Copdumilast Armephaco medicine for maintaining chronic obstructive pulmonary disease (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Roflumilast
Ingredient 120 Armephaco

Ingredient

Composition information	Content
Roflumilast	0.5mg

Uses

indications

COPDUMilast is indicated for treatment of severe chronic obstructive pulmonary disease (COPD) (FEV1

Pharmacology

Classification: Medicines for respiratory obstruction

ATC code: R03DX07

Roflumilast and its metabolites-Roflumilast N-OXI selective inhibitors Phosphodiesterase 4 (PDE4). As a result, the drug increases the accumulation of am intracellular amps.

Currently, the exact mechanism of the drug is unknown, but it is thought to be related to increasing the in intracellular AMP concentration in lung cells.

In patients with COPD, treated for 4 weeks with Roflumilast 0.5mg once a day, reducing neutropen leukocytes and nerves in phlegm 31% and 42%. In the study of pharmacological resources in healthy people, Roflumilast 0.5mg once a day reduces the total number of cells, neutrophils and narcissism in bronchial washing fluids, equivalent to 35%, 38%and 73%.

Pharmacokinetics

absorption

Absolute bioavailability after taking a 0.5mg dose of Roflumilast about 80%. The maximum drug concentration is about 1 hour after taken (ranging from 0.5 to 2 hours) in a state of hunger, while the concentration of metabolites n - oxid is achieved after nearly 8 hours (from 4 to 13 hours).

Food does not affect the total amount of drugs absorbed into the blood but slowed the time to reach the peak concentration (TMAX) about 1 hour and decreased the peak concentration (CMAX) by about 40%; However, CMAX and TMAX of metabolites are not affected. In In vitro study shows that both Roflumilast and N-OXID metabolites do not inhibit P-GP transportation.

Distribution

Original drugs and n-oxid metabolites associated with plasma proteins are 99% and 97%. The distribution volume with a single dose of 0.5mg Roflumilast is about 2.9L/kg. Research on mice with markers shows that the drug through the bloody barrier at a low rate.

Roflumilast conversion of main metabolism in phase I (cytochrome p450) and phase II (link). N-Oxid is the only metabolite found in plasma. The total amount of original drugs and n-oxid metabolites accounts for 87.5% of the total dose found in plasma. In urine, Roflumilast is not found while there is a trace of Roflumilast N- Oxide (less than 1%). Linking metabolites such as Roflumilast N-OXID Glucuronide and 4-Amino-3.5-Dichloropyridine N-Oxide are found in urine.

Meanwhile, the ability to inhibit the PDE4 enzyme of Roflumilast is 3 times stronger than Roflumilast N-OXID on In vitro, AUC research of Roflumilast N-OXID with about 10 times AUC of Roflumilast.

In vitro research and clinical drug interaction research show that the conversion of Roflumilast into Roflumilast N-Oxid is catalyzed by CYP1A2 and 3A4. Based on in vitro studies on human liver microsomes, at blood treatment concentrations, Roflumilast and N-OXID metabolites do not inhibit CYP 1A3, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4/5, or 4A9/11. Therefore, there is less risk of drug interaction between roflumilast and substances metabolized by the enzymes above. In addition, In vitro, Roflumilast studies do not stimulate CYP 1A2, 2A6, 2C9, 2C19, or 3A4/5 and stimulate weak CYP 2B6.

Elimination

Roflumilast's waste sale time when using a injection is about 9.6 l/h. After drinking, the sale time of Roflumilast and N-Oxid Roflumilast is about 17 and 30 hours. The drug concentration in the stable state of Roflumilast and N-Oxid is achieved after 4 days with Roflumilast and after 6 days with Roflumilast N-OXID when taking daily dose once. About 70% of the markers are found in the urine after injection or drinking Roflumilast.

Before taking Copdumilast Armephaco medicine for maintaining chronic obstructive pulmonary disease (3 blisters x 10 tablets)

How to use

oral medication, should be taken at the same time of the day and with lots of water. Can drink when hungry or full.

Dosage

The recommended dose of the drug is 1 tablet of COPDumilast (0.5mg of Roflumilast), once a day. The drug may need to be used for a few weeks to achieve maximum treatment effect. In clinical studies, the drug has been indicated for up to 1 year.

Special patient group:

Older people: No dose adjustment.

Patients with renal failure: No dose adjustment.

Patients with hepatic impairment: Clinical studies in patients with mild liver failure (Child-Pugh a) are not enough to propose the adjustment of the dose; Therefore, caution should be used with these patients.

Patients with average or severe liver failure are not used COPDumilast.

Children: Not only for patients under 18 years old.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when using overdose?

