Provexel

Each actuation delivers: Salbutamol (as sulfate) BP 100 mcg.
CFC/ODS-Free.

Pharmacology: Pharmacodynamics: Salbutamol is a selective short acting beta-2-adrenergic agonist with a preferential effect on beta-2-adrenergic receptors found in the respiratory tract. It stimulates adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). CAMP mediates cellular responses such as bronchial smooth muscle relaxation resulting in bronchodilation.
Pharmacokinetics: After oral inhalation of salbutamol, onset of bronchodilation is within 5 to 15 minutes; peaks in 0.5 to 3 hours and persists for 2 to 5 hours; bronchodilation in some patients may persist for up to 6 hours. Much of the salbutamol dose delivered by oral inhalation is deposited on the buccal mucosa and subsequently swallowed and absorbed from gastrointestinal tract.
Salbutamol is metabolized in the liver, being converted to salbutamol 4'-O-sulfate. This is then excreted in the urine and feces. In patients with asthma, about 70% of the inhaled dose is excreted in urine as unchanged drug and metabolites within 24 hours, and 80 to 100% within 72 hours; about 30% of the inhaled dose is excreted unchanged in the urine in 24 hours. About 10% of the inhaled dose may be excreted in the feces.
Animal studies show that salbutamol is capable of crossing the blood-brain barrier and the placenta. It may be secreted in breast milk, but concentrations are not known.

For the relief of bronchospasm associated with reversible obstructive airway diseases such as bronchial asthma and chronic obstructive pulmonary disease.
For the prevention of exercise-induced bronchospasm if the drug is given before exertion.

For Relief of Bronchospasm: Rapid-acting inhaled beta-2-agonists, such as salbutamol, should be used only on as-needed basis at the lowest dose and frequency required.
Adults and children more than 4 years old: 100 mg or 200 mg (1 or 2 inhalations) as needed every 4 to 6 hours, or as prescribed by a doctor.
The bronchodilator effect of each administration of salbutamol inhaler lasts for at least 4 hours. If a previously effective fixed dose fails to provide the usual relief, consult a physician for medical advice as this is a sign of worsening of asthma that would require reassessment of therapy.
For Prevention of Exercise-induced Bronchospasm: Adults: 200 mcg (2 inhalations) 15 to 30 minutes before exercise.
Children more than 4 years old: 100 or 200 mcg (1 or 2 inhalations) 15 to 30 minutes before exercise.

Symptoms of orally inhaled salbutamol overdose include extensions of the common undesirable effects (e.g., seizures, hypertension or hypotension, arrhythmias, palpitations, nervousness, dizziness, fatigue, malaise, insomnia/sleeplessness, headache, tremor, dry mouth, and nausea). Angina and tachycardia have also been reported following overdosage.
Hypokalemia and metabolic acidosis may also occur following overdose with salbutamol. Serum potassium concentrations should be monitored. Lactic acidosis has been reported in association with high therapeutic doses as well as overdoses of short-acting beta-agonist therapy.
Discontinue salbutamol and institute appropriate symptomatic therapy in cases of salbutamol overdose.
Administration of a beta-adrenergic blocking agent may be appropriate but use with caution if the patient is asthmatic.

Hypersensitivity to salbutamol or to any ingredient of the product.
In the management of premature labor.

Excessive use of sympathomimetic oral inhalations has been associated with fatalities. The exact cause of death is unknown but cardiac arrest following severe, acute asthmatic crisis and hypoxia is suspected.
Asthma Exacerbations: Patients who are overdependent on rapid-acting inhaled beta-2-agonists, especially those who use more than one canister of salbutamol (or equivalent) monthly is at high risk of asthma-related death. They require closer supervision by the physician and should be encouraged to seek urgent care early in the course of their exacerbations.
Paradoxical Bronchospasm: Paradoxical bronchospasm, a potentially life-threatening event, has been observed with inhaled salbutamol. If it occurs, discontinue use of the product immediately.
Deterioration of Asthma: Asthma may deteriorate acutely over a period of hours or chronologically over several days or longer. Increased use of beta-2-agonists, especially daily use, is a sign of deterioration of asthma control and indicates the need to reassess treatment. Possible need for anti-inflammatory treatment (e.g., corticosteroids) should be considered.
Hypokalemia: Therapy with salbutamol and other beta-2-agonists may produce a decrease in plasma potassium concentration possibly through intracellular shunting resulting in cardiovascular undesirable effects.
Use with caution in acute severe asthma where concomitant therapy with steroid, xanthine derivatives, or diuretics and by hypoxia may result in hypokalemia; potassium concentrations should be monitored in severe asthma.
Coexisting Conditions: Use with caution in patients with the following conditions: Cardiovascular disorders including coronary insufficiency, cardiac arrhythmias, or hypertension. Salbutamol, like all other beta-2-agonists, can produce clinically significant cardiovascular effects such as changes in pulse rate or blood pressure.
Convulsive disorders.
Hyperthyroidism.
Diabetes mellitus.
In patients who are unusually responsive to sympathomimetic amines.
Use in Children: The safety and efficacy of orally inhaled salbutamol aerosol with hydrofluoroalkane (HFA) propellant have not been established in children younger than 4 years old.
Use in the Elderly: Data on the use of salbutamol inhalation aerosol in patients 65 years and older are limited and are insufficient to determine whether the efficacy and safety are similar to those of younger patients.

