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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
What are the clinical uses of HRT?
Relief or prevention of menopausal symptoms & osteoporosis
26
Describe the MOA of Glucocorticoids
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
27
What are the side effects of glucocorticoids?
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 ## Footnote CORTICOSTEROIDS
28
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?
Corticosteroids
29
Describe the MOA of mineralocorticoids
They bind to cytoplasmic receptors & can effect gene transcription
30
What are the side effects of Mineralocorticoids
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
31
Describe the MOA of the anabolic steroid Methyltestosterone
It acts as an agonist at the androgen receptors to activate them
32
What are the side effects of Methyltestosterone?
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)
33
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?
Methyltestosterone
34
Describe the clinical uses of Methyltestosterone
1. Male hypogonadism 2. Anabolic actions (increase muscle mass, high RBC, & low nitrogen) 3. Precocious puberty in males
35
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?
Methyltestosterone
36
Describe the MOA of Hormonal contraceptives
They suppress LH & FSH which causes an absent mid-cycle surge of LH that causes a decrease in endogenous steroid levels thereby inhibiting ovulation
37
What are the side effects of oral contraception?
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
38
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?
Oral contraceptives
39
Describe the MOA of Leuprolide
It's a GnRH analog that acts on the pituitary gland GnRH receptors it has both pulsatile & continuous forms
40
Describe pulsatile leuprolide
it's a GnRH agonist to increase FSH & LH in pregnancy
41
Describe continuous leuprolide
A tumor flare (agonist) followed by a decrease in FSH & LH antagonists
42
Describe the MOA & Clinical uses of Ganirelix, cetrorelix, abarelix, & dagarelix?
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
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
Ganirelix, cetrorelix, abarelix, & dagarelix
44
What are the side effects of Leuprolide?
Hypogonadism Nausea/vomiting Erectile dysfunction Decreased libido
45
Hypogonadism Nausea/vomiting Erectile dysfunction Decreased libido Are the side effects of what drug?
Leuprolide | Leuprolide lacks libido :(
46
What are the clinical uses of Leuprolide?
Infertility Endometriosis Prostate cancer Precocious puberty Uterine fibroids
47
Uterine fibroids Infertility Prostate cancer Precocious puberty Prostate cancer Endometriosis Are all side effects of what drug?
Leuprolide
48
Describe the MOA of Flutamide
A non-steroidal competitive inhibitor at the androgen receptors (decrease testosterone)
49
What are the side effects of Flutamide?
Gynecomastia Breast tenderness Liver damage
50
What are the clinical uses of Flutamide?
Prostate cancer Acne Female Hirsutism PCOS (test symptoms)
51
Prostate cancer Acne Female Hirsutism PCOS (test symptoms) Are all side effects of what type of endocrine drug?
Flutamide
52
Describe the MOA of Finasteride
It inhibits 5-reductase at androgen receptors to decrease the conversion of testosterone to DTH
53
What are the side effects of Finasteride?
Gynecomastia Sexual dysfunction
54
What are the clinical uses of Finasteride?
BPH Male-pattern baldness | Men use Finastride to look fine
55
BPH Male-pattern baldness Can be treated with what endocrine drug?
Finasteride
56
Describe the MOA of Oxytocin
It stimulates the uterine smooth muscle to contract & it also had both vasopressor & antidiuretic effects
57
What are the clinical uses of Oxytocin?
Induce labor Controlling uterine hemorrhage Breast engorgement Uterine inertia
58
Induce labor Controlling uterine hemorrhage Breast engorgement Uterine inertia Can all be treated with which endocrine-specific drug?
Oxytocin
59
What are the side effects of Oxytocin?
Hypotension Arrythmias Electrolyte imbalance Increased uterine mobility Decreased uterine blood flow Abruptio placentae
60
Hypotension Arrythmias Electrolyte imbalance Increased uterine mobility Decreased uterine blood flow Abruptio placentae Are all side effects of which endocrine drug?
Oxytocin
61
Describe the MOA of ketoconazole
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
What are the side effects of ketoconazole?
Gynecomastia Amenorrhea
63
Gynecomastia & Amenorrhea are side effects of which endocrine-specific drug?
Ketoconazole
64
What are the clinical uses of ketoconazole?
PCOS Adrenal carcinoma Hirsutism Breast & prostate cancer Cushing's
65
PCOS Adrenal carcinoma Hirsutism Breast & prostate cancer Cushing's Can all be treated with which endocrine-specific drug?
Ketoconazole | "CHAPP-B lips"
66
Describe the MOA of Levonorgestrel/progastrin's
It's administered before an LH surge to inhibit ovulation, it also affects the cervical mucus, tubal functioning, & endometrial lining
67
What is the clinical use of Levonorgestrel/progastrin's?
