Name the main drug.
PHYTOMENADION
Describe the characteristics.
Synonyms
Vitamin K1 (phytomenadione, phytonadione, or phylloquinone)
Vitamin K2 (menaquinone)
Substance class: naphthoquinones
Chemical structure:
Vitamin K1
Vitamin K2
Inactive precursors (provitamins): none
Active form: vitamin K hydroquinone
Activation occurs via enzyme epoxide reductase.
Mutations in the VKORC1 (Vitamin K epOxide Reductase Complex subunit 1) gene impair the reduction of vitamin K epoxide, resulting in deficiencies in vitamin K-dependent clotting factors.
Sources
Leafy green vegetables (vitamin K1)
Eggs, dairy, and meat (vitamin K2)
Synthesized in small amounts by intestinal bacteria
Transport: via lipoproteins; no specific protein
Storage: liver
Excretion: bile and urine
Describe the functions of vitamin K.
Cofactor for γ-carboxylation of glutamate residues on vitamin-K-dependent proteins involved in:
Coagulation: maturation of factors II (prothrombin), VII, IX, and X, protein C, protein S
Bone formation: osteocalcin (bone Gla protein), matrix Gla protein
List uses.
Hypoprothrombinemia
Vit. K deficiendy bleeding neonates
Dietary requirements
What is a contraindication?
Known hypersensitivity to phytonadione or any ingredient in the formulation.
List commen adverse effects.
Parenteral Administration: Pain, swelling, and tenderness at the injection site, transient “flushing sensations,” “peculiar” sensations of taste (dysgeusia).
List the specific drug interactions.
Drug
Interaction
Comments
Anticoagulants, oral (coumarins and indandiones)
Vitamin K1 is a pharmacologic antagonist [ref]
Avoid concomitant use; only use concomitant phytonadione for treatment of excessive hypoprothrombinemia [ref]
Consider alternative to prothrombin-depressing anticoagulant (e.g., heparin) if necessary [ref]
Orlistat
Possible decreased GI absorption of fat-soluble vitamins, including phytonadione (vitamin K1) [ref]
Separate oral administration of orlistat and phytonadione by ≥2 hours [r
Describe the actions.
Same activity as naturally occurring vitamin K1, which is required for the synthesis of blood coagulation factors II (prothrombin), VII (proconvertin), IX (Christmas factor or plasma thromboplastin component), and X (Stuart-Prower factor) in the liver.
Involved in carboxylation of the preformed, inactive precursors of these coagulation factors, resulting γ-carboxyglutamyl residues are required for the calcium-dependent phospholipid binding exhibited by active vitamin K-dependent clotting factors.
Reverses the inhibitory effect of coumarin and indandione derivatives on the synthesis of these factors.
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