Final Version Flashcards

1
Q

MOA: inhibits phospholipase A2 and COX2 and works on concentration, distribution and function of peripheral leukocyte and macrophages?

A

Prednisone

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2
Q

What category does prednisone being in?

A

Corticosteroids

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3
Q

Other corticosteroids that work like prednisone

A

Methylprednisolone and dexamethasone

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4
Q

MOA: alkylating agent and signal 3 inhibitor
Non cell cycle specific
Inhibits b and T cells

A

Cyclophosphamide

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5
Q

MOA:
Antimetabolite and signal 3 inhibitor
Cell cycle specific
Inhibits T cells more than B cells

A

Azathiorpine

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6
Q
MOA: 
Antimetabolite and signal 3 inhibitor 
Cell cycle specific 
Inhibits B and T cells 
Used for Crohn's disease
A

Methotrexate

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7
Q

Mao: inhibits the synthesis of purines and signal 3 inhibitor.
Inhibits B and T cells

A

Mycophenolate

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8
Q

MOA:
Calcineurin phosphatase and signal 1 inhibition
T cell suppression

A

Cyclosporine

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9
Q

MOA:
CD3 receptor and signal 1 inhibition
T cell suppression

A

Muromonab-CD3

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10
Q

MOA:

T cell suppression

A

Lymphocyte immune globulin

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11
Q

Murine immunoglobulin

A

Muromonab-CD3

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12
Q

Horse immune globulin

A

Lymphocyte immune globulin.

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13
Q

Human IgG1 monoclonal antibody

A

Daclizumab

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14
Q

IL-2 receptor and signal inhibition

A

Daclizumab

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15
Q

Human immune globulin that helps passive immunity increase and helps prevent certain infection diseases in susceptible individuals

A

Gammagard

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16
Q

Suppresses immune response of Rh-negative individuals to Rh-positive blood cells

A

Rh0Gam

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17
Q

Antiviral and immunoregulatory activity but is not completely understood

A

Interferon beta

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18
Q

MOA:

Has phagocyte activating effects and antibody dependent cellular toxicity

A

Interferon gamma

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19
Q

Types of cytotoxic and proliferative agents

A

Cyclophosphamide, azathiorpine, methotrexate, mycophenolate

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20
Q

Category of T cell suppressants and other antibody immunosuppressive

A
Cyclosporine, micromanab-CD3, lymphocyte immune globulin, Daclizumab, Rh0
Immune globulin (Rh0Gam), immune globulin (gammagard)
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21
Q

