Mosby's 2014 Nursing Drug Reference (212 page)

BOOK: Mosby's 2014 Nursing Drug Reference
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Canada only   Side effects:
italics
= common;
bold
= life-threatening   
Nurse Alert

imatinib (Rx)

(im-ah-tin′ib)

Gleevec

Func. class.:
Antineoplastic—miscellaneous

Chem. class.:
Protein-tyrosine kinase inhibitor

ACTION:

Inhibits Bcr-Abl tyrosine kinase created in patients with chronic myeloid leukemia (CML), also inhibits tyrosine kinases including EGF, FGF, PDGF, SCF, VEGF, NFG

USES:

Treatment of chronic myeloid leukemia (CML); Philadelphia-chromosome–positive patients in blast-cell crisis or patients in chronic failure after treatment failure with interferon alfa; gastrointestinal stromal tumors (GIST) positive for c-Kit; chronic eosinophilic leukemia, acute lymphocytic leukemia, dermatofibrosarcoma protuberans, myelodysplastic syndrome, systemic mastocytosis

Unlabeled uses:
Desmoid tumor

CONTRAINDICATIONS:

Pregnancy (D), hypersensitivity

Precautions:
Breastfeeding, children, geriatric patients, cardiac/renal/hepatic/
dental disease, GI bleeding, bone marrow suppression, infection, thrombocytopenia, neutropenia, immunosuppression

DOSAGE AND ROUTES
Calculator
For the treatment of Philadelphia chromosome positive (Ph+) chronic myelogenous leukemia (CML) chronic phase as initial therapy

• Adult: PO
400 mg/day, continue as long as beneficial; may increase to 600 mg/day in the absence of severe adverse reactions and severe non–leukemia-related neutropenia or thrombocytopenia

• Adolescent/child >2 yr: PO
340 mg/m
2
/day, max 600 mg/day; the daily dose may be given as a single dose or split into 2 doses given once in the morning and once in the evening

Adult with Ph+ CML in chronic phase after the failure of interferon-alfa therapy

• Adult: PO
400 mg every day; continue as long as beneficial, may increase to 600 mg/day

Pediatric patients with Ph+ chronic phase CML whose disease has recurred after hematopoietic stem cell transplant or who are resistant to interferon-alfa therapy

• Adolescent/child >3 yr: PO
260 mg/m
2
/day as a single daily dose, or the dose may be divided given once in the morning and once in the evening; may increase to 340 mg/m
2
/day

Patients with Ph+ CML in accelerated phase or blast crisis

• Adult: PO
600 mg every day, continue as long as beneficial, may increase to 800 mg/day (400 mg bid)

Resistant or relapsed PH+ acute lymphocytic leukemia (ALL)

• Adult: PO
600 mg every day, continue as long beneficial

Kit
(CD117)-positive unresectable and/or metastatic GIST

• Adult: PO
400–600 mg every day, may increase to 400 mg bid

Adjuvant treatment of
kit
(CD117)-positive GIST after complete gross resection

• Adult: PO
400 mg/day

Patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIPL1L1-PDGFR α-fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIPL1L-PDGFR α-fusion kinase negative or unknown

• Adult: PO
400 mg/day in those who are FIPL1L-PDGFR α-fusion kinase negative or unknown; for HES/CEL patients with demonstrated FIP1L1-PDGFR α-fusion kinase, 100 mg/day, may increase to 400 mg

Myelodysplastic syndrome (MDS)/myeloproliferative disease (MPD) associated with the PDGFR (platelet-derived growth factor receptor) gene rearrangements

• Adult: PO
400 mg/day

Aggressive systemic mastocytosis (ASM) without D816V c-Kit mutation or with c-Kit mutation status unknown

• Adult: PO
400 mg/day in those without the FIP1L1-PDGFR-α c-Kit mutation; if c-Kit status is unknown or not available, give 400 mg/day

Unresectable, recurrent, and/or metastatic dermatofibrosarcoma protuberans (DFSP)

• Adult: PO
400 mg bid (800 mg/day)

Renal dose


 
Adult: PO
CCr 40-59 ml/min, max 600 mg/day; CCr 20-39 ml/min, decrease initial dose by 50%, max 400 mg/day; CCr <20 ml/min, use with caution, 100 mg/day

Hepatic dose


 
Adult: PO
Total bilirubin 1.5-3 × ULN and any AST, decrease initial dose to 400 mg/day; total bilirubin >3 × ULN and any AST, decrease initial dose to 300 mg/day

