Ventolin Inhaler

Ventolin Description

Ventolin is a selective beta2- adrenoreceptors agonist. In therapeutic doses it acts on bronchial smooth muscles beta2-adrenoreceptors, providing little or no effect on myocardium beta1-adrenoreceptors. Has pronounced bronchodilator effect, preventing or arresting bronchospasm, reduces airways resistance. Increases vital lung capacity (VLC). Increases mucociliary clearance (at chronic bronchitis up to 36%), stimulates mucus secretion, activates ciliated epithelium function.

In recommended therapeutic doses has no adverse effect on cardiovascular system, does not cause increase in blood pressure. To a lesser extent, as compared with drugs of this group, has positive chrono – and inotropic effect. Causes coronary arteries extension.

It has a number of metabolic effects: reduces potassium concentration in blood plasma affects glycogenolysis and insulin release, has hyperglycemic (especially at patients with bronchial asthma) and lipolytic effect, increases acidosis risk.

After inhalation, action develops rapidly, effect begins after 5 minutes, maximal – after 30 – 90 minutes (75% of maximal effect is achieved within 5 minutes), duration – 4 – 6 hours.

Composition

Micronized salbutamol sulphate excipients.

Pharmacokinetics

After inhalation, 10 – 20% of salbutamol dose reaches lower respiratory tract. The rest of the dose remains in inhaler or is deposited in oropharynx and then swallowed. Fraction deposited in airways is absorbed into pulmonary tissues and blood, but it is not metabolized in lungs.

Swallowed part of inhaled dose is absorbed from gastrointestinal tract and is extensively metabolized during «first passage» through liver, turning into inactive 4′-O-sulphate (phenolic sulphate).

Salbutamol and plasma protein binding is 10%. Cleared partially through kidneys unchanged and partially in the form of inactive 4′-O-sulphate (phenolic sulphate) which is also excreted mainly with urine. Only small amount of administered salbutamol dose is excreted with feces. Most of salbutamol dose, administered intravenously, orally or by inhalation, is excreted within 72 hours.

Indications

Bronchial asthma:

• relieve asthma symptoms when they occur;
• prevent bronchospasm attacks associated with exposure to allergen or exercise-induced;
• used as a component in long-term maintenance asthma treatment.

Other chronic pulmonary diseases accompanied by reversible airway obstruction, including chronic obstructive pulmonary disease (COPD), chronic bronchitis, pulmonary emphysema.

Bronchodilators should not be sole or main component of unstable or severe asthma therapy. If there is no response to salbutamol at patients with severe asthma, glucocorticosteroids therapy is recommended to achieve and maintain disease control. Lack of response to salbutamol therapy may indicate need for urgent medical advice or treatment.

Pharmaceutical Form

Dosed aerosol for inhalation (sometimes mistakenly referred to as spray).

Solution for inhalation in nebula in ampoules (Ventolin Nebula) (sometimes mistakenly referred to as syrup).

Instructions for Use and Dosage

Ventolin Inhaler is intended for administration by inhalation. Increased demand for beta2-adrenoreceptors agonists may be a sign of asthma exacerbation. In such situation re-evaluation of treatment scheme may be required considering reasonability of simultaneous GCS therapy.

Since overdose may be accompanied by adverse effects development, drug dosage or frequency of administration may be increased only on doctor’s advice.

Duration of salbutamol action at most patients is from 4 to 6 hours.

Patients, who experience difficulties with synchronizing inhalation with dosed aerosol inhaler under pressure, may use spacer.

At children and newborn receiving Ventolin drug, it is advisable to use pediatric spacer device with face mask.

To relieve bronchospasm attack at adults, recommended dosage is 100 or 200 mcg; at children – 100 mcg, dosage may be increased to 200 mcg if necessary. Ventolin asthma inhaler is not recommended to use more than 4 times a day. Need for frequent use of maximal Ventolin dosage or sudden increase in dosage indicates asthma exacerbation.

To prevent bronchospasm attacks associated with exposure to allergen or exercise-induced, adults – 200 mcg 10 – 15 minutes before exposure to provoking factor or exercise; children – 100 mcg 10 – 15 minutes before exposure to provoking factor or exercise, dosage may be increased up to 200 mcg if necessary.

In case of long-term maintenance treatment at adults – up to 200 mcg 4 times a day; at children – up to 200 mcg 4 times a day.

Application

Inhaler check up

Before first application or if inhaler is not used longer than a week, remove cap from mouthpiece, slightly squeezing it on each side, shake inhaler properly and make two air spraying in order to ensure that inhaler is in working condition.

Inhaler usage

1. Remove the cap from mouthpiece, gently squeezing it on each side.
2. Check mouthpiece inside and outside to make sure it is clean.
3. Shake inhaler.
4. Hold inhaler between pointer and thumb in a vertical bottom-up position, with the thumb placed on basis under mouthpiece.
5. Make a slow deep breath, grasp mouthpiece with your lips, without clenching teeth.
6. Making the deepest breath through your mouth at the same time press upper part of inhaler to release one dose of inhaled salbutamol.
7. Hold your breath for a few seconds, take mouthpiece out of your mouth, then slowly exhale.
8. For the second dose, holding inhaler in a vertical position, wait 30 seconds and then repeat steps 3 – 7.
9. Tightly cover mouthpiece with protective cap.

