Pharm of Anterior Pituitary Hormones Flashcards

1
Q

Three groups of anterior pituitary hormones

A

Somatotropic (GH, Prolactin)
Glycoprotein (LH, FSH, TSH)
Pro-opiomelanocortin (ACTH)

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2
Q

Common symptoms of adult hypopituitarism

A

Lack of milk, menstration, libido
Thin, soft, wrinkly skin
Diminished thyroid Fxn
Adrenal Deficiency

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3
Q

Symptoms of diminished thyroid fxn

A

Cold sensitivity
No sweat
Reduced metabolic rate
Poor radioiodine accumulation

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4
Q

Symptoms of adrenal deficiency

A

Sensitivity to physical stress
Increased rate of infection
Frequent episodes of collapse

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5
Q

Symptoms of hypopituitarism unique to kids

A

Dwarfism

Still responsive to stimulation by trophic hormones (thyroid and adrenal)

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6
Q

Oversecretion of ACTH –>

A

Cushing Syndrome

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7
Q

Hypersecretion of gonaadotropins in a pituitary tumor can cause..

A

precocious sexual development in children

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8
Q

Effects of Growth Hormone in hypopituitary dwarfs

A
  • Proportionate growth to normal individuals

- If continuous, leads to long limbs and short trunk

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9
Q

Three kinds of recombinant growth hormone

A

Somatropin
Somatrem
Nutropin Depot

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10
Q

How is Nutropin Depot different from other recombinant GH

A

Encapsulated in a biodegradable microspheres for intramuscular injection 1-2x per month

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11
Q

Important details for absorption/excretion of GH

A

Well absorbed, max concentration in 2-6 hrs

Cleared by liver + Kidney

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12
Q

Important details on GH Mode of Action

A

Dimerization of JAK STAT –>IP3+MAPK activation

Inducs production of IGFs (somatomedins) in liver

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13
Q

Important IGF details

A

Two kinds. IGF-1 is the primary mediator of IGF fxn. Type 1 receptors bind 1 and 2. Type 2 receptors just bind 2 to make receptors for lysosome directed substances.

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14
Q

In plasma, IGFs are bound by…

A

IGF-binding proteins (esp. IGFBP-3)

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15
Q

Three primary uses for GH therapy

A

Replacement therapy in deficiency children
Short pediatric patients
Replacement for adults with deficiency

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16
Q

Important characteristics to diagnose GH deficiency with

A

Under 4cm growth/year

Perform provocative test (give a stimulus like insulin induced hypglycemia and measure GH 45-90 mintues later.

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17
Q

GH replacement therapy is approved in children with height ____ standard deviations below national norm

A

2.25

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18
Q

Describe an adult with severe growth hormone dficiency

A

Generalized obesity, reduced muscle mass, reduced cardiac output.

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19
Q

Other than the main three, other uses for GH treatment

A

AIDS-associated wasting
Short Bowel Syndrome w/ total parenteral nutrition
Anti-aging program claims (not proven)

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20
Q

Some side effects associated with GH treatment in kids

A

Intracranial HTN
T2D
Scoliosis

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21
Q

Important side oeffects of GH treatment in adults

A

peripheral edema, arthralgia, carpal tunnel

Correlated with Increased mortality critically ill patients, like post-surgical or acute resp. failure

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22
Q

What are Macasermin and Mecasermin rinfabate? Why use them?

A

IGF-1 and IGF-1/IGFBP-3 analogs
Help patients with problems with IGF deficiencies, GH receptors problems, etc.
Think Laron-type dwarves (no GH receptors)

