Серевент

General characteristics. Structure:

Aerosol for inhalations dosed in the form of suspension of white or almost white color.

Active ingredient: salmeterola ксинафоат 36.3 mkg, including салметерол 25 mkg

Excipients: lecithin, trichlorofluoromethane, dichlorodifluoro methane.

Pharmacological properties:

The selection agonist β2-адренорецепторов long action (12 h).

The molecule of a salmeterol has a long side chain which contacts the external site of a receptor. Thanks to it салметерол the histamine - the induced bronchospasm is more effective for the prevention and causes longer (not less than 12 h) a bronkhodilatation in comparison with agonists β2-адренорецепторов short action.

Salmeterol inhibits release in fabrics of mediators of mast cells, such as a histamine, leukotrienes and D2 prostaglandin. Suppresses an early and late stage of allergic reaction; after introduction of one dose suppression of a late stage lasts to 30 h when the bronchodilatory effect is already absent. Single introduction of a salmeterol reduces hyperreactivity of bronchial tubes.

Salmeterol also increases the frequency of the movement of cilia of a ciliary epithelium, improves mukotsiliarny clearance, reduces the damage of an epithelium of respiratory tract caused by Haemophilus influenzae and Pseudomonas aeruginosa and also has anti-neutrophylic activity and ability to reduce hypostasis of a mucous membrane due to decrease in an exit of protein through a vascular wall.

Patients with bronchial asthma have a beginning of effect of drug (increase in volume of the forced exhalation for 1 sec./OFV1/> 15%) it is noted in 10-20 min. after inhalation. The full therapeutic effect develops after introduction of the first several doses of drug. Action of a salmeterol continues during 12 h. It is especially convenient for treatment of patients with night attacks of a bronchospasm and for the prevention of the attacks caused by an exercise stress.

 

Pharmacokinetics. Absorption

At Serevent's use in a dose of 50 mkg of 2 Cmax of a salmeterol makes 200 pg/ml, further concentration of active agent in plasma quickly decreases.

Removal

Salmeterol is brought with bile through intestines, mainly in the form of a hydroxylated metabolite.

Indications to use:

Adults

— bronchial asthma, including prevention of the bronchospasm caused by an exercise stress;

— the chronic obstructive pulmonary disease (COPD), including chronic obstructive bronchitis and emphysema of lungs.

Children are aged more senior than 4 years

— bronchial asthma, including prevention of the bronchospasm caused by an exercise stress.

Route of administration and doses:

Серевент it is intended for use only in the form of inhalations. Drug can be used through a spacer. For achievement of optimum therapeutic effect drug should be used regularly. Duration of a course of treatment is determined by the doctor.

The adult at treatment of bronchial asthma and HOBL the recommended drug dose - on 2 inhalations (2 x 25 mkg of a salmeterol) 2

The maximum dose (at more expressed obstruction of respiratory tracts at patients with bronchial asthma) - on 4 inhalations (4 x 25 mkg of a salmeterol) 2

To children 4 years the recommended dose - on 1-2 inhalations (25-50 mkg of a salmeterol) 2 are more senior

The maximum daily dose for children and teenagers aged from 4 up to 18 years - no more than 100 mkg of a salmeterol (no more than on 2 inhalations 2).

With renal failures and the patient of advanced age change of a dose of drug is not required to patients.

Features of use:

Серевент it is not necessary to appoint at the expressed deterioration in a current or an exacerbation of bronchial asthma (increase of symptoms of bronchial obstruction, decrease in efficiency and increase in need for high-speed inhalation bronchodilators, deterioration in indicators of a pikfluometriya and spirometry).

At an exacerbation of bronchial asthma, and also at patients with a hypoxia it is necessary to control potassium concentration in a blood plasma.

