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PTP 546 Endocrine Pharmacology

PTP 546 Endocrine Pharmacology. Module 11 Jayne Hansche Lobert, MS, RN, ACNS-BC, NP. Endocrine Pharmacology Adrenalcorticoids. Naturally Occurring Adrenal Corticoids Negative feedback loop Hypothalamus  CRH Pituitary  ACTH  adrenal cortex cortisol Glucocorticoids

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PTP 546 Endocrine Pharmacology

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  1. PTP 546Endocrine Pharmacology Module 11 Jayne Hansche Lobert, MS, RN, ACNS-BC, NP Lobert

  2. Endocrine PharmacologyAdrenalcorticoids • Naturally Occurring Adrenal Corticoids • Negative feedback loop • Hypothalamus CRH Pituitary  ACTH  adrenal cortex cortisol • Glucocorticoids • Cortisol, Corticosterone • Glucose, protein and lipid metabolism • Anti-Inflammatory effects • Immunosuppressive effect • Mineralcorticoids • Aldosterone • Fluid and electrolyte control Lobert

  3. Endocrine PharmacologyAdrenalcorticoids • Pharmacologic Glucocorticoids • Ex:Dexamethasone (Decadron) • Ex:Hydrocortisone (Cortef) • Ex:Methylpredisolone (Medrol) • Ex:Prednisone (Deltasone) • Ex:Triamcinolone (Azmacort) • Routes of Administration • IV, inhaled, oral, intraarticular, topical, nasal, ophthalmic, otic, etc. Lobert

  4. Endocrine PharmacologyAdrenalcorticoids • Glucocorticoids • Action: inhibit the production of proinflammatory substances suppression of inflammation; inhibit immune cell synthesis  suppression of the immune response • Therapeutic Use • Replacement associated with adrenal insufficiency • Reduce inflammation in many conditions • Suppression of the immune response Lobert

  5. Endocrine PharmacologyAdrenalcorticoids Inflammatory Disorders Organ Transplantations Crohn’s, Ulcerative Colitis Bronchial Asthma, COPD Pneumonias Scarcidosis Multiple Sclerosis, Myasthenia Gravis Systemic Lupus Erythematosus (SLE) • Allergic Reactions, Anaphylaxis • Psoriasis, Dermatitis • Osteoarthritis, Gouty Arthritis, Rheumatoid Arthritis • Bursitis, Synovitis • Leukemia's, Lymphomas • Closed Head Injury, Spinal Cord Injury, Brain Tumors Lobert

  6. Endocrine PharmacologyAdrenalcorticoids • Glucocorticoids • Side Effects: • Dyspepsia, gi upset, gi bleed, peptic ulcers • Increased risk for infection • Mood changes, labile emotions • Sodium retention, hypertension • Bone loss, osteoporosis, fracture risk • Muscle atrophy, delayed wound healing • Hyperglycemia • Increased appetite, weight gain • Changes in appearance: “Moon face”, truncal obesity, acne, “buffalo hump”, thin limbs, increased body hair • Side Effects: • Reflect an excess of adrenal hormone; Cushing’s Syndrome/Disease; Adrenal Hypersecretion Lobert

  7. Endocrine PharmacologyAdrenalcorticoids • Precautions • Avoid abrupt withdrawal • Taper off prior to discontinuation of med • Rapid Adrenal Insufficiency Addison’s Syndrome/Disease/ Adrenal Crisis • Life Threatening Effects: lethargy, confusion & coma • Recognize value of glucocorticoids • Recognize significant side effects of glucocorticoids Lobert

  8. Endocrine PharmacologyAdrenalcorticoids • Mineralcorticoids • Ex: Fludrocortisone (Florinef) • Action: causes sodium reabsorption & water retention, potassium loss in distal renal tubules • Therapeutic Effect: replacement of mineralcorticoids with conditions of adrenal insufficiency such as Addison’s Disease; Post Adrenalectomy • Side Effects: hypertension, sodium retention, water retention, edema, weight gain, hypokalemia Lobert

  9. Endocrine PharmacologySex Hormones • Naturally Occurring Male Sex Hormones • Androgens • Testosterone • Effect of Androgens • Development of male sexual characteristics • Increased body hair, increased skeletal muscle mass, voice change, maturation of external genitalia • Stimulation of spermatogenesis • Facilitate growth and maturation of developing sperm Lobert

  10. Endocrine PharmacologySex Hormones • Pharmacologic Androgens • Examples: • Fluxymesterone (Android) • Methylestesterone (Durabolin) • Oxandrolone (Oxandrin) • Testosterone Gel (Androderm) • Testosterone Transdermal (Androgel) Lobert

