Sabul Plus Respirator Solution (2.5 mg+500 mcg)/ml
Sabul Plus Respirator Solution (2.5 mg+500 mcg)/ml Uses, Dosage, Side Effects, Food Interaction and all others data.
Salbutamol is a selective beta2-adrenoceptor agonist. At therapeutic doses, it acts on the beta2-adrenoceptors of bronchial smooth muscle, with little or no action on the ß1-adrenoceptors of cardiac muscle. Salbutamol provides short acting (4-6 hours) bronchodilatation with a fast onset (within 5 minutes) in reversible airways obstruction. It also has an anti-inflammatory effect on mast cells causing inhibition of release of bronchoconstrictor mediators including histamine, neutrophil chemotactive factor (NCF) and prostaglandin D2.
Salbutamol (INN) or albuterol (USAN), a moderately selective beta(2)-receptor agonist similar in structure to terbutaline, is widely used as a bronchodilator to manage asthma and other chronic obstructive airway diseases. The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity. The R-enantiomer is available and sold in its pure form as levalbuterol and subsequently may produce fewer side-effects with only the R-enantiomer present - although this has not been formally demonstrated.
After oral and parenteral administration, stimulation of the beta receptors in the body, both beta-1 and beta-2, occurs because (a) beta-2 selectivity is not absolute, and (b) higher concentrations of salbutamol occur in the regions of these receptors with these modes of administration. This results in the beta-1 effect of cardiac stimulation, though not so much as with isoprenaline, and beta-2 effects of peripheral vasodilatation and hypotension, skeletal muscle tremor, and uterine muscle relaxation.
Metabolic effects such as hyperinsulinemia and hyperglycemia also may occur, although it is not known whether these effects are mediated by beta-1 or beta-2 receptors. The serum potassium levels have a tendency to fall.
| Trade Name | Sabul Plus Respirator Solution (2.5 mg+500 mcg)/ml |
| Generic | Salbutamol + Ipratropium (Solution for inhalation) |
| Weight | (2.5 mg+500 mcg)/ml |
| Type | Respirator Solution |
| Therapeutic Class | Combined bronchodilators |
| Manufacturer | Chemist Laboratories Ltd. |
| Available Country | Bangladesh |
| Last Updated: | October 19, 2023 at 6:27 am |
Uses
Salbutamol sulfate & Ipratropium bromide solution for inhalation is indicated for the treatment of reversible bronchospasm associated with obstructive airway diseases in patients who require more than a single bronchodilator.Sabul Plus Respirator Solution (2.5 mg+500 mcg)/ml is also used to associated treatment for these conditions: Asthma, Asthmatic Bronchitis, Bronchial Asthma, Bronchospasm, Chronic Asthma, Chronic Bronchitis, Cough, Emphysema, Exercise-Induced Bronchospasm, Hyperkalemia, Wheezing, Excess mucus or phlegm, Airway secretion clearance therapy, Bronchodilation
How Sabul Plus Respirator Solution (2.5 mg+500 mcg)/ml works
In vitro studies and in vivo pharmacologic studies have shown that salbutamol has a preferential effect on beta2-adrenergic receptors compared with isoproterenol. Although beta2 adrenoceptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1 adrenoceptors are the predominant receptors in the heart, there are also beta2-adrenoceptors in the human heart comprising 10% to 50% of the total beta-adrenoceptors. The precise function of these receptors has not been established, but their presence raises the possibility that even selective beta2-agonists may have cardiac effects.
Activation of beta2-adrenergic receptors on airway smooth muscle leads to the activation of adenyl cyclase and to an increase in the intracellular concentration of cyclic-3′,5′-adenosine monophosphate (cyclic AMP). This increase of cyclic AMP leads to the activation of protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in relaxation. Salbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Salbutamol acts as a functional antagonist to relax the airway irrespective of the spasmogen involved, thus protecting against all bronchoconstrictor challenges. Increased cyclic AMP concentrations are also associated with the inhibition of release of mediators from mast cells in the airway.
Salbutamol has been shown in most controlled clinical trials to have more effect on the respiratory tract, in the form of bronchial smooth muscle relaxation, than isoproterenol at comparable doses while producing fewer cardiovascular effects. Controlled clinical studies and other clinical experience have shown that inhaled albuterol, like other beta-adrenergic agonist drugs, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic changes.
