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FMS Week 10 > Pharmacotherapy of inflammation > Flashcards

Pharmacotherapy of inflammation Flashcards

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1
Q

H3 v(down arrow) cAMP

A

presynaptic autoreceptors

brain

myenteric plexus

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2
Q

Cox 1 vs 2

A
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3
Q

HPA axis and cortisol

A
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4
Q

Abatacept mechanism of action

A

blocking the costimulatory signal required for T cell activation

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5
Q
A

NSAID use

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6
Q

NSAID toxicities

A
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7
Q

What organ systems affected by histamine receptors

A

Cardiovascualr

pulmonary

nervous system

GI

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8
Q

Cox 2 derived PGs are involved in renal function; inhibition of COX-2…

A

reduced water and salt excretion byt the kidney, leading to peripheral edema, HTN, and exacerbation of pre-existing HTN

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9
Q

Rituxumab

A

inhibitor of B cell function

approved for pts that fail to respond to anti-TNF-a therapy

Approved for tx of nonhodgekins lymphoma

chimeric mab against CD20 antigen found on the surface of normal and malignant B lymphocytes. IgG1 and k immunoglobulin

2-1000mg IV infusions separated by 2 weeks

admin of glucocorticoid recommended prior to infusion to reduce incedence severity of infusion reaction

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10
Q

NSAID USE AND GI COMPLICATIONS

A

incidence of dyspepsia id >40% often amenable to tx with H2 receptor antagonist or a PPI

incedence of complicated or symptomatic ulcer is 2-5%. may be life treatening

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11
Q

How is the GI system affected by histamine receptors

A

increawse in acid secretion H2

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12
Q

PGE2

A

involved in all processes leading to the classical signs of inflammation: redness, swelling, and pain

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13
Q
A

glucocorticoid effects on the immune cells

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14
Q

ASA has been found to lower rates of what CA

A

colorectal cancer

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15
Q

NSAID side effects

asprin allergy

A

angioedema

anaphylazis

resp symptoms

skin rxns

increased leukotrienes

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16
Q

Abatacept

A

inhibitor of t cell activation

fusion protein of the extracellular domain of the CTLA4 molecule and the Fc doman of human IgG1

approved for pts who do not respond well to methotrexate and for pts who do not respond or cannot tolerate TNA antagonists

30 minute infusion given at 2 and 4 weeks after 1st infusion, every 4 weeks thereafter. Fixed dose. 10mg/kg

MOA: blocing the costimulatory molecule required for T cell activation B7 (CD80/86)

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17
Q

PGF2-alpha

A

high levels have been reported in patients suffereing from RA, OA,reactive arthritis, and psoriatic arthritis

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18
Q

PGI2

A

is rapidly produced following tissue injury and is an important mediator the the edema and pain associated with acute inflammation. It is the most abundant prostanoid in synovial fluid in human arthritic knee joints

AKA prostacycline

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19
Q

Autoimmune diseases being successfully treated with anti-TNA therapy

A

RA

crohns

ankylosing spondylitis

juvenile RA

psoriac arthritis

psoriasis

sarcoidosis

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20
Q

PGD2

A

produced by antigen presenting DCs and TH2 cells, suggesting a role in antigen-specific immune system responses

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21
Q

H2 (histamine receptor 2)

^ cAMP

A

gastric mucosa

blood vessels/ smooth muscle cells

mast cells

cardiac muscle cells

brain

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22
Q

H4 v(down arrow) cAMP

A

Eosinophils

Neutrophils

CD4 T cells

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23
Q

NSAID side effects

Reye’s syndome

A

varicella infection of influenza virus

liver damage and encephalopathy

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24
Q

Fexofenadine (allegra)

A

2nd/3rd generation H1 receptor competative antagonist

long duration (12-24 hours)

