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Introduction to Pharmacology > Steroid Hormones and NSAIDs > Flashcards

Steroid Hormones and NSAIDs Flashcards

1
Q

What is the endocrine system?

A

group of organs/glands that release hormones into circulation for regulating various physiological functions

(+ hypothalamus)

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2
Q

What 3 similarities are shared between hormones and neurotransmitters? What makes them different?

A

chemicals, functions, receptor sites in target cells

HORMONES: originate from glands of the endocrine system, transported in the blood, distal/local target organs, slow action, short and long-lived duration, involuntary response

NT: originate from neurones in the NS, transported by neurons, target local receptors on neurons, fast action, short-lived duration, voluntary and involuntary response

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3
Q

What are the 6 major glands of the endocrine system? What do they secrete?

A
  1. PITUITARY: GH, ACTH, TSH, LH, FSH, PRL, ADH, oxytocin
  2. THYROID: thyroxine, triiodothyronine, PTH
  3. ADRENAL: adrenalin, corticosteroids
  4. PANCREAS: insulin, glucagon
  5. TESTICLE/OVARY: testosterone, estrogen, progesterone
  6. HYPOTHALAMUS: gonadotropin-releasing hormone
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4
Q

What do hormones do? What are 5 specific functions?

A

control the functions of all organs - growth, development, reproduction, sexual characteristics, temperature, hunger

  1. send chemical signals everywhere in the body
  2. development of bones and muscles
  3. bodily changes - puberty
  4. control metabolism
  5. aid in the upkeep of homeostasis
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5
Q

What are the 3 classifications of hormones? What are some examples of each?

A
  1. STEROIDS: cholesterol, progesterone, testosterone, estrogen, cortisol
  2. AMINES: thyroxine, catecholamines, melatonin
  3. PEPTIDES/PROTEINS: insulin, oxytocin, vasopressin, growth hormone
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6
Q

What are the 4 major functions of steroids? Where are they produced?

A
  1. growth
  2. development
  3. sexual differentiation
  4. reproduction

ovaries, placenta, adrenal cortex. testicles

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7
Q

What are steroids produced from? How does this affect their movement in the body?

A

the lipid, cholesterol

easily crosses cell membranes

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8
Q

What are the 2 endogenous corticosteroids? 3 sex steroids?

A

GLUCOCORTICOIDS - cortisol; metabolism, immune system
MINERALOCORTICOIDS - aldosterone; sodium and water retention

ESTROGENS
PROGESTINS
ANDROGENS

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9
Q

What are the 3 major corticosteroid drugs? What 4 things are they commonly used to treat?

A
  1. cortisone
  2. hydrocortisone
  3. prednisone

rashes, inflammatory disease, asthma, cancer

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10
Q

What are the 2 most important effects of corticosteroids? 7 additional?

A

anti-inflammatory and immunosuppressive effects
- intermediary metabolism
- electrolytes and water balance
- CNS effects
- cardiovascular effects
- skeletal muscle effects
- blood cells and lymphoid tissue
- immunologic

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11
Q

What is the synthetic analog of cortisol?

A

hydrocortisone

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12
Q

What are the 8 common side effects of systemic steroids?

A
  1. increased appetite
  2. weight gain
  3. changes in mood
  4. muscle weakness
  5. blurred vision
  6. increased growth of body hair
  7. easy bruising
  8. lower resistance to infection
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13
Q

What 4 conditions are associated with prolonged use of steroids?

A
  1. adrenal atrophy
  2. osteoporosis
  3. immunosuppression
  4. euphoria
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14
Q

What is inflammation? What are 3 major causes? What is involved in this response?

A

non-specific immune response (innate immunity) to infection and injury

physical trauma, noxious chemicals, microbiological agents

immune cells, blood vessels, molecular mediators

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15
Q

What is the function of inflammation? How is it mediated?

A

elimination of the initial cause of cell injury, clear out necrotic cells and damaged tissue, and initiate tissue repair

chemical mediators from injured tissue, like histamine, prostaglandins, bradykinins, etc.

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16
Q

What are 8 common inflammatory diseases in dogs and cats?

A
  1. chronic intestinal inflammation - IBD, celiac in humans
  2. gastric and peptic ulcers
  3. septic and nonseptic inflammatory disease
  4. skin diseases
  5. neoplastic diseases
  6. inflammatory joint diseases
  7. inflammatory oral diseases
  8. primary inflammatory brain disorders
17
Q

What are the 5 classical signs of inflammation?

A
  1. pain
  2. heat
  3. redness
  4. swelling
  5. loss of function
18
Q

What are the 2 types of inflammation?

A

ACUTE - initial response of the body to harmful stimuli involving and increased movement of plasma and leukocytes from the blood into injured tissue (local vascular system, immune system)

CHRONIC: prolonged inflammation leading to the progressive shift in the type of cells at the site of inflammation to mononuclear cells with simultaneous destruction and healing of tissue

19
Q

What are 7 disorders caused by chronic inflammation?

