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Endocrine Pharmacology > Pharmacology of the Hypothalamus and Pituitary Gland > Flashcards

Pharmacology of the Hypothalamus and Pituitary Gland Flashcards

1
Q

List the drugs that act on the hypothalamus

A

Octreotide, bromocriptine, cabergoline

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2
Q

List the drugs that act on the anterior pituitary

A

Somatropin, mecasermin, pegvisomant

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3
Q

List the drugs that act on the posterior pituitary

A

Oxytocin, Vasopressin, Desmopressin, Conivaptan

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4
Q

Which drug(s) are somatostatin analogs?

A

Octreotide

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5
Q

Which drug(s) are Dopamine (D2) agonists?

A

Bromocriptine, cabergoline

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6
Q

Which drug(s) are recombinant GH?

A

Somatropin

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7
Q

Which drug(s) are insulin-like growth factor 1?

A

Mecasermin

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8
Q

Which drug(s) are GH antagonists?

A

Pegvisomant

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9
Q

Which drug(s) are Antidiuretic hormone and analogs?

A

Vasopressin, desmopressin

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10
Q

Which drug(s) are vasopressin antagonists?

A

Conivaptan

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11
Q

What family of receptors do GH receptors belong to?

A

JAK/STAT cytokine receptors

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12
Q

Describe the regulation of release of growth hormone

A
  • GHRH binds to its receptor on pituitary somatotrophs -> increase in intracellular cAMP and Ca2+
  • GHRH acts synergistically with Ghrelin to promote GH release
  • Ghrelin acts on a receptor that is distinct from the GHRH receptor
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13
Q

What is Mecasermin?

A

A recombinant form of IGF-1

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14
Q

Describe the interaction of IGF-1 and insulin receptors

A

Insulin receptors can activate IGF-1 receptors and vice versa

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15
Q

What is the therapeutic use of mecasermin?

A

In children with GH insensitivity syndromes d/t:

  • GH receptor mutation (Laron syndrome)
  • Mutation in the post-GH signaling pathway
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16
Q

What are the AE’s of Mecasermin?

A

Hypoglycemia (up to 40%) [must have a snack 20 min prior to dose]

17
Q

What are the adverse effects of growth hormone in children?

A
  • Scoliosis
  • Increased ICP
  • Headache
  • Hyperglycemia
  • Otitis media (in children with Turner syndrome)
18
Q

What are the adverse effects of GH in adults?

A
  • Peripheral edema (81%)
  • Headache (18%)
  • Arthalgias (23%)
  • Myalgias (10%)
  • Paresthesias (13%)
  • Hypoesthesia (11%)
  • Hyperglycemia
  • Nerve numbness, muscle or joint pain; carpal tunner syndrome
19
Q

What are the contraindications/precautions of GH?

A
  • Diabetic retinopathy
  • Pediatric patients w/ epiphyseal closure
  • Acute clinical illness, neoplastic disease
20
Q

Why is human somatostation not used?

A

It has limited therapeutic usefullness because of its short duration of action and its multiple effects in many secretory systems

21
Q

What is octrotide?

A

A somatostatin analog

22
Q

What is the MOA of somatostatin and its drugs?

A

Activation of somatostatin receptors decreases the synthesis of cAMP, which in turn leads to inhibition of GH secretion

23
Q

What are the side effects of somatostatin?

A

GI effects, multi organ effects. It inhibits virtually all exocrine and endocrine secretions of the

  • pancreas
  • stomach
  • intestine
  • parathyroid
24
Q

What is the therapeutic use of somatostatin?

A

It is used in patients suffering from gigantism and acromegaly.

(note: excessive GH secretion is almost always due to a pituitary adenoma)

25
Q

What drugs can be used to combat gigantism and acromegaly and what are their classes/MOA?

A
  • Octreotide - a somatostating analog
  • Cabergoline, a D2 dopamine antagonist
  • Pegvisomant, a GH receptor antagonist

(reminder: Gh receptors are JAK-STAT receptors)

26
Q

what are the actions of prolactin?

A
  • Stimulation of breast growth and milk production
  • Inhibition of ovulation
27
Q

What are the effects of hyperprolactinemia?

A
  • Gynecomastia, low libido, ED, infertility in men
  • Amenorrhea, galactorrhea in women (pre-menopausal)
28
Q

What are the half-lives of bromocriptine and cabergoline?

A

Bromocriptine ~ 10hrs

Cabergoline ~65hrs

29
Q

What are the AEs of dopamine agonists?

A
  • Nausea, anorexia, vomiting, constipation
  • Postural hypotension, cardiac arrhythmias
  • Dyskinesias
  • Headache, insomnia, nightmares, confusion
  • Delusions, hallucination
30
Q

What are the contraindications/precautions of D2 agonists?

A
  • Psychotic disorders
  • Hypertension
  • History of fibrotic disorders
31
Q

What are the therapeutic uses of D2 agonists?

A
  • very effective at lowering prolactin levels
  • tumor shrinkage (but will rebound upon discontinuation of drug)
  • Hyperprolactinemia
  • Cabergoline - acromegaly in combation with a somatostatin analog
32
Q

What is the physiologic role of Oxytocin?

A
  • Uterine muscle contraction
  • Elicits milk ejection from the breast
33
Q

What is the MOA of oxytocin?

A
  • acts through GPCR and IP3 second messenger system to contract uterine smooth muscle
  • Also stimulates release of PGs and LTs
34
Q

What is the therapeutic use of oxytocin?

A
  • induction and maintenance of labor
  • stimulate milk ejection (nasal oxytocin)
  • sometimes to control post-partum hemorrhage (however, ergot alkaloids are better)
35
Q

What are the AEs of oxytocin?

A
  • Hypertensive crisis
  • Fetal distress, placental abruption, uterine rupture
  • Fluid retention/water intoxication, hyponatremia, heart failure, seizures, death; fetal death
36
Q

What is vasopressin?

A

Vasopressin is an anti-diuretic hormone (literally ADH)

37
Q

What are the vasopressin receptors and what do they target?

A
  • V1 - vasoconstriction increased inositide turn over and increased intracellular Ca2+
  • V2 - increase cAMP (increase water permeability (via aquaporins) and resorption (via aquaporins) in the collecting tubules
38
Q

What is desmopressin?

A

An ADH analog that specifically targets V2 receptors to increase anti-diuretic effect while limiting the vasoconstriction effect. It also has a longer half-life.

39
Q

What are conivaptan and tolvaptan?

A

They are ADH antagonists.

Endocrine Pharmacology (5 decks)

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