growth hormone action

GHRH stimulates GH release via ______ pathways

• cAMP-CA2+ pathway

Ghrelin acts through _____, enhancing GH secretion

• GH Secretagogue receptors

somatostatin suppresses GH by activating ______

• Gi coupled receptors

what is first line for growth hormone excess

• surgical removal of GH-secreting adenomas

somatostatin analogues (increase/reduce) GH Secretion

• reduce

T/F: repetitive administration of somatostatin receptor agonists results in desensitization

• false

  • does NOT result in desensitization

what has to be monitored with somatostatin receptor agonists?

• IGF-I levels

which somatostatin receptor agonist can cause or worsen hyperglycemia?

a) Octreotide

b) Lanreotide

c) Pasireotide

d) Paltusotine

c) Pasireotide

which of the following is a non-peptide selective somatostatin receptor subtype 2 (SST2) agonist?

a) Octreotide

b) Lanreotide

c) Pasireotide

d) Paltusotine

d) Paltusotine

somatostatin receptor agonist adr

• GI symptoms, constipation/diarrhea, N/V

• cholelithiasis

• glucose dysregulation

• HTN

• bradycardia

Pegvisomant MOA

• GH receptor antagonist

  • mutated GH molecule with polymers to prolong half-life

Pegvisomant causes…

a) decreased IGF-I and GH

b) increased IGF-I and GH

c) decreased IGF-I and the same GH

d) the same IGF-I and decreased GH

c) decreased IGF-I and the same GH

ADR of Pegvisomant

• increase LFTs

• lipohypertrophy at injection sit and other sites

how do dopamine receptor agonists work? what can it help with?

• block pituitary release of GH

  • may inhibit GH secretion in some patients with mild acromegaly

what drug class is Octreotide?

• somatostatin analog

what drug class is Lanreotide?

• somatostatin analog

what drug class is Pasireotide

• somatostatin analog

what drug class is Paltusotine

• oral non-peptide somatostatin receptor agonist

what drug class is Pegvisomant

• GH receptor antagonist

what drug is class is Cabergoline

• Dopamine D2 receptor agonist

what drug class is Bromocriptine

• Dopamine D2 receptor agonist

which of the following can cause valvular heart disease at high doses

a) octreotide

b) cabergoline

c) bromocriptine

d) pegvisomant

• b) cabergoline

which of the following is first-line pharmacologic therapy that decreases GH and IGF-I and may shrink tumor?

a) lanreotide

b) pasireotide

c) pegvisomant

d) octreotide

d) octreotide

which of the following is used as along-acting deep SC injection every 4 weeks

a) lanreotide

b) pasireotide

c) pegvisomant

d) octreotide

a) lanreotide

T/F: Pasireotide is more potent than octreotide

• true

  • but causes hyperglycemia

which of the following is the first oral small-molecule somatostatin agonist for acromegaly?

a) pegvisomant

b) bromocriptine

c) paltusotine

d) octreotide

c) paltusotine

_____ stimulates GH secretion

_______ inhibits GH secretion

• GHRH + ghrelin

• somatostatin + IGF-I

what is the main therapy for the treatment of GH deficiency?

• recombinant human growth hormone (somatropin)

GH replacement ADR

• edema

• glucose intolerance

• intracranial HTN

• headaches

• increased IOP

what drug class is somatropin?

• recombinant human growth hormone

what drug class is Somapacitan?

• Long-acting GH analog

what drug class is Somatrogon?

• Long-acting GH analog

what drug class is Lonapegsomatropin?

• Long-acting GH prodrug

what drug class is Mecasermin?

• recombinant insulin-like growth factor-I (IGF-I)

what drug class is Sermorelin?

• Growth-hormone release hormone (GHRH) analog

which of the following is used as once-weekly GH therapy for adults?

a) Lonapegsomatropin

b) Somatrogon

c) Somapacitan

d) Somatropin

c) Somapacitan

which of the following is used as once-weekly GH therapy for pediatric patients?

a) Lonapegsomatropin

b) Somatrogon

c) Somapacitan

d) Somatropin

b) Somatrogon

Somatropin is titrated based on …

• IGF-I levels

Mecasermin counseling administration

• must be administered with meals/snacks to prevent hypoglycemia

Sermorelin requires ______ to be effective

• intact pituitary function

somatropin and long-acting analogs cause

a) hypoglycemia

b) hyperglycemia

b) hyperglycemia

which of the following causes hypoglycemia?

a) somatropin

b) sompacitan

c) somatrogon

d) mecasermin

d) mecasermin

Metabolic process stimulated by GH increasing free fatty acids

• lipolysis

Condition of GH excess before epiphyseal closure

• gigantism

GH effect promoting protein synthesis and growth

• anabolic

Active malignancy is a major contraindication with this class of drugs

a) recombinant IGF-I

b) GH receptor antagonists

c) somatotropins

d) dopamine receptor agonists

c) somatotropins

GH receptor requires this process for activation

• dimerization

Type of receptor activated by GH

cytokine

GH receptor antagonist that decreases IGF-1 levels

• pegvisomant

Recombinant insulin-like growth factor-1 that must be administered with meals to avoid hypoglycemia

• mecasermin

Somatostatin analog that may cause lipohypertrophy both at the injection site and in
other parts of the body

• Pegvisomant

Hormone stimulating hepatic IGF-1 production

• GH

Dopamine receptor agonist used in mild acromegaly with valvular heart disease as an ADR

• Cabergoline

GH secretion pattern characterized by highest release during sleep

• Pulsatile

Somatostatin analog with severe hyperglycemia as a potential ADR

• Pasireotide

Oral non-peptide somatostatin receptor agonist

• paltusotine

Drug used in acromegaly that activates somatostatin receptors

• octreotide

Recombinant human growth hormone that binds GH receptors to stimulate IGF-1
production

• somatotropin

Intracellular signaling pathway activated by GH receptor

• Jakstat

Requires intact pituitary function to be effective

• sermorelin

Hypothalamic hormone that inhibits GH via Gi-coupled receptors

• somatostatin

Hormone with anti-insulin effects increasing glucose levels

• GH

Disorder due to excess GH after epiphyseal closure

• acromegaly

Hypothalamic hormone that stimulates GH release via GPCR signaling

• GHRH

Peptide mediator produced in the liver in response to GH

• IGF-1