The use of dhea in the treatment of delays adrenarche
(57) Abstract:The invention relates to medicine. A method of treatment delays adrenarche using DHEA. The method provides normalization of hormone levels until age norms, while there is a strong effect. The invention relates to the field of medicine and relates to drug treatment of patients with delay of adrenarche, due to insufficient production of androgens by the adrenal cortex.Activation of androgen adrenal function in prepubertal period or adrenarche is a physiological mechanism preceding and contributing to the normal development of puberty.Decreased production of adrenal androgens in the cortical layer of the adrenal gland is a common condition and leads to a delay in sexual development.Information about treatment with dehydroepiandrosterone delays adrenarche in the known literary sources are not available.The aim of the invention is to identify the possibility of using DHEA for the treatment of delays adrenarche.The prototype method is presented in the article Dehydroepiandroster8, V 45, pp.1011-1015. In it the authors prescribe DHEA adolescents 15-18 years of age with obesity sublingually twice a day for 40 mg for 8 weeks.Based on this methodology, we developed a method of treatment delays adrenarche.The essence of the proposed method is as follows: when the delay of adrenarche sublingual assigned alcoholic solution of DHEA at a dose of 25 mg 2 times a day (morning and evening) to normalize the levels of DHEA and DHEA sulfate (DHEA-S).The effectiveness of the proposed method was confirmed in stationary conditions on volunteers and with the consent of their parents. The experiment involved 14 boys and girls aged 9 to 10 years with a decrease in the secretion of DHEA and DHEA From the adrenal glands, alerted its new form of medical treatment. They received sublingual alcohol solution degidroepiandrosterona in the dosage of 25 mg in the morning and evening to normalize the levels of DHEA and DHEA-s in basal blood continuously for 3 months.Control surveys hormonal status after 6 and 12 months 12 was normalized secretion of DHEA and DHEA-S, increasing to normal levels is the first drug treatment delay adrenarche, manifested by decreased secretion of DHEA and DHEA-S, has enabled us to implement it in daily practice since 1996.To date, the national Center for Human Reproduction by this technique have been treated for more than 40 patients. Liaising with 26 patients and their parents, we can talk about more than 80% of the success of the treatment. A new treatment has provided a lasting effect for a period of not less than 3 years (time of observation).Example 1. The boy's parents L. 10 years, the history N 1847, addressed to the Center 23.5.96 with complaints about lag in physical development of the child from their peers. In the examination Center: height 140 cm, weight 33 kg, absent pubic and axillary hair growth, we found a decrease in the basal level of LH - 1,3 IU/l, FSH 0.6 U/l, T of 1.1 nmol/l DHEA - 320 nmol/l DHEA-With 10 nmol/L. Child was assigned therapy DHEA 25 mg daily 2 times a day for 5 months. During the control study at the end of treatment was determined by the increase to age-related norms level of LH, FSH, T, DHEA, DHEA-S, the appearance of axillary and pubic body hair growth, growth increased to 144 cm, weight 38 kgSubsequent observation of the patient showed normal puberty.
ski development of the child from their peers. When surveyed in the Centre we found a decrease in the basal level of LH 1,2 U/l, FSH 0,5 IU/l, DHEA - 270 nmol/l DHEA-4.7 nmol/l, reduced growth and body weight. The child was assigned therapy DHEA 25 mg 2 times a day every day for 10 months. During the control study, basal levels of DHEA and DHEA-compliance is determined by the levels of hormones age norms, there is an increase in growth and body weight.Puberty in subsequent proceeded without features.Example 3. The boy's parents L. 10 years, the history N 1754, addressed to the Center with complaints of lag in physical development of the child from their peers. In the examination Center: height 142 cm, weight 38 kg, we found a decrease in basal levels of DHEA - 474 nmol/l DHEA-3.8 nmol/L. Child was assigned therapy DHEA 25 mg daily 2 times a day for 5 months. Treatment was accompanied by the appearance of axillary and pubic body hair growth, increased growth and body weight. During the control study, basal levels of DHEA and DHEA-s through 3 months, 6 months compliance is determined by the levels of hormones age norms, there was an increase in growth and body weight at puberty was proceeding without deviation.Pramodini). Analysis of patent scientific-practical medical literature has shown that information about the use of DHEA for the treatment of delays adrenarche missing. On this basis, the applicant considers that the proposed method of treatment delays adrenarche meets the requirements of the invention. Treatment delays adrenarche, characterized in that is used for this alcoholic solution of DHEA sublingual dosage 25 mg 2 times a day to normalize levels of dehydroepiandrosterone and dehydroepiandrosterone sulfate.