Patients should be warned that they should not stop reception of GKS or reduce their dose without recommendation of the doctor even if the state improved against the background of Serevent's use. Серевент does not replace GKS for intake or inhalations, and it is appointed in addition to them. Besides, it must be kept in mind that for stopping of symptoms of bronchial asthma it is not necessary to inhalate additional doses of Serevent, and it is recommended to use agonists β2-адренорецепторов short action.

As at use of agonists β2-адренорецепторов in high doses emergence of side reactions is possible, in case of need increases in a dose or frequency of introduction of Serevent control of the doctor is required.

The data obtained during placebo - the controlled research conducted to the USA in which safety of a salmeterol and the placebo appointed in addition to usual therapy of asthma within 28 weeks was compared showed small, but statistically significant increase in quantity of death connected with asthma among the patients receiving салметерол (13 cases on 13 174 patients - 0.099%) in comparison with the patients receiving placebo (4 of 13 179 - 0.03%). 8 of 13 patients of the first and 1 of 4 patients of the second group were the Afro-Americans that allowed to assume higher risk of death connected with asthma among representatives of this race. Remains not clear whether this fact is connected with the carried-out therapy, genetic predisposition or features of a social behavior of the Afro-Americans (late negotiability to the doctor and lack of strict following to recommendations of the doctor). Besides, extremely low general frequency of the registered cases does not give the grounds to draw an unambiguous conclusion by results of this research.

At regular use of Serevent for most of patients the need for additional use of short-range beta-adrenergic agonists decreases.

It is recommended to check whether correctly the patient uses an inhaler.

The therapeutic effect of drug can decrease when cooling an inhaler.

When cooling a barrel it is recommended to get it from the plastic case and to warm hands within several minutes.

The barrel should not be punctured, sorted or burned even if it is empty.

Side effects:

From cardiovascular system: the headache, heartbeat are possible; predisposed patients have disturbances of a cordial rhythm (a ciliary arrhythmia, supraventricular tachycardia and premature ventricular contraction).

From the alimentary system: change of flavoring feelings, abdominal pains, nausea, vomiting, irritation of mucous membranes of an oral cavity or throat.

Allergic reactions: small tortoiseshell, Quincke's disease, bronchospasm.

Others: tremor, myotonia, arthralgia, hypopotassemia, nervousness.

Серевент can cause a paradoxical bronchospasm which needs to be stopped immediately by means of high-speed inhalation bronchodilator (in such cases it is necessary to stop at once Serevent's use, to estimate the patient's condition, to conduct examination and if necessary to appoint alternative therapy).

Interaction with other medicines:

At simultaneous use with beta adrenoblockers (including with cardioselective) antagonism is observed.

At simultaneous use of Serevent with derivatives of xanthine, GKS and diuretics the risk of development of a hypopotassemia increases.

At simultaneous use with MAO inhibitors and tricyclic antidepressants the risk of development of side effects from cardiovascular system increases.

Let's combine with inhalation GKS and kromoglitsiyevy acid.

Contraindications:

— children's age up to 4 years;

— hypersensitivity to a salmeterol and other components of drug.

With care it is necessary to appoint drug at a thyrotoxicosis, arrhythmias, an ischemic heart disease (stenocardia of the III-IV functional class), an acute myocardial infarction, uncontrollable arterial hypertension, a hypoxia of various genesis, a pheochromocytoma, pregnancy, in the lactation period.

 

Use of drug CEPEBEHT at pregnancy and feeding by a breast

Use of drug at pregnancy and in the period of a lactation (breastfeeding) is not recommended except for cases when the expected advantage for mother exceeds potential risk for a fruit or the baby.

 

Use at renal failures

Change of a dose of drug is not required to patients with renal failures.

Overdose:

Symptoms: tremor, headache and tachycardia.

Treatment: administration of cardioselective beta adrenoblockers is preferable, at the same time care since these drugs can cause a bronchospasm is required.

Storage conditions:

List B. Drug should be stored at a temperature not above 30 °C in the place, unavailable to children. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

• an aerosol for ингал. doser. 25 mkg / 1 dose: inhalers of 60 doses or 120 doses.