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Intro to Pharmacology > Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) > Flashcards

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Flashcards

1
Q

The Endocrine system encompasses a group of organs/glands that release _______ into circulation for regulating various _________ functions.

Endocrine organs can also release _____. ____ and hormones have many similarities, but also have their differences.

A

hormones, physiological
NT, NT

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2
Q

Hormones versus Neurotransmittters
Origin

A

Hormones = Glands of the endocrine system

NT = Neurons of the NS

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3
Q

Hormones versus Neurotransmittters
Transport

A

Hormones = blood
NT = Neurons

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4
Q

Hormones versus Neurotransmittters
Target

A

Hormones = Distal and local organs
NT = Local receptors on neurons

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5
Q

Hormones versus Neurotransmittters
Action

A

Hormones = Slow (up to few days)
NT = Fast (up to milliseconds)

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6
Q

Hormones versus Neurotransmittters
Duration of effect

A

Hormones = Short and long lived
NT = Short lived

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7
Q

Hormones versus Neurotransmittters
Response

A

Hormones = Involuntary
NT = Voluntary and Involuntary

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8
Q

Endocrine System, Glands, and Hormones

A

Different hormones from different glands with different actions

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9
Q

List the similarities between hormones and NT?

A
  • Chemicals
  • Functions
  • Receptor sites in target cells
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10
Q

List the differences between hormones and NTs?

A

Regulate each other
* Feedback system

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11
Q

Neuroendocrines produce ?

A

neurotransmitters and hormones.

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12
Q

Hormones control the functions of ___ the organs. They affect diverse processes of ____ and ________, _______ and _____ characteristics, __________, _______.
▪ Sending _______ signals to everywhere in the body
▪ They play a role in the development of _____ and _____
▪ They are necessary for bodily changes such as _____
▪ They control _____
▪ They aid in the upkeep of ___________

A

all, growth, development, reproduction, sexual, temperature, hunger

chemical, bones, muscles, puberty, metabolism, homeostasis

There are about 20 different hormones produced in nonhuman animals

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13
Q

Classification of Hormones

A

Two groups: Steroids and non-steroids
Steroids include: cholesterol, progesterone, testosterone, estrogen, cortisol.

All are lipid derived, insoluble (stay longer in blood), cross membrane and ?

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14
Q

Steroids have an important role in ?

A

growth, development,
sexual differentiation and reproduction.

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15
Q

Steroid hormones are produced from a lipid called ________. They can _____ cross cell membranes

A

cholesterol, easily

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16
Q

Endogenous corticosteroids

A

Glucocorticoids ➢ Cortisol(metabolism and immune system)
Mineralocorticoids ➢ Aldosterone
(sodium and water retention

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17
Q

Corticosteroid drugs — including (3?) —
are useful in treating many conditions, such as _______, ________ diseases, _______, _____

A

cortisone, hydrocortisone and prednisone, rashes, inflammatory, asthma, cancer

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18
Q

Corticosteroids have…:
▪ Effects on ___________ metabolism
▪ Actions on ______ and ____ balance
▪ ___ effects
▪ ___________ effects
▪ ______ muscle effects
▪ Effects on ____ cells and ______ tissue
▪ ________ effects
▪ ____-_______ and ___________ effects

But these drugs also carry a risk of various ?

A

intermediary, electrolytes, water, CNS, Cardiovascular, Skeletal, blood, lymphoid, Immunologic, Anti-inflammatory, immunosuppressive, side effects

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19
Q

The Synthetic analog of cortisol is?

A

Hydrocortisone

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20
Q

Corticosteroids can cause unpleasant side effects, such as an _________
appetite, ____ changes and difficulty ______.

A

increased, mood, sleeping

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21
Q

Common side effects of systemic steroids include:
* ________ appetite
* Weight ____
* Changes in ____
* Muscle ________
* ________ vision
* Increased growth of body ____
* Easy ________
* _______ resistance to infection

A

Increased, gain, mood, weakness, Blurred, hair, bruising, Lower

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22
Q

Prolonged use of Corticosteroids is associated with:
* Adrenal ______
* Osteo_______
* Immuno________
* _________

A

atrophy, porosis, supression, Euphoria

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23
Q

Inflammation is a ____-______ immune response (_____ immune system) to _______ and _____.

A

non-specific, innate, infection, injury

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24
Q

Inflammation is an _____________ response of tissues injury caused by _______ trauma, ______ chemicals or __________ agents

A

immunovascular, physical, noxious, microbiologic

25
Q

Inflammation is a _______, ______ response involving ______ cells, _____ vessels, and molecular ________.

