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OMS II - Becom Exam 4 > Santos's Lectures > Flashcards

Santos's Lectures Flashcards

1
Q

Anterior Pituitary (adenohypophysis)

A

-INDIRECT connection w/ hypothalamus

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2
Q

Posterior Pituitary (neurohyphysis)

A

-DIRECT connection w/ hypothalamus

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3
Q

which 2 hypothalamic factors do NOT have any inhibitory factors?

A

-CRH and GnRH

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4
Q 
Growth Hormone (GH) 
-aka somatotropin
A
  • effects mediated through IGF-1 and IRS-1
  • measure IGF-1 levels to look at GH levels***

-used for BONE and muscle growth, decrease fat
-pulsatile secretion at night
-

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5
Q

what is an inhibitor of GH used for acromegaly and gigantism?

A

-somatostatin and dopamine

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6
Q

what are the 2 somatostatin analogs?

A

-Octreotide and Lanreotide

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7
Q

Pegvisomat

A

-GH receptor antagonist -> blocks receptor activation but not secretion

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8
Q

what condition is associated w/ failed IGF-1 release?

A

Laron Dwarfism

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9
Q

GH vs IGF-1

A
  • GH -> REDUCES insulin sensitivity -> diabetes

- IGF-1 -> insulin-like effects -> GLUT4 transporters

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10
Q

Somatropin

A
  • rhGH
  • targets GH receptor
  • used for Noonan, prader-willi, turner syndromes
  • used w/ wasting syndromes in HIV ptxs or short bowel syndrome
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11
Q

Mecasermine

A
  • IGF-1 analog -> IGF-1 production at GH receptor sites

- AE -> HYPOGLYCEMIA

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12
Q

Prolactin

A
  • blocked by DOPAMINE -> binds to D2 receptors on lactrotrophs
  • TRH and VIP stimulate release
  • lactation in mammary gland -> growth of ducts/lobules
  • NOT under feedback control of peripheral hormones
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13
Q

Bromocriptine

-also pergolide, cabergoline, quinagolide

A
  • dopamine receptor agonists -> blocks HYPERPROLACTINEMIA
  • bind to D2 receptors on lactotrophs

-also used for Parkinson’s disease

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14
Q

GnRH aka Gonadorelin

A

-release of LH, FSH
-used for hypogonadotropic hypogonadism
-used for INFERTILITY
-

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15
Q

function of LH

A
  • target theca cells -> androstenedione

- target leydig cells -> testosterone

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16
Q

function of FSH

A
  • target granulosa cells -> growth of follicle and activate aromatase
  • target Sertoli cells -> sperm maturation
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17
Q

what enzyme converts androgens to estrogen?

A

aromatase

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18
Q

intermittent (pulsatile) vs. continuous secretion of GnRH

A
  • pulsatile GnRH release -> increase LH, FSH

- continuous GnRH release -> inhibit LH, FSH

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19
Q

analogs of GnRH

A
  • Leuprolide
  • GnRH
  • Goserelin
  • Nafarelin
  • Triptorelin

-NOT used if pregnant

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20
Q

antagonists of GnRH

A
  • Ganarelix
  • Cetrorelix
  • Abarelix
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21
Q

hCG

A
  • made in placenta
  • mimics LH -> acts on LH receptor
  • diagnosis of PREGNANCY**
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22
Q

ACTH

A

-made from POMC** -> produces cortisol in adrenal cortex

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23
Q

Cosytropin

A

-synthetic form of ACTH

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24
Q

TRH

A
  • produce T3 (more acitve) and T4 (high levels, long lasting)
  • treat hypothyroidism
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25
Q

what enzyme converts T4 to T3?

A

-iodothyronin 5’-Deiodinase

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26
Q

stages of disease**

A
  • primary -> LOCAL effects at target organs
  • secondary -> PITUITARY related
  • tertiary -> HYPOTHALAMUS related
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27
Q

where are the hormones in the posterior pituitary synthesized?

