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terbutaline (Brethine, Bricanyl, Brethaine)
Tradenames: Brethine, Bricanyl, Brethaine.
Indications:
- bronchospasm
- chronic obstructive pulmonary disease (COPD)
- asthma
- bronchiectasis
- bronchitis
Contraindications:
- management of preterm labor (potential for maternal heart problems & death) [4]
Dosage:
1) 0.25 mg SC; may repeat in 15 minutes; hourly max: 0.5 mg
2) inhaler: 2 puffs every 4-6 hours
3) oral: 2.5-5 mg PO TID-QID; max 15 mg/day
4) 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:
1) subcutaneous
a) well absorbed
b) onset of action 15 minutes
c) duration of action: 60-240 minutes
2) oral
a) 50% absorbed
b) largely metabolized by 1st pass hepatic metabolism
c) onset of action: 30 minutes
d) duration of action: 4-8 hours
3) metabolized by the liver
4) eliminated in the urine
5) complete elimination is seen 2-3 days after a single dose
Adverse effects:
1) common (> 10%)
- nervousness, restlessness, trembling
2) less common (1-10%)
- dizziness, drowsiness, dry mouth, tachycardia, headache, diaphoresis, hypertension, muscle cramps, nausea/vomiting, insomnia, weakness, bad taste in mouth
3) uncommon (< 1%)
- chest pain, cardiac arrhythmias, paradoxical bronchospasm
4) other
- palpitations
- tremor
- hypokalemia
Drug interactions:
1) beta blockers: antagonize effects of terbutaline
2) MAO inhibitors, tricyclic antidepressants: increase cardiovascular toxicity
Mechanism of action:
1) beta-2 adrenergic receptor agonist
2) relaxation of bronchial tree
3) peripheral vasodilation
4) relaxes GI & uterine smooth muscle
5) high doses can cause tachycardia & CNS stimulation
Interactions
drug interactions
drug adverse effects (more general classes)
General
antiasthmatic agent
inhaled beta-2 adrenergic receptor agonist
Properties
AGONIST-FOR: beta-2 adrenergic receptor
MISC-INFO: elimination route LIVER
pregnancy-category B
safety in lactation -
Database Correlations
PUBCHEM correlations
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
- 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