Performing step 5, 6 and 7, you must not rush. You should begin to inhale as slowly as possible just before pressing inhaler valve. During first few times it is recommended to practice in front of the mirror. If you see «mist» coming from the top of inhaler or from corners of your mouth, it is necessary to start again from step 2.

If your doctor has given other instructions on inhaler usage, you should strictly abide them. If patients have difficulties with using inhaler, he should consult a doctor.

Cleaning inhaler

The inhaler should be cleaned at least once a week.

1. Remove metal container from plastic case and remove mouthpiece cup.
2. Rinse plastic case and mouthpiece cup with warm running water.
3. Dry plastic case and mouthpiece cup fully both outside and inside. Avoid overheating.
4. Put metal container in plastic case and put on mouthpiece cup.

Do not put metal container into water.

Overdose

Symptoms: signs and symptoms of salbutamol overdose are transient phenomena, pharmacologically mediated by beta-adrenoreceptors stimulation, such as low arterial blood pressure, tachycardia, muscle tremors, nausea, vomiting. Application of large salbutamol doses can cause metabolic changes, including hypokalemia, it is necessary to control potassium concentration in blood serum. At high doses, as well as at overdose with short-acting beta-agonists lactic acidosis was observed, so in case of overdose control over rise of serum lactate and possibility of metabolic acidosis can be indicated (especially at maintaining tachypnea or its exacerbations, despite eliminating other signs of bronchoconstriction, such as wheezing).

Side Effect

• angioedema;
• urticaria fever;
• bronchospasm;
• hypotension;
• collapse;
• hypokalemia;
• tremor;
• headaches;
• hyperactivity;
• tachycardia;
• arrhythmia (including atrial fibrillation, supraventricular tachycardia and extrasystoles);
• peripheral vasodilation;
• paradoxical bronchospasm;
• oral cavity and pharynx mucous membrane irritation;
• muscle cramps.

Contraindications

• carrying out premature birth;
• threatening abortion;
• hypersensitivity to drug components.

With caution salbutamol should be used by patients with thyrotoxicosis, tachyarrhythmia, myocarditis, cardiac abnormalities, aortic stenosis, ischemic heart disease, severe chronic heart insufficiency, arterial hypertension, pheochromocytoma, decompensated diabetes, glaucoma.

Pregnancy and Lactation Period

At pregnancy the drug should be used only if expected benefit to the mother outweighs potential risk to the fetus.

Post approval examination revealed rare cases of various congenital malformations at children, including «cleft palate» and limb malformations, while taking salbutamol during pregnancy. In some of these cases, mothers were taking several concomitant medications during pregnancy. In absence of permanent nature of defects and background congenital anomalies incidence frequency, ranging from 2 to 3%, causal relationship to drug intake has not been established.

Salbutamol is likely to penetrate breast milk and therefore it is not recommended for breastfeeding mothers unless expected benefit to the mother outweighs potential risk to the child. There is no data about salbutamol in breast milk harmful effect on child.

Fertility

There is no data on salbutamol effects on human fertility. Preclinical researches didn’t reveal adverse effect on fertility in animals.

Ventolin for Children

Ventolin asthma inhaler is contraindicated to children younger than 2 years (for Ventolin Nebula – up to 1,5 years).

Special Instructions

• Asthma treatment is recommended to be carried out gradually, controlling patient’s clinical response to treatment and respiratory function.
• Increasing demand for use of short-acting bronchodilators, in particular beta2-adrenergic receptors agonists, for asthma symptoms control indicates disease exacerbation. In such cases, you should re-consider patient’s treatment scheme. Sudden and progressive asthma exacerbation may pose potential threat to patient’s life, so in such cases, reasonability of appointing or increasing corticosteroids doses should be considered. At high-risk patients peak expiratory flow rate is recommended for daily monitoring.
• Beta2-adrenoceptors agonists therapy, particularly when administered parenterally or through nebulizer, can result in hypokalemia.
• It is advised to perform special caution in severe asthma attacks treatment, since in these cases, hypokalemia may be enhanced by simultaneous use of xanthine derivatives, corticosteroids, diuretics and also due to hypoxia. In such situations, it is recommended to monitor potassium level in blood serum.
• In absence of previously effective dose effect of inhaled salbutamol for at least 3 hours, patient should seek medical attention for need for any additional measures.
• Patients should be instructed on correct use of Ventolin Inhaler.

Drug Interactions

• Simultaneous use of salbutamol and non-selective beta-adrenoceptor blockers, such as propranolol, is not recommended.
• Salbutamol is not contraindicated to patients receiving MAO inhibitors.
• At patients with thyrotoxicosis, Ventolin enhances CNS stimulants effect, tachycardia.
• Theophylline and other xanthines combined with Ventolin increase tachyarrhythmia risk.
• Co-administration with anticholinergic drugs (including inhalants) can increase intraocular pressure.
• Diuretics and glucocorticosteroids (GCS) enhance salbutamol hypokalemic effect.