Serevent inhaler 120 doses GLAXOSMITHKLINE
Serevent inhaler 120 doses GLAXOSMITHKLINE
Qualitative and quantitative composition
Dosage formulation , wherein the release is 25 mcg ( micrograms ) salmeterol in the form of salmeterol xinafoate in each injection . Each canister contains 60 or 120 doses.
For excipients, see 6.1.
3 . Formulation
Suspension pressurized inhalation .
4 . Clinical data
For maintenance treatment of airway obstruction caused by asthma or chronic obstructive pulmonary disease - COPD ( chronic bronchitis and emphysema ) . Particularly suitable for the prevention of disease symptoms during the night and / or daytime symptoms caused by physical exertion or contact with allergens.
For maintenance treatment of reversible airways obstruction in asthma , including prevention of bronchoconstriction induced by exercise .
4.2 . Dosage and method of administration
Salmeterol is administered by inhalation through the mouth .
Each prescribed dose comprises at least two pulses .
Patients who have difficulties with dispensing a pressurized inhaler can be used for inhalation volumetric chamber with SEREVENT Inhaler
For full therapeutic result , regular use of salmeterol in the treatment of airway obstruction caused by asthma and COPD. The onset of bronchodilation effective ( more than 15 % improvement of FE01 ) occurs 10-20 min after drug administration in patients with asthma . The maximum effect of treatment is achieved after administration of several doses of the drug . The bronchodilator effect of salmeterol lasts 12 hours. It is particularly preferred for the treatment of nocturnal asthma symptoms in COPD , as well as to effort provoked symptoms of asthma .
Patients should be instructed need to treat the symptoms of the disease should not take extra doses of the drug and to take fast-acting inhaled B2 - agonist.
Since the application of this class of drugs in high doses may be adverse effects , the dosage and frequency of administration of SEREVENT should only be increased on medical advice .
Treatment of asthma and COPD ( chronic bronchitis and pulmonary emphysema ): Two inhalations (2 x 25 mCg salmeterol) twice daily.
In patients with asthma with more severe airways obstruction , the dose may be increased to 4 inhalations ( 4 x 25 mcg salmeterol) twice daily.
Children over 4 years of age
Two actuations (2 x 25 mcg salmeterol) twice daily.
Children under 4 years of age
Adequate clinical data and is not recommended to salmeterol in children under 4 years of age .
It is not necessary to adjust the dose in elderly patients and in patients with impaired renal function.
4.3 . Contraindications
Hypersensitivity to any component of the product.
4.4 . Special warnings and precautions for use
Treatment of asthma should normally follow a pattern and course of disease symptoms should be evaluated clinically and by lung function tests.
SEREVENT should not be used in patients with significantly worsening or acutely progressive asthma.
Sudden and progressive deterioration in asthma is potentially life threatening . Bronchodilators should not be the sole or primary treatment for patients with severe and unstable asthma. Severe asthma requires constant medical supervision and assessment as death may occur . Patients with severe asthma have constant symptoms and frequent exacerbations , with limited breathing capacity. The value of peak expiratory flow ( PEF ) is below 60 % of the expected baseline values by more than 30 % variation and does not reach the normal values after administration of a bronchodilator . These patients require higher doses of inhaled corticosteroids (e.g., more than 1 mg per day, beclomethasone dipropionate) or oral corticosteroids . Symptomatic treatment with adjunctive SEREVENT may be combined with an optimized background corticosteroid therapy. Sudden worsening of symptoms of the disease require increased corticosteroid dosage which should be done urgently under medical supervision.
Increased use of bronchodilators , especially short-acting inhaled B2 - agonists indicates deterioration of asthma control . If the patient is ascertained that the treatment with short-acting bronchodilators is less effective, or if they need more inhalations than usual, it is necessary to pay attention to the physician. In these cases, patients should be re-evaluated and the doctor eventually increase the dose of anti-inflammatory drugs (eg higher doses of inhaled corticosteroids or a course of oral corticosteroids ) . Severe exacerbations of asthma must be treated in the normal way.
Treatment with twice daily SEREVENT replaces , short ( 4 hours) of inhaled bronchodilator (eg salbutamol), when more than one admission per day or oral bronchodilators (eg salbutamol, theophylline).
SEREVENT not replace treatment with oral and inhaled corticosteroids .
Treatment with its complement treatment with corticosteroids. The patient should be warned not to stop treatment with corticosteroids and not to reduce consumption dose without a doctor even if you feel better from the application of SEREVENT. If the patient is taking anti-inflammatory therapy , early treatment with salmeterol should be discussed and its initiation.
