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HD > Pharmacology 3: Therapeutic Approach To Allergic Disorders > Flashcards

Pharmacology 3: Therapeutic Approach To Allergic Disorders Flashcards

1
Q

Definition: an overreaction of the immune system to a normally harmless substance called allergen.

A

Allergy.

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2
Q

List symptoms of hay fever?

A

Allergic conjunctivitis, itchiness, and runny nose.

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3
Q

What is the most important mediator in type 1 hypersensitivity?

A

Histamine.

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4
Q

What are the aims of symptomatic treatment of allergies?

A

1- prevent mediator release.
2- use mediator antagonists.
3- block mediator effects at target organs.

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5
Q

What is the most widely used agents for allergies?

A

1- anti-histamines.
2- leukotriene modifiers.
3- prostaglandin antagonists.

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6
Q

How does histamine cause inflammation?

A

By increasing vasodilation, capillary permeability, causing smooth muscle concentration, mucus secretion, and parasympathetic nerve stimulation.

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7
Q

Where is histamine present?

A

In mast cells, skin, GIT mucosa, lungs, liver and placenta.
Also present in blood, secretions, venoms and pathological fluids.

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8
Q

Where are non-mast cell histamines present?

A

In brain, epidermis, gastric mucosa and growing regions.

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9
Q

Antihistamines act on which histamine receptor?

A

H1.

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10
Q

Where is H2 receptor present?

A

In the stomach.

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11
Q

What are drugs that act on H2 receptor called?

A

H2 blockers.

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12
Q

List H1 receptor agonists?

A

Betahistadine.

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13
Q

List H1 receptor antagonists?

A

Mepyramine,
Chlorpheniramine,
Cetirizine.

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14
Q

What is H1 receptor type?

A

Gq-coupled receptor.

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15
Q

What is H1 effector pathway?

A

PIP2 hydrolysis - IP3/DAG intracellular Ca2+ release ptn. Kinase C-activation.

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16
Q

List H1 receptor distribution?

A
  • smooth muscles.
  • blood vessels.
  • afferent nerve endings-stimulation.
  • ganglionic cell +.
  • adrenal medulla - release of C.A’s.
  • brain - neurotransmitter.
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17
Q

List H2 receptor agonists?

A

4-methyl histamine,
Dimaprit,
Impromidine.

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18
Q

List H2 receptor antagonists?

A

Cimetidine,
Ranitidine.

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19
Q

What is H2 receptor type?

A

Gs-coupled receptor.

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20
Q

What is H2 effector pathway?

A

Adenylyl cyclase activation - CAMP- phosphorylation of specific proteins.

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21
Q

What is H2 receptor distribution?

A
  • gastric glands.
  • blood vessels.
  • heart.
  • uterus (rats).
  • brain - neurotransmitter.
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22
Q

List the pathophysiological role of histamine?

A

1- gastric acid secretions.
2- allergic phenomena - early type 1 hypersensitivity.
3- as transmitter.
4- inflammation.
5- tissue growth & repair.
6- asthma contraindications.

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23
Q

What is the therapeutic value of histamine?

A

Histamine is of no therapeutic value.

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24
Q

List 3 histamine uses?

A

1- testing gastric acid secretion; to test acid secreting ability of stomach.
2- diagnosis of pheochromocytoma; histamine releases CA and BP raises.
3- pulmonary function; to test for bronchial hyper activity.

^ all of these are no recommended anymore.

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25
Q

List the pharmacological action of antihistamines?

A

1- antagonism of histamines; blocks histamine receptor NOT histamine release.
2- local anesthetic action; membrane stabilizing activity.
3- fall in BP - on IV injection.

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26
Q

List the affect of antihistamines antagonism of histamines?

A

1- broncho constriction and smooth muscle constriction.
2- triple response.
3- fall in BP.
4- animal death (pre-treatment with H1 blockers).
5- adrenaline release.
6- vasoconstriction of large BV.
7- no action on gastric acid secretion.

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27
Q

What is the anticholinergic action of antihistamines?

A

Dryness of mouth, blurred vision, urinary retention.

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28
Q

Which antihistamines have high anticholinergic action?

A

1- promethazine.
2- diphenhydramine.
3- dimenhydrinate.
4- pheniramine.
5- cyproheptadine.

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29
Q

Which antihistamines have low anticholinergic action?

A

1- chlorpheniramine.
2- hydroxyzine.
3- tripolidine.
4- cyclizine.

30
Q

Which antihistamines have minimal/absent anticholinergic action?

A

1- fexofenadine.
2- astemizole.
3- loratadine.
4- cetirizine.
5- mizolastin.

31
Q

Which generation of antihistamine are long acting?

A

2nd generation.

32
Q

Which generation of antihistamine are short-intermediate acting?

A

1st generation.

33
Q

Which generation of antihistamine are able to penetrate the CNS?

A

1st generation - more sedative, cannot be used by persons requiring constant attention like truck drivers.

34
Q

Which generation of antihistamine have anticholinergic activity?

A

1st gen.

35
Q

Which generation of antihistamine have no anticholinergic activity?