Immunomodulators and immunostimulants

A

Interferon bets and interferon gamma

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22
Q

Used for relapsing/remitting multiple sclerosis

A

Interferon beta

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23
Q

Used for chronic granulomatoses disease and osteoporosis

A

Interferon gamma

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24
Q

ADRs:
nephrotoxicitt
hypertension
embryotoxic

A

cyclosporine

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25
ADRs: fever and chills sensitivity for Murine products
Muromonab-CD3
26
used for hemolytic disease of the newborn
Rh0Gam
27
used for hypogammaglobulinemia and to prevent infections in HIV patientes
imuune globulin (Gammagard)
28
used for renal, liver, and heart trasnplant rejections and may be used with corticosteroids and azathiorpine used for rheumatoid arthritis
cyclosporine
29
used for renal, liver, pancreas, an heart trasnplant rejection
muromonab-CD3
30
used for renal trasnplant rejection
lymphocyte immune globulin and daclizumab
31
used for rheumatoid arthritis, leukemias, and other tumors
cyclophosphamide
32
used for renal allotransplantation and rhumatoid arthrits in adults only
azathiorpine
33
used for Crohn's disease, rheumatoid arthritis, leukemias and other tremors
methotrexate
34
used for renal, liver, and heart transplant rejections. used with cyclosporine and other corticosteroids
mycophenolate
35
used for allergic disorders, hematalogic disorders, hepatic and renal disease, and collagen disorders
corticosteroids
36
``` ADR: no serious effects for short period long period: latogenic cushing's syndrome osteoporosis, infections, and ulcers ```
corticosteroids
37
ADR: N/V/D bone marrow suppression aspermia
cyclophosphamide
38
ADR: N/V bone marrow suppression infections
azathiorpine
39
ADR: N/V bone marrow suppression Hepatotoxicity
methotrexate
40
ADR: GI neutropenia infections
mycophenolate
41
ADR: fever and chills | sensitivity for equine products
lymphocyte immune globulin
42
ADR: | GI disorders
daclizumab
43
ADR: mild side effects contraindicated in Rh+ patients
Rh0 immune globulin (Rh0Gam)
44
ADR: | mild side effects
Immune Globulin (Gammagard)
45
``` ADR: flu-like symptoms depression suicidal ideation injection site reactions ```
interferon beta
46
ADR: | flu-like symptoms
Interferon Gamma
47
why can some immunosuppressives go in and activate the immune system?
drug allergy and drug hypersensitivity
48
what are the types of drug allergy/hypersensitivity?
``` anaphylaxis serum sickness drug fever vasculitis drug induced lupus ```
49
what factors affects the incidence of allergic reactions?
``` age and gender genetic factors associated illness (AIDS) previous drug administration drug-related factors ```
50
Anaphylactic (immediate response drug allergy)
Type 1
51
serum sickness or Arthus reaction drug allergy
Type 3
52
cytotoxic reaction
Type 2
53
in this type of reaction, the initial exposure to drugs makes IgE antibodies and IgE gets fixed to tissue mast cells and blood basophils. when re-exposed, mast cells and basophils release histamine, leukotrienes, and other mediators
Type 1/ anaphylactic (immediate response reaction)
54
this type of drug allergy requires IgG and IgM antibodies that activate complement cascade antibodies to tissue constituents or drug can be demonstrated
type 2 or cytotoxic reactions
55
The antagonists for this type of allergic reactions are prednisone, isoproterenol, epinephrine, and thephylline and even though desensitization can be tried, it may be hazardous
Type 1 or anaphylactic reaction
56
this type of drug allergy is most common and manifestations occur 7-21 days after exposure of drug through fever, urticaria, arthralgia, and lymphadenopathy but go away when drug is stopped. corticosteroids can be used to help
type 3 or serum sickness
57
this type of drug reaction involves IgM and IgG but NOT IgE. | these generate drug-antibody complexest that deposit in the blood vessels after activating complement
type 3 or serum sickness
58
type of drug reaction that mainly targets cells in the circulatory system. the reaction may disappear after stopping the drug for several months and corticosteroids may suppress severe reactions
type 2 or cytotoxic
59
in this type of drug reaction, vascular permeability increases and neutrophils after aggregating and invading the cell wall, induce a hemorrhagic vasculitic lesion
serum sickness
60
this type of drug reaction is mediated by sensitized T lymphocytes and macrophages and cause contact dermatitis. can be helped with corticosteroids
Type 4 or cell-mediated (delayed) hypersensitivity reaction
