Endrocrine drugs


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  • Regulation of: Metabolism Water and Electrolyte balance Red Blood Cell Production Control of: Reproduction Smooth, sequential growth and development
  • Oxytocin: Uterine contraction Milk ejection from Mammary gland Release stimulated by delivery and infant suckling Vasopressin (Antidiuretic Hormone): Enhances water retention by kidneys (hence antidiuretic) Major regulation of urinary water loss and overall water balance Causes contraction of arteriolar smooth muscle (vessel pressor effect) Little normal control of blood pressure Released via hypothalmic osmoreceptors when an increase in osmolarity is dected (ie, a decrease in plasma levels)
  • Growth Hormone (GH) responsible for regulating growth and development important in regulating metabolism (increases use of stored fats, decreases glucose utilization) Thyroid-Stimulating Hormone (TSH) Increases metabolic rate acting on thyroid gland Adrenocorticotropic Hormone (ACTH) Increases cortisol secretion by adrenal cortex Promotes growth of adrenal cortex Follicle-Stimulating Hormone (FSH) Males: required for sperm production Females: stimulates growth and devlopment of ovarian follicles Luteinizing Hormone (LH) Males:responsible for secretion of testosterone by testes Females: responsible for ovulation, secretion of estrogen and progesterone by ovaries Prolactin (PRL) Females: Enhances breast development and milk production
  • Thyroid Hormone: Effects virtually ever body tissue Increases the body’s overall basal metabolic rate or “idling speed” Increases Oxygen consumption and energy expenditure Slow action, long duration Increases heat production via increased metabolic rate (Calorigenic Effect) Sympathomimetic Effects with increased thyroid stimulation increased production of catecholmine receptors
  • Cretinism Exhibits signs of dwarfism because skeleton fails to grow or mature Severe Mental retardation In adult onset, causes Myxedma S/S: facial swelling, bradycardia, decreased body temperature, weakness, leathergy Treatment aimed at thyroid replacement
  • Exophthalmos Grave’s Disease Increased metabolism, tachycardia , heat intolerance, increased sweating, weight loss despite good apetite, insomnia, nervousness Treatment: surgical removal of part of thyroid gland or radiation therapy to destroy part of thyroid
  • Parathyroid hormone: Increases Calcium concentration in plasma and, therefore, ECF. Complete lack of parathyroid hormone leads to death within several days, usually due to hypocalcemic spasm of respiratory muscles
  • Alpha cells: glucagon Opposes action of insulin Increases blood sugar levels by: decreasing glycogen synthesis increasing glycogen breakdown into glucose Beta cells: insulin Decreases blood sugar by: Promotes glucose transport into most cells by increasing the number of glucose-transporter proteins available on cell membrane. Brain doesn’t require insulin for transport Increases glucogenesis (creation of glucose) Increases glycogenolysis (breakdown of glycogen) Delta cells: somatostatin Inhibits production and release of both glucogon and insulin
  • Medulla Epinephrine and Norepinephrine Part of SNS, responsible for catecholmine release which prolongs fight or flite response Cortex: Glucocorticoids, mineralocorticoids Glucocorticoids: increase blood glucose levels prevent inflammation are released in response to stress
  • Endrocrine drugs

    1. 1. Pharmacology Drugs that Affect the Endocrine System
    2. 2. Topics• Pituitary Drugs• Parathyroid/Thyroid Drugs• Adrenal Drugs• Pancreatic Drugs• Reproductive Drugs• Sexual Behavior Drugs
    3. 3. Functions• Regulation• Control
    4. 4. GlandsExocrine Endocrine• Secrete enzymes • Secrete hormones• Close to organs • Transport via bloodstream • Require receptors
    5. 5. Nervous Endocrine Wired WirelessNeurotransmitters Hormones Short Distance Long Distance Closeness Receptor Specificity Rapid Onset Delayed Onset Short Duration Prolonged DurationRapid Response Regulation
    6. 6. Mechanism of Action
    7. 7. Hypothalamus
    8. 8. Hypothalamic Control Pituitary
    9. 9. Posterior Pituitary Target ActionsOxytocin Uterus ↑ Contraction Mammary ↑ Milk let-downADH Kidneys ↑ Water reabsorption