A

normal, protective, immune, blood, mediators

26
Q

The function of inflammation is to eliminate the ______ course of cell injury, clear out ______ cells and _______ tissues, and initiate tissue ______.

A

initial, necrotic, damaged, repair

27
Q

Inflammation is mediated by release of ________ mediators from ______ tissues such
as?

A

chemical, injured, histamine, prostaglandins, bradykinins etc

28
Q

List some examples of Inflammatory Diseases in Dogs and Cats

A

Christine Sees Good Pins
▪ Chronic intestinal inflammation and intestinal disease in dogs (IBD, celiac in humans)
▪ Septic and nonseptic inflammatory diseases
▪ Gastric and peptic ulcer diseases
▪ Skin diseases
▪ Neoplastic diseases
▪ Inflammatory joint diseases
▪ Inflammatory oral diseases
▪ Primary inflammatory brain disorders

29
Q

List the classic signs of inflammation

A
  • Pain
  • Heat
  • Redness
  • Swelling
  • Loss of function
30
Q

Acute Inflammation
* ______ response of the body to harmful stimuli
* Increases movement of _____ and ______ from the blood into the injured tissues
* Biochemical events including the local ______ system, _____ system, and other cells

A

Initial, plasma, leukocytes, vascular, immune

31
Q

Chronic Inflammation
* ___________ inflammation
* Leads to a ________ shift in the type of cells at the site of inflammation, such as _______ cells
* Simultaneous ______ and _____ of the tissue from the inflammatory process

A

Prolonged, progressive, mononuclear, destruction, healing

32
Q

Chronic Inflammation can lead to?

A
  • Diabetes
  • Heart disease
  • Lung issues
  • Bone health
  • Cancer
  • Depression
  • Anger disorders and aggressive behavior
33
Q

Mechanism of inflammation represents a _____ of organized, dynamic responses including both _____ and _____ events with specific _______ secretions

A

chain, cellular, vascular, humoral

34
Q

The complex inflammatory response:
▪ Activation of ______________ (?) and release of __________ mediators of inflammation
▪** Arachidonic acid metabolism produces ?
▪ Vasoactive amines and peptides effect vascular _________
▪ _________ produce free radicals and other reactive
molecules
▪ Generation of ____-__________ cytokines

A

leukocytes (macrophages, neutrophils, lymphocytes), chemical, leukotrienes, thromboxanes, and prostaglandins, permeability, Neutrophils, pro-inflammatory

35
Q

Antipyresis = ?

A

reduction of fever

36
Q

Phopholipase A2 = important component of cell membranes. Releaed by phospholipids A2, whih is itself regualted by hormones and other stimuli such as trauma, (anything that causes inflammation). When inflammation hapens, A2 produces prostaglandins and A2 whihc collectively are called prostanoids. This process is medicated by COX enzymes COX 1 and 2. Corticosteroids which are steroids are coming from ?, have different MOA and alos inhibit prostaglandins, but mostly go through LOX pathway (lypooxygenase pathway). NSAIDs work on COX 1 and 2 inhibition whereas cortiocertoids works on LOX pathway. do prostaglandins as well, but mostly LOX pathway. Differneces dictate differences in NSAIDs.

A
37
Q

Same as previous slide. What to know:
NSAID inhibits arachinoid acid of prostaglandins? through COX 1 and 2.

A

Different prostaglandins, in all different tissues, and different receptors.

PGD2, PGE2, TxA2
Depends on cells present and site of inflammation (relisten to this part for location of each).
GPCRs mostly in contrast to GABA-A = ion channel receptor

38
Q

REgulate prostaglandins and TXA

A
39
Q

COX-1: ______= ______ level of activity
✓ ________ and ______ of ____ mucosa
✓ ______ homeostasis and platelet _______
✓ Maintenance of ?

Regulates expression of:?

A

Constitutive, Constant, Maintenance, protection, gastric, Vascular, aggregation, renal blood flow, PGs (PGE2), TXA

40
Q

COX-2: ______ = expressed at sites of ____
Prostaglandins : ?
COXs and Production of Prostaglandins

✓ Pain: ____-regulates sensitivity of __________ nociceptors
✓ __________: mediated by
✓ _______: pyrogens increase which happens mainly through ______
✓ ________: _____ is upregulated in various carcinomas

A

Inducible, injury, PGs (PGE2) TXA2, up, peripheral, Inflammation, Fever, PGE2, Cancer, COX2

PGD2; PGE2, PGF2α, PGI2
Bradykinin, PGE2, PGI2
PGE2

41
Q
  • COX-3 (AKA?): in the ______, regulates _____, discovered in ____
A

COX-1b, brain, fever, dogs

42
Q

5-LOX: ____-______________ _________

E.g.