A measurable decrease in airway resistance is typically observed within 5 to 15 minutes after inhalation of salbutamol. The maximum improvement in pulmonary function usually occurs 60 to 90 minutes after salbutamol treatment, and significant bronchodilator activity has been observed to persist for 3 to 6 hours.
Dosage
Sabul Plus Respirator Solution (2.5 mg+500 mcg)/ml dosage
Salbutamol sulfate & Ipratropium bromide solution for inhalation in ampoule may be administered from a suitable nebulizer or an intermittent positive pressure ventilator. Adults (including elderly): Use one 3 ml ampoule in the nebulizer four times a day. Two additional treatments may be used per day, if needed. Children: Use and dose must be determined by doctor. Patients should be advised to consult a doctor or the nearest hospital immediately in the case of acute or rapidly worsening dyspnoea if additional inhalations do not produce an adequate improvement. Step 1: Twist off the top of the ampoule. Be careful to hold the ampoule upright.Step 2: Squeeze the desired amount of the nebulizer solution into the nebulizer chamber.Step 3: If dilution is needed follow the physician’s direction.Side Effects
In common with other beta-agonists containing products, side effects of this solution can include fine tremor of skeletal muscles and nervousness and less frequently tachycardia, dizziness, palpitations or headache, especially in hypersensitive patients.Potentially serious hypokalaemia may result from prolonged and/or high dose beta2 agonist therapy.As with use of other inhalation therapy, cough, local irritation and less commonly inhalation induced bronchospasm can occur. As with other beta-mimetics, nausea, vomiting, sweating, weakness and myalgia/muscle cramps may occur. In rare cases decrease in diastolic blood pressure, increase in systolic blood pressure, arrhythmias, particularly after higher doses, may occur.In individual cases psychological alterations have been reported under inhalation therapy with beta-mimetics.The most frequent non-respiratory anticholinergic related adverse events are dryness of mouth and dysphonia. There have been isolated reports of ocular complications (i.e. mydriasis, increased intraocular pressure, angle closure glaucoma, and eye pain) when aerosolised ipratropium bromide either alone or in combination with adrenergic beta2 agonist, has escaped into the eyes. Ocular side effects, gastrointestinal motility disturbances and urinary retention may occur in rare cases and are reversible.Toxicity
The expected signs and symptoms with overdosage of albuterol are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the signs and symptoms of beta-adrenergic stimulation (e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats/min, arrhythmias, nervousness, headache, tremor, muscle cramps, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, insomnia, hyperglycemia, hypokalemia, metabolic acidosis). In particular, the signs of salbutamol overdosage are significant tachycardia and/or significant muscle tremor.
Hypokalaemia may occur following overdosage with salbutamol. Serum potassium levels should be monitored.
Lactic acidosis has been reported in association with high therapeutic doses as well as overdoses of short-acting beta-agonist therapy, therefore monitoring for elevated serum lactate and consequent metabolic acidosis (particularly if there is persistence or worsening of tachypnea despite resolution of other signs of bronchospasm such as wheezing) may be indicated in the setting of overdose.
Salbutamol is categorized as Pregnancy Category C. There are no adequate and well-controlled trials with salbutamolc or albuterol sulfate in pregnant women. During worldwide marketing experience, various congenital anomalies, including cleft palate and limb defects, have been reported in the offspring of patients being treated with salbutamol. Some of the mothers were taking multiple medications during their pregnancies. No consistent pattern of defects can be discerned, and a relationship between salbutamol use and congenital anomalies has not been established. Animal reproduction studies in mice and rabbits revealed evidence of teratogenicity. Salbutamol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetusLabel]. Women should be advised to contact their physicians if they become pregnant while taking salbutamol.
Since there exists a potential for beta-agonist interference with uterine contractility, the use of salbutamol during labour should be restricted to those patients in whom the benefits clearly outweigh the risk.
Plasma levels of albuterol sulfate and HFA-134a after inhaled therapeutic doses are very low in humans, but it is not known whether the components of salbutamol are excreted in human milk. Because of the potential for tumorigenicity shown for albuterol in animal studies and lack of experience with the use of salbutamol by nursing mothers, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Caution should be exercised when salbutamol is administered to a nursing woman.
The safety and effectiveness of salbutamol in children younger than 4 years of age has not yet been established.
