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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
Surgical intervention of Cushing's syndrome
Transsphenoidal Selective Adenomectomy | Adrenalectomy - unilateral & total bilateral
26
Adrenolytic agents | adrenal disorders
Mitotane - inhibits 11-beta hydroxylase & cholesterol side-chain cleavage enzymes
27
Adrenal steroid inhibitors | adrenal disorders
Metyrapone Ketoconazole Etomidate Aminoglutethimide
28
``` Glucocorticoid receptor (& progesterone receptor) antagonist (adrenal disorders) ```
Mifepristone - completely binds to glucocorticoid & progesterone receptors at high doses
29
What are neuroendocrine tumors (NETs)?
Rare tumors that occur in neuroendocrine cells in various organs Can be malignant or benign
30
Functioning vs. non-functioning NETs
Functioning - secretes biogenic amines or hormones Secretory but non-functioning - secretes peptides but cause no clinical symptoms Non-functioning - non-secretory
31
Carcinoid syndrome
Develops when carcinoid tumor metastasize to liver & liver function is compromised
32
Types of NETs
GIT - 50% - stomach - small & large intestines - pancreas Lungs - 20% Others - skin - prostate - uterus
33
Most common origin of carcinoid tumors
Small & large intestines
34
Carcinoid tumor causes: ↑ histamine ↑ bradykinin Which leads to? Symptoms of carcinoid syndrome:
→ Vasodilation | Symptom: flushing itching
35
Carcinoid tumor causes: ↑ serotonin Which leads to? (3) Symptoms of carcinoid syndrome:
→ Fibrosis Symptom: Pulmonary stenosis, tricuspid regurgitation → Bronchoconstriction Symptom: Asthma, shortness of breath, wheezing → ↓ tryptophan → ↓ niacin (Vitamin B3) Symptoms: Pellagra
36
Complications of carcinoid syndrome
Carcinoid heart disease Carcinoid crisis Bowel obstruction
37
Carcinoid heart disease
Thickening of heart valves may lead to leaking
38
Carcinoid crisis
Causes severe episodes of flushing, low bp, confusion & breathing difficulty
39
Bowel obstruction
Cancer that spreads to lymph nodes next to small intestine may cause narrowing & kinking of intestine
40
How to screen for carcinoid tumors?
Octreoscan - Carcinoid tumors express more somatostatin receptors Octreoscan can be used to image tumors that express an increased amount of somatostatin receptors
41
Pancreas NET arise from ______ cells.
Endocrine
42
Types of functional PanNETs
``` Insulinoma Gastrinoma VIPoma Glucagonoma Somatostatinoma ```
43
What is the most common type of PanNETs?
Insulinoma - arise from β cells - secrete insulin - usually benign - can cause hypoglycemia
44
Treatment of PanNETs | - functional
Functional: - stomatostatin analogues to ↓ hormone production (exception: somatostatinomas) - Octreotide - gastrinoma - PPI to block acid secretion - Omeprazole
45
Treatment of PanNETs | - non-functional
Large tumors can be managed by surgical removal
46
``` Somatostatin analogue (neuroendocrine tumor & treatment) ```
Octreotide - slows down or stops production of hormones
47
When are targeted cancer drugs given?
When NET has become metastatic & cannot be removed by surgery.
48
Sunitinib | neuroendocrine tumor & treatment
For advanced kidney cancer, GI stromal tumor & panNETs
49
Everolimus | neuroendocrine tumor & treatment
Advanced breast cancer, NET of stomach, bowel, lung or pancreas, & kidney cancer
50
First-line treatment for NETs
Somatostatin analogue
51
What is a carcinoid tumor?
Tumour that secretes chemical into circulation, common in GI tract & lungs.
52
Type 1 diabetes
Due to cellular-mediated autoimmune destruction of pancreatic β cells
53
Type 2 diabetes
Relative insulin deficiency & peripheral insulin resistance
54
Maturity-Onset Diabetes of the Young (MODY)
Impaired insulin secretion w minimal or no defects in insulin action Autosomal dominant 年青人成年型糖尿病
55
Neonatal diabetes
< 6 months of age Can be transient or permanent Autosomal dominant
56
Latent autoimmune diabetes in adults (LADA)
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
Type 1.5 diabetes
Clinical diagnosis of type 2 diabetes who test positive for autoantibodies
58
Gestational DM
Women who have DM during pregnancy
59
Insulin resistance symptoms
``` Altered fibrinolysis, Inflammation, Endothelial dysfunction Hyperinsulinemia Hypertension Hyperglycemia Dyslipidemia ```
60
Insulin resistance risks
Aging Obesity Sedentary lifestyle Genetics
61
Metabolic syndrome (syndrome X)
Insulin resistance & abnormal adipose deposition/function
62
Diabetic ketoacidosis (DKA)
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
Diabetic ketoacidosis (DKA) is common with pt with ______.
Type I Diabetes
64
Hyperosmolar hyperglycemic state (HHS)
Commonly seen in pt with Type 2 diabetes, who have concomitant illness that leads to reduced fluid intake
65
Steps in managing type 2 diabetes
1. Glucose control - improve glycemic control 2. Reduce cardiovascular risk - controlling lipids & bp 3. Manage comorbidities
66
Diabetic dyslipidemia symptoms & treatment
Symptoms: ↑ triglycerides ↓ HDL cholesterol Small dense LDL particles Treatment: Treat w statin initially
67
Hypertension (w diabetes) is treated w?
