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terbutaline (Brethaire, Brethine, Bricanyl)

 

Classes: Beta2 Agonists; Extravasation Antidotes

Dosing and uses of Brethaire, Brethine (terbutaline)

 

Adult dosage forms and strengths

tablet

  • 2.5mg
  • 5mg

injectable solution

  • 1mg/mL

 

Bronchospasm

PO

  • Initiate at 2.5 mg three/four times daily PO
  • Maintenance: 5 mg three times daily PO q6hr while patient is awake; reduce dose to 2.5 mg q6hr
  • Not to exceed 15 mg/Day

SC

  • 0.25 mg q15-30min x 3 doses PRN in lateral deltoid
  • Not to exceed 0.5 mg/4 hr

 

Preterm Labor (Off-label)

Initiate at 2.5-5 mcg/min IV

Increase gradually as tolerated at 20-30 minute intervals

Typical effective dose ranges between 17.5-30 mcg/min IV; some require doses up to 70-80 mcg/min

Continue infusion for 12 hr following cessation of uterine contractions; not to exceed 48-72 hr

PO use or prolonged IV use not recommended (see Black box warnings)

 

Renal Impairment

GFR <50 mL/min: reduce dose by 50%

GFR >50mL/min: Dose adjustment not necessary

 

Pediatric dosage forms and strengths

tablet

  • 2.5mg
  • 5mg

injectable solution

  • 1mg/mL

 

Bronchospasm

PO

  • <12 years: 0.05 mg/kg three times daily initially; increase PRN, not to exceed 5 mg/day
  • 12-15 years: 2.5 mg PO q6hr 3 times daily; not to exceed 7.5 mg/day
  • >15 years: 5 mg/dose PO q8hr three times daily; reduce dose to 2.5 mg q6hr; not to exceed 15 mg/24hr

SC (in lateral deltoid)

  • <12 years: 0.005-0.01 mg/kg (no more than 0.4 mg) q15-20min x 3; THEN q2-6hour PRN
  • >12 years: 0.25 mg q15-30min x 3 doses PRN in lateral deltoid; not to exceed 0.5 mg/4 hr

 

Brethaire, Brethine (terbutaline) adverse (side) effects

Frequency not defined

Nervousness

Restlessness

Transient hyperglycemia

Transient hypokalemia

Trembling

Tachycardia

HTn

Pounding heartbeat

Dizziness

Lightheadedness

Drowsiness

Headache

Insomnia

Dry mouth

Nausea

Vomiting

Bad taste in mouth

Muscle cramps

Weakness

Diaphoresis

Cardiac arrhythmias

Pulmonary edema

Myocardial ischemia

Myocardial infarction

Increased fetal heart rate

Hypoglycemia in some neonates born to women who received drug during labor

 

Warnings

Black box warnings

Risk of serious adverse events outweighs potential benefit to pregnant women receiving prlonged treatment with terbutaline injection (ie, >48-72 hr), or acute or prolonged treatment with oral terbutaline

Oral terbutaline should not be used for prevention or any treatment of preterm labor because efficacy has not been established and safety concerns similar to IV administration exist

Death and serious adverse reactions have been reported following prolonged administration of oral or injectable terbutaline to pregnant women

Serious events following prolonged use include tachycardia, transient hyperglycemia, hypokalemia, arrhythmias, pulmonary edema, and myocardial ischemia

 

Contraindications

Hypersensitivity to sympathomimetics

Use >72 hr in management or prevention of preterm labor

Oral administration in preterm labor

 

Cautions

Diabetes mellitus

Hypertension

Hyperthyroidism

History of seizures

History of cardiac disease, including ischemic heart disease or associated arrhythmias

Paradoxical bronchoconstriction may occur with excessive use

Fatalities reported with excessive use of sympathomimetics

Optimize anti-inflammatory treatment prior to administering terbutaline for asthma therapy

Beta-2 agonists may increase serum glucose; use caution in patients with diabetes mellitus

Use caution in glaucoma, hyperthyroidism, seizure disorders, and hypokalemia

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Distributed into breast milk, but in amounts generally considered insufficient to affect nursing infants (AAP Committee states compatible with nursing)

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Brethaire, Brethine (terbutaline)

Mechanism of action

Beta adrenergic receptor stimulator causing bronchial/uterine smooth muscle relaxation

 

Pharmacokinetics

Onset: 30-45 min (PO); 6-15 min (SC)

Duration: 90 min-4 hr

Peak plasma time: 30-60 min

Half-life: 11-16 hr

Protein binding: 25%

Absorbtion: 33-50%

Metabolism: Partially metabolized in liver, mainly to inactive sulfate conjugate

Excretion: 60% urine unchanged, up to 3% feces via bile; remainder in urine as the conjugate (w/ parenteral admin)

 

Administration

IV Preparation

Solution: dilute as required in D5W (available form: 1 mg/mL)

Administration: use infusion pump

Protect inj from light

Do not use if discolored