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

In clinical studies in COPD patients, about 16% of patients with ADR compared to 5% in the group using Placebo. The most common ADR includes diarrhea (5.9%), weight loss (3.4%), nausea (2.9%), abdominal pain (1.9%) and headache (1.7%). Most of these side effects are light and medium. These side effects mainly occur in the first weeks of medication and recover on their own.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

contraindicated

Copdumilast drug contraindicated in the following cases:

Do not use COPDumilast with patients with severe to severe liver failure (Child-Pugh B or C).

Caution when using

Emergency medicine: Copdumilast is not used as emergency medicine for patients with acute bronchospasm.

Weight loss: In 1 year studies, the proportion of patients with weight loss due to drug use is higher than the groupbo group. After stopping the drug, most patients gain weight again after 3 months.

Patient's weight should be checked for each examination. Patients should be recommended for periodic weight testing. If there is an unexplained weight loss and clinical concerns, need to stop the drug and follow the next weight.

Special clinical cases: Due to the inexperienced in clinical experience, should not or stop treatment with Roflumilast for patients with severe immunodeficiency (such as HIV -infected patients, multi -sclerosis, systemic lupus, progressive white substance), severe infections, cancer (except for basal cell cancer) or patients undergoing immunosuppressive drugs (Methotrexate, Azathoprine, Azathoprine, Azathoprine, Azathoprine, Azathoprine, Azathoprine, Azathoprine Infliximab, ethanercept, or oral corticosteroids except for short -term body corticosteroids). Experience in taking drugs with tuberculosis patients, viral hepatitis, herpes and herpes Zoster infections are limited.

The drug has not been researched for patients with congested heart failure (NYHA levels 3 and 4) should not recommend use for these patients.

Mental disorders: Roflumilast may increase the risk of mental disorders such as insomnia, anxiety, restlessness and depression. In some cases, patients who intend and commit suicide occur in patients with or without a history of depression, often occurring in the first weeks of taking drugs. Therefore, it is necessary to carefully assess the risk and benefits of treatment or continue treatment with Roflumilast for patients with a history or have mental symptoms or when used simultaneously with drugs at risk of mental complications.

The drug is not recommended for patients with a history of depression or suicide. Patients and caregivers should be instructed to notify the doctor but change in behavior and mood as well as the appearance of suicide. If the symptoms appear or these symptoms are more severe, or when the suicide intentions still need to stop using Roflumilast for patients.

Last tolerance: while some side effects such as diarrhea, nausea, abdominal pain, first pain occur mainly during the first few weeks of treatment and most will recover when continuing treatment; In some cases, it should be assessed if the signs of drug intolerance are not impaired. This can happen to some special patients such as non -smoking black women or patients taking CYP1A2/2C19/3A4 inhibitors (such as fluvoxamine and cimetidine) or CYP1A2/3A4 Enoxacin inhibitors.

Patients weighing under 60kg: The use of Roflumilast may increase the risk of sleep disorders (mainly insomnia) for patients who weigh less than 60kg, due to the higher PDE4 inhibitor effect in these patients.

Theophyllline: There is no clinical evidence of simultaneous use with theophylline in the maintenance treatment regimen. Therefore, simultaneous use with theophylline is not recommended.

Lactose: Because in the product formula containing lactose, caution should be used for patients with Galact

The effect of the drug on the ability to drive and operate machinery

unknown effects of the drug.

Using drugs for women during pregnancy and lactation

has not fully studied the effects of the drug on pregnant women.

Roflumilast does not cause gene mutations in mice, or rabbits. However, only using COPDumilast for pregnant women has fully assessed the risk and benefits of the drug with the fetus.

Do not use Roflumilast during labor and childbirth. Although there is no research on the effects of drugs on users during labor and childbirth, animal research shows that the drug interrupts the process of labor and childbirth in mice.

Roflumilast and/or its metabolites are excreted into milk in mice. The drug can be excreted in human milk, although it has not been studied, so it is not recommended to appoint the drug for nursing women.

Interactive drug

CYP P450 stimulants: The strong inhibitors of the CYP P450 enzyme reduces the amount of drug in the blood leading to reduced treatment effect of Roflumilast. Therefore, simultaneous use of CYP P450 stimulants (such as rifampicin, phenobarbital, carbamazepine, and phenytoin) are not recommended.

CYP P450 inhibitors: Concomplified use of CYP3A4 inhibitors or both CYP3A4 and CYP1A2 (such as erythromycin, ketoconazole, fluvoxamine, enoxacin, cimetidine) can increase blood drug levels leading to increased side effects of the drug. It is necessary to assess the risk and benefits before this coordination.

Oral contraceptives with Gestodene and Ethinyl Estradiol: Concomplifying these drugs with Roflumilast may increase the concentration of Roflumilast in the blood and increase the risk of side effects. Therefore, it is necessary to consider the risk and benefits when indicated.

Storage

Leave a cool place, avoid light, temperatures below 30⁰C.

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