Pharma 1: Pharamcology Of The Endocrine System Flashcards

1
Q

List the 3 causes for endocrine disorders? And what is their treatment?

A

1- Hormone deficiency > HRT.
2- Hormone excess > specific antagonists or release inhibitors.
3- Hormone resistance > sensitizers.

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2
Q

List the 3 sources of hormones?

A

1- Natural.
2- Biosynthetic.
3- Synthetic.

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3
Q

List 2 examples of hormones that come from a natural source?

A

1- Human (GH; LH & FSH; hCG).
2- Animal (insulin, T3 & T4).

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4
Q

List an example of hormones that come from a biosynthetic sources?

A

Insulin (pocrine & bovine).

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5
Q

List an example of hormones that come from a synthetic sources?

A

Most hormones and their antagonists (DNA recombinant technology).

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6
Q

What is the function of the pituitary gland?

A

Makes and releases hormones under regulation of the hypothalamus.

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7
Q

List the 6 hormones associated with the anterior pituitary?

A

1- Growth hormone (GH).
2- Thyroid-stimulating hormone (TSH).
3- Adrenocorticotropin (ACTH).
4- Follicle-stimulating hormone (FSH).
5- Leutinizing hormone (LH).
6- Prolactin.

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8
Q

What is the function of the posterior pituitary?

A

Stores and secretes hormones that are made in the hypothalamus.

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9
Q

List the 2 hormones associated with the posterior pituitary?

A

1- Oxytocin.
2- Antidiuretic hormone (ADH).

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10
Q

List 6 examples of hormones made in hypothalamus?

A

1- Growth hormone-releasing hormone (GHRH).
2- Growth hormone- releasing inhibiting hormone (GHRIH) (somatostatin).
3- Thyrotropin - releasing hormone (TRH).
4- Corticotropin - releasing hormone (CRH).
5- Gonadotropin - releasing hormone (GnRH).
6- Dopamine.

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11
Q

What stimulates the release of growth hormone?

A

Growth hormone - releasing hormone (GHRH).

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12
Q

What inhibits the release of growth hormone?

A

Growth hormone - releasing inhibiting hormone (GHRIH) - Somatostatin.

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13
Q

Growth hormone - releasing hormone (GHRH) is released from where? And in what fashion?

A

From the hypothalamus, in a pulsatile fashion, with 5-9 major pulses detected per day.

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14
Q

GHRH release is enhanced by which drugs?

A

Enhanced by an alpha-2-adrenergic agonists (e.g. clonidine) and opioids.

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15
Q

GHRH release is increased by what?

A

Increased by vigorous exercise.

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16
Q

What is the diagnostic use of GHRH?

A

To test pituitary function in patients with GH deficiency.

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17
Q

What is the pharmacological version of GHRH used for diagnostic use called?

A

Sermorelin.

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18
Q

How do we differentiate between GH deficiency because of a hypothalamic defect vs. a pituitary defect?

A

Hypothalamic defect: most common, GHRH will elicit an increase in GH release.
Pituitary defect: no increase in GH following GHRH administration.

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19
Q

What is the therapeutic uses of GHRH?

A

To enhance GH secretion.

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20
Q

How do we use GHRH to enhance GH secretion?

A

Pulsatile subcutaneous delivery of GHRH, mimicking the normal endogenous patterns.
IV, SC, intranasal.

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21
Q

Pulsatile subcutaneous delivery of GHRH is used for which type of GH deficiency?

A

Used to stimulate GH release in patients with GH deficiency that is not of pituitary origin.

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22
Q

What is the MOA of somatostatin (growth hormone-releasing inhibiting hormone (GHRIH))?

A

1- Inhibits GH release and TSH from the ant. pituitary.
2- Inhibits release of most GI hormones, reduces gastric acids and pancreatic secretion. (Glucagon, insulin and gastrin).

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23
Q

Why is somatostatin of no clinical value?

A

Because of its short half life (<3 min).

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24
Q

What do we use instead of somatostatin?

