Terbutaline Sulfate
Tablet · Oral, Subcutaneous
Uses
Terbutaline Sulfate Tablets USP are indicated for the prevention and reversal of bronchospasm in patients 12 years of age and older with asthma and reversible bronchospasm associated with bronchitis and emphysema.
Dosage and administration
Adults The usual oral dose of terbutaline sulfate tablets for adults is 5 mg administered at approximately six-hour intervals, three times daily, during the hours the patient is usually awake. If side effects are particularly disturbing, the dose may be reduced to 2.5 mg three times daily, and still provide a clinically significant improvement in pulmonary function. The total dose within 24 hours should not exceed 15 mg. Children Terbutaline sulfate tablets are not recommended for use in children below the age of 12 years. A dosage of 2.5 mg three times daily is recommended for children 12 to 15 years of age. The total dose within 24 hours should not exceed 7.5 mg. If a previously effective dosage regimen fails to provide the usual relief, medical advice should be sought immediately as this is often a sign of seriously worsening asthma that would require reassessment of therapy.
Contraindications
1. Tocolysis Oral terbutaline sulfate is contraindicated for the treatment of acute or maintenance tocolysis [see Boxed Warning: Tocolysis ] . 2. Hypersensitivity Terbutaline sulfate is contraindicated in patients known to be hypersensitive to sympathomimetic amines or any component of this drug product.
Warnings
Deterioration of Asthma Asthma may deteriorate acutely over a period of hours or chronically over several days or longer. If the patient needs more doses of terbutaline sulfate tablets than usual, this may be a marker of destabilization of asthma and requires reevaluation of the patient and the treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment, e.g., corticosteroids. Use of Anti-Inflammatory Agents The use of beta-adrenergic agonist bronchodilators alone may not be adequate to control asthma in many patients. Early consideration should be given to adding anti-inflammatory agents, e.g., corticosteroids. Cardiovascular Effects Terbutaline sulfate, like all other beta-adrenergic agonists, can produce a clinically significant cardiovascular effect in some patients as measured by pulse rate, blood pressure, and/or symptoms. Although such effects are uncommon after administration of terbutaline sulfate tablets at recommended doses, if they occur, the drug may need to be discontinued. In addition, beta-agonists have been reported to produce electrocardiogram (ECG) changes, such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression. The clinical significance of these findings is unknown. Therefore, terbutaline sulfate tablets, like all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension. Seizures There have been rare reports of seizures in patients receiving terbutaline; seizures did not recur in these patients after the drug was discontinued.
Precautions
General Terbutaline, as with all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, including ischemic heart disease, hypertension, and cardiac arrhythmias; hyperthyroidism; diabetes mellitus; hypersensitivity to sympathomimetic amines; and convulsive disorders. Significant changes in systolic and diastolic blood pressure have been seen and could be expected to occur in some patients after use of any beta-adrenergic bronchodilator. Immediate hypersensitivity reactions and exacerbation of bronchospasm have been reported after terbutaline administration. Beta-adrenergic agonist medications may produce significant hypokalemia in some patients, possibly through intracellular shunting, which has the potential to produce adverse cardiovascular effects. The decrease is usually transient, not requiring supplementation. Large doses of intravenous terbutaline sulfate have been reported to aggravate preexisting diabetes and ketoacidosis. Information for Patients The action of terbutaline sulfate tablets should last up to 6 hours or longer. Terbutaline sulfate tablets should not be used more frequently than recommended. Do not increase the dose or frequency of terbutaline sulfate tablets without consulting your physician. If you find that treatment with terbutaline sulfate tablets becomes less effective for symptomatic relief, your symptoms become worse, and/or you need to use the product more frequently than usual, you should seek medical attention immediately. While taking terbutaline sulfate tablets, other inhaled drugs and asthma medications should be taken only as directed by your physician. Common adverse effects include palpitations, chest pain, rapid heart rate, tremor or nervousness. If you are pregnant or nursing, contact your physician about use of terbutaline sulfate tablets. Effective and safe use of terbutaline sulfate tablets includes an understanding