Clinical trials of VENTOLIN HFA did not include sufficient numbers of subjects aged 65 years and older to determine whether older subjects respond differently than younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
The LD50 value was determined to be 1100 mg/kg (orally in mice).
Precaution
In the case of acute, rapidly worsening dyspnoea a doctor should be consulted immediately. Immediate hypersensitivity reactions may occur after administration of this solution as demonstrated by rare cases of urticaria, angioedema, rash, bronchospasm and oropharyngeal oedema.Interaction
The concurrent administration of other beta-mimetics, systemically absorbed anticholinergics and xanthine derivatives may increase the side effects.Beta-agonist induced hypokalaemia may be increased by concomitant treatment with xanthine derivatives, glucocorticosteroids and diuretics. This should be taken into account particularly in patients with severe airway obstruction.Hypokalaemia may result in an increased susceptibility to arrhythmias in patients receiving digoxin. It is recommended that serum potassium levels be monitored in such situations.A potentially serious reduction in bronchodilator effect may occur during concurrent administration of beta-blockers.Beta-adrenergic agonists should be administered with caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, since the action of beta adrenergic agonists may be enhanced.Inhalation of halogenated hydrocarbon anaesthetics such as halothane, trichloroethylene and enflurane may increase the susceptibility to the cardiovascular effects of beta-agonists.Volume of Distribution
The volume of distribution recorded for intravenously administered salbutamol has been recorded as 156 +/- 38 L.
Elimination Route
Following inhalation, salbutamol acts topically on bronchial smooth muscle and the drug is initially undetectable in the blood. After 2 to 3 hours low concentrations are seen, due presumably to the portion of the dose which is swallowed and absorbed in the gut.
In particular, the systemic levels of salbutamol are low after inhalation of recommended doses. A trial conducted in 12 healthy male and female subjects using a higher dose (1,080 mcg of albuterol base) showed that mean peak plasma concentrations of approximately 3 ng/mL occurred after dosing when salbutamol was delivered using propellant HFA-134a. The mean time to peak concentrations (Tmax) was delayed after administration of VENTOLIN (salbutamol) HFA (Tmax = 0.42 hours) as compared with CFC-propelled salbutamol inhaler (Tmax = 0.17 hours).
Half Life
The elimination half-life of inhaled or oral salbutamol has been recorded as being between 2.7 and 5 hours while the apparent terminal plasma half-life of albuterol has been documented as being approximately 4.6 hours.
Clearance
The renal clearance of salbutamol has been documented as 272 +/- 38 ml/min after oral administration and 291 +/- 70 ml/min after intravenous administration. Furthermore, the renal clearance of the predominant sulfate conjugate metabolite was recorded as 98.5 +/- 23.5 ml/min following oral administration.
Elimination Route
After oral administration, 58-78% of the dose is excreted in the urine in 24 hours, approximately 60% as metabolites. A small fraction is excreted in the feces.
Pregnancy & Breastfeeding use
Pregnancy category C. Animal studies with Salbutamoi Sulphate have demonstrated a teratogenic effect. It is not known whether this medication is harmful to the fetus. No evidence of abnormalities has been reported in women receiving albuterol during pregnancy. This solution should be used during pregnancy only if the potential benefit justifies. This solution should be used with caution before childbirth in view of Salbutamol's inhibitory effects on uterine contractions.Salbutamol Sulphate and Ipratropium Bromide are probably excreted in breast milk and their effects on neonates are not known. Although lipid-insoluble quaternary bases pass into breast milk, it is unlikely that this will happen to any extent especially when taken by inhalation. However, because many drugs are excreted in breast milk, caution should be exercised when This solution is administered to a nursing woman.Contraindication
This is contraindicated in patients with hypertrophic obstructive tachyarrhythmia and in patients with a history of hypersensitivity to atropine or its derivatives, or to any other component of the product.Acute Overdose
The effects of overdosage are expected to be primarily related to Salbutamol because acute overdosage with Ipratropium Bromide is unlikely as it is not well absorbed systemically after inhalation or oral administration.Symptoms: Manifestations of overdosage with salbutamol may include tachycardia, anginal pain, hypertension, hypotension , palpitations, tremor, widening of the pulse pressure, arrhythmia and flushing.Therapy: Administration of sedatives, tranquillisers; 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 bronchial asthma.Storage Condition
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.Innovators Monograph
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