PANTOTHENIC ACID — N-(2,4-диокси-3,3-диметилбутирил) - beta alanine — water-soluble vitamin. From two of its optical isomerides only D (+) - isomer with [a] 25 D +37,5 ° (H 2 O) has vitamin properties. The main biologically active form P. to. HOCH pantheteine is 2 C (CH 3 ) 2 CH(OH)CONH(CH 2 ) 2 CONH(CH 2 ) 2 SH, to-ry in the form of the 4th '-phospho-pantheteine is a part of a coenzyme And, is prosthetic group of a polyfermental complex of a sintetaza fat to - t of various tissues of mammals (including a liver of the person) and the polyfermental complexes synthesizing antibiotics and also is a necessary growth factor of nek-ry types of lactobacilli, in particular bifidobacteria. P.'s biotransformation to. in a coenzyme And (KOA) it is carried out by hepatocytes and nek-ry other cells (see. Coenzymes ). With participation of KOA oxidation of fatty acids, oxidizing decarboxylation of ketonic acids, synthesis of citric acid, steroids, gem is carried out, there is intracellular and transmembrane transport of acid residues (acyls), activation of the last to education atsetil-KOA or atsil-KOA. Atsetil-KOA is a universal donor of acyl groups in reactions of acetylation of amines, aminosugars, amino acids. A special role is played by reaction of acetylation of sincaline, as a result the cut is formed acetylcholine — the most important mediator of synoptic transfer of nervous impulse. At last, with the help atsetil-KOA one of the main pairing reactions of desintoxication of an organism — acetylation of the arylamines, sulphamides derivative of isonicotinic acid etc. is carried out. The inactivation of alien aromatic carboxylic acids is carried out by peptide conjugation which mechanism consists in formation of KOA — derivative carboxylic acids. In particular, interaction of KOA-proizvodnogo of the benzoic acid (benzoil-KOA) and glycine with education benzaminoacetic to - you is used as the test for anti-toxic function of a liver (a one-stage prothrombin time test — Pytelya). The daily need for P. to. 10 — 12 mg. It increases (to 15 — 20 mg) at pregnancy, a lactation, hard physical work. The item to. it is eurysynusic in products of plant and animal origin (tab).
Table. Content of pantothenic acid in some food &produktakhnbsp; (&mgnbsp; %)
In a heat treatment process of products of loss of vitamin can reach 25 — 50% and above in this connection there can sometimes be its deficit in a human body. Development of a vitamin deficiency is possible also at disturbance of absorption or P.'s removal to. at long intoxications, hron, diseases went. - kish. path, cardiovascular system and kidneys, hormonal imbalance, long himio-and antibiotic treatment, repeated use of diuretics. The expressed P.'s insufficiency to. in a human body it is noted as a result of inadequate food in extreme conditions, at tuberculosis, alcoholism and some other diseases. Specific symptoms of insufficiency of P. to. at the person are not described. At diagnosis and assessment of degree of insufficiency of this vitamin it is necessary to investigate at the same time the level of a free and general form P. to. in daily urine, the content of polyneuramin to a blood plasma and also to calculate quantity it in food inspected for 2 days.
Quantitative definition of P. to. and its derivatives it is carried out by colorimetric reactions with 1,2-naphthoquinone-4-sulphonate or sodium hypochlorite (sensitivity 10 - 3 — 10 - 4 d), method of a gas liquid chromatography (10 - 6 — 10 - 7 ), by means of microbiological definition with use of test cultures (10 - 7 — 10 - 8 ) Saccha-romycodes ludwigii, Lactobacillus arabinosus, etc. Blood of the adult usually contains 17 — 38 mkg of % of P. to., with urine it is excreted per day totally in the form of various forms 5,5 — 6,2 mg of P. to., including 3 — 4 mg of free P. to. It is considered that excretion less than 2 mg of free P. to. with urine per day points out insufficient security of an organism with vitamin.