R2IS-H, -OH, -O(C1-C4alkyl), EA6H5, CCA(C1-C6alkyl) , -OSO2(C2-C6alkyl), or halogen; R3- 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino or 1 hexamethyleneimino; n = 2 or 3; Z Is-O - or-S-, or their pharmaceutically acceptable salts
SUBSTANCE: method involves administering selective modulator of steroid sex hormones being in particular compounds of general formula(I) and some quantity of steroid sex hormones precursor selected from a group composed from dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-en-3β,17β-diol and compounds in vivo transformable into one of cited precursors. Bisphosphonates combined with selective estrogen receptor modulators and/or steroid sex hormones precursor are additionally introduced for medically treating and/or inhibiting osteoporosis progress.
EFFECT: enhanced effectiveness of treatment; excluded adverse side effects.
41 cl, 13 dwg, 4 tbl
SUBSTANCE: a patient with systemic lupus erythematosus (SLE) should be prescribed to apply efficient quantity of pharmaceutically active form of dehydroepiandrosterone (DHEA) and then, after prescription it is necessary to detect the values for disease activity and total symptoms of the process that characterizes SLE-patient's state, such as: index of SLE activity (IASLE), degree of SLE activity (DSLE), patient's visual analog scale (VAS) and coefficient of Krupp's severity degree (CSDK) to determine the difference between these above-mentioned values obtained before treatment and those taken during therapy, moreover, the decrease of three out of these four values or either the decrease of stabilization or the increase being not higher than by 5% in the fourth value shows that patients reacts to the intake of DHEA.
EFFECT: higher efficiency of therapy.
13 cl, 1 dwg, 8 tbl
FIELD: organic chemistry, steroids, medicine, chemical-pharmaceutical industry.
SUBSTANCE: invention relates to an agent exhibiting structure 7β-hydroxyepiandrosterone or 7β-dehydroepiandrosterone, or their pharmaceutically acceptable esters of the structural formula (I) used for protection of neurons against their damages. Compounds elicit high effectiveness and bioavailability.
EFFECT: valuable medicinal properties of compounds.
15 cl, 3 dwg, 3 tbl, 22 ex
SUBSTANCE: disclosed is application of 7-hydroxyepiandrosteron as active agent for protection from acute or chronic neuron damage caused by hypoxia, ischemia, stroke, brain trauma, Alzheimer's disease, Parkinson's disease, or spinal cord damage. 7-Hydroxyepiandrosteron increases number of pyramidal cell survivor after ischemia or hypoxia.
EFFECT: new agent with neuroprotective activity.
6 cl, 1 dwg, 2 tbl, 8 ex
SUBSTANCE: invention refers to medicine, namely to gynaecology and represents the combination for preparing the medical product, containing Anastrozol, Levonorgestrel and Ethynyl Estradiol, the pharmaceutical composition for endometriosis treatment containing Anastrozol, Levonorgestrel and Ethynyl Estradiol and endometriosis treatment method that involves introduction of Anastrozol, Levonorgestrel and Ethynyl Estradiol.
EFFECT: invention provides effective temporary symptom relief in women with severe endometriosis.
3 cl, 2 tbl
SUBSTANCE: invention claims compounds of the formula , where R1, R2, R3 and R4 are equal or different, and each element is oxo group, hydroxy group, mercapto group, hydrogen atom, halogen atom, alcoxy group or aryloxy group, and dot line shows possible simple or double link between one or respective hydrogen atom pairs; and their complex ethers, which can be injected transcutaneously.
EFFECT: most efficient application in plaster form, preferably with adhesive substance containing copolymer of 40-60 wt % of metoxyethylacrylate, 30-40 wt % of laurylacrylate or laurylmethylacrylate and 10-25 wt % of polar monomer.
18 cl, 7 tbl, 5 ex
SUBSTANCE: invention relates to medicine, namely to psychiatry and gynecology, and can be used in treatment of endometriosis in women with anxiety-and-depressive disorders. For this purpose one month after performing laparoscopy at the background of drug hormonal treatment during 6 months phenotropil in dose 100 mg/day is additionally administered for 90 days.
EFFECT: administration of phenotropil in said dose and introduction regimen makes it possible to reduce anxiety-and-depressive symptoms, and has positive impact on functional state of immune and vegetative nervous system.
4 tbl, 3 ex
7FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a combination of a co-drug (an auxiliary) and a compound o formula (IV) in which radicals and symbols have the values defined in cl. 1 of the patent claim, or salts, or tautomers, or N-oxides, or solvates of this compound; where the specified auxiliary is specified from a monoclonal antibody, an alkylating agent, a malignant growth agent, other cycline-dependent kinase (CDK) inhibitor and a hormone, a hormone agonist, a hormone antagonist or a hormone-modulating agent specified in cl. 1 of the patent claim. The offered combination is used for tumour cell growth inhibition.
