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Drug overview for ROFLUMILAST (roflumilast):
Generic name: ROFLUMILAST (roe-FLUE-mi-last)
Drug class: Phosphodiesterase-4 (PDE4) inhibitors
Therapeutic class: Respiratory Therapy Agents
Roflumilast is a selective phosphodiesterase type 4 (PDE4) inhibitor.
No enhanced Uses information available for this drug.
Generic name: ROFLUMILAST (roe-FLUE-mi-last)
Drug class: Phosphodiesterase-4 (PDE4) inhibitors
Therapeutic class: Respiratory Therapy Agents
Roflumilast is a selective phosphodiesterase type 4 (PDE4) inhibitor.
No enhanced Uses information available for this drug.
DRUG IMAGES
ROFLUMILAST 500 MCG TABLET
ROFLUMILAST 250 MCG TABLET
The following indications for ROFLUMILAST (roflumilast) have been approved by the FDA:
Indications:
Prevention of bronchospasm with chronic bronchitis
Professional Synonyms:
None.
Indications:
Prevention of bronchospasm with chronic bronchitis
Professional Synonyms:
None.
The following dosing information is available for ROFLUMILAST (roflumilast):
The recommended adult dosage of roflumilast to reduce the risk of chronic obstructive pulmonary disease (COPD) exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations is 500 mcg once daily.
Roflumilast is administered orally once daily without regard to meals.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| ROFLUMILAST 250 MCG TABLET | Maintenance | Adults take 1 tablet (250 mcg) by oral route once daily for 4 weeks |
| ROFLUMILAST 500 MCG TABLET | Maintenance | Adults take 1 tablet (500 mcg) by oral route once daily |
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| ROFLUMILAST 500 MCG TABLET | Maintenance | Adults take 1 tablet (500 mcg) by oral route once daily |
| ROFLUMILAST 250 MCG TABLET | Maintenance | Adults take 1 tablet (250 mcg) by oral route once daily for 4 weeks |
The following drug interaction information is available for ROFLUMILAST (roflumilast):
There are 0 contraindications.
There are 1 severe interactions.
These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.
| Drug Interaction | Drug Names |
|---|---|
| Apremilast; Roflumilast/Strong CYP3A4 Inducers SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: CYP3A4 inducers may induce the metabolism of apremilast(1) and roflumilast(2,3) by CYP3A4. CLINICAL EFFECTS: Concurrent or recent use of strong CYP3A4 inducers may reduce the clinical effectiveness of apremilast(1) and roflumilast.(2,3) PREDISPOSING FACTORS: Induction effects may be more likely with regular use of the inducer for longer than 1-2 weeks. PATIENT MANAGEMENT: Monitor patients receiving concurrent CYP3A4 inducers for decreased apremilast(1) and roflumilast(2,3) efficacy. Concurrent use is not recommended.(1,2) The dosage of roflumilast may need to be adjusted or additional COPD therapy may need to be adjusted during and for up to two weeks after therapy with a CYP3A4 inducer has been completed. DISCUSSION: Pretreatment with rifampin (600 mg daily for 15 days) decreased the maximum concentration (Cmax) and area-under-curve (AUC) of a single dose of apremilast by 43% and 72%, respectively.(1) In an open-label study in 16 healthy males, rifampin (600 mg daily) decreased AUC and Cmax of a single dose of roflumilast (500 mcg) by 80% and 68%, respectively. The AUC and Cmax of roflumilast N-oxide decreased by 56% and 30%, respectively.(2) The total PDE4 inhibitory activity of roflumilast decreased by 60%.(2-4) Strong CYP3A4 inducers linked to this monograph include: apalutamide, barbiturates, carbamazepine, encorafenib, enzalutamide, fosphenytoin, ivosidenib, lumacaftor, mitotane, natisedine, phenobarbital, phenytoin, primidone, rifampin, rifapentine and St. John's wort. |
ASA-BUTALB-CAFFEINE-CODEINE, ASCOMP WITH CODEINE, BRAFTOVI, BUTALB-ACETAMINOPH-CAFF-CODEIN, BUTALBITAL, BUTALBITAL-ACETAMINOPHEN, BUTALBITAL-ACETAMINOPHEN-CAFFE, BUTALBITAL-ASPIRIN-CAFFEINE, CARBAMAZEPINE, CARBAMAZEPINE ER, CARBATROL, CEREBYX, DILANTIN, DILANTIN-125, DONNATAL, EPITOL, EQUETRO, ERLEADA, FIORICET, FIORICET WITH CODEINE, FOSPHENYTOIN SODIUM, LYSODREN, MITOTANE, MYSOLINE, ORKAMBI, PENTOBARBITAL SODIUM, PHENOBARBITAL, PHENOBARBITAL SODIUM, PHENOBARBITAL-BELLADONNA, PHENOBARBITAL-HYOSC-ATROP-SCOP, PHENOHYTRO, PHENYTEK, PHENYTOIN, PHENYTOIN SODIUM, PHENYTOIN SODIUM EXTENDED, PRIFTIN, PRIMIDONE, RIFADIN, RIFAMPIN, SEZABY, TEGRETOL, TEGRETOL XR, TENCON, TIBSOVO, XTANDI |
There are 0 moderate interactions.
