Daxas

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

Indications Daxas

Daxas is prescribed for severe COPD conditions and frequent exacerbations of the disease as maintenance therapy.

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Release form

Daxas is available in the form of tablets, packed in blisters in cardboard boxes.

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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 main enzyme PDE4, which causes inflammation and is the main link that provokes the disease.

Daxas slows down the activity of PDE4, which ultimately leads to the normalization of the function of leukocytes, smooth muscle cells of the pulmonary vessels and respiratory tract, etc.

Test tube 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 is reduced.

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Pharmacokinetics

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

After taking the drug, the highest concentration in the blood is reached in about an hour (provided that it is taken on an empty stomach). The suppressive activity of the drug on PDE4 does not depend on food intake, but there is a delay in the highest concentration of the substance in the blood plasma.

The drug binds to blood proteins by approximately 97%, the active substance is distributed throughout all tissues and organs in a fairly short time, including penetrating into adipose tissue.

Preclinical studies show that roflumilast penetrates the blood-brain barrier in very low concentrations.

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

The suppressive activity of the drug is reduced in smokers; in elderly people, an increase in the suppressive activity of roflumilast is observed, but dose adjustments in this group of patients are not required, since all changes are not considered clinically significant.

In severe renal failure, the inhibitory activity of the drug is reduced by approximately 9%, but there is no need for dose adjustment.

In hepatic impairment, the inhibitory activity of roflumilast increases depending on the Child-Pugh classification.

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Dosing and administration

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

In case of impaired renal function, as well as in old age, there is no need to adjust the dosage.

The tablet should be washed down with a sufficient amount of water; it is necessary to try to take the drug at the same time.

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Use Daxas during pregnancy

Daxas is contraindicated in pregnant and lactating women. There is 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 contraception.

It is possible that Daxas may pass into breast milk, so if you need to take the drug, you should stop breastfeeding.

Contraindications

Daxas is not prescribed for hypersensitivity to some components of the drug, liver dysfunction. In addition, the safety of using the drug in people under 18 years of age has not been established.

There is insufficient data on the treatment of immunodeficiency, infectious diseases, cancer, heart failure, rare hereditary diseases, and severe depression with the drug.

Daxas should be used with caution in patients with a history of mental disorders and treatment with certain inhibitors.

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Side effects Daxas

Daxas often causes bowel disorder, abdominal pain, weight loss, nausea. As a rule, such side effects occur at the beginning of treatment, then the condition normalizes.

The drug can also cause digestive problems, insomnia, depression, and increased heart rate.

The drug can cause respiratory infections, headaches, tremors, and skin rashes.

Rarely, muscle spasms or weakness, general malaise occur.

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Overdose

When taken in larger doses than recommended, Daxas causes gastrointestinal disturbances, increased heart rate, headaches, sweating, etc.

In case of overdose, symptomatic treatment is carried out.

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Interactions with other drugs

Daxas should be used with caution in combination with ketoconazole, erythromycin, enoxacin, cimetidine. In this case, combination therapy may 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 containing ethinyl estradiol and gestodene, leads to an increase in suppressive activity.

Inhalation agents (salbutamol, formoterol, etc.), as well as oral medications (warfarin, montelukast, midazolam, digoxin), antacids do not affect the therapeutic effect of Daxas.

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Storage conditions

Daxas should be stored at a temperature not exceeding 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 relieve the attack. When treating Daxas, weight loss is often observed, but after stopping the drug, the weight usually returns to normal.

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Shelf life

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

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