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Daxas has phosphodiesterase inhibiting type 4, anti-inflammatory effect.
Maintenance therapy in the treatment of severe COPD (post-bronchodilation forced expiratory volume in the first second (FEV1) should be less than 50% of the calculated proper indicator) in adult patients with frequent exacerbations in history.
1 tab. contains roflumilast 500 mcg.
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Dosage and administration
Daxas drug is prescribed in tablets of 0.5 mg 1 time per day. Tablets must be washed down with water and taken daily at the same time, regardless of the meal. Treatment may take several weeks to achieve a therapeutic effect. There is evidence of clinical studies on the duration of the drug Daxas up to one year. Dose adjustment depending on the patient's age (over 65 years) is not required. Clinical data on the use of the drug Daxas in patients with impaired liver function class A according to the Child-Pugh classification are insufficient to recommend dose adjustment, so the drug should be used with caution in the treatment of such patients. Patients with kidney disease dose adjustment is not required.
The most frequent complaints are diarrhea (5.9%), weight loss (3.4%), nausea (2.9%), abdominal pain (1.9%) and headache (1.7%). Most of these adverse reactions are mild or moderate. Such adverse reactions mainly occur during the first weeks of treatment and in most cases disappear as the treatment continues.
Side effects are classified depending on the frequency of occurrence: the most frequent - ≥1 / 10; frequent - ≥1 / 100 and
Immune system disorders: infrequent - hypersensitivity.
Endocrine Disorders: rare - gynecomastia.
Metabolic and nutritional disorders: frequent - weight loss, loss of appetite.
Mental disorders: frequent - insomnia; infrequent - anxiety; rare - nervousness, depression. When conducting clinical trials, reports of rare cases of suicidal thinking and behavior (including completed suicide) were received. Patients should be instructed to inform their physician about all manifestations of suicidal thinking.
Nervous system disorders: frequent - headache; infrequent - tremor, vertigo, dizziness; rare - dysgeusia.
Violations by the CCC: infrequent - tachycardia.
Disorders of the respiratory system, organs of the chest and mediastinum: rare - infections of the respiratory tract (except pneumonia).
Violations of the gastrointestinal tract: frequent - diarrhea, nausea, abdominal pain; infrequent - gastritis, vomiting, gastroesophageal reflux disease, dyspepsia; rare - hematochezia, constipation.
Disorders of the liver and biliary tract: rare - increased GGT activity, increased AST activity.
Violations of the skin and subcutaneous tissues: infrequent - rash; rare - urticaria.
Musculoskeletal and connective tissue disorders: infrequent - muscle spasms and muscle weakness, myalgia, back pain; rare - an increase in blood creatine phosphokinase.
General complications and reactions at the injection site: infrequent - malaise, asthenia, fatigue.
Carefully: history of mental disorders; treatment with cytochrome CYP1A2 isoenzyme inhibitor fluvoxamine or two CYP3A4 / 1A2 inhibitors enoxacin and cimetidine. A mild form of liver failure (Child-Pugh class A).
The main step in roflumilast metabolism is the N-oxidation of roflumilast to roflumilast N-oxide using cytochrome CYP3A4 and CYP1A2. Both roflumilast and roflumilast N-oxide have an internal inhibitory activity of PDE4. Therefore, after taking roflumilast, the total inhibitory activity of PDE4 is the cumulative effect of both roflumilast and roflumilast N-oxide. Clinical studies of interactions with cytochrome CYP3A4 inhibitors erythromycin and ketoconazole showed an increase in total inhibitory activity of PDE4 by 9%. Studies of the interaction with the cytochrome CYP1A2 inhibitor fluvoxamine, and CYP3A4 and CYP31A2 inhibitors enoxacin and cimetidine, showed an increase in the total inhibitory activity of PDE4 by 59%, 25% and 47%, respectively. The combined use of the drug Daxas with these active substances can lead to increased action and the development of intolerance. In this case, it is necessary to reconsider the issue of treatment with Daxas.Acceptance of the cytochrome P450 inducer rifampicin resulted in a decrease in the total inhibitory activity of PDE4 by about 60%. Therefore, the use of powerful inducers of cytochrome P450 (for example, phenobarbital, carbamazepine, phenytoin) can reduce the therapeutic effect of roflumilast. Simultaneous administration with theophylline led to an 8% increase in the total inhibitory activity of PDE4. When studying the interaction with oral contraceptives containing gestodene and ethinyl estradiol, the total inhibitory activity of PDE4 increased by 17%. There was no interaction with inhaled (salbutamol, formoterol, budesonide) and intravenous (montelukast, digoxin, warfarin, sildenafil and midazolam) preparations. Simultaneous administration with antacid preparations (a combination of aluminum hydroxide and magnesium hydroxide) did not change the absorption rates or pharmacokinetic properties of roflumilast or roflumilast N-oxide.
