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Pharmacology > Repro-Endo: Pituitary / Hypothalamic > Flashcards

Repro-Endo: Pituitary / Hypothalamic Flashcards

1
Q

Leuprolide (Goserelin)

A
  • GnRH agonist
  • GnRH analog w/ longer half-life
  • Pulsatile –> Increase LH / FSH
    • Women w/ Amenorrhea who desire fertility
  • Continuous –> Suppress LH / FSH
    • Prostate cancer
    • Leiomyomas (smooth muscle tumor)
    • Endometriosis
  • SE: Bone pain, Feet / Ankle swelling
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2
Q

Somatotropin

A
  • GH analog
  • Increases Lean muscle mass
  • Tx:
    • Turner syndrome
    • Dwarfism
    • Wasting a/w AIDS or Malignancy
  • SE: Hand / Foot edema, Thickening of Bones/Jaw, Carpel tunnel syndrome, Increased organ growth, Decreased insulin sensitivity, Hyperglycemia
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3
Q

Octreotide

A
  • Somatostatin analog
  • Longer half-life than Somatostatin
  • Hypothalamic hormone that normally inhibits the release of GH, Glucagon, Insulin, Gastrin, and Vasoactive Intestinal Peptide (VIP)
  • Tx: Acromegaly, Gastrinoma, Glucagonoma, Esophageal varices, VIPomas, Carcinode syndrome, Acromegaly, Zollinger-Ellison Syndrome
  • SE: Gallbladder disease, Pancreatitis, Hypo- or Hyer- thyroidism, Cardiac Arrhythmias
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4
Q

Bromocriptine, Cabergoline

A
  • Dopamine receptor agonsits
  • Dopamine inhibits Prolactin secretion from the Hypothalamus
  • Tx: Prolactinomas, Parkinson disease (High dose)
  • SE: Psychotic symptoms, Dizziness, Headache, Nausea, Lightheadedness, Confusion
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5
Q

Desmopressin

A
  • Vasopressin analog (ADH)
  • Minimal V1 activity on Smooth muscle
  • More V2 receptors –> Renal collecting tubules –> Water reabsorption and von Willebrand Factor (vWF) release
  • Tx: Central DI (NOT Nephrogenic), von Willebrand Disease
  • SE: Hyponatremia, Transient headache, flushing
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6
Q

Oxytocin

A
  • Posterior pituitary hormone –> Milk secretion and Uterine contractions during Labor
  • Tx: Induces labor, Decreases postpartum bleeding by inducing contractions, Stimulates breast milk letdown in new mothers
  • SE: Chest pain, Confusion, Excessive vaginal bleeding, Palpitations, Seizures
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7
Q

Rx for Women w/ Amenorrhea who desire fertility?

A

Pulsatile Leuprolide

(GnRH agonist –> LH / FSH)

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8
Q

Rx for Prostate cancer?

A

Continous Leuprolide

(GnRH agonsit)

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9
Q

Rx for Leiomyomas (Smooth Muscle Tumor)?

A

Continuous Leuprolide

(GnRH agonist)

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10
Q

Rx for Endometriosis?

A

Continuous Leuprolide

(GnRH agonist)

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11
Q

Rx for Precocious Puberty?

A

Continuous Leuprolide

(GnRH agonist)

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12
Q

Rx for Dwarfism?

A

Somatotropin

(GH analog)

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13
Q

Rx for Wasting a/w AIDS or Malignancy?

A

Somatotropin

(GH analog)

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14
Q

Rx for Esophageal varices?

A

Octreotide

(Somatostatin analog)

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15
Q

Rx for VIPomas?

A

Octreotide

(Somatostatin analog)

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16
Q

Rx for Carcinoid Syndrome?

A

Octreotide

(Somatostatin analog)

17
Q

Rx for Acromegaly?

A

Octreotide

(Somatostatin analog)

18
Q

Rx for Zollinger-Ellison Syndrome?

A

Octreotide

(Somatostatin analog)

19
Q

Rx for Prolactinomas?

A

Bromocriptine, Cabergoline

(Dopamine receptor agonists)

20
Q

Rx for Parkinson Disease?

A

Bromocriptine, Cabergoline

(Dopamine receptor agonists)

21
Q

Rx for Central Diabetes Insipidus?

A

Desmopressin

(Vasopressin analog: ADH)

22
Q

Rx for von Willebrand Disease?

A

Desmopressin

(Vasopressin analog: ADH)

23
Q

Rx for Inducing labor and Stimulating Breast Milk?

