202 ES - Disease & Pharmacology Flashcards

1
Q

Drugs used in pituitary disorder

A

Gonadotropin-releasing hormone (GnRH) analogues - Buserelin
Somatostatin analogues - Octreotide
Prolactin inhibitors - Bromocriptine
Growth hormone
Adenocorticoptropic hormone (ACTH) - Corticotropin
Vasopressin and analogues - Desmopressin

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2
Q

Gonadotropin-releasing hormone (GnRH) analogues

pituitary disorder

A

Buserelin

  • stimulate FSH & LH
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3
Q

Somatostatin analogues

pituitary disorder

A

Octreotide
Lanreotide
Pariteotide

  • inhibit pathologically increased secretion of GH
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4
Q

Treatments for acromegaly

A

Radiation therapy
Somatostatin analogue
- if not work → pituitary-directed medical therapy - Pegvisomant

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5
Q

Acromegaly

A

Excess GH

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6
Q

Prolactin inhibitors

pituitary disorder

A

Bromocriptine
Cabergoline
Qionagolide

  • inhibit secretion of prolactin
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7
Q
Adrenocorticotropic hormone (ACTH)
(pituitary disorder)
A

Corticotropin

  • abandoned
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8
Q

Vasopressin and analogues

pituitary disorder

A

Desmopressin
Vasopressin
Terliopressin

  • sm vasoconstriction
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9
Q

Drugs used in thyroid & parathyroid disorders

A

Thyroid Hormone Replacements - Levothyroxine (synthetic T4), Liothyronine (T3)
Thyroid Hormone Suppression - Thioamides - Carbimazole

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10
Q

Thyroid Hormone Replacements

thyroid & parathyroid disorders

A

Levothyroxine (synthetic T4)
Liothyronine (T3)

  • converted to T3 which enters the nucleus and binds to a thyroid hormone receptor.
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11
Q

Thyroid Hormone Suppression

thyroid & parathyroid disorders

A

Thioamides:

  • Carbimazole
  • Methimazole
  • Propylthiouracil
  • Reduces the synthesis of thyroid hormones by inhibiting thyroperoxidase
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12
Q

Can radioactive iodine be used in pregnancy?

A

RAI is contraindicated in pregnancy & breastfeeding

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13
Q

Drugs for bone metabolism disorders

A

Antiresorptive drugs - Bisphosphonates, SERMs, Calcitonin, mAb
Anabolic Agents - Recombinant form of parathyroid hormone - teriparatide
Vitamin D Preparations - Ergocalciferol

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14
Q

Bisphosphonates

bone metabolism disorders

A

Alendronate

  • anchor to cell surface proteins on osteoclast membrane by prenylation
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15
Q

Selective estrogen receptor modulators (SERMs)

bone metabolism disorders

A

Raloxifene

  • inhibits cytokines that recruit osteoclasts
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16
Q

Calcitonin

bone metabolism disorders

A

Lowers blood calcium by:

Inhibits bone resorption by binding to a specific receptor on osteoclasts, inhibiting their action

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17
Q

Denosumab

bone metabolism disorders

A

Antiresorptive - mAb

IgG2 that inhibits RANKL - primary signal for bone resorption

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18
Q

Recombinant form of parathyroid hormone

bone metabolism disorders

A

Teriparatide

  • Stimulation of new bone formation by direct effects on osteoblasts
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19
Q

Vitamin D preparations

bone metabolism disorders

A

Ergocalciferol
Alfacalcidol
Calcitriol

  • act on receptors belonging to the steroid superfamily of receptors to increase serum calcium
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20
Q

Drugs used in adrenal disorders

A

Mineralocorticoid agonists (for Addison’s disease) & antagonists - fludrocortisone
Adrenal Hormone Replacement - Glucocorticoids
Adrenal Hormone suppression (Cushing’s syndrome) - adrenolytic agents, adrenal steroid inhibitors, glucocorticoid receptor (& progesterone receptor) antagonist

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21
Q

Fludrocortisone

adrenal disorders

A

Mineralocorticoid agonists

MOA: Mineralocorticoids interact with intracellular receptors in the kidney controlling transcription of specific genes that cause: ↑ number of Na+ channels, ↑ number of Na+ pumps.

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22
Q

Spironolactone

adrenal disorders

A

Mineralocorticoid antagonists

MOA: Competitive antagonist of aldosterone

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23
Q

Glucocorticoid

adrenal disorders

A

interact with intracellular receptors to inhibit the transcription of specific genes that code for various cytokines esp. IL-2.

