Terbutaline 3-agonist

Tocolytics are drugs such as the selective (32-adrenoceptor agonists, e.g. salbutamol or terbutaline, which inhibit both the spontaneous and oxytocin-induced contractions of the pregnant uterus by relaxing... 

Examples of sympathomimetic bronchodilators include albuterol (Ventolin), epinephrine (Adrenalin), salme-terol (Serevent), and terbutaline (Brethine). Many of the sympathomimetics used as bronchodilators have die subclassification of beta-2 ((32) receptor agonists (eg, albuterol, salmeterol, and terbutaline). Additional information concerning the various sympathomimetic dragp is given in the Summary Drug Table Bronchodilators. 

Recent work in our laboratory (Kompella, Mathias, and Lee, unpublished observation) has revealed that activation of the cAMP-regulated Cl channels in the conjunctiva also enhances the transcytosis of horseradish peroxidase. 8-Bromo-cAMP (a membrane-permeable analog of cAMP) and terbutaline (a p2-adrenergic agonist known to increase intracellular levels of cAMP in other epithelial tissues [238]), at 0.5 mM, were found to enhance the transport of 100 pg/ mL HRP from the mucosal side to the serosal side of the pigmented rabbit conjunctiva by a factor of 4 (Fig. 11). 

Relative extraction efficiencies of polar polymeric neutral, cation, and anion exchange sorbents (HLB, MCX, and MAX) for 11 beta antagonists and 6 beta agonists in human whole blood were probed.109 Initial characterization of MCX and MAX for acidic and basic load conditions, respectively, showed that both the agonists and antagonists were well retained on MCX, while they were recovered from MAX in the wash with either methanol or 2% ammonia in methanol (see Table 1.6). Blood samples were treated with ethanol containing 10% zinc sulfate to precipitate proteins and the supernatants loaded in 2% aqueous ammonium hydroxide onto the sorbents. After a 30% methanol and 2% aqueous ammonia wash, the analytes were eluted with methanol (HLB), 2% ammonia in methanol (MCX), or 2% formic acid in methanol (MAX). The best recoveries were observed with MCX under aqueous conditions or blood supernatant (after protein precipitation) spiked sample load conditions (see Table 1.7). Ion suppression studies by post-column infusion showed no suppression for propranolol and terbutaline with MCX, while HLB and MAX exhibited suppression (see Figure 1.6). 

Beta-2 Agonists—all are prohibited but some, such as salbutamol and terbutaline, are... 

Beta agonists (terbutaline, albuterol) Theophylline Antidepressants Bupropion Citalopram Escitalopram Duloxetine Fluoxetine Fluvoxamine... 

Orciprenaline is a partially selective adrenoceptor-agonist and hence it is more likely to have effects on the cardiovascular system, such as arrhythmias, than the selective adrenoceptor-agonists, such as salbutamol, terbutaline and the long-acting beta-agonists salmeterol and formoterol. Orciprenaline is available only as tablets or syrup and can be prescribed to 4-year-old children. 

The majority of the marketed products are used for asthma and COPD. Typical agents that are used for these indications are fl2-agonists such as salbutamol (albuterol), Terbutalin or formoterol, corticosteroids such as budesonide, FUxotide or beclomethasone and mast-cell stabilizers such as sodium cromoglycate or nedocromil. 

Tocolysis. The uterine relaxant effect of P2-adrenoceptor agonists, such as terbutaline or fenoterol, can be used to prevent premature labor. Vasodilation Ltillmann, Color Atlas of Pharmacology (... 

Terbutaline and albuterol are relatively selective Pj-adrenoceptor agonists. Both have a longer duration of action than isoproterenol because they are not metabolized by COMT. Like isoproterenol, they are not metabolized by MAO and are not transported into adrenergic neurons. Terbutaline and albuterol are effectively administered either orally or subcutaneously. Because of their selectivity for Pj-adrenoceptors, they produce less cardiac stimulation than does isoproterenol but are not completely without effects on the heart. 

Terbutaline, albuterol, salmeterol and other Pj-adrenoceptor agonists are used primarily in the management of asthma. Terbutaline and albuterol have very rapid onset of action and are indicated for acute symptom rehef Salmeterol, in contrast, has a slow onset of action but a long duration of action. Salmeterol is thus used as prophylactic therapy only, not to reverse acute symptoms. 

Terbutaline (Brethine, Bricanyl) is a relatively specific P2-adrenoceptor agonist (see Chapters 10 and 39). Terbutaline can prevent premature labor, especially in individuals who are more than 20 weeks into gestation and have no indication of ruptured fetal membranes or in whom labor is not far advanced. Its effectiveness in premature labor after 33 weeks of gestation is much less clear. Terbutaline can decrease the frequency, intensity, and duration of uterine contractions through its ability to directly stimulate Pj-adrenoceptors. While it appears to be especially selective for P2-receptor activation, terbutaUne does have some Pi activity as well. 

Terbutaline is frequently used in the management of premature labor, although it has not been marketed for such use. Its effectiveness, side effects, precautions, and contraindications are similar to those of all P2-adrener-gic agonists. Terbutaline can cause tachycardia, hypotension, hyperglycemia, and hypokalemia. It can be given orally in addition to subcutaneous or intravenous administration. 

Beta-2-adrenergic agonists, selective fenoterol hydrobromide salbutamol salbutamol sulfate terbutaline sulfate... 

Terbutaline is a similar drug that is occasionally used as an alternative to salbutamol in patients who have experienced marked sympathomimetic side effects. Other selective 32-adrenceptor agonists include fenoterol, reproterol, and rimiterol, all of which are available as aerosols. 

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