Durasal-CR

Durasal-CR

salbutamol

Manufacturer:

Raptakos, Brett

Distributor:

KMT
Full Prescribing Info
Contents
Salbutamol sulfate.
Description
Durasal-CR capsules contain salbutamol sulfate equivalent to salbutamol 4 mg.
Salbutamol [1-(4-(RS)-Hydroxy-3-hydroxymethylphenyl-2-(t-butylamino)ethanol] is a β2-adrenoceptor agonist.
Action
Pharmacology: Salbutamol sulfate is a selective β2-adrenoceptor agonist with effects on smooth and skeletal muscles. These include bronchodilation, relaxation of uterine muscle and tremor. Smooth muscle relaxation is dose dependent and is thought to occur via the adenyl cyclase-cyclic adenosine monophosphate (cAMP) system, with binding of the drug to the β-adrenergic receptor in the cell membrane causing conversion of ATP to cAMP, which activates protein kinase. This leads to phosphorylation of proteins, which ultimately increase bound intracellular calcium; the consequent reduced availability of ionized intracellular calcium inhibits actin-myosin linkage thus causing relaxation of smooth muscle.
β2-agonists eg, salbutamol sulfate also have an antiallergic effect on mast cells causing inhibition of release of bronchoconstrictor mediators including histamine, neutrophil chemotactive factor (NCF) and prostaglandin D2 (PGD2).
Bronchodilation occurs after administration of salbutamol sulfate in normal subjects and in patients with asthma or chronic obstructive pulmonary disease (COPD). Other actions in the respiratory system include enhanced mucociliary clearance, which have been demonstrated in patients with COPD and in normal subjects and an antiallergic effect due to inhibition of mediator release. Stimulation of β2-receptor results in widespread metabolic effects, including rise in free fatty acid, insulin, lactate and glucose levels and a fall in serum potassium concentration.
Pharmacokinetics: Salbutamol sulfate is well absorbed from the gastrointestinal tract with between 58 and 78% of a radiolabel appearing in the urine within 24 hrs and 65-84% in 72 hrs. Presystemic metabolism is considerable. The major metabolite is a sulphate conjugate, which is probably formed in the bowel mucosa and is inactive, 34-47% of a radiolabel appears in the urine as the conjugate and approximately half of this amount as unchanged drug. The proportion of circulating drug that is protein bound is approximately 10%. Transfer of the drug across the placenta has been demonstrated both in vitro and in vivo.
Indications/Uses
Relief and prevention of bronchospasm in patients with reversible obstructive airway disease.
Dosage/Direction for Use
Adults: 1 cap twice daily.
Overdosage
The expected symptoms with overdosage are those of excessive β-stimulation and/or occurrence or exaggeration of any of the symptoms listed under Adverse Reactions eg, seizures, angina, hypertension or hypotension, tachycardia, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise and insomnia. Hypokalemia may also occur. Treatment consists of discontinuation of salbutamol sulfate together with appropriate symptomatic therapy.
Contraindications
Patients with a history of hypersensitivity to salbutamol.
Warnings
General: Immediate hypersensitivity reactions may occur after administration of salbutamol sulfate, as demonstrated by rare cases of urticaria, angioedema, rash and oropharyngeal edema. Salbutamol sulfate can produce a significant cardiovascular effect in some patients as measured by pulse rate, blood pressure, symptoms and/or electrocardiographic changes.
Special Precautions
Salbutamol sulfate should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias and hypertension; in patients with convulsive disorders, hyperthyroidism or diabetes mellitus; and in patients who are unusually responsive to sympathomimetic amines.
Use in pregnancy & lactation: Salbutamol has been demonstrated to be teratogenic in mice.
It is not known whether salbutamol sulfate is excreted in human milk. Because of the potential for tumorigenicity shown for salbutamol sulfate in animal studies, 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.
Use in children: Safety and effectiveness in children <6 years have not been established.
Use In Pregnancy & Lactation
Salbutamol has been demonstrated to be teratogenic in mice.
It is not known whether salbutamol sulfate is excreted in human milk. Because of the potential for tumorigenicity shown for salbutamol sulfate in animal studies, 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.
Adverse Reactions
Salbutamol sulfate is generally well tolerated and serious toxic effects are few. The adverse reactions to salbutamol sulfate are similar in nature to reactions to other sympathomimetic agents, although the incidence of certain cardiovascular effects is lower with salbutamol sulfate. The most frequent adverse reactions to salbutamol sulfate are nervousness and tremor. Other reported reactions are headache, tachycardia and palpitations, muscle cramps, insomnia, nausea, weakness and dizziness. Rare cases of urticaria, angioedema, rash and oropharyngeal edema have been reported after the use of salbutamol sulfate. The reactions are generally transient in nature and it is usually not necessary to discontinue treatment with salbutamol sulfate. Inform the physician of the unwanted effects after administering.
Drug Interactions
The concomitant use of salbutamol sulfate and other oral sympathomimetic agents is not recommended since such combined use may lead to deleterious cardiovascular effects. Salbutamol sulfate should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants because the action of salbutamol sulfate on the vascular system may be potentiated. Beta-receptor-blocking agents and salbutamol sulfate inhibit the effect of each other. Caution is advised in the co-administration of β-agonists with non-potassium-sparing diuretics, it may result in hypokalemia.
Storage
Protect from heat and humidity.
ATC Classification
R03CC02 - salbutamol ; Belongs to the class of adrenergics for systemic use, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
Presentation/Packing
Cap 4 mg x 10 x 10's.
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