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Vykoura
leucovorin
Adult Dosing .
Dosage forms: INJ
leucovorin rescue, high-dose methotrexate
- [normal methotrexate elimination]
- Dose: 15 mg IM/IV q6h x10 doses; Start: 24h after methotrexate start; Info: use this regimen if methotrexate level approximately 10 micromolar at 24h, 1 micromolar at 48h, and <0.2 micromolar at 72h after methotrexate start; incr. to 14 doses with subsequent cycles if abnormal methotrexate elimination or renal impairment; use in combo with hydration and urinary alkalinization
- [delayed late methotrexate elimination]
- Dose: 15 mg IM/IV q6h; Info: continue until methotrexate level <0.05 micromolar; use this regimen if methotrexate level >0.2 micromolar at 72h and >0.05 micromolar at 96h after methotrexate start; use in combo with hydration and urinary alkalinization
- [delayed early methotrexate elimination and/or acute renal injury]
- Dose: 150 mg IM/IV q3h until methotrexate level <1 micromolar, then 15 mg IM/IV q3h; Info: continue until methotrexate level <0.05 micromolar; use this regimen if methotrexate level >50 micromolar at 24h or >5 micromolar at 48h OR if SCr incr. 100% from baseline at 24h after methotrexate start; use in combo with hydration and urinary alkalinization
leucovorin rescue, impaired methotrexate elimination or overdose
- [10 mg/m^2/dose IM/IV q6h]
- Start: ASAP after overdose or within 24h if impaired methotrexate elimination; Info: continue until methotrexate level <0.01 micromolar; incr. dose to 100 mg/m^2/dose IV q3h if SCr incr. 50% from baseline at 24h OR if methotrexate level >5 micromolar at 24h or >0.9 micromolar at 48h; use in combo with hydration and urinary alkalinization
megaloblastic anemia, folate deficiency-associated
- [up to 1 mg IV qd]
colorectal CA
- [combo with fluorouracil 370 mg/m^2/day]
- Dose: 200 mg/m^2/dose IV x1 on days 1-5 of 28-day cycle; Info: give x2 cycles, then continue 28-day cycles or extend to 35-day cycles; dosing protocols may vary; see pkg insert for 5-FU dose adjustments based on toxicity
- [combo with fluorouracil 425 mg/m^2/day]
- Dose: 20 mg/m^2/dose IV x1 on days 1-5 of 28-day cycle; Info: give x2 cycles, then continue 28-day cycles or extend to 35-day cycles; dosing protocols may vary; see pkg insert for 5-FU dose adjustments based on toxicity
renal dosing
- [not defined]
- renal impairment: not defined
- HD/PD: not defined
hepatic dosing
- [not defined]
Peds Dosing .
- Dosage forms: INJ
leucovorin rescue, high-dose methotrexate
- [normal methotrexate elimination]
- Dose: 15 mg IM/IV q6h x10 doses; Start: 24h after methotrexate start; Info: use this regimen if methotrexate level approximately 10 micromolar at 24h, 1 micromolar at 48h, and <0.2 micromolar at 72h after methotrexate start; incr. to 14 doses with subsequent cycles if abnormal methotrexate elimination or renal impairment; use in combo with hydration and urinary alkalinization
- [delayed late methotrexate elimination]
- Dose: 15 mg IM/IV q6h; Info: continue until methotrexate level <0.05 micromolar; use this regimen if methotrexate level >0.2 micromolar at 72h and >0.05 micromolar at 96h after methotrexate start; use in combo with hydration and urinary alkalinization
- [delayed early methotrexate elimination and/or acute renal injury]
- Dose: 150 mg IM/IV q3h until methotrexate level <1 micromolar, then 15 mg IM/IV q3h; Info: continue until methotrexate level <0.05 micromolar; use this regimen if methotrexate level >50 micromolar at 24h or >5 micromolar at 48h OR if SCr incr. 100% from baseline at 24h after methotrexate start; use in combo with hydration and urinary alkalinization
leucovorin rescue, impaired methotrexate elimination or overdose
- [10 mg/m^2/dose IM/IV q6h]
- Start: ASAP after overdose or within 24h if impaired methotrexate elimination; Info: continue until methotrexate level <0.01 micromolar; incr. dose to 100 mg/m^2/dose IV q3h if SCr incr. 50% from baseline at 24h OR if methotrexate level >5 micromolar at 24h or >0.9 micromolar at 48h; use in combo with hydration and urinary alkalinization
megaloblastic anemia, folate deficiency-associated
- [up to 1 mg IV qd]
renal dosing
- [not defined]
- renal impairment: not defined
- HD/PD: not defined
hepatic dosing
- [not defined]
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- hypersensitivity to levoleucovorin
- hypersensitivity to folic acid
- intrathecal use
- GI toxicity, unresolved (colorectal CA use)
Drug Interactions .