A

supraoptic and paraventricular nucleus of HYPOTHALAMUS

-stored in post. pituitary

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28
Q

only 2 hormones of posterior pituitary

A

oxytocin and ADH (vasopressin)

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29
Q

Vasopressin (ADH)

A
  • regulated plasma VOLUME and OSMOLALITY

- osmoreceptors in post. pituitary and hypothalamus

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30
Q

Desmopressin (DDAVP)

A
  • ADH analog

- treatment of NEUROGENIC diabetes insipidus

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31
Q

2 types of ADH receptors

A

V1 -> at arterioles for vasoconstriction; GpPCR

V2 -> at CD for H2O reabsorption; GsPCR; up regulate aquaporins

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32
Q

extra renal V2 receptors

A

release of factor 8 and vWF -> hyper coagulation

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33
Q

SIADH

A
  • caused by small cell lung cancer

- treat w/ hypertonic saline or ADH antagonist

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34
Q

Diabetes Insipidus

A

Neurogenic -> no ADH secretion
Nephrogenic -> decrease response to ADH

LITHIUM can be cause

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35
Q

Conivaptan

A
  • inhibit V1, V2 receptors
  • for euvolemic and hypervolemic hyponatremia
  • treat SIADH
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36
Q

Oxytocin

A
  • for uterine contraction and milk ejection
  • SMALL dose -> increase frequency and force of contraction
  • LARGE dose -> sustained contraction
  • LOVE HORMONE (chemical messenger)

-diagnosis: oxytocin challenge test

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37
Q

what happens with a really high [] of oxytocin?

A

+ ADH receptors

-antidiuretic and pressor activity

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38
Q

CYP17 (17alpha-hydroxylase)

A

enzyme used to form testosterone

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39
Q

steroid hormone binding globulin (SHBG)

A

-binds testosterone and estradiol for circulation

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40
Q

aromatase (aka CYP19)

A

testosterone -> estradiol

  • aromataziation of the A ring
  • A ring binds to ER-a and ER-b
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41
Q

5alpha-reductase

A

testosterone -> DHT

-Finasteride inhibits

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42
Q

how do you treat androgen deficiency?

A 
Testosterone Ester (IM)
-lasts longer and bypasses 1st pass metabolism
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43
Q

AR mutation associated w/ androgen deficiency?

A

Kennedy disease

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44
Q

androgens that are alkylated at 17 alpha position

A
  • ORAL
  • HEPATOTOXIC
  • slower metabolism
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45
Q

reasons for using androgens

A
  1. male hypogonadism
  2. athletic performance (DHEA, androstenedione)
  3. gynecologic disorders
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46
Q

androgen side effects

A
  • MASCULINIZATION
  • men: gynecomastia, azoospermia/small testicles w/ large doses
  • women: hirsutim, amenorrhea
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47
Q

use of anti androgens

A

-excess testosterone -> prostatic carcinoma and hirsutism

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48
Q

Testosterone Enanthate

A
  • ester

- synthetic androgen -> binds to AR

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49
Q

Methyltestosterone and Fluoxymesterone

A
  • alkylated
  • binds to AR
  • ORAL and HEPATOTOXIC
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50
Q

Flutamide

A
  • ANTIANDROGEN
  • inhibits androgen binding to AR
  • for prostate cancer
  • HEPATOTOXIC
  • Monitor INR if used w/ WARFARIN
51
Q

what is the most potent estrogen?

A

17-beta estradiol > estrone and estriol

52
Q

regulation of estrogen

A
  • GnRH from hypothalamus

- LH, FSH from ant. pituitary

53
Q

primary uses for estrogen

A
  • primary hypogonadism

- post-menopause

54
Q

one of the main reasons estrogen is contraindicated?

A

thromboembolic disorders or liver disease

55
Q

Tamoxifen and Toremifene

A
  • SERM

- treat BREAST cancer

56
Q

Raloxifene

A
  • SERM

- treat OSTEOPOROSIS

57
Q

Clomiphene

A
  • SERM

- treat INFERTILITY

58
Q

Fulvestrant

A
  • estrogen ANTAGONIST

- treat BREAST cancer

59
Q

Exemastane and Formestane

A
  • aromatase inhibitors
  • STEROIDAL
  • type I-IRREVERSIBLE AI
60
Q

Anastrozole and Letrozole

A
  • aromatase inhibitors
  • NON-STEROIDAL
  • type II-REVERSIBLE AI
61
Q

Progestins (progesterone)

A
  • PR-A, PR-B receptors
  • produced during LUTEAL phase -> decrease GnRH pulses -> reset HP axis
  • decrease sperm penetration
  • reduces aldosterone effects
62
Q

Mifepristone

A
  • antagonist of progresterone and glucocorticoid receptors
  • terminate early pregnancy

-also effective post-coital

63
Q

Ulipristal

A
  • selective progesterone receptor modulator -> partial agonist to PRs
  • EMERGENCY CONTRACEPTIVE
64
Q

most common form of contraception

A
  • MONOPHASIC (constant dose of both estrogen and progestin)
  • fewer side effects

-estrogen + progestin -> suppress ovulation

65
Q

what disorder is associated with methylation of the oxytocin receptor gene?

