Vitamin drugs

Vitamins are essential substances that, with rare exceptions, are not synthesized in the body and come with food or synthesized by intestinal microflora. Nutrition provides the daily requirement of vitamins. The study of their biological functions has created vitamin drugs, vitamin content of which is many times greater than the daily requirement of them, but such amounts show a valid pharmacological effect. Therefore, vitamin preparations are used for the treatment and prevention of various diseases. Diet does not allow so many vitamins as drugs.

The biological function of vitamins is mainly associated with their participation in the processes of metabolism. Historically, vitamins can be subdivided according to their physical and chemical properties – the ability to be dissolved in water. In this respect, we have water- and fat-soluble vitamins. Most water-soluble vitamins form coenzymes and become a part of the enzymes as a prosthetic (nonprotein) groups. The biological role of the majority of fat-soluble vitamins is associated with their participation in the construction and function of biological cell membranes.

Water-soluble vitamin drugs

(1) Thiamine 

(Vitamin B1). The approximate daily need is 1,2 mg. Medications: thiamine bromide, thiamine chloride.

Pharmacodynamics. It forms a coenzyme – thiamine diphosphate (thiamine pyrophosphate, kokarboksilaza), which is a part of enzymes: pyruvate dehydrogenase, transketolase, alcohol dehydrogenase. It is involved in the oxidative decarboxylation of keto acids and is actively involved in the metabolism of peripheral nerve, myocardium, GIT. It decreases tissue acidosis by reducing the production of lactic acid. Thiamine is called antineurotic vitamin (aneurine). The vitamin deficiency in the body associated with its insufficient amount in food, the development of diseases (diabetes, alcoholic neuropathy) is manifested by the disturbances in nerve system, cardiovascular and digestive systems. It also affects the conduction of nerve impulses in synapses.

Indications. Thiamine drugs are used for neuritis, neuralgia, sciatica, peripheral paralysis, paresis, diabetic, alcoholic polyneuropathy, as well as diseases of the cardiovascular and digestive systems.

Route of administration: oral and parenteral (IM, IV).

Undesirable side reactions. Allergic reactions (urticaria, angioedema, anaphylactic shock is possible).

Drug interaction. Pharmacological interactions: simultaneous parenteral administration of thiamine and pyridoxine (B6) and cyanocobalamin (B12) is not recommended. Pyridoxine impedes the conversion to thiaminediphosphate, cyanocobalamin enhances allergenic effect of thiamine. Pharmaceutical interaction: thiamine and penicillin or streptomycin cannot be mixed in the same syringe (destruction of thiamine).

Dosage forms. Thiamine chloride – tablets, in multivitamin dragees. 5% solution in ampoules of 1 and 2 ml. Thiamine bromide – tablets, in multivitamin dragees. 6% solution in 1 ml ampoules.

(2) Cocarboxylase 

(Cocarboxylasum), thiaminediphosphate. It is used as a drug for the following indications: diabetic acidosis, respiratory acidosis in patients with chronic pulmonary heart disease, diabetes and liver coma, peripheral neuritis, chronic alcoholism.

Routes of administration. IM, IV, sometimes in SC.

Dosing. For adults – 0.05 - 1 g; for children - 0.025 - 0.05 g, once a day. In diabetes (acidosis, coma) daily dose of 0.1 to 1 g

Side effects. Allergic reactions are possible when administered IM – itching and swelling at the injection site.

Dosage forms. Frozen-dried powder for injection solutions in ampoules – 0.05 to 0,025 g

(3) Riboflavin – 

vitamin B2. The approximate daily need is 1.3 mg. Medications: riboflavin.

Pharmacodynamics. It forms coenzymes: flavin adenine dinucleotide (FAD) and flavin mononucleotide (FMN), a part of flavin dehydrogenase – redox enzymes involved in energy supply of cells. It is involved in carbohydrate, protein and fat metabolism; in the maintenance of normal visual function of the eyes and the synthesis of hemoglobin. Excreted by kidneys.

