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Systems Pharmacology (CVS, Respiratory, Endocrine, Reproductive, GIT, Renal System) > Hypothalamic & Pituitary Hormones > Flashcards

Hypothalamic & Pituitary Hormones Flashcards

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1
Q

Effects of GH is primarily mediated by regulating the production of ______ in peripheral tissues.

A

Insulin-like Growth Factor 1

(IGF-1)

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2
Q

Recombinant form of human GH.

A

Somatropin.
-acts through GH receptors to increase production of IGH-I

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3
Q

GH/Somatropin in Children.

A
  1. Genetic diseases associated with short stature:
    - Turner syndrome.
    - Noonan syndrome.
    - Prader-Willi syndrome.
  2. To improve growth in children with failure to thrive due to chronic renal failure or the small-for-gestational-age condition.
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4
Q

Controversial use of GH/Somatotropin.

A

Idiopathic short stature who are not GH deficient.
-Great cost.
-Risk of toxicity.
Result: 1.5-3 inches average increase in final adult height.

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5
Q

GH/Somatotropin in Adults.

A
  1. Treatment of AIDS-associated wasting.
  2. GH deficiency.
  3. Improve GIT function in patients who have undergone intestinal resection and have subsequently developed a malabsorption syndrome.
  4. Increase in muscle mass for athletes.
  5. Recombinant bovine GH is used to increase milk production in cattle.
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6
Q

Antiaging programs use GH; sideeffects.

A

Analogs of GH and IGF-1 shorten lifespan.

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7
Q

Rare, serious adverse effects of GH in children.

A
  • Pseudotumor cerebri.
  • Slipped capital femoral epiphysis.
  • Progression of scoliosis.
  • Edema.
  • Hyperglycemia.
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8
Q

Adverse effects of GH in adults.

A
  • Peripheral edema.
  • Myalgia.
  • Arthralgia.
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9
Q

Recombinant human IGF-1.

A

Mecasermin.

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10
Q

______ is administered parenterally to children with IGF-1 deficiency.

A

Mecasermin

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11
Q

Toxicity of Mecasermin.

A

Hypoglycemia, intracranial hypertension, increased liver enzymes.

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12
Q

rhIGFBP-3.

A

In some countries, children are treated with Mecasermin Rinfabate, a combination of recombinant human IGF-1 and human insulin-like growth factor-binding protein-3.
Mecasermin rinfabate increases the half-life of IGF-1.

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13
Q

Growth hormone secreting pituitary adenomas.

A

Adults - Acromegaly.
Children and Adolescents - Gigantism

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14
Q

Somatostatin.

A

A 14 amino acid peptide.
Inhibits release of GH, Glucagon, Insulin, Gastrin.

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15
Q

Ocreotide and Lanreotide.

A

-Long-acting synthetic analogs of somatostatin.
Used to treat:
-Acromegaly
-Carcinoid
-Gastrinoma
-glucagonoma
-other endocrine tumors

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16
Q

Regular Octreotide.

A
  • Administered subcutaneously.
  • 2-4 times a day.
  • A somatostatin analogue having high potency and long duration of action.
  • It is preferred over somatostatin for all the indications.
  • Also inhibits TSH secretion and is the treatment of choice for TSH-secreting adenoma in patients who are not the candidates of surgery.
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17
Q

Slow-release intramuscular formulation of ocreotide or lanreotide.

A

Administered every 4 weeks for long-term therapy.

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18
Q

Side effects of Ocreotide and Lantreotide.

A
  • GIT disturbances
  • Gallstones
  • Cardiac conduction abnormalities
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19
Q

Hypothalamus secretes GHRH.

A

Increases GH release.

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20
Q

Somatostatin.

A

Inhibits GH release.

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21
Q

Sermorelin and Hexarelin.

A

Are recombinant GHRH analogs that are used for pituitary dwarfism.

22
Q

Pegvisomant.

A

Is a GH receptor antagonist
Indicated for the treatment of acromegaly.

23
Q

Pasireotide.

A

A new somatostatin analog approved for the treatment of Cushing’s disease.

24
Q

A Dopamine D2 receptor agonist.

A

Bromocriptine.

25
Q

Bromocriptine is more effective at inhibiting ___ release than inhibitong GH release.

A

Prolactin

26
Q

Normally, GH inititiates cellular signalling cascades by ___ing 2 GH receptor.

A

Dimerizing

27
Q

The 3 basic steps in ovulation induction protocols that use gonadotropins?

A
  1. Administration of a GnRH agonist or antagonist to inhibit endogenous gonadotropin production.
  2. Follicle development is driven by daily injections of a preparation with FSH activity i.e. menotropins, FSH, FSH analog.
  3. The final stage of oocyte maturation is induced with an injection of LH or LH analog hCG (Human Chorionic Gonadotropin)
28
Q

Gonadotropins.

