Block 1 Endocrine pharmacology Flashcards

1
Q

Describe the MOA of Raloxifine

A

It’s a selective estrogen receptor modulator which acts a:

  1. An antagonist at the breast & uterus
  2. An partial agonist at the bone
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2
Q

What are the side effects of Raloxafine?

A

Increased risk of thromboembolic events (DVT & PE)

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3
Q

Which one causes endometrial cancer? Raloxifene or Tamoxifen?

A

Tamoxifen

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4
Q

What are the clinical uses of Raloxifene?

A

Osteoporosis in post menopausal women
&
Breast cancer prophylaxis

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5
Q

Osteoporosis in post menopausal women
&
Breast cancer prophylaxis

Are clinical uses of which drug

A

Raloxifene

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6
Q

Describe the MOA of Tamoxifen

A

It’s a selective estrogen receptor modulator which acts a:

  1. An agonist in the bone & uterus
  2. antagonist in the breast
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7
Q

What are the side effects of Tamoxifen (9)

A
  1. Higher risk of thromboembolism (esp in smokers)
  2. Endometrial cancer
  3. Hot flashes
  4. Nausea/vomiting
  5. Menstrual irregularities
  6. Post menopausal bleeding
  7. Vaginal discharge
  8. Pruritis vulvae
  9. Dermatitis
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8
Q
  1. Higher risk of thromboembolism (esp in smokers)
  2. Endometrial cancer
  3. Hot flashes
  4. Nausea/vomiting
  5. Menstrual irregularities
  6. Post menopausal bleeding
  7. Vaginal discharge
  8. Pruritis vulvae
  9. Dermatitis

Are all side effects of which endocrine drug?

A

Tamoxifen

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9
Q

What are the clinical uses of Tamoxifen?

A

Treat & prevent the reoccurrence of ER/PR +ve breast cancers

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10
Q

What drug can be used to Treat & prevent the reoccurrence of ER/PR +ve breast cancers

A

Tamoxifen

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11
Q

Describe the MOA of Bisphosphonate (dronates)

A

They are analogs of pyrophosphate, so they can stabilize the hydroxyapatite bone structure
&
It also induces osteoblasts to secrete more osteoclastic inhibitors (reduce bone reabsorption)

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12
Q

What are the clinical uses of Bisphosphonates?

A
  1. Osteoporosis in post menopausal women
  2. Paget’s disease
  3. Hypercalcemia of malignancy
  4. Osteolytic bone metastases
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13
Q
  1. Osteoporosis in post menopausal women
  2. Paget’s disease
  3. Hypercalcemia of malignancy
  4. Osteolytic bone metastases

Can all be treated by which endocrine-specific drug?

A

Bisphosphonate

phospho pulls Ca2+ into bone

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14
Q

What are the side effects of Bisphosphonates?

A

Bone mineralization
GI diseases (esophageal ulcers)
Osteonecrosis

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15
Q

Bone mineralization
GI diseases (esophageal ulcers)
Osteonecrosis

Can be caused by which endocrine-specific drug?

A

Bisphosphonate

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16
Q

Describe the MOA of Aromatase inhibitors

A

They inhibit the peripheral conversion of androgens into estrogen (lower estrogen levels)

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17
Q

What are the clinical uses of Aromatase inhibitors?

A

Treat ER+ve breast cancer in post menopausal women who are resistant to Tamoxifen

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18
Q

Which drug would you use to treat ER +ve Breast cancer in postmenopausal women who are resistant to Tamoxifen?

A

Aromatase inhibitor

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19
Q

Letrozole, Anastrozole, & Exemestane are all examples of which type of drug class?

A

Aromatase inhibitors

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20
Q

What are the side effects of Aromatase inhibitors?

A
  1. Accelerated bone loss
    - Osteoporosis
    - Fractures
  2. Arthritic symptoms
  3. Hot flushes (nausea/diarrhea)

AA

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21
Q
  1. Accelerated bone loss
    - Osteoporosis
    - Fractures
  2. Arthritic symptoms
  3. Hot flushes (nausea/diarrhea)

Are side effects of which endocrine-specific drug?

