Terbutaline aifenesin Sulfate Gu

Terbutaline Sulfate
Guaifenesin
Bricanyl® Expectorant
1.5 mg/ 66.5 mg per 5 mL Syrup
Antiasthma
FORMULATION
Each teaspoon (5 mL) contains 1.5 mg terbutaline sulfate and 66.5 mg guaifenesin.
PHARMACODYNAMIC PROPERTIES
Terbutaline is an adrenergic agonist which predominantly stimulates β2-receptors, thus
producing relaxation of bronchial smooth muscle, inhibition of the release of endogenous
spasmogens, inhibition of edema caused by endogenous mediators, increased mucociliary
clearance and relaxation of the uterine muscle.
Guaifenesin is considered to give less viscous mucus production in the airways, to facilitate
expectoration and to relieve cough.
The bronchodilating effect of Terbutaline Sulfate/Guaifenesin (Bricanyl Expectorant) has in
clinical trials been shown to have a duration of up to 8 hours.
PHARMACOKINETIC PROPERTIES
There is considerable first-pass metabolism in the intestinal wall and in the liver. The
bioavailability is around 10% and increases to around 15% if terbutaline is taken on an empty
stomach. Maximum plasma concentration of terbutaline is reached within 3 hours. Terbutaline is
metabolized mainly by conjugation with sulfuric acid and excreted as the sulfate conjugate. No
active metabolites are formed.
INDICATIONS
Bronchial asthma, chronic bronchitis, emphysema and other lung diseases where
bronchospasm and secretion are complicating factors.
DOSAGE
Terbutaline Sulfate/Guaifenesin (Bricanyl Expectorant) should be used as maintenance therapy
in asthma and other pulmonary diseases where bronchospasm and secretion are complicating
factors.
Dosage should be individual.
Bricanyl Expectorant_ RITA.000-033-159.1.0
Page 1 of 4
Adults: 3 - 4.5 mg (10 – 15 mL) 3 times a day.
Children: 0.075 mg (0.25 mL)/kg body weight 3 times a day.
Suitable dosage:
Body Weight (kg)
4
6
8
10
12
14
16
Dosage
1 mL x 3
1.5 mL x 3
2 mL x 3
2.5 mL x3
3 mL x 3
3.5 mL x 3
4 mL x 3
Body Weight (kg)
18
20
24
28
32
36
40
Dosage
4.5 mL x 3
5 mL x 3
6 mL x 3
7 mL x 3
8 mL x 3
9 mL x 3
10 mL x 3
If an adequate response is not obtained with this dose, the dose may be doubled, provided
adverse reactions are not pronounced.
PRECAUTIONS
As for all β2-agonists, caution should be observed in patients with thyrotoxicosis and in patients
with severe cardiovascular disorder, such as ischemic heart disease, tachyarrhythmias or
severe heart failure.
Due to the hyperglycemic effects of β2-agonists, additional blood glucose controls are
recommended initially in diabetic patients.
Potentially serious hypokalemia may result from β2-agonist therapy. Particular caution is
recommended in acute severe asthma as the associated risk may be augmented by hypoxia.
The hypokalemic effect may be potentiated by concomitant treatments (see Interactions). It is
recommended that serum potassium levels be monitored in such situations.
INTERACTIONS
Beta-receptor blocking agents (including eye drops), especially those that are non-selective,
may partly or totally inhibit the effect of beta-receptor stimulants.
Hypokalemia may result from β2-agonist therapy and may be potentiated by concomitant
treatment with xanthine derivatives, steroids and diuretics (see Precautions).
PREGNANCY AND LACTATION
No teratogenic effects have been observed in patients or animals. However, caution is
recommended during the first trimester of pregnancy.
Bricanyl Expectorant_ RITA.000-033-159.1.0
Page 2 of 4
Terbutaline passes over to breast milk but an influence on the child is unlikely with therapeutic
doses.
Transient hypoglycemia has been reported in newborn preterm infants after maternal β2-agonist
treatment.
EFFECTS ON ABILITY TO DRIVE AND USE MACHINES
Terbutaline Sulfate/Guaifenesin (Bricanyl Expectorant) does not affect the ability to drive or use
machines.
UNDESIRABLE EFFECTS
The intensity of the adverse reactions depends on dosage and route of administration. Adverse
reactions which have been recorded, e.g. tremor, headache, tonic muscle cramps and
palpitations, are all characteristics of sympathomimetic amines. The majority of these effects
have reverse spontaneously within the first 1 – 2 weeks of treatment.
As for all β2-agonists, cardiac arrhythmias, e.g. atrial fibrillation, supraventricular tachycardia
and extrasystoles have been rarely reported.
Urticaria and exanthema may occur.
Sleep disturbances and behavioral disturbances, such as agitation, hyperactivity and
restlessness, have been observed.
OVERDOSE
Possible symptoms and signs: Headache, anxiety, tremor, nausea, tonic muscle cramps,
palpitations, tachycardia and cardiac arrhythmias. A fall in blood pressure sometimes occurs.
Laboratory findings: Hyperglycemia and lactacidosis sometimes occur. β2-agonists may cause
hypokalemia as a result of redistribution of potassium.
Treatment of Overdosage:
Usually no treatment is required. If it is suspected that significant amounts of terbutaline sulfate
have been swallowed, the following measures should be considered.
Gastric lavage, activated charcoal. Determine acid-base balanced, blood glucose and
electrolytes. Monitor heart rate and rhythm and blood pressure. The preferred antidote for
overdosage with Bricanyl is a cardioselective beta-receptor blocking agent, but beta-receptor
blocking drugs should be used with caution in patients with a history of bronchospasm. If the β2mediated reduction in peripheral vascular resistance significantly contributes to the fall in blood
pressure, a volume expander should be given.
Bricanyl Expectorant_ RITA.000-033-159.1.0
Page 3 of 4
PRECLINICAL SAFETY DATA
The major toxic effect of terbutaline, observed in toxicological studies, is focal myocardial
necrosis. This type of cardiotoxicity is well known class-effect, and the effect of terbutaline is
similar to or less pronounced than that of other β-receptor agonists. Terbutaline has been used
extensively over many years for the relief of bronchospasm without identifying any areas of
concern.
STORAGE
Store at a temperature not exceeding 30°C.
AVAILABILITY
Bottles of 60 mL and 120 mL.
CAUTION
Foods, Drugs, Devices and Cosmetics Act prohibits dispensing without prescription.
VALIDITY CODE
RITA.000-033-159.1.0
CDS dated 26 Mar 2002
Bricanyl is a trademark of the AstraZeneca group of companies.
Bricanyl Expectorant_ RITA.000-033-159.1.0
Page 4 of 4