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
Q

Why treat acro. w/ a dopamine agonist

A

Some GH secreting tumors come from prolactin secreting Pit cells.

26
Q

Important details on Pegvisomant

A

GH antagonist
Binds to 1 of the 2 binding sites of GH receptor, preventing the usual conformational modifications, stopping JAK STAT activation.

27
Q

Other than Prolactin, what may end up accidently binding and acivating Prolactin receptor?

A

Growth Hormone

Placental Lactogen

28
Q

Three causes of hyperprolactinemia

A
  1. Treatment with a dopamine antagonist
  2. Hypo/Pit disorder that interferes with PRIH/dopamine
  3. Prolactin Secreting Pituitary Tumors
29
Q

Symptoms of hyperporlactinemia

A

Galactorrhea, Amenorrhea, Infertility

30
Q

Primary pharmacological treatment for hyperprolactinemia?

A

Dopamine Agonist

31
Q

Important Dopamine agonists used to treat hyperprolactinemia (ergot derivatives)

A

Bromocriptine (7hr half life)

Carbegoline (65 hr half life)

32
Q

How are dopamine agonists metabolized

A

bile –> feces

33
Q

Plasma levels of LH and FSH are ___ after menopause

A

high

34
Q

Important details about absorption, degradation, and excretion of Gonadotropic hormones

A
  • Effective w/ Injection

- Degraged and cleared by liver + Kidney

35
Q

Name the Native Preparations of Gonadotropic Hormones and important details

A

Chorionic Gonadotropin, Menotropins, Urofollitropin
CH, LH+FSH, FSH Respectively
Made from preg, post-meno, post-meno piss
Injected

36
Q

Name the recombinant gonadotropic hormones

A

Follitropin alpha and beta
Lutropin alpha
Choriogonadotropin alpha

All still injected

37
Q

Two primary uses of gonadotropic preparations

A

Infertility (either gender)

IVF

38
Q

Toxicities and contraindications for gonadotropic preparations

A

Ovarian Hyperstimulation
Multiple Pregnancies
Gynecomastia

39
Q

Name for recombinant human TSH

How is it cleared

A

Thyrotropin (Thyrogen)

Kidney

40
Q

Use for thyrogen?

A

Tests involved in I uptake by residual gland

Metastasized thyroid carcinoma

41
Q

Name the six Gonadotropin releasing hormone analogs

A
Gonadorelin HCL
Leuprolide acetate
Histrelin acetate
Nafarelin acetate
Gosereli acetate
Triptorelin Pamoate
42
Q

GnRH is secreted in a pulsitile fashion. Low frequency will favor ___ while high pulse frequency will favor ___

A

FSH

LH

43
Q

Pulse frequency of GnRH that will stim FSH/LH secretion

A

0.5-1 / hr

44
Q

Effect of continuous GnRH secretion (2-4 weeks)

A

Over 2-4 weeks, results in suppression of plasma concentrations of gonadotropins and gonadal steroids
Causes desensitization fo GnRH receptors in pituitary cells

45
Q

Effect of continuous GnRH secretions (3-10 days)

A

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
Q

Important details on GnRH preparation absorption and excretion

A

Natural is degraded in minutes, but synthetic is slowly degraded when injectd (hours). Synthetic is poorly absorbed. Mostly cleared by kidney

47
Q

Four uses of GnRH treatmnet

A

Female Infertility
Male Infertility
Diagnosis of LH responsiveness (Hypogonadism)
Suppression of Gonadal Activity

48
Q

Pros and Cons of GnRH treatment of female infertility

A

Won’t cause ovarian hyperstimulation

Hard to get gonadotropins, inconvenience of pump

49
Q

Who might you try to use GnRH to suppress gonadal activity

A
Assisted eproduction therapy
Endometriosis
Uterine Fibroids
Prostate Cancer
Polycystic Ovarian Syndrome
50
Q

Potential toxicity of GnRH analogs

A

Headache, Nausea, Flashing

Reduced Bone Density, Decreased Hematocrit

51
Q

List Gonadotropin-Releasing Hormone Antagonists

A

Ganirelix (Assisted Repro)
Cetrorelix (Assisted Repro)
Abarelix (Advanced Prostate Cancer)
Degarelix (Advanced Prostate Cancer)

52
Q

Name the GH Releasing Hormone synthetic agonist

A

Sermorelin acetate

53
Q

When would you use GH Releasing Hormone synthetic agonist

A
Diagnostic purposes (distinguish pituitary and hypothalamic defect)
Kids with hypothalamix lesions
54
Q

Name the synthetic preparation for Thyroid releasing hormone and impt. details

A

Protirelin

Synthetic, IV, short half life

55
Q

Four important Somatostatin preparations

A

OCTREOTIDE ACETATE (clear in 80min)
Sandostatin-LAR (once/4 weeks)
Lanreotide (1/ 10-14 days)
Pasireotide

56
Q

Octreotide is used to treat…

A
Metastatic Carcinoid Tumors
VIP secreting adenomas
Gastrinoma, Glucagonoma
WDHA Syndrome
Acromegaly
57
Q

Side effects of somatostatin preparations

A

Nausea

Abdominal Cramps, Flatulence, Steatorrhea w/ bulky bowel movements