Read Mosby's 2014 Nursing Drug Reference Online
Authors: Linda Skidmore-Roth
Canada only Side effects:
italics
= common;
bold
= life-threatening
Nurse Alert
(e-tra′veer-een)
INTELENCE
Func. class.:
Antiretroviral
Chem. class.:
Nonnucleoside reverse transcriptase inhibitor (NNRTI)
Binds directly to reverse transcriptase, thus blocking the RNA- and DNA-dependent DNA polymerase action and causing a disruption of the enzyme’s catalytic site
In combination with other antiretroviral agents for HIV infection in treatment-experienced patients with evidence of HIV replication despite ongoing antiretroviral therapy
Breastfeeding, hypersensitivity
Precautions:
Pregnancy (B), children, geriatric patients, impaired hepatic function, antimicrobial resistance, hepatitis, hypercholesterolemia, hypertriglycerides, immune reconstitution syndrome
• Adult:
PO
200 mg bid after a meal, max 400 mg/day; not established for treatment-naive patients
Available forms:
Tabs 100, 200 mg
•
In combination with other antiretrovirals with food or after a meal
•
Tabs may be dispersed in water; once dispersed, stir well, give immediately, rinse glass, have patient drink to ensure all medication taken
CNS:
Headache, insomnia
, amnesia, anxiety, confusion, fatigue, nightmares, peripheral neuropathy,
seizures, stroke,
tremor
CV:
Atrial fibrillation,
hypertension, MI
EENT:
Blurred vision
GI:
Nausea, vomiting, diarrhea, anorexia
, abdominal pain, increased AST/ALT, constipation, flatulence, gastritis, GERD,
hematemesis, hepatitis,
hepatomegaly,
pancreatitis
GU:
Renal failure
HEMA:
Hemolytic anemia, neutropenia, thrombocytopenia, anemia
INTEG:
Rash
, erythema multiforme,
angioedema, Stevens-Johnson syndrome
MS:
Rhabdomyolysis
OTHER:
Diabetes mellitus, gynecomastia, hyperamylasemia, hypercholesterolemia, hyperglycemia, hyperlipidemia
RESP:
Dyspnea,
bronchospasm
99.9% plasma protein binding; metabolized by CYP3A4, 2C9, 2C19; half-life 21-61 hr; excreted in feces
•
Do not use concurrently with atazanavir, carBAMazepine, delavirdine, fosamprenavir, fosphenytoin, phenytoin, PHENobarbital, rifapentine, rifampin, tipranavir, rilpivirine
•
Altered effect of cycloSPORINE, tacrolimus, sirolimus
Increase:
myopathy, rhabdomyolysis—HMG-CoA reductase inhibitors
Increase:
etravirine levels—CYP3A4 inhibitors (fluconazole, itraconazole, ketoconazole, lopinavir, posaconazole, ritonavir, voriconazole)
Increase:
withdrawal symptoms—methadone
Increase:
levels of diazepam, rifampin, voriconazole, warfarin
Decrease:
levels of CYP3A4 inducers (amiodarone, atazanavir, clarithromycin, flecainide, fosamprenavir, lidocaine, mexiletine, propafenone, quiNIDine, sildenafil, tadalafil, vardenafil)
Decrease:
etravirine levels—darunavir, dexamethasone, disopyramide, efavirenz, nevirapine, ritonavir, saquinavir, tipranavir
Decrease:
etravirine—St. John’s wort
•
Symptoms of HIV
, possible infections; increased temp
Fatal hypersensitivity reactions:
fever, rash, nausea, vomiting, fatigue, cough, dyspnea, diarrhea, abdominal discomfort; treatment should be discontinued and not restarted
•
Blood dyscrasias
(anemia, granulocytopenia): bruising, fatigue, bleeding, poor healing
•
Renal failure:
BUN, serum uric acid, CCr before, during therapy; may be elevated throughout treatment
•
Hepatitis/pancreatitis:
hepatic studies before and during therapy: bilirubin, AST, ALT, amylase, alk phos, creatine phosphokinase, creatinine, monthly
•
HIV: monitor viral load, CD4 counts, plasma HIV RNA during treatment; watch for decreasing granulocytes, Hgb; if low, therapy may have to be discontinued and restarted after hematologic recovery; blood transfusions may be required; cholesterol/lipid profile
•
Storage in cool environment; protect from light
•
Therapeutic response: increased CD4 count, decreased viral load
•
That product is not a cure but will control symptoms; that patient is still infective, may pass AIDS virus to others