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24
Q

Adrenal hormone replacement therapy (2)

A

Glucocorticoid Replacement therapy - hydrocortisone

Mineralocorticoid replacement therapy - fludrocortisone

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25
Q

Surgical intervention of Cushing’s syndrome

A

Transsphenoidal Selective Adenomectomy

Adrenalectomy - unilateral & total bilateral

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26
Q

Adrenolytic agents

adrenal disorders

A

Mitotane

  • inhibits 11-beta hydroxylase & cholesterol side-chain cleavage enzymes
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27
Q

Adrenal steroid inhibitors

adrenal disorders

A

Metyrapone
Ketoconazole
Etomidate
Aminoglutethimide

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28
Q
Glucocorticoid receptor (& progesterone receptor) antagonist 
(adrenal disorders)
A

Mifepristone

  • completely binds to glucocorticoid & progesterone receptors at high doses
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29
Q

What are neuroendocrine tumors (NETs)?

A

Rare tumors that occur in neuroendocrine cells in various organs
Can be malignant or benign

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30
Q

Functioning vs. non-functioning NETs

A

Functioning - secretes biogenic amines or hormones
Secretory but non-functioning - secretes peptides but cause no clinical symptoms
Non-functioning - non-secretory

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31
Q

Carcinoid syndrome

A

Develops when carcinoid tumor metastasize to liver & liver function is compromised

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32
Q

Types of NETs

A

GIT - 50%

  • stomach
  • small & large intestines
  • pancreas

Lungs - 20%

Others

  • skin
  • prostate
  • uterus
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33
Q

Most common origin of carcinoid tumors

A

Small & large intestines

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34
Q

Carcinoid tumor causes: ↑ histamine ↑ bradykinin
Which leads to?
Symptoms of carcinoid syndrome:

A

→ Vasodilation

Symptom: flushing itching

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35
Q

Carcinoid tumor causes: ↑ serotonin
Which leads to? (3)
Symptoms of carcinoid syndrome:

A

→ Fibrosis
Symptom: Pulmonary stenosis, tricuspid regurgitation

→ Bronchoconstriction
Symptom: Asthma, shortness of breath, wheezing

→ ↓ tryptophan → ↓ niacin (Vitamin B3)
Symptoms: Pellagra

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36
Q

Complications of carcinoid syndrome

A

Carcinoid heart disease
Carcinoid crisis
Bowel obstruction

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37
Q

Carcinoid heart disease

A

Thickening of heart valves may lead to leaking

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38
Q

Carcinoid crisis

A

Causes severe episodes of flushing, low bp, confusion & breathing difficulty

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39
Q

Bowel obstruction

A

Cancer that spreads to lymph nodes next to small intestine may cause narrowing & kinking of intestine

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40
Q

How to screen for carcinoid tumors?

A

Octreoscan

  • Carcinoid tumors express more somatostatin receptors
    Octreoscan can be used to image tumors that express an increased amount of somatostatin receptors
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41
Q

Pancreas NET arise from ______ cells.

A

Endocrine

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42
Q

Types of functional PanNETs

A
Insulinoma
Gastrinoma
VIPoma
Glucagonoma
Somatostatinoma
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43
Q

What is the most common type of PanNETs?

A

Insulinoma

  • arise from β cells
  • secrete insulin
  • usually benign
  • can cause hypoglycemia
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44
Q

Treatment of PanNETs

- functional

A

Functional:

  • stomatostatin analogues to ↓ hormone production (exception: somatostatinomas) - Octreotide
  • gastrinoma - PPI to block acid secretion - Omeprazole
45
Q

Treatment of PanNETs

- non-functional

A

Large tumors can be managed by surgical removal

46
Q
Somatostatin analogue
(neuroendocrine tumor & treatment)
A

Octreotide

  • slows down or stops production of hormones
47
Q

When are targeted cancer drugs given?

A

When NET has become metastatic & cannot be removed by surgery.

48
Q

Sunitinib

neuroendocrine tumor & treatment

A

For advanced kidney cancer, GI stromal tumor & panNETs

49
Q

Everolimus

neuroendocrine tumor & treatment

A

Advanced breast cancer, NET of stomach, bowel, lung or pancreas, & kidney cancer

50
Q

First-line treatment for NETs

A

Somatostatin analogue

51
Q

What is a carcinoid tumor?