of the way that it should be administered. Drug Interactions The concomitant use of terbutaline sulfate tablets with other sympathomimetic agents is not recommended, since the combined effect on the cardiovascular system may be deleterious to the patient. However, this does not preclude the use of an aerosol bronchodilator of the adrenergic-stimulant type for the relief of an acute bronchospasm in patients receiving chronic oral therapy with terbutaline sulfate tablets. Monoamine Oxidase Inhibitors and Tricyclic Antidepressants Terbutaline sulfate should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents, since the action of terbutaline sulfate on the vascular system may be potentiated. Beta-Blockers Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-agonists, such as terbutaline sulfate, but may produce severe bronchospasm in asthmatic patients. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain circumstances, e.g., as prophylaxis after myocardial infarction, there may be no acceptable alternatives to the use of beta-adrenergic blocking agents in patients with asthma. In this setting, cardioselective beta-blockers could be considered, although they should be administered with caution. Diuretics The ECG changes and/or hypokalemia that may result from the administration of non-potassium sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded. Although the clinical significance of these effects is not known, caution is advised in the co-administration of beta-agonists with non-potassium sparing diuretics. Carcinogenesis, Mutagenesis, and Impairment of Fertility In a 2-year study in Sprague-Dawley rats, terbutaline sulfate caused a significant and dose-related increase in the incidence of benign leiomyomas of the mesovarium at dietary doses of 50 mg/kg, and above (approximately 25 times the maximum recommended daily oral dose for adults on a mg/m 2 basis). In a 21-month study in CD-1 mice, terbutaline sulfate showed no evidence of tumorigenicity at dietary doses up to 200 mg/kg (approximately 55 times the maximum recommended daily oral dose for adults on a mg/m 2 basis). The mutagenicity potential of terbutaline sulfate has not been determined. Reproduction studies in rats using terbutaline sulfate demonstrated no impairment of fertility at oral doses up to 50 mg/kg (approximately 25 times the maximum recommended daily oral dose for adults on a mg/m 2 basis). Teratogenic Effects There are no adequate and well-controlled studies of terbutaline sulfate in pregnant women. Published animal studies show that rat offspring exhibit alterations in behavior and brain development, including decreased cellular proliferation and differentiation when dams were treated subcutaneously with terbutaline during the late stage of pregnancy and lactation period. Terbutaline exposures in rat dams were approximately 6.5 times the common human dose in adults of 15 mg/day, on a mg/m 2 basis. Oral terbutaline sulfate has not been approved for and should not be used for acute or maintenance tocolysis. 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.
Side effects
Adverse reactions observed with terbutaline sulfate are similar to those commonly seen with other sympathomimetic amines. All of these reactions are generally transient in nature and usually do not require treatment. The frequency of these side effects appears to diminish with continued therapy. The following table lists the adverse reactions seen in 199 patients treated with terbutaline sulfate tablets during six double-blind crossover studies and four double-blind parallel studies (short- and long-term) performed in the United States. Percent Incidence of Adverse Reactions (Total Daily Dosage Range 5 to 15 mg) Terbutaline N=199 Reaction % Nervous System Nervousness 35.0 Tremor 15.0 Somnolence 5.5 Dizziness 3.5 Anxiety 1.0 Insomnia 1.5 Cardiovascular Palpitations 5.0 Tachycardia 3.5 Extrasystoles ventricular 1.5 Vasodilations 1.0 Digestive Nausea 3.0 Dry mouth 1.5 Body as a Whole Headache 7.5 Asthenia 2.0 Skin and Appendages Sweating 1.0 The following adverse reactions each occurred in fewer than 1% of patients: hallucinations, rash, paresthesia, hypertonia, (muscle cramps), vomiting. There have been rare reports of elevations in liver enzymes and of hypersensitivity vasculitis. To report SUSPECTED ADVERSE REACTIONS, contact ANI Pharmaceuticals, Inc. at 1-800-308-6755 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Drug interactions
Drug Interactions The concomitant use of terbutaline sulfate tablets with other sympathomimetic agents is not recommended, since the combined effect on the cardiovascular system may be deleterious to the patient. However, this does not preclude the use of an aerosol bronchodilator of the adrenergic-stimulant type for the relief of an acute bronchospasm in patients receiving chronic oral therapy with terbutaline sulfate tablets.
