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Lesson 12 Medications (drugs) Ex 1. Key-words: 1 endocrine problems 2 corticosteroids 3 adrenal cortex 4 blood electrolyte levels 5 behavior 6 the zona fasciculata and reticularis 7 Inhaled steroids 8 to treat the nasal mucosa, sinuses, bronchii, and lungs 9 injectables for intravenous and parenteral routes 10 brain tumors 11 adrenal insufficiency and congenital adrenal hyperplasia 12 hyperglycemia 13 insulin resistance 14 diabetes mellitus 15 gastritis 16 colitis 17 ictus 18 erectile dysfunction 19 hypogonadism 20 hypothyroidism 21 amenorrhoea 22 retinopathy 1 болезни эндокринной системы 2 кортикостероиды 3 надпочечная кора 4 уровень электролита крови 5 поведение 6 опоясывающий лишай fasciculata и reticularis 7 вдыхавших стероидов 8, рассматривать носовую слизистую оболочку, пазухи, bronchii, и легкие 9 injectables для внутривенных и парентеральных маршрутов 10 опухоли головного мозга 11 надпочечные недостаткои и врожденные надпочечник 12 гипергликемия 13 сопротивление инсулина 14 диабет 15 гастрит 16 колит 17 удар 18 способных выпрямляться дисфункций 19 hypogonadism 20 гипотиреоз 21 аменорея ретинопатия Ex 2. Read and translate the following: C21H30O4, C21H28O5, 17-hydroxy-11-dehydrocorticosterone, 21-hydroxylase and 17αhydroxylase, 11β-hydroxylase, an 18-oxidation, hydrocortisone-17-butyrate, hydrocortisone-17valerate, aclometasone dipropionate, betamethasone valerate, betamethasone dipropionate, prednicarbate, clobetasone-17-butyrate, clobetasol-17-propionate, fluocortolone caproate, fluocortolone pivalate, and fluprednidene acetate, 5-HT3 antagonists, Ex 3. Read some information about “Drugs for endocrine problems”: For endocrine problems androgens, antiandrogens, gonadotropin, corticosteroids, human growth hormone, insulin, antidiabetics (sulfonylureas, biguanides/metformin, thiazolidinediones, insulin), thyroid hormones, antithyroid drugs, calcitonin, diphosponate, vasopressin analogues. Text 25. Corticosteroid Definition. Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex. Corticosteroids are involved in a wide range of physiologic systems such as stress response, immune response and regulation of inflammation, carbohydrate metabolism, protein catabolism, blood electrolyte levels, and behavior. Glucocorticoids such as cortisol control carbohydrate, fat and protein metabolism and are anti-inflammatory by preventing phospholipid release, decreasing eosinophil action and a number of other mechanisms. Mineralocorticoids such as aldosterone control electrolyte and water levels, mainly by promoting sodium retention in the kidney. Some common natural hormones are corticosterone (C21H30O4), cortisone (C21H28O5, 17-hydroxy-11-dehydrocorticosterone) and aldosterone. Biosynthesis. The corticosteroids are synthesized from cholesterol within the adrenal cortex. Most steroidogenic reactions are catalysed by enzymes of the cytochrome P450 family. They are located within the mitochondria and require adrenodoxin as a cofactor (except 21hydroxylase and 17α-hydroxylase). Aldosterone and corticosterone share the first part of their biosynthetic pathway. The last part is either mediated by the aldosterone synthase (for aldosterone) or by the 11βhydroxylase (for corticosterone). These enzymes are nearly identical (they share 11βhydroxylation and 18-hydroxylation functions) but aldosterone synthase is also able to perform an 18-oxidation. Moreover, aldosterone synthase is found within the zona glomerulosa at the outer edge of the adrenal cortex; 11β-hydroxylase is found in the zona fasciculata and reticularis. Classification. Corticosteroids are generally grouped into four classes, based on chemical structure. Allergic reactions to one member of a class typically indicate an intolerance of all members of the class. This is known as the "Coopman classification” 1989. Group A (short to medium acting glucocorticoids) hydrocortisone, hydrocortisone acetate, cortisone acetate, tixocortol pivalate, prednisolone, methylprednisolone, and prednisone. Group B (triamcinolone acetonide, triamcinolone alcohol, mometasone, amcinonide, budesonide, desonide, fluocinonide, fluocinolone acetonide, and halcinonide). Group C (betamethasone, betamethasone sodium phosphate, dexamethasone, dexamethasone sodium phosphate, and fluocortolone). Group D (hydrocortisone-17-butyrate, hydrocortisone-17-valerate, aclometasone dipropionate, betamethasone valerate, betamethasone dipropionate, prednicarbate, clobetasone17-butyrate, clobetasol-17-propionate, fluocortolone caproate, fluocortolone pivalate, and fluprednidene acetate). Inhaled steroids for use to treat the nasal mucosa, sinuses, bronchii, and lungs. This group includes: Flunisolide Fluticasone propionate Triamcinolone acetonide Beclomethasone dipropionate Budesonide Oral forms such as prednisone and prednisolone. Systemic forms are available in injectables for intravenous and parenteral routes. Uses of corticosteroids. Synthetic pharmaceutical drugs with corticosteroid-like effect are used in a variety of conditions, ranging from brain tumors to skin diseases. Dexamethasone and its derivatives are almost pure glucocorticoids, while prednisone and its derivatives have some mineralocorticoid action in addition to the glucocorticoid effect. Fludrocortisone (Florinef) is a synthetic mineralocorticoid. Hydrocortisone (cortisol) is available for replacement therapy, e.g. in adrenal insufficiency and congenital adrenal hyperplasia. Synthetic glucocorticoids are used in the treatment of joint pain or inflammation (arthritis), temporal arteritis, dermatitis, allergic reactions, asthma, hepatitis, systemic lupus erythematosus, inflammatory bowel disease (ulcerative colitis and Crohn's disease), sarcoidosis and for glucocorticoid replacement in Addison's disease or other forms of adrenal insufficiency. Topical formulations are also available for the skin, eyes (uveitis), lungs (asthma), nose (rhinitis), and bowels. Corticosteroids are also used supportively to prevent nausea, often in combination with 5-HT3 antagonists (e.g. ondansetron). Typical undesired effects of glucocorticoids present quite uniformly as drug-induced Cushing's syndrome. Typical mineralocorticoid side effects are hypertension (abnormally high blood pressure), hypokalemia (low potassium levels in the blood), hypernatremia (high sodium levels in the blood) without causing peripheral edema, metabolic alkalosis and connective tissue weakness. There may also be impaired wound healing or ulcer formation because of the immunosuppressive effects. Clinical and experimental evidence indicates that corticosteroids can cause permanent eye damage by inducing central serous retinopathy (CSR, also known as central serous chorioretinopathy, CSC). A variety of steroid medications, from anti-allergy nasal sprays (Nasonex, Flonase) to topical skin creams, to eye drops (Tobradex), to prednisone have been implicated in the development of CSR. Side effects. Long-term corticosteroids use has several severe side effects as for example: hyperglycemia, insulin resistance, diabetes mellitus, osteoporosis, anxiety, depression, gastritis, colitis, hypertension, ictus, erectile dysfunction, hypogonadism, hypothyroidism, amenorrhoea, retinopathy. Text 26. Gliclazide Definition. Gliclazide is an oral hypoglycemic (anti-diabetic drug) and is classified as a sulfonylurea. It is marketed as Glyloc and Reclide in India and Diamicron in Canada. The modified-release formulation are also marketed now. Its classification has been ambiguous, as literature uses it as both a first-generation and second-generation sulfonylurea. Form and Composition. Each tablet contains 80, 60, or 30 mg of gliclazide. Gliclazide is not marketed in the United States and Philippines. In the Philippines, it is marketed under the brandname of Glubitor-OD in 30 mg or 80 mg doses. Indication. Gliclazide is used for control of hyperglycemia in gliclazide-responsive diabetes mellitus of stable, mild, non-ketosis prone, maturity-onset or adult type. It is used when diabetes cannot be controlled by proper dietary management and exercise or when insulin therapy is not appropriate. Mode of Action. Gliclazide binds to sulfonylurea receptors on the surface of the Beta islet cells found in the pancreas. This binding effectively closes the K+ ion channels. This decreases the efflux of potassium from the cell which leads to the depolarization of the cell. This causes voltage dependent Ca++ ion channels to open increasing the Ca++ influx. The calcium can then bind to and activate calmodulin which in turn leads to exocystosis of insulin vesicles leading to insulin release. Dosage. The dosage is 40 to 320 mg depending on the response of the patient. The drug is taken once or twice daily before food, with no more than 160 mg being ingested at a time. Properties Hypoglycemic sulfonylurea, restoring first peak of insulin secretion, increasing insulin sensitivity. Glycemia-independent hemovascular effects, antioxidant effect. No active circulating metabolites. Contraindications Type 1 diabetes Hypersensitivity to sulfonylureas Severe renal or hepatic failure Pregnancy and lactation Miconazole coprescription Metabolism. Gliclazide undergoes extensive metabolism to several inactive metabolites in humans, mainly methylhydroxygliclazide and carboxygliclazide. CYP2C9 is involved in the formation of hydroxygliclazde in human liver microsomes and in a panel of recombinant human P450sin vitro. But the pharmacokinetics of gliclazide MR are affected mainly by CYP2C19 genetic polymorphism instead of CYP2C9 genetic polymorphism. Interactions. Hyperglycemic action may be caused by danazol, chlorpromazine, glucocorticoids, progestogens, or β-2 agonists. Its hypoglycemic action may be potentiated by phenylbutazone, alcohol, fluconazole, β-blockers, and possibly ACE inhibitors. It has been found that rifampin increases gliclazide metabolism in humans in vivo. Adverse effects Hypoglycemia Gastrointestinal disturbance (reported) Skin reactions (rare) Hematological disorders (rare) Hepatic enzyme rises (exceptional) Overdosage. Gliclazide overdose may cause severe hypoglycemia, requiring urgent administration of glucose by IV and monitoring. Ex 4. Speak about side effects of corticosteroids. Why it happens? Ex 5. Writing. Write a report to the conference “Medications of new century”. Follow the sample. A Report to the Conference Plan 1. Introduction. 2. Starting the target. Define clearly the purpose of your report. 3. Providing an overview. Outline the main points of the report. 4. Conclusion. 5. References.