释义 |
roflumilast Translations
roflumilast
roflumilast (row-floo-mi-last) roflumilast, Daliresp (trade name), Daxas (trade name) Classification Therapeutic: copd agents Pharmacologic: phosphodiesterase inhibitors Pregnancy Category: C
IndicationsTo ↓ the risk of exacerbations in severe COPD patients that have a history of chronic bronchitis with exacerbations.ActionRoflumilast and one active metabolite (roflumilast N-oxide) act as selective inhibitors of phosphodiesterase 4 (PDE4), responsible for breaking down 3', 5'-adenosine monophosphate (cAMP). Resulting intracellular accumulation of cAMP in lung tissue.Reduces cells (neutrophils, eosinophils and total cells) in sputum.Therapeutic effects↓ exacerbations in COPD patients.PharmacokineticsAbsorption: Well absorbed following oral administration.Distribution: Parent drug and metabolites probably enter breast milk.Protein Binding: Roflumilast—99%; roflumilast N-oxide—97%.Metabolism and Excretion: Mostly metabolized (87.5%), primarily by CYP3A4 and CYP1A2 enzyme systems One metabolite, roflumilast N-oxide in pharmacologically active. Inactive metabolites excreted in urine.Half-life: Roflumilast—17 hr; roflumilast N-oxide—30 hr.Time/action profile (blood levels)ROUTE | ONSET | PEAK | DURATION |
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PO | unknown | 1 (4–13†) | 24 hr | †For roflumilast N-oxide.Contraindications/PrecautionsContraindicated in: Acute bronchospasm;Moderate to severe hepatic impairment;Concurrent use of strong inducers of CYP3A4 and CYP1A2 enzymes; Lactation: Avoid breast-feeding.Use Cautiously in: History of depression/suicidal thoughts; Obstetric: Use only if potential maternal benefit justifies potential risk to the fetus; Pediatric: Safety and effectiveness not established.Adverse Reactions/Side EffectsCentral nervous system- suicidal thoughts (life-threatening)
- anxiety
- depression
- dizziness
- headache
- insomnia
DermatologicGastrointestinal- diarrhea (most frequent)
- abdominal pain
- ↓ appetite
- dyspepsia
- gastritis
- nausea
- vomiting
MetabolicMusculoskeletalNeurologicMiscellaneous- hypersensitivity reactions including angioedema (life-threatening)
InteractionsDrug-Drug interactionStrong inducers of the CYP3A4 and CYP1A2 enzyme systems, including rifampicin, phenobarbital, carbamazepine, and phenytoin ↓ blood levels and effectiveness; concurrent use should be avoided.Blood levels and risk of adverse reactions ↑ by concurrent use of inhibitors of the CYP3A4 enzyme system and dual inhibitors of the CP3A4 and CYP1A2 enzyme systems including erythomycin, ketoconazole, fluvoxamine, and cimetidine.Gestodene and ethinyl estradiol may also ↑ levels and risk of adverse reactions; risk should be considered.Route/DosageOral (Adults) 500 mcg once daily.AvailabilityTablets: 500 mcg Nursing implicationsNursing assessment- Assess respiratory status periodically during therapy.
- Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of roflumilast.
- Assess mental status (orientation, mood, behavior) before and periodically during therapy. Assess for suicidal tendencies.
- Monitor for signs and symptoms of hypersensitivity reactions (angioedema, urticaria, rash). Discontinue therapy and treat symptomatically if symptoms occur.
Potential Nursing DiagnosesIneffective airway clearance
Implementation- Oral: Administer without regard to food.
Patient/Family Teaching- Instruct patient to take roflumilast as directed. Advise patient to read Medication Guide before starting therapy and with each Rx refill; new information may be available.
- Inform patient that roflumilast is not a bronchodilator and should not be used for treating sudden breathing problems.
- Advise patient to monitor weight regularly. If weight loss occurs, notify health care professional; may require discontinuation of therapy.
- Advise patient and family to notify health care professional if thoughts about suicide or dying, attempts to commit suicide, trouble sleeping, new or worse depression, new or worse anxiety, acting on dangerous impulses, or other unusual changes in behavior or mood or signs and symptoms of hypersensitivity reactions occur.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of Rx, OTC, and herbal products without consulting health care professional.
- Advise female patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Evaluation/Desired Outcomes- ↓ in the number of flare-ups or the worsening of COPD symptoms (exacerbations).
roflumilast A selective inhibitor the phosphodiesterase type 4 (PDE4), which is used as maintenance therapy of severe chronic obstructive pulmonary disease with a forced expiratory volume at one second < 50% of predicted in a background of chronic bronchitis. |