61
MOA: irreversible inhibition of COX-1 and COX-2 inhibits prostaglandin synthesis but not lipoxygenase
Aspirin
62
MOA: | reversible inhibition of COX-1 and COX-2
diflusinal, indomethacin, sulindac, diclofenac, tolemetin, ketorolac, naproxen, ibuprofen, ketoprofen, fenoprofen, flurbiprofen, oxaprozin, piroxicam, meloxicam, meclofenamate, mefenamic, nabumetone, etodolac, meloxicam and salicylate salts (basically all drugs but aspirin)
63
MOA: same as the other drugs but just have MORE COX-2 selectivity than COX-1
Etodolac, Nabumetone and Meloxicm
64
this drug is not a true salicylate
diflusinal
65
This drug is only taken once daily
oxaprozin
66
this drugs is activated by the liver
nabumetone
67
MOA: | only inhibits COX-2
celecoxib
68
MOA: analgesia by elevating pain threshold by weakly inhibiting COX-1, COX-2 and COX-3 antipyresis by acting on hypothalamic heat-regulating centers
acetaminophen
69
``` Use: analgesic antipyretic antiinflammatory antirheumatic (suppresses antigen-antibody reactions and prostaglandin mediated autoantibodies) ```
aspirin and salicylate salts
70
use: analgesic antiinflammatory weak antipyretic (recommended not to be used as one)
diflusinal
71
use: rheumatoid arthritis NOT for juvenile RA osteoarthrits tocolytic agent (suppress premature labor)
indomethacin
72
use: | rheumatoid arthritis and osteoarthrits
sulindac
73
use: rheumatoid arthritis osteoartritis post-op analgesia
etodolac
74
use: rheumatoid arthritis osteoarthritis analgesia/dysmenorrhea
diclofenac, ibuprofen, keoprofen and meclofenamate
75
use: rheumatoid arthritis Juvenile arthritis osteoartritis
tolmetin
76
use: | moderate to severe acute pain
ketorolac (toradol)
77
``` use: rheumatoid arthritis Juvenile RA osteoarthritis analgesia dymenorrhea ```
naproxen
78
use: rheumatoid arthritis osteoarthritis analgesia
fenoprofen
79
use: rheumatoid arthritis osteoarthritis
flurbiprofen, oxaprozin, piroxicam and nabumetone
80
Use: | osteoarthritis
meloxicam
81
use: analgesia and dysmenorrea NOT for RA or osteoarthritis
mefenamic acid
82
``` use: osteoarthritis RA dymenorrhea acute pain familial adenomatous polyposis ```
celecoxib
83
use: antipyretic and analgesic osteoarthrits (relief of pain)
acetaminophen
84
ADR: Minor (rash) rare potential hepatotoxicity and nephrotoxicity
acetaminophen
85
ADR: | minor disturbances for GI, CNS, respiratory rash and sulfonamide allergy
celecoxib
86
ADR: GI CNS: headaches
nabumetone | ketorolac
87
ADR: contraindicated for GI inflammation pre-existing renal problems autoimmune and hemolytic anemia
mefenamic acid
88
ADR: GI CNS: headaches rahs/dermatitis
meclofenamate
89
ADR: | GI
meloxicam piroxicam oxaprozin
90
ADR: GI CNS: dizziness and headache
flurbiprofen | diclofenac
91
ADR: GI: 30% of patients CNS: headache
ketoprofen
92
``` ADR: GI pre-existing renal hypersensitivity CNS: headache ```
fenoprofen
93
ADR: GI < indomethacin CNS < indomethacin hypersensitivit
naproxen
94
``` ADR: GI less than aspirin or indomethacin ocular disturbances hypersensitivity (rash/dermatitis) chronic use inhibits renal prostaglandin production ```
ibuprofen
95
this drug should be avoided during pregnancy or breast-feeding
ibuprofen
96
ADR: GI CNS: headache causes Anaphylactoid reactions (caution!!)
tolmetin
97
ADR: GI: less severe than indomethacin
etodolac
98
``` ADR: GI: less severe than indomethacin rash/dermatitis potential fatality pancreatitis ```
sulindac
99
``` ADR: GI: severe prolonged gestation renal CNS: headache and aggravate depression ```
indomethacin
100
``` ADR: GI: mild headache renal hypersensitivity ```
diflusinal
101
ADR: GI: not too bad no effect on platelets hypermagnesemia
salicylates
102
``` ADR: GI hepatic hypersensitivity reyes syndrome salicylism ```
Aspirin
103
category: | salicylic acid derivatives
aspirin salicylate salts diflusinal
104
category: | acetic acid derivatives
``` indomethacin etodolac diclofenac tolmetin ketorolac sulindac ```
105
category: | propionic acid derivatives
``` ibuprofen naproxen ketoprofen oxaprozin fenoprofen flurbiprofen ```
106
category: | enolic acid derivatives
piroxicam | meloxicam
107
category: | anthranilic acid derivatives
meclofenamate | mefenamic acid
108
category: | alkanones
nabumetone
109
this drug may prolong bleeding time because irreversible acetylation and inactivation of cyclooxygenase in platelets and megakaryocytes. the platelets cyclooxyenase is not resynthesized
aspirin
110
this drug is highly protein bound, ready crosses placental and BBB and is distributed in all tissues of the body
aspirin
111
this drug causes gastric mucosal damage, reactive latent gastric and duodenal ulcers and should be used in caution with patients that have active GI lesions
