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Pharm Exam 5 > 61: Antihistamines > Flashcards

61: Antihistamines Flashcards

1
Q

triple response of Lewis

A
  • red spot
  • flare
  • wheal
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2
Q

Mast cells are found in greater numbers where?

A

bronchial mucosa
intestinal mucosa
skin

they secrete just about everything

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3
Q

Mechanisms for histamine release form mast cells

A
  • Cytolytic
    • Membrane damage
    • High levels of certain drugs
    • Mechanical damage
  • NON-cytolytic
    • immune response that requires prior sensitization
    • non-immunologic response to polypeptide (substance P, wasp venom)
    • displacement from granules by substances such as opiods and antibiotics
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4
Q

where are H1 receptors primarily expressed?

A
  • smooth muscle cells
  • vascular endothelial cells
  • CNS neurons
  • peripheral sensory nerves
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5
Q

what type of signaling do H1 receptors use?

A

Gq with PLc-Ip3-Ca2+ pathway

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6
Q

where are H2 receptors primarily expressed?

A
  • gastric parietal cells
  • cardiac muscle
  • CNS neurons
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7
Q

what type of signaling do H2 receptors use?

A

Gs

increases adenylyl cyclase and cyclic AMP –> PKa

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8
Q

organ system effects of histamine =

A

vasodilation

decreased total peripheral resistance and fall in systemic blood pressure can cause reflex tachycardia and edema

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9
Q

H1 in lung smooth m. cells causes…

A

elevated secretion of airway fluid and electrolytes and bronchoconstriction

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10
Q

H1 in peripheral neurons…

A

activation in epidermis causes itch

- activation in dermis causes pain

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11
Q

histamine ______ the following things

  • vascular permeability
  • immune cell adhesion molecules (p-selectin)
  • chemotaxis of eosinophils and neutrophils
  • release of inflammatory cytokines
  • antigen presentation from APC cells
A

increases

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12
Q

name 3 diseases that increase histamine levels

A

myelogenous leukemia

gastric carcinoid tumros

mast cell leukemia

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13
Q

physiological antagonists of histamine

A

epinephrine

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14
Q

3 histamine release inhibitors

A

cromolyn
nedocromil
omalizumab

can be used as prophylactic treatment of allergy

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15
Q

why are 2nd gen antihistamines non-sedating?

A

they do not penetrate BBB

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16
Q

3 common conditions treated by 1st gen antihistamines

A

allergic rhinitis
allergic conjunctivitis
urticaria

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17
Q

H1 antihistamines are inverse agonists?

A

reversibly bind to receptor and stabilize the inactive form

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18
Q

what do you need to watch out for when giving first gen antihistamine to neonates and young children?

A

paradoxical excitation and seizures

19
Q

why are mydriasis, constipation, and dry mouth/throat adverse effects of first gen antihistamines?

A

binding to muscarininc receptors as well

20
Q

chlorpheniramine

A

1st gen antihistamine

21
Q

diphenydramine

A

1st gen antihistamine

22
Q

pyrilamine

A

1st gen antihistamine

23
Q

hydroxyzine

A

1st gen antihistamine

24
Q

meclizine

A

1st gen antihistamine

25
Q

promethazine

A

1st gen antihistamine

can also block dopamine receptors

26
Q

cyproheptadine

A

1st gen antihistamine

can be used to treat serotonin syndrome

27
Q

4 antihistamines with strongest antiemetic effects

A

diphenydramine
promethazine
hydroxyzine
Meclazine

28
Q

3 antihistamines with highest sedative effects

A

diphenydramine
hydroxyzine
promethazine

29
Q

which drugs are known for being anticholinergic?

A

diphenhydramine
promethazine

observe dry mouth, urinary retention, sinus tachycardia

30
Q

which drugs are known for being anti adrenergic?

A

promethazine

observe hypotension, izziness, reflex tachycardia

31
Q

which drug is know for being anti- serotonergic?

A

cyproheptadine

32
Q

antihistamine drugs ___ appetite

A

increase

33
Q

2nd generation antihistamines have a ____ selectivity towards H1 receptor than 1st gen

A

higher

  • they bind noncompetitively to H1 receptor
  • have a reduced lipophilicity
34
Q

Azelastine

A

2nd gen antihistamine

35
Q

Cetirizine

A

2nd gen antihistamine

36
Q

Levocetirizine

A

2nd gen antihistamine

37
Q

Desloratadine

A

2nd gen antihistamine

38
Q

Loratadine

A

2nd gen antihistamine

39
Q

Fexofenadine

A

2nd gen antihistamine

40
Q

MOA cromolyn and nedocromil

A

inhibit degranulation of mast cells by inhibition of chloride channels in cell membrane s

41
Q

treat chronic urticaria with

A

omalizumab

monoclonal antibody that bind IgE

also used in tx asthma

42
Q

MOA doxepin

A

TCA

useful in treatment chronic urticaria b/c inhibits both H1 and h2 receptors

43
Q

what would you use ketotifen for?

A

only an opthalmic preparation

treat allergic conjunctivitis

Pharm Exam 5 (11 decks)

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