For therapeutic purposes, it is used for hypo- and ariboflavinosis, hemeralopy, conjunctivitis, iritis, keratitis, corneal ulcers, cataracts, radiation sickness, intestinal problems, eczema and other diseases.

Route of administration and dosage. Prescribed for an oral use. Adult dose is 0.005 - 0.01 g per day. In severe cases – 0.01 g 3 times / day.

Dosage forms. Tablets – 0.002 g, 0.005 g, 0.01 g It is included in the multivitamin complexes.

(4) Pyridoxine –

 vitamin B6. Priridoxol, pyridoxal, pyridoxamine. The approximate daily need is 1.6 mg.

Pharmacodynamics. Coenzyme forms – pyridoxal phosphate and piridoksaminphosphate. It is a part of the enzyme transaminase performing transamination, deamination and decarboxylation of amino acids. It is involved in the metabolism of histamine, vitamin B12 and folic acid. It is necessary for the formation of gamma-aminobutyric acid (GABA), serotonin, glycine. Used for anemia, leukopenia, nervous system diseases, pregnant toxicosis. In case of seborrheic dermatitis, herpes zoster, neurodermatitis, psoriasis, exudative diathesis. It decreases toxic manifestation of anti-TB drugs (isoniazide, Phthivazide).

Route of administration and dosage. Administered orally, subcutaneously, IM and IV. Oral therapeutic doses are 0.08 g 3 times / day. When receiving anti-TB drugs – 0,005 - 0.01 g per day to prevent neuritis and other complications.

Side effects. Allergic reactions (urticaria).

Drug interaction. Pharmaceutical: not be mixed in the same syringe with cyanocobalamine and thiamine. Pharmacodynamic: In the treatment of Parkinson's disease it should not be administered at the same time with levodopa, due to lower efficiency of the latter.

Dosage forms. Tablets – 0.002, 0.005, 0.01 g Included in the multivitamin complexes. 1%, 2%, 5% solutions in vials.

(5) Pyridoxal phosphate 

(Pyridoxal phosphatum) has a rapid therapeutic effect in case of resistance to pyridoxine. Highly effective for skin diseases (urticaria, eczema, neurodermatitis, psoriasis).

Route of administration and dosage. Taken orally or parenterally. Daily dose for adults is 0.04 - 0.16 g. SC, IM, IV – 0,005 - 0.01 g 3 times / day.

Dosage forms. Tablets – 0.01 and 0.02 g, the lyophilized powder for injection solutions in ampoules – 0,005 or 0.01 g

(6) Nicotinic acid 

(Acidum nicotinicum) vitamin PP, niacin. Vitamin B3. In the body it turns into nicotinamide. The daily requirement is 16 mg. Medications: Nicotinamide, nicotinic acid.

Pharmacodynamics. It forms coenzymes: nicotinamide adenine dinucleotide and nicotinamide adenine dinucleotide phosphate (NAD and NADP), which are a part of redox enzymes involved in the processes of biological oxidation, oxidative phosphorylation, carbohydrate and fat metabolism. It has a vasodilating effect.

It is used as a lipid-lowering drug. It reduces the level of triglycerides to a large extent, less – total cholesterol and LDL cholesterol, increases HDL cholesterol. For pellagra, diseases of the liver.

Route of administration and dosage. Oral administration (after eating) and parenteral. SC and IV introduction of nicotinic acid is painful. You can use nicotinamide. The maximum oral daily dose – 0.5 g, IV – 0.3 g

Side effects. Niacin, especially when taken orally can cause flushing of the face and upper body, dizziness, feeling the tides to the head, allergic urticaria, paresthesia. It can cause the development of hepatic steatosis, have hyperuricemic effect, reduce glucose tolerance.

Contraindications. Ulcer disease, liver dysfunction, gout and hyperuricemia.

Dosage forms. Tablets – 0,025, 0.05, 0.1, 0.5 g; tablets retard – 0,125, 0.25, 0.5, 1 g.1% solution in ampoules of 1 ml; 10% solution for injection.

