terbutaline sulphate
Selective Bronchodilator
Composition
Each ml of solution for injection contains Terbutaline sulphate 0.5 mg.
Characteristics
Pharmacodynamic properties
Terbutaline is a sympathomimetic bronchodilator with a degree of selective β2 stimulant activity on the respiratory system, thus producing relaxation of bronchial smooth muscle, inhibiton of the release of endogenous spasmogens, inhibition of edema caused by endogenous mediators, increased mucociliary clearance.
After subcutaneous injection of terbutaline the duration of onset regarding the bronchodilating effect is less than 5 minutes. Maximum effect is reached within 30 minutes.
Pharmacokinetic properties
Terbutaline is metabolized mainly by conjugation, with the sulphuric acid and excreted as the sulphate 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.
Indication
'Bricasma' is indicating for the relief of bronchospasm in bronchial asthma and other bronchopulmonary disorders in which bronchospasm is a complicating factor.
Dosage and administration
The dose may be given intravenously or subcutaneously.
'Bricasma' injection, 1 ml ampoule, is intended for subcutaneous and intravenous injection.
Dosage should be individual.
Bronchospasm:
Intravenous injection
Adult: 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.
Contraindications
Patients with a history of hypersensitivity to any of its component or sympathomimetic amines.
Interaction with other medicaments and other forms of interaction
Beta-receptor blocking agent (including eye drops), especially those which are non selective may partly or totally inhibit the effect of β-receptor stimulants.
Hypokalemia may result from β2-agonist therapy and may be potentiated by concomitant treatment with xanthine derivatives, steroids and diuretics (see 'Warning and Precautions').
Side effects
Potentially serious hypokalaemia may result from β2-agonist therapy (see in 'Warning and Precautions').
In common with other β2-agonist maternal pulmonary oedema has been reported in association with the use of terbutaline for the management of premature labour; in some cases this has proved fatal. Predisposing factors include fluid overload, multiple pregnancy, pre-existing cardiac disease and maternal infection. Close monitoring of the patient's state of hydration is essential. If signs of pulmonary oedema develop (e.g. cough, shortness of breath), treatment should be discontinued immediately and diuretic therapy instituted.
The intensity of the adverse reactions depends on dosage and route of administration. An initial dose titration will often reduce the adverse reactions. Adverse reaction which have been recorded e.g. tremor, headache, tonic muscle cramp and palpitations, are all characteristic of sympathomimetic amines. The majority of these effect have reversed spontaneously within the first 1-2 weeks
of treatment.
Urticaria and exanthema may occur.
Sleep disturbances and behavioural disturbances, such as agitation, hyperactivity and restlessness, have been observed.
Other commonly reported reactions include increased heart rate and dizziness.
Other reported reactions include headache, drowsiness, vomiting, nausea, sweating, and muscle cramps. These reactions are generally transient and usually do not require treatment.
There have been rare reports of elevations in liver enzymes and of hypersensitivity vasculitis.
Precaution
As for all β2-agonist caution should be observed in patient with thyrotoxicosis and in patients with severe cardiovascular disorder, such as ischemic heart disease, tachyarrhythmias or severe heart failure.
Due to the hyperglycemic effect of β2-agonist, additional blood glucose controls are recommended initially in diabetic patients. If treatment becomes less effective or shorter acting, the patient's general condition should be reviewed.
Due to the positive inotropic effect of β2-agonist these drugs should not be used in patients with hypertrophic cardiomyopathy.
As terbutaline sulphate is largely excreted in urine, caution should be exercised in patients with renal impairment.
Increased tendency to uterine bleeding has been reported in connection with Caesarean section. However, this can be effectively stopped by propanolol 1-2 mg injected intravenously.
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 treatment (see Interactions). It is recommended that serum potassium levels are monitored in such situations.
Terbutaline is not indicated and should not be used for the management of preterm labor. Serious adverse reactions have been reported following administration of Terbutaline sulphate to women in labor.
These reports have included transient hypokalemia, pulmonary edema (sometimes after delivery), and hypoglycemia in the mother and / or neonatal child. Maternal death has been reported with terbutaline sulphate and other drugs of this class.
There have been rare reports of seizures occurring in patients receiving terbutaline, which do not recur when the drug is discontinued and have not been explained on any other basis.
Terbutaline sulphate is a sympathomimetic amine and such should be used with caution in patients with cardiovascular disorders (including arrythmias, coronary insufficiency and hypertension), in patients with hyperthyroidism or diabetes mellitus, history of seizures, or in patients who are unusually responsive to sympathomimetic amines.
Patients susceptible to hypokalemia should be monitored because transient early alls in serum potassium levels have been reported with β2-agonist.
Immediate hypersensitivity reactions and exacerbation of bronchospasm have been reported after terbutaline administration.
There are, however, no adequate and well controlled studies in pregnant women, this drug should be used during pregnancy only if clearly needed.
Terbutaline is excreted in breast milk. Caution should be exercised when this drug is administered to a nursing woman.
Safety and effectiveness in children below the age of 12 have not been established.
Overdosage
Too frequent administration, as with other sympathomimetic agents, may cause nausea, headaches, changes in blood pressure, anxiety, tension, insomnia, tremor. The symptoms and sign are those characteristic of excessive sympathetic stimulation.
Possible symptoms and signs: Headache, anxiety, tremor, tonic muscle cramps, palpitation, arrhythmia. 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. In severe cases of overdosage, the following measures should be considered:
Determine acid-base balance, blood glucose and electrolytes. Monitor heart rate and rhythm and blood pressure. The preferred antidote for overdosage with 'Bricasma' 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 β2-mediated reduction in peripheral vascular resistance significantly contributes to the fall in blood pressure, a volume expander should be given.
Effect on ability to drive and use machines
'Bricasma' does not affect the ability to drive or use machines.
Incompatiilities
'Bricasma' solution for injection should not be mixed with alkaline solutions, i.e.: solution with the pH higher than 7.0.
Presentation
Box of 5 ampoules @ 1 ml
(Reg. No.: DKI0451302243A1)
The ampoules should be stored at temperatures not exceeding 25°C and be protected from light.
HARUS DENGAN RESEP DOKTER
Manufactured by:
AstraZeneca AB, Sodertalje, Sweden
Imported by:
PT AstraZeneca Indonesia
Jakarta - Indonesia
Trade Marks herein are the property of the AstraZeneca group
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