A

Tumour that secretes chemical into circulation, common in GI tract & lungs.

52
Q

Type 1 diabetes

A

Due to cellular-mediated autoimmune destruction of pancreatic β cells

53
Q

Type 2 diabetes

A

Relative insulin deficiency & peripheral insulin resistance

54
Q

Maturity-Onset Diabetes of the Young (MODY)

A

Impaired insulin secretion w minimal or no defects in insulin action
Autosomal dominant

年青人成年型糖尿病

55
Q

Neonatal diabetes

A

< 6 months of age
Can be transient or permanent
Autosomal dominant

56
Q

Latent autoimmune diabetes in adults (LADA)

A

Adult onset autoimmune diabetes who were insulin independent for an extended time post-diagnosis

潛伏性成人自體免疫糖尿病

57
Q

Type 1.5 diabetes

A

Clinical diagnosis of type 2 diabetes who test positive for autoantibodies

58
Q

Gestational DM

A

Women who have DM during pregnancy

59
Q

Insulin resistance symptoms

A
Altered fibrinolysis, Inflammation, Endothelial dysfunction
Hyperinsulinemia
Hypertension
Hyperglycemia
Dyslipidemia
60
Q

Insulin resistance risks

A

Aging
Obesity
Sedentary lifestyle
Genetics

61
Q

Metabolic syndrome (syndrome X)

A

Insulin resistance & abnormal adipose deposition/function

62
Q

Diabetic ketoacidosis (DKA)

A

Characterized by hyperglycemia, ketoacidosis, ketonuria

  • insulin deficiency inhibits ability of glucose to enter cells for utilization as metabolic fuel - liver rapidly breaks down fat into ketones to employ as fuel source
63
Q

Diabetic ketoacidosis (DKA) is common with pt with ______.

A

Type I Diabetes

64
Q

Hyperosmolar hyperglycemic state (HHS)

A

Commonly seen in pt with Type 2 diabetes, who have concomitant illness that leads to reduced fluid intake

65
Q

Steps in managing type 2 diabetes

A
  1. Glucose control - improve glycemic control
  2. Reduce cardiovascular risk - controlling lipids & bp
  3. Manage comorbidities
66
Q

Diabetic dyslipidemia symptoms & treatment

A

Symptoms:
↑ triglycerides
↓ HDL cholesterol
Small dense LDL particles

Treatment:
Treat w statin initially

67
Q

Hypertension (w diabetes) is treated w?

A

Renin-angiotensin-aldosterone system inhibitors (RAASi)

68
Q

Insulin & insulin analogue - rapid-acting

insulin analogs

A

Insulin lispro
Insulin aspart
Insuline glulisine

69
Q

Thyroid eye disease

A

Autoimmune disease characterized by progressive inflammation & damage to tissues around the eyes, especially extraocular muscle, connective, and fatty tissue

70
Q

Which gender is more likely to have thyroid eye disease?

A

Women

71
Q

Sulfonylureas

treatment for diabetes

A

1st gen: Tolbutamide
2nd gen: Gibenclamide

Interact with the sulfonylurea receptor on surface of pancreatic b cells

72
Q

Meglitinides

treatment for diabetes

A

Repaglinide

Same action as sulfonylurea - interact w receptor on surface of pancreatic b cells

73
Q

Biguanides

treatment for diabetes

A

Metformin

Reduce hepatic glucose production through activation of AMP-activated protein kinase (AMPK)

1st line in T2DM

74
Q

Alpha-glucosidase inhibitors

treatment for diabetes

A

Acarbose

  • Inhibits intestinal α-glucosidase and pancreatic α-amylase so reduces the rise in blood glucose which follows a meal
75
Q

Thiazolidinediones

treatment for diabetes

A

Pioglitazone

  • ligands of peroxisome targeting the PPAR-γ receptor
76
Q

DPP-4 inhibitors

treatment for diabetes

A

Sitagliptin

Competitively inhibit DPP-4, thereby lowering blood glucose by potentiating endogenous incretins (GLP-1 and GIP) which stimulate insulin secretion.