Nicotinic acid is apart of the complex preparations: Nikoverin with papaverine, but with Nicospan with No-Spa, Xantinol nicotinat and picamilon. The action of these drugs is associated with a vasodilating action of nicotinic acid.

Enduracin is a prolonged dosage form of nicotinic acid. The course should be started with 1 tab. per a day (breakfast) and increased up to 3 times / day. Possible dose – 2-3 grams per day.

(7) Pantothenic acid, calcium pantothenate 

(Calcium Pantothenate) Vitamin B5. The daily requirement is 5 mg. The drug – calcium pantothenate.

Pharmacodynamics. It forms coenzyme A, an acceptor and transporter of acyl residues. It is nvolved in the biosynthesis of fatty acids and oxidation, oxidative decarboxylation of ketoacids, synthesis of corticosteroids and acetylcholine. Calcium pantothenate is used in pathological conditions associated with metabolic disturbances: polyneuritis, eczema, allergies, wounds, burns, trophic ulcers, pregnant toxicosis, chronic liver diseases, after operations on the gastrointestinal tract.

Pharmacokinetics. Well-absorbed from the GIT. In great amounts it is detected in the heart, liver, kidney, adrenals. Excreted in an unchanged form 2/3 – by kidneys, 1/3 – by intestines.

Route of administration and dosage. Administered orally, IM, IV. Oral administration – 0.1-0.2 g 2-4 times / day. Parenterally – 0.2-0.4 g (4.2 ml of a 10% solution and 1.2 ml of a 20% solution 1-2 times / day).

Dosage forms. Tablets of 0.1 g, 10% solution in vials for 2, 5, 10 ml. 20% - 2 ml. Calcium pantothenate is included into the composition of multivitamin complexes.

Dexpanthenol is a synthetic derivative of pantothenic acid. It turns into pantothenic acid.

Indications are the same as those of calcium pantothenate: wounds, burns, sores, trophic ulcer, dermatitis, radiation damage to the skin, intestinal atony, paralytic ileus. It is also used (Kornergel) in radiation, thermal, chemical burns of the conjunctiva and cornea, anterior eye injuries, erosive and dystrophic keratitis.

Route of administration and dosing. Local, oral and parenteral. The affected area of skin or mucosa is sprayed 3 - 4 times / day. The eye gel is put behind the eyelids 0.5 - 1 cm 3-6 times / day. Orally – sublingual tablets of 0.1 - 0.5 g / day. For the prevention of postoperative atony one uses SC, IM, IV 4ml 25% solution x 4 times / day.

Side effects. Dyspepsia and allergic reactions.

Dosage forms. Tablets – 0.1g; 25% solution in 2 ml ampoule; 5% ointment and cream in tubes of 30 g; 2.5% lotion in 200 and 400 ml vial; 5% eye gel in 5 and 10 g tubes.

(8) Pangamic acid 

(vitamin B15) and choline chloride – vitamin-like substances. There’s no avitaminosis at their deficiency.

Pharmacodynamics. They take part in biochemical processes as donators of methyl groups. The drug of pangamic acid – calcium pangamate. Calcium pangamate improves lipid metabolism, increases the absorption of oxygen by tissues, increases the amount of phosphocreatine in the muscles and glycogen in muscle and liver, removes hypoxia. Choline is a precursor of acetylcholine, and included into the composition of phospholipids.

Indications: liver disease, atherosclerosis, alcoholism, myocardial dystrophy, angina pectoris, hypothyroidism, cystinuria.

Routes of administration and dosing. Calcium pangamate is taken orally 0.05-0.1 g x 3-4 / day. Cholin chloride – orally 5 ml of 20% solution x 3-5 times / day. IV – with an IV drip – 1% solution on physiological solution or 5% glucose solution - 400 ml.

Side effects. Oral use of choline chloride occasionally cause dyspeptic symptoms. At the rapid IV introduction – sensation of heat, nausea and sometimes vomiting, bradycardia, decreased blood pressure. Associated with an activation of cholinergic systems.

