Peringatan Keamanan

High doses of vitamin K1 are not associated with toxicity.A234259 Intravenous administration has been associated with an increased risk of toxicity.A234284 These patients should be treated with symptomatic and supportive measures.

The intravenous LD50 in mice is 1170 mg/kg and the oral LD50 is >24180 mg/kg.L33345

Phylloquinone

DB01022

small molecule approved investigational

Deskripsi

Vitamin K1, also called phylloquinone or phytonadione, is a fat soluble vitamin.L33319,L33345 Phylloquinone is a cofactor of the enzyme ?-carboxylase, which modifies and activates precursors to coagulation factors II, VII, IX, and X.A234264,A234195,A234259 It is indicated in the treatment of coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by deficiency or interference in the activity of vitamin K.L33319

Phylloquinone has been synthesized since at least 1939,A234384 and was approved by the FDA prior to 1955.L33389

Struktur Molekul 2D

Berat 450.6957
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Intravenous phylloquinone has an initial half life of 22 minutes, followed by a half life of 125 minutes.[A234104]
Volume Distribusi The steady state volume of distribution of phylloquinone is 20 ± 6 L in subjects who are also taking phenprocoumon therapy.[A234374]
Klirens (Clearance) Intravenous phylloquinone is 90% cleared in 2 hours, and 99% cleared in 8 hours.[A234104,A234329] A 10 mg intravenous dose of phylloquinone has a mean clearance of 91 ± 24 mL/min.[A234344]

Absorpsi

A 4 µg oral dose of phylloquinone is 13% ± 9% bioavailable, with a Tmax of 4.7 ± 0.8 hours.A234264 1.5 ± 0.8 nmol is found in the plasma compartment, and 3.6 ± 3.4 nmol is found in the second compartment.A234264 A 10 mg intramuscular phylloquinone dose is 89.2% ± 25.4% bioavailable.A234344 The same dose reaches a mean Cmax of 67 ± 30 ng/mL, with a mean Tmax of 9.2 ± 6.6 hours, and an AUC of 1700 ± 500 h\*ng/mL.A234344 A 10 mg intravenous phylloquinone dose has a mean AUC of 1950 ± 450 h\*ng/mL.A234344

Metabolisme

Phylloquinone's phytyl side chain is omega hydroxylated by CYP4F2.A137578 The side chain is then cleaved to 5 or 7 carbons long, and then glucuronidated prior to elimination.A234104,A234109,A234114,A234119 Vitamin Ks in general undergo a cycle of reduction to vitamin K hydroquinone by vitamin K epoxide reductase (VKOR), oxidation to vitamin K epoxide by gamma-glutamyl carboxylase, and converted back to vitamin K by VKOR.A234259

Rute Eliminasi

Intravenous phylloquinone is 36% eliminated in the feces in 5 days and 22% recovered in urine in 3 days.A234104,A234329

Interaksi Obat

735 Data
Orlistat Orlistat can cause a decrease in the absorption of Phylloquinone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dicoumarol The therapeutic efficacy of Dicoumarol can be decreased when used in combination with Phylloquinone.
Phenindione The therapeutic efficacy of Phenindione can be decreased when used in combination with Phylloquinone.
Warfarin The therapeutic efficacy of Warfarin can be decreased when used in combination with Phylloquinone.
Phenprocoumon The therapeutic efficacy of Phenprocoumon can be decreased when used in combination with Phylloquinone.
Acenocoumarol The therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Phylloquinone.
4-hydroxycoumarin The therapeutic efficacy of 4-hydroxycoumarin can be decreased when used in combination with Phylloquinone.
Coumarin The therapeutic efficacy of Coumarin can be decreased when used in combination with Phylloquinone.
(R)-warfarin The therapeutic efficacy of (R)-warfarin can be decreased when used in combination with Phylloquinone.
Ethyl biscoumacetate The therapeutic efficacy of Ethyl biscoumacetate can be decreased when used in combination with Phylloquinone.
Fluindione The therapeutic efficacy of Fluindione can be decreased when used in combination with Phylloquinone.
Clorindione The therapeutic efficacy of Clorindione can be decreased when used in combination with Phylloquinone.
Diphenadione The therapeutic efficacy of Diphenadione can be decreased when used in combination with Phylloquinone.
Tioclomarol The therapeutic efficacy of Tioclomarol can be decreased when used in combination with Phylloquinone.
(S)-Warfarin The therapeutic efficacy of (S)-Warfarin can be decreased when used in combination with Phylloquinone.
Mineral oil The serum concentration of Phylloquinone can be decreased when it is combined with Mineral oil.
Cyclosporine Cyclosporine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Phylloquinone which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Phylloquinone which could result in a higher serum level.

Target Protein

Vitamin K-dependent gamma-carboxylase GGCX
Osteocalcin BGLAP

Referensi & Sumber

Synthesis reference: Manfred Dorner, "Method of making vitamin K1." U.S. Patent US5744624, issued June, 1964.
Artikel (PubMed)
  • PMID: 859820
    Barkhan P, Shearer MJ: Metabolism of vitamin K1 (phylloquinone) in man. Proc R Soc Med. 1977 Feb;70(2):93-6.
  • PMID: 7306367
    McBurney A, Shearer MJ, Barkhan P: Preparative isolation and characterization of the urinary aglycones of vitamin K1 (phylloquinone in man. Biochem Med. 1980 Dec;24(3):250-67. doi: 10.1016/0006-2944(80)90020-4.
  • PMID: 22516726
    Shearer MJ, Fu X, Booth SL: Vitamin K nutrition, metabolism, and requirements: current concepts and future research. Adv Nutr. 2012 Mar 1;3(2):182-95. doi: 10.3945/an.111.001800.
  • PMID: 32625486
    Turck D, Bresson JL, Burlingame B, Dean T, Fairweather-Tait S, Heinonen M, Hirsch-Ernst KI, Mangelsdorf I, McArdle HJ, Naska A, Nowicka G, Pentieva K, Sanz Y, Siani A, Sjodin A, Stern M, Tome D, Van Loveren H, Vinceti M, Willatts P, Lamberg-Allardt C, Przyrembel H, Tetens I, Dumas C, Fabiani L, Ioannidou S, Neuhauser-Berthold M: Dietary reference values for vitamin K. EFSA J. 2017 May 22;15(5):e04780. doi: 10.2903/j.efsa.2017.4780. eCollection 2017 May.
  • PMID: 24138531
    Edson KZ, Prasad B, Unadkat JD, Suhara Y, Okano T, Guengerich FP, Rettie AE: Cytochrome P450-dependent catabolism of vitamin K: omega-hydroxylation catalyzed by human CYP4F2 and CYP4F11. Biochemistry. 2013 Nov 19;52(46):8276-85. doi: 10.1021/bi401208m. Epub 2013 Nov 7.
  • PMID: 31869059
    Imbrescia K, Moszczynski Z: Vitamin K .
  • PMID: 17671443
    Jones KS, Bluck LJ, Wang LY, Coward WA: A stable isotope method for the simultaneous measurement of vitamin K1 (phylloquinone) kinetics and absorption. Eur J Clin Nutr. 2008 Nov;62(11):1273-81. doi: 10.1038/sj.ejcn.1602859. Epub 2007 Aug 1.
  • PMID: 24489112
    Shearer MJ, Newman P: Recent trends in the metabolism and cell biology of vitamin K with special reference to vitamin K cycling and MK-4 biosynthesis. J Lipid Res. 2014 Mar;55(3):345-62. doi: 10.1194/jlr.R045559. Epub 2014 Jan 31.
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