77
Q

GLP-1 Receptor Agonists

treatment for diabetes

A

Liraglutide

  • inhibits pancreatic glucagon secretion & ↑ insulin
78
Q

SGLT2 inhibitors

treatment for diabetes

A

Dapagliflozin

  • Act by promoting glucose excretion into the urine, thereby reducing the concentration of circulating glucose.
79
Q

Adverse effect of Sulfonylureas & Meglitinides

treatment for diabetes

A

Hypoglycemia

80
Q

Drugs for treatments of diabetes

A
Insulin
Sulfonylureas - Gibenclamide
Meglitinides - Repaglinide
Metformin
Alpha-glucosidase inhibitors - Acarbose
Thiazolidinediones - Pioglitazone
DPP-4 inhibitors - Sitagliptin
GLP-1 Receptor Agonists - Exenatide
SGLT-2 inhibitors - Canagliflozin
81
Q

Main form of energy storage

A

Fat in adipose tissue

82
Q

What hormones are orexigenic (stimulate feeding)?

A

Ghrelin
Neuropeptide Y
Orexin A & B

83
Q

What hormones are anorexigenic (signal satiety)?

A
Leptin
Insulin
Glucagon
Melanocortins (product of POMC)
Cholecystokinin
Glucagon-like peptide 1
84
Q

Main action of leptin

A

Reduces appetite & ↓ food consumption

85
Q

Leptin:

Over-feeding ______ concentration; Starvation ______ concentration

A

increases; decreases

86
Q

Leptin effects on energy store

- energy intake > energy expenditure

A

Adipose tissue - ↑ fat deposition, ↑ leptin secretion

→ hypothalamus - altered activity of integrating centers → ↓ energy intake, ↑ metabolic rate

87
Q

Leptin effects on energy store

- energy intake < energy expenditure

A

Adipose tissue - ↓ fat deposition, ↓ leptin secretion

→ hypothalamus - altered activity of integrating centers → ↑ energy intake, ↓ metabolic rate

88
Q

What receptor does leptin bind?

A

ObR

89
Q

Leptin binds to POMC expressing ObR results in?

A

↓ food intake

90
Q

Leptin binds to NPY expressing ObR results in?

A

Inhibiting NPY actions in ↑ food intake

∴ ↓ food intake

91
Q

Effects of neuropeptide Y

A

Stimulates food intake
↓ latency to eat
↑ motivation to eat
Delays satiety (increases meal size)

92
Q

NPY secretion is upregulated when?

A

Food deprivation/restriction

Lack of leptin

93
Q

Effect of POMC

A

↓ food intake & ↑ energy expenditure

94
Q

How does POMC suppress appetite?

A

By releasing α-melanocyte stimulating hormone (α-MSH).

95
Q

Leptin ______ BMR.

A

increases

96
Q

Leptin resistance

A

Diminished response to anorexigenic effects of leptin

97
Q

Actions of ghrelin

A

Appetite stimulator, regulated by feeding status
Stimulates NPY
Stimulates GH release

98
Q

Control of ghrelin secretion

A

Fasting/low-calorie diet → ↑ ghrelin secretion in stomach → ↑ hunger → ↑ food intake → stomach distention or caloric absorption → ↓ ghrelin secretion

99
Q

How does orexin work with ghrelin to stimulate appetite?

A

Orexin production is activated by ghrelin and inhibited by leptin.
Regulates arousal, wakefulness and appetite

100
Q

Ventral-medial hypothalamic NPY neurons ______ feeding

A

stimulate

101
Q

Lateral hypothalamic POMC neurons ______ satiety

A

stimulate

102
Q

What’s the only approved orexigenic drug for treatment of AIDS-induced anorexia?

A

Dronabinol

103
Q

Approved anorexigenic drugs (appetite-suppressing)

A

Orlistat
Liraglutide
Lorcaserin

104
Q

BMI (kg/m2) = ?

A

weight (kg)/ height^2 (m^2)

105
Q

What BMI is considered as obesity in Asian & white European populations?

A

Asian: ≥27.5

White European: ≥30

106
Q

Drugs to treat obesity

A

Orlistat

  • inhibition of lipases blocks absorption of dietary fat
107
Q

Treatment for Addison’s disease

A

Mineralcorticoid agonist - fludrocortisone

108
Q

Treatment for Cushing’s syndrome

A

Adrenal Hormone Suppression

Adrenolytic agents - Mitotane
Adrenal steroid inhibitors - Metyrapone
Glucocorticoid receptor (& progesterone receptor) - Mifepristone
Abiraterone

109
Q

Insulin & insulin analogue - intermediate-acting & long-acting
(insulin analogs)

A

NPH/isophane insulin
Insulin glargine
Insulin detemir