  11. Endocrine PharmacologySex Hormones • Pharmacologic Androgens • Action: mimic androgenic effects development of male sexual characteristics and mimics anabolic effects  development of muscles, increase in the lean muscle mass • Therapeutic Use: • Replacement therapy • Catabolic states • Delayed puberty • Breast Cancer Lobert

  12. Endocrine PharmacologySex Hormones • Pharmacologic Androgens • Side Effects: • Women: hair growth, voice deepening, irregular menstruation, acne • Male: bladder irritation, breast swelling, prolonged erections, increased risk of prostate cancer • Children: accelerated sexual maturation, impairment of bone growth • General: hypertension, elevation in lipid profile, liver damage, liver cancer Lobert

  13. Endocrine PharmacologySex Hormones • Naturally Occurring Female Hormones • Estrogen • Estradiol • Progestins • Progesterone • Effects: • Development of female sexual characteristics • Development of female reproductive system • Facilitation and maintenance of pregnancy Lobert

  14. Endocrine PharmacologySex Hormones • Pharmacologic Female Hormones • Examples: • Conjugated estrogens (Premarin) • Estradiol(Estraderm, Depo-Estradiol) • Medroxyprogesterone (Provera) • Levonorgestrel (Norplant) Lobert

  15. Endocrine PharmacologySex Hormones • Pharmacologic Female Hormones • Action: mimics naturally occurring hormones • Therapeutic Use: • Replacement therapy • Hypogonadism • Failure of ovarian development • Menstrual irregularities • Endometriosis • Carcinoma Lobert

  16. Endocrine PharmacologySex Hormones • Pharmacologic Female Hormones • Side Effects: • Myocardial Infarctions, thromboembolism, stroke • Abnormal clotting thrombophlebitis, pulmonary embolism • Increase risk for ovarian, endometrial and breast cancers • Transient nausea • Sodium and water retention Lobert

  17. Endocrine PharmacologySex Hormones • Selective Estrogen Receptor Modulators • Ex: Tamoxifen (Nolvadex) • Ex: Raloxifene (Evista) • Action: blocks estrogen receptors • Therapeutic Effect: used for treatment of hormone specific cancers • Side Effects: hot flashes, joint pain, nausea and vomiting Lobert

  18. Endocrine PharmacologySex Hormones • AntiProgestins • Ex: Mifepristone (RU486) • Action: stimulate uterine contractions embryo expulsion • Therapeutic Effect: pregnancy termination • Side Effects: excessive contractions, incomplete abortion, excessive bleeding Lobert

  19. Endocrine PharmacologySex Hormones • Hormonal Contraceptives • Ex: Estradiol & Norethidrone (Loestrin) • Ex: Estradiol & Etonogestrel (Nuva Ring) • Ex: Levonorgestrel (Norplant) • Ex: Medroxyprogesterone (Depo-Provera) Lobert

  20. Endocrine PharmacologySex Hormones • Hormonal Contraceptives • Action: inhibit ovulation, impairs uterine endometrial implantation • Therapeutic Effect: prevention of pregnancy • Side Effects: cardiovascular effects such as thromboembolism, stroke, MI, liver cancer with prolonged use, nausea, headache, weight gain Lobert

  21. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Naturally Occurring Thyroid Hormone • T4 (Thyroxine) and T3 (Triiodothyronine) • Maintain body temperature • Increase basal metabolic rate • Facilitates normal growth and development • Increase heart rate and myocardial contractility • Enhance glucose absorption • Enhance lipolysis Lobert

  22. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Drugs to Treat Hyperthyroidism • Antithyroid Agents • Ex: Methimazole (Tapazole) • Ex: Propylthiouracil (PTU) • Iodide • Ex: SSKI • Radioactive Iodine • Ex: RA 131 Lobert

  23. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Drugs to Treat Hyperthyroidism • Antithyroid Agents • Ex: Methimazole (Tapazole) • Ex: Propylthiouracil (PTU) • Action: inhibits conversion of T4T3; blocks thyroid peroxidase enzyme • Therapeutic Effect: reduction of thyroid hormone synthesis • Side Effects: agranulocytosis, itching, rash Lobert

  24. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Drugs to Treat Hyperthyroidism • Iodide • Action: inhibits all steps in thyroid hormone synthesis; dramatically reduces thyroid hormone in limited situations • Side Effects: stains teeth • Radioactive Iodine: RA 131 • Action: destroys thyroid tissue • Side Effects: hypothyroidism Lobert

  25. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Drugs to Treat Hypothyroidism • Thyroid Hormone • Ex: Levothyroxine (Levothroid, Synthroid) • Ex: Liothyronine (Cytomel) • Action: Supplement/replace T3 and/or T4 reduction of TSH; mimics function of the thyroid gland • Therapeutic Effect: treatment of thyroid deficiency related to hypothyroidism, thryroidectomy, etc. Lobert

