BRICANYL® Tablets BRICANYL® TURBUHALER®
Action And Clinical Pharmacology: Terbutaline produces bronchodilation by stimulation of the B2 adrenergic receptors in bronchial smooth muscle, thereby causing relaxation of muscle fibres. This action is manifested by an increase in pulmonary function as demonstrated by FEV1 measurements. Terbutaline also produces a decrease in airway and pulmonary resistance.
Following inhalation of terbutaline Turbuhaler, a significant improvement in pulmonary function measurements is well established after 5 minutes. Twenty to 30% of the metered dose is deposited in the lungs with an inspiration flow rate of about 60 L/min.
The maximal response is usually attained between 15 and 60 minutes following administration. Significant bronchodilator activity has been observed to persist for 4 to 7 hours.
Following administration of terbutaline tablets, a measurable change in flow rate is usually observed in 30 minutes, and improvement in pulmonary function occurs in 60 to 120 minutes. The maximum effect usually occurs within 120 to 180 minutes, and significant bronchodilator activity has been observed to persist for 4 to 8 hours.
Indications And Clinical Uses: For the symptomatic relief of bronchial asthma and for relief of reversible bronchospasm which may occur in association with bronchitis and emphysema.
Contra-Indications: Known hypersensitivity to sympathomimetic amines and, like other sympathomimetic amines, should not be used in patients with tachyarrhythmias.
Manufacturers’ Warnings In Clinical States: Like other b2-agonist inhalers, terbutaline should not be used on a regular daily basis without appropriate concomitant anti-inflammatory therapy (see Dosage).
Terbutaline should be used with caution in patients with diabetes, hypertension, hyperthyroidism and a history of seizures. As with other sympathomimetic bronchodilator agents, terbutaline should be administered cautiously to cardiac patients, especially those with associated arrhythmias, and coronary insufficiency, to elderly or to patients who are unusually responsive to sympathomimetic amines. Due to the hyperglycemic effects of b2-agonists, additional blood glucose controls are recommended initially in diabetic patients.
Occasionally, patients have been reported to have developed severe paradoxical bronchospasm with repeated use of sympathomimetic inhalant preparations. In such instances, the preparation should be discontinued immediately and alternate therapy instituted. Fatalities, the exact cause of which are unknown, have been reported following excessive use of aerosol preparations containing sympathomimetic amines. Cardiac arrest was noted in several instances.
Beta-receptor blocking agents (including eye-drops), especially those which are noncardioselective, may partially or totally inhibit the effect of beta-receptor stimulants. Severe resistant bronchospasm may be produced with the use of beta-blockers in asthmatic patients.
Potentially serious hypokalemia may result from B2-agonist therapy, mainly from parenteral or nebulized administration. Particular caution is advised in acute severe asthma as this may be potentiated by hypoxia and concomitant treatment with xanthine derivatives, steroids and diuretics; it is recommended that serum potassium levels be monitored in such situations.
Pregnancy: The safe use of terbutaline has not been established in human pregnancy. The use of this drug in pregnancy, lactation, or women of childbearing potential requires that the expected therapeutic benefit of the drug be weighed against its possible hazards to the mother or child. Animal reproductive studies have shown no adverse effects on fetal development.
Transient hypoglycemia has been reported in newborn preterm infants after maternal b2-agonist treatment.
Systemic B2-agonists should be used with caution before childbirth in view of their inhibiting effect on uterine contractions.
Lactation: Terbutaline is excreted in breast milk. Caution should be exercised when terbutaline is administered to nursing women.
Children: Terbutaline is not presently recommended for children below 6 years of age due to limited clinical data in this pediatric group.
Precautions: If therapy does not produce a significant improvement or if the patient’s condition gets worse, medical advice must be sought in order to determine a new plan of treatment. In the case of acute or rapidly worsening dyspnea, a doctor should be consulted immediately.
