Hypothalamic and Pituitary Drugs Flashcards

1
Q

Corticotropin (ACTH) - MoA

A

Increased activity of cholesterol side-chain cleavage enzyme, causing conversion of cholesterol to pregnenolone. This stimulates of adrenal cortex to produce: cortisol, aldosterone, & androgens.

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2
Q

Corticotropin preparations

A

Porcine corticotropin
Cosyntropin
Corticorelin ovine triflutate

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3
Q

Cosyntropin - Classification

A

Synthetic form of human corticotropin

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4
Q

Cosyntropin - Clinical use

A

Diagnose Adrenal insufficiency (pituitary adenoma vs adrenal tumor)

Distunguish Congenital adrenal hyperplasia from ovarrian hyperandrogenism.

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5
Q

Why is cosyntropin used for diagnosing adrenal insufficiancy?

A

It increases cortisol levels in healthy individuals but fails to increase cortisol in persons with adrenal insufficiency

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6
Q

Corticorelin ovine triflutate - Classification and Administration

A

Corticotropin releasing hormone (CRH)

IV administration

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7
Q

Corticorelin ovine triflutate - Clinical use

A

Diagnostic test to determine the cause of excessive levels of cortisol in persons with Cushing syndrome

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8
Q

Growth hormone (Somatotropin) - MoA

A

Direct stimulation of lipolysis and antagonize insulin to elevate blood glucose levels
Indirect stimulation of insulin-like growth factor 1 (IGF-1): skeletal muscle growth, amino acid transport, protein synthesis, nucleic acid synthesis, cell proliferation.

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9
Q

Growth hormone preparations

A

Somatropin

Mecasermin

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10
Q

Somatropin - Classification and Administration

A

Recombinant form of somatotropin (GH)

Subcutaneous

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11
Q

Somatropin - Clinical use

A
GH deficiency in children: 
Idiopathic growth hormone deficiency
Turner syndrome
Chronic renal failure
Prader-Willi syndrome
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12
Q

Somatropin - Contraindications

A

Malignancies, critically ill patients (increase mortality).

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13
Q

Which group of people are less responsive to somatropin?

A

Children who received craniospinal irradiation for treatment of childhood malignancy

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14
Q

Somatropin - Adverse effects

A

None are common

Psuedotumor cerebri
Slipped capital femoral Epiphysis
Progression of scoliosis
Edema
Hyperglycemia. 
Turner: otitis media
Myalgias
Arthralgia
Carpal tunnel syndrome
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15
Q

Mecasermin - Classification

A

Recombinant human IGF-1

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16
Q

Mecasermin - MoA

A

IGF-1 mechanisms: skeletal muscle growth, amino acid transport, protein synthesis, nucleic acid synthesis, cell proliferation.

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17
Q

Mecasermin - Clinical use

A

Growth failure in children with severe IGF-1 deficiency, GH receptor mutation, antibodies to GH

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18
Q

Mecasermin is produced by which bacteria?

A

E. coli

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19
Q

Mecasermin - Adverse effects

A

Hypoglycemia

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20
Q

How can you prevent hypoglycemia with the use of Mecasermin?

A

By eating a meal or snack before or soon after the time of injection

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21
Q

Growth hormone inhibitors

A

Somatostatin
Octreotide
Lanreotide
Cabergoline

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22
Q

Somatostatin - MoA

A

Inhibits GH secretion and insulin secretion from pancreas

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23
Q

Somatostatin - Clinical use

A

Limited use: short duration of action and multiple effects on secretory systems

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24
Q

Octreotide - Classification and Administration

A

Somatostatin analogue

Subcutaneous

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25
Q

Octreotide - MoA

A

Suppresses secretion of:
Growth hormone
IGF-1
Serotonin
GI-peptides (gastrin, motilin, secretin, VIP)
Greater effect on GH than insulin secretion

