Ventolin Inhaler

Ventolin Inhaler

salbutamol

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GlaxoSmithKline
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Contents
Salbutamol.
Description
Ventolin Inhaler is a pressurised metered-dose inhaler which delivers salbutamol (as sulphate) 100 mcg per actuation, into the mouthpiece of a specially designed actuator. Each canister contains at least 200 actuations. The inhaler also contains the CFC-free propellant 1, 1, 1, 2-tetrafluoroethane (also known as HFA 134a or norflurane) as an excipient.
Action
Pharmacology: Pharmacodynamics: Salbutamol is a selective β2-adrenoceptor agonist. At therapeutic doses it acts on the β2-adrenoceptors of bronchial muscle providing short-acting (4-6 hrs) bronchodilation with a fast onset (within 5 min) in reversible airways obstruction.
Clinical Studies: Special Patient Populations: Children <4 years: Paediatric clinical studies conducted at the recommended dose (SB020001, SB030001, SB030002) in patients <4 years with bronchospasm associated with reversible obstructive airways disease, show that the Inhaler has a safety profile comparable to that in children ≥ 4 years, adolescents and adults.
Pharmacokinetics: Absorption: After administration by the inhaled route, between 10 and 20% of the dose reaches the lower airways. The remainder is retained in the delivery system or is deposited in the oropharynx from where it is swallowed. The fraction deposited in the airways is absorbed into the pulmonary tissues and circulation but is not metabolised by the lung.
Distribution: Salbutamol is bound to plasma proteins to the extent of 10%.
Metabolism: On reaching the systemic circulation, salbutamol becomes accessible to hepatic metabolism and is excreted, primarily in the urine, as unchanged drug and as the phenolic sulphate.
The swallowed portion of an inhaled dose is absorbed from the gastrointestinal tract and undergoes considerable first-pass metabolism to the phenolic sulphate. Both unchanged drug and conjugate are excreted primarily in the urine.
Elimination: Salbutamol administered intravenously has a half-life (t½) of 4-6 hrs and is cleared partly renally and partly by metabolism to the inactive 4'-O-sulphate (phenolic sulphate) which is also excreted primarily in the urine. The faeces are a minor route of excretion. The majority of a dose of salbutamol given intravenously, orally or by inhalation is excreted within 72 hrs.
Toxicology:
Preclinical Safety Data: In common with other potent selective β2-receptor agonists, salbutamol has been shown to be teratogenic in mice when given subcutaneously. In a reproductive study, 9.3% of foetuses were found to have cleft palate, at 2.5 mg/kg, 4 times the maximum human oral dose. In rats, treatment at the levels of 0.5, 2.32, 10.75 and 50 mg/kg/day orally throughout pregnancy resulted in no significant foetal abnormalities. The only toxic effect was an increase in neonatal mortality at the highest dose level as the result of lack of maternal care. A reproductive study in rabbits revealed cranial malformations in 37% of foetuses at 50 mg/kg/day, 78 times the maximum human oral dose.
In an oral fertility and general reproductive performance study in rats at doses of 2 and 50 mg/kg/day, with the exception of a reduction in number of weanlings surviving to day 21 postpartum at 50 mg/kg/day, there were no adverse effects on fertility, embryofetal development, litter size, birth weight or growth rate.
HFA 134a has been shown to be non-toxic at very high vapour concentrations, far in excess of those likely to be experienced by patients, in a wide range of animal species exposed daily for periods of 2 years.
Indications/Uses
Treatment or prevention of bronchospasm. It provides short-acting (4 hrs) bronchodilation in reversible airways obstruction due to asthma, chronic bronchitis and emphysema. For patients with asthma, salbutamol may be used to relieve symptoms when they occur and to prevent them prior to a known trigger.
Bronchodilators should not be the only or main treatment in patients with persistent asthma. In patients with persistent asthma unresponsive to Ventolin, treatment with inhaled corticosteroids is recommended to achieve and maintain control. Failing to respond to treatment with Ventolin may signal a need for urgent medical advice or treatment.
Dosage/Direction for Use
Ventolin has a duration of action of 4-6 hours in most patients.
Increasing use of β2-agonists may be a sign of worsening asthma. Under these conditions a re-assessment of the patient's therapy plan may be required and concomitant glucocorticosteroid therapy should be considered.
As there may be adverse effects associated with excessive dosing, the dosage or frequency of administration should only be increased on medical advice.
