Daxas

Daxas belongs to non-steroidal anti-inflammatory drugs that are used as maintenance therapy for chronic obstructive pulmonary disease. Given that chronic obstructive pulmonary disease (abbreviated COPD) occurs mainly after 40 years, the appointment of the drug to patients under 40 years is only after confirmation of the diagnosis.

Indications Daxas

Daxas is prescribed in severe conditions of COPD and frequent exacerbation of swelling as maintenance therapy.

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Release form

Daxas are available in the form of tablets packed in blisters in cardboard packages.

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Pharmacodynamics

Daxas belongs to the group of anti-inflammatory drugs. The principle of action is aimed at eliminating inflammation in the lungs. The drug reduces the activity of the basic enzyme PDE4, which causes inflammation and is the main link provoking the disease.

Daxas slows the activity of PDE4, which as a result leads to a normalization of the function of leukocytes, smooth muscle cells of pulmonary vessels and respiratory tracts, etc.   

In vitro studies have shown that the drug stops the release of inflammatory mediators.

In patients with COPD, the drug reduces the number of neutrophils in sputum, and studies have also shown that in healthy patients, the influx of neutrophils and eosinophils into the respiratory tract decreases.

[3], [4], [5]

Pharmacokinetics

The main active ingredient Daxas is roflumilast, which upon ingestion forms an active metabolite of Roflumilast N-oxide. The drug reduces the activity of phosphodiesterase (PDE4).

After taking the drug after about an hour reaches the highest concentration in the blood (subject to reception on an empty stomach). From the intake of food does not depend on the inhibitory activity of the drug on PDE4, but there is a delay in the highest concentration of the substance in the blood plasma.

The drug is approximately 97% bound to blood proteins, the active substance for a fairly short time will be distributed to all tissues and organs, including. Penetrates into adipose tissue.

Pre-clinical studies show that roflumilast penetrates the blood-brain barrier at very low concentrations.  

The half-life of roflumilast in plasma is approximately 16-17 hours.  

The overwhelming activity of the drug is reduced in smokers, elderly people are experiencing an increase in the inhibitory activity of roflumilast, but no adjustments are required for this group of patients, since all changes are not considered clinically relevant. 

In severe renal failure, the inhibitory activity of the drug is reduced by about 9%, but there is no need to adjust the dose.

In liver failure, the inhibitory activity of roflumilast increases depending on the Child-Pugh classification.

[6], [7], [8]

Dosing and administration

Daxas is prescribed for 500 mg (1 tablet) per day. In some cases, a maximum therapeutic effect requires long-term treatment (up to 1 year).

If there is a violation of the kidneys, as well as in the elderly, there is no need to adjust the dosage.

The tablet is washed down with a sufficient amount of water, it is necessary to try to take the drug at one time.

[11], [12]

Use Daxas during pregnancy

Daxas is contraindicated in pregnant and lactating women. Very little data on the use of the drug during pregnancy.

In addition, the drug is not prescribed to women of childbearing age who do not use reliable contraceptives.

It is possible that Daxas can penetrate into breast milk, so if necessary, take the drug should abandon breastfeeding.

Contraindications

Daxas is not prescribed with increased susceptibility to certain components of the drug, impaired liver function. In addition, the safety of using the drug before the age of 18 is not established.

There is insufficient data on the treatment with immunodeficient, infectious diseases, oncological tumors, heart failure, rare hereditary diseases, severe depression.

Daxas is used with caution for mental disorders in the past and treatment with certain inhibitors.

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Side effects Daxas

Daxas often provokes upset of the stool, abdominal pain, weight loss, nausea. As a rule, such adverse reactions occur at the beginning of treatment, then the condition is normalized.

Also, the drug can cause dyspepsia, insomnia, depression, heart palpitations.

The drug can provoke infectious diseases of the respiratory tract, headaches, tremors, rashes on the skin.

Rarely there are spasms or weakness in the muscles, a general malaise.

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Overdose

Daxas, when taking more than the recommended dose causes a disruption of the digestive tract, palpitations, headaches, sweating, etc.

When an overdose is symptomatic treatment.

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Interactions with other drugs

Daxas is used with caution in the simultaneous treatment of ketokanazol, erythromycin, enoxacin, cimetidine. In this case, combined therapy can increase the activity of the drug and provoke intolerance.

Rifampicin, carbamazepine, phenobarbital, phenytoin reduce the inhibitory activity of the drug.

Interaction with theophylline, oral contraceptives, which contain ethinyl estradiol and gestodene, leads to an increase in inhibitory activity.

Inhalation products (salbutamol, formoterol, etc.), as well as preparations for oral administration (warfarin, montelukast, midazolam, digoxin), antacid agents do not affect the therapeutic effect of Daxas.

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Storage conditions

Daxas should be stored at a temperature of no higher than 30 ⁰ C. The drug should be stored in a place protected from moisture, sunlight and inaccessible to children.

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Special instructions

Daxas is not intended for the treatment of acute bronchospasm. In this case, the patient should use a special drug that will help to remove the attack. When treating Daxas, there is often a decrease in body weight, but after stopping the drug, weight, as a rule, returns to normal.

[16], [17]

Shelf life

Daxas is good for three years from the date of production. If the storage conditions are violated or the packaging integrity is violated, it is not recommended to use the drug.

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