folinic acid

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Related to Folinic: leucovorin, Calcium levofolinate

folinic acid

 [fo-lin´ik]
the 5-formyl derivative of tetrahydrofolic acid, a metabolically active derivative of folic acid used to treat folic acid deficiencies and as an antidote to folic acid antagonists. Called also citrovorum factor and leucovorin.

leucovorin calcium (citrovorum factor, folinic acid)

Calcium Folinate (UK), Lederfolin (UK), Refolinon (UK)

Pharmacologic class: Water-soluble vitamin

Therapeutic class: Vitamin, antidote to folic acid antagonist, antianemic, antineoplastic adjunct

Pregnancy risk category C

Action

Counteracts therapeutic and toxic effects of folic acid antagonists; may enhance therapeutic and toxic effects of fluoropyrimidines used in cancer therapy. Also supplements folic acid in folic acid deficiency.

Availability

Injection (expressed as base): 10 mg/vial, 50 mg/vial, 100 mg/vial, 200 mg/vial, 350 mg/vial, 500 mg/vial

Injection, preservative-free (expressed as base): 10 mg/vial, 50 mg/vial, 200 mg/vial, 350 mg/vial, 500 mg/vial

Tablets: 5 mg, 15 mg, 25 mg

Indications and dosages

Leucovorin rescue after high-dose methotrexate therapy

Adults: 15 mg (approximately 10 mg/m2) P.O., I.M., or I.V. q 6 hours, starting 24 hours after methotrexate infusion begins and continuing until serum methotrexate level drops below 10-8 M. If 24-hour serum creatinine level rises 50% over baseline or if 24-hour methotrexate level exceeds 5 × 10-6 M or 48-hour level exceeds 9 × 10-7 M, increase leucovorin dosage to 100 mg/m2 I.V. q 3 hours and continue hydration and urinary alkalization until methotrexate level drops below 10-8 M.

To reduce toxicity and counteract effects of impaired methotrexate elimination or inadvertent overdose of folic acid antagonist

Adults: 15 mg (roughly 10 mg/m2) I.M., I.V., or P.O. q 6 hours until serum methotrexate level drops below 10-8 M. If 24-hour serum creatinine level rises 50% over baseline or if 24-hour methotrexate level exceeds 5 × 10-6 M or 48-hour level exceeds 9 × 10-7 M, increase leucovorin dosage to 100 mg/m2 I.V. q 3 hours and continue hydration and urinary alkalization until methotrexate level drops below 10-8 M.

Advanced colorectal cancer

Adults: Usually given in one of the following regimens: 200 mg/m2 slow I.V. injection over at least 3 minutes, followed by I.V. injection of 5-fluorouracil (5-FU); or 20 mg/m2 I.V. injection, followed by I.V. injection of 5-FU. Treatment is repeated daily for 5 days, and may then be repeated at 28-day intervals for two courses and then at 4- to 5-week intervals, as prescribed.

Megaloblastic anemia secondary to folic acid deficiency

Adults: Up to 1 mg I.M. daily

Dosage adjustment

• In leucovorin rescue after high-dose methotrexate therapy: delayed early or late methotrexate elimination (serum methotrexate level still above 0.2 µM at 72 hours and above 0.05 µM [5 × 10-8] at 96 hours after administration)
• Evidence of acute renal injury

Contraindications

• Treatment of pernicious anemia and other megaloblastic anemias caused by vitamin B12 deficiency

Precautions

Use cautiously in:
• anemia (when vitamin B12 deficiency has been ruled out)
• patients receiving 5-FU concomitantly
• pregnant or breastfeeding patients
• children.

Administration

Recheck leucovorin dosage in current published protocols before giving as methotrexate rescue.
• Give parenterally in patients with GI toxicity, nausea, or vomiting.
• Reconstitute leucovorin injection with sterile or bacteriostatic water for injection containing benzyl alcohol. (When giving with 5-FU for colorectal cancer in dosages above 10 mg/m2, reconstitute only with sterile water for injection.)

Don't mix leucovorin injection with 5-FU, because precipitation will occur.

Give I.V. leucovorin slowly (no faster than 160 mg/minute) because of calcium content. Large doses may be infused over 1 to 6 hours as directed.

Don't give intrathecally; drug may be harmful or fatal by this route.
• Be aware that P.O. dosages above 25 mg are not recommended.