In patients who find co-ordination of a pressurised metered-dose inhaler difficult a spacer may be used with Ventolin Inhaler.
Babies and young children using the Ventolin Inhaler may benefit from the use of a paediatric spacer device with a face mask (eg, the Babyhaler) (See Pharmacology: Pharmacodynamics: Clinical Studies under Actions).
Relief of Acute Bronchospasm:
Adults: 100 or 200 mcg. Children: 100 mcg. The dose may be increased to 200 mcg if required.
Prevention of Allergen or Exercise-Induced Bronchospasm: Adults: 200 mcg before challenge or exertion. Children: 100 mcg before challenge or exertion. The dose may be increased to 200 mcg if required.
Chronic Therapy: Adults and Children: Up to 200 mcg 4 times daily.
On demand use of Ventolin should not exceed 4 times daily. Reliance on such supplementary use or a sudden increase in dose indicates deteriorating asthma (see Precautions).
Administration: Ventolin is administered by the oral inhaled route only.
Overdosage
The most common signs and symptoms of overdose with Ventolin are transient β-agonist pharmacologically mediated events (see Precautions and Adverse Reactions).
Hypokalaemia may occur following overdosage with Ventolin. Serum potassium levels should be monitored.
Lactic acidosis has been reported in association with high therapeutic doses as well as overdoses of short-acting β-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 eg, wheezing) may be indicated in the setting of overdose.
Contraindications
Hypersensitivity to any of components of Ventolin Inhaler (see Description). Non-IV formulations of Ventolin must not be used to arrest uncomplicated premature labour or threatened abortion.
Special Precautions
The management of asthma should normally follow a stepwise programme and patient response should be monitored clinically and by lung function tests.
Increasing use of short-acting bronchodilators, in particular β2-agonists to relieve symptoms indicates deterioration of asthma control. Under these conditions, the patient's therapy plan should be re-assessed.
Sudden and progressive deterioration in asthma control is potentially life-threatening and consideration should be given to starting or increasing corticosteroid therapy. In patients considered at risk, daily peak flow monitoring may be instituted.
Ventolin should be administered cautiously to patients with thyrotoxicosis.
Potentially serious hypokalaemia may result from β2-agonist therapy mainly from parenteral and nebulised administration.
Particular caution is advised in acute severe asthma as this effect may be potentiated by concomitant treatment with xanthine derivatives, steroids, diuretics and by hypoxia. It is recommended that serum potassium levels are monitored in such situations.
As with other inhalation therapy, paradoxical bronchospasm may occur, resulting in an immediate increase in wheezing after dosing. This should be treated immediately with an alternative presentation or a different fast-acting inhaled bronchodilator, if immediately available. Ventolin Inhaler should be discontinued, and if necessary a different fast-acting bronchodilator instituted for on-going use.
In the event of a previously effective dose of inhaled Ventolin failing to give relief for at least 3 hrs, the patient should be advised to seek medical advice in order that any necessary additional steps may be taken.
Patients' inhaler technique should be checked to make sure that aerosol actuation is synchronised with inspiration of breath for optimum delivery of the drug to the lungs.
Effects on the Ability to Drive or Operate Machinery: None reported.
Impairment of Fertility: There is no information on the effects of salbutamol on human fertility. There were no adverse effects on fertility in animals (see Pharmacology: Toxicology: Preclinical Safety Data under Actions).
Use in pregnancy: Administration of drugs during pregnancy should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus.
During worldwide marketing experience, rare cases of various congenital anomalies, including cleft palate and limb defects have been reported in the offspring of patients being treated with Ventolin. Some of the mothers were taking multiple medications during their pregnancies. As no consistent pattern of defects can be discerned, and baseline rate for congenital anomalies is 2-3%, a relationship with Ventolin use cannot be established.
Use in lactation: Salbutamol is probably secreted in breast milk, its use in nursing mothers is not recommended unless the expected benefits outweigh any potential risk. It is not known whether salbutamol in breast milk has a harmful effect on the neonate.
Use In Pregnancy & Lactation
Impairment of Fertility: There is no information on the effects of salbutamol on human fertility. There were no adverse effects on fertility in animals (see Pharmacology: Toxicology: Preclinical Safety Data under Actions).
Use in pregnancy: Administration of drugs during pregnancy should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus. During worldwide marketing experience, rare cases of various congenital anomalies, including cleft palate and limb defects have been reported in the offspring of patients being treated with Ventolin. Some of the mothers were taking multiple medications during their pregnancies. As no consistent pattern of defects can be discerned, and baseline rate for congenital anomalies is 2-3%, a relationship with Ventolin use cannot be established.
