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Godovan V. V. Pharmacology.2.Pdf V. V. GODOVAN PHARMACOLOGY IN PICTURES AND SCHEMES Vladlena Vladimirovna Godovan belongs to a new generation of the Odessa school of pharmacologists and clinical pharmacolo gists headed by a Corresponding Member of the National Academy of Medical Sciences of Ukraine, Honoured Worker of Science and PHARMACOLOGY Technology of Ukraine, professor V. I. Kre syun. Vladlena Vladimirovna occupies a pro minent place in it. Doctor of medical sci IN PICTURES AND SCHEMES ences, professor of the General and Clinical Pharmacology Department, dean of the Medical faculty of the Odessa National Medical University, scientific secretary of the Odessa department of the Ukrainian Pharma In 2 volumes cologists Association, a leading research worker of the State Expert Center of the Ministry of Health of Ukraine, scientific sec retary of a specialized council. Basic direc Volume 2 tions of her scientific activity are search and creation of drugs on the basis of natural metabolites of a human organism, including coordinating compounds of germanium with bioligands; elaborations in the field of clinical pharmacology of hepatoprotectors and drug usage safety. She is an author of more than 300 scientif ic works, including 2 monographs, 35 training handbooks, manuals, dictionaries in Uk rainian, Russian and English, 18 patents of Ukraine and certificates of authorship. The ODESSA NATIONAL 2 MEDICAL UNIVERSITY V. V. Godovan PHARMACÎLÎGY IN PICTURES A N D SCHEMES In 2 volumes Volume 2 Edited by a fellow of the NAMS of Ukraine, MD, professor V. I. Kresyun Оdessа The Odessa National Medical University 2011 UDC 615.015(075.8) BBC 52.81я73 Author: V. V. Godovan Reviewers: The head of the Pharmacology Department of the Lugansk State Medical University of MH of Ukraine, Honoured Science and Technology Worker of Ukraine, MD, professor V. D. Lukyanchuk The head of the Department of Experimental and Clinical Pharmacology with Clinical Immunology and Allergology of the Higher State Educational Establishment of Ukraine “The Ukrainian Medical Stomatological Academy” of MH of Ukraine, Honoured Science and Technnology Worker of Ukraine, MD, professor V. N. Bobyryov Translated from Russian after the edition : Годован В. В. Фармакология в рисунках и схемах : в 2-х томах / В. В. Годован. — Одесса : Одес. гос. мед. ун-т, 2009. — Т. 2. — 276 с. У даному пораднику, що складається з двох томів, відображені питання загальної та спеціальної фармакології, стисло викладена історія створення лікарських засобів, подаються сучасні класи- фікації фармакологічних груп, узагальнені дані про фармакокіне- тику, фармакодинаміку і фармакотоксикодинаміку ліків, які засто- совуються у сучасній медичній практиці. Матеріал висвітлений в інтеграції з іншими медико-біологічними та клінічними дисципліна- ми. Особливо, унікальне місце у виданні посідає схематичний ви- клад механізмів дії лікарських засобів та їх ефектів, що розвива- ються в результаті цього. Recommended by Scientific Council of the Odessa State Medical University (Proceedings N1 from 01.09.2008). © В. В. Годован, 2009 © Одесcкий государственный медицинский университет, 2009 © V. V. Gоdоvan, 2011 ISBN 978-966-443-019-4 (рус.) © The Odessa National Medical ISBN 978-966-443-045-3 University, 2011 2 Part V DRUGS AFFECTING METABOLISM Topic 18 HORMONAL DRUGS OF POLYPEPTIDE AND AMINOACID STRUCTURE. ANTIHORMONAL DRUGS NEUROHUMORAL REGULATION Hypothalamus inhibitor- releasing- factor factor Types of hormonal therapy: Pituitary • substitutive • stimulating hormone of • inhibiting endocrine trope pharmacodynamic gland hormone • • diagnostic Endocrine gland 3 CLASSIFICATION OF HORMONAL DRUGS (by chemical structure) ♦ Substances of protein and polypeptide structure — drugs of hormones of hypothalamus, pituitary, epiphysis, parathyroid and pancreas ♦ Derivatives of amino acids — drugs of hormones of thyroid gland, adrenal medulla ♦ Steroidal compounds — drugs of hormones of adrenal cortex and gonadal hormones, prostaglandins MECHANISMS OF HORMONES ACTION Polypeptide and Steroid amino acid hydro- testo- cortisone sterone Gs (+) adenylate cyclase Gi (-) АТP recep- cAMP tors Protein kinase • membrane permeability • lipolysis • glucogenolysis DNA • secretion • ↓ or ↑ iRNA and protein • movement of iones • effects (catabolism or • synthesis of substances anabolism) 4 DRUGS OF HYPOTHALAMIC AND PITUITARY HORMONES Statins: hypothalamus Liberins: prolactostatin corticoliberin somatostatin thyroliberin melanostatin prolactoliberin somatoliberin neuro- adeno- melanoliberin vasopressin pituitary pituitary gonadorelin oxytocin melanocyte- stimulating adreno- somato- thyro- pro- gonadotropic: tropic tropic tropic lactin follicle-stimulating (FSH), luteinizing (LH) cortico- somato- Т3, Т4 mammary sexual steroids medins glands glands