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23
Q

How to treat acromegaly

A
  1. GH secreting tumors treated w/ surgery +/- irradiation

2. Somatostatin analogs, dopamine agonists, growth hormone antagoniss

24
Q

Important somatostatin analogs

A

Lanreotide
OCTREOTIDE
Pasireotide

25
Why treat acro. w/ a dopamine agonist
Some GH secreting tumors come from prolactin secreting Pit cells.
26
Important details on Pegvisomant
GH antagonist Binds to 1 of the 2 binding sites of GH receptor, preventing the usual conformational modifications, stopping JAK STAT activation.
27
Other than Prolactin, what may end up accidently binding and acivating Prolactin receptor?
Growth Hormone | Placental Lactogen
28
Three causes of hyperprolactinemia
1. Treatment with a dopamine antagonist 2. Hypo/Pit disorder that interferes with PRIH/dopamine 3. Prolactin Secreting Pituitary Tumors
29
Symptoms of hyperporlactinemia
Galactorrhea, Amenorrhea, Infertility
30
Primary pharmacological treatment for hyperprolactinemia?
Dopamine Agonist
31
Important Dopamine agonists used to treat hyperprolactinemia (ergot derivatives)
Bromocriptine (7hr half life) | Carbegoline (65 hr half life)
32
How are dopamine agonists metabolized
bile --> feces
33
Plasma levels of LH and FSH are ___ after menopause
high
34
Important details about absorption, degradation, and excretion of Gonadotropic hormones
- Effective w/ Injection | - Degraged and cleared by liver + Kidney
35
Name the Native Preparations of Gonadotropic Hormones and important details
Chorionic Gonadotropin, Menotropins, Urofollitropin CH, LH+FSH, FSH Respectively Made from preg, post-meno, post-meno piss Injected
36
Name the recombinant gonadotropic hormones
Follitropin alpha and beta Lutropin alpha Choriogonadotropin alpha All still injected
37
Two primary uses of gonadotropic preparations
Infertility (either gender) | IVF
38
Toxicities and contraindications for gonadotropic preparations
Ovarian Hyperstimulation Multiple Pregnancies Gynecomastia
39
Name for recombinant human TSH | How is it cleared
Thyrotropin (Thyrogen) | Kidney
40
Use for thyrogen?
Tests involved in I uptake by residual gland | Metastasized thyroid carcinoma
41
Name the six Gonadotropin releasing hormone analogs
``` Gonadorelin HCL Leuprolide acetate Histrelin acetate Nafarelin acetate Gosereli acetate Triptorelin Pamoate ```
42
GnRH is secreted in a pulsitile fashion. Low frequency will favor ___ while high pulse frequency will favor ___
FSH | LH
43
Pulse frequency of GnRH that will stim FSH/LH secretion
0.5-1 / hr
44
Effect of continuous GnRH secretion (2-4 weeks)
Over 2-4 weeks, results in suppression of plasma concentrations of gonadotropins and gonadal steroids Causes desensitization fo GnRH receptors in pituitary cells
45
Effect of continuous GnRH secretions (3-10 days)
Increased gonadal hormone production from LH and FSH secretion. This is why you give estradiol/testosterone inhibitors in first few days of continuous treatmnet
46
Important details on GnRH preparation absorption and excretion
Natural is degraded in minutes, but synthetic is slowly degraded when injectd (hours). Synthetic is poorly absorbed. Mostly cleared by kidney
47
Four uses of GnRH treatmnet
Female Infertility Male Infertility Diagnosis of LH responsiveness (Hypogonadism) Suppression of Gonadal Activity
48
Pros and Cons of GnRH treatment of female infertility
Won't cause ovarian hyperstimulation | Hard to get gonadotropins, inconvenience of pump
49
Who might you try to use GnRH to suppress gonadal activity
``` Assisted eproduction therapy Endometriosis Uterine Fibroids Prostate Cancer Polycystic Ovarian Syndrome ```
50
Potential toxicity of GnRH analogs
Headache, Nausea, Flashing | Reduced Bone Density, Decreased Hematocrit
51
List Gonadotropin-Releasing Hormone Antagonists
Ganirelix (Assisted Repro) Cetrorelix (Assisted Repro) Abarelix (Advanced Prostate Cancer) Degarelix (Advanced Prostate Cancer)
52
Name the GH Releasing Hormone synthetic agonist
Sermorelin acetate
53
When would you use GH Releasing Hormone synthetic agonist
``` Diagnostic purposes (distinguish pituitary and hypothalamic defect) Kids with hypothalamix lesions ```
54
Name the synthetic preparation for Thyroid releasing hormone and impt. details
Protirelin | Synthetic, IV, short half life
55
Four important Somatostatin preparations
OCTREOTIDE ACETATE (clear in 80min) Sandostatin-LAR (once/4 weeks) Lanreotide (1/ 10-14 days) Pasireotide
56
Octreotide is used to treat...
``` Metastatic Carcinoid Tumors VIP secreting adenomas Gastrinoma, Glucagonoma WDHA Syndrome Acromegaly ```
57
Side effects of somatostatin preparations
Nausea | Abdominal Cramps, Flatulence, Steatorrhea w/ bulky bowel movements