Salbutamol Health Dictionary

The sites in the body on which ADRENALINE and comparable stimulants of the SYMPATHETIC NERVOUS SYSTEM act. Drugs which have an adrenaline-like action are described as being adrenergic. There are ?ve di?erent types of adrenergic receptors, known as alpha1, alpha2, beta1, beta2 and beta3 respectively. Stimulation of alpha receptors leads to constriction of the bronchi, constriction of the blood vessels with consequent rise in blood pressure, and dilatation of the pupils of the eyes. Stimulation of beta1 receptors quickens the rate and output of the heart, while stimulation of beta2 receptors dilates the bronchi. Beta3 receptors are now known to mediate so-called non-shivering thermogenesis, a way of producing heat from specialised fat cells that is particularly relevant to the human infant.

For long it had been realised that in certain cases of ASTHMA, adrenaline had not the usual bene?cial e?ect of dilating the bronchi during an attack; rather it made the asthma worse. This was due to its acting on both the alpha and beta adrenergic receptors. A derivative, isoprenaline, was therefore produced which acted only on the beta receptors. This had an excellent e?ect in dilating the bronchi, but unfortunately also affected the heart, speeding it up and increasing its output – an undesirable e?ect which meant that isoprenaline had to be used with great care. In due course drugs were produced, such as salbutamol, which act predominantly on the beta2 adrenergic receptors in the bronchi and have relatively little e?ect on the heart.

The converse of this story was the search for what became known as BETA-ADRENOCEPTORBLOCKING DRUGS, or beta-adrenergic-blocking drugs. The theoretical argument was that if such drugs could be synthesised, they could be of value in taking the strain o? the heart – for example: stress ? stimulation of the output of adrenaline ? stimulation of the heart ? increased work for the heart. A drug that could prevent this train of events would be of value, for example in the treatment of ANGINA PECTORIS. Now there is a series of beta-adrenoceptor-blocking drugs of use not only in angina pectoris, but also in various other heart conditions such as disorders of rhythm, as well as high blood pressure. They are also proving valuable in the treatment of anxiety states by preventing disturbing features such as palpitations. Some are useful in the treatment of migraine.... adrenergic receptors

Substances that can be inhaled into the body through the lungs. They may be delivered in traditional form dissolved in hot water and inhaled in the steam, or as an aerosol – a suspension of very small liquid or solid particles in the air. The latter are now usually delivered by devices in which the aerosol is kept under pressure in a small hand-held cylinder and delivered in required doses by a release mechanism.

Aerosols Asthmatic patients (see ASTHMA) ?nd aerosol devices to be of value in controlling their attacks. They provide an e?ective and convenient way of applying drugs directly to the bronchi, thus reducing the risks of unwanted effects accompanying SYSTEMIC therapy. BRONCHODILATOR aerosols contain either a beta-sympathomimetic agent or ipratropium bromide, which is an ANTICHOLINERGIC drug.

ISOPRENALINE was the ?rst compound to be widely used as an aerosol. It did however stimulate beta1 receptors in the heart as well as beta2 receptors in the bronchi, and so produced palpitations and even dangerous cardiac arrhythmias. Newer beta-adrenoceptor agonists are speci?c for the beta2 receptors and thus have a greater safety margin. They include SALBUTAMOL, TERBUTALINE, rimiterol, fenoterol and reproterol. Unwanted effects such as palpitations, tremor and restlessness are uncommon with these, more speci?c preparations. In patients who get insu?cient relief from the beta-adrenoreceptor agonist, the drug ipratropium bromide is worth adding. Salmeterol is a longer-acting choice for twice-daily administration: it is not intended for the relief of acute attacks, for which shorter-acting beta2 stimulants such as salbutamol should be used. Salmeterol should be added to existing corticosteroid therapy (see CORTICOSTEROIDS), rather than replacing it.

Patients must be taught carefully and observed while using their inhalers. It is important for them to realise that if the aerosol no longer gives more than slight transient relief, they should not increase the dose but seek medical help.... inhalants

A nebuliser makes an aerosol (see under INHALANTS) by blowing air or oxygen through a solution of a drug. Many inhaled drugs such as SALBUTAMOL, ipratropium and beclomethasone can be given in this way. It has the advantage over a metered dose inhaler (MDI) that no special e?ort is required to coordinate breathing, and a nebuliser allows a much greater volume of the drug to be delivered to where it is needed (the airways) compared with that of MDIs. The use of higher doses of bronchodilator drugs made possible by the nebuliser means that the risk of unwanted side-effects is also increased. Fortunately the safety pro?le of anti-asthmatic drugs such as salbutamol is extremely high and overdose is generally well-tolerated.... nebulisers

