Mosby's 2014 Nursing Drug Reference (369 page)

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

sirolimus (Rx)

(seer-oh-lie′mus)

Rapamune

Func. class.:
Immunosuppressant

Chem. class.:
Macrolide

ACTION:

Produces immunosuppression by inhibiting T-lymphocyte activation and proliferation

USES:

Organ transplants to prevent rejection; recommended use is with cycloSPORINE and corticosteroids

CONTRAINDICATIONS:

Breastfeeding, hypersensitivity to this product, components of product

Precautions:
Pregnancy (C), children <13 yr, severe cardiac/renal/hepatic disease; diabetes mellitus, hyperkalemia, hyperuricemia, hypertension, interstitial lung disease, hyperlipidemia

 

Black Box Warning:

Lymphomas, infection, other malignancies

DOSAGE AND ROUTES
Calculator

• Adult/adolescent ≥40 kg:
PO
2 mg/day with 6 mg loading dose

• Child >13 yr weighing <40 kg (88 lb):
PO
1 mg/m
2
/day, 3 mg/m
2
loading dose

Hepatic dose

• Adult/child ≥13 yr/<40 kg:
PO
reduce by 33% for maintenance dose (mild to moderate hepatic impairment); reduce by 50% for maintenance dose (severe hepatic impairment)

Available forms:
Oral sol 1 mg/ml; tabs 0.5 mg, 1 mg, 2 mg

Administer:

• 
Prophylaxis for
Pneumocystis jiroveci
pneumonia for 1 yr after transplantation; prophylaxis for CMV is recommended for 90 days after transplantation in those at increased risk for CMV

• 
All medications PO if possible, avoid IM inj; bleeding may occur

• 
For 3 days before transplant surgery; patients should be placed in protective isolation; give at same time of day, give 4 hr after cycloSPORINE oral sol or caps; do not give with grapefruit juice

• 
Use amber oral dose syringe and withdraw amount of oral sol needed from bottle, empty correct dose into plastic/glass container holding 60 ml of water/orange juice, stir vigorously and have patient drink at once, refill container with additional 120 ml water/orange juice, stir vigorously and have patient drink at once; if using a pouch, squeeze entire contents into container, follow above directions

• 
Store protected from light, refrigerate; stable for 30 days after opening (sol)

• 
Do not crush, chew; store tabs at room temp

SIDE EFFECTS

CNS:
Tremors, headache, insomnia, paresthesia
, chills, fever

CV:
Hypertension,
atrial fibrillation, CHF, hypotension, palpitation, tachycardia
, peripheral edema,
thrombosis

EENT:
Blurred vision, photophobia

GI:
Nausea, vomiting, diarrhea, constipation,
hepatotoxicity

GU:
UTIs,
albuminuria, hematuria, proteinuria, renal failure, nephrotic syndrome,
increased creatinine

HEMA:
Anemia, leukopenia, thrombocytopenia, purpura, pancytopenia

INTEG:
Rash, acne
, photosensitivity

META:
Hyperglycemia, increased creatinine, edema, hypercholesterolemia,
hyperlipemia
, hypophosphatemia, weight gain, hypo/hyperkalemia, hyperuricemia, hypomagnesemia, hypertriglyceridemia

MS:
Arthralgia

RESP:
Pleural effusion, atelectasis,
dyspnea
, pneumonitis, pulmonary embolism/fibrosis

SYST:
Lymphoma, exfoliative dermatitis

PHARMACOKINETICS

Rapidly absorbed; peak 1 hr single dose, 2 hr multiple dosing; protein binding 92%; extensively metabolized by CYP3A4 enzyme system, half-life 57-63 hr

INTERACTIONS

 
Increase:
angioedema—ACE inhibitors, angiotensin-II–receptor antagonists, cephalosporins, iodine-containing radiopaque contrast media, neuromuscular blockers, NSAIDs, penicillins, salicylates, thrombolytics

Increase:
blood levels—antifungals, calcium channel blockers, cimetidine, danazol, erythromycin, cycloSPORINE, metoclopramide, bromocriptine, HIV-protease inhibitors

Decrease:
blood levels—carBAMazepine, PHENobarbital, phenytoin, rifamycin, rifapentine

Decrease:
effect of vaccines

Drug/Herb

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

Drug/Food

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

Drug/Lab Test

Increase:
LFTs, alk phos, lipids, triglycerides, total cholesterol, BUN, creatinine, LDH, phosphate

Decrease:
platelets, sodium

Increase or Decrease:
magnesium, glucose, calcium

NURSING CONSIDERATIONS
Assess:

• 
Blood levels in patients who may have altered metabolism, trough level ≥15 ng/ml are associated with increased adverse reactions; monitor trough concentrations in all patients

• 
Creatinine/BUN, CBC, serum potassium

• 
Lipid profile:
cholesterol, triglycerides; lipid-lowering agent may be needed

 

Black Box Warning:

Infection and development of lymphoma; only those experienced in immunosuppressant therapy and organ transplantation should use this product; use only in renal transplant

• 
High risk:
those with Baniff grade 3 acute rejection or vascular rejection before cycloSPORINE withdrawal, dialysis dependent, creatinine >4.5 mg/dl, African American patient, re-transplants, multiorgan transplant, high panel of reactive antibodies

• 
Pulmonary fibrosis, pulmonary effusion, pneumonitis:
dyspnea, cough, hypoxia; some fatal cases have occurred

• 
Wound dehiscence and anastomotic disruption:
wound, vascular, airway, ureteral, biliary, inhibition of growth factors; do not combine with corticosteroids

• 
Anaphylaxis, angioedema, exfoliative dermatitis:
more common when given with ACE inhibitors; do not use if a hypersensitivity reaction occurs

 
Bone marrow suppression:
Hgb, WBC, platelets during treatment each mo; if leukocytes
<
3000/mm
3
or platelets
<
100,000/mm
3
, product should be discontinued or reduced; decreased hemoglobin level

 
Hepatotoxicity:
alk phos, AST, ALT, amylase, bilirubin, dark urine, jaundice, itching, light-colored stools; product should be discontinued

Evaluate:

• 
Therapeutic response: absence of graft rejection; immunosuppression with autoimmune disorders

Teach patient/family:

 
To report fever, rash, severe diarrhea, chills, sore throat, fatigue; serious infections may occur; clay-colored stools, cramping
(hepatotoxicity)

• 
To avoid crowds, persons with known infections to reduce risk for infection

• 
To use contraception before, during, for 12 wk after product discontinued; to avoid breastfeeding

• 
To use sunscreen, protective clothing to prevent burns, skin cancer

• 
Not to use with grapefruit juice

• 
To avoid vaccines

• 
That lifelong use will be required to prevent rejection

• 
That continuing follow-up exams and blood work will be required

• 
Not to get on skin

• 
How to use product

• 
To take with or without regard to food, at same time, consistently

• 
Take 4 hr after cycloSPORINE

BOOK: Mosby's 2014 Nursing Drug Reference
12.61Mb size Format: txt, pdf, ePub
ads

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