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26
Q

Octreotide - Clinical use

A

Acromegaly.
Tumors secreting insulin, glucagon, gastrin, thryotropin, and vasoactive intestinal peptide
Carcinoid tumors secreting serotonin and kallikrein

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27
Q

Octreotide - Adverse effects

A

Nausea, vomiting, abdominal cramps, steatorrhea, gallstones

Arrhythmias (brady, disturb conduction).
(Hyper)+ hypoglycemia
Constipation
Flatulence
B12-def in long-term use.
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28
Q

Lanreotide - Classification and Administration

A

Cyclic octapeptide analogue of somatostatin

Deep subcutaneous

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29
Q

Lanreotide - Clinical use

A

Acromegaly

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30
Q

Cabergoline - Classification

A

Selective dopamine 2 agonist

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31
Q

Cabergoline - MoA

A

Reduce GH, IGF-1 and prolactin

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32
Q

Cabergoline - Clinical use

A

Acromegaly
Hyperprolactinemia
Parkinson

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33
Q

Growth hormone receptor antagonist

A

Pegvisomant

34
Q

Pegvisomant - MoA

A

GH receptor antagonist in target tissue, reduces IGF-1 levels in dose-dependent manner

35
Q

Pegvisomant - Clinical use

A

Acromegaly in patients resistant to somatostatin analogs

Improve symptoms of tissue swelling, arthralgia, headache, perspiration, fatigue

36
Q

Pegvisomant - Adverse effects

A

Good safety profile

Elevation of liver enzymes (Should be monitored)

37
Q

Gonadotropins

A
Menotropins
Chorionic gonadotropin
Choriogonadotropin alpha
Follitropin alfa & beta
Urofollitropin
Lutropin alfa
38
Q

Gonadotropins - MoA

A

FSH: ovarian follicle maturation, estrogen production, spermatogenesis

LH: follicle development, induces ovulation, testosterone production

39
Q

Gonadotropins - Clinical use

A

Infertility in men and women

Hypogonadism (men)

40
Q

Gonadotropins - Adverse effects

A

Ovarian hyperstimulation syndrome (acites, hydrothorax, hypovolemia, shock)
Multiple pregnancies
Headache, depression, edema.

41
Q

Menotropins - Classification

A

Human menopausal gonadotropins (LH+FSH)

42
Q

Chorionic gonadotropin - Classification

A

Human chorionic gonadotropin (Placental hCG)

Essentially identical to LH in structure and function

43
Q

Chorionic gonadotropin - Clinical use

A

Cryptorchidism and hypogonadism (puberty): Testosterone production and descending of testes

44
Q

Choriogonadotropin alpha - Classification

A

Recombinant hCG

45
Q

Follitropin alfa and beta - Classification

A

Recombinant FSH

46
Q

Urofollitropin - Classification

A

Highly purified FSH

47
Q

Lutropin alfa - Classification

A

Recombinant LH

48
Q

Lutropin alfa is used in combination with?

A

Follitropin

49
Q

GnRH agonists

A
Histrelin
Goserelin
Leuprolide
Nafarelin
Triptorelin
50
Q

GnRH agonists - MoA

A

Binds to G protein-coupled receptors (GnRH-receptors).
Pulsatile adm: stimulate release of FSH & LH from pituitary.

Continuous adm: Down-regulation of GnRH-receptors & decreased FSH & LH secretion.

51
Q

GnRH agonists - Clinical use

A

Advanced prostate and breast cancer, endometriosis and uterine fibroids

Central precocious puberty

Suppress the premature estrogen-induced LH surge that would otherwise occur during the use of gonadotropins in the treatment of infertility

52
Q

GnRH agonists - Contraindications

A

Pregnancy and breast-feeding

53
Q

GnRH agonists - Adverse effects

A
Symptoms of menopause: 
Hot flashes
Depression
Decreased libido
Vaginal dryness
Generalized pain
Ovarian cysts
Osteoporosis (prolonged treatment)
54
Q

Histrelin - Clinical use

A

Central precocious puberty (12 month subcutaneous implant)

