Pharmacology Exam 6

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Pharmacology Exam 6
2011-04-16 18:18:02
Hypothalamic Pituitary Hormones

Hypothalamic and Pituitary Hormones
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  1. Pharmacologic applications of hormones
    • replacement therapy for hormone deficiency
    • antagonists for diseases that result from excess production of P.H.
    • diagnostic tools for endocrine abnormalities
  2. 3 classifications of hormones based on structure and type of receptor activated
    • GH & PRL
    • TSH, FSH & LH
    • ACTH
  3. GH and PRL
    • single chain proteins
    • both activate JAK/STAT super family
  4. TSH, FSH, and LH
    • dimeric proteins
    • activate GPCRs
    • share common alpha chains
  5. ACTH
    single peptide cleaved from a larger chain
  6. GNRH & Somatostatin
    GNRH stimulates and Somatostatin inhibits GH and somatotropin from AP which bind ILGF 1 on liver, muscle, bone & kidney
  7. Thyrotropin Releasing hormone
    stimulates release of thyroid stimulating hormone from the AP which causes release of thyroxine and triiodothyronine from the thyroid
  8. Corticotropin releasing hormone
    stimulates release of adrenocorticotropin from the AP which acts on the adrenal cortext to secrete glucocorticoids, androgens and mineral corticoids
  9. GnRH
    stimulates release of FSH and LH from the AP which binds on the gonads to stimulate release of estrogen, progesterone and testosterone
  10. Dopamine
    • inhibits release of prolactin from the AP
    • target organ is breast
  11. Clinical use of GHRH
    used rarely as a diagnostic test for GH responsiveness
  12. Clinical use of TRH/Protirelin
    used rarely to diagnose hypo/hyperthyroidism
  13. clinical use of CRH
    Used rarely to distinguish Cushing's Disease from ectopic ACTH secretion
  14. clinical use of GnRH
    used rarely in pulses to treat infertility cuased by hypothalamic dysfunction
  15. clinical uses of Dopamine
    DA agonists used for hyperprolactinemia
  16. Diagnostic use of TSH and Thyrotropin
    thyroid carcinoma
  17. Diagnostic use of ACTH
    adrenal insufficiency
  18. Clinical uses of growth hormone
    • growth
    • improve metabolic state
    • increase lean body mass
    • increase sense of well being
    • increase weight and physical endurance
    • improved GI function
  19. Orlistat MoA and Toxicity
    • GI lipase inhibitor
    • reduces absorption of fats
    • flatulence, steatorrhea, fecal incontinence
  20. Sibutramine
    • inhibits SERT/NET in the CNS
    • reduces appetite
    • tachycardia and HTN
  21. Rimonabant
    • CB1 receptor antagonist in the CNS
    • reduces appetite
    • depression, anxiety, nausea
  22. Mecasermin
    • IGF1 - Agonist
    • restores normal and metabolic IGF-1 effects in individuals with IGF-1 deficiency
  23. Growth hormone antagonists
    • somatostatin analogs that inhibit release of GH, glucagon, insulin, gastrin
    • somatostatin T1/2 = 1-3 min
  24. Octreotide
    • somatostatin analog
    • greater selectivity for inhibition of GLU, GH and Insulin
  25. Octreotide indications
    • VIPomas
    • watery diarrhea
    • AIDS associated diarrhea
    • acromegaly
  26. Octreotide drug interactions
    interferes with cyclosporins by decreasing bioavailability
  27. Octreotide ADEs
    • Abd pain
    • n/v
    • diarrhea
    • chills
    • headache
    • injection site reaction
  28. Pegvisomant
    GH receptor antagonist used for acromegaly
  29. Somatropin
    • recombinant GH
    • less immunogenic
  30. Somatropin indication
    • growth failure
    • turner's syndrome
  31. somatropin warnings
    • use cautiously in pt with diabetes
    • pt with untreated hypothyroidism will have an inadequate response
  32. ADEs with somatropin
    • intracranial hypertension
    • visual changes/headache
    • n/v
    • increase serum P+, Alkaline phosphatase and parathyroid hormone
    • increase CYP metabolism
    • arthralgia
    • gynecomastia
  33. Sermorelin
    synthetic parenteral GHRH to treat GH deficiency
  34. Sermorelin Drug interactions
    • decreases insulin
    • decreases clotting factors (do not give with ASA)
    • indomethacin affects the secretion of somatotrope
  35. Sermorelin ADEs
    • transient warmth
    • face flushing
    • injections site reaction
    • n/v
    • headache
  36. Leuprolide
    • GnRH synthetic analog
    • for treatment of prostate cancer, early puberty and anemia due to fibroid tumors
    • used for ovairan/breast cancer
  37. Oxytocin
    • stimulates contraction of uterus smooth muscle
    • can cause premature delivery, herpes, eclampsia, cervical cancer, chest pain, difficulty breathing and confusion
  38. Vasopressin
    reduces amount of urine excreted from the body
  39. Vasopressin indicated for
    • prevention and treatment of post operative distention
    • abdominal roentergenography to dispel gas shadows
    • to treat diabetes insipidus
  40. Two main actions of ADH and Vasopressin
    • causes kidney to reabsorb water
    • causes narrowing of blood vessels
  41. Vasopressin ADEs
    • allergic reactions
    • anaphylaxis
    • cardiac arrest
  42. Drugs that decrease vasopressin effects
    • demeclocycline
    • norepinephrine
    • lithium
    • heparin
  43. Drugs that potentiate vasopressin effects
    • fludrocortisone
    • TCAs