A

autism

66
Q

MOA of oxytocin muscle contraction

A

+ PLCbeta-IP3-Ca2+ path -> + Ca2+ channels -> calmodulin -> + MLCK -> phosphorylate myosin -> contraction

more uterine contractions by stimulating prostaglandins and leukotrienes

67
Q

Dinoprostone (PGF2alpha)

A

-oxytocic

68
Q

Misoprostol (PGE1)

A

-oxytocic

  • for cervical ripening and early pregnancy termination
  • AE -> MISCARRIAGE, UTERINE RUPTURE**
  • black box: can cause birth defects, abortion, premature birth, uterine rupture in pregnancy women**
69
Q

Terbutaline

A

-tocolytic

  • Adrenergic agonist (B2 selective) -> inactive MLCK
  • OFF LABEL
70
Q

Ritodine

A

B2 agonist

-only tocolytic to gain FDA approval

71
Q

Nifedipine

A
  • tocolytic

- Ca2+ channel blocker -> inhibit Ca2+ influx

72
Q

Atosiban

A
  • tocolytic

- oxytocin receptor antagonist

73
Q

Iodide

A
  • charged, inorganic
  • LOW levels -> T4 synthesis
  • HIGH levels -> inhibit T4 synthesis/release
74
Q

TPO

A
  1. takes iodide -> iodine
  2. organification -> DIT, MIT
  3. coupling -> T3, T4
75
Q

ratio of T4 to T3

A

5: 1
- more T4 in circulation
- T3 is active and potent

76
Q

5’ Deiodinase

A

converts T4 -> T3 in peripheral tissues

77
Q

what 2 domains does T3 bind to in the nucleus?

A
  • TR-DBD -> + TRE
  • TR-LBD -> binding of T3

-bind domains -> expression at TRE

78
Q

does T3 or T4 bind to the nuclear receptors?

A

T3***

79
Q

thyroid hormone effects on SNS

A

-SNS overactivity -> increase # of adrenergic beta receptors and amplifies signaling

80
Q

Levothyroxine (T4)

A
  • for hypothyroidism
  • thyroid replacement and suppression therapy

-Tirosint less affected by gastric pH or coffee

81
Q

Liothyronine (T3)

A
  • NOT replacement therapy

- for short term TSH suppression

82
Q

how should T4 be administered?

A

on EMPTY stomach -> food interferes w/ absorption

83
Q

Methimazole

A

-treat hyperthyroidism

  • 10x more potent than PTU
  • 2nd-3rd trimester pregnancy
  • NO liver damage, unlike PTU
84
Q

Propylthiouracil (PTU)

A

-treat hyperthyroidism

  • 1st trimester pregnancy
  • AE -> HEPATITIS**
85
Q

Radioactive iodine (RAI)

A

-treat hyperthyroidism

  • 131 I***
  • contraindicated in PREGNANCY
  • if ptx has heart disease -> treat with methimazole
86
Q

other adjunct therapy for hyperthyroidism

A
  1. B-blocker -> propanolol, metoprolol
  2. diltiazem
  3. barbiturates
  4. bile acid sequestrates (chelestyramine)
87
Q

enzymes that make aldosterone

A

CYP11B2

88
Q

enzymes that make cortisol

A

CYP11B1 and CYP17

89
Q

enzymes that make androgens

A

CYP17

90
Q

cortisol binding globulin (CBG)

A 
transports corticoids (aldosterone and cortisol) 
-higher affinity for cortisol
91
Q

rate limiting enzyme in steroidogenesis

A

CYP11A1** (cholesterol side chain cleavage)

