Tocofersolan

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Bulgaria: Vedrop; Czech Republic: Vedrop; Denmark: Vedrop; Estonia: Vedrop; Germany: Vedrop; Ireland: Vedrop; Latvia: Vedrop; Lithuania: Vedrop; Luxembourg: Vedrop; Malta: Vedrop; Netherlands: Vedrop; Portugal: Vedrop; Romania: Vedrop; Slovakia: Vedrop; Slovenia: Vedrop; Sweden: Vedrop.

Drug combinations

Chemistry

Tocofersolan: C~35~H~58~O~6~. Mw: 574.83. (1) D-α-tocopherol-polyethylene glycol 1000 succinate; (2) 1-O-(2-hydroxyethyl)4-O-[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-ihydrochromen-6-yl] butanedioate; CAS-9002-96-4.

Pharmacologic Category

Vitamins; Vitamin E. Other Plain Vitamin Preparations. (ATC-Code: A11HA08).

Mechanism of action

The active substance D-α-tocopherol-polyethylene glycol 1000 succinate (tocofersolan) is a pro-drug; the active metabolite is D-α-tocopherol. At low concentrations, tocofersolan forms micelles which enhance absorption of non-polar lipids such as fat-soluble vitamins. The hydrolysis of tocofersolan occurs in the gut lumen. Taken up by cells, the α-tocopherol moiety appears in chylomicrons in the lymph in a manner identical to vitamin E absorbed from the diet. Cellular uptake does not require receptors, binding proteins or metabolic processes and does not occur by pinocytosis. Absorption of deuterated tocofersolan showed a normal pattern in lipoproteins: α-tocopherol peaked first in chylomicrons, then in very low-density lipoproteins (VLDL) and finally in low-density lipoproteins (LDL) and high-density lipoproteins (HDL). Located principally on cell membranes, within mitochondria and microsomes, vitamin E is ubiquitously distributed (red blood cells, brain, muscle, liver, platelets) and fat tissues are its major reservoir. Vitamin E is the principal lipo-soluble antioxidant in the organism. It acts as a free radical chain-breaking molecule, stopping the peroxidation of polyunsaturated fatty acids, and is involved in maintaining the stability and integrity of cell membranes.

Therapeutic use

Indicated in vitamin E deficiency due to digestive malabsorption in pediatric patients suffering from congenital chronic cholestasis or hereditary chronic cholestasis, from birth (in term newborns) to 16 or 18 years of age, depending on the region.

Pregnancy and lactiation implications

Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or post-natal development. Caution should be exercised when prescribing to pregnant women. Not recommended during lactation.

Unlabeled use

Contraindications

Hypersensitivity to the active substance or to any of the excipients. Must not be used in prematures.

Warnings and precautions

As large doses of vitamin E have been reported to increase bleeding tendency in vitamin K-deficient patients or those taking oral anti-vitamin K treatment, monitoring prothrombin time and international normalized ratio (INR) is recommended; a possible adjustment of the dose of oral anticoagulant may be necessary. Should be administered with caution and under close monitoring of renal and hepatic function in patients with renal (due to the potential for renal toxicity of polyethylene glycols) and hepatic (due to limited data in these patients) impairment. Renal function and serum osmolarity should be evaluated and monitored under treatment with tocofersolan. Contains sodium methyl parahydroxybenzoate (E219) and sodium propyl parahydroxybenzoate (E217) which may cause allergic reactions.

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