  26. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization Side Effects of too little thyroid hormone replacement Side Effects of excess thyroid hormone replacement Fatigue Weight loss Diarrhea Tachycardia Muscle wasting Increased appetite Insomnia Menstrual irregularities Exopthalmos • Lethargy • Weight gain • Constipation • Bradycardia • Weakness • Facial edema • Concentration difficulties • Fatigue • Coarse skin Lobert

  27. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Regulation of Bone Mineral Homeostasis • Parathyroid Hormone (PTH) • Increases blood calcium levels & increases phosphate excretion; stimulates Vitamin D  increased calcium absorption from intestines • High levels of PTH bone breakdown • Normal levels of PTH bone synthesis • Vitamin D • Helps increase calcium, phosphate enhances bone formation • Calcitonin • Physiologic antagonist of PTH; lowers blood calcium by stimulating bone formation; incorporates phosphate into bone Lobert

  28. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Phamacoloigics for Bone Mineral Homeostasis • Calcium Supplements • Vitamin D • Biphosphonates • Calcitonin • Estrogen Lobert

  29. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Calcium Supplements • Ex: Calcium Carbonate (Os-Cal); Calcium Citrate (Citracal) • Action: mimics calcium effects in body • Therapeutic Effect: supports bone formation assoc. with dietary insufficiency, hypoparathyroidism; rickets • Side Effects: constipation, fatigue • Post Menopausal Intake: 1200-1500 mg/day Lobert

  30. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Vitamin D Supplements • Ex: Vitamin D (OsCal & D) • Action: mimics Vit D effects in body; necessary for calcium absorption in the intestines • Therapeutic Effect: enhances bone mineralization • Side Effects: headache, thirst, metallic taste Lobert

  31. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Biphosphonates • Ex: Alendronate (Fosamax) • Action: directly reduces bone resorption • Therapeutic Effect: prevent bone loss assoc with steroid use; treatment of osteoporosis to reduce risk of vertebral fractures; treatment of Pagets disease • Side Effects: gi upset and esophagitis (remain upright for 30 minutes following administration to prevent) Lobert

  32. Endocrine PharmacologyThyroid & Parathyroid Hormones & Drugs Affecting Bone Mineralization • Calcitonin • Ex: Calcitonin (Calcimar) • Action: mimics endogenous calcitonin decreased blood calcium levels ensuring calcium availability for bone mineralization • Therapeutic Effect: use in conditions that are characterized by increased bone resorption • Side Effects: redness & swelling following injections, gi upset Lobert

  33. Endocrine PharmacologyTreatment of Diabetes Mellitus • Type I Diabetes • Etiology: young age, viral trigger for autoimmune response • Pathophysiology: destruction of pancreatic beta cells total lack of insulin production • Clinical Signs & Symptoms: rapid onset of the clinical manifestations of polyuria, polydipsia, polyphagia Lobert

  34. Endocrine PharmacologyTreatment of Diabetes Mellitus • Type II Diabetes • Etiology: aging individuals; genetic predisposition; obesity, lack of exercise, poor dietary intake • Pathophysiology: reduced tissue sensitivity to insulin (insulin resistance); reduction in insulin production; irregular release of insulin • Clinical Signs & Symptoms: slow and gradual onset of the clinical manifestations of delayed wound healing, fatigue; blurred vision Lobert

  35. Endocrine PharmacologyTreatment of Diabetes Mellitus • Complications of Diabetes • Microvascular • Retinopathies blindness • Nephropathies renal failure • Neuropathies • Sensory • Autonomic • Macrovascular • Hypertension, myocardial infarction, cerebral vascular accidents, peripheral arterial disease, amputations Lobert

  36. Endocrine PharmacologyTreatment of Diabetes Mellitus • Prevention of Complications • Diabetes Control and Complications Trial (DCCT) & United Kingdom Prospective Diabetes Study (UKPDS) • Prolonged elevations in blood glucose structural and functional changes in vascular cells • Tight Glycemic Control Prevents Complications • Maintain blood glucose 70-100mg/dl • Side Effect: risk for hypoglycemia Lobert

  37. Endocrine PharmacologyTreatment of Diabetes Mellitus • Management of Diabetes Mellitus • Diet • Exercise • Medications • Oral hypoglycemic agents • Insulin • Blood Glucose Monitoring Lobert

  38. Endocrine PharmacologyTreatment of Diabetes Mellitus • Insulin • Types (Onset/Peak/Duration) • Immediate Acting (<0.5 hr/1.5 hr/3-6hr) • Lispro (Humalog); Aspart (Novolog) • Rapid Acting (.5 hr/2-4hr/5-7 hr) • Regular (Humulin R, Novolin R) • Intermediate Acting (1-3 hr/6-12hr/18-24 hr) • Isophane (Humulin N, Novolin N) • Insulin Zinc (Humulin L, Novolin L) • Long Acting ( 2hr/ no peak/24 hrs) • Glargine (Lantus) Lobert