Adverse reactions

Skin: urticaria

Other: allergic sensitization reactions, anaphylactoid reactions

Interactions

Drug-drug.5-FU: enhanced fluorouracil toxicity

Methotrexate, other folic acid antagonists: negated therapeutic and toxic effects of these drugs

Phenobarbital, phenytoin, primidone: negated anticonvulsant effect, increased frequency of seizures in susceptible children

Patient monitoring

Monitor serum creatinine and methotrexate levels every 24 hours.

Monitor closely for adverse reactions. Continue leucovorin therapy, hydration, and urinary alkalization until serum methotrexate level drops below 10-8 M.

Monitor CBC with white cell differential and platelet count before leucovorin/5-FU therapy starts. Repeat weekly during first two courses and then once each cycle at anticipated white blood cell nadir.
• Check electrolyte levels and liver function tests before each treatment for first three cycles. Thereafter, check before every other cycle.
• Assess for adequate hydration when giving with 5-FU or high-dose methotrexate.
• Watch for hypersensitivity reactions, especially anaphylactoid reactions.

Patient teaching

• Teach patient about drug and protocol.

Stress importance of taking leucovorin as prescribed with high-dose methotrexate therapy. Emphasize that it's not just a vitamin.
• Tell patient to immediately report signs or symptoms of allergic reaction, such as hives.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.

fo·lin·ic ac·id

(fō-lin'ik as'id),
1. The active form of folic acid that acts as a formyl group carrier in transformylation reactions; the calcium salt, leucovorin calcium, has therapeutic use.
2. The term is occasionally applied to other folates.

folinic acid

/fo·lin·ic ac·id/ (fo-lin´ik) leucovorin; the 5-formyl derivative of tetrahydrofolic acid; it can act as a coenzyme carrier in certain folate-mediated reactions and is used, as the calcium salt leucovorin calcium, in the treatment of some disorders of folic acid deficiency.

folinic acid

(fō-lĭn′ĭk)
n.
Leucovorin.

folinic acid

[fōlin′ik]
an active form of folic acid. It is used to treat megaloblastic anemias that are not caused by vitamin B12 deficiency and to counteract the toxic effects of antineoplastic folic acid antagonists, such as methotrexate. Also called citrovorum factor, leucovorin.

fo·lin·ic ac·id

(fō-lin'ik as'id)
The active form of folic acid, which acts as a formyl group carrier in transformylation reactions; the calcium salt, leucovorin calcium, has therapeutic use.
Synonym(s): citrovorum factor.

folinic acid

A drug used to treat MEGALOBLASTIC ANAEMIA that has resulted from folic deficiency. A brand name is Refolinon.

folinic acid

5-formyltetrahydrofolic acid, a metabolically active derivative of folic acid used to treat folic acid deficiency and as an antidote to folic acid antagonists. Called also citrovorum factor, CF, leucovorin, 5-formyltetrahydropteroylglutamic acid.
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The efficacy of folic acid and folinic acid in reducing methotrexate gastrointestinal toxicity in rheumatoid arthritis.
LAHORE, February 03, 2012 (Frontier Star): Death toll of victims of suspected medicine reaction increased as 2 new cardiac patients died on Thursday on this count while the patients were administered folinic acid injection in hospitals.
Intravenous folinic acid 15 mg daily was also given in view of the potential methotrexate overdose.
Concomitant administration of high-dose folinic acid rescue and dexamethasone are recommended in all published reports (1).
Effect of folic or folinic acid supplementation on the toxicity and efficacy of methotrexate in rheumatoid arthritis: a forty-eight-week, multicenter, randomized, doubleblind, placebo-controlled study.
Pharmacological dose of vitamin B12 is as effective as low-dose folinic acid in correcting hyperhomocysteinemia of hemodialysis patients.
5,10) Co-factor therapy with thiamine, pyridoxine, and magnesium, to enhance the metabolism of glycolic acid, may be considered; similarly, folinic acid administration can be used in cases of MTH poisoning since it may augment the conversion of toxic to nontoxic metabolites.
Standard combination chemotherapy regimens comprising 5-fluorouracil (5-FU) plus leucovorin [LV, also known as folinic acid (FA)] in combination with irinotecan, typically FOLFIRI or oxaliplatin (FOLFOX) have been reported to facilitate the resection of 9%-40% of initially unresectable metastases [1, 2], with data emerging from randomized trials suggesting that the addition of targeted agents and a third cytotoxic might be even more effective.
The new research, funded by Cancer Research UK and published in the British Journal of Cancer, shows that patients who had surgery and chemotherapy with a drug called 5FU alongside folinic acid, had a five year survival rate of 24%.
Folfiri is a combination of a synthetic form of folinic acid, fluorouracil, which is made by companies including Teva Pharmaceutical Industries Ltd.