Plan B
68
What are the clinical side effects of Levonorgestrel/progastrin's?
Headaches Nausea Fatigue Abdominal pain Dizziness Tender breasts
69
Headaches Nausea Fatigue Abdominal pain Dizziness Tender breasts Are all side effects of which endocrine-specific drug?
Levonorgestrel/progastrin's
70
What are the zero order kinetics drugs
Phenytoin Ethyl alcohol Theophylline Aspirin
71
Describe the MOA of Octreotide
It inhibits the release of GH, certain Gi & pancreatic hormones, & decreases splenic blood flow
72
What are the clinical uses of Octreotide?
Acromegaly Carcinoid syndrome Gastronome Esophageal varices Pituitary adenoma Diabetic diarrhea
73
Acromegaly Carcinoid syndrome Gastronome Esophageal varices Pituitary adenoma Diabetic diarrhea Can all be treated with which endocrine-specific drug?
Octreotide
74
What are the side effects of Octreotide?
Loose stools Steatorrhea Malabsorption Nausea Flatulence Gallstones
75
Loose stools Steatorrhea Malabsorption Nausea Flatulence Gallstones Are all side effects of which endocrine-specific drug?
Octreotide | ate(8) too much
76
Describe the MOA of Bromocriptine/cabergoline
It acts as a dopamine receptor agonist which are activated by lactotroph dopamine D2 receptors that cause lactin to be inhibited
77
What are the general side effects of Bromocriptine?
Dyskinesia Psychosis Nausea/vomiting Dizziness Nasal stuffiness Orthostatic hypotension Cold-induced vasospasms (Ergot effect)
78
What are the side effects of oral bromocriptine (Alendronate or Risectronate)
Gi upset Gastric reflux esophageal ulcers
79
Gi upset Gastric reflux esophageal ulcers are side effects of which type of bromocriptine durgs
Oral: Alendronate Risechdronate
80
Dyskinesia Psychosis Nausea/vomiting Dizziness Nasal stuffiness Orthostatic hypotension Cold-induced vasospasms (Ergot effect) Are side effects of which endocrine-specific drug?
Bromocriptine
81
Describe the following for calcitonin: Clinical uses
Pagets disease & hypercalcemia
82
What are the clinical uses of Bromocriptine?
Hyperprolactinemia Acromegaly Galactorrhea Parkinsons | BromoPIT-ine = pituitary conditions
83
Hyperprolactinemia Acromegaly Galactorrhea Parkinsons Can all be treated with which endocrine-specific drug?
Bromocriptine
84
What are the drug treatment options of acromegaly?
Bromocriptine/cabergoline Octreotide Somatostatin Pevisomant
85
Bromocriptine/cabergoline Octreotide Somatostatin Pevisomant Can all be used to treat which condition?
Acromegaly
86
What are the triggers for G6PD deficiency?
1) Food (fava beans) 2) Antibiotics (Sulfa drugs, dapsone, nitrofurantoin, & isoniazid) 3) Anti-malarial (Primaquine, Chloroquine, & quinidine) 4) Aspirin & acetaminophen
87
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?
G6PD deficiency
88
Nandrolone propionate Nandrolone decanoate Stanazolol Oxandroline Are all examples of which type of drug?
Anabolic steroids
89
Anabolic steroids (that you need to know x4)
Nandrolone propionate Nandrolone decanoate Stanazolol Oxandroline | "PODS"
90
Describe the MOA for Clomiphene citrate
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
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?
Clomiphene citrate
92
What are the clinical uses & side effects of clomiphene citrate?
Uses: Infertility Side effects: 1) Multiple births 2) Hot flashes 3) Allergic dermatitis 4) Visual disturbances
93
Uses: Infertility Side effects: 1) Multiple births 2) Hot flashes 3) Allergic dermatitis 4) Visual disturbances Describe the use of which drug ?
Clomiphene citrate
94
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)
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
Corticosteroids have impacts on various systems: What are the impacts of corticosteroids on the carbohydrate system?
Hyperglycemia (more gluconeogenesis & less peripheral uptake) be careful with diabetics
96
Corticosteroids have impacts on various systems: What are the impacts of corticosteroids on the lipid metabolism system?
They cause redistribution of fa giving the classic buffalo hump & moon face appearance (careful with long tern use!)
97
Corticosteroids have impacts on various systems: What are the impacts of corticosteroids on the calcium metabolism system?
It decreases intestinal absoprtion & increases renal excretion meaning there's a high risk of developing osteoporosis
98
Corticosteroids have impacts on various systems: What are the impacts of corticosteroids on the protein metabolism system?
causes a negative nitrogen imbalance which can lead to muscle aches & eventual myopathy in long term use

Pharm SJSM (23 decks)

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