•
To notify prescriber of sore throat, swollen lymph nodes, malaise, fever; other infections may occur; to stop product and notify prescriber immediately if skin rash, fever, cough, SOB, GI symptoms occur; to advise all health care providers that allergic reaction has occurred with etravirine
•
That follow-up visits must be continued, since serious toxicity may occur; blood counts must be performed
•
To use contraception during treatment; that patient still able to transmit disease
•
About information on medication guide and warning card; discuss points on guide
•
That other products may be necessary to prevent other infections
•
To take medication after a meal
Canada only Side effects:
italics
= common;
bold
= life-threatening
Nurse Alert
(e-ve-ro′li-mus)
Afinitor, Afinitor Disperz, Zortress
Func. class.:
Antineoplastic—miscellaneous
Chem. class.:
Immunosuppressant, macrolide
Do not confuse:
everolimus
/sirolimus/tacrolimus/temsirolimus
Proliferation signal inhibitor that inhibits mammalian target of rapamycin (mTOR); this pathway is dysregulated in cancer
Renal cell cancer in those with failed treatment with sorafenib or SUNItinib kidney transplant rejection prophylaxis with cycloSPORINE, subependymal giant cell astrocytoma, progressive pancreatic neuroendocrine tumor (PNET) with unresectable locally advanced/metastatic disease, breast cancer hormone receptor positive/HER-2 negative, renal angiomyolipoma, tuberous sclerosis complex
Breastfeeding; hypersensitivity to this product, Rapamune, torisel, pregnancy (D)
Precautions:
Children, renal/hepatic disease; diabetes mellitus, hyperlipidemia, plural effusion
Black Box Warning:
lmmunosuppression, infection, renal artery thrombosis, renal impairment, renal vein thrombosis
• Adult:
PO
0.75 mg q12hr with cycloSPORINE in combination with basiliximab, corticosteroids, reduced doses of cycloSPORINE
• Adult:
PO
10 mg daily as long as clinically beneficial; with strong 3A4 inducers 10 mg daily then may increase by 5 mg increments to 20 mg daily
• Adult:
PO
10 mg daily, reduce dose to 5 mg daily if intolerable adverse reactions occur
• Adult/adolescent/Child:
4.5 mg/m
2
q day, then titrate to a target trough of 5-15 ng/ml
• Adult:
PO
(Child-Pugh A): Afinitor 7.5 mg/day; (Child-Pugh B) Afinitor: 5 mg/day; Zortress: 0.75 mg/day divided q12hr; (Child-Pugh C) Afinitor 2.5 mg/day
Available forms:
Tabs 0.25, 0.5, 0.75 (Zortess); 2.5, 5, 7.5, 10 mg (Afinitor)
•
Follow procedure for proper handling of antineoplastics
•
Swallow tabs whole with a full glass of water; do not chew, crush, or break
•
Afinitor:
take at same time of day; if unable to swallow, consistently with or without food, disperse in 30 ml of water
•
Zortress:
must take consistently with/without food, give at same time of day q12hr with cycloSPORINE
•
Store protected from light at room temp
•
Grade 1, asymptomatic with radiographic findings only: No dosage change
•
Grade 2, symptomatic but no interference with activities of daily living (ADL): Consider withholding therapy, resume Afinitor at a lower dosage when symptoms improve to ≤ grade 1; discontinue Afinitor if symptoms do not improve within 4 wk
•
Grade 3, symptomatic and interfering with ADL and oxygen therapy indicated: hold therapy. Consider resuming Afinitor at a lower dosage when symptoms improve to ≤ grade 1. Consider discontinuing Afinitor if grade 3 toxicity recurs
•
Grade 4, life-threatening and ventilator support indicated: discontinue therapy
•
Grade 1, minimum symptoms and normal diet: No dosage adjustment required
•
Grade 2, symptomatic but can eat and swallow modified diet: Hold therapy until symptoms improve to ≤ grade 1 and resume Afinitor at the same dosage. If grade 2 toxicity recurs, hold therapy and resume Afinitor at a lower dosage when symptoms improve to ≤ grade 1
•