Increasing use of B2-agonists to control symptoms of bronchial obstruction, especially administration on a regular basis or in high amounts, indicates deterioration of asthma control. Under these conditions, the patient’s therapy plan has to be revised. It is inadequate simply to increase the use of bronchodilators under these circumstances, in particular over extended periods of time (see Dosage). The revised treatment regimen should include concomitant use of other anti-asthma drugs, such as anti-inflammatory agents.
To ensure optimal delivery of drug to the bronchial tree, the patient should be properly instructed in the use of Turbuhaler.
In patients in whom terbutaline administration induces cardiac irregularities, the administration of the drug should be stopped.
The concomitant use of terbutaline tablets with other orally administered sympathomimetic agents is not recommended, since their combined effect on the cardiovascular system may be deleterious to the patient. However, an inhaled bronchodilator of the sympathomimetic type can be used for the relief of acute bronchospasm in patients receiving chronic oral therapy.
If a reduced response to terbutaline becomes apparent, the patient should seek medical advice.
In patients requiring concomitant treatment with terbutaline and a beta-blocker, it is recommended that a beta-blocker (e.g., metoprolol) with less predominant B2-blocking effects be considered. If concomitant treatment is necessary, patients should be monitored carefully for possible deterioration in pulmonary function and the need to adjust the dosage of either drug (see Drug Interactions).
Immediate hypersensitivity reactions and exacerbation of bronchospasm have been reported after terbutaline administration.
Drug Interactions: Sympathomimetic Bronchodilators and Epinephrine: The concomitant use of terbutaline with other sympathomimetic bronchodilators is not recommended since their combined effect on the cardiovascular system may be deleterious to the patient. This recommendation does not preclude the judicious use of an inhaled bronchodilator of the sympathomimetic type in patients receiving terbutaline tablets. Such concomitant use, however, should be individualized and not given on a routine basis. If regular co-administration is required, alternative therapy should be considered.
MAO Inhibitors and Tricyclic Antidepressants: Terbutaline should be administered with caution in patients being treated with MAO inhibitors or tricyclic antidepressants, since the action of terbutaline on the vascular system may be potentiated.
Beta-Adrenergic Receptor Blockers: Beta-adrenergic receptor blocking agents not only block the pulmonary effect of terbutaline but may produce severe asthmatic attacks in asthmatic patients. Therefore, patients requiring treatment for both bronchospastic disease and hypertension should be treated with medication other than beta-adrenergic blocking agents for their hypertension.
Terbutaline Turbuhaler contains terbutaline sulfate which is sensitive to moisture. Patients should be instructed to avoid exhaling into the device and to replace the cover after using Turbuhaler.
Adverse Reactions: When treatment is started, the following adverse reactions can be classified as frequent (i.e. >1/100): tremor, palpitations, restlessness, headache, muscle cramps, nervousness. Other reported reactions include increased heart rate, ectopic beats, drowsiness, nausea, vomiting, sweating and dizziness.
These adverse reactions are all characteristic of sympathomimetic amines and initial dose titrations will often reduce these reactions. With the possible exception of muscle cramps, all have been spontaneously reversible within the first 2 weeks of treatment. Urticaria and exanthema may also occur.
Sleep disturbances and behavioral disturbances, such as agitation, hyperactivity and restlessness, have been observed.
As with other inhalation therapy, the potential for paradoxical bronchospasm should be kept in mind with terbutaline Turbuhaler. If it occurs, the preparation should be discontinued immediately and alternative therapy instituted.
Potentially serious hypokalemia may result from b2-agonist therapy.
Symptoms And Treatment Of Overdose: Symptoms and Treatment: The symptoms of overdosage are similar to those described under Adverse Effects, and are attributable to excessive b-adrenergic stimulation. To antagonize the effect of excessive stimulation, the judicious use of a b-adrenergic blocking agent such as propranolol may be considered, bearing in mind the danger of inducing an asthmatic attack.
Dosage And Administration: Dosage should be individualized, and patient response should be monitored by the prescribing physician on an ongoing basis.