Contraindications. Calcium pangamate – glaucoma, hypertension.

Dosage forms. Cholin chloride forms – powder; 20% solution in 10 ml ampoules; 1% solution. It is included into the composition of multivitamin complexes.

(9) Choline alfoscerate 

(glycerylphosphorylcholine hydrate) is a neuroprotective agent used in traumatic brain injury, dementia, and other disorders of the central nervous system.

Dosage forms. Capsules of 0.4 g orally 3 times / day. The course of 3-6 months. Solution for IM and IV administration (Gliatilin, Cerepro).

Lipoic acid (Acidum lipoicum).

Pharmacodynamics. Coenzyme that participates in the oxidative decarboxylation of pyruvic acid and α- ketoacid involved in energy formation. Antioxidant. It has lipotropic and detoxifying effects.

Indications. Neuropathy, including diabetic polyneuritis, disturbances of visual functions, intoxication. Liver disease, atherosclerosis.

Routes of administration and dosage. Orally (after eating) 0,025 - 0.05 g x 2-3 times / day. It can be administered IV – 0.5% solution of 2 ml ampoules. The drugs: Berlition, Thiogamma, Thioctacid, Espa-LIPON contain lipoic acid in 0.3 g capsules, tablets, 0.2, 0.3, 0.6 and 2.5%, 3% solutions for injections. Included in the multivitamin complexes.

(10) Lipamide 

(Lipamidum) is used as a hepatoprotector, for the treatment of atherosclerosis in diabetic polyneuritis. Better tolerated than lipoic acid.

Dosage form: tablets of 0.025 g.

(11) Ascorbic acid 

(Acidum ascorbinicum), vitamin C. Daily requirement is 60-100 mg.

Pharmacodynamics. It has pronounced restoring properties. It is involved in the metabolism of the main substance of connective tissue, provides permeability; in the metabolism of cholesterol, bile acids, corticosteroids, contributes to the accumulation of glycogen in the liver, stimulates immunity.

Indications. The drugs of vitamin C provide additional amount for the prevention and treatment of scurvy, hemorrhagic diathesis, infectious diseases - stimulates the immune system, liver diseases. In case of increased physical and mental work, pregnancy, lactation.

Route of administration and dosage. Oral (after eating), IM, IV. As a preventative measure – 0.05 - 0.1 g / day. Therapeutic doses orally – 0.1 - 0.2 g / day., Parenterally – 5-10% solution of sodium ascorbate 1-5 ml.

Side effects. It can cause irritation of the digestive tract, hyperprothrombinemia, disrupt the function of insular apparatus of the pancreas, contribute to the development of hyperglycemia, glycosuria, thrombocytosis, thrombus formation.

Drug interactions. Ascorbic acid increases blood levels of salicylates, penicillin, tetracycline. Decreases - oral anticoagulants. It improves the intestinal absorption of iron drugs. Calcium chloride, salicylates, glucocorticosteroids deplete vitamin C in the body.

Dosage forms. Tablets (dragees) – 0.05 g, 0.075 g, 0,1g. 5% and 10% solutions for injections in 1, 2 and 5 ml ampoules. It is included into the composition of multivitamin medications.

(12) Rutin 

(Rutinum), vitamin P. The daily requirement is 30-50 mg.

Pharmacodynamics. Decreases capillary permeability, inhibits aggregation and increases the elasticity of red blood cells.

Pharmacokinetics. When taken orally, 10-15% of the dose is absorbed. Cmax – 1-9 h. T1 / 2 - 10-25 h; excretion – with bile.

Indications. In the cases involving the disturbance of vascular permeability.

Dosage form. 0.02 g tablets.

Ascorutin (Ascorutinum) ate the tablets containing 0,05 g of Rutin and ascorbic acid and 0,2 g of glucose. 1 tab. 2-3 times/day.

Drugs of fat-soluble vitamins

(1) Retinol 

(Retinolum) vitamin A. The daily requirement – 0.8 - 1 mg (4000 - 5000 IU). Medications: retinol acetate, retinol palmitate.

