 adrenergic agonists are a large group of drugs that mimic the actions of naturally occurring catecholamines such as norepinephrine, epinephrine and dopamine. Direct agonists directly interact with the adrenergic receptors, whereas indirect agonists typically stimulate the release of endogenous catecholamines. The beta-2 adrenergic agonists act mainly on the smooth muscle of the vasculature, bronchial tree, intestines and uterus. These agents also act on the liver stimulating glycogenolysis and release of glucose from the liver and muscle (particularly if used in high doses). The beta-2 adrenergic agonists are used largely as bronchodilators in the management of asthma, both in control of acute symptomatic attacks as well as chronic, long term prevention and management. These agents are some of the most commonly prescribed drugs for asthma and are widely used and proven to be well tolerated and safe. The use of beta adrenergic agonists in asthma has not been associated with elevations in serum aminotransferase or alkaline phosphatase levels or in causing clinically apparent liver disease. When given in large doses or after intentional overdose, beta adrenergic agonists can cause liver injury. Most case reports of liver damage from these agents have been associated with their use in control of premature labor (for their effects on relaxation of uterine smooth muscle). The liver injury typically arises within a few days of starting high dose intravenous beta adrenergic agonists, is usually asymptomatic, not associated with jaundice, and rapidly reversed once the medication is stopped.|A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.

Terbutaline sulfate Basic Attributes

548.648

548.24

245-386-3

DTXSID3045437

2922504500

Characteristics

228

4.24840

Solid

1.1840 (rough estimate)

246-248 °C

419.2ºC at 760 mmHg

165.3ºC

1.6900 (estimate)

H2O: soluble 100mg/mL, clear to slightly hazy, colorless to yellow

8.92E-08mmHg at 25°C

153.9 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

NONH for all modes of transport

3

R42/43;R63

S26-S36

DN9000000

Xn:Harmful;

P281

H361

|Warning|H361 (93.18%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P260, P281, P308+P313, P314, P405, and P501|Aggregated GHS information provided by 44 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Prospective studies have shown that ALT elevations occur in less than 1% of patients receiving long term oral therapy with typical beta adrenergic bronchodilators, but instances of clinically apparent liver injury have not been reported in any detail. However, several cases of acute elevations in serum aminotransferase levels have been described in pregnant women receiving high doses of beta adrenergic agents intravenously for prevention or control of premature labor (Case 1). Serum alkaline phosphatase, GGT and bilirubin levels are generally normal or within the normal range for later stages of pregnancy. The serum aminotransferase elevations are usually asymptomatic, but may be associated with nausea and right upper quadrant pain. Bilirubin elevations are minimal and cases with jaundice have not been reported. The abnormalities resolve promptly (within 1 to 3 weeks) upon stopping therapy and have not been associated with fatalities or chronic liver injury.

Drug Information

The beta-2 adrenergic agonists are a large group of drugs that mimic the actions of naturally occurring catecholamines such as norepinephrine, epinephrine and dopamine. Direct agonists directly interact with the adrenergic receptors, whereas indirect agonists typically stimulate the release of endogenous catecholamines. The beta-2 adrenergic agonists act mainly on the smooth muscle of the vasculature, bronchial tree, intestines and uterus. These agents also act on the liver stimulating glycogenolysis and release of glucose from the liver and muscle (particularly if used in high doses). The beta-2 adrenergic agonists are used largely as bronchodilators in the management of asthma, both in control of acute symptomatic attacks as well as chronic, long term prevention and management. These agents are some of the most commonly prescribed drugs for asthma and are widely used and proven to be well tolerated and safe. The use of beta adrenergic agonists in asthma has not been associated with elevations in serum aminotransferase or alkaline phosphatase levels or in causing clinically apparent liver disease. When given in large doses or after intentional overdose, beta adrenergic agonists can cause liver injury. Most case reports of liver damage from these agents have been associated with their use in control of premature labor (for their effects on relaxation of uterine smooth muscle). The liver injury typically arises within a few days of starting high dose intravenous beta adrenergic agonists, is usually asymptomatic, not associated with jaundice, and rapidly reversed once the medication is stopped.

Antiasthmatic Agents

Drugs that prevent preterm labor and immature birth by suppressing uterine contractions (TOCOLYSIS). Agents used to delay premature uterine activity include magnesium sulfate, beta-mimetics, oxytocin antagonists, calcium channel inhibitors, and adrenergic beta-receptor agonists. The use of intravenous alcohol as a tocolytic is now obsolete. (See all compounds classified as Tocolytic Agents.)|Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS. (See all compounds classified as Adrenergic beta-2 Receptor Agonists.)|Drugs that mimic the effects of stimulating postganglionic adrenergic sympathetic nerves. Included here are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters. (See all compounds classified as Sympathomimetics.)|Agents that cause an increase in the expansion of a bronchus or bronchial tubes. (See all compounds classified as Bronchodilator Agents.)

Arubendol

Terbutaline sulfate Use and Manufacturing

Uses

betaadrenergic agonist, bronchodilator Anti Asthmatic A B-Adrenergic receptor agonist. A Bronchodilator

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:548.6
Hydrogen Bond Donor Count:10
Hydrogen Bond Acceptor Count:12
Rotatable Bond Count:8
Exact Mass:548.24036665
Monoisotopic Mass:548.24036665
Topological Polar Surface Area:228
Heavy Atom Count:37
Complexity:286
Undefined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

Material

Drug Function and Efficacy

Terbutaline selectively stimulates beta 2 adrenergic receptors and relaxes bronchial smooth muscle.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Registered Holders

  • Jining Shenzhou Pharmaceutical Co., Ltd.

    China China
    Active
  • MELODY HEALTHCARE PVT LTD

    United States United States
    Active
  • CAMBREX PROFARMACO MILANO SRL

    Brazil Brazil
    Active

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