    10. 10. Anterior Pituitary Target ActionGH Most tissue ↑GrowthTSH Thyroid ↑TH secretionACTH Adrenal ↑Cortisol Cortex secretion
    11. 11. Anterior Pituitary Target ActionFSH Ovaries Follicles Testes Estrogen SpermLH Ovaries Ovulation Testes Progesterone Testosterone
    12. 12. Anterior Pituitary Target ActionProlactin Mammary Milk Gland production
    13. 13. Pituitary Hormones
    14. 14. Thyroid
    15. 15. Thyroid Target ActionThyroxine Most cells ↑ BMRTriiodothyronineCalcitonin Mostly bone ↓ Calcium
    16. 16. Hypothyroidism
    17. 17. Hyperthyroidism
    18. 18. Parathyroid
    19. 19. Parathyroid Target ActionParathyroid Bone ↑Calcium(PTH) Kidney GI Tract
    20. 20. Calcium Regulation
    21. 21. Pancreas
    22. 22. Pancreas• Alpha cells: glucagon• Beta cells: insulin
    23. 23. Pancreas Target ActionGlucagon Liver ↑GlucoseInsulin General ↓Glucose
    24. 24. Glucose Regulation
    25. 25. Adrenal
    26. 26. Adrenal Medulla Target ActionNorepi Heart ProlongsEpi Blood SNS Effects vessels Liver
    27. 27. Adrenal Cortex Target ActionAldosterone Kidney ↑Na reabsobtion ↑Water retentionCortisol Most Tissue ↑Glucose ↓inflammation
    28. 28. Anterior Pituitary Drugs Inadequate Growth Excessive Growth Hormone Hormone• Dwarfism • Acromegaly• somatrem (Protropin®) • Gigantism• homatropin • Surgical removal 1º (Humatrope®) • octreotide (Sandostatin®)
    29. 29. Posterior Pituitary Drugs• Oxytocin• ADH – Diabetes insipidus – Nocturnal enuresis• vasopressin (Pitressin®)• desmopressin (Stimate®)• lypressin (Diapid®)
    30. 30. Parathyroid Diseases• Hypoparathyroidism – Inadequate calcium levels • TX: increased dietary calcium• Hyperparathyroidism – Excessive calcium levels • TX: surgical removal
    31. 31. Thyroid Disease• Hypothyroidism – Hormone replacement – levothyroxine (Synthroid®)• Hyperthyroidism – Thyrotoxicosis – Surgical removal – propylthiouracil (PTU)
    32. 32. Adrenal Cortex ACTH Hypersecretion ACTH Hyposecretion Cushing’s Disease Addison’s Disease• Surgical removal • Replacement therapy• Inhibit adrenal • Cortisone (Cortistan®) secretion • Hydrocortisone – ketoconazol (Nizoral ®) (SoluCortef®)• Symptomatic tx: • Fludrocortisone – Antihypertensives (Florinef Acetate®)
    33. 33. Pancreas Blood Potassium Blood Glucose
    34. 34. Insulin Preparations• Regular Insulin – Natural insulin• Modified Insulin – Increased duration of action – NPH (neutral protamin Hagedorn) • Natural plus protamin – Lente • Attached to zinc to prolong absorption
    35. 35. Oral Hypoglycemic Agents Sulfonylureas Alpha-glucosidase⇑ insulin secretion inhibitorstolbutamide (Orinase®) • Delay carbohydratechlorpropamide (Diabinese®) metabolism acarbose (Precose®)glipizide (Glucotrol®) miglitol (Glyset®)glyburide (Micronase®) Biguanides Thiazolidinedionesmetformin (Glucophage®) ⇑ Insulin effectiveness⇓ Glucose synthesis troglitazone (Rezulin®)⇑ Glucose uptake
    36. 36. Hyperglycemic Agents• Glucagon • diazoxide ⇑ gluconeogenesis (Proglycem®) – Inhibits insulin release• D50W
    37. 37. Estrogens & Progestins• Estrogens used for • Progestin post-menopausal – Diminish side effects hormone replacement of estrogen therapy therapy. – Nausea, fluid retention, – estradiol (Estrace®) breast tenderness – conjugated estrogens – medroxyprogesterone (Premarin®) acetate (Provera®) – estropipate (Ogen®) – norethindrone acetate (Aygestin®)
    38. 38. Oral Contraceptives• Combination of estrogen and progestin – Loestrin®, Levora®, Nordette®, Ovocon®, Norinyl® plus many others• Minipill: progestin only – Micronor®, Nor-Q.D.®, Orvette®• Prime side effect: ⇑ risk of thromboembolism
    39. 39. Uterine Stimulants &Relaxants• Stimulants (Oxytocics) • Relaxants (tocolytics)∀ ⇑ uterine contraction • Relax uterine smooth• Indication: muscle – Induce labor • Beta2 agonists – Postpartum hemorrhage – terbutaline (Brethine®)• oxytocin (Pitocin®) – ritodrine (Yuptopar®)• ergonovine (Ergotrate®)
    40. 40. Infertility Agents• Promote maturation of ovarian follicles• clomiphene (Clomid®)• urofollitropin (Metrodin®)
    41. 41. Male Reproductive Agents• Testosterone Replacement – methyltestosterone (Metandren®) – fluoxymesterone (Halotestin®)• Benign Prostatic Hypertrophy – Surgery – finasteride (Proscar®)
    42. 42. Sexual Behavior• Most are side effects from other medications – Antihypertensives & psychoactive drugs• sildenafil (Viagra®)