Grade 3, symptomatic and unable to adequately eat or hydrate orally: Hold therapy. Resume Afinitor at a lower dosage when symptoms improve to ≤ grade 1
•
Grade 4, symptomatic and life-threatening: discontinue therapy
•
Grade 1:
No dosage adjustment required if toxicity is tolerable
•
Grade 2:
No dosage adjustment required if toxicity is tolerable. If toxicity is intolerable, hold therapy until symptoms improve to ≤ grade 1 and resume Afinitor at the same dosage. If grade 2 toxicity recurs, hold therapy and resume Afinitor at a lower dosage when symptoms improve to ≤ grade 1
•
Grade 3:
Hold therapy. Consider resuming Afinitor at a lower dosage when symptoms improve to ≤ grade 1. If grade 3 toxicity recurs, consider discontinuing therapy
•
Grade 4:
Discontinue Afinitor therapy
•
Grade 1 or 2:
No dose adjustment required
•
Grade 3:
Temporarily withhold therapy. Resume Afinitor at a lower dosage
•
Grade 4:
Discontinue Afinitor therapy
CNS:
Headache, insomnia, paresthesia
, chills, fever, seizure/personality changes/dizziness
CV:
Hypertension, CHF, peripheral edema
EENT:
Blurred vision, photophobia
GI:
Nausea, vomiting, diarrhea, constipation, stomatitis
GU:
Renal failure
HEMA:
Anemia, leukopenia, thrombocytopenia
INTEG:
Rash, acne
META:
Hyperglycemia, increased creatinine,
hyperlipemia
, hypophosphatemia, weight loss
RESP:
Pleural effusion,
dyspnea
, noninfectious pneumonitis, pulmonary embolism
Rapidly absorbed; peak 1-2 hr; protein binding 74%; extensively metabolized by CYP3A4 enzyme system; half-life 30 hr; reduced by high-fat meal; excreted in feces (80%), urine (5%)
Increase:
Everolimus effect—CYP3A4 inhibitors (strong, moderate), antifungals, calcium channel blockers, cimetidine, danazol, erythromycin, cycloSPORINE, HIV-protease inhibitors
Decrease:
blood levels of everolimus—carBAMazepine, PHENobarbital, phenytoin, rifamycin, rifapentine
Increase:
nephrotoxicity—immunosuppressants
Decrease:
effect of live vaccines
•
St. John’s wort: may decrease effect of everolimus
•
Alters bioavailability; use consistently with/without food; do not use with grapefruit juice
Increase:
bilirubin, calcium, cholesterol, glucose, potassium, lipids, phosphate, triglycerides, uric acid
Decrease:
calcium, glucose, potassium, magnesium, phosphate
•
Lipid profile: cholesterol, triglycerides, lipid-lowering agent may be needed; blood glucose
Black Box Warning:
Immunosuppression:
CBC with differential during treatment monthly; if leukocytes <3000/mm
3
or platelets <100,000/mm
3
, product should be discontinued or reduced; decreased hemoglobulin level may indicate bone marrow suppression
•
Hepatic/renal studies: AST, ALT, amylase, bilirubin, creatinine, phosphate, and for hepatotoxicity: dark urine, jaundice, itching, light-colored stools; product should be discontinued
Black Box Warning:
Infection:
bacterial fungal infections can occur and are more common with combination immunosuppression therapy
•
Renal artery/vein thrombosis (Zortress):
May result in graft loss within 30 days after transplantation
•
Obtain everolimus blood levels in kidney transplant, hepatic disease, CYP3A4 inducers, inhibitors
•
Therapeutic response
Black Box Warning:
To report fever, rash, severe diarrhea, chills, sore throat, fatigue; serious infections may occur; to report clay-colored stools, cramping (hepatotoxicity)
Black Box Warning:
To avoid crowds, persons with known infections to reduce risk for infection
•
Pregnancy:
to notify prescriber if pregnancy is planned or suspected, pregnancy (D)
•
To use contraception before, during, and 12 wk after product discontinued; to avoid breastfeeding
•
Not to use with grapefruit juice
•
To avoid live vaccines
•
That product may decrease male, female fertility
•
That drinking alcohol is not recommended
•
To take consistently with or without food
•
To report vision changes, weight gain, edema, shortness of breath