55
Q

Goserelin, Leuprolide - Clinical use and Administration

A

Advance prostate cancer, brest cancer, and endometriosis

Subcutaneous implant

56
Q

Goserelin, Leuprolide - Special considerations

A

Should be given with testosterone antagonist (flutamide or bicalutamide) because of transient increase in testosterone levels when treatment of prostate cancer has begun

57
Q

Nafarelin - Clinical use

A

Endometriosis in women

Central precocius puberty in children

58
Q

GnRH antagonists

A

Ganirelix
Cetrorelix
Degarelix

59
Q

GnRH antagonists - MoA

A

Competitive antagonists at GnRH receptors.

Dose-dependently inhibit the secretion of FSH and LH

60
Q

GnRH antagonists - Contraindications

A

Pregnancy

61
Q

GnRH antagonists - Adverse effects

A
Hypersensitivity
Allergic reactions (anaphylaxis)
62
Q

Ganirelix, Cetrorelix - Clinical use

A

Inhibit LH surges in women undergoing ovarian stimulation as an infertility treatment

63
Q

Degarelix - Clinical use

A

Advanced prostate cancer: inhibitions of gonadotropin secretion and testosterone release

64
Q

Prolactin inhibitors

A

Dopamine agonists:
Cabergoline
Bromocriptine

65
Q

Prolactin inhibitors - Clinical use

A

Symptomatic treatment for hyperprolactinemia:
Galactorrhea, hypogonadism, infertility
Parkinson

66
Q

Which prolactin inhibitor can be used for mixed growth hormone and prolactin-secreting pituitary adenoma?

A

Cabergoline

67
Q

Prolactin inhibitors - Adverse effects

A

Most common:
Nausea
Headache
Dizziness

Psychiatric manifestations
Erythromelalgia

68
Q

Posterior pituitary hormones

A

Oxytocin

Vasopressin

69
Q

Oxytocin - MoA

A

Increased strength of uterine contractions and causes milk ejection by contracting myoepithelial cells that line the ducts of the breast

70
Q

Oxytocin - Clinical use

A

Induce or enhance uterine contractions during labor (IV injection)
Postpartum uterine hemorrhage (IM injection)
Milk let-down (Nasal spray)

71
Q

Oxytocin - Contraindications

A

Fetal distress
Abnormal fetal presentation
Prematurity
Cephalopelvic disproportion

72
Q

Oxytocin - Adverse effects

A

Uncommon

Cardiac arrhythmias
CNS stimulation
Excessive uterine contractions
Hyponatremia

73
Q

Vasopressin analogues

A

Desmopressin
Conivaptan
Tolvaptan

74
Q

Vasopressin - MoA

A

V1 receptors in vascular smooth muscle: vasoconstriction

V2 receptors (renal) activated by production of cAMP: Increased water reabsorption (by insertion of aquaporins).
Expands ECF volume, concentrates urine.
75
Q

Desmopressin - MoA

A

More potent antidiuretic effect than ADH (V2), less vasoconstriction.

Stimulates the release of von Willebrand factor (vWF) and factor VIII in blood vessel walls

76
Q

Desmopressin - Clinical use

A

Diabetes indipidus:
Prevent nocturnal urine production and enuresis.
Nocturnal enuresis in children
Von Willebrand disease
Hemophilia A
Control bleeding caused by esophageal varices or colonic diverticula

77
Q

Desmopressin - Contraindication

A

Coronary artery disease because of vasoconstrictive effects

78
Q

Conivaptan - MoA

A

V1+V2 receptor antagonist

79
Q

Conivaptan - Clinical use

A

Euvolemic and hypovolemic hyponatremia in hospitalized patients

80
Q

Tolvaptan - MoA

A

Selective V2 receptor antagonist

81
Q

Tolvaptan - Clinical use

A

Clinically significant hypervolemic and euvolemic hyponatremia, including patients with heart failure, cirrhosis, and SIADH