Phylloquinone is often called vitamin K1 or phytonadione. It is a fat-soluble vitamin that is stable to air and moisture but decomposes in sunlight. It is found naturally in a wide variety of green plants. Phylloquinone is also an antidote for coumatetralyl. Vitamin K is needed for the posttranslational modification of certain proteins, mostly required for blood coagulation. MEPHYTON (Phytonadione tablets) are indicated in the following coagulation disorders which are due to faulty formation of factors II, VII, IX and X when caused by vitamin K deficiency or interference with vitamin K activity: anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives; hypoprothrombinemia secondary to antibacterial therapy; hypoprothrombinemia secondary to administration of salicylates; hypoprothrombinemia secondary to obstructive jaundice or biliary fistulas but only if bile salts are administered concurrently, since otherwise the oral vitamin K will not be absorbed. MEPHYTON tablets possess the same type and degree of activity as does naturally-occurring vitamin K, which is necessary for the production via the liver of active prothrombin (factor II), proconvertin (factor VII), plasma thromboplastin component (factor IX), and Stuart factor (factor X). The prothrombin test is sensitive to the levels of three of these four factors II, VII, and X. Vitamin K is an essential cofactor for the gamma-carboxylase enzymes, which catalyze the posttranslational gamma-carboxylation of glutamic acid residues in inactive hepatic precursors of coagulation factors II (prothrombin), VII, IX, and X. Gamma-carboxylation converts these inactive precursors into active coagulation factors, which are secreted by hepatocytes into the blood. Supplementing with Phylloquinone results in a relief of vitamin K deficiency symptoms, which include easy bruisability, epistaxis, gastrointestinal bleeding, menorrhagia and hematuria. Oral phytonadione is adequately absorbed from the gastrointestinal tract only if bile salts are present. After absorption, phytonadione is initially concentrated in the liver, but the concentration declines rapidly. Very little vitamin K accumulates in tissues. Little is known about the metabolic fate of vitamin K. Almost no free unmetabolized vitamin K appears in bile or urine. In normal animals and humans, phytonadione is virtually devoid of pharmacodynamic activity. However, in animals and humans deficient in vitamin K, the pharmacological action of vitamin K is related to its normal physiological function; that is, to promote the hepatic biosynthesis of vitamin K-dependent clotting factors. MEPHYTON tablets generally exert their effect within 6 to 10 hours.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P38435 Gene ID: 2677.0 Gene Symbol: GGCX Target Organism: Homo sapiens (Human) |
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Target ID: Q9BQB6 Gene ID: 79001.0 Gene Symbol: VKORC1 Target Organism: Homo sapiens (Human) |
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Target ID: CHEMBL2012 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16929463 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Preventing | VITAMIN K1 Approved UseVitamin K1 Injection is indicated in: (1) anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives; (2) prophylaxis and therapy of hemorrhagic disease of the newborn; (3) hypoprothrombinemia due to antibacterial therapy; (3) hypoprothrombinemia secondary to factors limiting absorption or synthesis of vitamin K, e.g., obstructive jaundice, biliary fistula, sprue, ulcerative colitis, celiac disease, intestinal resection, cystic fibrosis of the pancreas, and regional enteritis; (4) other drug-induced hypoprothrombinemia where it is definitely shown that the result is due to interference with vitamin K metabolism, e.g., salicylates. Launch Date4.27766415E11 |
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Primary | VITAMIN K1 Approved UseVitamin K1 Injection is indicated in: (1) anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives; (2) prophylaxis and therapy of hemorrhagic disease of the newborn; (3) hypoprothrombinemia due to antibacterial therapy; (3) hypoprothrombinemia secondary to factors limiting absorption or synthesis of vitamin K, e.g., obstructive jaundice, biliary fistula, sprue, ulcerative colitis, celiac disease, intestinal resection, cystic fibrosis of the pancreas, and regional enteritis; (4) other drug-induced hypoprothrombinemia where it is definitely shown that the result is due to interference with vitamin K metabolism, e.g., salicylates. Launch Date4.27766415E11 |
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Preventing | VITAMIN K1 Approved UseVitamin K1 Injection is indicated in: (1) anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives; (2) prophylaxis and therapy of hemorrhagic disease of the newborn; (3) hypoprothrombinemia due to antibacterial therapy; (3) hypoprothrombinemia secondary to factors limiting absorption or synthesis of vitamin K, e.g., obstructive jaundice, biliary fistula, sprue, ulcerative colitis, celiac disease, intestinal resection, cystic fibrosis of the pancreas, and regional enteritis; (4) other drug-induced hypoprothrombinemia where it is definitely shown that the result is due to interference with vitamin K metabolism, e.g., salicylates. Launch Date4.27766415E11 |
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Secondary | MEPHYTON Approved UseMEPHYTON is indicated in the following coagulation disorders which are due to faulty formation of factors II, VII, IX and X when caused by vitamin K deficiency or interference with vitamin K activity. MEPHYTON tablets are indicated in: anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives; hypoprothrombinemia secondary to antibacterial therapy; hypoprothrombinemia secondary to administration of salicylates; hypoprothrombinemia secondary to obstructive jaundice or biliary fistulas but only if bile salts are
administered concurrently, since otherwise the oral vitamin K will not be absorbed. Launch Date-4.49884815E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
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32.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28107923/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
PHYTONADIONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
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146 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28107923/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
PHYTONADIONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28107923/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
PHYTONADIONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED |
Doses
Dose | Population | Adverse events |
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200 mg 1 times / day steady, intravenous Highest studied dose Dose: 200 mg, 1 times / day Route: intravenous Route: steady Dose: 200 mg, 1 times / day Sources: |
unhealthy, 39 years n = 1 Health Status: unhealthy Condition: overdose of brodifacoum Age Group: 39 years Sex: M Population Size: 1 Sources: |
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1000 mg single, intravenous MTD Dose: 1000 mg Route: intravenous Route: single Dose: 1000 mg Sources: |
