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Endocrine Pharmacology > Drugs Affecting Hypothalamic, Pituitary and Thyroid Function > Flashcards

Drugs Affecting Hypothalamic, Pituitary and Thyroid Function Flashcards

1
Q

Anterior Pituitary Hormones

Hormones of the adenohypophysis or anterior pituitary or are essential for:

A
  1. Regulating growth and development
  2. Stimulating the reproductive system
  3. Providing a response to stress and
  4. Regulating intermediary metabolism
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2
Q

Anterior Pituitary Hormones

Synthesis and secretion of these hormones are controlled by:

A
  • hypothalamic factors
  • peripheral hormones
  • drugs
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3
Q

Three Classes Anterior Pituitary Hormones

A
  1. Somatotropic hormones
  2. Glycoprotein hormones
  3. Proopiomelanocortin (POMC)
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4
Q

Somatotropic hormones

A

growth hormone (GH) and prolactin (Prl)

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5
Q

Glycoprotein hormones

A

thyrotropin (TSH), luteinizing hormone (LH), and follicle-stimulating hormone (FSH) (α-subunit the same, β-subunit different) Also, placental chorionic gonadotropin (CG)

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6
Q

Proopiomelanocortin (POMC)

A

derived hormones – corticotropin (ACTH), α- and β- melanocytestimulating hormones (α-MSH and β-MSH)

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7
Q

(GHRH)

A

Growth Hormone-Releasing Hormone

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8
Q

(GnRH)

A

Gonadotropin-Releasing Hormone

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9
Q

(TRH)

A

Thyrotropin-Releasing Hormone

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10
Q

(CRH)

A

Corticotropin-Releasing Hormone

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11
Q

Somatostatin negatively regulates secretion of?

A

GH and TSH

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12
Q

Dopamine inhibits secretion of?

A

Prl

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13
Q

GH has direct effects, but also acts on some target

tissues to produce?

A

Insulin-like growth factor 1 (IGF-1).

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14
Q

GH what occurs with Hypoglycemia & Hyperglycemia?

A

Hypoglycemia stimulates GH release, hyperglycemia

inhibits GH release.

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15
Q

GH effects?

A 
Decrease Insulin sensitivity
Increase Lipolysis
Increase IGF-1
Increase Protein Synthesis
Increase Epiphyseal (Bone) Growth
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16
Q

Somatropin is the generic name of all?

A

GH that is identical with hGH.

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17
Q

Somatrem is the generic name for?

A

GH with an additional methionine.

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18
Q

IGF-1 Deficiency?

A

IGF-1 deficiency occurs in a small number of children. They do not respond to hGH.

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19
Q

Mecasermin is a complex of?

A

hIGF-1 and hIGFBP-3 (IGF binding protein 3. The binding protein is necessary to produce a longer half-life.

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20
Q

Children with severe IGF-1 deficiency

usually have?

A

IGFBP deficiency also.

21
Q

Growth Hormone Excess Causes?

A

(Gigantism and Acromegaly)

22
Q

Somatostatin analogs are the best treatment when?

A

Pituitary surgery is impossible.

23
Q

Most widely used drug for growth hormone excess and what are side effects?

A

Octreotide. 3x daily injections (short half-life)

Side effects are GI – diarrhea, nausea, abdominal pain.

24
Q

A long-acting, slow release form Sandostatin-LAR

is available and is Injected once every

A

4 weeks.

25
Q

Lanreotide is

A

Drug for growth hormone excess now available in the U.S.

26
Q

Pegvisomant is?

A

Growth hormone receptor antagonist - treatment of acromegaly - decreases IGF-1.

27
Q

PEG (polyethylene glycol) is?

A

Covalently bound - decreases renal clearance and so increases half-life.

28
Q

Prolactin rises during?

A

Pregnancy, remains elevated until birth, and falls thereafter unless the mother breast-feeds her infant.

29
Q

Hyperprolactinemia is?

A

Relatively common. Caused by pituitary adenomas (or diseases that interfere with dopamine signalling.)

30
Q

Drugs used in treatment of hyperprolactinemia:

A

Cabergoline: Higher affinity for D2 receptors, longer half-life.
Bromocriptine: Not well tolerated, but FDA approved.

31
Q

The gonadotropic hormones are?

A

LH, FSH and CG because of their actions on the gonads.

32
Q

GnRH regulates systhesis and secretion of?

A

LH and FSH.

33
Q

In men, LH acts on the testicular Leydig

cells to stimulate synthesis of?

A

Androgens, primarily testosterone, necessary for spermatogenesis.

34
Q

Synthetic GnRH are available, but half lives are?

A

2 to 4 min.

35
Q

What is Leuprolide and how is it special?

A

Synthetic GnRH. Analogues have substitutions at aa position 6 that inhibit proteolysis prolong half life plus C-terminal substitutions improve receptor binding

36
Q

One synthetic GnRH (gonadorelin hydrochloride) is used for?

A

Diagnostic purposes to differentiate between pituitary and hypothalamic defects in patients with hypogonadotropic hypogonadism.

37
Q

Chorionic gonadotropins (CG) is secreted by the placenta in early stages?

A

Of pregnancy.

38
Q

Chorionic gonadotropins drug and action?

A

Pregnyl from urine of pregnant women, mimic action of LH and are used to treat infertility in women.

39
Q

Urine from postmenopausal women contains?

A

FSH and LH, is called menotropin. Administered IM.

40
Q

Recombinant FSH (rFSH) is also available? How is it admisitered?

A

(follitropin α and follitropin β). Administeded SC. These preparations are also used in women in treatment of infertility.

41
Q

GnRH Receptor Antagonists drugs?

A

Cetrorelix and ganirelix and Degarelix.

42
Q

Cetrorelix and ganirelix are?

A

Decapeptide antagonists of GnRH receptors used in in vitro fertilization. They delay premature LH surge.
Delays ovulation to allow collection of ova (controlled
ovarian hyperstimulation). Follows FSH therapy.

43
Q

Degarelix is approved for?

A

Men with advanced prostate cancer. GnRH Receptor Antagonists.

44
Q

GnRH Agonists drugs?

A

Leuprolide

45
Q

Leuprolide is an agonist of and used in the treatment?

A

GnRH used in treatment of prostate cancer. Initially increases LH production, then decreases LH and testosterone dramatically due to receptor downregulation.

46
Q

Thyrotropin-Releasing Hormone (TRH) drugs?

A

Thyrotropin alpha hTRH

47
Q

Thyrotropin alpha hTRH Used in?

A

Diagnostics for thyroglobulin levels.

48
Q

Corticotropin-Releasing Hormone (CRH) used for?

A

Used only for diagnostics. To distinguish Cushing’s disease from ectopic ACTH syndrome (tumors of lung, thymus, pancreas, thyroid, and adrenal gland).

Endocrine Pharmacology (5 decks)

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