It includes retinol (vitamin A), degidroretinol (vit. A2), retinal (retinene, vitamin A-aldehyde), retinoic acid (vitamin A-acid) and their esters and spatial isomers. Provitamins A - carotenoids (α-, β -, ɣ- isomers) in the body convert into vitamin A. β- carotene is wide-spread and it forms 2 molecules of vitamin A.

Pharmacodynamics. Retinol is a growth vitamin. It stimulates the synthesis of proteins, lipids, mucopolysaccharides, purine and pyrimidine bases. Involved in photoreception. It activates the immune system.

Indications. Prescribed for certain eye diseases: retinitis pigmentosa, xerophthalmia, gemerolapiya, Keratomalacia, conjunctivitis, eczematous lesions of eyelids. Skin lesions: frostbite, burns, ichthyosis, senile hyperkeratosis. In treatment of infectious diseases, rickets, malnutrition, acute respiratory infections, diseases of the gastrointestinal tract and liver.

Routes of administration and dosages. Vitamin A medications are prescribed for internal use, IM, topically (locally). Administered IM, solutions are to be warmed up to the body temperature. Therapeutic doses are up to 0.01 mg / day. In case of eye diseases – to 50,000 - 100,000 IU (0.02 mg / day).

Side effects. Hypervitaminosis is possible: drowsiness, headache, flushing, nausea, vomiting, irritability, disorders of gait, pain in the limbs. At the local administration – the formation of infiltrates.

Dosage forms. Retinol acetate dragee – 3300 IU (0.00114 g); tablets – 33000 IU (0.0114 g); solution in oil – 3.44% and 8.6%, in one drop – 3300 - 5000 IU / ml; 0.2 g capsules; solution for i / m injection 2,500 - 10,000 IU / ml.

Retinol palmitate in dragee – 3300 IU (0.00182 g) .It is included intot he composition of multivitamin complexes.

(2) Tocopherol (Tocopherol) – 

vitamin E. Daily requirement – 15 mg. 7 tocopherols, their isomers and synthetic derivatives, are known. The most active one is α- tocopherol. α- tocopherol acetate (alfa-Tocopherolacetate)

Pharmacodynamics. It suppresses peroxidation of lipids, has a hepatoprotective effect. It activates protein synthesis in tissues, spermatogenesis, immune system, heme synthesis and heme-containing enzymes, tissue respiration.

Indications. Muscular dystrophy, systemic diseases of muscle tissue, mensis disorders, menopause, decreased sexual function. Used in geriatric practice.

The routes of administration and in dosage. Orally and IM – 0.1 - 0.3 g / day.

Contraindications. Cardiosclerosis and myocardial infarction.

Dosage forms. Dragee – 0.15 g, 0.1; capsules – 0.1-0,5 g. 5%, 10%, 30% oil solution in 1 ml ampoules. Included in the multivitamin complexes.

(3) Calciferol (Calciferolum) – 

vitamin D. Includes ergocalciferol (vitamin D2) and cholecalciferol (vitamin D3). The daily requirement is about 10 micrograms (400 IU). Medications: ergocalciferol, cholecalciferol, calcitriol (the active metabolite) calcifediol.

Pharmacodynamics. In the body it undergoes oxidation in the liver and kidney to form 1,25 dioxycalciferol. Involved in the metabolism of calcium and phosphate, regulates bone mineralization.

Indications. Treatment and prevention of rickets, osteoporosis, including glucocorticoid osteoporosis; dysfunctions of parathyroid grands, bone diseases.

Side effects. Hypervitaminosis is possible.

Contraindications. Hypercalcemia, active forms of pulmonary tuberculosis, peptic ulcer disease, liver disease, kidney disease, organic heart disease.

Dosage forms. Dragee of ergocalciferol – 500 IU, oil solution in 500 and 1000 IU capsules. Colecalciferol B.O.N. – oil solution (200,000 IU / ml) for oral administration in vials of 10 ml and IM injections in 1 ml ampoules.