EFFECT: invention also refers to a pharmaceutical composition based on the offered combination, application of the combination and its separate ingredients and methods of treating, preventing and relieving the cancer symptoms in a patient.
77 cl, 2 dwg, 8 tbl, 257 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to pharmaceutics and medicine and concerns using 7α-hydroxy-epiandrosterone or 7β-hydroxy-epiandrosterone for preparing a drug for an inflammatory state specified in inflammation, inflammation disease of peripheral organs specified in liver or kidneys, inflammation respiratory disease, diabetes mellitus, inflammation-associated pain, inflammatory skin disease, multiple sclerosis, rheumatoid arthritis, osteoarthritis and complications thereof.
EFFECT: development of the drug preparation for the inflammatory state.
4 cl, 18 tbl, 7 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: there are described steroid compounds showing higher metabolism resistance and higher water solubility, as well as methods for preparing them.
EFFECT: substances are applicable for producing pharmaceutical preparations used for treating CNS disorders associated with steroid functions or caused by steroid action, as well as according to methods for prevention, relief or treatment of said disorders.
9 cl, 19 ex, 7 tbl
FIELD: veterinary science.
SUBSTANCE: a sow should be twice injected with oxytocin and, additionally, intramuscularly about 2-4 h after afterbirth detachment one should introduce clathroprostin at the dosage of 1 ml. The innovation suggested is very efficient in preventing metritis-mastitis-agalactia and endometritis in sows, as well.
EFFECT: higher efficiency of prophylaxis.
1 ex, 1 tbl
FIELD: medicine, gynecology.
SUBSTANCE: the present innovation deals with carrying out hormone-substitution therapy in women during menopause period or in sterilized women. For this purpose the above-mentioned therapy consists of the phase of relative dominant estrogen activity including three daytime dosages of a substance inducing estrogen activity being equivalent to approximately to 1 mg 17beta-estradiol daily, and the phase of relative dominant progestogen activity including combination of a substance inducing estrogen activity being equivalent to approximately 1 mg 17beta-estradiol daily and a substance that demonstrates progestogen activity being equivalent to approximately 90 mcg norgestimate daily. To fulfill such a therapy a pharmaceutical preparation is, also, suggested and a set of mentioned preparations. The innovation provides maximal weakening the symptoms of the disease, in particular, congestions along the safety of application due to decreased risk of known complications of estrogen therapy.
EFFECT: higher efficiency of therapy.
31 cl, 1 dwg, 1 ex, 2 tbl
FIELD: organic chemistry, pharmacy.
SUBSTANCE: invention relates to a new derivative of bicyclic heteroaromatic compound of the general formula (I) or its pharmaceutically acceptable salt eliciting agonistic activity with respect to luteinizing hormone (LH). Compounds can be used for preparing medicinal agents for control ability for conception. In compounds of the general formula (I) R1 represents R7 wherein R7 represents (C6-C10)-aryl optionally substituted with halogen atom at ortho- and/or meta-position; NHR8, OR8 wherein R8 means (C1-C8)-alkyl that can be substituted with halogen atom, (C1-C8)-alkylcarbonyl, (C1-C8)-alkylcarbonyloxy-group, phenyl, (C6-C10)-arylcarbonylamino-group, 5-methyl-2-phenylimidazol-4-yl, (C6)-heterocycloalkyl wherein 1-2 heteroatoms are taken among nitrogen and oxygen atoms, ethyloxycarbonylmethylthio-(C1-C4)-alkoxy-group, amino-group, (C6-C7)-heteroaryl; or (C5-C6)-heteroaryl comprising nitrogen, oxygen or sulfur atom as a heteroatom; R2 represents (C1-C8)-alkyl or (C6-C10)-aryl optionally substituted with one or more substitutes taken among (C1-C8)-alkoxy-group; or (C5-C6)-heteroaryl comprising nitrogen, oxygen or sulfur atom as a heteroatom; R3 represents (C1-C8)-alkyl possibly substituted with (C6-C14)-aryl possibly substituted with halogen atom, (C1-C4)-alkoxy-group, (C1-C4)-alkoxycarbonyl, mono- or tri-(C6-C10)-cycloalkyl, (C6-C10)-aryl, (C5-C6)-heteroaryl comprising nitrogen, oxygen or sulfur atom as a heteroatom; (C5-C7)-heterocycloalkyl comprising 2 heteroatoms taking among nitrogen or oxygen atom; (C3-C8)-cycloalkyl, (C2-C7)-heterocycloalkyl comprising 2 heteroatoms taking among nitrogen or oxygen atom; or (C6-C10)-aryl optionally substituted with one or more substitutes taken among (C1-C8)-alkoxy-group; X represents sulfur atom (S) or N(R4); Y represents nitrogen atom (N); R4 represents (C1-C8)-alkyl, phenyl-(C1-C8)-alkyl; or X represents sulfur atom (S), and Y represents CH; Z represents NH2 or OH; A represents sulfur (S), oxygen atom (O) or a bond. Also, invention relates to a pharmaceutical composition.
