Roflumilastum

Roflumilastum Uses, Dosage, Side Effects, Food Interaction and all others data.

Roflumilastum is a phosphodiesterase-4 (PDE-4) inhibitor which, due to its selective inhibition of the PDE4 isoenzyme, has potential antiinflammatory and antimodulatory effects in the pulmonary system. It is thought that the increased levels of intracellular cyclic AMP are responsible for the therapeutic actions of Roflumilastum.

Roflumilastum (and its active metabolite, roflumilast N-oxide) increases cyclic adenosine-3′, 5′-monophosphate (cAMP) in lung cells by inhibiting PDE4. Increased cAMP activates PKA, which inactivates transcription factors involved in inflammation. Romflumilast also decreases the amount of sputum neutrophils and eosinophils in COPD patients.

Trade Name Roflumilastum
Availability Prescription only
Generic Roflumilast
Roflumilast Other Names Roflumilast, Roflumilastum
Related Drugs Trelegy Ellipta, ProAir Digihaler, prednisone, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA, Spiriva, Anoro Ellipta
Type
Formula C17H14Cl2F2N2O3
Weight Average: 403.207
Monoisotopic: 402.034954148
Protein binding

Roflumilast is 99% plasma protein bound.

Groups Approved
Therapeutic Class Antihistamines anti-allergies & hypo-sensitisation
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Roflumilastum
Roflumilastum

Uses

Roflumilastum is used for:

  • As add-on therapy to bronchodilator treatment.
  • For the maintenance treatment of severe Chronic Obstructive Pulmonary Disease (COPD) associated with chronic bronchitis (i.e. patients with a history of chronic cough and sputum) in adult patients with a history of frequent exacerbations.

Roflumilastum should not be used as a rescue medication.

Roflumilastum is also used to associated treatment for these conditions: Chronic Obstructive Pulmonary Disease (COPD)

How Roflumilastum works

Roflumilastum is a phosphodiesterase-4 (PDE-4) inhibitor which, due to its selective inhibition of the PDE4 isoenzyme, has potential antiinflammatory and antimodulatory effects in the pulmonary system. It is thought that the increased levels of intracellular cyclic AMP are responsible for the therapeutic actions of Roflumilastum.

Dosage

Roflumilastum dosage

The recommended dosage for patients with COPD is one 500 mcg tablet daily, with or without food.

Side Effects

General disorders: Fatigue.

Metabolism and nutrition disorders: Decreased appetite, Weight decreased.

Musculoskeletal and connective tissue disorders: Back pain, muscle spasms.

Nervous system disorders: Dizziness, Headache, Tremor.

Psychiatric disorders: Anxiety, Depression, Insomnia.

Toxicity

Headache, weight loss, GI upset, insomnia, and loose stools.

Precaution

Not as emergency treatment for relief of acute brochospasm. Monitor body wt regularly. Severe immunological disease, severe acute infections, cancers (except basal cell carcinoma) or patients on immunosuppressants; CHF (NYHA grades III & IV). History of depression associated with suicidal ideation or behavior. Galactose intolerance, Lapp-lactase deficiency or glucose-galactose malabsorption. Hepatic impairment. Pregnancy & lactation.

Interaction

A major step in Roflumilastum metabolism is the N-oxidation of Roflumilastum to Roflumilastum N-oxide by CYP3A4 and CYP1A2. Therefore, the use of strong cytochrome P450 enzyme inducers (e.g. rifampicin, phenobarbital, carbamazepine, phenytoin) with Roflumilastum is not recommended. The co-administration of Roflumilastum with CYP3A4 inhibitors or dual inhibitors that inhibit both CYP3A4 and CYP1A2 simultaneously (e.g., erythromycin, ketoconazole, fluvoxamine, enoxacin, cimetidine) may increase Roflumilastum systemic exposure and may result in increased adverse reactions. The co-administration of Roflumilastum with oral contraceptives containing gestodene and ethinyl estradiol may increase roflumilast systemic exposure and may result in increased side effects.

Food Interaction

  • Take with or without food. Administering roflumilast with a high-fat meal reduced and delayed the Cmax and Tmax, respectively, but did not impact the AUC of roflumilast or its active metabolite (roflumilast N‐oxide).

[Minor] Food intake does not affect the total exposure to roflumilast and its pharmacologically active N-oxide metabolite, but delays the time to maximum concentration (Tmax) of roflumilast by one hour and reduces its peak plasma concentration (Cmax) by approximately 40%.

The Tmax and Cmax of
roflumilast N-oxide are unaffected.

Roflumilastum may be taken with or without food.

Roflumilastum Disease Interaction

Major: hepatic impairmentModerate: depression, weight loss

Volume of Distribution

Roflumilastum has a Vd of 2.9L/kg with a dose of 500mcg. Permeability of roflumilast across the blood-brain barrier appears to be poor in rat studies.

Elimination Route

After a 500mcg dose, the bioavailability of roflumilast is about 80%. In the fasted state, maximum plasma concentrations are reached in 0.5 to 2 hours. While in the fed state, Cmax is reduced by 40%, Tmax is increased by one hour, and total absorption is unchanged.

