Bricanyl

Bricanyl

terbutaline

Manufacturer:

AstraZeneca

Distributor:

Zuellig
Full Prescribing Info
Contents
Terbutaline sulfate.
Description
Tablet: One tablet contains 2.5 mg terbutaline sulfate.
Injection: 1 mL contains terbutaline sulfate 500 mcg.
Action
Pharmacotherapeutic Group: Selective β2-agonist, terbutaline. ATC Code: R03C C03.
Pharmacology: Pharmacodynamics: 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 in obstructive lung diseases and, thereby, facilitates the transport of viscous secretion, and relaxation of the uterine muscle.
The bronchodilating effect of Terbutaline sulfate (BRICANYL) tablets has in clinical trials been shown to have a duration for up to 8 hours.
Injection: After a subcutaneous injection of terbutaline, the duration of onset regarding the bronchodilating effect is less than 5 minutes. Maximum effect is reached within 30 minutes.
Pharmacokinetics: Tablet: There is a 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 sulphuric acid and excreted as the sulfate conjugate. No active metabolites are formed.
Injection: Terbutaline is metabolized mainly by conjugation with sulphuric acid and excreted as the sulfate conjugate. No active metabolites are formed. The plasma half life is about 16 hours. After intravenous and subcutaneous administration of terbutaline 90% is excreted renally during 48-96 hours. Of this, about 60% consists of unmetabolized terbutaline.
Toxicology: Preclinical Safety Data: The major toxic effect of terbutaline, observed in toxicological studies, is focal myocardial necrosis. This type of cardiotoxicity is a 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.
Indications/Uses
Bronchial asthma. Chronic bronchitis, emphysema and other lung diseases where bronchospasm is a complicating factor. Pre-term labor.
Dosage/Direction for Use
Tablet: Terbutaline sulfate (BRICANYL) tablets should be used as maintenance therapy in asthma and other pulmonary diseases where bronchospasm is a complicating factor. Preterm labour.
Dosage should be individually titrated.
Bronchospasm: Adults: During the first 1-2 weeks 2.5 mg (1 tablet) 3 times in a 24 h period is recommended. The dose may then, if necessary, be increased to 5 mg (2 tablets) 3 times in 24 hours.
Children: 0.075 mg/kg body weight 3 times in 24 hours.
Suitable dosage: 20 kg: ¼-½ tablet 3 times in 24 hours.
20-30 kg: ½-1 tablet 3 times in 24 hours.
>30 kg:
1-2 tablets 3 times in 24 hours.
Preterm Labour: The drug must be individually titrated. Pulse rate and blood pressure should be carefully monitored during treatment. Initially 5 ug/min I.V. of Terbutaline sulfate (BRICANYL) solution for injection could be given as an infusion during 20 minutes. The dose can then be increased by 2.5 ug/min at 20 minutes intervals until contractions stop. More than 10 ug/min should seldom be given and 20 ug/min should not be exceeded. Let the infusion continue for 1 h at the chosen infusion rate, and then decrease the rate of infusion in steps of 2.5 ug/min at 20 minutes interval down to the lowest maintenance dose that produces continued suppression of the contractions. Keep the infusion at this rate for 12 h and then continue with oral maintenance therapy (5 mg x 3).
The oral treatment should be continued until the end of the 36th week of pregnancy. As an alternative treatment, subcutaneous injections (0.25 mg four times in a 24 h period) could be given for a few days before oral treatment is started.
Injection: The dose may be given intravenously or subcutaneously.
Terbutaline sulfate (BRICANYL) solution for injection, 1 mL ampoule, is intended for subcutaneous and intravenous injection.
Terbutaline sulfate (BRICANYL) solution for injection, 5 mL ampoule, is intended for infusion after dilution with infusion solutions.
Dosage should be individual.
Bronchospasm: Intravenous Injection: Adults: 0.25-0.5 mg (0.5-1 mL) is injected slowly intravenously. The solution for injection is diluted with sterile physiological saline up to 10 mL and is given slowly intravenously during 5 minutes. The dose may have to be repeated with short intervals (a few hours). The dose should not exceed 2 mg in 24 hours.
Intravenous Infusion: Adults: 1-2 mg (2-4 mL) is given during a 24 hour interval as a continuous infusion. An initial loading dose up to 0.10 mg (0.2 mL) can be given over 10 minutes.
Children: Up to 25 μg/kg b.w. (0.05 mL/kg b.w.) is given during a 24 hour interval as a continuous infusion. An initial loading dose up to 1.5 μg/kg b.w. (0.003 mL/kg b.w.) can be given over 10 minutes.
Subcutaneous Injection: Adults: 1-2 mg (2-4 mL) is given during a 24 hour interval, split into at least 4 occasions.
Children: Up to 25 μg/kg b.w. (0.05 mL/kg b.w.) is given during a 24 hour interval, split into at least 4 occasions.
Preterm Labour: The dose must be individually titrated. Pulse rate and blood pressure should be carefully monitored during treatment. Initially 5 μg/min could be given as an infusion during 20 minutes. The dose can then be increased by 2.5 μg/min at 20 minute intervals until contractions stop. More than 10 μg/min should seldom be given, and 20 μg/min should not be exceeded. Let the infusion continue for 1 h at the chosen infusion rate, and then decrease the rate of infusion in steps of 2.5 μg/min at 20 minute intervals down to the lowest maintenance dose that produces continued suppression of the contractions. Keep the infusion at this rate for 12 h and then continue with oral maintenance therapy (5 mg x 3).