92
Q

Ketoconazole

A
  • inhibit CYP11A1 and CYP17,20 lyase

- used for hypercortisolism

93
Q

Trilostane

A

-inhibit 3B-OHSD

94
Q

Metyrapone

A

-inhibit 11B-hydroxylase -> sift to androgen path

95
Q

main effects of cortisol

A
  • LIBERATE ENERGY for heart and brain
  • adapt to stress/starvation
    • osteoclast
  • Na+ retention
  • lung maturation
  • initiate lactation
  • inhibit PLA2*** -> no conversion to AA, prostaglandins, leukotrienes
96
Q

Cushingoid Syndrome

A

-BUFFALO hump, MOON facies, OSTEOPOROSIS, HTN

97
Q

Glucocorticoid deficiency

A

Hyperpigmentation (no cortisol -> excess ACTH)

98
Q

the 2 long acting glucocorticoids - anti-inflammatory action

A
  1. Betamethasone (active 25-40hr.)

2. Dexamethasone (active 30 hr.)

99
Q

Glucocorticoid w/ mineralcorticoid properties***

A

FLUDROCORTISONE***

  • Salt-retention
  • mineralcorticoid replacement
100
Q

causes of Addison’s disease

A

AUTOIMMUNE or TB**

101
Q

Cosytropin

A
  • synthetic ACTH

- diagnostic b/w primary and secondary adrenal insufficiency

102
Q

Hydrocortisone

A
  • synthetic form of cortisol
  • 2/3 dose in morning, 1/3 dose in evening
  • treat 1ry and 2ry adrenal insufficiency
103
Q

Betamethasone, hydrocortisone, beclomethasone, dexamethasone, Triamcinolone

A

TOPICAL anti-inflammatory

  • Fluorinated -> better skin penetration***
  • SKIN-LIGHTENING cosmetics
104
Q

drug used to treat Cushing disease

A

Dexamethasone

105
Q

drug used for integrity of HPA axis

A

Metopirone

106
Q

drugs used for adrenal insufficiency and ectopic ACTH production

A

Cosyntropin

107
Q

primary hyperaldosteronism (Conn’s syndrome)

A

adrenal tumor

108
Q

secondary hyperaldosteronism

A

activation of RAS

109
Q

Deoxycorticosterone (DOC)

A
  • precursor to aldosterone

- secretion under control of ACTH

110
Q

Cabergoline

A
  • D2 receptor agonist -> decrease ACTH, PRL secretion

- treat ACTH & PRL over secretion

111
Q

Corticorelin

A
  • synthetic CRH

- diagnostic to distinguish b/w Cushing from ectopic ACTH

112
Q

Etomidate

A

inhibits CYP11B1

  • anesthetic
  • decrease cortisol production at sub-anesthetic doses
113
Q

Mitotane

A

-inhibits CYP11A1 -> treat adrenocortical carcinoma

114
Q

Mifepristone

A
  • GR antagonist

- treat hypercortisolism and anti-progesterone effect to terminate pregnancy

115
Q

the 2 mineralcorticoid antagonists

A
  1. Spironolactone**
    - K+ sparing diuretic
    - treat primary aldosteronism
    - also androgen antagonist -> treat hirsutism and acne
  2. Eplerenone
    - treat HTN, HF
    - more selective
116
Q

what is the active form of vit. D?

A

Calcitriol** aka 1,25-dihydroxyvit. D

  • 1st hydroxylation in LIVER
  • 2nd hydroxylation in KIDNEY
117
Q

Teriparatide and Abaloparatide

A
  • recombinant PTH 1-34

- treat osteoporosis

118
Q

rhPTH 1-84 (full-length PTH)

A

-treat hypoparathyroidism

119
Q

Raloxifene

A
  • SERM

- beneficial on bone w/o increased risk for breast/endometrial cancer

120
Q

Etidronate, Pamidronate, Alendronate…“-dronate”

A
  • bisphosphonates
  • give on EMPTY STOMACH
  • not given w/ renal issues
  • treat osteoporosis
121
Q

Denosumab

A
  • monoclonal Ab -> inhibit RANKL
  • treat osteoporosis
  • risk of infection, osteonecrosis, hypocalcemia
  • can use in renal disease
122
Q

Hydrochlorothiazide

A
  • diuretic -> block Na2+ reabsorption

- enhance Ca2+ reabsorption -> treat Ca2+ oxalate stones**

123
Q

Cinacalcet

A
  • activates CaSR -> reduce PTH

- treat secondary hyperparathyroidism and parathyroid carcinoma

OMS II - Becom Exam 4 (8 decks)

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