Method for treating the cases of osteoarthrosis
SUBSTANCE: method involves applying napkin impregnated with medicament to an injured articulation area. The medicament contains hydrocortisone acetate in the amount of 0.4mg/cm2, dimexide - 1.4 mg/cm2 and sodium alginate - 4.1 mg/cm2. The napkins are applied to internal and external side of the articulation for 6 days, changing them in three days.
EFFECT: accelerated treatment course.
The invention relates to medicine and can be used mainly during exacerbation of deforming osteoarthrosis (OA).
There is a method of treatment of osteoarthritis, including local therapy with nonsteroidal anti-inflammatory drugs in the form of ointment, cream or gel that is applied onto the skin in the area of the affected joint (Consilium medicum, 2001, Vol.3, No. 9, s).
The disadvantage of this method is that it requires frequent application, at least four, local means a day (and with active inflammation up to six times a day), because it is short. In addition, the elderly this method is ineffective because difficult the penetration of the drug through the skin.
The closest is a method of treating joint diseases, including osteoarthritis, including the laying of wipes their dialdehydes with immobilized trypsin containing Mexidol or Mexidol and copper followed by magnet (Patent RF №2195977, IPC A 61 N 2/04, publ. 2003).
The disadvantage of this method is that a number of patients due to contraindications cannot be applied magnetic therapy, to relieve pain syndrome usually need at least two weeks. In patients with severe degenerative changes of the joints, the effect may not occur.
The present invention is is to remedy these disadvantages by providing a more complete impact of drugs on the area of the affected joint, extend the relief of the inflammatory and painful manifestations.
For this purpose, the method of treatment of osteoarthritis, including the imposition of medicinal wipes at the area of the affected joint, it is proposed to use wipes that contain hydrocortisone acetate 0.4 mg/cm2, dimexide 1.4 mg/cm2and sodium alginate to 4.1 mg/cm2when this overlay napkins with the inner and outer sides of the joint for 6 days with the change in 3 days.
The combination of the proposed remedies, drawn on a napkin, lets you prolong the inflammation of the joint, to reduce pain, relieve swelling of the synovial membrane, cartilage, reduce the amount of synovial fluid, thereby to improve the function of the joint. The application of this method does not cause allergic reactions.
The implementation of the method is demonstrated on specific clinical examples.
Patient I., 68 years old, came with complaints of pain and swelling of the right knee joint. Pain increases with prolonged stay in an upright position, after prolonged exercise notes the appearance of pain in the night.
From the anamnesis it is known that pain in the right knee joint was first introduced 5 years ago after injury. Took painkillers, used topical ointments. 2 years ago due to the presence in Orinoko synovitis was conducted intra-articular injection of diprospan in the knee with a positive effect. In the past year pain became constant. The last 2 months - swelling of the right knee joint, limitation of movements.
Objectively, height 165 cm, weight 75 kg Skin and mucous regular color. Peripheral lymph nodes are not enlarged. Varicose veins of the lower extremities. Defigure right knee joint due to exudative changes. Limitation of motion in the knee joint due to pain. The borders of relative cardiac dullness is not increased. Heart sounds are clear, correct rhythm, the number of heartbeats 74 min in HELL 130/80 mm Hg auscultation of the lungs vesicular breathing, wheezing no. The abdomen is soft, painless on palpation. Liver, spleen not enlarged. Peripheral edema no.
During examination: hemoglobin 138 g/l, erythrocytes 4,91×10 /l, leukocytes 4,9×10 /l, ESR 15 mm/hour. In the biochemical analysis of blood all the indicators are within normal limits. Urinalysis and urine analysis according to Nechyporenko without pathology. ECG: sinus rhythm, the vertical position of the electrical axis of the heart. Ultrasound of internal organs: diffuse changes of a liver.
Radiography of the knee: a picture of gonarthrosis, Art. II ultrasound examination of the right knee: medial increase the density of the cartilage structures of the fibrous soft tissue changes. Lateral - con is URS articular surfaces fuzzy, synovium with symptoms of moderate hypertrophy, lockerooms fluid in the cavity of a joint.
Clinical diagnosis: Osteoarthritis with predominant impairment of the knee, St, TN-1. Varicose disease of the lower extremities.
The patient on the external and internal surfaces of the right knee joint were imposed wipes containing hydrocortisone acetate 0.4 mg/cm2, dimexide 1.4 mg/cm2and sodium alginate to 4.1 mg/cm26 days with the change in 3 days. Swipe supported in the wet state, moistening as drying water. The skin tissues were fixed with a bandage or adhesive plaster, with a napkin on top was placed a polyethylene film as a moisture retaining material.
