Mosby's 2014 Nursing Drug Reference (166 page)

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

etravirine (Rx)

(e-tra′veer-een)

INTELENCE

Func. class.:
Antiretroviral

Chem. class.:
Nonnucleoside reverse transcriptase inhibitor (NNRTI)

ACTION:

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

USES:

In combination with other antiretroviral agents for HIV infection in treatment-experienced patients with evidence of HIV replication despite ongoing antiretroviral therapy

CONTRAINDICATIONS:

Breastfeeding, hypersensitivity

Precautions:
Pregnancy (B), children, geriatric patients, impaired hepatic function, antimicrobial resistance, hepatitis, hypercholesterolemia, hypertriglycerides, immune reconstitution syndrome

DOSAGE AND ROUTES
Calculator

• Adult:
PO
200 mg bid after a meal, max 400 mg/day; not established for treatment-naive patients

Available forms:
Tabs 100, 200 mg

Administer:

• 
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

SIDE EFFECTS

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

PHARMACOKINETICS

99.9% plasma protein binding; metabolized by CYP3A4, 2C9, 2C19; half-life 21-61 hr; excreted in feces

INTERACTIONS

• 
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

Drug/Herb

Decrease:
etravirine—St. John’s wort

NURSING CONSIDERATIONS
Assess:

• 
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

Perform/provide:

• 
Storage in cool environment; protect from light

Evaluate:

• 
Therapeutic response: increased CD4 count, decreased viral load

Teach patient/family:

• 
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

everolimus (Rx)

(e-ve-ro′li-mus)

Afinitor, Afinitor Disperz, Zortress

Func. class.:
Antineoplastic—miscellaneous

Chem. class.:
Immunosuppressant, macrolide

Do not confuse:
everolimus
/sirolimus/tacrolimus/temsirolimus

ACTION:

Proliferation signal inhibitor that inhibits mammalian target of rapamycin (mTOR); this pathway is dysregulated in cancer

USES:

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

CONTRAINDICATIONS:

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

DOSAGE AND ROUTES
Calculator
Kidney transplant rejection prophylaxis (Zortress)

• Adult:
PO
0.75 mg q12hr with cycloSPORINE in combination with basiliximab, corticosteroids, reduced doses of cycloSPORINE

Advanced renal cancer (Afinitor)

• 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

Progressive neuroendocrine tumor (PNET) (Afinitor only)

• Adult:
PO
10 mg daily, reduce dose to 5 mg daily if intolerable adverse reactions occur

Subependymal giant-cell astrocytoma (SEGA) (Afinitor only)

• Adult/adolescent/Child:
4.5 mg/m
2
q day, then titrate to a target trough of 5-15 ng/ml

Hepatic dose

• 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)

Administer:

• 
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

Afinitor adjustments for toxicity
Noninfectious pneumonitis

• 
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

Stomatitis

• 
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

Other nonhematologic toxicity (excluding metabolic events)

• 
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

Metabolic events (hyperglycemia, dyslipidemia)

• 
Grade 1 or 2:
No dose adjustment required

• 
Grade 3:
Temporarily withhold therapy. Resume Afinitor at a lower dosage

• 
Grade 4:
Discontinue Afinitor therapy

SIDE EFFECTS

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

PHARMACOKINETICS

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%)

INTERACTIONS

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

Drug/Herb

• 
St. John’s wort: may decrease effect of everolimus

Drug/Food

• 
Alters bioavailability; use consistently with/without food; do not use with grapefruit juice

Drug/Lab Test

Increase:
bilirubin, calcium, cholesterol, glucose, potassium, lipids, phosphate, triglycerides, uric acid

Decrease:
calcium, glucose, potassium, magnesium, phosphate

NURSING CONSIDERATIONS
Assess:

• 
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

Evaluate:

• 
Therapeutic response

Teach patient/family:

 

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

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