The following contraindication information is available for ROFLUMILAST (roflumilast):
Drug contraindication overview.
Moderate or severe hepatic impairment (Child-Pugh class B or C). (See Hepatic Impairment under Warnings/Precautions: Specific Populations, in Cautions.)
Moderate or severe hepatic impairment (Child-Pugh class B or C). (See Hepatic Impairment under Warnings/Precautions: Specific Populations, in Cautions.)
There are 3 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Child-pugh class B hepatic impairment |
| Child-pugh class C hepatic impairment |
| Lactation |
There are 3 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Depression |
| Suicidal |
| Suicidal ideation |
There are 1 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Weight loss |
The following adverse reaction information is available for ROFLUMILAST (roflumilast):
Adverse reaction overview.
Adverse effects reported in 2% or more of patients receiving roflumilast include diarrhea, weight loss, nausea, headache, back pain, influenza, insomnia, dizziness, and decreased appetite.
Adverse effects reported in 2% or more of patients receiving roflumilast include diarrhea, weight loss, nausea, headache, back pain, influenza, insomnia, dizziness, and decreased appetite.
There are 3 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
| None. | None. |
| Rare/Very Rare |
|---|
|
Angioedema Suicidal Suicidal ideation |
There are 23 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Back pain Diarrhea Headache disorder Nausea Weight loss |
Acute abdominal pain Anorexia Dizziness Dyspepsia Gastritis Influenza Insomnia Muscle spasm Rhinitis Sinusitis Symptoms of anxiety Tremor Urinary tract infection Vomiting |
| Rare/Very Rare |
|---|
|
Depression Gynecomastia Skin rash Urticaria |
The following precautions are available for ROFLUMILAST (roflumilast):
Safety and efficacy of roflumilast have not been established in pediatric patients; chronic obstructive pulmonary disease (COPD) does not occur in children.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
Category C. (See Users Guide.) Roflumilast should not be used during labor and delivery. The effect of roflumilast on preterm labor or labor at term in humans is unknown; however, disruption of labor and delivery has occurred in animals receiving the drug.
Roflumilast and/or its metabolites are distributed into milk in rats. Roflumilast and/or its metabolites are likely distributed into human milk. The effects of roflumilast on breast-fed infants have not been established. Roflumilast should not be used in nursing women.
Approximately 46% of patients with COPD who received roflumilast in clinical studies have been older than 65 years of age and about 11% have been older than 75 years of age. Although no substantial differences in safety and efficacy relative to younger adults have been observed, and other clinical experience revealed no evidence of age-related differences, the possibility of increased sensitivity in some older patients cannot be ruled out. Dosage adjustment is not necessary in geriatric patients.
The following prioritized warning is available for ROFLUMILAST (roflumilast):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for ROFLUMILAST (roflumilast)'s list of indications:
| Prevention of bronchospasm with chronic bronchitis | |
| J41 | Simple and mucopurulent chronic bronchitis |
| J41.0 | Simple chronic bronchitis |
| J41.1 | Mucopurulent chronic bronchitis |
| J41.8 | Mixed simple and mucopurulent chronic bronchitis |
| J42 | Unspecified chronic bronchitis |
| J44 | Other chronic obstructive pulmonary disease |
| J44.9 | Chronic obstructive pulmonary disease, unspecified |
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