Terbutaline (terbutaline sulfate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Terbutaline sulfate, a synthetic sympathomimetic amine, is a short-acting beta2-agonist bronchodilator (SABA).
Terbutaline sulfate is a short-acting beta2-agonist bronchodilator (SABA). In vitro and in vivo pharmacologic studies have demonstrated that terbutaline exerts a preferential effect on beta2 -adrenergic receptors. While it is recognized that beta2-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta2-receptors in the human heart, existing in a concentration of 10-50%.
The precise function of these receptors has not been established. In controlled clinical studies in patients given terbutaline sulfate orally, proportionally greater changes occurred in pulmonary function parameters than in heart rate or blood pressure. While this suggests a relative preference for the beta-receptors in man, the usual cardiovascular effects commonly associated with other sympathomimetic agents were also observed with terbutaline sulfate.
Additionally, controlled clinical studies in patients given terbutaline subcutaneously have not revealed a preferential beta-adrenergic effect.
The pharmacologic effects of beta-adrenergic agonists, including terbutaline, are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic 3', 5'-adenosine monophosphate (cAMP). Increased cAMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
Controlled clinical studies have shown that terbutaline sulfate administered orally or subcutaneously relieves bronchospasm in patients with chronic obstructive pulmonary disease (COPD) by significantly increasing pulmonary function (e.g., an increase of 15% or more in forced expiratory volume in one second (FEV1)). After administration of terbutaline sulfate, a measurable change in flow rate usually occurs within 30 minutes after oral administration and within 5 minutes after subcutaneous injection. A clinically significant improvement in pulmonary function occurs within 60-120 minutes after oral administration and within 15 minutes after subcutaneous injection.
The maximum effect usually occurs within 120-180 minutes after oral administration and within 30-60 minutes after subcutaneous administration. Terbutaline sulfate also produces a clinically significant decrease in airway and pulmonary resistance, which persists for 4 hours or longer after oral administration and between 1.5-4 hours after subcutaneous administration. Significant bronchodilator action (as measured by airway resistance, forced expiratory flow or peak expiratory flow rate) has also been demonstrated for up to 8 hours in some studies with oral terbutaline.
In studies comparing the effectiveness of terbutaline sulfate with that of ephedrine for up to 3 months, both drugs maintained a significant improvement in pulmonary function throughout this period of treatment.
Following oral administration of terbutaline sulfate 5 mg tablets or terbutaline sulfate 5 mg solution in 17 healthy adult male subjects, peak plasma concentrations were observed at median (range) times of 2 (1-3) and 1.5 (0.5-3.0) hours after dosing. After oral administration of terbutaline 51-62 mcg/kg to 3 healthy male subjects, peak plasma concentrations were observed 1-3 hours later. After 3 days only 30-50% of the dose was recovered from urine and the remainder from feces, which may indicate poor absorption.
After an oral dose of terbutaline sulfate in asthmatic patients, the elimination half-life of the drug was approximately 3.4 hours.
After subcutaneous administration of terbutaline sulfate 0.5 mg in healthy adult male subjects, peak plasma concentrations were observed at a median (range) time of 0.5 (0.08-1.0) hours after dosing. The mean terminal half-life in 9 of the 17 subjects was 5.7 hours. Elimination half-life of the drug in 10 of 14 patients was approximately 2.9 hours after subcutaneous administration, but the other 4 patients had longer elimination half-lives (between 6-14 hours).
About 90% of the drug was excreted in the urine at 96 hours after subcutaneous administration, approximately 60% of which was unchanged drug. The sulfate conjugate is a major metabolite of terbutaline.
USES: Terbutaline is used to treat wheezing and shortness of breath from lung problems (such as asthma, chronic obstructive pulmonary disease-COPD, bronchitis, emphysema). Terbutaline belongs to a class of drugs known as bronchodilators. It works by relaxing the muscles around the airways so that they open up and you can breathe more easily.
Generic name: terbutaline sulfate
Pronunciation: (ter-BYOO-ta-leen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Terbutaline
Indications
The following indications are listed for Terbutaline:
- Exacerbation Of Chronic Obstructive Pulmonary Disease
- Status Asthmaticus
Also known as: Acute Severe Asthma, Acute Severe Asthma Attack, Acutely Deteriorating Chronic Obstructive Pulmonary Disease, Asthma With Status Asthmaticus, Exacerbation Of Copd, Severe Asthma Exacerbation.
Dosing
No dosing information is available for this tab.
Terbutaline sulfate is administered orally or subcutaneously (usually into the lateral deltoid area).
Terbutaline sulfate also has been used IV+ in selected patients to inhibit uterine contractions in preterm labor+ (tocolysis).
The drug also has been administered by IV infusion+ for the emergency treatment of acute asthma exacerbations in young children. However, administration of parenteral terbutaline sulfate by routes or methods other than subcutaneous injection (e.g., IV) is not recommended by the manufacturer.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Prolonged or maintenance tocolysis (terbutaline injection).
*Acute or maintenance tocolysis (terbutaline tablets).
*Hypersensitivity to sympathomimetic amines or any component of the drug product.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects of terbutaline sulfate tablets reported in >=1% of patients include nervousness, tremor, somnolence, dizziness, anxiety, insomnia, palpitations, tachycardia, ventricular extrasystoles, vasodilation, nausea, dry mouth, headache, asthenia, and sweating.
The most common adverse effects of terbutaline sulfate injection reported in >=2% of patients include tremor, nervousness, dizziness, headache, drowsiness, palpitations, tachycardia, dyspnea, nausea/vomiting, flushed feeling, and sweating.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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The manufacturer does not recommend terbutaline sulfate for patients younger than 12 years of age because of insufficient clinical data to establish safety and effectiveness.
There are no adequate and well-controlled studies of terbutaline sulfate in pregnant women. Published animal studies in rats showed alterations in behavior and brain development in the offspring, including decreased cellular proliferation and differentiation, when dams were treated subcutaneously with terbutaline during the late stage of pregnancy and lactation period.
Oral terbutaline sulfate has not been approved and should not be used for acute or maintenance tocolysis. Terbutaline injection has not been approved and should not be used for prolonged tocolysis (beyond 48-72 hours). In particular, terbutaline sulfate should not be used for tocolysis in the outpatient or home setting. Serious adverse reactions, including death, have been reported after administration of terbutaline sulfate to pregnant women. In the mother, these adverse reactions include increased heart rate, transient hyperglycemia, hypokalemia, cardiac arrhythmias, pulmonary edema, and myocardial ischemia. Increased fetal heart rate and neonatal hypoglycemia may occur as a result of maternal administration.
Terbutaline crosses the placenta. After administration of a single IV dose of terbutaline to 22 women in late pregnancy who required elective Cesarean section due to clinical reasons, umbilical blood levels of terbutaline were found to range from 11-48% of the maternal blood levels. Because of the potential for beta-agonist interference with uterine contractility, use of terbutaline sulfate for relief of bronchospasm during labor should be restricted to those patients in whom the benefits clearly outweigh the risk.
It is not known whether terbutaline is excreted in human milk. The drug should be used during nursing only if the potential benefit justifies the possible risk to the infant.
The manufacturer makes no specific dosage recommendations for geriatric patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Clinical studies of terbutaline sulfate did not include sufficient numbers of patients 65 years of age and older to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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