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Organ System Pharmacology
                   Drugs that Affect the Endocrine System
                             IVMS BMS Endocrinology 4 of 4
                                   Prepared and presented by:
                                    Marc Imhotep Cray, M.D.
    COMPANION RLOs:
IVMS Endocrine Secretion
      and Action
         Part I
        Part II
        Part III

  WebPath Pathology:
   Endocrine Pathology
       70 Images

Recommended Reading:
 Management of Diabetes

 Formative Assessment
  Practice question set #1
Topics Discussed
I.     Endocrine Glands / Hormones
       Action and Secretion Review
I.     Pituitary Drugs
II.    Parathyroid and Thyroid Drugs
III.   Adrenal Drugs
IV.    Pancreatic Drugs
V.     Reproductive Drugs


                                       2
Endocrine Glands / Hormones
     Action and Secretion Review
Functions
 Regulation
 Control




                                   3
Glands
Exocrine              Endocrine

   Secrete enzymes      Secrete hormones
   Close to organs      Transport via
                          bloodstream
                         Require receptors




                                              4
Nervous         versus      Endocrine


     Wired                        Wireless

Neurotransmitters                Hormones

 Short Distance                Long Distance

    Closeness                 Receptor Specificity

  Rapid Onset                  Delayed Onset

 Short Duration              Prolonged Duration

Rapid Response                   Regulation          5
Mechanism of Action




                      6
Hypothalamus




               7
Hypothalamic Control Pituitary




                                 8
Posterior Pituitary

            Target    Actions


Oxytocin    Uterus     Contraction
            Mammary    Milk
                      let-down
ADH         Kidneys    Water
                      reabsorption

                                 9
Anterior Pituitary

          Target        Action
GH        Most tissue    Growth
TSH       Thyroid        TH
                        secretion
ACTH      Adrenal        Cortisol
          Cortex        secretion


                                     10
Anterior Pituitary

          Target     Action


FSH       Ovaries    Follicles
          Testes     Estrogen
                     Sperm
LH        Ovaries    Ovulation
          Testes     Progesterone
                     Testosterone
                                11
Anterior Pituitary

             Target    Action



 Prolactin   Mammary   Milk
             Gland     production



                                    12
Pituitary Hormones




                     13
Thyroid




          14
Thyroid

                 Target       Action


Thyroxine        Most cells    BMR
Triiodothyronine
Calcitonin       Mostly bone  Calcium



                                         15
Hypothyroidism




                 16
Hyperthyroidism




http://library.med.utah.edu/WebPath/ENDOHTML/ENDOIDX.html




                                                            17
Parathyroid




              18
Parathyroid

               Target     Action

 Parathyroid   Bone        Calcium
 (PTH)         Kidney
               GI Tract




                                      19
Calcium Regulation




                     20
Pancreas




           21
Pancreas
 Alpha cells: glucagon
 Beta cells: insulin




                          22
Pancreas
           Target    Action

Glucagon   Liver      Glucose

Insulin    General    Glucose




                                 23
Glucose Regulation




                     24
Adrenal




          25
Adrenal Medulla
         Target    Action



Norepi   Heart     Prolongs
Epi      Blood     SNS Effects
         vessels
         Liver


                                 26
Adrenal Cortex
           Target      Action
Aldosterone Kidney      Na
                       reabsobtion
                        Water
                       retention

Cortisol   Most Tissue  Glucose
                       inflammation

                                       27
Anterior Pituitary Drugs

     Inadequate Growth            Excessive Growth
          Hormone                      Hormone
   Dwarfism                   Acromegaly
   somatrem (Protropin®)      Gigantism
   homatropin                 Surgical removal 1º
    (Humatrope®)               octreotide
                                (Sandostatin®)


                                                      28
Posterior Pituitary Drugs

   Oxytocin
   ADH
       Diabetes insipidus
       Nocturnal enuresis
   vasopressin (Pitressin®)
   desmopressin (Stimate®)
   lypressin (Diapid®)

                               29
Parathyroid Diseases

   Hypoparathyroidism
       Inadequate calcium levels
            TX: increased dietary calcium
   Hyperparathyroidism
       Excessive calcium levels
            TX: surgical removal




