Levoleucovorin

Levoleucovorin Brand Names- Fusilev | KHAPZORY

What is Levoleucovorin

Levoleucovorin is approved by the FDA as rescue therapy following high-dose methotrexate (12 grams/m2 IV over 4 hours) treatment in patients with osteosarcoma and to reduce toxicity associated with inadvertent folic acid antagonist overdose or impaired methotrexate elimination.

The Fusilev and Khapzory brands are also approved for the palliative treatment of advanced metastatic colorectal cancer, in combination with 5-fluorouracil.

Levoleucovorin is the levo isomeric form of racemic (d,l)-leucovorin and the pharmacologically active isomer of 5-formyl tetrahydrofolic acid (folinic acid).

Levoleucovorin does not require reduction by the enzyme dihydrofolate reductase; it forms 5-methyltetrahydrofolate (5-MTHF), a reduced (active) folate.

Levoleucovorin counteracts the toxic effects of folic acid antagonists such as methotrexate and is used to ameliorate the hematologic toxicity associated with high-dose methotrexate therapy or other folic acid antagonist overdose.

Levoleucovorin also enhances the therapeutic and toxic effects of fluoropyrimidines, such as 5-fluorouracil.

Indications

  • colorectal cancer
  • methotrexate toxicity prophylaxis

For methotrexate toxicity prophylaxis

as rescue therapy following the administration of high-dose methotrexate (12 grams/m2 IV over 4 hours) in patients with osteosarcoma

NOTE: The FDA has designated levoleucovorin as an orphan drug for use in conjunction with high-dose methotrexate in the treatment of osteosarcoma.

Side Effects

  1. abdominal pain
  2. abdominal pain
  3. alopecia
  4. alopecia
  5. anorexia
  6. anorexia
  7. asthenia
  8. asthenia
  9. atopic dermatitis
  10. atopic dermatitis
  11. chills
  12. confusion
  13. diarrhea
  14. diarrhea
  15. dysgeusia
  16. dyspepsia
  17. dyspnea
  18. fatigue
  19. fatigue
  20. fever
  21. malaise
  22. malaise
  23. nausea
  24. nausea
  25. peripheral neuropathy
  26. pruritus
  27. rash
  28. seizures
  29. stomatitis
  30. stomatitis
  31. syncope
  32. typhlitis
  33. vomiting
  34. vomiting

Monitoring Parameters

  • serum creatinine

Contraindications

  • breast-feeding
  • children
  • dehydration
  • diarrhea
  • folic acid hypersensitivity
  • geriatric
  • pernicious anemia
  • pregnancy
  • renal disease
  • renal impairment
  • seizure disorder
  • vitamin B12 deficiency megaloblastic anemia

Levoleucovorin is contraindicated in patients with a history of folic acid hypersensitivity or folinic acid hypersensitivity.

Interactions

  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Amobarbital
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Barbiturates
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Butabarbital
  • Capecitabine
  • Floxuridine
  • Fluorouracil, 5-FU
  • Fosphenytoin
  • Glucarpidase
  • Mephobarbital
  • Methohexital
  • Pentobarbital
  • Phenobarbital
  • Phenytoin
  • Primidone
  • Secobarbital
  • Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
  • Thiopental
  • Trimethoprim
  • Trimetrexate
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