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Konakion

Phytomenadione

 

Composition

Active ingredient: phytomenadione (synthetic vitamin K1).

Chewable dragees 10 mg.

Ampoules MM 10 mg/ml (in a bile acid/lecithin mixedmicelle solution).

 

Excipients: Chewable dragees: silicon dioxide, sucrose, anhydrous dextrose, skim milk powder, cacao, theobroma oil (cacao butter), carob bean gum, glycerol, rice starch, titanium dioxide, ethyl vanillin, spray-dried acacia, light liquid paraffin, hard paraffin, talc, sodium carboxymethylcellulose.

Ampoules: glycocholic acid, sodium hydroxide, lecithin, hydrochloric acid, water for injections.

 

Properties and effects

Vitamin K1 (phytomenadione), the active ingredient of Konakion, is a procoagulant factor. As a component of a hepatic carboxylase system, vitamin K1 is involved in the post-translational carboxylation of clotting factors II (prothrombin), VII, IX and X and the clotting inhibitors protein C and protein S. Coumarins inhibit the reduction of vitamin K1 (quinone form) to vitamin K1 hydroquinone and also prevent the vitamin K1 epoxide arising after carboxylation from being reduced to the quinone form.

 

Vitamin K1 is an antagonist of coumarin-type anticoagulants, e.g. phenprocoumon (active ingredient of Marcoumar). It does not, however, neutralize the activity of heparin (active ingredient of Liquemin); protamine is the antagonist of heparin.

 

Vitamin K1 is ineffective in hereditary hypoprothrombinemia or hypoprothrombinemia induced by severe hepatic failure.

 

In the 10 mg MM ampoules, vitamin K1 is solubilized by means of a physiological colloid system of bile acid-lecithin micelles, a transport medium also found in the body. This mixed-micelle system is characterized by better local and systemic tolerance than previous, conventional solutions for injection.

 

Pharmacokinetics

Absorption

Oral doses of vitamin K1 are absorbed primarily from the middle portions of the small intestine. Optimal absorption requires the presence of bile and pancreatic juice. Systemic availability following oral dosing is approximately 50%, with a wide range of interindividual variability. Onset of action occurs approximately 1-3 hours after intravenous administration and 4-6 hours after oral doses.

 

Distribution

The primary distribution compartment corresponds to the plasma volume. In blood plasma 90% of vitamin K1 is bound to lipoproteins (VLDL fraction). Normal plasma concentrations of vitamin K1 range from 0.4 to 1.2 ng/ml. After i.v. administration of 10 mg vitamin K1 (Konakion MM), the plasma level after 1 hour is about 500 ng/ml and about 50 ng/ml at 12 hours. Vitamin K1 does not readily cross the placenta and is poorly distributed into breast milk.

 

Metabolism

Vitamin K1 is rapidly converted into more polar metabolites, including vitamin K1-2, 3-epoxide. Some of this metabolite is reconverted into vitamin K1.

 

Elimination

Following metabolic degradation, vitamin K1 is excreted in the bile and urine as glucuronide and sulfate conjugates. Less than 10% of a dose is excreted unchanged in the urine. The elimination half-life in adults has been reported to be about 14 6 hours (i.v.).

 

Pharmacokinetics in special clinical situations

Intestinal absorption of vitamin K1 is impaired by various conditions, including malabsorption syndromes, short bowel syndrome, biliary atresia and pancreatic insufficiency. Elderly anticoagulated patients are more sensitive than younger ones to parenteral vitamin K1.

 

Indications and usage

Hemorrhage or risk of hemorrhage as a result of severe 'hypoprothrombinemia' (i.e. deficiency of clotting factors II, VII, IX and X) of various etiologies, including overdosage of coumarin-type anticoagulants, their combination with phenylbutazone and other forms of hypovitaminosis K (e.g. in obstructive jaundice as well as liver and intestinal disorders, and after prolonged treatment with antibiotics, sulfonamides or salicylates). For prophylaxis and treatment of hemorrhagic disease in the newborn, Konakion MM paediatric ampoules (2 mg/0.2 ml) should be used.

 

Dosage and administration

Konakion MM ampoules are for i.v. injection. The ampoule solution should not be diluted or mixed with other injectables, but may be injected, where appropriate, into the lower part of the infusion set, during continuous infusion of sodium chloride 0.9% or dextrose 5%.

 

Standard dosage

Severe hemorrhage, e.g. during anticoagulant therapy:

The anticoagulant should be withdrawn and an i.v. injection of Konakion MM given slowly (in at least 30 seconds) in a dose of 10-20 mg (1 to 2 ampoules). The prothrombin level should be estimated 3 hours later, and if the response has been inadequate, the dose should be repeated. Not more than 40-50 mg of Konakion MM should be given i.v. in 24 hours. Konakion MM therapy should be accompanied, when necessary i.e. in life-threatening situations, by a more immediately effective treatment such as transfusions of whole blood or blood-clotting factors.

 

Mild hemorrhage or hemorrhagic tendency:

1 chewable dragee. This should be followed by a second, possibly larger dose of 2 chewable dragees if no effect is seen within 8-12 hours. In general, oral anticoagulants should be discontinued temporarily.

 

Special dosage instructions

Use in the elderly:

Elderly patients tend to be more sensitive to reversal of anticoagulation with Konakion. The dosage for this patient group should therefore be at the lower end of the ranges recommended.

 

Children over one year of age:

If, on the recommendation of a physician, a child is treated with Konakion, a dosage of 5-10 mg is suggested.

 

Infants under one year of age:

For this patient group, Konakion MM paediatric should be used.

 

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