DRUGS OF HYPOTHALAMIC HORMONES Hormones Drugs Stimulators of secretion Somatotropin-releasing hormone Sermorelin, somatoliberin Corticotropin-releasing- CRH hormone (CRH) Thyrotropin-releasing- Protirelin (rifatiroin) hormone Gonadotropin-releasing- Gonadorelin, leuprolid, hormone nafarelin, etc. Inhibitors of secretion Somatotropin-inhibiting- Somatostatin, octreotide, hormone lantreotide Different Danasole, bromcriptin 5 DRUGS OF HYPOTHALAMIC HORMONES Drugs Indications Stimulators of secretion Sermorelin, Diagnosis of somatotropic hormone somatoliberin deficit Corticotropin- Diagnosis of Cushing’s syndrome; releasing hormone stimulating therapy after prolong glucocorticoids usage Protirelin Diagnosis of hyper-, hypothyroidism; (rifathyroin) Treatment of thyroid gland carcinoma Gonadorelin, 1. Diagnosis of hypogonadism leuprolid, 2. Therapy: nafarelin, etc. • stimulating: hypogonadism, cryptorchism, delay of pubescence • inhibiting: prostatic cancer, uterine fibrosis, endometriosis, polycystic ovary, premature pubescence DRUGS OF HYPOTHALAMIC HORMONES Drugs Indications Inhibitors of secretion Somatostatin, • Inhibiting therapy: acromegaly, tumours of the octreotide, gastroenteropancreatic endocrine system, lantreotide tumours with the hyperproduction of vasoactive intestinal peptide, glucagonom, gastrinom, tumours with hyperproduction of somatoliberin, resistant diarrhea in AIDS patients Bromcriptin • Inhibiting therapy: prolactinoms, conditions related to hyperprolactinemia (amenorhea, galactorrhea, infertility, hypogonadism, etc.); for depression of lactation in period after abortion, births • As dopaminomimetic: for treatment of parkinsonism, with cocaine abstinence 6 DRUGS OF PITUITARY HORMONES Hormones Drugs Anterior lobe Somatotropic Somatotropin, somatrem ACTH Corticotropin and its synthetic analog — tetracosatrin (cinacten-depot, cosyntropin) Thyreotropic Thyreotropin Gonadotropic FSH (urofollitropin, follitropin-alpha and beta), FSH+LH (menopausal human gonadotropin or menotropin), similar to LH from placenta (human chorionic gonadotropin) Prolactin Lactin Medium lobe Melanotropic Intermedin Posterior lobe Oxytocin Oxytocin Vasopressin Desmopressin, terlipressin DRUGS OF PITUITARY HORMONES Drugs Pharmacodynamics/Indications Somatotropin, Metabolic effect (primarily insulin-like action, then somatrem insulin-antagonistic); anabolic: growth of bones and muscles, ↑ glycogen in them, etc. Replacement therapy: deficit of growth hormone in children (pituitary dwarfism) Pharmacodynamic: (?) osteoporosis, delayed wound healing, burns Corticotropin, its Formation and secretion of corticosteroids with synthetic analog adrenal cortex — tetracosatrin Stimulating therapy: hypofunction of adrenal cortex (tetracosactide, with prolong usage of glucocorticoids cinacten-depot, cosyntropin) Diagnosis: adrenal insufficiency; congenital adrenal hyperplasia, etc. 7 DRUGS OF PITUITARY HORMONES Drugs Pharmacodynamics/Indications Thyrotropin Formation and secretion of hormones of thyroid, ↑ its sizes and vascularization; in the fatty tissue lipid release Stimulating therapy: afterwards or during application of radioactive iodide at thyroid carcinoma (for ↑ iodide capture by the organ) Diagnosis: forms of hypothyroidism From urine of FSH: in women development of follicles, menopausal women: secretion of estrogens and ovulation (with urofollitropin (mainly LH); in men — spermatogenesis FSH), gonadotropin LH: in women — ovulation, corpus luteum human menopausal stimulation, ↑ progesteron; in men — (FSH+LH) ↑ secretion of androgens From the placenta: Replacement therapy: hypothalamopituitary gonadotropin human hypogonadism with infertility; stimulating: chorionic, similar infertility with insufficiency of sexual glands, to LH polycystic ovaries, etc.; with fertilization in vitro; cryptochism (hCG) Diagnosis: cryptochism (hCG) DRUGS OF PITUITARY HORMONES Drugs Pharmacodynamics/Indications Lactin ↑ lactation; proliferation of corpus luteum; mitogenic activity of lymphocytes Stimulating therapy: lactation in the postpartum period Intermedin ↑ visual acuity, adaptation to darkness Pharmacodynamic therapy: degenerative changes of retina, hemeralopy, pigmental retinitis, etc. Oxytocin, Causes uterine contractions; mammary gland desamino- alveoli cells ⇒ promotes milk rejection; oxytocin weak antidiuretic and pressor activity (sandopart) Pharmacodynamic therapy: labour activity, uterine bleeding in the postpartum or postabortion periods Diagnosis: placental circulation 8 DRUGS OF PITUITARY HORMONES Drugs Pharmacodynamics/Indications Vasopressin, ↓ diuresis; vasoconstriction; ↑ contractions of the desmopressin, myometrium and intestine; ↑ thrombocyte felipressin, aggregation, VIII factor of blood clotting pituitrin, Replacement therapy: pituitary insipidus
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