aspirin
112
this drug should not be taken with alcohol because in increases GI bleeding
aspirin
113
this drug has antiulcer effects and is a prostaglandin analogue
Misoprostol
114
hepatotoxicity occurs after 1-4 weeks when blood levels reach 200-250 micrgrams/mL hepatic function MUST be monitored in these patients
aspirin/salicylates
115
rarely any renal problems but in overdose situations, may cause acute tubular necrosis and a reduced renal clearance still should be very carefully monitored in patients that have renal problems
aspirin/salicylates
116
in patients with congestive heart failure, this drug should be avoided
highly buffered aspirin with high sodium content
117
this drug should be discontinued 5-7 days before surgery and is contraindicated in patients with bleeding problems
aspirin.salicylates
118
what is the aspirin triad?
asthma and nasal polyps because off aspirin sensitivity
119
true or false | salicylates should not be used in children/teenagers with varicella or influenza
true because it increases the chance of getting Reye's syndrome
120
can salicylates be used in pregnancy?
has shown to have teratogenic and embryocidal effects in animals and may lead to maternal and fetal hemorrhagic complications
121
what is salicylism?
chronic salicylate intoxication from prolonged therapy with high doses
122
what is acute salicylate
overdosage from a single toxic dose of salicylate
123
what symptoms does salicylism present with?
tinnitus and hearing loss in adults hyperventilation and CNS effects in children metabolic acidosis and respiratory alkalosis
124
what is a salicylate jag?
when there is an increase in CNS stimulation becaue of salicylate intoxication and then is later replaced by CNS depression
125
how do you know if there is a salicylate overdose?
acid base disorders dehydration hyperpyrexia hyperglycemia/hypoglycemia
126
drug interactions to salicylates
protein-bound drugs since salicylates are highly protein bound anticoagulants thrombolytic agents uricosuric agents antidiabetic agents (enhanced effect) corticosteroids (increase renal clearance of salicylates) alcohol (GI bleeding and ulcers/erosions) NSAIDs (GI effects are increased)
127
these drugs inhibit lipoxygenase pathway and inhibit lysosomal enzyme release and inhibit neutrophil activation reduces prostaglandins and thomboxane B2
NSAIDs
128
which NSAIDs do not treat RA?
ketorolac, meloxicam, ad mefenamic acid
129
which NSAIDs do not treat osteoarthritis?
ketorolac and mefenamic acid
130
which NSAIDs treat juvenile RA?
tolmetin and naproxen
131
which NSAIDs should not be used in children under 14?
indmethacin mefenamic acid meclofenamate
132
what are the major GI problems with the use of chronic NSAIDs?
ilcers (gastric, duodenal, intestinal, and gingival)
133
which NSAID causes autoimmune hemolytic anemia?
tolmetin
134
how are NSAIDs excreted?
renally and that's why renal should be monitored
135
renal problems associated with NSAIDs
interstitial nephritis (inhibition of prostaglandin) hyperkalemia hypernatremia papillary necrosis
136
contraindications for celecoxib
patients that are allergic to celecoxib patients that are allergic to sulfonamides patients that have asthma, urticaria, or allergic reactions to aspirin or NSAIDs
137
this drug is toxic to both the liver and the kidney
acetaminophen
138
how to relieve acetaminophen toxicity
gastric lavage and mucomyst (protects liver by restoring glutathione levels)
139
how do you inhibit the release reaction (degranulation)
cromolyn sodium agents that increase cyclic AMP and stabilize mast cells (not primary effect) corticosteroids
140
this drug inhitbits the lipoxygenase enzyme and decreases the formation of leukotrienes
zileuton
141
these drugs block leukotriene receptors
zafirlukast and monteleukast
142
hwo do you block receptors for autocoid or broncoconstrictors?
H1 antihistamines anticholinergic (ipratropium and tiotropium) autocoid antagonist like the antagonists for leukotrienes
143
how do you dilate the bronchioles?
physiologic antagonists like beta adrenergic agonists (epinephrine, isoproterenol, terbutaline, salmeterol) methylxantines (theophylline and aminophylline)
144
how do you prevent inflammation and cell-mediated immunologic reactions?
corticosteroids and immunosuppressives
145
how do you neutralize IgE?
olizumab...monoclonal antibody | given parenterally and allergic reactions are common
146
overview approaches to treat hypersensitivity, anaphylaxis, and asthma