Turbuhaler: Adults and children over 6 years: The generally recommended dose is 1 inhalation (0.5 mg) taken as required. This will usually be adequate to relieve bronchospasm in the majority of patients; however, if required, a second dose may be taken, preferably after waiting 5 minutes for the effect of the first dose to be obtained. If a more severe attack has not been relieved by the second administration, higher doses may be required. In these cases, patients should immediately consult their doctor or the nearest hospital.
More than 6 doses (6 inhalations of Turbuhaler) should not be necessary in any 24 hour period.
If a previously effective dosage regimen fails to provide the usual relief, or the effects of a dose last for less than 3 hours, medical advice should be sought immediately; this is a sign of seriously worsening asthma that requires reassessment of therapy.
Treatment with b2-agonists in bronchial asthma should be on demand, e.g., symptoms oriented. Patients must not use them on a daily basis for control of bronchospasm without using other concomitant antiasthma medication(s) according to the present practice for asthma treatment to control airway inflammation.
The daily dose of terbutaline Turbuhaler should not be increased without adequate reassessment of the therapy plan.
As with other b2-agonists, increasing demand for terbutaline in bronchial asthma is a sign of poor asthma control and indicates that the treatment plan should be revised.
When prescribing terbutaline Turbuhaler to children, it is necessary to ascertain that they can follow the instructions for use. Terbutaline Turbuhaler is not recommended for use in children below the age of 6 years.
Note: The medication from terbutaline Turbuhaler is delivered to the lungs as the patient inhales and, therefore, it is important to instruct the patient to breathe in forcefully and deeply through the mouthpiece. The patient may not taste or feel any medication when using terbutaline Turbuhaler due to the small amount of drug dispensed.
Tablets: Terbutaline tablets must not be used for relief of acute symptoms or without concomitant optimal anti-inflammatory asthma medications(s). If in spite of other adequate maintenance therapy, regular use of oral B2-agonists remains necessary, the recommended dose is:
Adults: The usual oral dose is 5 mg administered at approximately 6-hour intervals 3 times daily, during the hours the patient is usually awake. In the event of excessive side effects in individual patients, the dose may be reduced to 2.5 mg 3 times daily. In adults, a total dose of 15 mg should not be exceeded in a 24-hour period.
Children 12 to 15 years: Usual oral dose is 2.5 mg 3 times daily. A total of 7.5 mg should not be exceeded in a 24-hour period.
Children 6 to 11 years: In younger children the dose should be according to body weight i.e. 0.075 mg/kg body weight 3 times daily.
Suitable Dosage (2.5 mg tablets): 30 kg: 1 tablet (2.5 mg) 3 times in 24 hours.
The tablets are not recommended for use in children below the age of 6 years.
Availability And Storage: Tablets: 2.5 mg: Each white, scored tablet, engraved 2.5, contains: terbutaline sulfate 2.5 mg (equivalent to 2.05 mg free base). Nonmedicinal ingredients: cornstarch, lactose, magnesium stearate, microcrystalline cellulose and polyvinylpyrrolidone. Energy: 2.76 kJ (0.66 kcal). Gluten-, sodium- and tartrazine-free. Bottles of 100. Store at room temperature between 15 and 30°C.
5 mg: Each white, scored tablet, engraved 5, contains: terbutaline sulfate 5 mg (equivalent to 4.1 mg free base). Nonmedicinal ingredients: cornstarch, lactose, magnesium stearate, microcrystalline cellulose and polyvinylpyrrolidone. Energy: 2.72 kJ (0.65 kcal). Gluten-, sodium- and tartrazine-free. Bottles of 100. Store at room temperature between 15 and 30°C.
Turbuhaler: Each Turbuhaler contains: 50 or 200 doses of micronized terbutaline sulfate. Each inhalation from the multiple-dose powder inhaler contains: terbutaline sulfate 0.5 mg; no additives or carrier substances are included in the inhalation. Turbuhaler cannot be refilled and should be discarded when empty. Store with the cover tightened at room temperature between 15 and 30°C, in a dry place, away from moisture.
BRICANYL® Tablets BRICANYL® TURBUHALER® Astra Terbutaline Sulfate Bronchodilator