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Pharmacology > Hypothalamic and Pituitary Drugs > Flashcards

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
Octreotide - MoA
Suppresses secretion of: Growth hormone IGF-1 Serotonin GI-peptides (gastrin, motilin, secretin, VIP) Greater effect on GH than insulin secretion
26
Octreotide - Clinical use
Acromegaly. Tumors secreting insulin, glucagon, gastrin, thryotropin, and vasoactive intestinal peptide Carcinoid tumors secreting serotonin and kallikrein
27
Octreotide - Adverse effects
Nausea, vomiting, abdominal cramps, steatorrhea, gallstones ``` Arrhythmias (brady, disturb conduction). (Hyper)+ hypoglycemia Constipation Flatulence B12-def in long-term use. ```
28
Lanreotide - Classification and Administration
Cyclic octapeptide analogue of somatostatin Deep subcutaneous
29
Lanreotide - Clinical use
Acromegaly
30
Cabergoline - Classification
Selective dopamine 2 agonist
31
Cabergoline - MoA
Reduce GH, IGF-1 and prolactin
32
Cabergoline - Clinical use
Acromegaly Hyperprolactinemia Parkinson
33
Growth hormone receptor antagonist
Pegvisomant
34
Pegvisomant - MoA
GH receptor antagonist in target tissue, reduces IGF-1 levels in dose-dependent manner
35
Pegvisomant - Clinical use
Acromegaly in patients resistant to somatostatin analogs Improve symptoms of tissue swelling, arthralgia, headache, perspiration, fatigue
36
Pegvisomant - Adverse effects
Good safety profile Elevation of liver enzymes (Should be monitored)
37
Gonadotropins
``` Menotropins Chorionic gonadotropin Choriogonadotropin alpha Follitropin alfa & beta Urofollitropin Lutropin alfa ```
38
Gonadotropins - MoA
FSH: ovarian follicle maturation, estrogen production, spermatogenesis LH: follicle development, induces ovulation, testosterone production
39
Gonadotropins - Clinical use
Infertility in men and women | Hypogonadism (men)
40
Gonadotropins - Adverse effects
Ovarian hyperstimulation syndrome (acites, hydrothorax, hypovolemia, shock) Multiple pregnancies Headache, depression, edema.
41
Menotropins - Classification
Human menopausal gonadotropins (LH+FSH)
42
Chorionic gonadotropin - Classification
Human chorionic gonadotropin (Placental hCG) Essentially identical to LH in structure and function
43
Chorionic gonadotropin - Clinical use
Cryptorchidism and hypogonadism (puberty): Testosterone production and descending of testes
44
Choriogonadotropin alpha - Classification
Recombinant hCG
45
Follitropin alfa and beta - Classification
Recombinant FSH
46
Urofollitropin - Classification
Highly purified FSH
47
Lutropin alfa - Classification
Recombinant LH
48
Lutropin alfa is used in combination with?
Follitropin
49
GnRH agonists
``` Histrelin Goserelin Leuprolide Nafarelin Triptorelin ```
50
GnRH agonists - MoA
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
GnRH agonists - Clinical use
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
GnRH agonists - Contraindications
Pregnancy and breast-feeding
53
GnRH agonists - Adverse effects
``` Symptoms of menopause: Hot flashes Depression Decreased libido Vaginal dryness Generalized pain Ovarian cysts Osteoporosis (prolonged treatment) ```
54
Histrelin - Clinical use
Central precocious puberty (12 month subcutaneous implant)
55
Goserelin, Leuprolide - Clinical use and Administration
Advance prostate cancer, brest cancer, and endometriosis Subcutaneous implant
56
Goserelin, Leuprolide - Special considerations
Should be given with testosterone antagonist (flutamide or bicalutamide) because of transient increase in testosterone levels when treatment of prostate cancer has begun
57
Nafarelin - Clinical use
Endometriosis in women | Central precocius puberty in children
58
GnRH antagonists
Ganirelix Cetrorelix Degarelix
59
GnRH antagonists - MoA
Competitive antagonists at GnRH receptors. | Dose-dependently inhibit the secretion of FSH and LH
60
GnRH antagonists - Contraindications
Pregnancy
61
GnRH antagonists - Adverse effects
``` Hypersensitivity Allergic reactions (anaphylaxis) ```
62
Ganirelix, Cetrorelix - Clinical use
Inhibit LH surges in women undergoing ovarian stimulation as an infertility treatment
63
Degarelix - Clinical use
Advanced prostate cancer: inhibitions of gonadotropin secretion and testosterone release
64
Prolactin inhibitors
Dopamine agonists: Cabergoline Bromocriptine
65
Prolactin inhibitors - Clinical use
Symptomatic treatment for hyperprolactinemia: Galactorrhea, hypogonadism, infertility Parkinson
66
Which prolactin inhibitor can be used for mixed growth hormone and prolactin-secreting pituitary adenoma?
Cabergoline
67
Prolactin inhibitors - Adverse effects
Most common: Nausea Headache Dizziness Psychiatric manifestations Erythromelalgia
68
Posterior pituitary hormones
Oxytocin | Vasopressin
69
Oxytocin - MoA
Increased strength of uterine contractions and causes milk ejection by contracting myoepithelial cells that line the ducts of the breast
70
Oxytocin - Clinical use
Induce or enhance uterine contractions during labor (IV injection) Postpartum uterine hemorrhage (IM injection) Milk let-down (Nasal spray)
71
Oxytocin - Contraindications
Fetal distress Abnormal fetal presentation Prematurity Cephalopelvic disproportion
72
Oxytocin - Adverse effects
Uncommon Cardiac arrhythmias CNS stimulation Excessive uterine contractions Hyponatremia
73
Vasopressin analogues
Desmopressin Conivaptan Tolvaptan
74
Vasopressin - MoA
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
Desmopressin - MoA
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
Desmopressin - Clinical use
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
Desmopressin - Contraindication
Coronary artery disease because of vasoconstrictive effects
78
Conivaptan - MoA
V1+V2 receptor antagonist
79
Conivaptan - Clinical use
Euvolemic and hypovolemic hyponatremia in hospitalized patients
80
Tolvaptan - MoA
Selective V2 receptor antagonist
81
Tolvaptan - Clinical use
Clinically significant hypervolemic and euvolemic hyponatremia, including patients with heart failure, cirrhosis, and SIADH

Pharmacology (55 decks)

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