inhibit release reaction inhibit formation of generated autocoids block receptors for autocoids or bronchoconstrictors bronchodilate through physiologic antagonists prevent inflammation and cell-mediated immunologic reactions neutralize IgE
147
what are autocoids?
ex: kinins, leukotrienes, superoxides, platelet activating factor
148
this drug is mainly used for the prophylactic treatment of bronchial asthma not effective in acute attacks
cromolyn sodium
149
how does cromolyn sodium work?
inhibit release of histamine and other autocoids from sensitized mast cells
150
what are cromolyn and similar drugs most useful for and how are they used?
treat extrinsic asthma that's caused by specific allergens | used in conjunction with other therapy like bronchodilators
151
what can cromolyn sodium be used for?
allergic rhinits allergic conjuntivitis GI allergies
152
what are H1 antagonists used for?
``` allergic rhinitis allergic dermatitis (urticaria) ```
153
these drugs are not effective in treating bronchospastic conditions like asthma and anaphylaxis
H1 antihistamines
154
these drugs inhibit bronchospasms induced by acetylcholine and nothing else so limited effectiveness dries secretions so not well liked
anticholinergic agents | ipratropium, atrovent, tiotropium, spiriva
155
____ is a quaternay ammonium so not well absorbed (limited effect)
ipratropium
156
these drugs act bronchodilators and inhibit release of autocoids from mast cells fairly effective in treating acute asthma attacks
Beta adrenergic agonists
157
______ and otehr adrenergic bronchodilators are drugs of choice in treating life-threatening anaphylactic reactions
epinephrine
158
true or false | tolerance can occur and rebound bronchoconstriction is possible with beta agonists
true
159
these drugs cause bronchodilation and inhibit release of mediators from mast cells
methylxanthines (theophylline and aminophylline)
160
MOA: | inhibits phosphodiesterase --> increased cAMP
methylxanthines
161
type of methylxanthine that is taken orally with other agents for severe asthma
theophylline
162
type of methyxanthine that is given IV that is given for severe asthma
aminophylline
163
what do we have to watch out for with methyxanthines?
they have a narrow therapeutic window and so monitor blood levels carefully
164
ADRs: N/V headache, insomnia, nervousness in severe toxicity cardiac arrythmias and seizures
methyxanthines
165
these drugs have anti-inflammatory activity and they inhibit recruitment of leukotrienes and other autocoids like prstaglandins
corticosteroids
166
very effective as prophylactic agents but not as effective in acute attacks because they reduce the severity of cell mediated immunological damage
corticosteroids
167
``` ADRS: cataracts (from inhaled) cushings syndrome immune system suppression osteoporosis peptic ulceration suppression of growth in children (systemic) menstrual and reproductive problems ```
corticosteroids
168
these agents interfere with production/actions of leukotrienes and help treat asthma
leukotriene modulators
169
cysteinyl leukotriene receptor antagonist not for acute attacks less effective than corticosteroids
zafirelukast and montelukast
170
5-lipoxygenase inhibitor reduces frequency of attacks elevates liver enzymes and hepatotoxicity
zileuton
171
drug of choice for treatment of mild allergies
H1 antihistamines but mast cell stabilizers or corticosteroids may be used in severe allergies
172
_____ are commonly used to treat COPD
anticholinergics: tiotropium (spiriva) aclidinum (tudorza)
173
category: | adrenergic bronchodilators
``` epinephrine isoproterenol metaproterenol albuterol levalbuterol salmeterol terbutaline pirabuterol ```
174
category: | methylxanthine bronchodilators
theophylline and aminophylline
175
category: | corticosteroids
``` beclomethasone flunisolide triamcinolone fluticasone budesonide prednisone mometasone ciclesonide methylprednisolone ```
176
category: | mast cell stabilizers
cromolyn sodium
177
category: | leukotriene modulators
monteleukast zafirleukast zileuton
178
category: | antimuscarinic
ipratropium tiotropium aclidinum (COPD)
179
catergory: | combination products for asthma
advair diskus combivent symbicort duera
180
category: | anti IgE
omaizumab
181
category: | H1 histamine antagonist
diphenhydramine fexofenadine cetirizine loratadine
182
short-acting glucocorticoids
hydrocortisone
183
long-acting glucocorticoid
dexamethasone
184
intermediate acting glucocorticoid
prednisone and triamcinolone
185
short acting mineralocorticoid
fludricortisone and spironolactone
186
this corticoid stimulate the adrenal cortex and secretion of glucocorticoids, andronergic substance and aldosterone
cosyntropin
187
3 zones in the adrenal cortex
