Mosby's 2014 Nursing Drug Reference (378 page)

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

suprofen ophthalmic

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

tacrolimus (Rx) (PO, IV)

(tak-row′lim-us)

Prograf

tacrolimus (topical) (Rx)

Protopic

Func. class.:
Immunosuppressant

Chem. class.:
Macrolide

ACTION:

Produces immunosuppression by inhibiting T-lymphocytes

USES:

Organ transplants to prevent rejection;
topical:
atopic dermatitis

Unlabeled uses:
Severe recalcitrant psoriasis, contact dermatitis, GVHD prophylaxis/disease, pancreas/heart/kidney/liver/lung/small bowel transplant rejection, uveitis, ulcerative colitis, nephrotic syndrome, lichen sclerosus

CONTRAINDICATIONS:

Children <2 yr (topical); hypersensitivity to this product or to some kinds of castor oil (IV); long-term use (topical)

Precautions:
Pregnancy (C), breastfeeding, severe renal/hepatic disease; diabetes mellitus, hyperkalemia, hyperuricemia, hypertension, acute bronchospasm, African American patients, heart failure, seizures, QT prolongation

 

Black Box Warning:

Children <12, lymphomas, infection, neoplastic disease, neonates, infants, requires a specialized setting, requires an experienced clinician

DOSAGE AND ROUTES
Calculator
Kidney transplant rejection prophylaxis

• Adult:
IV
0.03-0.05 mg/kg/day as
CONT INF,
give no sooner than 6 hr after transplantation

Liver transplant rejection prophylaxis

• Adult:
PO
0.10-0.15 mg/kg/day in 2 divided doses q12hr, give no sooner than 6 hr after transplantation;
IV
0.03-0.05 mg/kg/day as
CONT INF,
give no sooner than 6 hr after transplantation

Heart transplant rejection prophylaxis

• Adult:
PO
0.075 mg/kg/day in 2 divided doses q12hr, give no sooner than 6 hr after transplantation;
IV
0.01 mg/kg/day as
CONT INF,
give no sooner than 6 hr after transplantation

Atopic dermatitis

• Adult:
TOP
use 0.03% or 0.1% ointment, apply bid × 7 days after clearing of signs

• Child ≥ 2-15 yr:
TOP
0.03% ointment, apply bid × 7 days after clearing of signs

Graft-versus-host disease (orphan drug)

• Adult and adolescent:
IV
0.1 mg/kg/day in 2 divided doses given with other immunosuppressants or
PO
0.3 mg/kg/day in 2 divided doses

• Child:
CONT IV INF
0.1 mg/kg/day

Graft-versus-host prophylaxis (unlabeled)

• Adult:
CONT IV INF
0.03 mg/kg/day starting 1-2 days before bone marrow transplant;
PO
0.12 mg/kg/day in 2 divided doses

• Adolescent and child:
PO
0.12 mg/kg/day in 2 divided doses

Heart transplant rejection (unlabeled)

• Adult:
IV
0.05 mg/kg/day or
PO
0.2-0.3 mg/kg/day in 2 divided doses; adjust to maintain whole blood conc 7-15 ng/ml

Lung transplant rejection (unlabeled)

• Adult:
PO
0.15 mg/kg/day, maintain 12-hr trough, whole blood conc 1-1.5 ng/ml

Small bowel transplant rejection (unlabeled)

• Adult:
IV
0.1-0.15 mg/kg/day then
PO
0.3 mg/kg/day in divided doses

Contact dermatitis (unlabeled)

• Adult:
TOP
0.1% ointment, apply bid × 8 wk

Available forms:
Inj 5 mg/ml; caps 0.5, 1, 5 mg; ointment 0.03%, 0.1%

Administer:
PO route

• 
Give on empty stomach, food decreases absorption

• 
For several days before transplant surgery, patients should be placed in protective isolation

Topical route

• 
Apply thin layers to affected skin only, rub in gently

• 
Do not use occlusive dressings

• 
Use on small area of skin

• 
Topical ointment has risk of developing cancer, use only when other options have failed

Continuous IV INF route

• 
After diluting in 0.9% NaCl or D
5
W to 0.004 to 0.02 mg/ml as continuous inf over 24 hr

