Terbutaline Sulfate
Pronunciation: (ter-BYOO-tuh-leen SULL-fate)Class: Sympathomimetic
Trade Names:
Brethaire
- Aerosol 0.2 mg/actuation
Trade Names:
Brethine
- Tablets 2.5 mg
- Tablets 5 mg
- Injection 1 mg/mL
Trade Names:
Bricanyl
- Tablets 2.5 mg
- Tablets 5 mg
- Injection 1 mg/mL
Pharmacology
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Produces bronchodilation by relaxing bronchial smooth muscle through beta 2 -receptor stimulation.
Pharmacokinetics
Absorption
Terbutaline C max is approximately 8.5 ng/mL; T max is about 1 to 3 h, and AUC is approximately 54 h•ng/mL. Terbutaline bioavailability is 103%.
Metabolism
The sulfate conjugate is the major metabolite.
Elimination
Terbutaline t ½ is about 3.4 h. Approximately 90% is excreted in urine at 96 h after subcutaneous administration, with about 60% being unchanged drug. Urinary excretion is the primary route of elimination.
Onset
Onset of action is 30 min.
Peak
Time to peak effect of terbutaline is 120 to 180 min.
Duration
Duration of action is 4 h or longer.
Indications and Usage
Treatment of reversible bronchospasm associated with asthma, bronchitis, and emphysema.
Contraindications
Cardiac arrhythmias associated with tachycardia.
Dosage and Administration
Adults and Children older than 15 yr of agePO 2.5 to 5 mg at 6 h intervals, 3 times daily during waking hours. Do not exceed 15 mg in 24 h.
Children 12 to 15 yr of agePO 2.5 mg 3 times daily. Do not exceed 7.5 mg in 24 h. Subcutaneous 0.25 mg given in lateral deltoid area. May repeat in 15 to 30 min. Do not exceed 0.5 mg in 4 h.
General Advice
- For IV administration, obtain baseline potassium level prior to administration and place patient on cardiac monitor to assess for tachycardia or arrhythmias. Toxic symptoms have been documented in patients with CV disorders.
- Do not allow patient to use inhaler form of medication more than 6 times/day.
- Limit subcutaneous doses to up to 0.5 mg in 4 h.
Storage/Stability
Store at room temperature. Protect from light.
Drug Interactions
Beta-blockersBlock bronchodilator effect of terbutaline.
MAOIsHypertension may occur.
Tricyclic antidepressantsCV effects of terbutaline may be enhanced.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Palpitations; tachycardia; chest discomfort or pain; arrhythmias; BP changes/hypertension.
CNS
Stimulation; tremor; dizziness; nervousness; drowsiness; headache; weakness.
GI
Nausea; vomiting; GI distress.
Hepatic
Elevated liver enzymes.
Metabolic
Hypokalemia (with high doses).
Respiratory
Dyspnea.
Miscellaneous
Flushing; sweating; muscle cramps; hypersensitivity vasculitis; ECG changes (eg, sinus pause, atrial premature beats, AV block, ventricular premature beats, ST-T-wave depression, T-wave inversion, sinus bradycardia, atrial escape beat with aberrant conduction); increased heart rate; muscle cramps; central stimulations; pain at injection site; elevations in liver enzymes; seizures; hypersensitivity vasculitis.
Precautions
Pregnancy
Category B .
Lactation
Excreted in breast milk.
Children
Safety and efficacy in children younger than 12 yr of age not established.
Elderly
Lower doses may be required.
Labor and Delivery
May inhibit uterine contractions and delay preterm labor.
Hypersensitivity
Hypersensitivity (allergic) reactions can occur after administration.
Carcinogenesis
A significant increase in the incidence of leiomyomas of the mesovarium and ovarian cysts has been demonstrated.
CV effects
Toxic symptoms in patients with CV disorders may occur.
CNS effects
CNS stimulation may occur; use cautiously in patients with history of seizures or hyperthyroidism.
Diabetes
Dosage adjustment of insulin or oral hypoglycemic agent may be required.
Excessive use
Paradoxical bronchospasm and cardiac arrest have been associated with excessive inhalant use.
Hypokalemia
Decreases in potassium levels have occurred.
Tolerance
If previously effective dose fails to provide relief, therapy may need to be reassessed.
Overdosage
Symptoms
Tremor, palpitations, increased heart rate, decreased BP, seizures, hypokalemia, muscle cramps, headache, hyperglycemia.
Patient Information
- Instruct patient on proper technique for use of inhalers and evaluate return demonstration.
- Demonstrate use of spacer or peak flow meter if prescribed.
- Caution patient not to use inhaler form of medication more than 6 times/day.
- Advise patient to take tablets with food to avoid GI upset.
- Inform patient that the drug can stop working over time. If this is noted or if the inhalation makes breathing worse, notify the health care provider at once.
- Instruct patient to report these symptoms to health care provider: chest pain, dizziness or headache, persisting symptoms of asthma.
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