Peringatan Keamanan

Overdose of levomefolic acid is unlikely to cause clinically significant adverse events.

Levomefolic acid

DB11256

small molecule approved investigational

Deskripsi

Levomefolic acid (INN) is the metabolite of folic acid (Vitamin B9) and it is a predominant active form of folate found in foods and in the blood circulation, accounting for 98% of folates in human plasma A19276. It is transported across the membranes including the blood-brain barrier into various tissues where it plays an essential role in the DNA synthesis, cysteine cycle and regulation of homocysteine, where it methylates homocysteine and forms methionine and tetrahydrofolate (THF). Levomefolate is approved as a food additive and is designated a GRAS (generally regarded as safe) compound L773. It is available commercially as a crystalline form of the calcium salt (Metafolin(R)), which has the stability required for use as a supplement A19276. Supplementation of levomefolic acid is desired over folic acid due to reduced potential for masking vitamin B12 deficiency symptoms.

Struktur Molekul 2D

Berat 459.4558
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life is approximately 3 hours after 5mg of oral L-methylfolate, administered daily for 7 days [L775].
Volume Distribusi Circulates in its free form or loosely bound to plasma proteins
Klirens (Clearance) -

Absorpsi

Absorbed in the proximal small intestines via the active proton-coupled folate transporter (PCFT) that transports both oxidized and reduced folic acids. Passive diffusion also occurs at the proximal and distal portions of the small intestines A19277. A single oral dose of 906nmol of levomefolic acid in healthy females resulted in the mean peak plasma concentration of 39.4nmol/L A19276.

Metabolisme

Levomefolic acid is further converted into tetrahydrofolate (THF) via the vitamin B12-dependent enzyme methionine synthase before effective polyglutamylation by folylpolyglutamate synthetase (FPG). Polyglumate forms of folic acids are more effective substrates for associated enzymes in folate-dependent reactions.

Rute Eliminasi

Mainly eliminated through renal or fecal excretion. Small proportion of excreted levomefolic acid is in unchanged form as over 99% of tissue folate is in polyglutamate form. Some portions of levomefolic acid is secreted into bile.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Recommendations vary from product to product - consult individual product monographs for additional information.

Interaksi Obat

19 Data
Fosphenytoin The serum concentration of Fosphenytoin can be decreased when it is combined with Levomefolic acid.
Raltitrexed The therapeutic efficacy of Raltitrexed can be decreased when used in combination with Levomefolic acid.
Sulfasalazine The serum concentration of Levomefolic acid can be decreased when it is combined with Sulfasalazine.
Phenytoin The serum concentration of Phenytoin can be decreased when it is combined with Levomefolic acid.
Glucarpidase The serum concentration of the active metabolites of Levomefolic acid can be reduced when Levomefolic acid is used in combination with Glucarpidase resulting in a loss in efficacy.
Primidone The serum concentration of Primidone can be decreased when it is combined with Levomefolic acid.
Methylphenobarbital The serum concentration of the active metabolites of Methylphenobarbital can be reduced when Methylphenobarbital is used in combination with Levomefolic acid resulting in a loss in efficacy.
Phenobarbital The serum concentration of the active metabolites of Phenobarbital can be reduced when Phenobarbital is used in combination with Levomefolic acid resulting in a loss in efficacy.
Valproic acid The serum concentration of Levomefolic acid can be decreased when it is combined with Valproic acid.
Colestipol The serum concentration of Levomefolic acid can be decreased when it is combined with Colestipol.
Carbamazepine The serum concentration of Levomefolic acid can be decreased when it is combined with Carbamazepine.
Fluorouracil The risk or severity of adverse effects can be increased when Levomefolic acid is combined with Fluorouracil.
Flucytosine The risk or severity of adverse effects can be increased when Levomefolic acid is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Levomefolic acid is combined with Capecitabine.
5-fluorouridine The risk or severity of adverse effects can be increased when Levomefolic acid is combined with 5-fluorouridine.
Uracil The risk or severity of adverse effects can be increased when Levomefolic acid is combined with Uracil.
Tegafur The risk or severity of adverse effects can be increased when Levomefolic acid is combined with Tegafur.
Doxifluridine The risk or severity of adverse effects can be increased when Levomefolic acid is combined with Doxifluridine.
Pafolacianine Levomefolic acid may decrease effectiveness of Pafolacianine as a diagnostic agent.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 22171769
    Fruzzetti F: Beyaz(R): an oral contraceptive fortified with folate. Womens Health (Lond). 2012 Jan;8(1):13-9. doi: 10.2217/whe.11.68.
  • PMID: 22067790
    Bart S Sr, Marr J, Diefenbach K, Trummer D, Sampson-Landers C: Folate status and homocysteine levels during a 24-week oral administration of a folate-containing oral contraceptive: a randomized, double-blind, active-controlled, parallel-group, US-based multicenter study. Contraception. 2012 Jan;85(1):42-50. doi: 10.1016/j.contraception.2011.05.013. Epub 2011 Jul 13.
  • PMID: 21877996
    Rapkin RB, Creinin MD: The combined oral contraceptive pill containing drospirenone and ethinyl estradiol plus levomefolate calcium. Expert Opin Pharmacother. 2011 Oct;12(15):2403-10. doi: 10.1517/14656566.2011.610791. Epub 2011 Aug 31.
  • PMID: 21967158
    Wilson SM, Bivins BN, Russell KA, Bailey LB: Oral contraceptive use: impact on folate, vitamin B(6), and vitamin B(1)(2) status. Nutr Rev. 2011 Oct;69(10):572-83. doi: 10.1111/j.1753-4887.2011.00419.x.
  • PMID: 21311704
    Ginsberg LD, Oubre AY, Daoud YA: L-methylfolate Plus SSRI or SNRI from Treatment Initiation Compared to SSRI or SNRI Monotherapy in a Major Depressive Episode. Innov Clin Neurosci. 2011 Jan;8(1):19-28.
  • PMID: 24392264
    Shelton RC, Sloan Manning J, Barrentine LW, Tipa EV: Assessing Effects of l-Methylfolate in Depression Management: Results of a Real-World Patient Experience Trial. Prim Care Companion CNS Disord. 2013;15(4). pii: PCC.13m01520. doi: 10.4088/PCC.13m01520. Epub 2013 Aug 29.
  • PMID: 14769778
    Willems FF, Boers GH, Blom HJ, Aengevaeren WR, Verheugt FW: Pharmacokinetic study on the utilisation of 5-methyltetrahydrofolate and folic acid in patients with coronary artery disease. Br J Pharmacol. 2004 Mar;141(5):825-30. Epub 2004 Feb 9.
  • PMID: 20608755
    Pietrzik K, Bailey L, Shane B: Folic acid and L-5-methyltetrahydrofolate: comparison of clinical pharmacokinetics and pharmacodynamics. Clin Pharmacokinet. 2010 Aug;49(8):535-48. doi: 10.2165/11532990-000000000-00000.
Menampilkan 8 dari 11 artikel.

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International Brands
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