Daxas
Instructions for use:
- 1. Release form and composition
- 2. Indications for use
- 3. Contraindications
- 4. Method of application and dosage
- 5. Side effects
- 6. Special instructions
- 7. Drug interactions
- 8. Analogs
- 9. Terms and conditions of storage
- 10. Terms of dispensing from pharmacies
Daksas - PDE4 inhibitor; anti-inflammatory drug.
Release form and composition
Dosage form - film-coated tablets: D-shaped, yellow, engraved with "D" on one side; on the break, a white core is visible (10 pcs. in blisters, in a cardboard box of 1, 3 or 9 blisters).
Active ingredient: roflumilast, 1 tablet - 0.5 mg.
Additional components:
- excipients: corn starch, magnesium stearate, lactose monohydrate, povidone K90;
- shell: titanium dioxide (E171), macrogol 4000, hypromellose 2910, dye iron oxide yellow (E172).
Indications for use
Daxas is used for the maintenance therapy of severe chronic obstructive pulmonary disease (COPD) (in the case of a post-bronchodilatory FEV1 value of less than 50% of the calculated proper indicator) in adult patients with frequent exacerbations in history.
Contraindications
Absolute contraindications:
- moderate and severe hepatic impairment (classes B and C according to the Child-Pugh classification);
- pregnancy;
- lactation;
- age up to 18 years;
- hypersensitivity to drug components.
Contraindications due to lack of data on safety and efficacy of use due to insufficient experience of use:
- cancers (with the exception of the slowly growing type of skin cancer and basal cell carcinoma);
- rare hereditary diseases such as glucose-galactose malabsorption, galactose intolerance and lactase deficiency;
- serious acute infectious diseases (for example, tuberculosis and acute hepatitis);
- serious immunodeficiency diseases (such as progressive multifocal leukoencephalopathy, multiple sclerosis, systemic lupus erythematosus, HIV infection);
- depression associated with the appearance of suicidal thoughts and behavior;
- chronic heart failure of 3 and 4 functional classes according to the NYHA classification;
- the simultaneous use of immunosuppressive drugs (such as infliximab, methotrexate, etanercept, azathioprine);
- use of oral glucocorticosteroids as maintenance therapy (with the exception of short-term courses of systemic corticosteroids).
Relative contraindications (conditions / diseases in which Daxas should be used with extreme caution due to the risk of complications):
- history of mental disorders;
- mild hepatic impairment (class A according to the Child-Pugh classification);
- the simultaneous use of an inhibitor of the CYP1A2 isoenzyme fluvoxamine or two CYP3A4 / 1A2 inhibitors cimetidine and enoxacin.
It is not recommended to prescribe Daxas to women of childbearing age who do not use reliable methods of contraception.
Method of administration and dosage
Daksas should be taken orally 1 time per day, at about the same time, swallowing the tablets whole and drinking water, regardless of meals.
Single dose for adults - 1 tablet.
The duration of treatment is determined individually. For some patients, several weeks of continuous use of the drug are enough to achieve a therapeutic effect, others - up to a year.
The elderly and patients with kidney disease do not need to adjust the dose.
Side effects
The most common side effects are: diarrhea (5.9%), weight loss (3.4%), nausea (2.9%), abdominal pain (1.9%), headache (1.7%) - these reactions usually occur in the first weeks of treatment, are often mild or moderate in nature and, as a rule, go away on their own as therapy continues.
Possible side effects:
- from the nervous system and psyche: often (from ≥ 1/100 to <1/10) - headache, insomnia; infrequently (from ≥ 1/1000 to <1/100) - vertigo, tremor, anxiety; rarely (from ≥ 1/10 000 to <1/1000) - nervousness, dysgeusia, depression; very rarely (<1/10 000) - suicidal thinking and behavior (including suicide);
- from the digestive system: often - diarrhea, abdominal pain, nausea; infrequently - dyspepsia, vomiting, gastritis, gastroesophageal reflux disease; rarely - constipation, hematochezia, increased activity of gamma-glutamyltransferase, aspartate aminotransferase;
- from the respiratory system: rarely - respiratory tract infections (with the exception of pneumonia);
- on the part of the cardiovascular system: infrequently - tachycardia;
- on the part of metabolism and nutrition: often - decreased appetite, weight loss;
- from the endocrine system: rarely - gynecomastia;
- from the musculoskeletal system: infrequently - back pain, muscle spasms, myalgia, muscle weakness; rarely - an increase in creatine phosphokinase in the blood;
- dermatological and allergic reactions: infrequently - rash, hypersensitivity reactions; rarely - urticaria, Quincke's edema;
- others: infrequently - asthenia, malaise, fatigue.