A

Aromatase inhibitor

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22
Q

Describe the MOA of HRT’s

A

They increase estrogen & reduce osteoclastic activity (reduce bone loss)

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23
Q

What are the side effects of HRT when unopposed estrogen replacement is used?

A

Higher risk of;
Endometrial cancer
Cardiovascular disease

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24
Q

When unopposed estrogen replacement is used (HRT), what can be used to reduce the risk of Endometrial cancer?

A

Progesterone & progestin to avoid this

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25
Q

What are the clinical uses of HRT?

A

Relief or prevention of menopausal symptoms & osteoporosis

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26
Q

Describe the MOA of Glucocorticoids

A

They interact on specific receptors within target tissues to regulate their expression of corticosteroid-responsive genes which can either increase/or/decrease the expression of these genes to control the synthesis of inflammatory mediators

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27
Q

What are the side effects of glucocorticoids?

A

Cushing’s
Osteoporosis
Retarded growth (muscle atrophy)
Thin skin
Immunosuppression
Cataracts/gluacoma
Osteonecrosis
Suppression of HPA-axis
Teratogenic effects
Emotional disturbances (depression)
Rising BP
Obesity (truncal)
Increased hair (Hirsutism)
Diabetes Mellitus
Striae

CORTICOSTEROIDS

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28
Q

Cataracts
Cushings
Diabetes mellitus
Edema
Glaucoma
Muscle atrophy (limbs)
Osteoporosis
Osteonecrosis
Peptic ulcer disease
Risk of infection
Suppression of HPA-axis

Are all side effects of which endocrine-specific drug?

A

Corticosteroids

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29
Q

Describe the MOA of mineralocorticoids

A

They bind to cytoplasmic receptors & can effect gene transcription

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30
Q

What are the side effects of Mineralocorticoids

A

Cataracts
Cushings
Diabetes mellitus
Edema
Glaucoma
Muscle atrophy (limbs)
Osteoporosis
Osteonecrosis
Peptic ulcer disease
Risk of infection
Suppression of HPA-axis
&
EDEMA
WORSE CARDIAC CONDITION

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31
Q

Describe the MOA of the anabolic steroid Methyltestosterone

A

It acts as an agonist at the androgen receptors to activate them

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32
Q

What are the side effects of Methyltestosterone?

A
  1. Excessive masculinization
  2. Premature closure of the epiphysis
  3. Cholestatic jaundice
  4. Dependence
  5. Acne
  6. Gonadal atrophy
  7. Decreased intratesticular testosterone
  8. Dyslipidemia (high LDL & low HDL)
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33
Q
  1. Excessive masculinization
  2. Premature closure of the epiphysis
  3. Cholestatic jaundice
  4. Dependence
  5. Acne
  6. Gonadal atrophy
  7. Decreased intratesticular testosterone
  8. Dyslipidemia (high LDL & low HDL)

Are all symptoms of which anabolic steroid?

A

Methyltestosterone

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34
Q

Describe the clinical uses of Methyltestosterone

A
  1. Male hypogonadism
  2. Anabolic actions (increase muscle mass, high RBC, & low nitrogen)
  3. Precocious puberty in males
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35
Q
  1. Male hypogonadism
  2. Anabolic actions (increase muscle mass, high RBC, & low nitrogen)
  3. Precocious puberty in males

Are all conditions that can be treated with which anabolic steroid?

A

Methyltestosterone

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36
Q

Describe the MOA of Hormonal contraceptives

A

They suppress LH & FSH which causes an absent mid-cycle surge of LH that causes a decrease in endogenous steroid levels thereby inhibiting ovulation

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37
Q

What are the side effects of oral contraception?