Pediatric use
Pediatric Use Terbutaline sulfate tablets are not recommended for patients under the age of 12 years because of insufficient clinical data to establish safety and effectiveness [see Dosage and Administration ] .
Geriatric use
Geriatric Use Clinical studies of terbutaline sulfate did not include sufficient numbers of subjects aged 65 and over 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 or other drug therapy.
Overdosage
The median subcutaneous lethal dose of terbutaline sulfate in mature rats is approximately 165 mg/kg (approximately 90 times the maximum recommended daily oral dose for adults on a mg/m 2 basis). The median subcutaneous lethal dose of terbutaline sulfate in young rats is approximately 2000 mg/kg (approximately 1100 times the maximum recommended daily oral dose for adults on a mg/m2 basis). The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under ADVERSE REACTIONS, e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats per minute, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, and insomnia. Hypokalemia may also occur. There is no specific antidote. Treatment consists of discontinuation of terbutaline sulfate tablets together with appropriate symptomatic therapy. The judicious use of a cardioselective beta-receptor blocker may be considered, bearing in mind that such medication can produce bronchospasm. There is insufficient evidence to determine if dialysis is beneficial for overdosage of terbutaline sulfate. In the alert patient who has taken excessive oral medication, the stomach should be emptied by induced emesis followed by lavage. In the unconscious patient, the airway should be secured with a cuffed endotracheal tube before lavage, and emesis should not be induced. Instillation of activated charcoal slurry may help reduce absorption of terbutaline. Adequate respiratory exchange should be maintained, and cardiac and respiratory support provided as needed. The patient should be monitored until signs and symptoms of overdosage have subsided.
Description
Terbutaline sulfate USP, the active ingredient of Terbutaline Sulfate Tablets USP, is a beta-adrenergic agonist bronchodilator available as tablets of 2.5 mg (2.05 mg of the free base) and 5 mg (4.1 mg of the free base) for oral administration. Terbutaline sulfate is ±-α-[( tert -butylamino)methyl]-3,5-dihydroxybenzyl alcohol sulfate (2:1) (salt). The empirical formula is (C 12 H 19 NO 3 ) 2
• H 2 SO 4 and the structural formula is: Terbutaline sulfate USP is a white to gray-white crystalline powder. It is odorless or has a faint odor of acetic acid. It is soluble in water and in 0.1N hydrochloric acid, slightly soluble in methanol, and insoluble in chloroform. Its molecular weight is 548.65. Inactive Ingredients: Microcrystalline cellulose, lactose monohydrate, magnesium stearate, povidone, and corn starch. WARNING: TOCOYSIS Oral terbutaline sulfate has not been approved for and should not be used for acute or maintenance tocolysis. In particular, terbutaline sulfate should not be used for maintenance tocolysis in the outpatient or home setting. During pregnancy, 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. [See Contraindications-Tocolysis ] structure
How supplied
Terbutaline Sulfate Tablets USP are available as: 2.5 mg: White to faintly yellow, oval, biconvex tablets debossed with ‘ANI’ and ‘721’ on one side and bisected on the reverse side. They are packaged in high density polyethylene (HDPE) bottles of 100 tablets (NDC 62559-721-01). 5 mg: White to faintly yellow, round, biconvex tablets debossed with ‘ANI’ and ‘722’ on one side and bisected on the reverse side. They are packaged in high density polyethylene (HDPE) bottles of 100 tablets (NDC 62559-722-01). Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Dispense in tight, light-resistant container (as defined in the USP). Manufactured by: ANI Pharmaceuticals, Inc. Baudette, MN 56623 10141 Rev 09/18 ani.jpg
Patient information
Information for Patients The action of terbutaline sulfate tablets should last up to 6 hours or longer. Terbutaline sulfate tablets should not be used more frequently than recommended. Do not increase the dose or frequency of terbutaline sulfate tablets without consulting your physician. If you find that treatment with terbutaline sulfate tablets becomes less effective for symptomatic relief, your symptoms become worse, and/or you need to use the product more frequently than usual, you should seek medical attention immediately. While taking terbutaline sulfate tablets, other inhaled drugs and asthma medications should be taken only as directed by your physician. Common adverse effects include palpitations, chest pain, rapid heart rate, tremor or nervousness. If you are pregnant or nursing, contact your physician about use of terbutaline sulfate tablets. Effective and safe use of terbutaline sulfate tablets includes an understanding of the way that it should be administered.
