Source: Health Products and Food Branch (CA) Revision Year: 2014
Orciprenaline sulphate has been found useful in the following conditions:
Orciprenaline sulphate is also useful in sarcoidosis, silicosis, carcinoma of the lung and tuberculosis when bronchospasm contributes to the disability.
The efficacy of orciprenaline sulphate has been demonstrated by improvement of flow rates (FEV1, MMFR, MEFR) and airways resistance measurements (body plethysmography). Repeated measurements of pulmonary function made over a 4–hour period show that orciprenaline sulphate 20 mg orally gives a generally better result regarding duration of action and magnitude of response than placebo, 100 mg methoxyphenamine, 30 mg ephedrine by mouth, or 10 mg isoproterenol sublingually.
The effect of an inhalant bronchodilator may be potentiated by oral administration of 20 mg of orciprenaline sulphate 90 minutes prior to use of the inhalant. No additive effect occurs when the drugs are given in reverse order. The probable reason for this is that a bronchodilator delivered to the lungs via the vascular system (intravenous or oral medication) acts upon bronchioles whether or not they are occluded. Such an effect causes a wider distribution in the lungs of a subsequently given drug, and consequently the bronchodilation is more intense. Knowledge of this interaction is of value when instructing patients in the combined use of oral and inhalant forms of orciprenaline sulphate.
Orciprenaline sulphate may be given orally in dosages ranging from 60 mg to 120 mg daily. An effective clinical response in adults and children above 12 years can be achieved by 20 mg orciprenaline sulphate 3 times daily, and at this dosage side effects are not significantly different from those following placebo. Orciprenaline sulphate at a dosage of 20 mg 4 times daily is well tolerated and side effects are usually mild. Only at dosages of 100 mg daily and above, do palpitations and tremulousness become troublesome. If high doses of orciprenaline sulphate are necessary, it may be possible to eliminate the side effects whilst continuing the same total daily dose, by administering 10 mg single doses at more frequent intervals.
The low incidence of side effects together with effective bronchodilation make orciprenaline sulphate acceptable to patients with chronic bronchial asthma for continuous use either alone or concurrently with corticosteroids. Some of these patients may be controlled with orciprenaline sulphate as the sole medication, and it may be possible to avoid the use of steroid therapy. In a proportion of individuals who are already taking corticosteroids, it may be possible to withdraw this medication and continue with orciprenaline sulphate alone. However, caution should be observed in this regard as many patients, particularly those with severe bronchial asthma, can be managed satisfactorily only if steroids and bronchodilators are given together.
Prolonged studies have shown that patients with bronchitis and emphysema respond to continuous therapy with orciprenaline sulphate. The frequency and severity of acute attacks decrease, and patients experience relief of wheezing, chest congestion and shortness of breath. A close association is apparent between objective measurements of pulmonary function and the subjective response.
Dosage should be individualized, and patient response should be monitored by the prescribing physician on an ongoing basis.
If a previous effective dosage regimen fails to provide the usual relief, medical advice should be sought immediately as this is a sign of seriously worsening asthma that requires reassessment of therapy.
In accordance with the present practice for asthma treatment, concomitant anti-inflammatory therapy should be part of the regimen when a β2-agonist needs to be used on a regular daily basis.
The following recommended dosages represent general guidelines that are suitable for the majority of patients.
Syrup:
Adult Dosage: 20 mg (10 mL) t.i.d. or q.i.d.
Pediatric Dosage:
Ages:
4-12: 10 mg (5 mL) t.i.d
Above 12: 20 mg (10 mL) t.i.d.
The symptoms of overdosage are those of excess beta stimulation including exaggeration of the known pharmacological effects, i.e. any of the symptoms listed under adverse reactions, the most prominent being tachycardia, palpitation, tremor, hypertension, hypotension, widening of the pulse pressure, anginal pain, arrhythmias, and flushing.
Therapy may include administration of sedative, tranquilizers or in severe cases, intensive therapy.
Beta-receptor blockers, preferably beta1-selective, are suitable as specific antidotes; however, a possible increase in bronchial obstruction must be taken into account and the dose should be adjusted carefully in patients suffering from asthma. If has been shown that the beta-blocker propranolol effectively antagonizes the action of orciprenaline sulphate and the use of this agent should be considered under these circumstances.
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