A

Synthetic somatostatin analogues,
1- Octreotide, has a longer duration of action.
2- Lanreotide, is much longer acting, and is administered only twice a month.

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25
Q

What is somatostatin (or its analogues) used to treat?

A

Used to treat: acromegaly, gastrinoma, glucagonoma and other endocrine tumors, and esophageal varices bleeding.

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26
Q

What are the adverse effects of somatostatin?

A

1- GI disturb.
2- Postprandial hyperglycemia.
3- Gall stones *, often as a result of decreased biliary flow and gallbladder contraction.

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27
Q

What is the clinical use of Thyrotioin-Releasing hormone (TRH)?

A

It stimulates the release of TSH from the anterior pituitary.
It is used in diagnostic testing of thyroid dysfunction.

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28
Q

What is the pharmacological drug of TRH called? And how it is given?

A

Protirelin, given IV.

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29
Q

What is the clinical use of corticotropin releasing hormone (CRH)?

A

It stimulates secretion of both ACTH and beta-endorphin (a closely related peptide) from the anterior pituitary.
CRH can be used in the diagnosis of abnormalities of ACTH secretion.

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30
Q

What does gonadotropin-releasing hormone (GnRH) stimulate?

A

Stimulates the gonadotroph cell to produce and release LH and FSH.

31
Q

List 3 examples of GnRH agonists ?

A

1- Gonadorelin.
2- Buserelin,
3- Nafarelin.

32
Q

List the clinical uses of GnRH?

A

1- Stimulates ovulation.
2- Inhibits gonadotropin release.
3- Diagnosis and treatment of hypogonadal states in females and males.
4- Sex hormone-dependent conditions: prostate and breast caners, uterine fibroids, endometriosis, or precocious puberty.

33
Q

Which type of GnRH agonist dosing stimulates ovulation?

A

GnRH agonists, SC infusion in pulses mimic physiological GnRH, stimulates ovulation.

34
Q

Which type of GnRH agonist dosing inhibits gonadotropin release?

A

Steady dosing inhibits gonadotropin release by causing down-regulation (desensitization) of GnRH receptors in pituitary cells that normally release gonadotropins.

35
Q

Which type of GnRH agonist dosing diagnosis and treats hypogonadal states?

A

Pulsatile administration.

36
Q

Which type of GnRH agonist dosing is used in sex hormone-dependent conditions?

A

Continuous GnRH.

37
Q

What is the physiologic inhibitor of prolactin release?

A

Dopamine.

38
Q

Why isn’t dopamine useful in the control of hyperprolactinemia?

A

Because of its peripheral effects and the need for parenteral administration.

39
Q

What is used instead of dopamine in the case of hyperprolactinemia?

A

Bromocrptine, and other orally active ergot-derivatives (e.g. Cabergoline, Pergoline).

40
Q

Why is Bromocrptine, and other orally active ergot-derivatives (e.g. Cabergoline, Pergoline) preferred?

A

They are effective in reducing prolactin secretion from the normal glands as well as from prolactinomas.
They are also used in the treatment of acromegaly.

41
Q

List the 2 adverse effects of PIH?

A

1- Orthostatic hypotension.
2- Psychiatric manifestations.

42
Q

GH secretion is high in ________, decreasing at ________ to an intermediate level, which is then maintained until _________, when there is further decline.

A

GH secretion is high in newborns, decreasing at 4 yr to an intermediate level, which is then maintained until puberty, when there is further decline.

43
Q

What is Insulin-like growth factor 1 (IGF-1)?

A

Released from the liver, inhibits GH secretion by stimulating somatostatin secretion from the hypothalamus.

44
Q

List the 4 GH activity?

A

1- Increases plasma free fatty acids (source of energy for muscle tissue).
2- Increases hepatic glucose output.
3- Decreases insulin sensitivity in muscle.
4- Is a protein anabolic hormone.

45
Q

List 4 causes for GH deficiency?

A

1- Damage to the pituitary or hypothalamus by a tumor.
2- Infection.
3- Surgery.
4- Radiation therapy.

