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Yr 2: Pharmacology and Therapeutics (MGEM2016 UNUK) > Itches, scratches and Sneezes > Flashcards

Itches, scratches and Sneezes Flashcards

1
Q

Allergic response

Outline the allergic response

A
  1. Allergen
  2. white blood cells respond to allergen with antibodies
  3. memory cells remember antigen
  4. when re-exposure occurs, allergen is engulfed and digested
  5. mast cells then release inflammatory mediators
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2
Q

functions of mast cells

what 3 things do mast cells release when allergens or pathogens bind to them

A

they release:

  • histamine
  • prostaglandins and leukotrienes
  • cytokines
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3
Q

functions of mast cells

what is does histamine, LTC4 and PGD2 do to epithelial permeability?

A

increases epithelial permeability and secretion

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4
Q

functions of mast cells

what can histamine and LTC4 also affect other than epithelial permeability

A

can effect:

  • blood flow
  • vascular permeability
  • coagulation
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5
Q

functions of mast cells

what can histamine, proteases and PGD2 do in the nervous system, gastrointestinal tract and bronchi

A

can:

  • have neuroimmune interactions
  • aid peristalsis
  • cause bronchoconstriction
  • can cause pain
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6
Q

pharmacological strategy

what are 4 phamacological strategies to decrease immune mediator action

A
  1. immunotherapy
  2. prevent release of mediators from mast cells
  3. block action of mediators using a receptor antagonist
  4. inhibit synthesis of mediators
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7
Q

Preventing Release

what does cromoglicate do and what can it be used in

A

cromoglicate stabilises mast cells, inhibiting degranulation (stopping release of inflammatory mediators)

used in:
- eye drops
- nasal spray
- some times asthma

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8
Q

histamine

what 3 things does H1 histamine receptor subtype cause

A

causes:
- contraction of smooth muscle (ileum, bronchi, uterus)
- vasodilation
- plasma exudation

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9
Q

antihistaminnes: 1st Gen

why do diphenhydramine, dimenhydrinate, chlorpheniramine and promethazine cause drowsiness?

A

because they cross they cross the blood brain barrier

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10
Q

antihistamines: 2nd and 3rd Gen

what Generation antihistamine is terfenadine, why is it non-sedating and why was it withdrawn infavour of newer generation antihistamines?

A
  • 2nd generation
  • non-sedating as does not cross BBB
  • withdrawn as it can cause arrhytmias (irregular heartbeat)
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11
Q

antihistamines: 2nd and 3rd gen

name 3 third generation antihistamine drugs

A
  • fexodenadine
  • cetirizine
  • loratadine
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12
Q

Synthesis of Prostagladins and leukotrienes

how are prostagladins and leukotrienes synthesised?

A

from membrane phospholipids that are broken down to form arachidonic acid

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13
Q

synthesis of prostaglandins and leukotrienes

outline how prostaglandins and leukotrienes are synthesised

A
  1. membrane phospholipids are cleaved using phospholipase A2.
  2. this releases arachidonic acid, which is acted upon by cyclooxygenase (COX), leading to to production of protaglandins
  3. arachidonic acid are also acted by lipoxygenase, leading to production of leukotrienes
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14
Q

Prostaglandins

what receptors do PGI2 act on and what are the effects of activation of this receptor

A
  • acts on IP receptors
  • effects include:
    vasodilator
    production of pain
    inhibits platelet aggregation
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15
Q

Prostaglandins

what receptors does PGF2a act on and what are the effects of activation of this receptor?

A
  • acts on FP receptors
  • effects include:
    bronchoconstrictor
    myometrial contraction
    coughs
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16
Q

prostaglandins

what receptors does PGD2 act on and what are the effects of activation of this receptor

A
  • acts on DP
  • effects of activation:
    vasodilator
    broncho-constriction
    chemotaxis
    inhibits platelet aggregation
17
Q

Prostaglandins

what receptors does PGE2 act on and what are the effects of activation of this receptor

A
  • acts on EP receptors

effects:
- vasodilation
- pain
- cough
- mucus secretion

18
Q

prostaglandins

what receptors does TXA2 (thromboxane) act on and what are the effects of activation of this receptor

A
  • acts on TP receptors

effects:
- vaso-constriction
- increases platelet aggregation

19
Q

prostaglandins

what prostaglandins do these cells produce:
- platelets
- endothelium
- mast cells
- many other cells

A
20
Q

NSAIDs

what do NSAIDs inhibit?

A

NSAIDs are COX inhibitors

21
Q

NSAIDs

How can NSAIDs be antipyretic

A

they can be antipyretic due to inhibition of prostaglandin production in the hypothalamus (eg paracetamol)

paracetamol is NOT anti-inflammatory

22
Q

Leukotrienes

what 2 things do LTC4, LTD4 and LTE4 do?

A
  • bronchoconstriction
  • increased microvascular permeability
23
Q

leukotrienes

what 2 things does LTB4 do?

A
  • Chemoattractant for neutrophils
  • Stimulates release of lysosomal enzymes from macrophages
24
Q

leukotrienes

what can zileuton do?

A

can inhibit lipoxygenase, stopping production of leukotrienes

25
Q

lekotrienes

what are examples of leukotriene receptor antagonists

A

antagonists:

  • zafirlukast
  • montelukast
26
Q

asipirin-intolerant asthmatics

why would aspirin not necessarily be beneficial for someone with asthma

A
  1. it is believed that leukotrienes play a role in the bronchoconstriction in asthma
  2. Aspirin inhibits COX action
  3. this, however, leads to increased arachidonic acid concentration, which leads to increased leukotriene production, thus promoting more asthmatic bronchoconstriction
27
Q

steriods

where do corticosteroids come from?

A

corticosteroids come from the adrenal cortex

28
Q

steroids

outline how corticosteroids decrease inflammatory response

A
  1. diffuse across cell membrane
  2. enter cytoplasm
  3. combine with a receptor to enter nucleus
  4. then affect gene transcription to decrease inflammatory response
29
Q

glucocorticoids

what is the adverse affect of glucocorticoids decreasing inflammatory and immulogical response?

A

increases susceptibility to infection

30
Q

synthetic glucocorticoids

how can adverse effects of glucocortoids be limited

A

via route of administration

31
Q

Glucocorticoids: Mechanism of Action

what do 2 things do glucocorticoids do regarding lipocortin and what does this lead to regarding PLA2,COX-2 and interleukin-2 receptors

A
  • stimulates synthesis of lipocortin, which inhibits PLA2
  • suppresses genes for PLA2, COX-2 and IL-2 receptors

Yr 2: Pharmacology and Therapeutics (MGEM2016 UNUK) (20 decks)

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