Half Life

Plasma half-life of roflumilast is 17 hours and its metabolite is 30 hours (oral dose).

Clearance

~9.6 L/hour.

Elimination Route

Roflumilastum is excreted 70% in the urine as roflumilast N-oxide.

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Roflumilastum should not be used during pregnancy & lactation.

Contraindication

Hypersensitivity to Roflumilastum or to any of the excipients. Moderate to severe liver impairment.

Special Warning

Geriatrics ( 65 years of age): There were no overall differences in safety and effectiveness of Roflumilastum in the elderly compared to younger patients with COPD. Therefore, no dose adjustment is necessary.

Pediatrics (<18 years of age): Safety and effectiveness of Roflumilastum in children and adolescents below 18 years of age have not been established.

Hepatic Impairment: Roflumilastum is not recommended for use in patients with moderate or severe liver impairment.

Renal impairment: No dosage adjustment is necessary for patients with renal impairment

Acute Overdose

No case of overdose has been reported in clinical studies with Roflumilastum. However, during the Phase I studies of Roflumilastum, at an increased rate after a single oral dose of 2500 mcg and a single dose of 5000 mcg,

The following symptoms were observed: headache, gastrointestinal disorders, dizziness, palpitations, lightheadedness, clamminess and arterial hypotension.

Missed Dose: Patients should be advised that if they forget to take a tablet at the usual time, they should take the tablet as soon as they remember or continue on the next day with the next tablet at the usual time. Patients should not take a double dose to make up for a forgotten dose.

Storage Condition

Store below 30° C, keep away from light, moisture. Keep out of the reach of children.

Innovators Monograph

You find simplified version here Roflumilastum

Roflumilastum contains Roflumilast see full prescribing information from innovator Roflumilastum Monograph, Roflumilastum MSDS, Roflumilastum FDA label

FAQ

What is Roflumilastum used for?

Roflumilastum is used in people with severe chronic obstructive pulmonary disease  to reduce the number of episodes or worsening of COPD symptoms.

How safe is Roflumilastum?

As for the safety of Roflumilastum treatment, the overall cumulative incidence of adverse drug reaction was 54.2% in the Roflumilastum group and 48.2% in the placebo group.

How does Roflumilastum work?

Roflumilastum works by decreasing swelling in the lungs.

What are the common side effects of Roflumilastum?

Common side effects of Roflumilastum are include:

  • diarrhea.
  • nausea.
  • dizziness.
  • headache.
  • back pain.
  • muscle spasm.
  • decrease in appetite.
  • uncontrollable shaking of a part of your body.

Is Roflumilastum safe during pregnancy?

The manufacturer makes no recommendation regarding use during pregnancy.Roflumilastum disrupted the labor and delivery process in animal studies. Do not use this drug during labor and delivery.

Is Roflumilastum safe during breastfeeding?

Excretion into human milk is probable.Animals given 1 mg/kg of this drug orally had breastmilk concentrations of active drug or its metabolites of 0.32 mcg/gram after 8 hours.

When should best taken of Roflumilastum?

It is usually taken with or without food once a day. Take Roflumilastum at around the same time every day.

How quickly does Roflumilastum work?

Your breathing difficulty and other symptoms of chronic obstructive pulmonary disease may improve within several weeks of taking Daliresp.

Does Roflumilastum cause depression?

Depression, anxiety, and insomnia occur about twice as often in patients taking Roflumilastum as in those taking placebo.

Who should not take Roflumilastum?

You should not use Roflumilastum if you are allergic to it, or if you have moderate or severe liver disease. Tell your doctor if you have ever had: liver disease,depression, mental illness, or suicidal thoughts or actions.

Can I take Roflumilastum for a long time?

You should take it once daily for the first 4 weeks only. After the first 4 weeks, you will increase to the 500-mcg dose. The 250-mcg dose is a starting dose only.Roflumilastum is not the effective dose and should not be taken for more than the first 4 weeks.

What happens if I miss a dose of Roflumilastum?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Does Roflumilastum cause weight loss?

Roflumilastum can cause weight loss. You should check your weight on a regular basis. You will also need to see your doctor regularly to have your weight checked. If you notice that you are losing weight, call your doctor.

What is Roflumilastum indication?

Roflumilastum is indicated as a treatment to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations.Roflumilastum is not a bronchodilator, and it is not indicated for the treatment of acute bronchospasm.

Can Roflumilastum be crushed?

Nothing in the prescribing information accompanying the drug would indicate that the tablets cannot be crushed.

What happens if I overdose of Roflumilastum?

Seek emergency medical attention.

Can I stop Roflumilastum suddenly?

You should keep taking Roflumilastum until your doctor discontinues the treatment. Do not stop taking Roflumilastum without talking to your doctor, even if you are feeling better and are no longer having symptoms of chronic obstructive pulmonary disease.

*** Taking medicines without doctor's advice can cause long-term problems.
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