Drugs and Allergy Flashcards

1
Q

Name 6 different allergic disorders

A
allergic rhinitis (hay fever)
allergic conjunctivitis (pink eye)
atopic dermatitis (eczema)
urticaria (hives)
asthma
anaphylaxis
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2
Q

what is an allergy?

A

an autoimmune disorder where there is a hyperimmune response to allergens

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3
Q

what causes an allergy?

A

maladaptive immune system response creating memory to antigens

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4
Q

what are 7 key players involved in an allergic reaction? which are involved in the immediate reaction?

A
Immediate: IgE, mast cells, basophils
eosinophils
dendritic cells
T-cell (Th1 and 2)
B cells
All components involved in late phase reaction
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5
Q

What is the initial response to an allergen?

A

allergen binds to dendritic cells
an antigen acts on the T cells
Th2 acts on the B cells
B cells act on plasma cells
Creates IgE antibodies that will bind to mast cell upon exposure to the allergen
upon subsequent exposures, allergen binds directly with IgE bound to mast cell, causing release of IL-4 and TNFalpha, that act on Th2, which releases IL-4 that binds to plasma cell and releases IgE antibodies

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6
Q

what are mast cells?

A

tissue cells of the immune system found in loose connective tissue, organs, vasculature, nerves, skin, respiratory tract, etc.
not present in epidermal cells, CNS, gastric mucosa

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7
Q

what is the function of mast cells?

A

store histamine, interleukins, proteoglycans and various enzymes in their granules at cytoplasm

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8
Q

what 3 things occur when the mast cell is degranulated?

A

1) increased blood flow and permeability of blood vessels (inflammation and swelling)
2) contraction of smooth muscles
3) increased mucus production and fluid secretion

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9
Q

what mediators are associate with tickling, itching, nose rubbing, and allergic salute?

A

histamine and prostaglandins released by mast cells

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10
Q

what mediators are associated with sneezing, runny nose, post nasal drip, and throat clearing?

A

histamine and leukotrienes released by mast cells, eosinophils and basophils

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11
Q

what mediators are associated with nasal congestion, mouth breathing, stuffy nose, and snoring?

A

histamine, leukotrienes, bradykinin, and platelet activating factor released by mast cells, eosinophils, and basophils

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12
Q

what is histamine?

A
an autacoid (self-relief) which function like hormones but are not actually hormones
stored in tissue mast cells and blood basophils
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13
Q

what will cause antihistamine release?

A
antigens
allergic responses
drugs (morphine, succinylcholine)
insect venoms
scratching, cold
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14
Q

what is the H1 receptor important for?

A

important for allergic disorders and is the target of classic antihistamines

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15
Q

what effects does the H1 receptor exert when bound to histamine?

A

1) contraction; gastrick and respiratory smooth muscle
2) vasodilation
3) increased vascular permeability
4) pruritus
5) increased bronchial secretions and viscosity

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16
Q

what effects does the H2 receptor exert when stimulated? inhibited?

A

stim: gastric acid secretion
inhibited: decreased gut acidity
also involved in vasodilation

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17
Q

what is the H3 receptor involved with?

A

cholinergic neurotransmission

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18
Q

what types of cells are H4 receptors involved with?

A

eosinophils
neutrophils
CD4 T cells

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19
Q

what is the triple response of histamine when pricked into the skin?

A

1) red area at site of injection due to vasodilation
2) wheal replaces red area (edema)
3) bright red flare - indirect vasodilation

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20
Q

what are some symptoms of allergic rhinitis?

A
rhinorrhea
plugged nasal passages
itching (eyes, nose, throat)
tearing
fatigue
headache
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21
Q

what are the two different kinds of allergic rhinitis?

A

seasonal (airborne pollen)

perennial (animal dander, mold, dust)

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22
Q

what are the various treatment options for AR? (8 points)

A

1) antihistamines
2) intranasal glucocorticoids
3) leukotriene modifiers
4) decongestants
5) mast cell stabilizers
6) anticholinergic
7) anti-IgE therapy
8) systemic steroids

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23
Q

how do antihistamines work?

A

block the action of histamine by blocking the H1 receptor

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24
Q

what are the effects of antihistamines?

A
decreased itching
decreased vascular permeability
decreased bronchial secretions
relaxation of bronchial smooth muscle
decreased cough receptor stimulation
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25
Q

what are some additional effects of 1st gen AH?

A

non-histamine blocking actions leading to sedation, atropinic and anti-emetic effects

26
Q

what are some additional effects of 2nd and 3rd gen AH?

