DESCRIPTION
AQUAMEPHYTON * (Phytonadione) is a vitamin, which is a clear, yellow to amber, viscous, odorless or nearly odorless liquid. It is insoluble in water, soluble in chloroform and slightly soluble in ethanol. It has a molecular weight of 450.70.
Phytonadione is 2-methyl-3-phytyl-1,4-naphthoquinone. Its empirical formula is C31H46O2 and its structural formula is:
AquaMEPHYTON injection is a yellow, sterile, aqueous colloidal solution of vitamin K1, with a pH of 5.0 to 7.0, available for injection by the intravenous, intramuscular, and subcutaneous routes. Each milliliter contains:
Phytonadione..........................................................2 mg or 10 mg
Inactive ingredients:
Polyoxyethylated fatty acid
derivative.........................................................................70 mg
Dextrose.........................................................................37.5 mg
Water for Injection, q.s.........................................................1 mL
Added as preservative:
Benzyl alcohol.......................................................................0.9%
*Registered trademark of MERCK & CO., INC.
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CLINICAL PHARMACOLOGY
AquaMEPHYTON aqueous colloidal solution of vitamin K1 for parenteral injection, possesses 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 a microsomal enzyme that catalyzes the post-translational carboxylation of multiple, specific, peptide-bound glutamic acid residues in inactive hepatic precursors of factors II, VII, IX, and X. The resulting gamma-carboxyglutamic acid residues convert the precursors into active coagulation factors that are subsequently secreted by liver cells into the blood.
Phytonadione is readily absorbed following intramuscular administration. 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.
The action of the aqueous colloidal solution, when administered intravenously, is generally detectable within an hour or two and hemorrhage is usually controlled within 3 to 6 hours. A normal prothrombin level may often be obtained in 12 to 14 hours.
In the prophylaxis and treatment of hemorrhagic disease of the newborn, phytonadione has demonstrated a greater margin of safety than that of the water-soluble vitamin K analogues.
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