phytonadione: profile and news

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Other information

Indication
For the treatment of haemorrhagic conditions in infants, antidote for coumarin anticoagulants in hypoprothrombinaemia

Pharmacology
Phytonadione is a vitamin, indicated in the treatment of 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. Phytonadione 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).

Mechanism Of Action
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, VII, IX and X. Gamma-carboxylation converts these inactive precursors into active coagulation factors which are secreted by hepatocytes into the blood. Supplementing with Phytonadione results in a relief of vitamin K deficiency symptoms which include easy bruisability, epistaxis, gastrointestinal bleeding, menorrhagia and hematuria.

Drug Category
Antifibrinolytic Agents; Vitamins (Vitamin K);

Brand Names/Synonyms
Phylloquinone; VITAMIN K1; Mephyton (TN); Phytonadione (JP14/USP); AquaMEPHYTON; Aquamephyton; Konakion; M.V.I. Pediatric; Mephyton; Phytonadione; Vitamin K1; Vitaped; α-Phylloquinone; 1,4-Naphthoquinone, 2-methyl-3-phytyl-; 2', 3'-trans-Vitamin K1; 2-Methyl-3-phythyl-1,4-naphthochinon; 3-Phytylmenadione; Antihemorrhagic vitamin; Aqua-Mephytin; Combinal K1; K-Ject; Kativ N; Kephton; Kinadion; Menadione; Mono-Kay; Monodion; Phyllochinon; Phythyl-menadion; Phythyl-menadion (GERMAN); Phytomenadione; Phytylmenadione; Synthex P; Vitamin K; Vitamin K1 (VAN)

Dosage Forms
LIQUID

Absorption
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.

Interactions
Interactions for Phytonadione: Temporary resistance to prothrombin-depressing anticoagulants may result, especially when larger doses of phytonadione are used. If relatively large doses have been employed, it may be necessary when reinstituting anticoagulant therapy to use somewhat larger doses of the prothrombin-depressing anticoagulant, or to use one which acts on a different principle, such as heparin sodium. Laboratory Tests Prothrombin time should be checked regularly as clinical conditions indicate.

Chemical IUPAC Name
2-methyl-3-(3,7,11,15-tetramethylhexadec-2-enyl)naphthalene-1,4-dione

Chemical Formula
C31H46O2

Half Life
Not Available

Drug Type
Approved Drug

# Accession No
APRD00464

CAS Registry Number
84-80-0