Little to no anticholinergic, and alpha-adrenergic, and anti-serotonergic actions

less sedation than 1st generation H1 blackers

not useful for N or motion sickeness

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25
Zafirlukast and Montelukast
Leukotriene pathway inhibitor LTD4 receptor antagonist inhibits CYP3A4 and CYP2C9 -\> increased warfarin t1/2 orally active for mild to moderate asthma considered an alternative to low dose inhaled corticosteroid
26
Cortisol
Cortisol is the primary glucocorticoid in hiumans glucocorticoids exert a wide range of physioklogic effects, including regulation of immune fn, growth, and carbohydrate, fat, and protein metabolism cortisol is synthesized from cholesterol the secretion of cortisol follows a circadian rhythm ans is controlled by pulses of ACTH tht peak in the early morning and after meals
27
Chronic NSAID use linked to an increased risk of...
MI
28
Histidine ------\> histamine enzynme
histidine decarboxylase
29
Factors to conside (preexisting) when giving NSAIDs
stomach ulcer or bleeding heart dz, inclduding MI or stroke kidney dz/ HTN co-administered meds/ supplements
30
chronic use of glucocorticoids is associated with...
high risk for adverse affects
31
Leukotriene pathways of arachadonic acid breakdown
32
Arachadonic acid and COX pathway
33
How is the nervous system affected by histamine receptors
stimulant of nerve endings H1
34
Laratadine (claratin)
2nd/3rd generation H1 receptor competative antagonist long duration (12-24 hours) Little to no anticholinergic, and alpha-adrenergic, and anti-serotonergic actions less sedation than 1st generation H1 blackers not useful for N or motion sickeness
35
Prednisone
glucocorticoid short to medium acting antiinflammatory 4x as much as cortisol has high affinity for CBG and albumin 70-80 % protein bound
36
3 cell types affected by intradermal weal and flare response
1) dilation of vasculature in the microcirculation causing reddening 2) increased permeability pf capillary of venular endothelium causes edematous wheal (a smooth, slightly elevated patch) 3) stimulation of sensory nerve endings causes a red, irregular flare surrounding the wheal; may be accompanied by itching sensation
37
Apremilast
PDE-4 inhibitor indicated for moderate to severe plaque psoriasis increases intracellular cAMP, decreased TNAa production Most common adverse affect N and D in first year of tx, nasopharyngitis, URI Metabolized by CYP3A4 with subsequent glucuronidation and non-CYP mediated hydrolysis excretion: 58% urine, 39% feces, severe renal impairment associated with increased risk depression
38
Side effects of high dose or prolonged glucocorticoid therapy
39
Mechanism of histamine induced edema
contraction of endothelial cells happens along vasculature
40
Classic mechanism of glucocorticoid action
you have your glucocorticoid comes and binds to receptor which has a head shock protein component that dissociates GR and GCS go to nucleaus and upregulate and downregulate certain genes
41
Untoward effects of anti TNA therapy
TNFa is an important component of stress responses TNA a is important for host defense mechanisms pts on anti TNF therapy display increased incidence of infection, lupus, exacerbatiob of dymyelinating dz, and heart failure may or may not be associated with increased risk of lymphoma
42
H1 (histamine receptor 1) ^ IP3/DAG
blood vessels endothelial cells sensory nerve endings GI smooth muscle cells broncial smooth muscle brain MAIN one that the drugs target. Think of inflammation when you think of this
43
How is the pulmonary system affected by histamine receptors
bronchoconstriction H1
44
How is the cardiovascular system affected by histamine receptors
vasodilation of arterioles and precapillary sphincters via H1 (some H2) Increase vascular permeability H1 (hives) also edema Increase heart rate (direct effect and reflex tachycardia)
45
46
Cetrizine (zyrtec)
2nd/3rd generation H1 receptor competative antagonist long duration (12-24 hours) Little to no anticholinergic, and alpha-adrenergic, and anti-serotonergic actions less sedation than 1st generation H1 blackers not useful for N or motion sickeness
47
Mechanism of histamine induced vasofilaiton
GC is guanylyl cyclase influx of calcium happens
48
Tofacitinib