Because the action will occur more slowly ( 10-20 min ), SEREVENT should not be used in an acute asthma attack , wherein the appropriate application of short-acting bronchodilators onset within 5 minutes ( eg salbutamol ) . Patients should be advised to have such drugs.
You need to check the way in which the patient inhales the drug. To achieve optimal drug to the lungs to be synchronized breathing and injection salmeterol.
SEREVENT should be used with caution in patients with thyrotoxicosis , coronary insufficiency , arrhythmias and uncontrolled hypertension .
4.5 . Interactions
Should avoid the use of beta- receptor blockers ( both non-selective and selective ) in patients with obstructive airway disease , unless there is an overriding need for their application .
4.6 . Pregnancy and lactation
Studies in animals have shown some effects on the fetus , typical of B2 -agonists occur at doses greatly in excess of the therapeutic . Extensive studies of other B2 agonists showed no evidence of such effects in women receiving therapeutic doses.
Experience of the use of salmeterol during pregnancy is limited.
As with any drug use in pregnant women is justified only if the expected benefit of its use outweighs the potential risk to the fetus.
Plasma levels of salmeterol after inhalation at therapeutic doses is negligible , so it is assumed that the amount excreted in breast milk is relatively low . However, because the experience in the use of salmeterol in nursing mothers is small , it should not be used by them only when the expected benefit outweighs the potential risk to the fetus.
Animal studies confirm that the amount of salmeterol, separation breast milk is negligible .
4.7 . Effects on ability to drive and use machines
No data available.
4.8 . Undesirable effects
Adverse reactions are presented by system frequency.
Common and uncommon events were generally determined from clinical trial data . Placebo responses are not taken into account. Very rare adverse events in a large part is determined by the post-marketing data .
The following adverse reactions have been observed at the standard dose OT_50_mcg twice daily. The frequency at higher doses of 100 mcg twice daily were also taken
account, where appropriate.
Disorders Immune system
Hypersensitivity reactions :
Uncommon : Rash .
Very rare: edema and angioedema
Disorders of the nervous system
Common: Tremor and headache.
Side effects such as tremor and headache observed during treatment with B2
agonists are transient and reduce with regular therapy. Tremor was observed more frequently when administered at higher doses of 50 mcg twice daily.
Disorders of the cardiovascular system part
Common: Palpitations .
Side effects such as subjective palpitations that occur during treatment with B2
agonists are transient and reduce with regular therapy.
Uncommon : tachycardia.
Tachycardia occurs more commonly when administered at higher doses of 50 mcg twice daily.
Very rare : Cardiac arrhythmias (including atrial fibrillation , supraventricular tachycardia and extrasystoles ) .
Disorders of respiratory , thoracic and mediastinal disorders
Very rare: Oropharyngeal irritation and paradoxical bronchospasm .
As in treatment with other inhaled medicines may appear paradoxical bronchospasm , which is manifested by an increase in wheezing immediately after dosing of the drug. It should be treated immediately with a fast-acting inhaled bronchodilator . Inhaler treatment with SEREVENT should be discontinued immediately and the patient to undergo a re-evaluation , and, if necessary, be an alternative treatment .
Violations by the locomotor system
Common: Muscle spasms
Very rare: Arthralgia .
4.9 . overdose
Symptoms of salmeterol overdose are tremor, headache and tachycardia. treatment
The preferred antidote for overdosage with salmetereol is a cardioselective beta blocker. Cardio -selective beta- blockers should be used with caution in patients with a history of bronchospasm.
5 . Pharmacological
Pharmacotherapeutic group : Adrenergics and other anti-asthmatics
ATC code : R03AC12
5.1. Pharmacodynamic properties
Mechanism of action
SEREVENT selective B2 -adrenoceptor agonist with a long 12 hours) operation , with a long side chain , which is associated with the outer surface of the receptor.
These pharmacological properties of salmeterol permit more effective protection against histamine - induced bronchoconstriction and provide long lasting ( at least 12 hour ) bronchodilation compared to kratkotraynodeystvashtite B2 - agonists. In vitro studies show that salmeterol is a potent long-acting inhibitor of mast cell mediators , such as histamine , leukotrienes and prostaglandin D2, released from human lung .
In humans, salmeterol inhibits the early and late phase response to inhaled allergens. Late phase persists more than 30 hours after taking a dose of spray when the bronchodilator effect has already been terminated . Single dose salmeterol attenuates bronchial hyper . These properties indicate that there is an additional non-bronchodilator SEREVENT activity, but the clinical significance is not yet clear . Its mechanism of action is different from the anti-inflammatory effect of corticosteroids , which should not be suspended or reduced , when the prescribed SEREVENT.