Y-site compatibilities:
Alemtuzumab, alfentanil, amifostine, amikacin, aminophylline, amiodarone, amphotericin B colloidal, amphotericin B liposome, anidulafungin, argatroban, atracurium, aztreonam, benztropine, bivalirudin, bleomycin, bumetanide, buprenorphine, busulfan, butorphanol, calcium acetate/chloride/gluconate, CARBOplatin, carmustine, caspofungin, ceFAZolin, cefoperazone, cefotaxime, cefoTEtan, cefOXitin, cefTAZidime, ceftizoxime, cefTRIAXone, cefuroxime, chloramphenicol, chlorproMAZINE, cimetidine, ciprofloxacin, cisatracurium, CISplatin, clindamycin, cyclophosphamide, cycloSPORINE, cytarabine, DACTINomycin, DAPTOmycin, dexamethasone, dexmedetomidine, dexrazoxane, digoxin, diltiazem, diphenhydrAMINE, DOBUTamine, DOCEtaxel, dolasetron, DOPamine, doripenem, doxacurium, DOXOrubicin hydrochloride, doxycycline, droperidol, enalaprilat, ePHEDrine, EPINEPHrine, epirubicin, ertapenem, erythromycin, esmolol, etoposide, etoposide phosphate, famotidine, fenoldopam, fentaNYL, fluconazole, fludarabine, foscarnet, fosphenytoin, gemcitabine, gentamicin, glycopyrrolate, granisetron, haloperidol, heparin, hydrALAZINE, hydrocortisone, HYDROmorphone, IDArubicin, ifosfamide, imipenem/cilastatin, inamrinone, insulin, isoproterenol, ketorolac, labetalol, leucovorin, levofloxacin, levorphanol, lidocaine, linezolid, LORazepam, magnesium sulfate, mannitol, mechlorethamine, meperidine, meropenem, mesna, metaraminol, methotrexate, methyldopate, methylPREDNISolone, metoclopramide, metoprolol, metroNIDAZOLE, micafungin, midazolam, milrinone, mitoMYcin, mitoXANtrone, mivacurium, morphine, multivitamins, nafcillin, nalbuphine, naloxone, nesiritide, niCARdipine, nitroglycerin, nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, PACLitaxel, palonosetron, pancuronium, PEMEtrexed, penicillin G, pentamidine, pentazocine, perphenazine, phentolamine, phenylephrine, piperacillin/tazobactam, potassium chloride/phosphates, procainamide, prochlorper
azine, promethazine, propranolol, quinapristin/dalfopristin, ranitidine, remifentanil, rocuronium, sodium acetate/bicarbonate/phosphates, streptozocin, succinylcholine, SUFentanil, teniposide, theophylline, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, tolazoline, trimethobenzamide, vancomycin, vasopressin, vecuronium, verapamil, vinCRIStine, vinorelbine, voriconazole, zidovudine, zoledronic acid

SIDE EFFECTS

CNS:
Tremors, headache
, insomnia, paresthesia, chills, fever,
seizures,
posterior reversible encephalopathy syndrome, BK-virus–associated nephropathy

CV:
Hypertension, myocardial hypertrophy,
prolonged QTc,
cardiomyopathy

EENT:
Blurred vision, photophobia

GI:
Nausea, vomiting, diarrhea, constipation,
GI bleeding

GU:
UTIs,
albuminuria, hematuria, proteinuria, renal failure, hemolytic uremic syndrome

HEMA:
Anemia, leukocytosis, thrombocytopenia, purpura

INTEG:
Rash, flushing, itching, alopecia

META:
Hirsutism, hyperglycemia, hyperuricemia, hypo/hyperkalemia, hypomagnesemia

MS:
Back pain, muscle spasms

RESP:
Pleural effusion, atelectasis, dyspnea, interstitial lung disease

SYST:
Anaphylaxis,
infection, malignancy

PHARMACOKINETICS

PO:
Extensively metabolized, half-life 10 hr, 75% protein binding

INTERACTIONS

 
Increase:
QT prolongation—class IA/III antidysrhythmics, some phenothiazines, β agonists, local anesthetics, tricyclics, haloperidol, chloroquine, droperidol, pentamidine; CYP3A4 inhibitors (amiodarone, clarithromycin, erythromycin, telithromycin, troleandomycin), arsenic trioxide, levomethadyl; CYP3A4 substrates (methadone, pimozide, QUEtia-pine, quiNIDine, risperiDONE, ziprasidone); do not use together

 
Increase:
toxicity—aminoglycosides, CISplatin, cycloSPORINE

Increase:
blood levels—antifungals, calcium channel blockers, cimetidine, danazol, mycophenolate, mofetil

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

Decrease:
effect of live-virus vaccines

Drug/Herb

Decrease:
immunosuppression—astragalus, echinacea, melatonin

Decrease:
effect—ginseng, St. John’s wort

Drug/Food

Increase:
effect—grapefruit juice

Decreased absorption:
food

Drug/Lab Test

Increase:
glucose, BUN, creatinine

Increase or decrease:
LFTs, potassium

Decrease:
magnesium, Hgb, platelets

NURSING CONSIDERATIONS
Assess:

• 
Blood studies: Hgb, WBC, platelets 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 studies: alk phos, AST, ALT, amylase, bilirubin; for hepatotoxicity: dark urine, jaundice, itching, light-colored stools; product should be discontinued

• 
Serum creatinine/BUN, serum electrolytes, lipid profile, serum tacrolimus conc

 
Anaphylaxis:
rash, pruritus, wheezing, laryngeal edema; stop infusion, initiate emergency procedures

• 
QT prolongation:
ECG, ejection fraction; assess for chest pain, palpitations, dyspnea

Evaluate:

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

Teach patient/family:
PO route

• 
To report fever, rash, severe diarrhea, chills, sore throat, fatigue; that serious infections may occur; to report clay-colored stools, cramping
(hepatotoxicity), nephrotoxicity,
signs of diabetes mellitus

• 
To avoid crowds, persons with known infections to reduce risk for infection; to avoid eating raw shellfish

• 
To avoid exposure to natural or artificial sunlight

• 
Not to breastfeed while taking product

• 
That repeated lab tests will be needed during treatment

• 
To avoid vaccines

• 
Not to use with alcohol, grapefruit

• 
To report if pregnancy is planned or suspected

 

Black Box Warning:

To report symptoms of lymphoma

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