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Pharmacology Block 9 > Hypothalamic & Pituitary Hormones > Flashcards

Hypothalamic & Pituitary Hormones Flashcards

1
Q

What is somatotropin?

A

A recombinant human growth hormone synthesized in E.Coli

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2
Q

What is the mechanism of action of somatotropin?

A

Binds to the HGHR

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3
Q

What happens once the human growth hormone binds to its receptor?

A

There is dimerization of GHR, activation of the GHR- associated JAK2 tyrosine kinase, and tyrosyl phosphorylation of both JAK and GHR

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4
Q

Growth hormone induces changes in

A

Enzymatic activity, transport function, gene expression that ultimately culminate in changes in growth and metabolism

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5
Q

What are some malignancies associated with somatotropin?

A

Leukemia, histiocytosis X, osteogenic sarcoma

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6
Q

What are some CNS tumors associated with somatotropin?

A

Craniopharyngioma, gliobastoma/glioma, astrocytoma

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7
Q

Somatotropin leads to diabetes mellitus type 1 and 2 after how long?

A

1 year of treatment

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8
Q

Intracranial hypertension can result from the use of somatotropin after how long?

A

6 months to 2 years after start of treatment

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9
Q

What other adverse effects are associated with somatotropin?

A

Slipped capital femoral epiphysis, scoliosis, pancreatitis

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10
Q

What is mecasermin?

A

Recombinant DNA engineering human insulin-like growth factor-1

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11
Q

IGF-1 consists of how many amino acids?

A

70 in a single chain with 3 intramolecular disulfide bridges and a molecular weight of 7649 daltons

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12
Q

Mecasermin is indicated for whom?

A

The long term treatment of growth failure in pediatric patients with primary IGFD or with GH gene deletion who have developed neutralizing antibodies to GH

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13
Q

What is the mechanism of action of mecasermin?

A

Binds to the type 1 IGF-1 receptor

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14
Q

The type 1 IGF-1 receptor exerts signaling activity in a number of processes that involve what?

A

Statural growth, mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates and increases in organ growth

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15
Q

What are some adverse effects of mecasermin?

A

Hypoglycemia, acromegaly

Affects fetal development at higher doses

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16
Q

What is octreotide?

A

Long acting octapeptide with pharmacologic properties mimicking those of natural hormone somatostatin

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17
Q

Octreotide is indicated for what?

A

Treatment of acromegaly, reduction of side effects from cancer chemotherapy, gastrointestinal fistulas

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18
Q

What is the mechanism of action of octreotide?

A

Binds to somatostatin receptors

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19
Q

The somatostatin receptors are coupled with pertussis toxin sensitive G proteins which lead to inhibition of?

A

Adenylyl cyclase

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20
Q

Octreotide binding to the somatostatin receptors stimulates phosphotyrosine phosphatase and activation of what?

A

Na(+) /H(+) exchanger via pertussis toxin insensitive G proteins

21
Q

What are some adverse effects of octreotide?

A

Nausea, abdominal cramps, diarrhea, flatulence, fat malabsorption, biliary sludge, gallstones

22
Q

What is oxytocin?

A

Synthetic 9 residue cyclic peptide

23
Q

Oxytocin cannot be used for?

A

Elective induction of labor there must be clear medical requirment

24
Q

How does oxytocin promote uterine contractions?

A

By increasing intracellular Ca2+ which in turn activates myosin’s light chain kinase

25
Q

Oxytocin receptor concentration increases greatly in

A

Pregnancy reaching a maximum in early labor at term

26
Q

What are the targets of oxytocin?

A

Oxytocin receptor agonist

Oxytocin-neurophysin 1 binder

27
Q

Oxytocin can produce a severe what?

A

Water intoxication due to its antidiuretic effect

28
Q

High doses or hypersensitivity to oxytocin may cause what?

A

Uterine hypertonicity, spasm, tetanic contraction, or rupture of the uterus

29
Q

Atosiban is a…

A

Inhibitor of the hormones oxytocin and vasopressin

30
Q

Atosiban is used to?

A

Used intravenously to halt premature labor

31
Q

what is the mechanism of action of atosiban?

A

Synthetic peptide oxytocin antagonist

32
Q

Atosiban binds to membrane bound oxytocin receptors on the myometrium and prevents what?

A

Oxytocin stimulated increases in inositol triphosphate production

33
Q

Vasopressin and desmopressin are indicated for?

A

The treatment of enuresis, polyuria, diabetes insipidus, polydipsia and esophageal varices with bleeding

34
Q

what is the mechanism of action of vasopressin and desmopressin?

A

Acts on three different receptors V1a (vasopressin) , vasopressin receptor V1b, and vasopressin receptor V2

35
Q

What does vasopressin receptor V1a do?

A

Initiates vasoconstriction, liver gluconeogenesis, platelet aggregation, release of factor VIII

36
Q

What does vasopressin receptor V1b do?

A

Mediates corticothrophin secretion from the pituitary

37
Q

What does vasopressin receptor V2 do?

A

Controls free water reabsorption in the renal medulla

38
Q

What is conivaptan?

A

A non peptide inhibitor of antidiuretic hormone (vasopressin)

39
Q

What is conivaptan used for?

A

The treatment of euvolemic or hypervolemic hyponatremia. Or in the setting of hypothyroidism, adrenal insufficiency, pulmonary disorders in hospitalized patients

40
Q

What is the mechanism of action of conivaptan?

A

Dual AVP antagonist with nanomolar affinity for human arginine vasopressin V1A and V2 receptors in vitro. This antagonism occurs in the renal collecting ducts resulting in aquaresis or excretion of free water

41
Q

What is melatonin?

A

A biogenic amine that is found in animals, plants and microbes

42
Q

The secretion of melatonin increases and decreases when?

A

Increases during the night and decreases during the day

43
Q

Melatonin regulates the what by chemically causing drowsiness and lowering body temperature

A

Sleep-wake cycle

44
Q

Melatonin is also implicated in the regulation of what?

A

Mood, learning, memory, immune activity, dreaming, fertility and reproduction

45
Q

Melatonin is also an effective what?

A

Antioxidant

46
Q

Melatonin is also indicated for what conditions?

A

Benzodiazapine and nicotine withdrawl

47
Q

The melatonin receptors are

A

G protein coupled receptors

48
Q

When it comes to children, melatonin levels are inversely related to

A

Gonadal development

49
Q

When it comes to pregnancy, high doses of melatonin administered orally or parenterally may inhibit what

A

Ovulation

Pharmacology Block 9 (7 decks)

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