A

2nd gen.

36
Q

Which generation of antihistamine have antihistaminic action?

A

1st gen.

37
Q

Which generation of antihistamine have antiallergic action?

A

2nd gen.

38
Q

Which generation of antihistamine work on both central and peripheral HR?

A

1st gen.

39
Q

Which generation of antihistamine work only on peripheral HR?

A

2nd gen.

40
Q

Which generation of antihistamine impairs psychomotor performances?

A

1st gen.

41
Q

List the actions of 1st generation antihistamines?

A

Antipruritic, antiemetic and antitussive, anticholinergic and antiparkinonian.

42
Q

List the actions of 2nd generation antihistamines?

A

Only antihistamines and anti-allergic, urticaria, dermographisim, atopic eczema, food and drug allergy.

43
Q

Which generation of antihistamines has synergistic actions i.e., DI?

A

1st gen.

44
Q

List highly sedative antihistamines?

A

1- dimenhydrinate.
2- diphenhydramine.
3- doxylamine.
4- hydroxyzine.
5- promethazine.

45
Q

What is the duration of action of highly sedative antihistamines?

A

4–6 hours.

46
Q

List the uses of highly sedative antihistamines?

A

1- anti-motion sickness.
2- used as sleep aid.
3- anti emetic.

47
Q

List moderately sedative antihistamines?

A

1- pheniramine.
2- cyproheptadine.
3- meclizine.
4- buclizine.
5- cinnarizine.

48
Q

What is the duration of action of moderately sedative antihistamines?

A

4-6 hrs.

49
Q

List the uses of moderately sedative antihistamines?

A

1- anti serotonin effects.
2- anti motion sickness.

50
Q

List mildly sedative antihistamines?

A

1- cyclizine.
2- chlorpheniramine.
3- dimethindine.
4- tripolidine.

51
Q

What is the duration of action of mildly sedative antihistamines?

A

4-6 hrs.

52
Q

List 2nd generation antihistamines?

A

1- fexofenadine.
2- loratadine.
3- des loratadine.
4- astemizole.
5- cetirizine.
6- levo cetirizine.
7- azelastine.
8- ebastine.

53
Q

What is the duration of action of 2 gen antihistamines?

A

12-24 hrs.

54
Q

List the uses of 2nd gen antihistamines?

A

Sneezing, itching but do not significantly improve nasal congestion.

55
Q

Which drug is life saving in laryngeal angioedema and anaphylactic shock?

A

Adrenaline.

56
Q

Which drug is used for seasonal asthma?

A

Cetirizine.

57
Q

Antihistamine are ineffective in which conditions?

A

Asthma, humoral and cell mediated allergies.

58
Q

List the antipruritic actions of older antihistamines?

A

1- motion sickness.
2- morning sickness.
3- vertigo.
4- preanesthetic medication.

59
Q

Which older antihistamines are used in morning sickness?

A

1- promethazine.
2- dimenhydrinate.
3- cyclizine.

60
Q

Which antihistamines are used in vertigo?

A

H1, M1 and 5HT blocker, sedative, vasodilator and CA2+ influx - cinnarizine,

61
Q

Which antihistamine is used as a preanesthetic?

A

Promethazine.

62
Q

Which antihistamines are used as sedative, hypnotic and anxiolytic?

A

Promethazine and hydroxyzine.

63
Q

Which antihistamines are used as appetite stimulant?

A

Cyproheptadine.

64
Q

What is disodium cromoglyate?

A

Mast cell stabilizer.

65
Q

List histamine release inhibitors?

A

1- nedocromil.
2- lodoxasmide.
3- permirolast.
4- ketotifen.

66
Q

How do histamine release inhibitors act?

A

They act by preventing mast cell degranulation due to immunological reaction.
Prevent the release of H and other inflammatory mediators.

67
Q

What is ketotifen used for?

A

It has mast cell stabilizing property, good for patients with multiple allergic manifestations.

68
Q

What are histamine release inhibitors used in?

A

Bronchial asthma and allergic rhinitis.

69
Q

List the therapeutic aspects of immunotherapy (desensitization)?

A

1- slowly increasing doses of allergen.
2- administration is usually SC, although nasal, bronchial, sublingual and oral routes are possible.
3- patients should be observed at least 20 min after injection for avoidance of side effects.
4- must be used for at least 2 years in order to maintain benefit.

70
Q

List the indications of immunotherapy (desensitization)?

A

1- allergic rhinitis and allergic asthma: pollen, house dust, mite, cat and dog, immunotherapy is beneficial.
2- Hymenoptera sensitivity: efficacy of immunotherapy in case of insect venom has been established.

No evidence to support the use of food immunotherapy.

71
Q

List the first line treatment of allergies?

A

1- adrenaline: at first sign of anaphylaxis, given IM.
2- tourniquet.
3- oxygen.
4- anti-histaminics IV.
5- corticosteroids IV.

72
Q

List second line of treatment of allergies?

A

1- IV fluids.
2- IV aminophylline.
3- intubation and tracheostomy.
4- maintain supportive therapy.

HD (14 decks)

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