A

pro-inflammatory leukotriens
LTB4

Called housekeeping enzyme?
COX2 is inducible at the sites of injury

43
Q

PGs control processes such as ?
PGs promote ?

A

inflammation, blood flow, the formation of blood clots

inflammation, pain, and fever

44
Q

Lipid compounds have diverse ________-like effects

A

hormone

45
Q

What is produced in almost every tissue in animals (lungs, GI, kidney, liver, blood vessels)?

A

Prostaglandins

46
Q

Different PGs have ______ effects in different tissues depending on the ______ of receptor they interact with.

A

various, type

47
Q

High concentrations of prostaglandins cause ______ by ______ action upon ______ endings

A

pain, direct, nerve

48
Q

COX2 is inducible

A
49
Q

Thromboxane A2 (TXA2) activation mediates several physiological and pathophysiological responses
▪ Platelet _______ and _____, ________ muscle contraction, and
activation of __________ ________ responses
▪ TXA2 is predominantly derived from ?

A

adhesion, aggregation, smooth, endothelial, inflammatory, platelet COX-1

50
Q

Potential benefits in inhibiting LOX pathway:
▪ Higher ?
▪ Greater _______ efficacy

A

GI safety, analgesic

51
Q

The Stunning Complexity of Prostanoids in Inflammation
▪ Different molecules have ____________ effects on both the _______ and __________ of inflammation
▪ The same product is formed by different enzymes –COX-1 and COX-2 – may either ______ or ______ inflammation
▪ Products of the _____ enzyme may promote or resolve inflammation in ______ models
▪ Different cell types that predominate at varying stages of disease progression generate _______ that have _______ effects on inflammation
▪ Individual prostanoids ________ considerably in their biological effects with other mediators

A

conflicting, promotion, resolution, promote, resolve same, different, prostanoids, contrasting, overlap

52
Q

Given this complexity, how we can develop drugs that are
reasonably well tolerated and reasonably effective?

A
53
Q

What are the three Main Functions of NSAIDs?

A

❖ Analgesia - reduction of perception of pain
❖ Antipyresis - reduction in fever
❖ Anti-inflammation – reduction of inflammation

54
Q

Non-Steroidal Anti-Inflammatory Drugs (“______” analgesics)

Uses:
▪ _______________
▪ ___________ arthritis (AKA?)
▪ ______________
▪ _______ pain
▪ ____ inflammation

Adverse Effects:
▪ Increase risk of ___ complications
▪ Deteriorate __________

A

weak, Osteoarthritis, Rheumatoid, Ankylosing spondylitis, Pancreatitis, Dental, Skin, GI, osteoarthritis

55
Q

True or False: There are more NSAIDs available for dogs than there are for cats?

A

True.

56
Q

No NSAIDs are approved for long-term in ______.

A

cats

57
Q

NSAID Overdose in cats can lead to:
▪ Stomach ______ with bleeding into the _____ tract
▪ Kidney _____ and _______
▪ _____ problems
▪ _____ damage

A

ulcers, GI, damage, failure, Liver, Brain

58
Q

There are 2 FDA-approved NDAIDS for short-term use in cats:

A

Robenacoxib
Meloxicam

59
Q

NSAIDs: PK properties
▪ Well ___________, and _____ does not substantially change their bioavailability
▪ Circulating NSADs are bound by ______ which ________ volume of distribution
▪ Displacement from albumin due to _________ by other drugs for the albumin binding sites or ___________ can lead to _____ levels of unbound drug, which can predispose the patient to drug-induced adverse effects on the _____-term basis
▪ Highly metabolized in the ____
▪ _____/______ elimination
▪ Very little PK information is available in ____. Since cats have inefficient
_______________ _____ and __________ conjugation system; the extrapolation of dosages from other species needs to be carefully considered
▪ ______ and ____ patients may require smaller doses of NSAIDs due to weak ____ and _____ status, which may result in _____ elimination rates

A

absorbed, food, albumin, decreases, competition, hypoalbuminemia, higher, short, liver, Urine/feces, cats, cytochrome P450, glucuronidation, Young, old, liver, kidney, lower

Intro to Pharmacology (31 decks)

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