Overview
leucovorin
folate analog
- glucarpidase substrate
- hypercalcemia
- levoleucovorin is the active isomer of racemic leucovorin; similar interactions anticipated
Avoid/Use Alternative
- capecitabine
- pafolacianine
- sulfamethoxazole
- trimethoprim
Monitor/Modify Tx
- abaloparatide
- burosumab
- calcipotriene topical
- calcitriol
- calcitriol topical
- calcium acetate
- calcium carbonate
- calcium chloride
- calcium citrate
- calcium gluconate
- chlorothiazide
- chlorthalidone
- cholecalciferol (vitamin D3)
- digoxin
- doxercalciferol
- ergocalciferol (vitamin D2)
- glucarpidase
- hydrochlorothiazide
- indapamide
- methyltestosterone
- metolazone
- palopegteriparatide
- paricalcitol
- teriparatide
- testosterone
Caution Advised
- fluorouracil
- fosphenytoin
- pentobarbital
- phenobarbital
- phenytoin
- primidone
Adverse Reactions .
Serious Reactions
- anaphylactoid reaction
- GI toxicity (colorectal CA use)
- hypercalcemia (IV use)
Common Reactions
- stomatitis (colorectal CA or high-dose methotrexate leucovorin rescue use)
- nausea (colorectal CA use)
- diarrhea (colorectal CA use)
- vomiting (colorectal CA or high-dose methotrexate leucovorin rescue use)
- alopecia (colorectal CA use)
- dermatitis (colorectal CA use)
- urticaria
Safety/Monitoring .
Monitoring Parameters
Colorectal CA: CBC with diff before every cycle, then qwk during 1st 2 cycles, then once per cycle during anticipated WBC nadir; electrolytes, LFTs before each cycle x3, then before every other cycle
Leucovorin Rescue: Cr, methotrexate level at least q24h
Other Indications: no routine tests recommended
Benzyl Alcohol Content
if dose >10 mg/m^2 use sterile water for injection as diluent to avoid benzyl alcohol toxicity
Look/Sound-Alike Drug Names
leucovorin confused with: Leukeran; LEVOleucovorin; Leukine; levothyroxine
Pregnancy/Lactation .
Pregnancy
Clinical Summary
may use during pregnancy; no known risk of fetal harm based on human data
Lactation
Clinical Summary
may use while breastfeeding; no human data available, though risk of infant harm not expected based on drug properties; no human data available to assess effects on milk production
Pharmacology .
Metabolism: for leucovorin: liver, GI tract; CYP450: unknown; Info: active metabolite
Excretion: for leucovorin: urine (primarily), feces; Half-life: 3.5-5.7h (PO route), 6.2-9.5h (IM/IV route)
Subclass: Folate Derivatives, Oncologic ; Supportive Care: Folate Analog Toxicity ; Toxicity: Drugs
Mechanism of Action
for leucovorin: participates in reactions utilizing folates, counteracting folate antagonists (folic acid analog)
Formulary .
No Formulary Selected
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