unhealthy, adult n = 2 Health Status: unhealthy Condition: HCC Age Group: adult Sex: unknown Population Size: 2 Sources: |
PubMed
Title | Date | PubMed |
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Absorption of tritiated vitamin K1 in patients with fat malabsorption. | 1970 Dec |
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Chemiluminescence analysis of menadione sodium bisulfite and analgin in pharmaceutical preparations and biological fluids. | 1999 Dec |
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The anticoagulant factor, protein S, is produced by cultured human vascular smooth muscle cells and its expression is up-regulated by thrombin. | 2000 Mar 15 |
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A new model of isolated systolic hypertension induced by chronic warfarin and vitamin K1 treatment. | 2003 Feb |
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Vitamin B12-associated localized scleroderma and its treatment. | 2004 Sep |
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Vitamin K suppresses lipopolysaccharide-induced inflammation in the rat. | 2006 Apr |
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APOE genotype makes a small contribution to warfarin dose requirements. | 2006 Aug |
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Amelioration of carcinogenesis and tumor growth in the rat liver by combination of vitamin K2 and angiotensin-converting enzyme inhibitor via anti-angiogenic activities. | 2006 Jan |
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Timing of fresh frozen plasma administration and rapid correction of coagulopathy in warfarin-related intracerebral hemorrhage. | 2006 Jan |
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Gradual improvement of liver function after administration of ursodeoxycholic acid in an infant with a novel ABCB11 gene mutation with phenotypic continuum between BRIC2 and PFIC2. | 2007 Nov |
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Chronic angiotensin-converting enzyme inhibition up-regulates mouse kidney growth arrest specific-6 protein and the AXL subfamily of receptor tyrosine kinases. | 2008 Dec |
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Effect of cell differentiation for neuroblastoma by vitamin k analogs. | 2009 Apr |
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CYP4F2 is a vitamin K1 oxidase: An explanation for altered warfarin dose in carriers of the V433M variant. | 2009 Jun |
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Effects of CYP4F2 genetic polymorphisms and haplotypes on clinical outcomes in patients initiated on warfarin therapy. | 2009 Oct |
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Dietary vitamin K alleviates the reduction in testosterone production induced by lipopolysaccharide administration in rat testis. | 2011 Jul |
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Eicosapentaenoic acid reduces warfarin-induced arterial calcification in rats. | 2011 Mar |
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Effects of CYP4F2 polymorphism on response to warfarin during induction phase: a prospective, open-label, observational cohort study. | 2012 Apr |
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An endogenous vitamin K-dependent mechanism regulates cell proliferation in the brain subventricular stem cell niche. | 2012 Apr |
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Vitamin K1 exerts antiproliferative effects and induces apoptosis in three differently graded human colon cancer cell lines. | 2015 |
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Vitamin K1 distribution following intravenous vitamin K1-fat emulsion administration in rats. | 2015 Dec |
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Finding the optimal dose of vitamin K1 to treat vitamin K deficiency and to avoid anaphylactoid reactions. | 2017 Oct |
Sample Use Guides
Prophylaxis of Hemorrhagic Disease of the Newborn: A single intramuscular dose of (E)-phytonadione (Vitamin K1 Injection) 0.5 to 1 mg within one hour of birth is recommended. Treatment of Hemorrhagic Disease of the Newborn: 1 mg should be given either subcutaneously or intramuscularly. Anticoagulant-Induced Prothrombin Deficiency in Adults: the dose of 2.5 mg to 10 mg or up to 25 mg is recommended. Hypoprothrombinemia due to other causes: a dosage of 2.5 to 25 mg or more (rarely up to 50 mg) is recommended.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3684371
Curator's Comment: Vitamin K1 (VK1) inhibited the expression of heat-shock protein 72 (Hsp72) but did not affect the constitutive expression of Hsc70 or calnexin in vitro and in vivo. VK1 and VK2 sensitized A549 cells to heat-shock induced cell death, while the compounds alone had no effect on cell viability. The suppression of Hsp72 was apparently at the protein level because the mRNA expression of Hsp72 was unchanged.
Human lymphocytes were incubated with (E)-phytonadione at a dose of 1 uM. At this concentration (E)-phytonadione significantly increased Sister Chromatid Exchange.
Substance Class |
Mixture
Created
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Record UNII |
A034SE7857
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Validated (UNII)
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N0000175965
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B02BA01
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LOINC |
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NCI_THESAURUS |
C943
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9622-2
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2515 (Number of products:1261)
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WHO-VATC |
QB02BA01
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LIVERTOX |
NBK548213
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N0000180191
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WHO-ESSENTIAL MEDICINES LIST |
10.2
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N0000175966
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208 (Number of products:446)
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28384
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CHEMBL1201519
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D010837
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Vitamin K
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SUB16472MIG
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A034SE7857
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PHYLLOQUINONE
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All of the following components must be present:
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PARENT -> CONSTITUENT ALWAYS PRESENT |
SERVING SIZE 1/2 UP
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PARENT -> CONSTITUENT ALWAYS PRESENT |
Nutritional value per 100 g (3.5 oz) - 101.6 ug (97%)
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METABOLITE -> PARENT |
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IMPURITY -> PARENT |
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ACTIVE MOIETY |