Dosing & Uses
Dosing Form & Strengths
tablet
- 250mcg
- 500mcg
Chronic Obstructive Pulmonary Disease
Indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations
500 mcg PO qDay
Starting treatment with 250 mcg PO qDay for 4 weeks and increasing to 500 mcg qDay thereafter may reduce the rate of treatment discontinuation in some patients
NOTE: 250 mcg/day is not the effective (therapeutic) dose
Also see Administration
Dosage Modifications
Renal impairment
- No dosage adjustment required
Hepatic impairment
- Mild (Child-Pugh class A): Not sufficiently studied; AUCs of roflumilast and roflumilast N-oxide are increased by 51% and 24%, respectively; benefits of administration must be weighed against risks
- Moderate-to-severe (Child-Pugh class B or C): Contraindicated
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (17)
- bosentan
bosentan will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- carbamazepine
carbamazepine will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
carbamazepine will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness - dexamethasone
dexamethasone will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- etravirine
etravirine will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- fosphenytoin
fosphenytoin will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- nafcillin
nafcillin will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- nevirapine
nevirapine will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- oxcarbazepine
oxcarbazepine will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- pentobarbital
pentobarbital will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- phenobarbital
phenobarbital will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
phenobarbital will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness - phenytoin
phenytoin will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- primidone
primidone will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
primidone will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness - rifabutin
rifabutin will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- rifampin
rifampin will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
rifampin will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness - rifapentine
rifapentine will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- St John's Wort
St John's Wort will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
Serious - Use Alternative (12)
- abametapir
abametapir will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.
- apalutamide
apalutamide will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- dabrafenib
dabrafenib will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- enzalutamide
enzalutamide will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fexinidazole
fexinidazole will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- idelalisib
idelalisib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- ivosidenib
ivosidenib will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- lonafarnib
lonafarnib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
- ritonavir
ritonavir will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- secobarbital
secobarbital will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tucatinib
tucatinib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- voxelotor
voxelotor will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (43)
- amiodarone
amiodarone increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
- armodafinil
armodafinil will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Concomitant therapy may reduce therapeutic effectiveness.
- cenobamate
cenobamate will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- ceritinib
ceritinib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cigarette smoking
cigarette smoking will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- cimetidine
cimetidine increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
- cobicistat
cobicistat will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- efavirenz
efavirenz will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration not recommended; strong cytochrome P450 enzyme inducers decrease systemic exposure to roflumilast and may reduce the therapeutic effectiveness
- elagolix
elagolix decreases levels of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
- encorafenib
encorafenib, roflumilast. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- erythromycin base
erythromycin base increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
- erythromycin lactobionate
erythromycin lactobionate increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
- erythromycin stearate
erythromycin stearate increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
- fedratinib
fedratinib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fluvoxamine
fluvoxamine increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
- ifosfamide
roflumilast will increase the level or effect of ifosfamide by immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- indinavir
indinavir will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- itraconazole
itraconazole will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ketoconazole
ketoconazole increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
ketoconazole will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - lenacapavir
lenacapavir will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- levoketoconazole
levoketoconazole increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
levoketoconazole will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - lomustine
roflumilast will increase the level or effect of lomustine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- lopinavir
lopinavir will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Concomitant therapy may reduce therapeutic effectiveness.
- lorlatinib
lorlatinib will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mechlorethamine
roflumilast will increase the level or effect of mechlorethamine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- melphalan
roflumilast will increase the level or effect of melphalan by immunosuppressive effects; risk of infection. Use Caution/Monitor. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects.
- mitotane
mitotane decreases levels of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.
- modafinil
modafinil will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Concomitant therapy may reduce therapeutic effectiveness.
- omeprazole
omeprazole will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Concomitant therapy may reduce therapeutic effectiveness.
- oxaliplatin
roflumilast and oxaliplatin both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Use of oxaliplatin with concomitant immunosuppressants or with impaired immune systems may increased risk for serious infections.
- procarbazine
roflumilast will increase the level or effect of procarbazine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- ribociclib
ribociclib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- riociguat
riociguat, roflumilast. Either increases toxicity of the other by additive vasodilation. Modify Therapy/Monitor Closely. Riociguat is contraindicated with specific PDE-5 inhibitors (eg sildenafil, tadalafil, vardenafil) and nonspecific PDE-5 inhibitors (eg theophylline, dipyridamole) due to risk of hypotension; data are limited with other PDE inhibitors (eg, milrinone, cilostazol, roflumilast).
- ritonavir
ritonavir will decrease the level or effect of roflumilast by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Concomitant therapy may reduce therapeutic effectiveness.
- rucaparib
rucaparib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- stiripentol
stiripentol, roflumilast. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
- tazemetostat
tazemetostat will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- tipranavir
tipranavir will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- voriconazole
voriconazole will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- zafirlukast
zafirlukast increases levels of roflumilast by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration with dual inhibitors of CYP3A4 and CYP1A2 may increase systemic exposure and result in increased adverse reactions.