A

Oxytocin

(Posterior Pituitary Hormone)

24
Q

Demeclocycline

A
  • ADH antagonist
  • Member of the Tetracycline family
  • Tx: SIADH
  • SE: Nephrogenic DI, Photosensitivity, Bone and Teeth abnormalities
25
Q

Flutamide

A
  • Prevents the binding of Endogenous Androgens to the Androgen receptor
  • Pure Androgen antagonist w/out Intrinsic steroidal activity
  • 3 x daily
  • 1 week increase in LH and FSH –> Testosterone surge
  • Tx: Metastatic prostate cancer, often combind w/ GnRH agonists
  • Se: Diarrhea, Gynecomastia, Hepatotoxicity (rare)
  • Flutamide, Bicalutamide, Enzalutamide
26
Q

Bicalutamide

A
  • Nonsteroidal antiandrogen
  • More effective at Tx of Prostate cancer than Flutamide
  • Promotes translocation of Androgen receptors to the cell nucleus
  • Tx: Prostate cancer
  • Se: Less Diarrhea or other side effects
27
Q

Enzalutamide

A
  • Non-steroidal antiandrogens
    • Acts as an Antagonist at the Adnrogen Receptor
  • Tx: Metastatic castration-resistant prostate cancer who have previosuly recieved Docetaxel
  • 5x higher affinity than Bicalutamide for Androgen receptor
  • Enzalutamide Does Not promotre translocation of Androgen receptors to the cell nucleus
  • BUT it does penetrate the BBB
28
Q

GnRH Agonists and Antagonists

A
  • GnRH agonists (Leuprolide or Goserelin) and Androgen receptor antagonists (Bicalutamide or Flutamide) work together
  • The initial surge of FSH and LH and resulting elevation of Testosterone is blocked
  • Diethylstilbestrol is used because it inhibits LH and FSH but has Se (gynecomastia, nausea, thromboembolism, vomiting)
  • Abarelix - inhibits LH and FSH and inhibits Testosterone
29
Q

Ketoconazole

A
  • Antifungal drug
  • Effective inhibitor of P450 enzymes involved in Steroid biosynthesis
  • 2nd line agent for Tx of Prostate cancer
30
Q

Abiraterone acetate

A
  • Tx: Metastatic, castration-resistant prostate cancer
  • Inhibits biosynthesis of Androgens (& to a lesser extend, Glucocorticoids) by inhibiting CYP17
  • Combined w/ Prednisone (counter inhibition of Glucocorticoid synthesis)
  • Se: HTN, Hypokalemia, and Fluid retention due to Mineralocorticoid excess
31
Q

Rx for Hirsuitism in Women?

A
  • Spironolactone and Cyproterone Acetate
  • Weak antagonists at androgen receptor
  • Spironolactone is also a weak inhibitor of Testosterone production
32
Q

Rx for Benign Prostatic Hyperplasia (BPH)?

A
  • Finasteride, Dutasteride, PDE5 inhibitors
  • Finasteride Blocks Type II (prostate specific) 5α-reductase and prevents the conversion of Testosterone to DHT
  • Also approved for the Tx of Male Patterend Baldness
  • Dutasteride blocks both Type I and Type II forms of 5α-reductase –> works in all tissues.
  • PDE5 inhibitors - relax smooth muscle in the Urogenital tract and be be used to Tx BPH
33
Q

Sildenafil

A
  • Inhibits Phosphodiesterase 5 (PDE5) that is expressed in the Genital tissue
  • PDE5 causes the hydrolysis of cGMP, Sildenafil causes a large increase in cGMP –> enhanced and prolonged erection
  • Nerves must be initially functional for Sildenafil to work
  • Se: Priapism (long erection), Hypotension
  • Sildenafil may increase the risk of Melanomas
34
Q

Alprostadil

A
  • A Prostaglandine E1 agonist
  • Simulate a PGE1 receptor and cause an increase in cAMP
  • Cyclic AMP also causes a relaxation of Cavernosal Smooth muscle and causes erection w/out functional neurons
  • Must be injected
35
Q

Papavarine

A
  • Non-selective Phosphodiesterase Inhibitor that inhibits that breakdown of both cGMP
  • Injected directly into the Penis
36
Q

Phentolamine

A
  • Nonselective Alpha adrenergic receptor agonsit
  • Prevents NorEpi from causing Constrction of Arterioles supplying blood to the Corpor Cavernosa
  • -> Promotes erection
  • Injected directly into the Penis

Pharmacology (29 decks)

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