Renin-angiotensin-aldosterone system inhibitors (RAASi)
68
Insulin & insulin analogue - rapid-acting | insulin analogs
Insulin lispro Insulin aspart Insuline glulisine
69
Thyroid eye disease
Autoimmune disease characterized by progressive inflammation & damage to tissues around the eyes, especially extraocular muscle, connective, and fatty tissue
70
Which gender is more likely to have thyroid eye disease?
Women
71
Sulfonylureas | treatment for diabetes
1st gen: Tolbutamide 2nd gen: Gibenclamide Interact with the sulfonylurea receptor on surface of pancreatic b cells
72
Meglitinides | treatment for diabetes
Repaglinide Same action as sulfonylurea - interact w receptor on surface of pancreatic b cells
73
Biguanides | treatment for diabetes
Metformin Reduce hepatic glucose production through activation of AMP-activated protein kinase (AMPK) 1st line in T2DM
74
Alpha-glucosidase inhibitors | treatment for diabetes
Acarbose - Inhibits intestinal α-glucosidase and pancreatic α-amylase so reduces the rise in blood glucose which follows a meal
75
Thiazolidinediones | treatment for diabetes
Pioglitazone - ligands of peroxisome targeting the PPAR-γ receptor
76
DPP-4 inhibitors | treatment for diabetes
Sitagliptin Competitively inhibit DPP-4, thereby lowering blood glucose by potentiating endogenous incretins (GLP-1 and GIP) which stimulate insulin secretion.
77
GLP-1 Receptor Agonists | treatment for diabetes
Liraglutide - inhibits pancreatic glucagon secretion & ↑ insulin
78
SGLT2 inhibitors | treatment for diabetes
Dapagliflozin - Act by promoting glucose excretion into the urine, thereby reducing the concentration of circulating glucose.
79
Adverse effect of Sulfonylureas & Meglitinides | treatment for diabetes
Hypoglycemia
80
Drugs for treatments of diabetes
``` 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
Main form of energy storage
Fat in adipose tissue
82
What hormones are orexigenic (stimulate feeding)?
Ghrelin Neuropeptide Y Orexin A & B
83
What hormones are anorexigenic (signal satiety)?
``` Leptin Insulin Glucagon Melanocortins (product of POMC) Cholecystokinin Glucagon-like peptide 1 ```
84
Main action of leptin
Reduces appetite & ↓ food consumption
85
Leptin: | Over-feeding ______ concentration; Starvation ______ concentration
increases; decreases
86
Leptin effects on energy store | - energy intake > energy expenditure
Adipose tissue - ↑ fat deposition, ↑ leptin secretion | → hypothalamus - altered activity of integrating centers → ↓ energy intake, ↑ metabolic rate
87
Leptin effects on energy store | - energy intake < energy expenditure
Adipose tissue - ↓ fat deposition, ↓ leptin secretion | → hypothalamus - altered activity of integrating centers → ↑ energy intake, ↓ metabolic rate
88
What receptor does leptin bind?
ObR
89
Leptin binds to POMC expressing ObR results in?
↓ food intake
90
Leptin binds to NPY expressing ObR results in?
Inhibiting NPY actions in ↑ food intake | ∴ ↓ food intake
91
Effects of neuropeptide Y
Stimulates food intake ↓ latency to eat ↑ motivation to eat Delays satiety (increases meal size)
92
NPY secretion is upregulated when?
Food deprivation/restriction | Lack of leptin
93
Effect of POMC
↓ food intake & ↑ energy expenditure
94
How does POMC suppress appetite?
By releasing α-melanocyte stimulating hormone (α-MSH).
95
Leptin ______ BMR.
increases
96
Leptin resistance
Diminished response to anorexigenic effects of leptin
97
Actions of ghrelin
Appetite stimulator, regulated by feeding status Stimulates NPY Stimulates GH release
98
Control of ghrelin secretion
Fasting/low-calorie diet → ↑ ghrelin secretion in stomach → ↑ hunger → ↑ food intake → stomach distention or caloric absorption → ↓ ghrelin secretion
99
How does orexin work with ghrelin to stimulate appetite?
Orexin production is activated by ghrelin and inhibited by leptin. Regulates arousal, wakefulness and appetite
100
Ventral-medial hypothalamic NPY neurons ______ feeding
stimulate
101
Lateral hypothalamic POMC neurons ______ satiety
stimulate
102
What's the only approved orexigenic drug for treatment of AIDS-induced anorexia?
Dronabinol
103
Approved anorexigenic drugs (appetite-suppressing)
Orlistat Liraglutide Lorcaserin
104
BMI (kg/m2) = ?
weight (kg)/ height^2 (m^2)
105
What BMI is considered as obesity in Asian & white European populations?
Asian: ≥27.5 | White European: ≥30
106
Drugs to treat obesity
Orlistat - inhibition of lipases blocks absorption of dietary fat
107
Treatment for Addison's disease
Mineralcorticoid agonist - fludrocortisone
108
Treatment for Cushing's syndrome
Adrenal Hormone Suppression Adrenolytic agents - Mitotane Adrenal steroid inhibitors - Metyrapone Glucocorticoid receptor (& progesterone receptor) - Mifepristone Abiraterone
109
Insulin & insulin analogue - intermediate-acting & long-acting (insulin analogs)
NPH/isophane insulin Insulin glargine Insulin detemir

MBBS (28 decks)

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