Budezonid LEK-AM: composition and pharmaceutical form
The pack holds neither a pressurised inhaler nor ampoules, but hard capsules and a separate capsule inhaler. One capsule is one inhaled dose and contains 200 or 400 µg of budesonide. The inhaler from the pack is the only device through which the medicine may be inhaled: these capsules are not designed for other inhalers.
From the form follows a warning that stands on its own in the leaflet: the capsules are intended for inhalation only and must not be swallowed. Cases are known of patients taking a capsule by mouth by mistake, and in most of them there were no adverse reactions — but no therapeutic effect either. The second detail of the composition is lactose: because of it the medicine is unsuitable for people with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome.
How Budezonid LEK-AM works
The first thing worth knowing about budesonide is its pace. Control of asthma after the start of treatment appears within about ten days, and no inhalation brings relief in the first minutes. The medicine deals not with the attack but with the inflammation that leads to the attack: it acts on intracellular glucocorticoid receptors and through them suppresses the production of a whole set of cytokines, enzymes and adhesion molecules — the substances by which chronic inflammation in the airways is maintained.
The mechanism of action of glucocorticoids in asthma is still not fully deciphered, but the result of regular use is described precisely: inflammation in the lungs decreases, lung function improves, symptoms weaken, bronchial hyperreactivity falls — the tendency to answer cold, smells and exertion with spasm — and exacerbations become rarer. All these effects rest on the word «regularly»: the medicine is taken every day, including when nothing is troubling you, because the point of the treatment is preventive.
Indications
The leaflet lists two indications: bronchial asthma and chronic obstructive pulmonary disease. Both belong to conditions in which chronic inflammation runs in the airways, and both require long-term treatment rather than a short course.
It is worth noticing the asymmetry of the document itself: the dosing schedules are written out for asthma — separately for adults and for children over six years — whereas for COPD the leaflet gives no numerical schedules. That means that with this diagnosis the dose and the regimen are set by the doctor, relying on current treatment guidance.
Method of use and dosage
Asthma treatment follows current guidelines, the dose is chosen individually and the aim is the lowest effective dose for maintenance therapy. This medicine has a feature that suspensions and aerosols do not: the dose steps in capsules, so below a certain threshold it is simply not used. If a single dose has to be smaller than 200 µg, or the daily dose smaller than 400 µg in divided doses, another product is needed. When switching from one type of inhaler to another the dose is reviewed: the same figure on the pack does not mean the same dose reaching the lungs.
In adults with mild asthma treatment may start with 200 µg once a day; the usual dose is 200-400 µg twice a day, that is, 400-800 µg per day. If symptoms worsen, when switching from tablet corticosteroids to inhaled budesonide, or when the tablet dose is being reduced, the daily dose is raised to 1600 µg divided into two to four doses. In children over six years treatment starts with 200 µg once a day, the usual dose is 200 µg twice a day and the maximum daily dose is 800 µg; the child performs the inhalation under adult supervision, and the very choice of this form depends on whether they can handle the inhaler correctly. Under six years the medicine is not prescribed: there are no data on efficacy and safety at that age. Clinical studies were not carried out in people over 65, nor in renal and hepatic impairment; because of the hepatic metabolism of budesonide, caution is needed in liver disease. After each inhalation the mouth is rinsed thoroughly — this reduces the risk of fungal infection, throat irritation and general steroid effects.
Contraindications
The first contraindication is the usual one: hypersensitivity to budesonide or to any excipient, including the lactose of the base. The second sounds more serious for an inhaled steroid: the medicine is not used in active pulmonary tuberculosis. The reason lies in the nature of glucocorticoids themselves — they suppress the local immune response, and the tuberculous process gains an advantage in those conditions.
The line between prohibition and caution runs here through the word «active». In latent pulmonary tuberculosis, and also in fungal and viral infections of the airways, the medicine is not forbidden but requires particular caution and monitoring. The same group includes bronchiectasis and pneumoconiosis: in them the likelihood of fungal infection under a steroid is higher.
Special warnings and precautions
Anyone treated with this medicine should always carry two things: a short-acting inhaled bronchodilator to relieve acute symptoms and a card stating that they have asthma. Budesonide does not interrupt acute bronchospasm and is not the treatment of choice in status asthmaticus or in an attack. If attacks become more frequent, if the bronchodilator is needed more often or respiratory symptoms do not go away, the condition is reassessed and a decision is made on whether anti-inflammatory treatment needs strengthening — raising the dose of the inhaled steroid or adding tablets, and an antibiotic if there is an infection. Rarely the inhalation itself provokes bronchospasm; such a paradoxical response means immediate withdrawal of the medicine and, if necessary, other treatment — it is relieved with a fast-acting inhaled bronchodilator.