Minor (4)
- acetazolamide
acetazolamide will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
1-10%
Diarrhea (9.5%)
Weight loss (7.5%)
Nausea (4.7%)
Headache (4.4%)
Back pain (3.2%)
Insomnia (2.4%)
Decreased appetite (2.1%)
Dizziness (2.1%)
1-10%
Abdominal pain (1-2%)
Anxiety (1-2%)
Depression (1-2%)
Dyspepsia (1-2%)
Gastritis (1-2%)
Muscle spasms (1-2%)
Rhinitis (1-2%)
Sinusitis (1-2%)
Tremor (1-2%)
Urinary tract infection (1-2%)
Vomiting (1-2%)
Frequency Not Defined
Suicidality
Postmarketing Reports
Hypersensitivity reactions including angioedema, urticaria, rash
Gynecomastia
Warnings
Contraindications
Hypersensitivity
Moderate-to-severe liver impairment (Child-Pugh class B or C)
Cautions
Not indicated for relief of acute bronchospasm; drug is not bronchodilator
Psychiatric events, including suicidality, reported (monitor for emergence or worsening of insomnia, mood disturbance, or anxiety)
Monitor for clinically significant weight loss; this may be reversible upon discontinuance
Drug interaction overview
- Strong CYP3A4 inducers may reduce therapeutic effectiveness of roflumilast; coadministration not recommended
CYP P450 enzyme inhibitors
- CYP3A4 inhibitors or dual inhibitors that inhibit both CYP3A4 and CYP1A2 simultaneously may increase roflumilast systemic exposure and increase risk for adverse effects
Pregnancy & Lactation
Pregnancy
Data are not available regarding use in pregnant women
Lactation
Probable that roflumilast, its metabolites, or both are excreted into milk; avoid use
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Selective phosphodiesterase (PDE)-4 inhibitor; PDE-4 inhibition leads to accumulation of intracellular cyclic adenosine monophosphate (cAMP) in lung tissue and is thought to be underlying mechanism of action
Absorption
80% absorbed
Peak plasma time: 1 hr (range, 0.5-2 hr); active metabolite, 8 hr
Distribution
Protein bound: 99%
Vd: 2.9 L/kg
Metabolism
Extensively metabolized via phase I (CYP450) and phase II (conjugation) reactions; N-oxide metabolite is only major metabolite observed in human plasma; together, roflumilast and roflumilast N-oxide account for 87.5% of total dose administered in plasma
Biotransformation of roflumilast to N-oxide metabolite is mediated by CYP1A2 and CYP3A4
Elimination
Half-life: Roflumilast, 17 hr; N-oxide metabolite, 30 hr
Clearance: 9.6 L/hr
Excretion: Urine (70%)
Administration
Oral Administration
May take with or without food
May titrate dose from 250 mcg/day to 500 mcg/day (therapeutic dose) over 4 weeks to improve tolerability (see Dosing)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| roflumilast oral - | 500 mcg tablet |  | |
| roflumilast oral - | 500 mcg tablet |  | |
| roflumilast oral - | 500 mcg tablet |  | |
| roflumilast oral - | 500 mcg tablet |  | |
| Daliresp oral - | 500 mcg tablet |  | |
| Daliresp oral - | 250 mcg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
roflumilast oral
ROFLUMILAST - ORAL
(roe-FLUE-mi-last)
COMMON BRAND NAME(S): Daliresp
USES: Roflumilast is used to control and prevent symptoms (wheezing and shortness of breath) caused by ongoing lung disease (chronic obstructive pulmonary disease-COPD which includes bronchitis). It should be used along with other medications (bronchodilators such as salmeterol, ipratropium) to treat COPD. It works by reducing the irritation and swelling of the airways. Controlling symptoms of breathing problems can decrease time lost from work or school.This medication must be used regularly to be effective. It does not work right away and should not be used to relieve sudden shortness of breath or wheezing. If sudden breathing problems occur, use your quick-relief inhaler (such as albuterol, also called salbutamol in some countries) as prescribed.
HOW TO USE: Read the Medication Guide and, if available, the Patient Information Leaflet from your pharmacist before you start taking roflumilast and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily.Use this medication regularly in order to get the most benefit from it. This medication works best if used at evenly spaced intervals. To help you remember, use it at the same time each day. Do not increase your dose, use this medication more frequently, or stop using it without first consulting your doctor.Tell your doctor if your condition does not improve or if it worsens.
SIDE EFFECTS: Diarrhea, weight loss, stomach/abdominal pain, nausea, loss of appetite, headache, or dizziness may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Check your weight regularly while taking this medication. Tell your doctor right away of any unusual or extreme weight loss.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as nervousness, depression, thoughts of suicide), trouble sleeping, shaking (tremors), fast/irregular heartbeat.A very serious allergic reaction to this product is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking roflumilast, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, cancer, heart disease (such as heart failure), current/past infections (such as tuberculosis, herpes), mental/mood disorders (depression, thoughts of suicide), unexplained/extreme weight loss, immune system disorders (such as lupus, HIV).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some medications can affect the removal of roflumilast from your body, which may affect how this product works. Examples include rifamycins (such as rifampicin), drugs used to treat seizures (such as carbamazepine, phenytoin), among others.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe dizziness, fast/pounding heartbeat.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as lung function, weight) may be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised December 2022. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
