Names and pronunciation
(floo-kon′a-zole) Canesoral , Diflucan, Diflucan One
Source page 568
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Individual generic drug information
Extracted information for fluconazole only.
(floo-kon′a-zole) Canesoral , Diflucan, Diflucan One
Source page 568
Func. class.: Antifungal, systemic; azole
Source page 568
Do not confuse: Diflucan/Diprivan
Source page 568
ACTION: Inhibits fungal sterols, causes direct damage to fungal membrane phospholipids
Source page 568
USES: Oropharyngeal candidiasis, chronic mucocutaneous candidiasis; sys- temic, vaginal, urinary candidiasis; cryp- tococcal meningitis; prevention of candidiasis in bone marrow transplant in those who receive chemotherapy and/or radiation therapy; cystitis, fungal prophy- laxis, peritonitis, pneumonia, pyelone phritis
Source page 568
Unlabeled uses: Prophylaxis, systemic candidiasis in very-low-birthweight pre- mature infants, blastomycosis, chemo- therapy-induced neutropenia, coccidi- oidomycosis cryptococcosis prophylaxis, endocarditis, endophthalmitis, histo- plasmosis, infectious arthritis, myocar- ditis, osteomyelitis, pericarditis
Source page 568
Extracted information for fluconazole only.
CONTRAINDICATIONS: Hyper- sensitivity to this product or azoles, pregnancy Precautions: Breastfeeding, renal/ hepatic disease, torsades de pointes
Source page 568
SIDE EFFECTS CNS: Headache, seizures CV: QT prolongation, torsades de pointes GI: Nausea, vomiting, diarrhea, cramp- ing, flatus, increased AST, ALT, hepatotox- icity, abdominal pain, cholestasis HEMA: Agranulocytosis, eosinophilia, leukopenia, neutropenia, thrombocytope- nia INTEG: Stevens-Johnson syndrome, angioedema, anaphylaxis, exfoliative der- matitis, toxic epidermal necrolysis
Source page 570
INTERACTIONS Increase: hypoglycemia—oral sulfonyl- ureas (glipiZIDE) Increase: anticoagulation—warfarin Increase: plasma concentrations/toxic- ity—cycloSPORINE, phenytoin, theophyl- line, rifabutin, tacrolimus, sirolimus, zidovudine, zolpidem Increase: myopathy, rhabdomyolysis risk—HMG-CoA reductase inhibitors: lov- astatin, simvastatin Increase: effect of zidovudine, metha- done, SUFentanil, alfentanil, buprenor- phine, saquinavir, fentaNYL, ergots Decrease: effect of calcium channel blockers Decrease: fluconazole effect—proton pump inhibitors Drug/Lab Test Increase: alk phos, LFTs Decrease: WBC, platelets
Source page 570
Extracted information for fluconazole only.
DOSAGE AND ROUTES Vulvovaginal candidiasis • Adult: PO 150 mg as a single dose; prevention of recurrence (unlabeled) 150 mg/day × 3 days, then weekly × 6 mo Serious fungal infections • Adult: PO/IV Most serious infections loading dose 800 mg, then continue at 400-800 mg daily for 4-6 wk • Child: PO/IV 6-12 mg/kg/day • Neonates <14 days, 30-36 wk gesta- tion: PO/IV same as child except q48hr Oropharyngeal candidiasis • Adult: PO/IV 200 mg initially, then 100 mg/day for ≥2 wk • Child >14 days: PO/IV 6 mg/kg ini- tially, then 3 mg/kg/day for ≥2 wk • Neonate <14 days, 30-36 wk gesta- tion: PO/IV 6 mg/kg/dose once, then 3 mg/kg/dose once daily Esophageal candidiasis • Adult: PO/IV 200 mg on 1st day, then 100 mg daily × ≥3 wk and for ≥2 wk after resolution of symptoms • Child >14 days: PO/IV 6 mg/kg on 1st day, then 3 mg/kg × ≥3 wk and for ≥2 wk after resolution of symptoms • Neonate: PO/IV 6 mg/kg q 24-48hr Cryptococcal meningitis • Adult: PO/IV 400 mg on 1st day, then 200 mg/day × 10-12 wk after CSF culture negative, suppressive therapy 200 mg/day • Child/infant/neonate ≥14 days: PO/IV 12 mg/kg on 1st day, then 6-12 mg/kg daily × 10-12 wk after CSF culture nega- tive, max 600 mg/day, suppressive ther- apy 6 mg/kg/day • Neonate 0-14 days: PO/IV 12 mg/kg on 1st day, then 6-12 mg/kg q72hr × 10-12 wk after CSF culture negative Prevention of candidiasis in bone marrow transplant • Adult: PO/IV 400 mg/day, those an- ticipated to have neutrophils <500/ mm3, start several days before antici- pated onset of neutropenia and con- tinue for 7 days after rise of neutrophils >1000/mm3 • Child >14 days: PO/IV 10-12 mg/kg/ day, max 600 mg/day Renal disease • Adult: PO/IV CCr ≤50 mL/min, after loading dose, give 50% of usual dose; hemodialysis give 100% of usual dose after dialysis treatment, give dose as per CCr on non-dialysis days