Drugs that are used to delay the premature delivery of a fetus. Beta2-adrenoceptor stimulants, such as salbutamol, relax the muscle of the uterus and may postpone labour for days or weeks in at-risk pregnancies of 24–33 weeks’ gestation. Delay of premature labour for up to 48 hours allows time for corticosteroid drugs to be given to the mother to help the fetal lungs to mature.... uterine muscle relaxants

n. an agent that causes widening of the air passages by relaxing bronchial smooth muscle. *Sympathomimetic drugs that stimulate ?2 adrenoceptors, such as *formoterol, *salbutamol, and *terbutaline, are potent bronchodilators and are used for relief of bronchial asthma and chronic obstructive pulmonary disease. These drugs are often administered as aerosols, giving rapid relief, but at high doses they may stimulate the heart. Some antimuscarinic drugs (e.g. *ipratropium and *theophylline) are also used as bronchodilators.... bronchodilator

Asthma is a common disorder of breathing characterised by widespread narrowing of smaller airways within the lung. In the UK the prevalence among children in the 5–12 age group is around 10 per cent, with up to twice the number of boys affected as girls. Among adults, however, the sex incidence becomes about equal. The main symptom is shortness of breath. A major feature of asthma is the reversibility of the airway-narrowing and, consequently, of the breathlessness. This variability in the obstruction may occur spontaneously or in response to treatment.

Cause Asthma runs in families, so that parents with asthma have a strong risk of having children with asthma, or with other atopic (see ATOPY) illnesses such as HAY FEVER or eczema (see DERMATITIS). There is therefore a great deal of interest in the genetic basis of the condition. Several GENES seem to be associated with the condition of atopy, in which subjects have a predisposition to form ANTIBODIES of the IgE class against allergens (see ALLERGEN) they encounter – especially inhaled allergens.

The allergic response in the lining of the airway leads to an in?ammatory reaction. Many cells are involved in this in?ammatory process, including lymphocytes, eosinophils, neutrophils and mast cells. The cells are attracted and controlled by a complex system of in?ammatory mediators. The in?amed airway-wall produced in this process is then sensitive to further allergic stimuli or to non-speci?c challenges such as dust, smoke or drying from the increased respiration during exercise. Recognition of this in?ammation has concentrated attention on anti-in?ammatory aspects of treatment.

Continued in?ammation with poor control of asthma can result in permanent damage to the airway-wall such that reversibility is reduced and airway-narrowing becomes permanent. Appropriate anti-in?ammatory therapy may help to prevent this damage.

Many allergens can be important triggers of asthma. House-dust mite, grass pollen and animal dander are the commonest problems. Occupational factors such as grain dusts, hard-metals fumes and chemicals in the plastic and paint industry are important in some adults. Viral infections are another common trigger, especially in young children.

The prevalence of asthma appears to be on the increase in most countries. Several factors have been linked to this increase; most important may be the vulnerability of the immature immune system (see IMMUNITY) in infants. High exposure to allergens such as house-dust mite early in life may prime the immune system, while reduced exposure to common viral infections may delay the maturation of the immune system. In addition, maternal smoking in pregnancy and infancy increases the risk.

Clinical course The major symptoms of asthma are breathlessness and cough. Occasionally cough may be the only symptom, especially in children, where night-time cough may be mistaken for recurrent infection and treated inappropriately with antibiotics.

The onset of asthma is usually in childhood, but it may begin at any age. In childhood, boys are affected more often than girls but by adulthood the sex incidence is equal. Children who have mild asthma are more likely to grow out of the condition as they go through their teenaged years, although symptoms may recur later.

The degree of airway-narrowing, and its change with time and treatment, can be monitored by measuring the peak expiratory ?ow with a simple monitor at home – a peak-?ow meter. The typical pattern shows the peak ?ow to be lowest in the early morning and this ‘morning dipping’ is often associated with disturbance of sleep.

Acute exacerbations of asthma may be provoked by infections or allergic stimuli. If they do not respond quickly and fully to medication, expert help should be sought urgently since oxygen and higher doses of drugs will be necessary to control the attack. In a severe attack the breathing rate and the pulse rate rise and the chest sounds wheezy. The peak-?ow rate of air into the lungs falls. Patients may be unable to talk in full sentences without catching their breath, and the reduced oxygen in the blood in very severe attacks may produce the blue colour of CYANOSIS in the lips and tongue. Such acute attacks can be very frightening for the patient and family.