Label text from the FDA structured product label by ANI Pharmaceuticals, Inc. (revised Nov 15, 2019). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Terbutaline Sulfate in 17 products
Terbutaline Sulfate NDC products (17)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 0115-2622 | Terbutaline Sulfate 5 mg/1 Tablet | Amneal Pharmaceuticals of New York LLC | ANDA |
| 0115-2611 | Terbutaline Sulfate 2.5 mg/1 Tablet | Amneal Pharmaceuticals of New York LLC | ANDA |
| 62135-524 | Terbutaline Sulfate 2.5 mg/1 Tablet | Chartwell RX, LLC. | ANDA |
| 62135-525 | Terbutaline Sulfate 5 mg/1 Tablet | Chartwell RX, LLC. | ANDA |
| 63323-665 | Terbutaline Sulfate 1 mg/mL Injection, Solution | Fresenius Kabi USA, LLC | ANDA |
| 0404-9962 | Terbutaline Sulfate 1 mg/mL Injection, Solution | Henry Schein, Inc. | ANDA |
| 0143-9375 | Terbutaline Sulfate 1 mg/mL Injection | Hikma Pharmaceuticals USA Inc. | ANDA |
| 0143-9746 | Terbutaline Sulfate 1 mg/mL Injection | Hikma Pharmaceuticals USA Inc. | ANDA |
| 0527-1311 | Terbutaline Sulfate 5 mg/1 Tablet | Lannett Company, Inc. | ANDA |
| 0527-1318 | Terbutaline Sulfate 2.5 mg/1 Tablet | Lannett Company, Inc. | ANDA |
| 71872-7080 | Terbutaline Sulfate 1 mg/mL Injection | Medical Purchasing Solutions. LLC | ANDA |
| 71205-938 | Terbutaline Sulfate 2.5 mg/1 Tablet | Proficient Rx LP | ANDA |
| 71205-939 | Terbutaline Sulfate 5 mg/1 Tablet | Proficient Rx LP | ANDA |
| 24979-133 | Terbutaline Sulfate 5 mg/1 Tablet | Upsher-Smith Laboratories, LLC | ANDA |
| 24979-132 | Terbutaline Sulfate 2.5 mg/1 Tablet | Upsher-Smith Laboratories, LLC | ANDA |
| 62559-721 | Terbutaline Sulfate 2.5 mg/1 Tablet | ANI Pharmaceuticals, Inc. | NDA AUTHORIZED GENERIC |
| 62559-722 | Terbutaline Sulfate 5 mg/1 Tablet | ANI Pharmaceuticals, Inc. | NDA AUTHORIZED GENERIC |
Frequently asked questions
What is Terbutaline Sulfate used for?
Terbutaline Sulfate Tablets USP are indicated for the prevention and reversal of bronchospasm in patients 12 years of age and older with asthma and reversible bronchospasm associated with bronchitis and emphysema.
What are the side effects of Terbutaline Sulfate?
Adverse reactions observed with terbutaline sulfate are similar to those commonly seen with other sympathomimetic amines. All of these reactions are generally transient in nature and usually do not require treatment. The frequency of these side effects appears to diminish with continued therapy. The following table lists the adverse reactions seen in 199 patients treated with terbutaline sulfate… See the full label for the complete list.
Who makes Terbutaline Sulfate?
Terbutaline Sulfate is listed by 10 labelers in the FDA NDC directory, including Amneal Pharmaceuticals of New York LLC, Chartwell RX, LLC., Fresenius Kabi USA, LLC, Henry Schein, Inc..