Available forms:
Tabs 100, 400 mg

Administer:

• 
With meal and large glass of water to decrease GI symptoms; doses of 800 mg should be given as 400 mg bid

• 
Tab may be dispersed in a glass of water or apple juice, use 50 ml of liquid for 100-mg tab, 200 ml liquid for 400-mg tab

• 
Continue as long as beneficial

SIDE EFFECTS

CNS:
CNS hemorrhage,
headache, dizziness, insomnia

CV:
Hemorrhage, heart failure, cardiac tamponade, hypereosinophilia, cardiac toxicity

EENT:
Blurred vision, conjunctivitis

GI:
Nausea
,
hepatotoxicity, vomiting, dyspepsia,
GI hemorrhage,
anorexia, abdominal pain
,
GI perforation,
diarrhea

HEMA:
Neutropenia, thrombocytopenia, bleeding

INTEG:
Rash, pruritus
, alopecia, photosensitivity

META:
Fluid retention, hypokalemia, edema

MISC:
Fatigue, epistaxis, pyrexia, night sweats, increased weight, flulike symptoms, hypothyroidism

MS:
Cramps, pain, arthralgia, myalgia

RESP:
Cough, dyspnea, nasopharyngitis, pneumonia, upper respiratory tract infection,
pleural effusion,
edema

PHARMACOKINETICS

Well absorbed (98%); protein binding 95%; metabolized by CYP3A4; excreted in feces, small amount in urine; peak 2-4 hr; duration 24 hr (imatinib), 40 hr (metabolite); half-life 18-40 hr

INTERACTIONS

Increase:
hepatotoxicity—acetaminophen

Increase:
imatinib concentrations—CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, clarithromycin)

Increase:
plasma concentrations of simvastatin, calcium channel blockers, ergots

Increase:
plasma concentration of warfarin; avoid use with warfarin; use low-molecular-weight anticoagulants instead

Decrease:
imatinib concentrations—CYP3A4 inducers (dexamethasone, phenytoin, carBAMazepine, rifampin, PHENobarbital)

Drug/Herb

Decrease:
imatinib concentration—St. John’s wort

Drug/Lab Test

Increase:
bilirubin, amylase, LFTs

Decrease:
albumin, calcium, potassium, sodium, phosphate, platelets, neutrophils, leukocytes, lymphocytes

NURSING CONSIDERATIONS
Assess:


 
Bone marrow suppression:
ANC, platelets; during chronic phase, if ANC <1 × 10
9
/L and/or platelets <50 × 10
9
/L, stop until ANC >1.5 × 10
9
/L and platelets >75 × 10
9
/L; during accelerated phase/blast crisis, if ANC <0.5 × 10
9
/L and/or platelets <10 × 10
9
/L, determine whether cytopenia related to biopsy/aspirate; if not, reduce dose by 200 mg; if cytopenia continues, reduce dose by another 100 mg; if cytopenia continues for 4 wk, stop product until ANC ≥1 × 10
9
/L


 
Renal toxicity:
if bilirubin >3 × IULN, withhold imatinib until bilirubin levels return to <1.5 × IULN


 
Hepatotoxicity:
monitor LFTs, before treatment monthly; if liver transaminases >5 × IULN, withhold imatinib until transaminase levels return to <2.5 × IULN


 
Monitor CBC for first month, biweekly next month and periodically thereafter; neutropenia (2-3 wk) and thrombocytopenia (3-4 wk) and anemia may occur; may need dosage decrease or discontinuation

• 
Signs of fluid retention, edema: weigh, monitor lung sounds, assess for edema; some fluid retention is dose dependent

Perform/provide:

• 
Nutritious diet with iron, vit supplement, low fiber, few dairy products

• 
Storage at 77° F (25° C)

Evaluate:

• 
Therapeutic response: decrease in leukemic cells or size of tumor

Teach patient/family:

• 
To report adverse reactions immediately: shortness of breath, swelling of extremities, bleeding

• 
About reason for treatment, expected results

• 
That effect on male infertility is unknown

• 
Not to stop or change dose—to avoid hazardous activities until response is known, dizziness may occur

• 
To take with food and water; for those unable to swallow tabs, to mix in liquid (30 m for 100 mg) or 200 ml for 400 mg) after dissolved, stir and consume

• 
To avoid OTC products unless approved by prescriber


 
To notify prescriber if pregnancy is planned or suspected, pregnancy (D), do not breastfeed

Canada only   Side effects:
italics
= common;
bold
= life-threatening   
Nurse Alert

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