On the background of using napkins were observed reduction in pain at rest and during movement in 2 days, reducing functional disability and swelling of the knee joint after 6 days. In addition, there was a positive dynamics of synovitis (clinical and ultrasound). The absence of pain and signs of inflammation of the joints were observed within 6 months.
Patient R., 71, appealed to the MHC of the Ministry of internal Affairs of the Russian Federation in April 2001 with complaints of swelling of the knee, pain with prolonged walking, while descending the stairs, sometimes a night of pain in the knee joints.
From the anamnesis and the known, for the first time the appearance of pain in the joints when the load began to notice about 10 years ago, took NSAIDs, ointments topically. 3 years ago began to notice swelling of the joints, the rheumatologist put dz. - deforming osteoarthrosis. Since 2000, intraarticular was introduced kenalog with good effect, but short-lived. In the last 4 months notes deterioration, manifested by increased pain and swelling of the knee joints.
About-but: amyotrophy of the quadriceps muscles of the thighs, more pronounced on the left. Swelling of the left hip joint, the movement in it is limited.
As a result of inspection: radiographic signs 2 tbsp. coxarthrosis.
DZ. Deforming spondylosis 2 tbsp., TN 2 tbsp.
Due to the presence of clinical and radiological signs of OA, secondary phenomena synovitis patient received a kit containing 2 wipes with active ingredient is hydrocortisone-acetate 0.4 mg/cm2.
Dynamic observation within 1.5 months showed that after using wipes with SC 0.4 mg/ cm2for 2 consecutive days reached a significant positive effect: a clinical and ultrasound dynamics of synovitis, pain at rest, the patient is not disturbed significantly decreased pain during movement. Needs taking painkillers also does not arise. Bornological increasing physical activity: it has become more a long time to walk, decreased difficulty when using public transport, almost stopped limping.
In the MHC of the interior Ministry in such methods treated 100 patients, 40 people with OA of the knee, 40 - with OA of the hip joints, 20 with OA of the shoulder joints with good therapeutic effect.
Complications during treatment and upon completion was not observed.
As a result of application of this method of treatment was able to significantly reduce the time of stay of the patient on the bed due to the rapid clinical effect, also, given the long action of the drug, to reduce the number of readmissions, reducing financial costs to the patient and his hospital stay.
The method of treatment of osteoarthritis, including the imposition of medicinal wipes at the area of the affected joint, characterized in that use wipes that contain hydrocortisone acetate 0.4 mg/cm2, dimexide 1.4 mg/cm2and sodium alginate to 4.1 mg/cm2at the same time impose a napkin with the inner and outer sides of the joint for 6 days with the change in 3 days.
FIELD: organic chemistry and pharmaceutical compositions.
SUBSTANCE: invention relates to new 3-(5)-heteroaryl-substituted pyrazoles of formula I , tautomers or pharmaceutically acceptable salt of compounds and tautomers. In formula R1 is hydride, piperidinyl substituted with methyl, lower alkyl optionally substituted with halogen, hydroxyl, lower alkylanimo or morpholino; R2 is hydride, lower alkyl, amino, aminocarbonylamino, lower alkylaminocarbonylamino, lower alkylsulfonylamino, aminosulfonylamino, lower alkylaminosulfonylamino; Ar1 is phenyl optionally substituted with one or more independently selected halogen; HetAr2 is pyridinyl with the proviso that R2 is not amino or n-propyl when HetAr2 is pyridinyl; and HetAr2 is not 2-pyriridinyl when R2 is hydrogen or lower alkyl. Compounds of formula I have kinase p38 inhibitor activity and are useful in pharmaceutical compositions for treatment of various diseases.
EFFECT: new effective kinase p38 inhibitors.
23 cl, 6 dwg, 1 tbl, 1 ex
SUBSTANCE: the present innovation deals with cyclosporin-containing and practically oil-free compositions being of immunosuppressive action. The composition contains a hydrophilic surface-active substance, a lipophilic component, a lipophilic surface-active substance and ethanol. As a hydrophilic surface-active substance this composition contains ether of fatty acid and polyoxyethylene sorbitane and product of either natural or hydrogenised castor oil and ethylenoxide; as a lipophilic component and lipophilic surface-active substance it contains ether of fatty acid and sorbitane. The suggested composition has been designed as a gelatinous capsule with solid covering. The present innovation solves the problem dealing with stability of galena compositions with cyclosporin: at treating with water the composition develops practically stable microemulsion.