special instructions
In the general population of COPD, patients over 40 years of age predominate. In this regard, when Daksas is prescribed to patients under the age of 40, spirometric confirmation of the diagnosis of COPD is necessary. In this case, the indicator of post-bronchodilatory FEV1 should be less than 50% of the calculated proper indicator.
Roflumilast is not intended or effective for the treatment of acute bronchospasm (dyspnea attack). The physician should warn patients: to relieve seizures, they should always have the prescribed appropriate drug with them.
In underweight patients, weight should be monitored at each visit to the doctor. Also, the patients themselves should be advised to constantly monitor their body weight. In the case of clinically significant or unexplained weight loss, Daxas should be canceled and the dynamics should be monitored.
Experience with patients with latent infections (eg, viral hepatitis, tuberculosis, viral herpes, shingles) is limited.
The use of roflumilast is associated with an increased risk of the onset of disorders such as nervousness, anxiety, insomnia, and depression. There are isolated cases of suicidal thoughts and behavior. For this reason, with extreme caution, after a thorough assessment of the benefits / risks, the drug is prescribed to patients with symptoms from the psyche (including a history) and people who are simultaneously prescribed or planned to prescribe other drugs with a possible effect on the psyche and nervous system. Patients should be warned about the need to see a doctor if they have changes in behavior or mood, if they have suicidal thoughts.
Due to the lack of clinical data on the safety of the simultaneous use of theophylline as maintenance therapy, concomitant administration of theophylline is not recommended.
Side effects such as nausea, diarrhea, abdominal pain and headache mostly occur in the first weeks of treatment and usually resolve on their own as treatment continues. If these symptoms persist, it is necessary to consult a doctor to decide whether to continue using Daxas.
Roflumilast intolerance is possible in certain patient populations, in particular in nonsmoking black women and patients receiving the CYP1A2 isoenzyme inhibitor fluvoxamine or two CYP3A4 / 1A2 inhibitors cimetidine and enoxacin.
Due to the risk of side effects from the nervous system and psyche during the period of treatment with Daksas, care should be taken when driving and performing work that requires high attention and speed of reactions.
Drug interactions
- inhibitors of the CYP3A4 isoenzyme ketoconazole and erythromycin, an inhibitor of the CYP1A2 isoenzyme fluvoxamine and inhibitors of CYP3A4 and CYP31A2 enoxacin and cimetidine: the total inhibitory activity of PDE4 increases by 9, 59, 25 and 47%, respectively, as a result of which an increase in the effect of roflumi intolerance is possible;
- phenytoin, carbamazepine, phenobarbital, rifampicin: the total inhibitory activity decreases by about 60%, as a result of which the therapeutic effect of roflumilast may decrease;
- theophylline and oral contraceptives containing gestodene and ethinyl estradiol: the total inhibitory activity of PDE4 increases by 8 and 17%, respectively.
Interaction reactions do not occur when roflumilast is combined with inhalation agents (budesonide, formoterol and salbutamol), as well as with oral drugs (midazolam, warfarin, digoxin, montelukast, sildenafil).
With the simultaneous use of antacid preparations (containing a combination of aluminum hydroxide and magnesium hydroxide), the absorption and pharmacological properties of roflumilast and its active metabolite do not change.
Analogs
Daksas analogs are: Insanovin, Epistat, Erespal, Erispirus.
Terms and conditions of storage
Store at a temperature not exceeding 30 ° C, out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
