Description overdue on 09/16/2014

• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use Foradil (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Analogs
• Reviews
• Price, where to buy

Composition

The composition of one capsule part 12, 5 mg of active substance Formoterol fumarate .

As an auxiliary substance acts lactose   (25 mg).

Product form

The drug is available as Foradil capsules which contain a white free-flowing powder for inhalation. On the transparent colorless capsules size №3 present marking " CG "(On the cap) and" FXF "(In the body). Markings applied to the capsule black ink.

The capsules are packaged in blisters of 10 pieces which are placed together with aerolayzerom (inhalation device) into cardboard boxes.

Each carton box can be 3 or 6 blisters with capsules.

Pharmacological action

Formoterol fumarate   It is a selective agonist of β2-adrenergic receptors. Its pharmacological effect is that it can be used as a bronchodilator agent as patients with reversible airways obstruction, and with irreversible.

Foradil main advantages over other drugs with similar pharmacological action, is that Formoterol fumarate   It acts quickly (within 3 minutes), and its action lasts about 12 hours after the inhalation procedure. Also this drug when it is receiving therapeutic doses virtually no significant effect on the cardiovascular system of the patient.

Pharmacodynamics and pharmacokinetics

Formoterol fumarate   both hinders the process of release leukotrienes And histamine   from mast cells. During experiments on animals have been identified and sufficiently strong anti-inflammatory abilities of formoterol. It is proved that the drug inhibits and blocks the development of edema and accumulation of inflammatory cells.

As a result of experimental studies on animals in vitro was also found that the (R, R) - and (S, S) enantiomers of racemic formoterol   like himself have properties highly selective agonists of β2-receptors. Note that the (S, S) -enantiomer was significantly less potent than (R, R) -enantiomer (800-1000 times), which confirms that it has no adverse effect on the ability of (R, R ) -enantiomer with respect to tracheal smooth muscles. During the experiments, and by comparison of these two enantiomers of a racemic mixture of experts it was determined pharmacological evidence advantages of using (R, R) - and (S, S) enantiomers.

During the research, which was attended by people, it was found that Formoterol fumarate   It is very effective in preventing bronchospasm Which may be called as potent allergens, cold air and exercise and takmi substances as histamine   and methacholine . Due to the fact that Foradil has a pronounced bronchodilatory effect over 12 hours after the inhalation procedure, the taking of the drug at the indicated doses 2 times a day allows in most cases completely bronchospasm control both in the daytime and during the night.

With COPD (chronic obstructive pulmonary disease) stable flow Foradil, which is applied using the device for inhalation (aerolayzerom) of 12 or 24 mg 2 times a day, contributes to the rapid onset of bronchodilator effect, the duration of which is at least 12 hours.

Absorption

During the experiment, it was determined that for a single inhalation dose of 120 mg drug is rapidly absorbed into the plasma and the plasma Cmax was achieved within 10 minutes after the procedure and was 266 pmol / L. When using formoterol 12 or 24 mg 2 times a day for 10-12 weeks in patients COPD (chronic obstructive pulmonary disease) formoterol concentration in plasma (when measured after 15 minutes, 2 hours and 5 hours after the inhalation procedure) varied between 11.6 and 25.8 pmol / L, and 23.4 and 50.4 pmol / l.

The survey also studied the excretion of both total   formoterol And its two enantiomers urine. As a result, proportional increase was observed in the systemic circulation amount formoterol   with increasing dose.

Note that during inhalation of the drug during maintenance therapy the excretion of the active substance in the urine of patients suffering from bronchial asthma increases by 64-74%, while those diagnosed COPD   increased by 20-39%. This is an indication that formoterol cumulated in plasma after repeated treatments. But at the same time after repeated inhalation showed no more significant accumulation of enantiomers formoterol .

So how formoterol   applied using an inhaler, the norm is that part of the active substance is swallowed and absorbed from the gastrointestinal tract.