46
Q

What is the signs and symptoms of GH deficiency in children?

A

Short stature and adiposity and hypoglycemia.

47
Q

What is the signs and symptoms of GH deficiency in adults?

A

Generalized obesity and reduced muscle mass.

48
Q

What is the cause of growth hormones excess?

A

Mainly benign pituitary tumor.

49
Q

What does growth hormone excess causes in adults?

A

Acromegaly.

50
Q

What does growth hormone excess causes in children before the long bone epiphyses closes (children)?

A

Leads to gigantism.

51
Q

List 4 treatments of excess GH disorders? And give examples?

A

1- Synthetic somatostatin (Octreotide).
2- DA agonists (Bromocriptine).
3- Surgical removal/Radiotherapy of the tumor.
4- GH antagonists (Pegvisomant).

52
Q

What is the MOA of Octeriotide and Bromocriptine in GH excess?

A

Low GH level in blood, by inhibiting anterior pituitary hormone secretion.

53
Q

What is the MOA of Pegvisomant?

A

Doesn’t decrease blood level of GH, only blocks receptors.

54
Q

What are the clinical uses of GH?

A

1- GH deficiency in children and adults.
2- Children with short stature that is due to factors other than GH deficiency: Idopathic short stature, Turner syndrome, Chronic renal failure.

55
Q

List 4 adverse effects of somatotropin?

A

1- Hypothyroidism.
2- Pancreatitis.
3- Gynecomastia.
4- Possibilities of abuse, e.g. creation of “super” sports people.

56
Q

What is the diagnostic use of TSH?

A

In patients who have been treated surgically for thyroid carcinoma, to test for recurrence.

57
Q

What is the diagnostic use?

A

As a test of the capacity of the adrenal cortex to produce cortisol.

58
Q

List the 3 preparations available for clinical use of FSH?

A

1- Urofollitropin: purified from the urine of post-menopausal women.
2- Follitropin alpha: recombinant form.
3- Follitropin beta: recombinant form.

59
Q

What is the FSH used to treat?

A

Used in combination with other drugs to treat infertility in women and men.

60
Q

List the preparation available for clinical use of LH?

A

Lutropin alpha.

61
Q

What is lutropin alpha used for?

A

Approved for use in combination with follitropin alpha from stimulation of follicular development in infertile women with profound LH deficiency.

62
Q

List the preparation available for clinical use of prolactin?

A

No preparation of prolactin is available for use in prolactin deficient patients.
For patients with symptomatic hyperprolactinemia inhibition of prolactin secretion can be achieved with dopamine agonists.

63
Q

What is the function of oxytocin?

A

1- Effective stimulant of uterine contractions and is used intravenously to induce or reinforce labor.
2- Induces the release of milf (NOT production).

64
Q

What is the clinical uses of oxytocin?

A

IV and IM.
1- Induction of labor (given in the active phase of labor).
2- Control of postpartum bleeding.

65
Q

List the adverse effects of oxytocin?

A

1- Fetal distress.
2- Placental abruption or uterine rupture .
3- Excessive fluid retention.

66
Q

Oxytocin is contraindicated in which group of patients?

A

Not given to women who have heart failure.

67
Q

What will the kidneys do when there is a high level of ADH secretion?

A

Reabsorb water.

68
Q

What will the kidneys do when there is low levels of ADH secretion?

A

Release water in dilute urine.

69
Q

What increases ADH release?

A

Hypotension or when the blood becomes too salty.

70
Q

How does ADH help to elevate blood pressure?

A

ADH causes peripheral blood vessels constriction to elevate blood pressure.

71
Q

List 2 clinical uses of ADH?

A

1- Diabetes insipidus.
2- Nocturnal enuresis (by decreasing nocturnal urine production).

72
Q

List 2 adverse effects of ADH?

A

1- Hyponatremia.
2- Seizures.

73
Q

List 2 examples of synthetic ADH drugs? And how is it given?

A

1- Vasopresssin: IV, IM.
2- Desmopressin: IV, IM. PO, Intranasal.