zona glomerulosa zona fasiculata zona reticularis
188
what hormone is secreted from zona glomerulosa?
mineralocorticoids (aldosterone)
189
what hormone is secreted from zona fasiculata?
glucocorticoids (cortisol)
190
what hormone is secreted from zona reticularis?
androgens, progesterones, and estrogens
191
what components are involved in the biosynthesis of cortisol and other hormones?
ACTH and MC2R and several cytochrome P450 enzyme | cholesterol
192
what are the 2 types of negative feedback systems to control ACTH secretion of glucocorticoids
fast feedback system | delayed feedback system (suppresses basal CRH and ACTH)
193
how do mineralocoticoids regulate secretion?
aldoseterone works with the renin system no significant feedback on ACTH serum concentrations peak in the morning
194
how doe glucocorticoids and mineralocorticoids affect carbohydrate, protein, and fat metabolism? ____ glucose production and insulin release _____ hepatic gluconeogenesis ______ peripheral glucose utilization (insulin resistance in muscle cells) _____proteolysis and amino acids ______fatty acid mobilization, lipolysis, and ____ release of fatty acids and glycerol all this is done to maintain an adequate supply of glucose to _____
``` increase stimulates decrease increase enhance increases ``` brain
195
how do mineralocorticoids keep water and electrolyte balance?
through control of renal excretion ions | they promote reabsorption of small amounts of sodium but excrete potassium and hydrogen ions
196
glucocorticoids regulate blood cells and cardiovasuclar by: _____ vasoconstriction on small vessels ______ capillary permeability by _____histamine release by basophils and mast cells ____ plasma hemoglobin concentration, ____ erythrocytes and neutrophils in blood and ______wthite blood cell count _____number of eosinophils, basophils, monocytes, and lymphocytes
``` potentiate decrease reducing increase increase decrease ```
197
mineralocorticoids regulate blood cells and cardiovascular by:
retaining sodium and maintaining normal blood volume
198
glucocorticoids maintains the immune system by:
inhibiting prostaglading and leukotrienes by inducing production of lipocortins that inhibit phospholipase A2 reduce inflammation suppress cytokines and chemokines
199
role of corticoids in CNS
influence mood, sleep patterns and EEG
200
mood changes (irrtability and depression) are associated with what?
adrenal insufficiency
201
corticoids are needed for skeletal muscle...but what happens when there is a large amount present?
stimulate proteolysis in myocytes causing pain and muscle weakness
202
secretion of which corticoid is increased with stress?
cortisol | has protective effect
203
what are the non-endocrine uses for glucocorticoids?
inflammatory allergic immunological disorders
204
what kind of doses do you need to use for chronic diseases such as chronic asthma
need suppressive doses and a therapuetic regimen after careful consideration
205
what allergic disorders are corticoids used for?
``` seasonal allergies (systemic) mild-moderate asthma (inhaled steroids) ```
206
what type of cerebral edema are treated with glucocorticoids?
vasogenic type edema (brain tumors) | brain abcesses...closed head injury so less responsive
207
corticoid treatments for allergic disorders
prednisone methylprednisolone triamcinolone dexamethasone
208
corticoid treatments for cerebral edema
prednisone
209
how is bacterial meningitis treated with corticoids
anti-inflammatory effects of glucocorticoids reduces brain edema, TNF-alpha, IL-1, and prostaglandins E2. help treat acute, non-tb bacterial meningitis
210
how do glucocorticoids help collagen disorders?
beneficial for acute exacerbations used for systemic lupus erythematosus polymyositis and dermatomysostitis use glucocorticoids as drugs of choice polyarteritis nodosa (combination therapy) polymyalgia rheumatica (high dose steroid therapy)
211
corticoid treatments for collagen disorders
prednisone, methylprednisolone, triamcinolone, and dexamethasone
212
hematological disorders treated with glucocorticoids
autoimmune hemolytic anemia initial therapy for idiopathic thrombocytopenic purpura inhibit phagocytosis and icrease platelet lifespan
213
corticoid treatments for hematalogic disorders
prednisone triamcinolone dexamethasone
214
glucocorticoids in hepatic diseases
initial therapy for subacute hepatic necrosis and autoimmune chronic hepatits
215
corticoid treatments for hepatic disease
prednisone and azathiorpine
216
corticoid in renal diseases
idiopathic nephrotic syndrome in pts <16
217
corticoid treatments for renal disorder
methyprednisolone
218
corticoids in respiratory disorders
