Relast

Uses

Relast 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.

Relast should not be used as a rescue medication.

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

How Relast works

Relast 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 Relast.

Dosage

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

Relast may be taken with or without food.

Relast Drug Interaction

Moderate: budesonide / formoterolUnknown: fluticasone / salmeterol, fluticasone / vilanterol, rosuvastatin, duloxetine, apixaban, fluticasone nasal, furosemide, atorvastatin, guaifenesin, esomeprazole, albuterol, pantoprazole, tiotropium, tiotropium, fluticasone / umeclidinium / vilanterol, albuterol, cyanocobalamin, ascorbic acid, cholecalciferol

Relast Disease Interaction

Major: hepatic impairmentModerate: depression, weight loss

Volume of Distribution

Relast 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

Relast 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. Relast should not be used during pregnancy & lactation.

Contraindication

Hypersensitivity to Relast 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 Relast in the elderly compared to younger patients with COPD. Therefore, no dose adjustment is necessary.

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

Hepatic Impairment: Relast 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 Relast. However, during the Phase I studies of Relast, 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

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