Source pages 568, 569
Available forms: Tabs 50, 100, 150, 200 mg; inj 2 mg/mL; powder for oral susp 10 mg/mL, 40 mg/mL
Source page 569
Administer: PO route • Shake oral susp before each use, use within 2 wk Intermittent IV INFUSION route • After diluting according to package di- rections, run at ≤200 mg/hr; do not use plastic containers in connections; check for bag leaks • Use infusion pump; check for extrava- sation and necrosis q2hr • Do not use if cloudy or precipitated • Do not admix; do not refrigerate • Store protected from moisture and light; diluted sol stable 24 hr; do not freeze Y-site compatibilities: Acyclovir, aldes- leukin, alfentanil, allopurinol, amifos- tine, amikacin, aminocaproic acid, aminophylline, amiodarone, anidulafun- gin, ascorbic acid injection, atenolol, atracurium, atropine, azaTHIOprine, az- treonam, benztropine, bivalirudin, bleo- mycin, bumetanide, buprenorphine, butorphanol, calcium chloride, CARBO- platin, caspofungin, ceFAZolin, cefepime, cefmetazole, cefonicid, cefoTEtan, cefOXitin, cefpirome, cefTAZidime, cefti- zoxime, ceftobiprole, cephalothin, cep- hapirin, chlorproMAZINE, cimetidine, cisatracurium, CISplatin, codeine, cya- nocobalamin, cyclophosphamide, cyclo- SPORINE, cytarabine, DACTINomycin, DAPTOmycin, dexamethasone, diltiazem, dimenhyDRINATE, diphenhydrAMINE, F DOBUTamine, DOCEtaxel, DOPamine, doripenem, doxacurium, DOXOrubicin, DOXOrubicin liposomal, doxycycline, droperidol, drotrecogin alfa, enalaprilat, ePHEDrine, EPINEPHrine, epirubicin, epoetin alfa, eptifibatide, ertapenem, erythromycin, esmolol, etoposide, fa- motidine, fenoldopam, fentaNYL, filgras- tim, fludarabine, fluorouracil, folic acid, foscarnet, gallium, ganciclovir, gatifloxacin, gemcitabine, gentamicin, glycopyrrolate, granisetron, heparin, hydrocortisone, HYDROmorphone, IDA- rubicin, ifosfamide, IV immune globulin, inamrinone, indomethacin, insulin (regular), irinotecan, isoproterenol, ke- torolac, labetalol, lansoprazole, leucovo- rin, levofloxacin, lidocaine, linezolid, LORazepam, LR, magnesium sulfate, mannitol, mechlorethamine, melphalan, meperidine, meropenem, metaraminol, methicillin, methotrexate, methoxamine, methyldopate, methylPREDNISolone, metoclopramide, metoprolol, metroNI- DAZOLE, mezlocillin, miconazole, mid- azolam, milrinone, minocycline, mito- XANtrone, morphine, moxalactam, mul- tiple vitamins injection, mycophenolate, nafcillin, nalbuphine, naloxone, nesirit- ide, nitroglycerin, nitroprusside, norepi- nephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, PACLitax- el, palonosetron, pamidronate, pan- curonium, papaverine, PEMEtrexed, penicillin G potassium/sodium, pentazo- cine, PENTobarbital, PHENobarbital, phenylephrine, phenytoin, phytonadione, piperacillin-tazobactam, polymyxin B, potassium chloride, procainamide, pro- chlorperazine, promethazine, propofol, propranolol, protamine, pyridoxine, quiNIDine, quinupristin-dalfopristin, ra- nitidine, remifentanil, Ringer’s, rito- drine, riTUXimab, rocuronium, sargramostim, sodium acetate/bicarbon- ate, succinylcholine, SUFentanil, tacroli- mus, temocillin, teniposide, theophylline, thiotepa, ticarcillin-clavulanate, tigecy- cline, tirofiban, TNA, tobramycin, tolazo- line, TPN, trastuzumab, trimetaphan, urokinase, vancomycin, vasopressin, ve- curonium, verapamil, vinCRIStine, vinorelbine, voriconazole, zidovudine, zoledronic acid
Source pages 569, 570
Extracted information for fluconazole only.
