Method for pharmacological correction of calcium deficiency in patients with osteoporosis

FIELD: medicine, therapy.

SUBSTANCE: simultaneously for 20 d one should prescribe calcium D3 two times daily in the morning and in the evening per 1 tablet or Beresh Plus drops. The quantity of drops for daily intake is equal to patients body weight in kg and they should be introduced in three stages during meals by drinking them up with sufficient amount of water. Application of the suggested method optimizes calcium exchange in patients with osteoporosis, enables to achieve earlier and more stable results in normalization of calcium content in bones by preventing, thus, osteoporotic fractures.

EFFECT: higher efficiency of pharmacological correction.

1 ex

 

The invention relates to medicine, namely to therapy.

It is known that the leading critical link osteoporosis is a disorder of calcium metabolism, insufficient intake in his body, in violation of his learning, as well as transporting the ionized form of calcium in bone tissue. Optimal drug absorption which maximum is calcium D3, containing calcium carbonate and active metabolites of vitamin D3, complementary deficiency of calcium and vitamin D3 and normalizing the metabolism of calcium and phosphorus in bone tissue (Case of medicines in Russia. Radar - the encyclopedia of drugs - 10th ed., revised and enlarged supplementary / Ed. Ufraw. - M.: radar - 2003. S).

It is also known that a significant role in biologically active reactions are not only vitamins and minerals, and trace elements. About 1/4 of all known enzymes for the manifestation of the full catalytic activity require the presence of micronutrients (Vitamins and trace elements in clinical pharmacology / edited Vasodilan. - M.: Paley-M, 2001. - S-250).

It is known that the most complete and best set of trace elements presented in the drug “Béres Drops Plus”, including in its membership the salts of iron, zinc, sodium, magnesium, manganese, potassium, copper, molybdenum, vanadium, Nickel, boron, fluorine, chlorine, cobalt, and Béres drops plus my IMM is nonodorous, complementary deficiency of micronutrients (Register of medicines of Russia. Radar - the encyclopedia of drugs - 10th ed., revised and enlarged supplementary / Ed. Ufraw. - M.:radar - 2003. S).

The technical result of the invention is to improve the effectiveness of treatment for normalization of calcium metabolism, reducing the degree of progression of osteoporosis to prevent fractures caused by the reduction of calcium in the bones.

The technical result is achieved by the fact that at the same time within 20 days appointed calcium D3 twice a day, morning and evening one tablet, sucking them or chewing during eating and Béres drops Plus, with the number of drops for daily intake is equal to the weight of the patient, but is applied in three steps during eating, drinking sufficient amount of water.

Example. Patient K., 1946 birth, suffers from generalized osteoporosis in rheumatoid arthritis seropositive polyarthritis, activity III, radiographic stage III, FN 2. The weight of the patient - 75 kg for two years every day takes 10 mg of prednisolone. The level of blood calcium 1.8 mmol/l Drinking within two weeks of calcium D3 has not changed much calcium in the blood, it was 1.9 mmol/l Within 20 days of the patient K. was appointed calcium D3 in the same dose in combination with Béres drops Plus 25 drops twice a day during meals. The level of blood calcium returned to normal on day 6 of admission, accounting for 2.8 mmol/l, remained constant during the whole period of admission, but in the subsequent month.

The use of the proposed method optimizare calcium metabolism in patients with osteoporosis, thus allowing for earlier and more stable results in the calcium content in the bones, preventing osteoporosis-related fractures.

How pharmacological correction of calcium deficiency in patients with osteoporosis, including the appointment of the drug Calcium D3 2 times a day morning and evening 1 tablet during the meal, characterized in that it further assigned Béres drops Plus in the amount equal to the weight of patient in kg divided by 3 divided doses during the meal the course of 20 days.



 

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FIELD: organic synthesis.

SUBSTANCE: invention provides compounds of general formula I:

, where R1 represents -CO-Ra, -SO2-Rb, or aryl optionally substituted by lower alkoxy, wherein Ra represents cycloalkyl, cycloalkyl(lower)alkyl, cycloalkyloxy, aryl, aryloxy, aryl(lower)alkyl, aryl(lower)alkoxy, aryloxy(lower)alkyl, aryl-S-(lower)alkyl, aryl(lower)alkenyl, provided that aryl group can be optionally substituted by halogen, lower alkyl, hydroxy, nitro, cyano, lower alkoxy, phenyl, CF3, cyano(lower)alkyl, lower alkyl-C(O)NH, lower alkyl-CO, and lower alkyl-S; heteroaryl, heteroaryl(lower)alkyl, or heteroaryl(lower)alkoxy, provided that heteroaryl group is 5- or 6-membered ring or bicyclic aromatic group constituted by two 5- or 6-membered rings including 1-3 heteroatoms selected from oxygen, nitrogen, and sulfur and that heteroaryl group can be optionally substituted by lower alkoxy; Rb represents aryl, aryl(lower)alkyl, or heteroaryl, aryl group optionally substituted by halogen, cyano, or lower alkyl-C(O)NH; R2 and R3 represent hydrogen atoms; R4 representshydrogen or lower alkyl; R5 represents hydrogen, lower alkyl, cycloalkyl, benzodioxyl, or aryl optionally substituted by lower alkyl, halogen, lower alkoxy, hydroxy, or (lower)alkyl-C(O)O; n is 1 or 2; and pharmaceutically acceptable salts thereof and/or pharmaceutically acceptable esters thereof. Invention also provides a pharmaceutical composition exhibiting inhibitory activity with regard to cysteine proteases of the cathepsin family, which composition comprises compound of formula I, pharmaceutically acceptable recipient, and/or adjuvant.

EFFECT: increased choice of cysteine protease inhibitors.

34 cl, 1 tbl, 13 ex

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Formula 1

where X = -O - or-S- ; m = 1, 2, 3; R1and R2-H or alkyl; R4-H; R5Is H, OH or R4and R5together form a double 16, 17 connection, R3- YR8where Y is-O - or-S-,

R8-H, alkyl, possibly substituted by F or cycloalkyl, or-NR9R10where R9and R10-H, alkyl, possibly substituted by F or cycloalkyl, R6-OH, possibly substituted, R7-H or a protective group

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