Pregnancy: Pregnancy Category C: There have been reports of congenital anomalies (e.g. cleft palate and limb defects) in children of patients treated with salbutamol. Some of the mothers, however, were receiving various medications in the course of their pregnancies. Since there is no consistent pattern of congenital abnormality development, a relationship between the use of salbutamol and the development of congenital anomalies cannot be established. Therefore, salbutamol should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.
Labor and Delivery: Since beta-2-agonists may interfere with uterine contraction, the product should be used in labor only if the potential benefit justifies the potential risk.
Lactation: Salbutamol may be secreted in breast milk. Therefore, do not administer to breastfeeding women unless, in the opinion of a physician, the potential benefit of the drug justifies the potential risk.

Hypersensitivity reactions: Urticaria, angioedema, rash, bronchospasm, anaphylaxis, hypotension, collapse.
Endocrine and metabolic disorders: Diabetes mellitus, hypokalemia, metabolic acidosis.
Nervous system: Tremors, headache, hyperactivity, nervousness, dizziness, vertigo, central nervous stimulation, sleeplessness.
Cardiovascular: Tachycardia, palpitations, hypertension, hypotension, cardiac arrhythmias (including atrial fibrillation, supraventricular tachycardia, and extrasystoles), peripheral vasodilation, angina, myocardial ischemia.
Respiratory/Nasopharyngeal: Paradoxical bronchospasm, bronchitis, asthma, exacerbation, dyspnea, epistaxis, cough, dysphoria or voice alterations, drying or irritation of oropharynx, hoarseness, laryngitis, lung disorders, oropharyngeal edema, nasopharyngitis, rhinitis, flu-like syndrome, upper respiratory inflammation, upper respiratory tract infection, viral respiratory infections.
Gastrointestinal: Nausea and/or vomiting, diarrhea, constipation, gastroenteritis, heartburn, eructation, flatulence, dry mouth, tongue ulceration, glossitis, altered taste, mouth and throat irritation, gaggling.
Musculoskeletal: Muscle cramps, musculoskeletal pain, rigors, back pain.
Others: Ear disorder or ear pain, sweating, urinary tract infection, pyrexia.

Sympathomimetics agents: Salbutamol should not be administered concomitantly with other short-acting sympathomimetic aerosol bronchodilators or epinephrine. If additional sympathomimetic agents are to be administered by any route, these agents should be used with caution to avoid deleterious cardiovascular effects.
Beta-adrenergic blocking agents (e.g., propranolol): Beta-adrenergic blocking agents may inhibit the effect of beta-agonists such as salbutamol. It may also produce severe bronchospasm. These drugs should be administered with caution.
Diuretics: Administration of non potassium-sparing diuretics (e.g., loop or thiazide diuretics) may result in ECG changes and/or hypokalemia and can be acutely worsened by administration of beta-agonists such as salbutamol, especially when the recommended dose of the beta-agonist is exceeded.
Digoxin: Following administration of single-dose intravenous or oral salbutamol to healthy individuals who had received digoxin for 10 days, a 16% to 22% decrease in serum digoxin concentration was observed. Although the clinical importance of these findings for patients who are receiving inhaled salbutamol and digoxin on a chronic basis is unclear, patients receiving such concomitant therapy should have their serum digoxin concentration carefully evaluated.
Monoamine oxidase inhibitors (MAOls) or Tricyclic antidepressants (TCAs): Salbutamol should be used with caution in patients receiving MAOls or TCAs or within 2 weeks of discontinuation of such agents, because the effect of salbutamol on the vascular system may be potentiated. Alternative therapy should be considered in patients taking MAOls or TCAs.

Directions for Use: Before initial use and if the product has not been used for several days, remove the cap from the mouthpiece and shake the inhaler well, then release 4 puffs into the air (away from the face).
Using the inhaler: 1. Remove the cap from the mouthpiece and hold inhaler upright.
2. Shake the inhaler well.
3. Breath out fully, then place the mouthpiece into the mouth and close lips firmly around it.
4. Press down the inhaler to release salbutamol, while breathing in slowly (3 to 5 seconds) and deeply at the same time. Synchronize inhaler actuation and inhalation for optimum drug delivery to the lungs.
5. Remove inhaler from the mouth, hold breath for 10 seconds or as long as possible, and breathe out slowly.
6. Repeat puff as directed. Wait one minute between puffs for better lung penetration.
7. Replace the cap.
Cleaning instructions: 1. Remove the metal aerosol canister containing the drug from the inhaler.
2. Wash the plastic case and cap regularly in warm running water.
3. Allow plastic parts to dry completely.
4. Replace the aerosol container and mouthpiece cap.

Store at temperatures not exceeding 30°C.
Protect from direct sunlight or heat.
Do not freeze or refrigerate.
The efficacy of this medicine may decrease when the metal canister is cold.
Do not break, puncture or burn the canister even when apparently empty.
Shelf-Life: 24 months.

Antiasthmatic & COPD Preparations

R03AC02 - salbutamol ; Belongs to the class of adrenergic inhalants, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.

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