Assess: • Infection: clearing of CSF and other culture during treatment, obtain C&S baseline and throughout treatment, product may be started as soon as cul- ture is taken • QT prolongation: avoid with other products that cause QT prolongation • Hepatotoxicity: monitor for increasing AST, ALT, baseline and periodically alk phos, bilirubin; for renal status: BUN, creatinine • Skin symptoms: color, lesions, inj-site reactions; if lesions progress, stop prod- uct; monitor rash, usually appears after 2nd wk of treatment and disappears in 2 wk if continuing product • Pregnancy/breastfeeding: birth de- fects may occur if used in 1st trimester; do not use in pregnancy, breastfeeding
Source page 570
Evaluate: • Therapeutic response: decreasing oral candidiasis, fever, malaise, rash; negative C&S for infection organism
Source page 570
CLINICAL CONSIDERATIONS
Source page 570
Patient and caregiver information: • That long-term therapy may be needed to clear infection, not to add new medica- tions, herbs without prescriber approval • That medication may be taken with food to reduce GI effects • To notify prescriber of nausea, vomiting, diarrhea, jaundice, anorexia, clay-colored stools, dark urine, skin rash, abdominal pain, fever, bruising, bleeding HIGH ALERT
Source page 570
Extracted information for fluconazole only.
PHARMACOKINETICS Peak 1-2 hr, bioavailability (PO) >90%, widely distributed (peritoneum, CSF), excreted in breast milk, excreted unchanged in urine 80%, metabolized by CYP3A enzyme system at dose >200 mg/ day, half-life 30 hr (adult); child 19-25 hr (PO); premature neonates (46-74 hr)
Source page 570
Filter the extracted dose blocks for this individual drug.
Vulvovaginal candidiasis
• Adult: PO 150 mg as a single dose; prevention of recurrence (unlabeled) 150 mg/day × 3 days, then weekly × 6 mo Serious fungal infections
Candidate age grouping · source pages 568, 569
Vulvovaginal candidiasis
• Adult: PO/IV Most serious infections loading dose 800 mg, then continue at 400-800 mg daily for 4-6 wk
Candidate age grouping · source pages 568, 569
Vulvovaginal candidiasis
• Adult: PO/IV 200 mg initially, then 100 mg/day for ≥2 wk
Candidate age grouping · source pages 568, 569
Vulvovaginal candidiasis
• Adult: PO/IV 200 mg on 1st day, then 100 mg daily × ≥3 wk and for ≥2 wk after resolution of symptoms
Candidate age grouping · source pages 568, 569
Vulvovaginal candidiasis
• Adult: PO/IV 400 mg on 1st day, then 200 mg/day × 10-12 wk after CSF culture negative, suppressive therapy 200 mg/day
Candidate age grouping · source pages 568, 569
Vulvovaginal candidiasis
• Adult: PO/IV 400 mg/day, those an- ticipated to have neutrophils <500/ mm3, start several days before antici- pated onset of neutropenia and con- tinue for 7 days after rise of neutrophils >1000/mm3
Candidate age grouping · source pages 568, 569
Vulvovaginal candidiasis
• Adult: PO/IV CCr ≤50 mL/min, after loading dose, give 50% of usual dose; hemodialysis give 100% of usual dose after dialysis treatment, give dose as per CCr on non-dialysis days
Candidate age grouping · source pages 568, 569