A
  1. Thromboembolism
  2. Pulmonary embolism
  3. Stroke
  4. Hypertension
  5. Genital carcinomas
  6. Gall bladder disease
  7. Breakthrough bleeding
  8. Weight gain
  9. Acne
  10. Hirsutism
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38
Q
  1. Thromboembolism
  2. Pulmonary embolism
  3. Stroke
  4. Hypertension
  5. Genital carcinomas
  6. Gall bladder disease
  7. Breakthrough bleeding
  8. Weight gain
  9. Acne
  10. Hirsutism

Are all side effects of what drug?

A

Oral contraceptives

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39
Q

Describe the MOA of Leuprolide

A

It’s a GnRH analog that acts on the pituitary gland GnRH receptors it has both pulsatile & continuous forms

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40
Q

Describe pulsatile leuprolide

A

it’s a GnRH agonist to increase FSH & LH in pregnancy

41
Q

Describe continuous leuprolide

A

A tumor flare (agonist) followed by a decrease in FSH & LH antagonists

42
Q

Describe the MOA & Clinical uses of Ganirelix, cetrorelix, abarelix, & dagarelix?

A

MOA:
they are GnRH receptor agonists t=which when combined with GnRH analogs like leuprolide they can be used to avoid a tumor flare

Rx:
Advanced prostate cancer
Endometriosis

43
Q

MOA:
they are GnRH receptor agonists t=which when combined with GnRH analogs like leuprolide they can be used to avoid a tumor flare

Rx:
Advanced prostate cancer
Endometriosis

A

Ganirelix, cetrorelix, abarelix, & dagarelix

44
Q

What are the side effects of Leuprolide?

A

Hypogonadism
Nausea/vomiting
Erectile dysfunction
Decreased libido

45
Q

Hypogonadism
Nausea/vomiting
Erectile dysfunction
Decreased libido

Are the side effects of what drug?

A

Leuprolide

Leuprolide lacks libido :(

46
Q

What are the clinical uses of Leuprolide?

A

Infertility
Endometriosis
Prostate cancer
Precocious puberty
Uterine fibroids

47
Q

Uterine fibroids
Infertility
Prostate cancer
Precocious puberty
Prostate cancer
Endometriosis

Are all side effects of what drug?

A

Leuprolide

48
Q

Describe the MOA of Flutamide

A

A non-steroidal competitive inhibitor at the androgen receptors (decrease testosterone)

49
Q

What are the side effects of Flutamide?

A

Gynecomastia
Breast tenderness
Liver damage

50
Q

What are the clinical uses of Flutamide?

A

Prostate cancer
Acne
Female Hirsutism
PCOS (test symptoms)

51
Q

Prostate cancer
Acne
Female Hirsutism
PCOS (test symptoms)

Are all side effects of what type of endocrine drug?

A

Flutamide

52
Q

Describe the MOA of Finasteride

A

It inhibits 5-reductase at androgen receptors to decrease the conversion of testosterone to DTH

53
Q

What are the side effects of Finasteride?

A

Gynecomastia
Sexual dysfunction

54
Q

What are the clinical uses of Finasteride?

A

BPH
Male-pattern baldness

Men use Finastride to look fine

55
Q

BPH
Male-pattern baldness

Can be treated with what endocrine drug?

A

Finasteride

56
Q

Describe the MOA of Oxytocin

A

It stimulates the uterine smooth muscle to contract & it also had both vasopressor & antidiuretic effects

57
Q

What are the clinical uses of Oxytocin?

A

Induce labor
Controlling uterine hemorrhage
Breast engorgement
Uterine inertia

58
Q

Induce labor
Controlling uterine hemorrhage
Breast engorgement
Uterine inertia

Can all be treated with which endocrine-specific drug?

A

Oxytocin

59
Q

What are the side effects of Oxytocin?

A

Hypotension
Arrythmias
Electrolyte imbalance
Increased uterine mobility
Decreased uterine blood flow
Abruptio placentae

60
Q

Hypotension
Arrythmias
Electrolyte imbalance
Increased uterine mobility
Decreased uterine blood flow
Abruptio placentae

Are all side effects of which endocrine drug?