Some cases of chronic asthma are included in the internationally agreed description CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) – a chronic, slowly progressive disorder characterised by obstruction of the air?ow persisting over several months.

Treatment The ?rst important consideration in the treatment of asthma is avoidance of precipitating factors. When this is a speci?c animal or occupational exposure, this may be possible; it is however more di?cult for house-dust mite or pollens. Exercise-induced asthma should be treated adequately rather than avoiding exercise.

Desensitisation injections using small quantities of speci?c allergens are used widely in some countries, but rarely in the UK as they are considered to have limited value since most asthma is precipitated by many stimuli and controlled adequately with simple treatment.

There are two groups of main drugs for the treatment of asthma. The ?rst are the bronchodilators which relax the smooth muscle in the wall of the airways, increase their diameter and relieve breathlessness. The most useful agents are the beta adrenergic agonists (see ADRENERGIC RECEPTORS) such as salbutamol and terbutaline. They are best given by inhalation into the airways since this reduces the general side-effects from oral use. These drugs are usually given to reverse airway-narrowing or to prevent its onset on exercise. However, longer-acting inhaled beta agonists such as salmeterol and formoterol or the theophyllines given in tablet form can be used regularly as prevention. The beta agonists can cause TREMOR and PALPITATION in some patients.

The second group of drugs are the antiin?ammatory agents that act to reduce in?ammation of the airway. The main agents in this group are the CORTICOSTEROIDS. They must be taken regularly, even when symptoms are absent. Given by inhalation they have few side-effects. In acute attacks, short courses of oral steroids are used; in very severe disease regular oral steroids may be needed. Other drugs have a role in suppressing in?ammation: sodium cromoglycate has been available for some years and is generally less e?ective than inhaled steroids. Newer agents directed at speci?c steps in the in?ammatory pathway, such as leukotriene receptor-antagonists, are alternative agents.

Treatment guidelines have been produced by various national and international bodies, such as the British Thoracic Society. Most have set out treatment in steps according to severity, with objectives for asthma control based on symptoms and peak ?ow. Patients should have a management plan that sets out their regular treatment and their appropriate response to changes in their condition.

Advice and support for research into asthma is provided by the National Asthma Campaign.

See www.brit-thoracic.org.uk

Prognosis Asthma is diagnosed in 15–20 per cent of all pre-school children in the developed world. Yet by the age of 15 it is estimated that fewer than 5 per cent still have symptoms. A study in 2003 reported on a follow-up of persons born in 1972–3 who developed asthma and still had problems at the age of nine. By the time these persons were aged 26, 27 per cent were still having problems; around half of that number had never been free from the illness and the other half had apparently lost it for a few years but it had returned.... asthma

A group of drugs that widen the bronchioles (small airways in the lungs) to increase air flow and improve breathing, especially in the treatment of asthma and chronic obstructive pulmonary disease (see pulmonary disease, chronic obstructive). There are 3 main types of bronchodilator: sympathomimetic drugs (such as salbutamol), anticholinergic drugs, and xanthine drugs (such as aminophylline). Sympathomimetic drugs are used primarily for the rapid relief of breathing difficulty. Anticholinergic and xanthine drugs are more often used for the long-term prevention of attacks of breathing difficulty. Drugs can be given by inhaler, in tablet form, or, in severe cases, by nebulizer or injection.

The main side effects of sympathomimetics are palpitations and trembling.

Anticholinergics may cause dry mouth, blurred vision, and, rarely, difficulty in passing urine.

Xanthines may cause headaches, nausea and palpitations.... bronchodilator drugs

adj. having the effect of stimulating the *sympathetic nervous system. The actions of sympathomimetic drugs are adrenergic: they act on alpha or beta *adrenoceptors. Alpha-adrenergic stimulants (alpha agonists) stimulate alpha receptors. They include *vasoconstrictors (e.g. *ephedrine, *phenylephrine, *metaraminol), used to treat nasal congestion and severe hypotension, and the selective ?2 agonists *apraclonidine and *brimonidine, which are used in the treatment of glaucoma. Beta-adrenergic stimulants (beta agonists) stimulate ?1 and/or ?2 adrenoceptors. ?2 agonists such as *salbutamol, *salmeterol, and *terbutaline relax bronchial smooth muscle and are used as *bronchodilators. Some ?2 agonists, including salbutamol, relax uterine muscle and are sometimes used in the treatment of premature labour (see tocolytic). ?1 agonists (e.g. *dobutamine) stimulate ?1 receptors in the heart and are therefore used for their *inotropic effects.... sympathomimetic