The oral treatment should be continued until the end of the 36th week of pregnancy. As an alternative treatment, subcutaneous injections (0.25 mg four times in a 24 h period) could be given for a few days before oral treatment is started.
Suggestion for Dilution: 5 mg (2 ampoules of 5 mL) in 1000 mL of dextrose solution or physiological saline. Prepared solution contains 5 μg/mL and should be used within 12 hours. Terbutaline sulfate (BRICANYL) should not be diluted in alkaline solutions. Saline should be avoided during pregnancy since the risk of producing pulmonary edema may increase when this diluent is used in pregnant women. If saline has to be used, the patient should be carefully monitored. Terbutaline sulfate (BRICANYL) can be added to infusion solutions in glass bottles as well as in PVC plastic bags.
Overdosage
Symptoms: Headache, anxiety, tremor, nausea, tonic muscle cramps, palpitations, tachycardia and cardiac arrhythmias. A fall in blood pressure sometimes occurs.
Laboratory Findings: Hyperglycemia and lactic acidosis sometimes occur. β2-agonists may cause hypokalemia as a result of redistribution of potassium.
Treatment: 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 balance, blood glucose and electrolytes.
Monitor heart rate and rhythm, and blood pressure. The preferred antidote for overdosage with Terbutaline sulfate (BRICANYL) is a cardioselective beta-receptor blocking agent, but it should be used with caution in patients with a history of bronchospasm.
If the β2-mediated reduction in peripheral vascular resistance significantly contributes to the fall in blood pressure, a volume expander should be given.
Injection: Preterm Labour: Pulmonary Edema: A normal dose of loop diuretic (eg, furosemide) should be given intravenously. Increased tendency to bleeding in connection with caesarea section: Give propranolol, 1-2 mg intravenously.
Contraindications
Tablet: Hypersensitivity to any of the ingredients.
Injection: Hypersensitivity to any of the ingredients. In obstetrics: Intrauterine infection, severe preeclampsia, ablatio placentae.
Special Precautions
As for all β2-agonists, caution should be observed in patients with thyrotoxicosis and in patients with severe cardiovascular disorders eg, 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 are monitored in such situations.
Effects on the Ability to Drive and Use Machines: Terbutaline sulfate (BRICANYL) does not affect the ability to drive or use machines.
Use in Pregnancy & Lactation: No teratogenic effects have been observed in patients or in animals. However, caution is recommended during the first trimester of pregnancy. 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.
Use In Pregnancy & Lactation
No teratogenic effects have been observed in patients or in animals. However, caution is recommended during the first trimester of pregnancy.
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.
Adverse Reactions
The intensity of the adverse reactions depends on dosage and route of administration. An initial dose titration will often reduce the adverse reactions. Adverse reactions which have been recorded, e.g. tremor, headache, tonic muscle cramps, tachycardia and palpitations, are all characteristic of sympathomimetic amines. The majority of these effects have reversed spontaneously within the first 1-2 weeks of treatment.
As for all β2-agonist, cardiac arrhythmias, e.g. atrial fibrillation, supraventricular tachycardia and extrasystole have been rarely reported.
Urticaria and exanthema may occur.
Sleep disturbances and behavioural disturbances, such as agitation, hyperactivity and restlessness, have been observed.
Injection: During treatment of preterm labour, when high doses of Terbutaline sulfate (BRICANYL) are used, diabetic mothers may develop hyperglycaemia and lactacidosis. In these patients glucose and acid-base balance should be carefully monitored. High doses of β2-stimulants may cause hypokalemia as a result of redistribution of potassium. Symptoms of pulmonary edema have also been reported following treatment of preterm labour. An increased tendency to bleeding has been described in connection with caesarean section (give Propranolol, 1-2 mg i.v.) in patients treated with Terbutaline sulfate (BRICANYL) for preterm labour.
Drug 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).
Caution For Usage
Incompatibilities: Tablet: Not applicable.
Injection: Terbutaline sulfate (BRICANYL) solution for injection should not be mixed with alkaline solutions, i.e. solutions with a pH higher than 7.0.
Storage
Tablet: Store at a temperature not exceeding 30°C.
Injection: Store at a temperature not exceeding 30°C. Protect from light.
ATC Classification
R03CC03 - terbutaline ; Belongs to the class of adrenergics for systemic use, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
Presentation/Packing
Tab 2.5 mg x 500's. Inj (amp) 0.5 mg/mL x 1 mL x 10's.
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