JAK inhibitor Blocks JAK 1 and 3 and to a lesser degree 2 approved for moderate to severe RA for pts that do not respond well to methotrexate Side effects: inflammation of nasal passages and upper pharynx, URI, Increased risk TB and lymphoma, HA Metabolized by CYP3A4
49
diphenhydramine
## Footnote 1st generation H1 receptor competative antagonist short duration (3-6 hours) anticholinergic anti a-adrenergic, anti serotonergic effeccts (penetration into CNS) cause sedation antiemetic, anti motion sickness
50
Asprin (Acetylsalicylic acid)
weak acid analgesic (anti pain) Antipyretic anti-platelet anti inflammatory rapidly absorbed from the stomach and intestine in unionized form due to it being acidic IRRIVERSIBLY inhibits prostaglandin biosynthesis by ACETYLATING the enxyme CYCLOOXYGENASE (COX)
51
How does ASA irriversibly inhibit prostaglandin biosynthesis
Acytelating COX
52
chloropheniramine
1st generation H1 receptor competative antagonist short duration (3-6 hours) anticholinergic anti a-adrenergic, anti serotonergic effeccts (penetration into CNS) cause sedation antiemetic, anti motion sickness
53
Retuximan MOA
54
Histamine storage sites
blood basophils and tissue mast cells gastric mucosal cells neurotransmitter vessicles
55
Nabumetone
NSAID Shows some selectivity for COX2 (in vitro)
56
Indomethacin
NSAID associated with increase risk of CV event (mostly MI) side effects : hypersensativity, GI, slight renal toxicity depression. HA- similar to seratonin in structure
57
Tofacitinib MOA
Jak inhibitor ultimately blocks transcription
58
Anakinra
cytokine blocker inhibitor of IL-1 recombinant, nonglycosylated synthetic form of the human IL-1 receptor antagonist (IL-1Ra), an endogenous regularot of IL 1 action
59
Celecoxib
Cox 2 selective inhibitor has not been shown to be any better than NSAIDS for upper GI (stomach) complications but has been shown to be associated with a significantly reddulced incidence of small bowel inflammatino and mucosal breaks than NSAIDS It is a sulfonamide t1/2 6-12 hours Metabolized by CYP2c9 Inhibits CYP26( metabolism of metoprolol, SSRI, tricyclic antidepressants) Significan 1st pass metabolism RA and OA but not general pain
60
Acetaminophen
weak base analgesic and antipyretic NOT ANTI INFLAMMATORY No anti platelet effefcts Severe HEPATOTOXICITY with oversidage caused by reactive quinone metabolites. Normally these metabolites are rapidly inactivated by conjugation with glutathione. With high toic levels of the drug, hepatic glutathione becomes depleted. The drug N-acetylcysteine is used to prevent hepatotoxicity
61
Uses of H2 receptor antagonists
(H2 in the gut) May be useful for reducing NSAID induced dyspepsia Gastric and pepti ulcers ( most peptic ulcers due to h pylori. NSAID induced are usually gastric) there is no evidence that H2 antagonists prevent drug induced ulcers and their complications esophageal reflux few side effects infrequent GI irritation cimetidine is a potent inhibitor of P450 metabolism
62
Use of COX-2 inhibitors in pts with ASA induced asthma
5-20% of pts with chron asthma are hypersensative to ASA. Likely due to cox 1 inhibition, leading to lipoxygenase pathway activation and production of cysteinyl leukotrienes -\> bronchospasm and nasal obstruction Some ppl have been ok with COX2 inhibitors but there is still a warning label on med
63
Infliximab
cytokine blocker inhibitor of TNF-a chimeric mAb (human contant, mouse variable) given IV increased risk for TB
64
Functions of histamine
mediator of immediate allergic and inflammatory reactions role in gastric acid secretion neurotransmitter and neuromodulator chemotactic factor for neutrophils, eosinophils, basophils, monocytes, and lymphocytes
65
Zileuton
Leukotriene pathway inhibitor Inhibits 5-lipoxygenase inhibits CYP3A4 can influence metabolism of terfenadine, warfarin, and theophulline orally active for mild to moderate asthma considered an alternative to low dose inhaled corticosteroid
66
2 areas of inhibition for leukotriene pathway of arachadonic acid
67
NSAID side effects Inhibition of COX-1
stomach irritation prolonged bleed time renal toxicity CNS effects
68
entanercept
cytokine blocker inhibitor of TNF-a Human TNF receptor linked to the Fc portion of human IgG1 Basically sponge for TNF-a. Like a decoy recep. Given 2x/ week

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