Names and pronunciation
Daliresp, Daxas
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Individual generic drug information
Extracted information for roflumilast only.
Daliresp, Daxas
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Func. class.: Respiratory antiinflam- matory agent
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Chem. class.: Phosphodiesterase-4 (PDE4) inhibitor
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ACTION: Roflumilast (and the active metabolite roflumilast N-oxide) selectively inhibit phosphodiesterase-4 (PDE4); not a bronchodilator; decreases inflammatory activity, PDE4 inhibition may affect migra- tion and actions of proinflammatory cells
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USES: Add-on treatment to bronchodilator use; for the prevention of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations
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Extracted information for roflumilast only.
CONTRAINDICATIONS: Moder- ate to severe hepatic disease (Child-Pugh B or C) Precautions: Pregnancy, breastfeeding, neonates, infants, children, adolescents, acute bronchospasm, anxiety, insomnia, depression, suicidal ideation or behavior
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SIDE EFFECTS CNS: Insomnia, anxiety, depression, headache, dizziness, tremors, suicidal ideation EENT: Rhinitis, sinusitis GI: Weight loss, diarrhea, nausea, anorexia, abdominal pain, dyspepsia, gastritis, vomiting GU: Urinary tract infection MS: Back pain, muscle cramps/spasm SYST: Infections, influenza
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INTERACTIONS Increase: roflumilast effect—CYP3A4/ CYP1A2 inhibitors (enoxacin, cimetidine, delavirdine, indinavir, isoniazid, itracon- azole, dalfopristin, quinupristin, tipranavir) Increase: roflumilast effect—oral contra- ceptives (gestodene and ethinyl estradiol) Decrease: roflumilast effect—CYP3A4 inducers (rifAMPin, barbiturates, carBA- Mazepine, phenytoin, erythromycin, keto- conazole, fluvoxaMINE, alcohol, etra- virine, ritonavir, bexarotene, rifabutin, OXcarbazepine, nevirapine, modafinil, metyraPONE, PHENobarbital, bosentan, dexamethasone) Altered effect of: fosamprenavir Drug/Herb Decrease: roflumilast effect—St. John’s wort
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Extracted information for roflumilast only.
DOSAGE AND ROUTES COPD exacerbation • Adult: PO 250 mcg/day × 4 wk, then increase to 500 mcg/day
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Available forms: Tabs 250, 500 mcg
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Administer: PO route • Give without regard to meals • Store at room temperature
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Extracted information for roflumilast only.
Assess: • Lung sounds and respiratory function baseline and periodically thereafter • Behavioral changes including mood, depression, suicidal thoughts/behaviors • Liver function tests baseline and peri- odically thereafter; if increases in liver function studies occur, product should be discontinued • CV status: rate, rhythm, chest pain, dyspnea, palpitations, supraventricular dysrrthmias are common • GI symptoms: Weight; weight loss is common, diarrhea • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; do not breastfeed, excreted in breast milk
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Evaluate: • Decreasing exacerbations in COPD
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CLINICAL CONSIDERATIONS R
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Patient and caregiver information: • To take product as directed; not to skip or double doses; to take missed doses as soon as remembered unless al- most time for next dose • Not to use OTC or other products without prescriber approval; not to dis- continue other respiratory products un- less approved by prescriber • Not to be used for acute broncho- spasm but may be continued during acute asthma attacks • Suicidal thoughts/behaviors: to no- tify prescriber of worsening depression or suicidal thoughts/behaviors
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Extracted information for roflumilast only.
PHARMACOKINETICS 80% bioavailability; protein binding 99% (roflumilast); 97% (N-oxide metabolite); extensively metabolized (liver); metabo- lism by CYP3A4 and CYP1A2 produces active metabolite N-oxide; half-life parent drug 17 hr, metabolite 30; 70% excreted in urine; parent drug peak 1 hr (range, 0.5-2 hr), metabolite peak 8 hr (range, 4-13 hr)
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Filter the extracted dose blocks for this individual drug.
COPD exacerbation
• Adult: PO 250 mcg/day × 4 wk, then increase to 500 mcg/day
Candidate age grouping · source page 1177