Daxas tabs 0.5mg #30

Daxas tabs instruction

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Composition

In 1 tablet of roflumilast 0,5 mg. Lactose monohydrate, corn starch, povidone, magnesium stearate, as auxiliary substances.

Form of issue

Tablets in a film coat 0.5 mg.

pharmachologic effect

Anti-inflammatory.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Non-steroidal anti-inflammatory agent - inhibitor of phosphodiesterase-4. Eliminates inflammation in chronic obstructive pulmonary disease. The mechanism of action is due to the inhibition of phosphodiesterase-4, an enzyme involved in inflammatory processes in COPD. The action of the drug is directed to PDE4A, 4B and 4D.
The selectivity of action is also applicable to the main active metabolite of roflumilast N-oxide. Inhibition of this enzyme results in an increase in intracellular cAMP. Maintaining a high level of cAMP in neutrophils and macrophages provides anti-inflammatory action, reduces the dysfunction of smooth muscle cells, endothelial cells and pulmonary vessels. There is also a decrease in edema of the bronchial mucosa. Roflumilast inhibits the release of leukotriene B4, tumor necrosis factor and reactive oxygen species.

Pharmacokinetics

Bioavailability is 80% and after 1 hour the maximum concentration of the active substance is determined in the blood, and the N-oxide metabolite is determined after 8 hours. Eating for one hour delays the timing of achieving C max. Binding to proteins is about 99%. Rflumilast is well distributed into tissues. An insignificant amount penetrates through the BBB. In adipose tissue and organs does not cumulate. Metabolized in two stages to form the N-oxide metabolite (under the action of cytochromes CYP1A2 and 4A4), more active and important with respect to the inhibition of PDE 4.
When administered orally, the half-life of roflumilast is 17 hours, and the N-oxide is 30 hours. Stable concentration is achieved in 4-6 days. About 20% is excreted with feces and 70% with urine.
In elderly people and women, the inhibitory activity of the drug increases and decreases somewhat in smokers. However, these changes have no clinical significance. In severe renal failure, inhibitory activity is reduced by 9% and dose adjustment is not required.

Indications for use

As part of complex therapy used in adults for maintenance therapy of COPD severe course with frequent exacerbations.

Contraindications

    hypersensitivity;
    severe hepatic impairment;
    severe heart failure;
    age to 18 years;
    pregnancy and lactation;
    depression and suicidal moods;
    tuberculosis, HIV infection;
    oncological diseases;
    deficiency of lactase.
With caution is prescribed in the presence of mental disorders in history, liver failure, simultaneous treatment with fluvoxamine, cimetidine and enoxacin.

Side effects

Befor you buy Daxas online, you should know side effects.
Adverse reactions are mild and occur more often in the first weeks of treatment.
Common side effects:
    decreased appetite;
    insomnia;
    weight loss;
    headache.
Rarely encountered adverse reactions:
    hypersensitivity;
    diarrhea, abdominal pain, nausea;
    gynecomastia;
    anxiety;
    nervousness, depression;
    tremor, dizziness;
    tachycardia;
    respiratory tract infections;
    gastritis, GERD, dyspepsia;
    increased levels of aspartate aminotransferase and creatine phosphokinase;
    rash;
    hives;
    muscular spasms, myalgia and muscle weakness;
    malaise, fatigue.

Daxas, instructions for use (Method and dosage)

Tablets are taken orally 0.5 mg per day, at the same time, with water. Their intake does not depend on the time of ingestion.
For the best effect, long-term treatment is required - from several weeks to one year. In individuals over 65 years, dose adjustment is not performed. With concomitant diseases of the kidneys, correction is also not carried out.
The drug is not intended for the treatment of bronchospasm. Do not start treatment in patients who are constantly receiving glucocorticosteroid treatment inside. It is not recommended simultaneous therapy with theophylline.

Overdose

Overdose manifests itself as headache, dizziness, diarrhea, abdominal pain, tachycardia, severe sweating and lowering of blood pressure.
Symptomatic therapy is performed. Hemodialysis is not effective, since roflumilast is largely associated with blood proteins.

Interaction

Combined use with cytochrome inhibitors CYP31A2 and CYP3A4 (erythromycin, fluvoxamine, enoxacin, ketoconazole and cimetidine) can enhance the effect of this drug and induce intolerance. Inductors cytochrome P450 (phenobarbital, phenytoin, rifampicin, carbamazepine) reduce the therapeutic effect of roflumilast.
Simultaneous reception of theophylline and contraceptives leads to increased action. There are no interactions with budesonide, salbutamol, formoterol, digoxin, montelukast, warfarin, midazolam. Admission with antacids does not change the pharmacokinetic properties of the drug.

Storage conditions

Temperature up to 30 ° С.
Shelf life - 3 years.

Reviews about Daxas

The drug has appeared relatively recently in the pharmacy chain since 2011. This is a representative of a new class that effectively controls the inflammatory process in COPD, one of the goals of therapy is to reduce exacerbations. Supplement to the basic therapy of this drug has allowed not only to significantly reduce the number of exacerbations, but also to achieve improvement in lung function. These positive effects were achieved already at 4-8 weeks of treatment.
The main advantages of the drug are: suppression of specific inflammation, strengthening the effect of bronchodilators and the availability of a good safety profile.
All these moments are reflected in the patients' reviews, which note that severe exacerbations were noted much less frequently, if they were, they were distinguished by a lighter course. All patients took the drug in addition to bronchodilation therapy - he did not replace the treatment with inhalants, but helped significantly. Has a delayed effect, but generally improves the quality of life.
    "... It does not help right away, you have to take it for a long time. Has noticed improvement in the first winter which has passed or took place without exacerbations of a bronchitis ».
    "... The first 3 weeks was a disorder of the stool after taking Daxas, the doctor prescribed antidiarrhoeals."
    "... I've been taking a whole year. I can say that it does not give a quick improvement, but personally I have reduced the frequency of exacerbations - it used to be 3-4 years in a year, and now - once and that because I got sick with flu, getting infected from my husband. "
    "... For me, the side effect (weight loss) was favorable, because I have excess weight and it was so hard to walk and breathe."