                                             30
Thyroid Disease

   Hypothyroidism
       Hormone replacement
       levothyroxine (Synthroid®)
   Hyperthyroidism
       Thyrotoxicosis
       Surgical removal
       propylthiouracil (PTU)


                                     31
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®)

                                                           32
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


                                                      33
Oral Hypoglycemic Agents

          Sulfonylureas                    Alpha-glucosidase
     insulin secretion                           inhibitors
    tolbutamide (Orinase®)               Delay carbohydrate
    chlorpropamide (Diabinese®)
                                          metabolism
                                      acarbose (Precose®)
    glipizide (Glucotrol®)
                                      miglitol (Glyset®)
    glyburide (Micronase®)

        Biguanides                    Thiazolidinediones
metformin (Glucophage®)
                                   Insulin effectiveness
 Glucose synthesis               troglitazone (Rezulin®)
 Glucose uptake
                                                               34
Hyperglycemic Agents

   Glucagon                   diazoxide
        gluconeogenesis       (Proglycem®)
                                   Inhibits insulin release
   D50W




                                                           35
Estrogens & Progestins

   Estrogens used for            Progestin
    post-menopausal                   Diminish side effects of
    hormone replacement                estrogen therapy
    therapy.                          Nausea, fluid
       estradiol (Estrace®)           retention, breast
                                       tenderness
       conjugated estrogens
        (Premarin®)                   medroxyprogesterone
                                       acetate (Provera®)
       estropipate (Ogen®)
                                      norethindrone acetate
                                       (Aygestin®)

                                                             36
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

                                                  37
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®)



                                                             38
Infertility Agents

   Promote maturation of ovarian follicles
   clomiphene (Clomid®)
   urofollitropin (Metrodin®)




                                              39
Male Reproductive Agents

   Testosterone Replacement
       methyltestosterone (Metandren®)
       fluoxymesterone (Halotestin®)
   Benign Prostatic Hypertrophy
       Surgery
       finasteride (Proscar®)



                                          40
End of Session




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                                                                                                  41

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IVMS Endo IV-Organ System Pharmacology- Drugs that Affect the Endocrine System