A

Hormones synthesized and released by the anterior pituitary.

29
Q

Menotropins?

A

These gonadotropins consist of a mixture of FSH and LH purified from the urine of postmenopausal women.

30
Q

Three forms of FSH analogs.

A
  1. Urofollitropin is a purified extracted from the urine of postmenopausal women.
  2. Follitropin alpha and 3. Folitropin beta, are recombinant forms of FSH, they differin composition of their carbohydrate side chains.
31
Q

LH and its analogs.

A
  1. hCG (placental protein, structure identical to LH, activates LH receptors)
  2. Lutropin, a recombinant form of human LH.
32
Q

Use of synthetic GnRH (gonadorelin).

A

To differentiate between pituitary and hypothalamic defects in hypogonadotropic hypogonadism > if Lh levels increase (>10mIU/ml) after administarion of GnRH, it indicates that pituitary is normal.

33
Q

GnRH.

A
  • A decapeptide.
  • Stimulates gonadotropin release when it is secreted in a pulsatile pattern by the hypothalamus.
34
Q

Long-acting GnRH agonists.

A
  • Leuprolide
  • Goserelin
  • Histrelin
  • Nafarelin
  • Triptorelin
35
Q

How do GnRH agonists inhibit gonadotropin release?

A

By down regulating GnRH receptors in the pituitary cells that normally release gonadotropins.

36
Q

Long-term treatment with GnRH agonist.

A
  1. In women, symptoms of menopause i.e. hot flushes, sweats, headache. Also, long-term treatment is avoided due to risk of bone loss and osteoporosis.
  2. In men, hot flush, sweats, gynecomastia, reduced libido, decreased hematocrit and bone density.
37
Q

What conditions can be exarcerbated in first few weeks of therapy with GnRH agonist?

A
  1. In men, prostrate cancer.
  2. In children with precocious puberty.
38
Q

Ganirelix, cetrorelix and degarelix are GnRH antagonists. Uses.

A
  • Ganirelix and cetrorelix are used in ovulation induction in place of GnRH agonists to suppress endogenous gonadotropin production.
  • Degarelix is used for advanced prostate cancer.
39
Q

Prolactin Antagonists (Dopamine D2 receptor agonists)

A

“Dopamine is the physiologic inhibitor of prolactin release.”
Prolactin-secreting adenomas usually retain their sensitivity to dopamine.

40
Q

Drugs for hyperprolactinemia.

A

Prolactin antagonists; bromocriptine and other orally active D2 dopamine receptor agonists (e.g. cabergoline, pergolide).
They reduce serum prolactin levels and restore fertility.

41
Q

Oxytocin

A
  • A nonapeptide.
  • Synthesized in the paraventricular nuclei of the hypothalamus.
  • Transported through the axons of these cells to the posterior pituitary.
42
Q

Tocolytic.

A

A drug used to suppress preterm labor.

43
Q

Oxytocin antagonist.

A

Atosiban; an antagonist of the oxytocin receptor which is used in some countries as a tocolytic.

44
Q

Acromegaly.

A

A rare syndrome of growth hormone (GH) excess in adults characterized by abnormal growth of tissues, metabolic abnormalities, and cardiac function.

45
Q

Vasopressin (Antidiuretic Hormone)

A
  • Synthesized in neuronal cell bodies in hypothalamus.
  • Released from nerve terminals in posterior pitutary.
  • Acts through V2 receptors in kidney.
  • External V2 like receptors regulate the release of coagulation factor VIII and Von Willebrand factor.
46
Q

Vasopressin agonist.

A

Desmopressin;

  • V2 receptor selective.
  • administered orally, nasally or parenterally.
  • For diabetes insipidus, mild heophilia A or von Willebrand disease.
47
Q

To treat bleeding from esophageal varices and colon diverticula.

A

-Vasopressin.
Contracts vascular smooth muscle by activating V1 receptors.

48
Q

Conivaptan and Tolvaptan.

A
  • Antagonists of vasopressin receptors.
  • They offset the fluid retention resulting from excessive production of vasopressin in hyponatremia or acute heart failure.
49
Q

Dopamine increases GH release in normal subjects but ____ it in acromegalics.

A

Dopamine increases GH release in normal subjects but decreases it in acromegalics.

50
Q

Sermorelin and hexarelin

A

Sermorelin and hexarelin are recombinant GHRH analogs that are used for pituitary dwarfism.

51
Q
A

Systems Pharmacology (CVS, Respiratory, Endocrine, Reproductive, GIT, Renal System) (8 decks)

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