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
What is somatostatin (or its analogues) used to treat?
Used to treat: acromegaly, gastrinoma, glucagonoma and other endocrine tumors, and esophageal varices bleeding.
26
What are the adverse effects of somatostatin?
1- GI disturb. 2- Postprandial hyperglycemia. 3- Gall stones *, often as a result of decreased biliary flow and gallbladder contraction.
27
What is the clinical use of Thyrotioin-Releasing hormone (TRH)?
It stimulates the release of TSH from the anterior pituitary. It is used in diagnostic testing of thyroid dysfunction.
28
What is the pharmacological drug of TRH called? And how it is given?
Protirelin, given IV.
29
What is the clinical use of corticotropin releasing hormone (CRH)?
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.
30
What does gonadotropin-releasing hormone (GnRH) stimulate?
Stimulates the gonadotroph cell to produce and release LH and FSH.
31
List 3 examples of GnRH agonists ?
1- Gonadorelin. 2- Buserelin, 3- Nafarelin.
32
List the clinical uses of GnRH?
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
Which type of GnRH agonist dosing stimulates ovulation?
GnRH agonists, SC infusion in pulses mimic physiological GnRH, stimulates ovulation.
34
Which type of GnRH agonist dosing inhibits gonadotropin release?
Steady dosing inhibits gonadotropin release by causing down-regulation (desensitization) of GnRH receptors in pituitary cells that normally release gonadotropins.
35
Which type of GnRH agonist dosing diagnosis and treats hypogonadal states?
Pulsatile administration.
36
Which type of GnRH agonist dosing is used in sex hormone-dependent conditions?
Continuous GnRH.
37
What is the physiologic inhibitor of prolactin release?
Dopamine.
38
Why isn’t dopamine useful in the control of hyperprolactinemia?
Because of its peripheral effects and the need for parenteral administration.
39
What is used instead of dopamine in the case of hyperprolactinemia?
Bromocrptine, and other orally active ergot-derivatives (e.g. Cabergoline, Pergoline).
40
Why is Bromocrptine, and other orally active ergot-derivatives (e.g. Cabergoline, Pergoline) preferred?
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
List the 2 adverse effects of PIH?
1- Orthostatic hypotension. 2- Psychiatric manifestations.
42
GH secretion is high in ________, decreasing at ________ to an intermediate level, which is then maintained until _________, when there is further decline.
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
What is Insulin-like growth factor 1 (IGF-1)?
Released from the liver, inhibits GH secretion by stimulating somatostatin secretion from the hypothalamus.
44
List the 4 GH activity?
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
List 4 causes for GH deficiency?
1- Damage to the pituitary or hypothalamus by a tumor. 2- Infection. 3- Surgery. 4- Radiation therapy.
46
What is the signs and symptoms of GH deficiency in children?
Short stature and adiposity and hypoglycemia.
47
What is the signs and symptoms of GH deficiency in adults?
Generalized obesity and reduced muscle mass.
48
What is the cause of growth hormones excess?
Mainly benign pituitary tumor.
49
What does growth hormone excess causes in adults?
Acromegaly.
50
What does growth hormone excess causes in children before the long bone epiphyses closes (children)?
Leads to gigantism.
51
List 4 treatments of excess GH disorders? And give examples?
1- Synthetic somatostatin (Octreotide). 2- DA agonists (Bromocriptine). 3- Surgical removal/Radiotherapy of the tumor. 4- GH antagonists (Pegvisomant).
52
What is the MOA of Octeriotide and Bromocriptine in GH excess?
Low GH level in blood, by inhibiting anterior pituitary hormone secretion.
53
What is the MOA of Pegvisomant?
Doesn’t decrease blood level of GH, only blocks receptors.
54
What are the clinical uses of GH?
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
List 4 adverse effects of somatotropin?
1- Hypothyroidism. 2- Pancreatitis. 3- Gynecomastia. 4- Possibilities of abuse, e.g. creation of “super” sports people.
56
What is the diagnostic use of TSH?
In patients who have been treated surgically for thyroid carcinoma, to test for recurrence.
57
What is the diagnostic use?
As a test of the capacity of the adrenal cortex to produce cortisol.
58
List the 3 preparations available for clinical use of FSH?
1- Urofollitropin: purified from the urine of post-menopausal women. 2- Follitropin alpha: recombinant form. 3- Follitropin beta: recombinant form.
59
What is the FSH used to treat?
Used in combination with other drugs to treat infertility in women and men.
60
List the preparation available for clinical use of LH?
Lutropin alpha.
61
What is lutropin alpha used for?
Approved for use in combination with follitropin alpha from stimulation of follicular development in infertile women with profound LH deficiency.
62
List the preparation available for clinical use of prolactin?
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
What is the function of oxytocin?
1- Effective stimulant of uterine contractions and is used intravenously to induce or reinforce labor. 2- Induces the release of milf (NOT production).
64
What is the clinical uses of oxytocin?
IV and IM. 1- Induction of labor (given in the active phase of labor). 2- Control of postpartum bleeding.
65
List the adverse effects of oxytocin?
1- Fetal distress. 2- Placental abruption or uterine rupture . 3- Excessive fluid retention.
66
Oxytocin is contraindicated in which group of patients?
Not given to women who have heart failure.
67
What will the kidneys do when there is a high level of ADH secretion?
Reabsorb water.
68
What will the kidneys do when there is low levels of ADH secretion?
Release water in dilute urine.
69
What increases ADH release?
Hypotension or when the blood becomes too salty.
70
How does ADH help to elevate blood pressure?
ADH causes peripheral blood vessels constriction to elevate blood pressure.
71
List 2 clinical uses of ADH?
1- Diabetes insipidus. 2- Nocturnal enuresis (by decreasing nocturnal urine production).
72
List 2 adverse effects of ADH?
1- Hyponatremia. 2- Seizures.
73
List 2 examples of synthetic ADH drugs? And how is it given?
1- Vasopresssin: IV, IM. 2- Desmopressin: IV, IM. PO, Intranasal.