Names and pronunciation
(er-loe′tye-nib) Tarceva
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Individual generic drug information
Extracted information for erlotinib only.
(er-loe′tye-nib) Tarceva
Source page 495
Func. class.: Antineoplastic— miscellaneous
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Chem. class.: Epidermal growth factor receptor inhibitor
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ACTION: Not fully understood; inhibits intracellular phosphorylation of cell-surface receptors associated with epidermal growth factor receptors
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USES: Non–small-cell lung cancer (NSCLC) including EGFR exon 19 deletions or exon 21 substitution muta- tions, pancreatic cancer
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Extracted information for erlotinib only.
CONTRAINDICATIONS: Preg- nancy, breastfeeding Precautions: Children, geriatric patients, ocular/pulmonary/renal/hepatic disorders, diverticulitis
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SIDE EFFECTS CNS: CVA, anxiety, depression, head- ache, rigors, insomnia CV: MI/ischemia EENT: Ocular changes, conjunctivitis, eye pain, hypertrichosis GI: Nausea, diarrhea, vomiting, anorexia, mouth ulceration, hepatic failure, GI perforation GU: Renal impairment/failure HEMA: Deep vein thrombosis, bleeding INTEG: Rash, Stevens-Johnson–like skin reaction, toxic epidermal necrolysis MISC: Fatigue, infection RESP: Interstitial lung disease, cough, dyspnea SYST: Hepatorenal syndrome
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INTERACTIONS Increase: GI bleeding, may be fatal— warfarin, NSAIDs Increase: erlotinib concentrations— CYP3A4 inhibitors (ketoconazole, itra- conazole, erythromycin, clarithromycin, telithromycin) Increase: plasma concentrations of war- farin, metoprolol Increase: myopathy—HMG-CoA reduc- tase inhibitors Decrease: erlotinib levels—CYP3A4 inducers (phenytoin, rifAMPin, carBA Mazepine, PHENobarbital), proton pump inhibitors Drug/Herb Decrease: erlotinib levels—St. John’s wort Drug/Smoking Decrease: erlotinib level; dose may need to be increased Drug/Food Increase: effect of erlotinib—grapefruit juice Drug/Lab Test Increase: INR, PT, AST, ALT, bilirubin
Source page 496
Extracted information for erlotinib only.
DOSAGE AND ROUTES Non–small-cell lung cancer (NSCLC), maintenance, after failure of at least one chemotherapy regimen • Adult: PO 150 mg/day Pancreatic cancer • Adult: PO 100 mg/day in combination with gemcitabine 1000 mg/m2 cycle 1, days 1, 8, 15, 22, 29, 36, 43 of 8-wk cycle; E cycle 2 and subsequent cycles, days 1, 8, 15 of 4-wk cycle, used with gemcitabine CYP3A4 inducers concurrently (rifAMPin, phenytoin) • Increase dose by 50 mg q2wk (max 450 mg/day) CYP3A4 inhibitors (atazanavir, cla rithromycin, indinavir, itraconazole, ketoconazole, telithromycin, ritonavir, saquinavir, troleandomycin, nelfinavir) or CYP3A4 and CYP1A2 inhibitors con- currently (ciprofloxacin) • Decrease dose by 50 mg as needed
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Available forms: Tablets 25, 100, 150 mg
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Administer: • 1 hr prior to or 2 hr after food; at same time of day
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Extracted information for erlotinib only.
Assess: • Serious skin toxicities: toxic epider- mal necrolysis, Stevens-Johnson syn- drome; check for rash, blistering; discon- tinue treatment, may need corticosteroids, antiinfectives • MI/ischemia, CVA in patients with pancreatic cancer • Pulmonary changes: lung sounds, cough, dyspnea; interstitial lung disease may occur, may be fatal; discontinue therapy if confirmed • Ocular changes: eye irritation, cor- neal erosion/ulcer, aberrant eyelash growth, discontinue if ulcers are present in the cornea, hold for keratitis (grade 3 or 4) • GI symptoms: frequency of stools; if diarrhea is poorly tolerated, therapy may be discontinued for ≤14 days, monitor for dehydration, fluid status during pe- riod of vomiting and diarrhea, may use antidiarrheal • Blood studies: INR, LFTs, PT; elevated INR and hemorrhage are increased when used with warfarin • Hepatic failure: interrupt if severe changes to liver function occur (total bilirubin >3× ULN and/or transaminases >5× ULN when normal pretreatment LFTs) • GI perforation/bleeding: some cases have been fatal; usually occurs in those using NSAIDs, taxanes, or in those with diverticulitis or peptic ulcer disease; dis- continue if these occur • Pregnancy/breastfeeding: do not use in pregnancy or for 1 mo after last dose; do not breastfeed during or for 2 wk after final dose
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Evaluate: • Therapeutic response: decrease in NSCLC cells, pancreatic cancer cells
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To report adverse reactions immedi- ately: SOB, severe abdominal pain, persis- tent diarrhea or vomiting, ocular changes, skin eruptions (face, upper chest/back) • About reason for treatment, expected results; to take on empty stomach 1 hr prior to or 2 hr after meals • To use sunscreen, protective clothing to prevent sunburn • To avoid use with other products, herbs, supplements unless approved by provider, not to use with grapefruit or grapefruit juice • To avoid smoking; decreases effect of this product • Pregnancy/breastfeeding: To use re- liable contraception during treatment; to avoid breastfeeding
Source page 496
Extracted information for erlotinib only.
PHARMACOKINETICS Slowly absorbed (60%); peak 3-7 hr; dura- tion up to 24 hr; excreted in feces (86%), urine (<4%); metabolized by CYP3A4; half- life 36 hr; protein binding 93%; inhibits tyrosine kinase, which is a factor in epider- mal growth factor receptor (EGFR)
Source page 495
Filter the extracted dose blocks for this individual drug.
Non–small-cell lung cancer (NSCLC), maintenance, after failure of at least one chemotherapy regimen
• Adult: PO 150 mg/day Pancreatic cancer
Candidate age grouping · source page 495
Non–small-cell lung cancer (NSCLC), maintenance, after failure of at least one chemotherapy regimen
• Adult: PO 100 mg/day in combination with gemcitabine 1000 mg/m2 cycle 1, days 1, 8, 15, 22, 29, 36, 43 of 8-wk cycle; E cycle 2 and subsequent cycles, days 1, 8, 15 of 4-wk cycle, used with gemcitabine CYP3A4 inducers concurrently (rifAMPin, phenytoin)
Candidate age grouping · source page 495
Non–small-cell lung cancer (NSCLC), maintenance, after failure of at least one chemotherapy regimen
• Increase dose by 50 mg q2wk (max 450 mg/day) CYP3A4 inhibitors (atazanavir, cla rithromycin, indinavir, itraconazole, ketoconazole, telithromycin, ritonavir, saquinavir, troleandomycin, nelfinavir) or CYP3A4 and CYP1A2 inhibitors con- currently (ciprofloxacin)
Candidate age grouping · source page 495
Non–small-cell lung cancer (NSCLC), maintenance, after failure of at least one chemotherapy regimen
• Decrease dose by 50 mg as needed
Candidate age grouping · source page 495