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Pharma S1Y2 > GH antagonist and agonists > Flashcards

GH antagonist and agonists Flashcards

1
Q

which gland releases GH?

A

anterior pituitary

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2
Q

which hormones released by hypothalamus control GH?

A

growth hormone releasing hormone GHRH

GH inhibiting releasing hormone GHIH

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3
Q

what is the other regulatory effect of somatostatin?

A

somatostatin which is GHIH :

inhibit GH

ALSO INHIBIT TSH

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4
Q

what would do the effect of inhibiting TSH result in terms pharmacodynamics?

A

it will lead to hypothyrodism due to TSH suppression

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5
Q

how is GH administered ?

A

Always as injection cannot be given orally

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6
Q

What is recombinant somatotropin ? rhGH?

A

biosynthetic form of human growth hormone

given to patients with GH deficiency

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7
Q

in cause of dwarfism, how often is somatotropin administered ?

A

subcutaneously ONCE DAILY

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8
Q

what are examples of somatostatin administered ?

A

Somapacitan

Lonapegsomatropin

Somatrogon

all given once weekly and long acting

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9
Q

describe somapacitan?

A

Long acting rhGH analog

given to children 2.5 years old and OLDER

CANT BE GIVEN FOR KIDS YOUNGER THAN 2.5 YEARS OLD

GIVEN ONCE WEEKLY

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10
Q

describe lonapegsomatropin ?

A

sustained release preparation of rhGH

given to children 1 year of age and older

cant be given to children less than 1 years old

prodrug of somatropin

once weekly

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11
Q

describe somatrogon ?

A

long acting rhGH analong

once weekly

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12
Q

what is mecasermin ?

A

recombinant form of human IGF1

only drug in the market has similar to IGF1

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13
Q

when is mecaserin used?

A

severe primary igf-1 deficiency

hormone receptor mutation

patients with neutralizing antibodies

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14
Q

what is the side effect of mecaserin?

A

IGF 1 has insulin like effects

it can induce HYPOGLYCEMIA so must be initiated at lower doses

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15
Q

what is sermorelin ?

A

synthetic growth hormone releasing hormone ( GHRH )

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16
Q

what are the uses of sermorelin?

A

idiopathic GH deficiency in children

GH deficiency secondary to Hypothalamus damage rather than pituitary abnormalities

( IN THIS CASE PITUITARY SOMATOTROPES CAPABLE OF SECRETING GH AND ARE FUNCTIONING )

17
Q

how and when sermorelin is administered?

A

subcutaneous injection

DAILY

18
Q

what is the effect of glucocorticoid on GH?

A

inhibit the effects of recombinant GH

so when patient is taking both long term glucocorticoids and rhGH ——> the glucocorticoid will inhibit the growth effect of GH —->GROWTH FAILURE

19
Q

what would compromise the final height of a patient ?

A

androgens , estrogens and thyroid hormones + anabolic steroids

these would accelerate epiphyseal closure of bones –> stopping the lengthening of the bones

20
Q

what is the example of GHIH?

A

somatostatin like drugs –> END WITH EOTIDE

octreotide –> synthetic somatostatin

Lanreotide aceate –> prolonged secretion

pasireotide –> higher affinity

21
Q

what are the uses of octreotide ?

A

acromegaly –> excessive GH

neoplastic diseases:

carcinoid syndrome

pituitary adenomas that secrete thyrotropin

tumors that produce vasoactive intestinal polypeptide

22
Q

how and when octreotide is administered ?

A

subcutaneously every 8 hours

long acting intramuscular formula given once monthly

oral formulation

23
Q

how is octreotide administered orally even though it is peptidal?

A

it is formulated with transient permeability enhancer which allows it to be absorbed easily

24
Q

what is lanreotide acetate?

A

prolonged release formulation of octreotide

given subcutaneous injection once every 4 weeks

25
Q

what is pasireotide?

A

somatostatin analog that has broader affinity for somatostatin receptors than octreotide and lanreotide

this high affinity results in greater GH inhibition

26
Q

when is pasireotide used?

A

ocrtoetide / lanreotide resistant adenomas

27
Q

what are the pharmacokinetics/dynamics of Somatostatin analogs?

A

Transient GI disturbances are common but usually subside within the first 3 months of therapy

Inhibit gallbladder contractility and decrease bile secretion —> lead to development of biliary sludge and asymptomatic gallstones —> Cholelithiasis

Cholelithiasis —> occur in patients treated for 12 month or longer ( it is only time related not age or gender related )

alter balance of hormones –> hypoglycemia / hyperglycemia

GHIH May suppress pituitary release of TSH because GHIH inhibit both GH and TSH leading to decreased thyroid hormone secretion –> hypothyroidism –> Commonly with octreotide

Sinus bradycardia, conduction abnormalities and arrhythmias —>commonly with octreotide and lanreotide

28
Q

what is administered with somatostatins to reduce the adverse effects?

A

insulin

oral hypoglycemia agents

beta blocker

calcium channel blockers

require careful dosage adjustment

29
Q

what is cabergoline?

A

dopamine agonists

another example is bromocriptine

30
Q

what can dopamine agonists do GH?

A

reduce circulating levels of GH , IGF1, Prolactin

31
Q

when are dopamine agonists can be used?

A

treatment of person with elevated growth hormone and prolactin secretion

32
Q

what you should monitor when administering dopamine agonists?

A

visual disturbances, menstrual cycles ( cuz prolactin inhibit it ), sexual function ( men )

prolactin serum concentration every 3 to 4 weeks

33
Q

what is pegvisomant?

A

GH receptor antagonist

34
Q

what is the MOA of pegvisomant?

A

blocks the receptor and stops IGF1 and from binding to the receptor

35
Q

when is pegvisomant used?

A

acromegaly patients with Resistance to octreotide like pasireotide

36
Q

what are the non pharmacolgical treatments of acromegaly?

A
  • transsphenoidal surgical resection of adenoma
  • radiation therapy

Pharma S1Y2 (10 decks)

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