Pregnancy and Lactation
Pregnancy.Data on the use of roflumilast in pregnant women is limited. According to preclinical studies, roflumilast penetrates the placental barrier. Animal studies have shown reproductive toxicity of the drug. The drug Daxas is not recommended for pregnant women and women of reproductive age who do not use contraceptives.
Lactation.Available pharmacokinetic data obtained in animals showed the release of roflumilast or its metabolites into milk. You can not exclude the risk of receiving the drug a child. Daxas is not recommended for use during lactation.
Daxas is a non-steroidal anti-inflammatory agent intended for the maintenance treatment of patients with severe COPD with frequent exacerbations. Due to the fact that in the general population of COPD, patients over the age of 40 years predominate significantly, when prescribing the drug to patients under 40 years of age, a spirometric confirmation of the diagnosis of COPD is required. According to the indications for use of the drug, it is necessary that the value of post-bronchodilation FEV1 should be less than 50% of the calculated proper indicator. Daxas is not intended for the treatment of an acute attack of shortness of breath (acute bronchospasm). To relieve an acute attack, it is important to have a medicine prescribed by a doctor that you will always have on hand to cope with the attack. Daxas drug in this situation will not help.
In the course of studies conducted during the year, there was more often a decrease in body weight in patients who took the drug Daxas, compared with patients who took a placebo. After discontinuation of the drug Daxas, most patients regained their body weight within 3 months. In patients with underweight should be monitored weight at each visit to the doctor. Patients should be advised to regularly monitor their body weight. In the case of an unexplained or clinically significant weight loss, you should stop taking Daxas and monitor the dynamics.
Specific clinical conditions
Due to the lack of sufficient experience, one should not start treatment with Daxas in individuals who receive continuous maintenance therapy with oral GCS, with the exception of short-term courses of systemic GCS. Experience with the use of Daxas in patients with latent infections such as tuberculosis, viral hepatitis, herpes virus and shingles is limited.
The use of Daxas is associated with an increased risk of mental disorders such as insomnia, anxiety, nervousness, and depression. In clinical trials, rare cases of suicidal thinking and behavior have been identified.Therefore, if patients report previously manifested symptoms from the psyche, or they present symptoms at the present time, or if concomitant therapy with other drugs is planned, related to the likelihood of mental disorders, a careful assessment of the risks and benefits associated with starting or continuation of treatment with Daxas. Patients should be instructed to notify the physician prescribing the treatment of any changes in the behavior, mood or occurrence of suicidal thoughts of any nature.
Despite the fact that adverse reactions such as diarrhea, nausea, abdominal pain and headache occur mainly in the first weeks of treatment and in most cases go away with continued treatment, if these symptoms persist, the issue of treatment with Daxas should be reconsidered. Intolerance can occur in the case of special populations, in particular, black non-smoking women or patients who are treated with a fluoresimal CYP1A2 inhibitor or two CYP3A4 / 1A2 inhibitors enoxacin and cimetidine.
There is no clinical data regarding concomitant treatment with theophylline as maintenance therapy. Therefore, concomitant therapy with theophylline is not recommended.
Influence on ability to drive vehicles and mechanisms
Due to the possibility of the development of adverse reactions, care should be taken when driving and occupying other potentially hazardous activities that require increased concentration and psychomotor speed.
During the first phase of clinical studies after taking a single oral dose of 2.5 mg and a single dose of 5 mg (10 times more than the recommended dose), the following symptoms were more often observed: headache, gastrointestinal dysfunction, tachycardia, dizziness, clouding of consciousness, sweating and hypotension. In case of overdose, it is recommended to carry out appropriate symptomatic therapy. Since Iroflumilast is largely bound to plasma proteins, hemodialysis is not an effective method for its elimination. There is no evidence of whether roflumilast is amenable to peritoneal dialysis.
- Brand name: Daxas
- Active ingredient: Roflumilast
- Dosage form: pills, film coated.
- Manufacturer: Takeda GmbH
- Country of Origin: Japan
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