A
  1. diabetes
  2. heart disease
  3. lung issues
  4. bone health
  5. cancer
  6. depression
  7. anger disorders and aggressive behavior
20
Q

What are the 5 aspects of the complex immune response?

A
  1. activation of leukocytes (macrophages, neutrophils, lymphocytes) and the release of chemical mediators of inflammation
  2. arachidonic acid metabolism produces leukotrienes, thromboxanes, and prostaglandins
  3. vasoactive amines and peptides affect vascular permeability
  4. neutrophils produce free radicals and other reactive molecules
  5. pro-inflammatory cytokines are generated
21
Q

What are the mechanisms of action of corticosteroids and NSAIDs?

A

CORTICOSTEROIDS block the production of arachidonic acid and lipoxygenase, which decreases the production of leukotrienes

NSAIDs block cyclooxygenase (COX-1 and COX-2), which decreases the production of prostanoids

22
Q

Prostaglandins and NSAIDs:

A
23
Q

What 2 molecules are cyclooxygenase enzymes responsible for producing?

A
  1. prostaglandins
  2. thromboxane A2
24
Q

What is the difference between COX-1 and COX-2?

A

COX-1: constitutive with constant levels of activity; maintains and protects gastric mucosa, vascular homeostasis and platelet aggregation, maintains renal blood flow (PGs, TXA2)

COX-2: inducible and expressed at sites of injury; up-regulates sensitivity to peripheral nociceptors to induce pain, mediated by inflammation, causes fever by increasing pyrogens, upregulated in carcinomas (PGD2, PGE2, PGF2α, PGI2, bradykinin)

25
Q

What is COX-3 and 5-LOX?

A

COX-3 (COX-1b): found in the brain and regulates fever; discovered in dogs

5-LOX: proinflammatory leukotriene (LTB4)

26
Q

What 3 processes do prostaglandins control? What do they promote?

A
  1. inflammation
  2. blood flow
  3. formation of blood clots

inflammation, pain, fever

27
Q

What are prostaglandins? What do high concentrations commonly cause?

A

lipid compounds that have diverse hormone-like effects in almost every tissue (lungs, GI, kidney, liver, blood vessels)

pain by direct action upon nerve endings

28
Q

What actions is thromboxane A2 responsible for? From where is it predominantly derived?

A
  1. platelet adhesion and aggregation
  2. smooth muscle contraction
  3. activation of endothelial inflammatory responses

platelet COX-1

29
Q

Where are leukotrienes derived from? What are 2 potential benefits in blocking this pathway?

A

lipoxygenase (LOX)

  1. higher GI safety
  2. greater analgesic efficacy
30
Q

Why are prostanoids so complex?

A

different molecules have conflicting effects on both the promotion and resolution of inflammation

  • same product formed from different enzymes (COX-1 vs. COX-2) may promote or resolve inflammation in different models
  • different cell types that predominate at varying stages of disease progression can generate prostanoids that have contrasting effects
  • prostanoids overlap considerably in their biological effects with other mediators
31
Q

What are the main 3 functions of NSAIDs? How does the availability of these drugs compare in dogs and cats?

A
  1. analgesia - reduce the perception of pain (“weak”)
  2. antipyresis - reduce fever
  3. anti-inflammation

more drugs available in dogs than cats

32
Q

What are the 5 most common uses for NSAIDs? What are 2 common adverse effects?

A
  1. osteoarthritis
  2. rheumatoid arthritis (ankylosing spondylitis)
  3. pancreatitis
  4. dental pain
  5. skin inflammation

increased risk of GI complications, deteriorated osteoarthritis

33
Q

Are there any NSAIDs approved for long-term use in cats? What are 4 signs of NSAID overdose in cats?

A

NO

  1. stomach ulcers with bleeding into GI tract
  2. kidney damage and failure
  3. liver problems
  4. brain damage
34
Q

What are the 2 FDA-approved NSAIDs for short-term use in cats?

A
  1. Robenacoxib - Onsior
  2. Meloxicam - Metacam
35
Q

How does the high availability of NSAIDs affect their absorption? What decreases the volume of distribution of NSAIDs?

A

well-absorbed and food does not change this

bound by albumin
- displacement due to competition and hypoalbuminemia can cause higher levels of unbound drug, which can predispose to drug-induced adverse effects

36
Q

Why does the extrapolation of NSAID dosages from other species for cats need to be carefully considered?

A

NSAIDs are highly metabolized in the liver and cats have inefficient cytochrome P450

(young and old patients may require smaller doses due to weak liver and kidney status causing lower elimination rates)

Introduction to Pharmacology (39 decks)

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