Distribution of

Foradil has a fairly strong connection to plasma proteins, which reaches 61-64%.

Metabolism

The main route metabolism   drug Foradil - a direct glucuronidation . Seconded by metabolism It is O-demethylation and subsequent glucuronidation.

Also pathway may include conjugation of the active substance and subsequent deformilirovanie sulfate. In the process of glucuronidation participate following isoenzymes: 1A7, UGT1A1, 1A10, 1A3 i1A6 and 1A8, 1A9, 2B7 and 2B15. A 0-demethylation process involved isoenzymes: 2A6 and CYP2D6, and 2C9 and 2C19.

Withdrawal

Patients taking Foradil for 12 months, and suffering asthma   in the urine of 10% of formoterol was determined in unaltered form, and in patients with a diagnosis of COPD   approximately 7%. Proportion of (R, R) - and (S, S) -enantiomers of formoterol is in the urine of about 40% (in patients with asthma ) And 60% (in patients with COPD ).

The active substance and its metabolites   excreted from the body entirely (1/3 of the total dose is excreted in the faeces and 2/3 - in the urine).

The renal clearance of the drug Foradil varies between 150 and 160 ml / min.

End T1 / 2 of the drug from the plasma after a single administration of a dose of 120 mg of 10 hours; and T1 / 2 enantiomers formoterol   were 13.8 and 12.2 respectively.

Pharmacokinetics in special clinical situations

When corrected for body weight pharmacokinetic characteristics formoterol   both men and women remain the same.

Pharmacokinetic studies formoterol   in elderly patients and people with impaired liver and / or kidney disease have been conducted.

Indications

It is recommended to use the drug Foradil:

• in the prophylaxis and treatment of bronchospasm   patients asthma   (Foradil drug used as an adjunct to therapy with inhaled corticosteroids);
• in the prevention bronchospasm , Which is caused by a strong exercise, cold air or inhalation of allergens (drug Foradil is used as an adjunct to therapy with inhaled corticosteroids);
• the prevention and treatment of symptoms caused by bronchial obstruction in patients with chronic bronchitis . emphysema , and COPD   (drug Foradil is used as a reversible and irreversible at bronchial obstruction ).

Contraindications

Do not use the drug Foradil:

• in children under 5 years old;
• during   Lactation   (breastfeeding);
• in case of hypersensitivity to the drug.

With extreme caution should be used drug Foradil:

• at coronary heart disease ;
• at   cardiac arrhythmias ;
• at severe heart failure ;
• at idiopathic subvalvular aortic stenosis ;
• at hypertrophic obstructive cardiomyopathy ;
• at thyrotoxicosis ;
• when known or suspected QT prolongation ;
• at diabetes .

Side effects

During treatment, patients may experience Foradilom enough discomfort from the following side effects:

• On the side   the immune system: of hypersensitivity reactions ( hypotension . hives . angioneurotic edema . itching . exanthema ).
• Mental disorders: from agitation . anxiety . hyperexcitability . insomnia .
• On the side   Nervous system: from headache .   tremor . dizziness . taste disturbances .
• On the side   Cardiovascular system: from palpitations . tachycardia . peripheral edema .
• On the side   respiratory system: from bronchospasm Including paradoxical.
• Local reactions from   irritation of the mucous membrane of larynx and pharynx .
• On the side   digestive system: from nausea .
• On the side   the musculoskeletal system: from cramps in the muscles . myalgia .
• Other: distortion of taste sensations.

Note that when using this drug in clinical practice were observed quite serious changes results of these laboratory studies as hyperglycemia I   and hypokalemia , and QT prolongation .

During clinical trials when used in the treatment regimens of the drug Foradil was found and a slight increase in the frequency of exacerbations asthma   compared with placebo.

Instructions for use Foradil (method and dosage)

In accordance with the instructions for use of the drug Foradil it is for inhalation use in the treatment regimens of adults and children older than 5 years. The drug is available as a powder for inhalation that is applied using aerolayzera (special device for inhalation).