EFFECT: valuable properties of compounds and composition.
14 cl, 1 tbl, 119 ex
FIELD: pharmaceutical industry.
SUBSTANCE: pharmaceutical form contains (i) peptides with aggregation tendency in the form of their salts: acetates, gluconates, glucuronates, lactates, citrates, benzoates, or phosphates, which are dissolved of dispersed, and (ii) acids corresponding to above-listed salts.
EFFECT: lowered aggregation tendency and improved release of active substance resulting in improved bioavailability of peptide active substances.
22 cl, 9 tbl, 3 ex
SUBSTANCE: invention relates to method for treatment, prevention and alleviation of testosterone deficit development; or symptoms associated with testosterone deficit in mammalian females. Claimed method includes application of gel containing (wt.%) testosterone 0.1-10; isopropylmyristate 0.1-5 %; ethanol 98 % or less; and thickening agent 0.1-5 % on skin of subject.
EFFECT: convenient method for maintenance of daily reproducible testosterone levels.
8 cl, 5 tbl, 4 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel derivatives of benzimidazole of the general formula (I): wherein A represents -CH2- or -C(O)-; Y represents -S- or -NH-; R1 and R2 represent independently hydrogen atom, (C1-C8)-alkyl, (C5-C9)-bicycloalkyl optionally substituted with one or some similar or different (C1-C6)-alkyl radicals, or radical of the formula -(CH2)n-X wherein X represents amino-group, (C3-C7)-cycloalkyl and other values of radicals also given in the invention claim; R3 represents -(CH2)p-W-(CH2)p'-Z3 wherein W3 represents a covalent bond, -CH(O)- or -C(O)-; Z3 represents (C1-C6)-alkyl, aryl radical, heteroaryl and other values of radical also; V3 represents -O-, -S-, -C(O)-, -C(O)-O-, -SO2- or a covalent bond; Y3 represents (C1-C6)-alkyl radical optionally substituted with one or some halogen-radicals, amino-group, di-((C1-C6)-alkyl)-amino-group, phenylcarbonylmethyl, heterocycloalkyl or aryl radicals; p, p' and p'' represent independently a whole number from 0 to 4; R4 represents radical of the formula: -(CH2)s-R''4 wherein R''4 represents heterocycle comprising at least one nitrogen atom and optionally substituted with (C1-C6)-alkyl or aralkyl, and other values of radicals given in the invention claim also. Also, invention relates to a pharmaceutical composition showing antagonistic property with respect to GnRH and based on these compounds. Also, using above proposed compounds for preparing a medicament is considered. Invention provides synthesis of novel compounds, preparing pharmaceutical composition and medicament based on thereof in aims for treatment of such diseases as endometriosis, fibroma, polycystic ovary, breast, ovary and endometrium cancer, gonadotropic hypophysis desensitization in medicinal stimulation of ovary in fertility treatment in females.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.
18 cl, 2 tbl, 538 ex
FIELD: chemistry of peptides, medicine, drugs, pharmacy.
SUBSTANCE: invention relates to pharmaceutical compositions containing polymer of lactic and glycolic acids with the ratio of average molecular mass and medium-numbered molecular mass about 1.90 or less, or its salt and physiologically active peptide as agonist of LH-RH of formula: 5-oxo-Pro-His-Trp-Ser-Tyr-Y-Leu-Arg-Pro-Z (I) wherein Y means D-Leu, D-Ala, D-Trp, D-Ser (tBu), D-2-Nal or D-His; Z means HN-C2H5 or Gly-NH2 or its salt, in particular, peptide of the formula: 5-oxo-Pro-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NH-C2H5 (II) or its acetate, and to polymer of lactic and glycolic acids with the ratio of average molecular mass and medium-numbered molecular mass about 1.90 or less. Also, invention relates to a method for preparing indicated polymer and to a microsphere containing indicated polymer and peptide of the formula (II), and to a medicinal agent used in prophylaxis or treatment of prostate cancer, prostatomegaly, endometriosis, uterus myoma, metrofibroma, premature sexual maturation and dysmenorrhea, or for a contraceptive agent comprising indicated microsphere, and to methods for prophylaxis or treatment of indicated diseases. Invention provides preparing compositions with delayed release and containing physiologically active substance of peptide nature and providing the stable rate of release of active substance for the prolonged period (up to 1 month) in inhibition of high initial release of indicated active substance.
EFFECT: improved preparing method, valuable medicinal properties of composition.
37 cl, 4 tbl, 9 ex