A

prevent mast cell release of mediators that cause inflammation

27
Q

what are some examples of AH’s? indicate which is 1st, 2nd, or 3rd gen

A
first:
chlorpheniramine
diphenhydramine
second:
cetirizine
loratadine
3rd:
fexofenadine
28
Q

why do 2nd and 3rd gen AH have minimal sedating/anticholinergic effects?

A

they don’t pass through the BBB very easily so CNS effects are minimal

29
Q

what are antihistamines usually combined with?

A

decongestants such as pseudoephedrine and phenylephrine

30
Q

describe the PK for antihistamines?

A

half lives variable (8-24h)
concentration in breast milk parallels concentration in plasma
most metabolized by Cyt P450 (Cyp3A4)
grapefruit juice may block metabolism

31
Q

what are the routes of admin for AH?

A
oral
intranasal
intravenous (anaphylaxis)
32
Q

what are the indications for antihistamines?

A

drug of choice for mild-mod allergic rhinitis
relieves sneezing, itching, nasal discharge, and ocular symptoms (tearing, itching, erythema)
best for exudative allergies (hay fever)

33
Q

what is the drug of choice for severe AR?

A

intranasal glucocorticoid (fluticasone)

34
Q

what are some side effects of first gen AH?

A
atropinic effects
somnolence (drowsiness)
problems with cognition
learning and memory impairment
psychomotor effects
35
Q

what is the youngest age that can use first gen AH?

A

6 y.o

36
Q

what is the name of the intranasal second gen AH?

A

azelastine

37
Q

which second gen AH is best to use in children?

A

cetirizine

38
Q

what is fluticasone effective for?

A

nasal and ocular symptoms; itching, sneezing, discharge, congestion
most effective for prevention and treatment

39
Q

what is the dosing for fluticasone and how long does it take to reach max effect?

A

OD dosing

may take 7 days

40
Q

what is the function of leukotrienes?

A

involved in infiltration of inflammatory cells, mucous secretion, and affect airway constriction
released during allergic inflammation by mast cells, eosinophils, basophils, and inflammatory cells

41
Q

name a leukotriene receptor antagonist

A

montelukast

42
Q

what is the indication for montelukast?

A

modest relief of congestion, itching, discharge
less effective than intranasal glucocorticoids
normally used with AH or intranasal glucocorticoid

43
Q

what is the mechanism of phenylephrine?

A

alpha 1 receptor agonist to cause

increased vasoconstriction, reduced nasal swelling

44
Q

what is phenylephrine helpful for?

A

congestion only

not helpful for sneezing, itching, discharge

45
Q

what are the side effects of decongestants?

A
insomnia
nervousness
headache
palpitations
hypertension
urinary retention
46
Q

what is an important counselling point for decongestants?

A

if you use more than 3-5 days, could cause rebound congestion

47
Q

what do mast cells do?

A

activated by response to allergens by releasing mediators such as histamine, leukotrienes, PG, PAF, etc.

48
Q

what is an example of a mast cell stabilizer? what does it do?

A

cromolyn sodium

inhibits mast cell degranulation and release of mediators

49
Q

what are some counselling tips for mast cell stabilizers?

A

less effective than intranasal corticosteroids
must be given before exposure
almost no local/systemic toxicity

50
Q

what is an example of an anticholinergic?

A

ipratropium

51
Q

how does ipratropium help with allergic rhinitis

A

reduces mucus secretion
no effect on inflammation
no relief of sneezing, itching, congestion
useful if primary symptom is nasal discharge

52
Q

what are some side effects to ipratropium?

A

atropinic like:
dry mucous membranes
urinary retention

53
Q

who should use caution when using ipratropium?

A

glaucoma

prostatic hypertrophy

54
Q

what is another drug used to treat allergic rhinitis?

A

Omalizumab

55
Q

how does omalizumab work?

A

anti-IgE antibody - given SC that selectively bind human immunoglobulin E (IgE)
prevents IgE bindings to cells and reduces free IgE in serum

56
Q

why are oral glucocorticoids not preferred for allergic rhinitis?

A

major side effects

57
Q

how does allergen specific immunotherapy work treat allergic rhinitis?

A

subcutaneous allergen immunotherapy
administer increasing doses of a solution of allergens sc to which a patient is shown to be sensitive (skin test)
weekly then monthly injections for years - dose increased until fewer symptoms with natural exposure
once desired dose established, monthly maintenance

58
Q

how long does allergen specific immunotherapy last?

A

3-5 years

benefit may continue when discontinued

59
Q

who should avoid allergen specific immunotherapy?

A

severe asthma patients
CV disease pts
those using a high dose of beta blockers
pregnant patients

60
Q

what are the indications for immunotherapy?

A

IgE in the serum or skin sensitivity to allergen
poor pharmacotherapy response or side effects
patient preference