SEREVENT been studied in the treatment of conditions associated with COPD and the results of treatment have shown that its use improves lung function and quality of life of the patient. As p2 - agonist salmeterol acts on the reversible component of the disease. In vitro salmeterol increased the mucociliary clearance of human bronchial epithelial cells. Also reduces the toxic effect of the acid of the toxin of Pseudomonas to epithelial bronchial mucosa in patients with cystic fibrosis.
5.2 . pharmacokinetics
Salmeterol acts locally in the lung, which gives grounds to assume that plasma levels do not determine the therapeutic effect . There are few data on the pharmacokinetics of salmeterol because of the technical difficulties associated with the determination of the drug in plasma, as after inhalation of the drug plasma concentration is very low (approximately 200 pg / ml or less) .
After inhalation of salmeterol xinafoate, in the bloodstream can be found hydroxynaphtoic acid, reaching equilibrium concentrations of about 100 ng / ml. These concentrations were 1000 -fold lower than the levels observed in the toxicity studies .
These concentrations after prolonged use (more than 12 months) in patients with pulmonary obstruction disease do not cause change.
5.3 . Preclinical safety data
In reproduction studies in animals at very high doses , the fetus were observed some effects typical of B2 - agonist.
Salmeterol xinafoate did not show genotoxicity, which is confirmed by in vivo or in vitro studies with cell prokaryotic or eukaryotic systems in rats .
Long-term studies with salmeterol xinafoate indicate the occurrence of benign tumors of the smooth muscle of rats and mezovariuma uterus of mice. Literature and our pharmacological studies confirm that these effects are very specific for this type and occur in clinical use .
6 . Pharmaceutical particulars
6.1. List of excipients and their amounts
1,1,1,2-tetrafluoroethane (Norflurane, HFA 134a )
Quantity per injection / dose to 75 mg
6.2 . Incompatibilities
No data available.
6.3. Expiration date
6.4 . Special precautions for storage
Salmeterol inhaler stored at temperatures below 30 ° C.
Protect from frost and direct sunlight.
As with other inhaled medicines in dosage form of pressure , the therapeutic effect of this product may be reduced when the vial is cold .
Metal packaging must not be broken, punctured or burn even when apparently empty.
6.5. Packaging Data
Outer packing : carton .
Immediate packaging: The aluminum container sealed with a metering valve. The container is placed in a plastic device with spray nozzle, mouthpiece and protective cap. Each container contains 60 or 120 doses (sprays ) .
6.6. Recommendations for use
1. Remove the cap by gently squeezing both sides and check that the mouthpiece is clean inside and out.
2 . Shake the inhaler well.
3 . Hold the inhaler upright between fingers and thumb , thumb on the base , below the mouthpiece .
4 . Exhale as possible and then place the mouthpiece in your mouth between your teeth and close your lips around it , but do not bite .
5 . Soon as you start to breathe in through your mouth , press down on the top of the inhaler to spray the medicine as long and inhale deeply.
6 . While holding your breath, take the inhaler from your mouth and remove your fingers from the top of the inhaler . Hold your breath as you can.
7 . If you need to take a greater number of doses , hold the inhaler upright and wait half a minute , then repeat the action from point 2 to point 6 .
8 . After use, always put the cap on the mouthpiece by pressing and click. This is necessary to prevent contamination .
Do not rush the implementation of the points 4, 5 and 6. Important to start to breathe as much as possible before slowly inhaling .
Practice before a mirror the first few times . If after inhaling droplets see your inhaler or the sides of your lips , you must repeat the steps sequentially from 2.
If your doctor has given you different instructions described must carefully follow them. Ask your doctor if you have any difficulties.
Younger children may need help from their parents in the use of
inhaler . Ask the child to exhale and press the inhaler when the child begins to breathe . Practice together. Older children and people with weak hands should hold the inhaler with both hands. Put both index fingers on top of the inhaler and both thumbs on the base , below the mouthpiece .
Inhaler should be cleaned at least once a week as follows:
1. Remove the cap from the mouthpiece .
2 . • Do not remove the metal canister from the plastic part .
3 . Wipe the inside and outside of the mouthpiece with a dry cloth .
4 . Put the cap on the mouthpiece.
Insert a metal container in the water.
Before using the inhaler for the first time or if the inhaler has not used for a long time ( a week or more) , remove the plastic cap on the mouthpiece by pushing on both sides, shake the inhaler well and spray once in the air to make sure it works.