  • 1. Organ System Pharmacology Drugs that Affect the Endocrine System IVMS BMS Endocrinology 4 of 4 Prepared and presented by: Marc Imhotep Cray, M.D. COMPANION RLOs: IVMS Endocrine Secretion and Action Part I Part II Part III WebPath Pathology: Endocrine Pathology 70 Images Recommended Reading: Management of Diabetes Formative Assessment Practice question set #1
  • 2. Topics Discussed I. Endocrine Glands / Hormones Action and Secretion Review I. Pituitary Drugs II. Parathyroid and Thyroid Drugs III. Adrenal Drugs IV. Pancreatic Drugs V. Reproductive Drugs 2
  • 3. Endocrine Glands / Hormones Action and Secretion Review Functions  Regulation  Control 3
  • 4. Glands Exocrine Endocrine  Secrete enzymes  Secrete hormones  Close to organs  Transport via bloodstream  Require receptors 4
  • 5. Nervous versus Endocrine Wired Wireless Neurotransmitters Hormones Short Distance Long Distance Closeness Receptor Specificity Rapid Onset Delayed Onset Short Duration Prolonged Duration Rapid Response Regulation 5
  • 9. Posterior Pituitary Target Actions Oxytocin Uterus  Contraction Mammary  Milk let-down ADH Kidneys  Water reabsorption 9
  • 10. Anterior Pituitary Target Action GH Most tissue  Growth TSH Thyroid  TH secretion ACTH Adrenal  Cortisol Cortex secretion 10
  • 11. Anterior Pituitary Target Action FSH Ovaries Follicles Testes Estrogen Sperm LH Ovaries Ovulation Testes Progesterone Testosterone 11
  • 12. Anterior Pituitary Target Action Prolactin Mammary Milk Gland production 12
  • 14. Thyroid 14
  • 15. Thyroid Target Action Thyroxine Most cells  BMR Triiodothyronine Calcitonin Mostly bone  Calcium 15
  • 19. Parathyroid Target Action Parathyroid Bone  Calcium (PTH) Kidney GI Tract 19
  • 21. Pancreas 21
  • 22. Pancreas  Alpha cells: glucagon  Beta cells: insulin 22
  • 23. Pancreas Target Action Glucagon Liver  Glucose Insulin General  Glucose 23
  • 25. Adrenal 25
  • 26. Adrenal Medulla Target Action Norepi Heart Prolongs Epi Blood SNS Effects vessels Liver 26
  • 27. Adrenal Cortex Target Action Aldosterone Kidney  Na reabsobtion  Water retention Cortisol Most Tissue  Glucose inflammation 27
  • 28. Anterior Pituitary Drugs Inadequate Growth Excessive Growth Hormone Hormone  Dwarfism  Acromegaly  somatrem (Protropin®)  Gigantism  homatropin  Surgical removal 1º (Humatrope®)  octreotide (Sandostatin®) 28
  • 29. Posterior Pituitary Drugs  Oxytocin  ADH  Diabetes insipidus  Nocturnal enuresis  vasopressin (Pitressin®)  desmopressin (Stimate®)  lypressin (Diapid®) 29
  • 30. Parathyroid Diseases  Hypoparathyroidism  Inadequate calcium levels  TX: increased dietary calcium  Hyperparathyroidism  Excessive calcium levels  TX: surgical removal 30
  • 31. Thyroid Disease  Hypothyroidism  Hormone replacement  levothyroxine (Synthroid®)  Hyperthyroidism  Thyrotoxicosis  Surgical removal  propylthiouracil (PTU) 31
  • 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®) 32
  • 33. 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 33
  • 34. Oral Hypoglycemic Agents Sulfonylureas Alpha-glucosidase  insulin secretion inhibitors tolbutamide (Orinase®)  Delay carbohydrate chlorpropamide (Diabinese®) metabolism acarbose (Precose®) glipizide (Glucotrol®) miglitol (Glyset®) glyburide (Micronase®) Biguanides Thiazolidinediones metformin (Glucophage®)  Insulin effectiveness  Glucose synthesis troglitazone (Rezulin®)  Glucose uptake 34
  • 35. Hyperglycemic Agents  Glucagon  diazoxide   gluconeogenesis (Proglycem®)  Inhibits insulin release  D50W 35
  • 36. Estrogens & Progestins  Estrogens used for  Progestin post-menopausal  Diminish side effects of hormone replacement estrogen therapy therapy.  Nausea, fluid  estradiol (Estrace®) retention, breast tenderness  conjugated estrogens (Premarin®)  medroxyprogesterone acetate (Provera®)  estropipate (Ogen®)  norethindrone acetate (Aygestin®) 36
  • 37. 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 37
  • 38. 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®) 38
  • 39. Infertility Agents  Promote maturation of ovarian follicles  clomiphene (Clomid®)  urofollitropin (Metrodin®) 39
  • 40. Male Reproductive Agents  Testosterone Replacement  methyltestosterone (Metandren®)  fluoxymesterone (Halotestin®)  Benign Prostatic Hypertrophy  Surgery  finasteride (Proscar®) 40
  • 41. End of Session Services provided by Imhotep Virtual Medical School Individualized Webcam facilitated USMLE Step 1 Tutorials with Dr. Cray Starting at $50.00/hr., depending on pre-assessment. 1 BMS Unit is 4 hr. General Principles and some Organ System require multiple units to complete in preparation for the USMLE Step 1 A HIGH YIELD FOCUS in Biochemistry / Cell Biology, Microbiology / Immunology, the 4 P’s-Physiology, Pathophys., Path and Pharm and Intro to Clinical Medicine Webcam Facilitated USMLE Step 2 Clinical Knowledge and Clinical Skills didactic tutorials starting at $75.00 per hour /1 Unit is 4 hours, individualized one-on-one and group sessions, Including Introduction to Clinical Medicine and all Internal Medicine sub-specialities at the clerkship level. For questions or more information. drcray@imhotepvirtualmedsch.com ALL e-books and learning tools provided 41