A

Oxytocin

61
Q

Describe the MOA of ketoconazole

A

It inhibits steroid synthesis by inhibiting 17,20 desmolase & 17 hydroxylase)
&
It inhibits the CYPP450 enzymes needed for the synthesis of steroids at the Leydig cells (less testosterone)

62
Q

What are the side effects of ketoconazole?

A

Gynecomastia
Amenorrhea

63
Q

Gynecomastia & Amenorrhea are side effects of which endocrine-specific drug?

A

Ketoconazole

64
Q

What are the clinical uses of ketoconazole?

A

PCOS
Adrenal carcinoma
Hirsutism
Breast & prostate cancer
Cushing’s

65
Q

PCOS
Adrenal carcinoma
Hirsutism
Breast & prostate cancer
Cushing’s

Can all be treated with which endocrine-specific drug?

A

Ketoconazole

“CHAPP-B lips”

66
Q

Describe the MOA of Levonorgestrel/progastrin’s

A

It’s administered before an LH surge to inhibit ovulation, it also affects the cervical mucus, tubal functioning, & endometrial lining

67
Q

What is the clinical use of Levonorgestrel/progastrin’s?

A

Plan B

68
Q

What are the clinical side effects of Levonorgestrel/progastrin’s?

A

Headaches
Nausea
Fatigue
Abdominal pain
Dizziness
Tender breasts

69
Q

Headaches
Nausea
Fatigue
Abdominal pain
Dizziness
Tender breasts

Are all side effects of which endocrine-specific drug?

A

Levonorgestrel/progastrin’s

70
Q

What are the zero order kinetics drugs

A

Phenytoin
Ethyl alcohol
Theophylline
Aspirin

71
Q

Describe the MOA of Octreotide

A

It inhibits the release of GH, certain Gi & pancreatic hormones, & decreases splenic blood flow

72
Q

What are the clinical uses of Octreotide?

A

Acromegaly
Carcinoid syndrome
Gastronome
Esophageal varices
Pituitary adenoma
Diabetic diarrhea

73
Q

Acromegaly
Carcinoid syndrome
Gastronome
Esophageal varices
Pituitary adenoma
Diabetic diarrhea

Can all be treated with which endocrine-specific drug?

A

Octreotide

74
Q

What are the side effects of Octreotide?

A

Loose stools
Steatorrhea
Malabsorption
Nausea
Flatulence
Gallstones

75
Q

Loose stools
Steatorrhea
Malabsorption
Nausea
Flatulence
Gallstones

Are all side effects of which endocrine-specific drug?

A

Octreotide

ate(8) too much

76
Q

Describe the MOA of Bromocriptine/cabergoline

A

It acts as a dopamine receptor agonist which are activated by lactotroph dopamine D2 receptors that cause lactin to be inhibited

77
Q

What are the general side effects of Bromocriptine?

A

Dyskinesia
Psychosis
Nausea/vomiting
Dizziness
Nasal stuffiness
Orthostatic hypotension
Cold-induced vasospasms (Ergot effect)

78
Q

What are the side effects of oral bromocriptine (Alendronate or Risectronate)

A

Gi upset
Gastric reflux
esophageal ulcers

79
Q

Gi upset
Gastric reflux
esophageal ulcers

are side effects of which type of bromocriptine durgs

A

Oral:

Alendronate
Risechdronate

80
Q

Dyskinesia
Psychosis
Nausea/vomiting
Dizziness
Nasal stuffiness
Orthostatic hypotension
Cold-induced vasospasms (Ergot effect)

Are side effects of which endocrine-specific drug?

A

Bromocriptine

81
Q

Describe the following for calcitonin:

Clinical uses

A

Pagets disease & hypercalcemia

82
Q

What are the clinical uses of Bromocriptine?