Adults with asthma you need to take 12-24 mg (1-2 capsules) 2 times a day. If necessary, the dose can be increased to 12-24 mg per day. If the use of additional doses of Foradil becomes constant, not episodic (more than 2 days a week), then the patient should consult a doctor to review the regimen because frequent reception of additional doses may be indicative of worsening of the underlying disease.

When prevention bronchospasm Which occurs when strong physical exertion or imminent exposure to allergens, 15 minutes before the contact or load need to take 12 mg (1 capsule). Patients with asthma   severe stage can be used in a single dose of 24 micrograms.

Patients suffering from chronic obstructive pulmonary disease,   with regular maintenance therapy should take 12 or 24 mg (1-2 capsules), 2 times a day.

Children aged 5 years and older should take 12 mg 2 times a day during maintenance therapy. If necessary, additionally take 12 or 24 mg of the drug per day. If the use of additional doses of Foradil becomes constant, not episodic (more than 2 days a week), then the patient should consult a doctor to review the regimen, ie. A. Frequent reception of additional doses may be indicative of worsening the underlying disease.

For prevention   bronchospasm   in children, the causes of which can be severe physical exertion or exposure to a known unavoidable allergen, 10-15 minutes prior to the contact or load necessary to use 12 mcg Foradil (1 capsule).

Overdose

If overdose Foradil patient may experience discomfort from the strong nausea . vomiting . headaches, tremors, drowsiness, heart palpitations, tachycardia, ventricular arrhythmias, metabolic acidosis , and hypokalemia   and hyperglycemia .

To remove the symptoms of overdose it is recommended to supportive and symptomatic therapy. In the case of severe overdose may require hospitalization.

Under the supervision of a doctor can be used beta-blockers .

Cooperation

Since Foradil is beta2-agonists , It is necessary to take extreme caution to patients who have been using in their treatment regimens drugs such as procainamide . dizopiramid . quinidine   and phenothiazines . It is also not recommended in conjunction with Foradil antihistamines . MAO inhibitors And strong tricyclic antidepressants And other drugs which promote QT prolongation Since it may not only adversely affect the cardiovascular system, but also increase the risk of   ventricular arrhythmias .

Note also that the simultaneous reception of Foradil with other sympathomimetic agents may provoke side effects of the drug.

Reflect on the potential gipokaliemicheskoe effect of beta2-agonists may also be simultaneous with Foradilom diuretics . xanthine   and GCS .

Hypokalemia   It helps to increase the patient's susceptibility to the occurrence and development cardiac arrhythmias If their treatment regimen present preparations   foxglove .

Much can weaken the effect of Foradil beta-blockers .

Terms of sale

Foradil may be purchased at the pharmacy with a prescription.

Storage conditions

The drug Foradil should be stored in a dry place at a temperature not exceeding 25 ° C.

Shelf life

Foradil is stored for 2 years when stored.

Analogs

Today, Foradil has about 20 analogues of pharmacological action of drugs among domestic and foreign production. The main counterparts of the drug on the market are Foradil Ketotifen, Ascoril, Ribomunil   and Stoptussin .

Reviews Foradile

The average score on the forums Foradil is 4, 8 to 5-point scale.
The advantages of the drug Visitors forums include:

• efficiency;
• reception, 2 times a day.

Outs preparation participants in medical forums and websites are:

• aerolayzer uncomfortable;
• the occurrence of side effects.

After analyzing the responses about Foradile doctors, it can be concluded that many experts are actively using this drug in the practice, but are advised to pay attention to their patients and the drug Foradil Combi Which also has proven himself gives excellent results in removal asthmatic attacks .

Information about the drug Foradil in Wikipedia is not.

Price Foradil where to buy

The average price of Foradil in Ukraine is 900 UAH (30 capsules).

In Moscow, you can buy a Foradil for 661 rubles. (30 capsules) and 1123 rubles. (60 capsules).