Pharmacological action of Serevent Diskus
Serevent Diskus Selective β2-adrenoceptor agonist long-acting (12 h).
Salmeterol molecule has a long side chain that binds to the outer section of the receptor. Due to this salmeterol is more effective to prevent histamine-induced bronchospasm and causes more long (at least 12 hours) bronchodilation compared with β2-adrenergic agonists short action.
Salmeterol inhibits the release of tissue mast cell mediators such as histamine, leukotrienes and prostaglandin D2. Inhibits early and late stage allergic reaction after a single dose suppression of late stage lasts up to 30 hours when the bronchodilatory effect is absent. Single dose of salmeterol reduces bronchial hyperreactivity.
Serevent also increases the frequency of movement of cilia of ciliated epithelium, improves mucociliary clearance, reduces damage to the epithelium of the respiratory tract caused by Haemophilus influenzae and Pseudomonas aeruginosa, and also has antineytrofilnoy activity and the ability to reduce swelling of the mucosa by reducing the release of protein through the vessel wall.
In patients with asthma onset of action of the drug (increase in forced expiratory volume in 1 sec / FEV 1 /> 15%) were reported in 10-20 minutes after inhalation. The full therapeutic effect develops after the first few doses. Action of salmeterol continued for 12 h. This is particularly useful for the treatment of patients with nocturnal attacks of bronchospasm and for prevention of attacks, caused by physical stress.
Pharmacokinetics Serevent Diskus
Suction
In applying Sereventa a dose of 50 mg 2 times a day Serevent Cmax of 200 pg / ml, in a further concentration of the active substance in the plasma decreases rapidly.
Breeding
Serevent is excreted in the bile through the intestines, primarily in the form of hydroxylated metabolite.
Indications Serevent Diskus
Adults
- Bronchial asthma, including prevention of bronchospasm caused by physical stress;
- Chronic obstructive pulmonary disease (COPD) including chronic obstructive bronchitis and emphysema.
Children aged 4 years
- Bronchial asthma, including prevention of bronchospasm caused by exercise.
Dosage Serevent Diskus
Serevent is intended solely for use by inhalation. The drug can be applied through the spacer. To achieve optimal therapeutic effect the drug should be used regularly. The duration of treatment determined by the physician.
Adults in the treatment of asthma and COPD is the recommended dose – to 2 inhalations (2 x 25 mcg salmeterol) two times a day.
The maximum dose (for more severe airway obstruction in patients with bronchial asthma) – 4 inhalations (4 x 25 mcg salmeterol) two times a day.
Children over 4 years the recommended dose – 1-2 inhalations (25-50 mcg salmeterol) two times a day.
The maximum daily dose for children and adolescents aged 4 to 18 years – less than 100 micrograms of salmeterol (no more than 2 inhalations 2 times / day).
Patients with impaired renal function and elderly patients change dose is not required.
Side effects of Serevent Diskus
With the cardiovascular system: possible headache, palpitation, in predisposed patients – cardiac arrhythmia (atrial fibrillation, supraventricular tachycardia and extrasystoles).
From the digestive system: a change of taste sensations, abdominal pain, nausea, vomiting, irritation of the mucous membranes of the mouth or throat.
Allergic reactions: urticaria, angioedema, bronchospasm.
Other: tremor, muscle cramps, arthralgia, hypokalemia, nervousness.
Serevent may cause paradoxical bronchospasm, which must be immediately cut short by rapid inhalation bronchodilator (in such cases should immediately stop using Serevent, assess the condition of the patient, conduct a survey and if necessary, appoint an alternative therapy).
Contraindications
- Children up to age 4 years;
- Hypersensitivity to Serevent and other ingredients.
Precautions should be prescribed the drug for hyperthyroidism, arrhythmias, coronary heart disease (angina III-IV functional class), acute myocardial infarction, uncontrolled hypertension, hypoxia of different genesis, pheochromocytoma, pregnancy, lactation.
Application of pregnancy and breastfeeding
Use of the drug during pregnancy and lactation (breastfeeding) is not recommended except when the expected benefits to the mother outweighs the potential risk to the fetus or infant.
Use in renal impairment
Patients with impaired renal function change in dose is required.
Special instructions Serevent Diskus
Serevent should not appoint pronounced worsening or exacerbation of asthma (increase symptoms of bronchial obstruction, decreased efficiency and increased demand for high-speed inhaled bronchodilators, deterioration pikfluometrii and spirometry).
During exacerbation of asthma, as well as in patients with hypoxia is necessary to control the concentration of potassium in blood plasma.
Patients should be warned that they should not stop taking corticosteroids or reduce their dose without a doctor’s recommendation, even if the condition had improved during treatment Sereventa. Serevent is not a substitute for oral corticosteroids or inhaled, and is appointed in addition to them. Furthermore, it should be borne in mind that for the relief of asthma symptoms should not be inhaled Sereventa additional doses, and recommended agonists β2-adrenoceptor short action.
Since the use of β2-adrenergic agonists in high doses may cause adverse reactions, if necessary increase the dose or frequency of administration Sereventa require medical supervision.
Data obtained during the placebo-controlled study in the U.S., which compared the safety of salmeterol and placebo groups designated in addition to usual asthma therapy for 28 weeks showed a small but statistically significant increase in the number of deaths related to asthma among patients treated with salmeterol (13 deaths per 13,174 patients – 0.099%) compared with patients receiving placebo (4 out of 13 179 – 0.03%). 8 out of 13 patients of the first and 1 out of 4 patients of the second group are African Americans, suggesting that a higher risk of death associated with asthma among the members of this race. It remains unclear whether this fact is associated with the therapy, genetic predisposition or the peculiarities of social behavior of African Americans (late uptake to the doctor and the lack of strict adherence to doctor’s recommendations). In addition, extremely low overall incidence of reported cases does not justify an unambiguous conclusion on the results of this study.
With regular use Sereventa most patients reduced the need for additional use of short-range beta-agonists.
It is recommended to verify whether the patient uses an inhaler.
The therapeutic effect of the drug may be reduced by cooling the inhaler.
When cooling spray is recommended to get it out of the plastic body and warm your hands in minutes.
The balloon should not puncture, disassemble, or burn, even if it is empty.
Overdose Serevent Diskus
Symptoms: tremor, headache, and tachycardia.
Treatment: Introduction preferably cardioselective beta-blockers, this requires caution, because these drugs can cause bronchospasm.
Serevent Diskus Drug Interactions
In an application with beta-blockers (including with cardioselective) observed antagonism.
While the application Sereventa with xanthine derivatives, corticosteroids and diuretics increases the risk of hypokalemia.
In an application with MAO inhibitors and tricyclic antidepressants increases the risk of side effects of the cardiovascular system.
Compliance with inhaled corticosteroids and cromoglicic acid.