A

Hyperprolactinemia
Acromegaly
Galactorrhea
Parkinsons

BromoPIT-ine = pituitary conditions

83
Q

Hyperprolactinemia
Acromegaly
Galactorrhea
Parkinsons

Can all be treated with which endocrine-specific drug?

A

Bromocriptine

84
Q

What are the drug treatment options of acromegaly?

A

Bromocriptine/cabergoline
Octreotide
Somatostatin
Pevisomant

85
Q

Bromocriptine/cabergoline
Octreotide
Somatostatin
Pevisomant

Can all be used to treat which condition?

A

Acromegaly

86
Q

What are the triggers for G6PD deficiency?

A

1) Food (fava beans)

2) Antibiotics (Sulfa drugs, dapsone, nitrofurantoin, & isoniazid)

3) Anti-malarial (Primaquine, Chloroquine, & quinidine)

4) Aspirin & acetaminophen

87
Q

1) Food (fava beans)

2) Antibiotics (Sulfa drugs, dapsone, nitrofurantoin, & isoniazid)

3) Anti-malarial (Primaquine, Chloroquine, & quinidine)

4) Aspirin & acetaminophen

Are all triggers for which condition?

A

G6PD deficiency

88
Q

Nandrolone propionate
Nandrolone decanoate
Stanazolol
Oxandroline

Are all examples of which type of drug?

A

Anabolic steroids

89
Q

Anabolic steroids (that you need to know x4)

A

Nandrolone propionate
Nandrolone decanoate
Stanazolol
Oxandroline

“PODS”

90
Q

Describe the MOA for Clomiphene citrate

A

A non-steroidal used to induce ovulation. It’s a mixed agonist & antagonist for estrogen receptors & it acts on the hypothalamus to deplete ER & blocks the negative feedback of estradiol this results in higher levels of GnRH, FSH, & LH aka ovulation

91
Q

A non-steroidal used to induce ovulation. It’s a mixed agonist & antagonist for estrogen receptors & it acts on the hypothalamus to deplete ER & blocks the negative feedback of estradiol this results in higher levels of GnRH, FSH, & LH aka ovulation

Describes the MOA for which drug?

A

Clomiphene citrate

92
Q

What are the clinical uses & side effects of clomiphene citrate?

A

Uses:
Infertility

Side effects:
1) Multiple births
2) Hot flashes
3) Allergic dermatitis
4) Visual disturbances

93
Q

Uses:
Infertility

Side effects:
1) Multiple births
2) Hot flashes
3) Allergic dermatitis
4) Visual disturbances

Describe the use of which drug ?

A

Clomiphene citrate

94
Q

Describe the following for cushings:

What are the treatment options?

What is the diagnostic test?

What are the symptoms?

Apart from cancer or a fungus what can cause it (in babies)

A

Rx:
surgery to remove the adenoma
OR
Ketoconazole (antifungal) to block ergosterol synthesis of the fungi

Test:
Dexamethasone suppression test

Side effects:
1) Gynecomastia (ketoconazole_
2) Buffalo hum & moon face
3) purple striae
4) Hyperpigmentation (MSH)

Other cause:
Glucocorticoids which increase annexin-1 (lipocortin) phospholipase A2 inhibition

95
Q

Corticosteroids have impacts on various systems:

What are the impacts of corticosteroids on the carbohydrate system?

A

Hyperglycemia (more gluconeogenesis & less peripheral uptake) be careful with diabetics

96
Q

Corticosteroids have impacts on various systems:

What are the impacts of corticosteroids on the lipid metabolism system?

A

They cause redistribution of fa giving the classic buffalo hump & moon face appearance (careful with long tern use!)

97
Q

Corticosteroids have impacts on various systems:

What are the impacts of corticosteroids on the calcium metabolism system?

A

It decreases intestinal absoprtion & increases renal excretion meaning there’s a high risk of developing osteoporosis

98
Q

Corticosteroids have impacts on various systems:

What are the impacts of corticosteroids on the protein metabolism system?

A

causes a negative nitrogen imbalance which can lead to muscle aches & eventual myopathy in long term use