Use in lactation: Salbutamol is probably secreted in breast milk, its use in nursing mothers is not recommended unless the expected benefits outweigh any potential risk. It is not known whether salbutamol in breast milk has a harmful effect on the neonate.
Adverse Reactions
Adverse events are listed below by system organ class and frequency. Frequencies are defined as: Very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1000) and very rare (<1/10,000) including isolated reports. Very common and common events were generally determined from clinical trial data. Rare and very rare events were generally determined from spontaneous data.
Immune System Disorders: Very Rare: Hypersensitivity reactions including angioedema, urticaria, bronchospasm, hypotension and collapse.
Metabolism and Nutrition Disorders:
Rare: Hypokalaemia.
Potentially serious hypokalaemia may result from β2-agonist therapy.
Nervous System Disorders: Common: Tremor, headache. Very Rare: Hyperactivity.
Cardiac Disorders: Common: Tachycardia. Uncommon: Palpitations. Very Rare: Cardiac arrhythmias including atrial fibrillation, supraventricular tachycardia and extrasystoles.
Vascular Disorders: Rare: Peripheral vasodilatation.
Respiratory, Thoracic and Mediastinal Disorders: Very Rare: Paradoxical bronchospasm.
Gastrointestinal Disorders: Uncommon: Mouth and throat irritation.
Musculoskeletal and Connective Tissue Disorders:
Uncommon: Muscle cramps.
Drug Interactions
Salbutamol and non-selective β-blocking drugs eg, propranolol, should not usually be prescribed together.
Ventolin is not contraindicated in patients under treatment with monoamine oxidase inhibitors (MAOIs).
Caution For Usage
Instructions for Use and Handling:
Testing the Inhaler: Before using for the first time, remove the mouthpiece cover by gently squeezing the sides of the cover, shake the inhaler well, and release 2 puffs into the air to make sure that it works. If it has not been used for ≥5 days, shake it well and release 2 puffs into the air to make sure that it works.
Using the Inhaler: 1. Remove the mouthpiece cover by gently squeezing the sides of the cover.
2. Check inside and outside of the inhaler including the mouthpiece for the presence of loose objects.
3. Shake the inhaler well to ensure that any loose objects are removed and that the contents of the inhaler are evenly mixed.
4. Hold the inhaler upright between fingers and thumb with the thumb on the base, below the mouthpiece.
5. Breathe out as far as is comfortable and then place the mouthpiece in the mouth between the teeth and close the lips around it but do not bite.
6. Just after starting to breathe in through the mouth press down on the top of the inhaler to release Ventolin while still breathing in steadily and deeply.
7. While holding the breath, take the inhaler from the mouth and take the finger from the top of the inhaler. Continue holding the breath for as long as is comfortable.
8. If you are to take further puffs keep the inhaler upright and wait about ½ a minute before repeating steps 3-7.
9. Replace the mouthpiece cover by firmly pushing and snapping the cap into position.
Important: Do not rush stages 5, 6 and 7. It is important that the patient start to breathe in as slowly as possible just before operating the inhaler.
Practise in front of a mirror for the first few times. If the patient see 'mist' coming from the top of the inhaler or the sides of the mouth, the patient should start again from stage 2.
If the physician has given the patient different instructions for using the inhaler, follow them carefully. Inform the physician if the patient have any difficulties.
Cleaning: Inhaler should be cleaned at least once a week.
1. Remove the metal canister from the plastic casing of the inhaler and remove the mouthpiece cover.
2. Rinse the actuator thoroughly under warm running water.
3. Dry the actuator thoroughly inside and out.
4. Replace the metal canister and mouthpiece cover.
Do not put the metal canister into water.
Storage
Store below 30°C. Protect from frost and direct sunlight.
Replace the mouthpiece cover firmly and snap it into position.
As with most inhaled medications in aerosol canisters, the therapeutic effect of Ventolin inhaler may decrease when canister is cold.
The canister should not be broken, punctured or burnt, even when apparently empty.
Shelf-Life: 24 months.
ATC Classification
R03AC02 - salbutamol ; Belongs to the class of adrenergic inhalants, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
Presentation/Packing
Inhaler 100 mcg/inhalation (metered-dose, with a specially designed actuator) x 200 doses.
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