EFFECT: higher efficiency of application.
11 cl, 2 ex
FIELD: organic chemistry, steroids, medicine, pharmacy.
SUBSTANCE: invention relates to 3-methylene-steroid derivative of the general formula (1):
wherein R1 means hydrogen atom (H), or in common with R3 it forms β-epoxide; or R1 is absent in the presence of 5-10-double bond; R2 means (C1-C5)-alkyl; R3 means βH, βCH3 or in common with R1 it forms β-epoxide; either R3 is absent in the presence of 5-10-double bond; R4 means hydrogen atom, lower alkyl; Y represents [H, H], [OH, H], [OH, (C2-C5)-alkenyl], [OH, (C2-C5)-alkynyl] or (C1-C6)-alkylidene, or =NOR5 wherein R5 means hydrogen atom (H), lower alkyl; dotted lines represent optional double bond. Compound can relate also to its prodrug used for treatment of arthritis and/or autoimmune diseases.
EFFECT: valuable medicinal properties of compounds, improved method for treatment.
38 cl, 1 tbl, 18 ex
FIELD: organic chemistry, biochemistry, medicine, pharmacy.
SUBSTANCE: invention relates to new aminobenzophenones of the formula (I):
or their pharmaceutically acceptable salts. These compounds elicit properties of inhibitors of cytokines secretion, in particular, 1β-interleukin (IL-1β) and tumor necrosis α-factor (TNF-α) and to secretion of polymorphonuclear superoxide that are useful for treatment of inflammatory diseases, for example, skin diseases, such as psoriasis, atopic dermatitis. In the formula (I) R1 is taken among the group consisting of halogen atom, hydroxy-, mercapto-group, trifluoromethyl, amino-group, (C1-C3)-alkyl, (C2-C3)-olefinic group, (C1-C3)-alkoxy-, (C1-C3)-alkylthio-, (C1-C6)-alkylamino-group, (C1-C3)-alkoxycarbonyl, cyano-group, carbamoyl, phenyl or nitro-group under condition that when R1 means a single substitute then it at ortho-position, and when R1 means more one substitute then at least one substitute of R1 is at ortho-position; R2 means one substitute at ortho-position being indicated substitute is taken among the group consisting of (C1-C3)-alkyl, (C1-C3)-alkoxy-group; R3 means hydrogen, halogen atom, hydroxy-, mercapto-group, trifluoromethyl, amino-group, (C1-C3)-alkyl, (C2-C3)-olefinic group, (C1-C3)-alkoxy-, (C1-C3)-alkylthio-, (C1-C6)-alkylamino-group, (C1-C3)-alkoxycarbonyl, phenyl, cyano-, carboxy-group or carbamoyl; R4 means hydrogen atom or (C1-C3)-alkyl; Q means a bond or -SO2-; Y means (C1-C15)-alkyl, (C3-C10)-carbocyclic group or phenyl being each of them can be substituted optionally with one or some similar or different substitutes designated by the formula R5; R5 means halogen atom, (C1-C4)-alkyl, amino-, (C1-C3)-alkoxy-group, (C1-C3)-alkoxycarbonyl or -COOH; X means oxygen or sulfur atom. Also, invention relates to a pharmaceutical composition and to a method for treatment and/or prophylaxis of inflammatory diseases.
EFFECT: valuable medicinal properties of compounds and composition.
9 cl, 2 sch, 2 tbl, 29 ex
FIELD: veterinary science.
SUBSTANCE: the suggested method should be implemented under conditions of experimental modeling dystrophic process due to intramuscular injection of glucosamine hydrochloride at the dosage of 15-25 mg/kg once or twice weekly for 1 mo. The method provides good effect in treating a lesion induced in the course of an experiment due to matching adequate dosages and a certain mode of injecting chondroprotector in animals.
EFFECT: higher efficiency of correction.
FIELD: veterinary science.
SUBSTANCE: the suggested method should be performed under conditions of experimental modeling dystrophic process due to intraosseous introduction of glucosamine hydrochloride at the dosage of 15-25 mg/kg 1-2 times weekly during a month. The method provides high local concentrations of medicinal preparation, at its steady entering the circulation by leaving aside hepatic barrier and, as a result, optimization of chondroprotector action of glucosamine hydrochloride and better treatment of articular alterations induced in the course of an experiment in animals.
EFFECT: higher efficiency of correction.
8 dwg, 1 ex