treat pulmonary sarcoidosis (prednisone) | respiratory stress syndrome especially in premature neonates (betamethasone and dexamethasone)
219
These drugs have variable mineralocorticoid activity so they can cause sodium and potassium retention
hydrocortisone, cortisone, prednisone, and prednisolone
220
different routes of administration for corticosteroids
``` nonsystemic (intraarticular) local (can have side effects) depot preps (intralesion, intra/extra articular) intrasynovial injection rectal (inflammatory bowel) parenteral (septic shock) oral (chronic use) ```
221
how do you pick a glucocorticoid?
``` look for severity anticipated dose and duration of therapy factors predisposing to complications alternative drug therapy ```
222
what do the ADRs for corticosteroids correlate with?
``` dose frequency duration route age and condition of patient underlying disease ```
223
GI ADRs for corticosteroids
``` increase gastric acid and pepsinogen production gastric ullcers (steroid should be slowly removed and start on antiulcer therapy gastric bleeding (look in stools) ```
224
Edema ADRs for corticosteroids:
``` fluid retention (bad for heart/kidney disease patients) to treat: restrict dietary sodium ```
225
carb and lipid metabolism ADRs for corticosteroids:
``` hyperglycemia enhanced gluconeogenesis aggravate diabetes triglycerides are elevated elevated lipoproteins so increased risk of atherosclerosis vascular disease ```
226
electrolyte ADRs for corticosteroids:
hypokalemia and metabolic acidosis leading to paralysis, arrhythmias and cardiac arrest avoid by restricting sodium and eat potassium rich foods (spinach, raisins, OJ) and steroid with low mineralocorticoid therapy hypophosphatemia (rare) severe muscle weakness. consume dairy to treat
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bone ADRs for corticosteroids:
osteonecrosis from fat embolism and swelling of fat cells and increase in intraosseous pressure joint pain and stiffness from prolonged corticosteroid treatmetn
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nitrogen ADRs for corticosteroids:
negative nitrogen balance from excessive protein breakdown. | eat high protein diet to treat
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CNS ADRs for corticosteroids:
personality and behavioral changes. euphoria insomnia, increased appetite, nervousness, irritability, psychotic and manic episodes and paranoid state symptoms disappear after a while
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growth ADRs for corticosteroids:
suppression of growth so should be restricted in children or alternate day therapy
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muscle ADRs for corticosteroids:
causes myopathy because of protein catabolism | associated with triamcinolone and is reversible
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skin and soft tissue ADRs for corticosteroids:
skin thinning and purpura non-melanoma skin cancer (oral glucocorticoids) acne, alopecia, hypertrichosis, striae cushingoid syndrome: truncal obesity, buffalo hump, moon face, weight gain
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ocular ADRs for corticosteroids:
elevates intraocular pressure. exaggerated in diabetics and myopes enhance development of secondary ocular infections by fungi or viruses ocular herpes pts at risk for corneal perforation
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infection ADRs for corticosteroids:
decreases resistance to infections because inflammation mechanisms are depressed
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HPA ADRs for corticosteroids:
suppresses HPA (hypothalamic-petuitary-adrenal axis) through negative feedback
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pregnancy ADRs for corticosteroids:
``` placenta can metabolize glucocorticoids fetal adrenal hypoplasia hypoadrenalism cleft palate in offspring category C ```
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withdrawal from glucocorticoid therapy leads to
malaise, fever, myalgia, arthralgia, fatigue, and restlessness
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why is dose reduction therapy needed to taken off of glucocorticoid
because coticoid causes HPA suppression so you will need to get that started up as well
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____promotes reabsorption of sodium
aldosterone
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what is the reabsorption of sodium coupled to?
excretion of potassium and hydrogen ions
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what happens when there is excess in aldosterone?