  39. Endocrine PharmacologyTreatment of Diabetes Mellitus • Insulin • Routes: IV, subcutaneous injections, insulin pump subcutaneous • Action: mimics endogenous insulin; facilitates glucose transport into cells • Therapeutic Effect: reduction of blood glucose • Side Effects: Hypoglycemia Lobert

  40. Endocrine PharmacologyTreatment of Diabetes Mellitus • Antidiabetic Agents • Sulfonylureas • Ex: Glipizide (Glucotrol) • Biguanides • Ex: Metformin (Glucophage) • Alpha-Glucosidase Inhibitors • Ex: Acarbose (Precose) • Thiazolinediones • Ex: Rosiglitazone (Avandia) • Meglitinides • Ex: Repaglinide (Prandin) • Glucagon Like Peptide/ Incretin Mimic • Ex: Exenatide (Byetta) • Dipeptidyl Peptidase-4 Inhibitor (DDP-4) Lobert

  41. Endocrine PharmacologyTreatment of Diabetes Mellitus • Oral Antidiabetic Agents • Sulfonylureas • Ex: Glipizide (Glucotrol); Glyburide (DiaBeta) • Action: increase insulin secretion from pancreatic beta cells • Therapeutic Effect: reduces blood glucose; reduces hepatic glucose production • Side Effects: weight gain, hypoglycemia, gi upset Lobert

  42. Endocrine PharmacologyTreatment of Diabetes Mellitus • Oral Antidiabetic Agents • Biguanides • Ex: Metformin (Glucophage) • Action: decreases hepatic glucose production; increases muscle tissue sensitivity to insulin • Therapeutic Effect: reduction of blood glucose • Side Effects: diarrhea, gi disturbances; rarely lactic acidosis occurs, to avoid  hold IV contrast media for 48 hrs Lobert

  43. Endocrine PharmacologyTreatment of Diabetes Mellitus • Oral Antidiabetic Agents • Alpha-Glucosidase Inhibitors • Ex: Acarbose (Precose) • Action: inhibits breakdown of glucose and delays absorption of glucose in the intestine • Therapeutic Effect: reduction of blood glucose • Side Effects: gi disturbances, bloating, gas, diarrhea Lobert

  44. Endocrine PharmacologyTreatment of Diabetes Mellitus • Oral Antidiabetic Agents • Thiazolinediones • Ex: Rosiglitazone (Avandia) • Action: increases glucose uptake in muscles, decreases glucose production • Therapeutic Effect: reduces blood glucose • Side Effects: weight gain, edema Lobert

  45. Endocrine PharmacologyTreatment of Diabetes Mellitus • Oral Antidiabetic Agents • Meglitinides • Ex: Repaglinide (Prandin) • Action: stimulates rapid release of insulin from the pancreas • Therapeutic Effect: reduces blood glucose • Side Effects: weight gain, hypoglycemia Lobert

  46. Oral Antidiabetic Agents • Dipeptidyl Peptidase-4 Inhibitor (DDP-4) • Ex: Sitagliptin (Januvia) • Action: enhances incretin system, stimulates release of insulin from the pancreas, decreases hepatic glucose production • Therapeutic Effect: reduces blood glucose • Side Effects: upper respiratory tract infections, sore throat, diarrhea Lobert

  47. Endocrine PharmacologyTreatment of Diabetes Mellitus • Miscellaneous Injectable Antidiabetic Agents • Glucagon Like Peptide/Incretin Mimic • Ex: Exenatide (Byetta) • Amylin Analog • Ex: Pramlintide (Symlin) • Action: decrease gastric emptying, decrease glucagon production, increased satiety • Therapeutic Effect: reduces blood glucose • Side Effects: hypoglycemia, nausea, vomiting Lobert

  48. Endocrine PharmacologyTreatment of Diabetes Mellitus • Hypoglycemic Side Effect • Signs & Symptoms • Confusion, irritability, diaphoresis, tremors, hunger, weakness, visual disturbances coma, seizures, death • Treatment • Oral Glucose • 10-15 g of CHO= 6 oz. Orange juice, 8 oz. milk • Glucose tablets, glucose paste • IV Glucose • 50% Dextrose Injection • Intramuscular Glucagon Lobert

  49. Endocrine PharmacologyTreatment of Diabetes Mellitus • Hypoglycemia • Causes/Contributing Factors • Imbalance of exercise, meds and meals • Hypoglycemic unawareness • Prevention • Education • Awareness • Preparedness Lobert

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