A story of its own is the switch from tablet steroids to inhaled ones, and it is done only when the patient is relatively stable. For about ten days high doses of inhaled budesonide are used together with the previous tablets; then the tablet dose is reduced gradually — for example, by 2.5 mg of prednisolone or an equivalent dose per month — down to the lowest possible. Neither the tablets nor budesonide itself may be stopped abruptly. The first month after the switch calls for special attention: it must be confirmed that the reserve of adrenal cortex hormones is enough for a stressful situation — injury, surgery, severe infection — and in such cases some patients are given an additional corticosteroid. The function of the hypothalamic-pituitary-adrenal axis is monitored regularly. A side effect of the switch itself is that the tablets were suppressing more than asthma: after they are withdrawn, allergic rhinitis or eczema may show up, and lethargy, muscle and joint pain, nausea or vomiting may appear — allergic manifestations are treated with antihistamines or topical steroids. General steroid effects are possible with inhalation too, especially with high doses used for a long time, although their likelihood is markedly lower than with oral administration: suppression of adrenal function, excessive production of their hormones and Cushing's syndrome, growth retardation in children and adolescents, reduced bone mineral density, cataract and glaucoma, hypersensitivity reactions and, less often, psychiatric changes. That is why children treated for a long time with inhaled steroids have their growth measured regularly, and if it slows, the treatment is reviewed, an attempt is made to reduce the dose to the minimum sufficient one and a consultation with a paediatric pulmonologist is considered; the long-term consequences of such slowing, including final height in adulthood, are unknown. Separate caution is needed with prolonged administration of budesonide together with a strong CYP3A4 inhibitor. Oral candidiasis is prevented by rinsing the mouth after each inhalation, and if it does appear, in most cases topical antifungals are enough and treatment does not have to be interrupted.
Drug interactions
Budesonide is metabolised mainly by the CYP3A4 isoenzyme of the cytochrome P450 system, and with that the whole logic of its interactions is exhausted. Substances that inhibit this enzyme slow down the metabolism of budesonide, and its overall amount in the body rises. They include itraconazole, atazanavir, ketoconazole, ritonavir, nelfinavir, amiodarone and clarithromycin — that is, some antifungals, HIV medicines, an antiarrhythmic and a macrolide antibiotic, all of which appear in prescriptions fairly often.
The practical consequence is simple: with concomitant use the function of the adrenal cortex is monitored and the budesonide dose is adjusted according to the response to treatment, while a long combination with a strong CYP3A4 inhibitor requires separate caution. The opposite case is substances that strongly stimulate CYP3A4, of which the leaflet names rifampicin: they speed up the metabolism of budesonide and its amount in the body falls, and with it the anti-inflammatory effect weakens.
Pregnancy and breastfeeding
The leaflet contains no special recommendations for women of childbearing age. In pregnancy the medicine is used only in those cases where, in the doctor's opinion, the benefit to the mother outweighs the possible risk to the foetus. There is also a reverse argument, which the leaflet states outright: if glucocorticoids cannot be avoided in a pregnant woman, inhaled ones are preferred, because their general effect on the body is weaker than that of the same hormones in tablets. There are no data on the effect of budesonide on human fertility.
For breastfeeding a concrete figure is known: budesonide given by inhalation passes into milk, and the expected concentration of the medicine in the child's plasma is about one six-hundredth of the concentration in the mother's plasma. Such amounts look safe, but the clinical effect of the mother's long-term treatment on a breastfed child has not been studied, and the leaflet does not hide that gap. The decision is made by the doctor, weighing the need to treat asthma against the duration of breastfeeding.
Adverse reactions
From the respiratory tract, cough is noted commonly. Rare reactions of the same area include paradoxical bronchospasm, candidiasis of the mouth and throat, hoarseness and throat irritation — all of them connected with the powder passing through the mouth and throat, and it is precisely their likelihood that rinsing reduces. Systemic manifestations are also considered rare: suppression of adrenal function, Cushing's syndrome, excessive production of adrenal cortex hormones, growth retardation in children and adolescents, reduced bone mineral density, cataract and glaucoma, hypersensitivity reactions — rash, urticaria, angioedema, itching — and also behavioural disturbances including depression, described in children.
After the medicine reached the market a number of reports were added whose frequency cannot be estimated, because they came in voluntarily and from an unknown number of people: psychomotor hyperactivity, sleep disorders, anxiety, depression, aggression and changes in behaviour — mainly in children — as well as contact dermatitis as a delayed, fourth-type hypersensitivity reaction. In addition, in long-term clinical studies of medicines containing budesonide, skin bruising and pneumonia have been described.
Overdose
The most serious thing threatened by inhaling large doses over a short time is suppression of the hypothalamic-pituitary-adrenal axis, that is, of the system that governs the production of one's own adrenal cortex hormones. The acute toxicity of budesonide is at the same time low, and the danger of overdose is measured not by poisoning but by a failure of regulation.
Such a situation requires no specific treatment. The leaflet recommends not abandoning the medicine but continuing to use it in the recommended doses so that asthma stays under control: withdrawing an inhaled steroid after going over the dose creates more problems than the excess itself.
How to get a prescription for Budezonid LEK-AM online
This form of budesonide assumes that the person can handle a capsule inhaler, and its dose steps by 200 µg, so the doctor needs to know what was used before, what the daily dose was and on which device. If an inhaled steroid is being prescribed to a child for the first time, age and the ability to take the breath correctly are considered separately.
Budezonid LEK-AM is a prescription medicine, and a prescription at e-zdrowie.com can be arranged remotely: you fill in a medical questionnaire, the doctor studies the answers and issues an electronic prescription, the code arrives by message, and the medicine is dispensed at any Polish pharmacy. When the device or the dose changes, that conversation with the doctor is not a formality: the same figures on different inhalers do not mean the same dose in the lungs.