leads to hypokalemia, metabolic alkalosis, increase in plasma volume and hypertension
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this drug (potent steroid) has both glucocorticoid and mineralocorticoid
fludricortisone
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what does fludricortisone used for?
treat adrenocortical insufficiency associated with mineralocorticoid deficiency
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hypercortisolism or hyperadrenocortism
cushings syndrome
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what is cushings disease?
a tumor in the pituitary gland and it releases large amounts of ACTH and so there is an excessive release of cortisol the pituitary gland does not respond to negative feedback and just continues to produce ACTH
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ACTH independent cortisol hyper secretion
patients present with benign adrenal adenomas and adrenocortical carcinomas
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Conn's syndrome
hyperaldosteronism
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what happens when there is increased aldosterone?
there is decreased plasma renin activity, hypokalemia, metabolic alkalosis, and hypertension
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``` functions: mediator for tissue/cell injury mediator of inflammatory response in allergic reactions regulator of cell growth and repair regulator of gastric acid secretion neurotransmitter in the CNS regulator of cardiac function (possibly) ```
histamine
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what are the mechanisms that histamine is released by?
drug chemical induced response to cell tissue/damage immunologic stimulation (mas cells with IgE antibodies) neuronal and endocrine stimulation (neuronal stimulation through Ach at muscarinic receptors and when histamine is released, it binds to H2 receptors (endocrine) and stimulates secretion of HCl
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what is the "triple response" of histamine?
when histamine is injected into the skin, you get: red spot (local) -- from dilation of minute blood vessels flare -- dilation of neighboring arterioles wheal -- increased capillary permeability
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what is histamine shock?
when histamine is given in a large doses or released during anaphylaxis and you have a huge drop in BP because of the vasodilation and leakage of fluid in the Extravascular space -- resembles other shocks
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the effect of histamine on acid secretion is initiated by what receptor?
H2
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in blood vessels, what does histamine do?
causes intense dilation | can cause pulsatory headaches
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what are the effects of histamine on the heart?
increases force of contraction | slows AV conduction
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what are the different types of histamine receptors and where are they located?
H1: skin, blood vessels, heart, airway, CNS H2: GI tract, heart, brain, blood vessels H3: CNS H4: hematopoetic cells
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what do H1 receptors do?
mediate rapid vasodilation, increased capillary permeability, bronchoconstriction, irritation of peripheral nerve endings
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what do H2 receptors do?
mediate gastric acid secretion | MAY have some effect in hypersensitivity reactions
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what do H3 receptors do?
presynaptic autoreceptors to regulate release of histamine
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what do H4 receptors do?
may be involved in inflammation
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what kind antihistamines do we use for H1 receptors?
"antihistamines"
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what do we use to block H2 receptors?
H2 antagonist like cimetidine and it reduces gastric acid secretion. widely used to treat peptic ulcer disease
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what are the first generation of antihistamines that are very sedating?
doxylamine promethazine hydroxyzine
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what are the first generation of antihistmines that are sedating?
diphenhydramine dimenhydrinate chlorpheniramine meclizine
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second generation, non sedating H1 antagonists
loratadine/desloratadine cetirizine/levocetirizine fexofenadine