Drugs of pantothenic acid
Calcium pantothenate, Calcii pantothenas, is drug pantothenic to - you are (PACK ICE). It is white fine-crystalline powder, water soluble, malotoksichen; only at high doses and prolonged use the phenomena of dyspepsia (heartburn, nausea, vomiting) are noted, to-rye usually pass independently at decrease in a dosage. Contraindications for use are not described.
In intestines there is a dissociation of drug, and through a wall of intestines the PACK ICE gets already itself, and absorption happens quickly. Pharmakol, effect of calcium of pantothenate is caused by activity of PACK ICE anion. In turn and the PACK ICE is not biologically active substance yet; it gains the activity only as a part of KOA. Formation of KOA happens, apparently, in all fabrics, but is preferential in a liver; allocation for 60% is carried out by kidneys.
In therapeutic clinic of calcium pantothenate is applied at various disturbances of exchange processes; circulatory unefficiencies (in combination with cardiac glycosides); katara of upper respiratory tracts and bronchitis; allergic states (dermatitis, hay fever, bronchial asthma). It is effective at polyneurites, neuralgia, paresthesias. Drug is used for treatment of burns and trophic ulcers, and also for elimination of a postoperative atony of intestines. Calcium pantothenate is often applied to reduction of the toxic effects developing at prolonged use of the drugs containing arsenic, streptocides and PASK, drugs GINK and antibiotics of group of streptomycin.
It is appointed inside parenterally (subcutaneously, intravenously and intramusculary), and also locally. Inside appoint the adult 0,1 — 0,2 and 2 — 4 times a day; to children of 3 — 14 years on 0,1 — 0,2 g 2 times a day. A daily dose for adult from 0,4 to 0,8 g; for children it is not higher than 0,4 g. Parenterally adult enter 20% solution, no more than 4 ml a day. Duration of reception at oral and parenteral administration up to 4 months, depending on effect. Locally for lotions and rinsings 5% solution of calcium of pantothenate are appointed. At burns, trophic ulcers and inertly healing wounds 5% ointment of calcium of pantothenate are applied.
Drug is produced in tablets on 0,1 g and in ampoules on 2 ml of 20% of solution.
Pantogamum, Calcii homopantothenas; Pantogam. Like calcium to pantothenate dissociates and it is soaked up in the form of D-gomopantotenovoy to - you are (GPK). The mechanism of effect of drug is studied insufficiently. It is supposed, however, that pharmakol, effects of Pantogamum are caused by formation of a special coenzyme like KOA.
Has sedative and anticonvulsant properties. In a wedge, practice it is used at epilepsy and hyperkinesias (in particular at children), at parkinsonism, a tremor and a myoclonus, and also for treatment of complications after encephalitis. It is effective at treatment of children with a delay of intellectual development. In these cases Pantogamum appoint in a dose 0,5 g of 4 — 5 times a day within 3 months. Side effect and contraindications to use of Pantogamum are not described.
Drug is produced in tablets on 0,25 and 0,5 g
See also Vitamins .
Bibliography: Clinical pharmacology, under the editorship of V. V. Zakusov, page 353, M., 1978; Likhtsiyer I. B. is pirichev V. B. Pantothenic acid, in book: Vitamins, under the editorship of M. I. Smirnov, page 371, M., 1974; Moyseenok A. G. Pantothenic acid, Minsk, 1980; Chemistry, biochemical functions and use of pantothenic acid, under the editorship of A. G. Moyseenk, Minsk, 1977; Experimental vitaminology, under the editorship of Yu. M. Ostrovsky, page 267, Minsk, 1979; Decker K. Die aktivierte Essigsaure, Das Coenzym A und seine Acylderivate im Stoffwechsel der Zelle, Stuttgart, 1959; S z about y d at I. Die klinische Bedeutung der Pantothen-saure unter besonderer Berucksichtigung der Kinderheilkunde, Szeged, 1967, Bibliogr.; Vitamine, hrsg. v. J. Fragner, Bd 2, S. 1199, Jena, 1965.
A. G. Moyseenok; Ya. B. Maksimovich (pharm.).