terbutaline (Brethine, Bricanyl, Brethaine)
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Introduction
Tradenames: Brethine, Bricanyl, Brethaine.
Indications
Contraindications
- management of preterm labor (potential for maternal heart problems & death)[4]
Dosage
- 0.25 mg SC; may repeat in 15 minutes; hourly max: 0.5 mg
- inhaler: 2 puffs every 4-6 hours
- oral: 2.5-5 mg PO TID-QID; max 15 mg/day
- children 12-15 yo: 2.5 mg PO TID. <12 yo: DO NOT USE
Tabs: 2.5 & 5 mg.
Aerosol: 0.2 mg/actuation (10.5 g)
Injection: 1 mg/mL (1 mL). Dose adjustment in renal failure:
| creatinine clearance | dosage |
|---|---|
| 10-50 mL/min | 50% |
| < 10 mL/min | avoid usage |
Pharmacokinetics
- subcutaneous
- well absorbed
- onset of action 15 minutes
- duration of action: 60-240 minutes
- oral
- 50% absorbed
- largely metabolized by 1st pass hepatic metabolism
- onset of action: 30 minutes
- duration of action: 4-8 hours
- metabolized by the liver
- eliminated in the urine
- complete elimination is seen 2-3 days after a single dose
elimination via liver
Adverse effects
- common (> 10%)
- nervousness, restlessness, trembling
- less common (1-10%)
- dizziness, drowsiness, dry mouth, tachycardia, headache, diaphoresis, hypertension, muscle cramps, nausea/vomiting, insomnia, weakness, bad taste in mouth
- uncommon (< 1%)
- other
- drug adverse effects of adrenergic receptor agonists
- drug adverse effects of beta-adrenergic receptor agonists
- drug adverse effects of sympathomimetic(s)
Drug interactions
- beta blockers: antagonize effects of terbutaline
- MAO inhibitors, tricyclic antidepressants: increase cardiovascular toxicity
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of beta-2 adrenergic receptor agonists with loop diuretics
- drug interaction(s) of beta-2 adrenergic receptor agonists with thiazide diuretics
Mechanism of action
- beta-2 adrenergic receptor agonist
- relaxation of bronchial tree
- peripheral vasodilation
- relaxes GI & uterine smooth muscle
- high doses can cause tachycardia & CNS stimulation
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 FDA MedWatch, Feb 17, 2011 Terbutaline: Label Change - Warnings Against Use for Treatment of Preterm Labor http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm243843.htm
- ↑ Deprecated Reference