Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Anti-inflammatory drugs > Anti-histamines > Flashcards

Anti-histamines Flashcards

1
Q

What is the function of H1 receptor?

A

Mediates inflammatory and allergic reactions.
Vasodilation and cardiac stimulation.
SM contraction
Immune Response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the effect of H2 receptor?

A

Mediates gastric acid secretion.
Cardiac stimulation (increase HR and contractility)
Stimulation of gastric acid secretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the effect of H3 receptor?

A

CNS modulation. Presynaptic receptors. inhibit neurotransmitter release.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the 3 effects of activation of histamine receptors?

A
  1. Increased expression of endothelial adhesion molecules
  2. Release of cytokines and eicosanoids
  3. Activation of pro-inflammatory transcription factor NFkappaB
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Give 4 examples of eicosanoids

A

Prostaglandins, Prostacyclins, Thromboxanes, Leukotrienes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Give 2 Type 1 Hypersensitive reactions of H1 receptor stimulation

A

Anaphylaxis and Allergic rhinitus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the 3 dangerous effects of massive histamine release?
What are they collectively known as?

A
  1. Increased vascular permeability which can lead to sudden decrease in bp
  2. Bronchoconstriction, which can cause difficulty breathing
  3. Laryngeal oedema, which will lead to suffocation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Why is glucocorticoids given in an anaphylactic shock? Give an example of a glucocorticoid

A

Glucocorticoid helps to reduce rate of inflammatory mediators like prostaglandin and leukotrienes.
An example is Hydrocortisone.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are inverse agonists? give 2 examples

A

An adverse agonist reduce activity below the basal level of activity.
Histamine receptor reverse agonist: Ioratadine and Fexofenadine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Give 2 examples of neutral antagonist. State which is withdrawn from use

A

Terfenadine (withdrawn from use) and Cetirizine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are the common adverse effects of 1st generation of antihistamines? Give the explanations

A

Dry mouth and drowsiness.
They are able to cross the bbb and act on CNS modulators, leading to drowsiness.
They are not specific for H1 receptors and can act on muscarinic receptors, leading to dry mouth, blurred vision, constipation and urinary retention. or transient bradycardia followed by tachycardia.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Describe second generation anti-histamines. Give 2 examples of this generation of drugs.

A

Second generation anti-histamines have fewer side effects than 1st gen and there is less sedation. Does not cross the bbb, and are hydrophilic at body pH.
Examples are Cetirizine and Terfinadine (withdrawn from use)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Describe 3rd gen anti-histamines and give an example.

A

Less cardiotoxicity, less anti-muscarinic effects, are mostly active metabolites, such as Fexofenadine which is an active metabolite of Terfinadine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

H1 receptor activation results in?

A
  1. Postcapillary venule dilation: Erythema
  2. Separation of endothelial cells: Oedema
  3. Sensitisation of irritant receptors: itch, etc
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Give an example of 1st generation anti-histamine

A

Diphenhydramine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the 2 pathways that leads to production of icosanoids?
Which substance are icosanoids derived from?

A

Lipoxygenase pathway and COX Pathway

Derived from arachidonic acid

17
Q

What is the enzyme that converts arachidonic acid to leukotrienes?

A

Lipoxygenase

18
Q

Which enzyme converts arachidonic acid to prostaglandin?

A

Cyclic oxygenase (COX)

19
Q

How is prostacyclin and thromboxanes formed?

A

From prostaglandin, by cyclic endoperoxidase

20
Q

Which chemicals can stimulate pain and which can potentiate pain sensations?

A

Stimulation of pain: Serotonin 5-HT and Kinins, such as bradykinin
Potentiation of pain: Prostaglandins, etc

21
Q

Most of the anti-inflammatory actions are by COX-1 or COX-2?

How about most of the major side effects?

A

Anti-inflammatory effects by COX-2 whereas major side effects are due to COX-1.

22
Q

Name the NSAIDs

A

Aspirin, Ibuprofen and Celecoxib

23
Q

Which 2 NSAIDs should be avoided by pregnant women? In which trimester?

A

Ibuprofen and Celecoxib should be avoided by pregnant women in the third trimester.

24
Q

State the function of aspirin and its disadvantages

A

Aspirin: Anti-platelet activity, irreversible inhibitor, acetylates COX
Disadv: Increased risk of GI bleeding and irritation

25
Q

State the function of ibuprofen and its disadv

A

Ibuprofen: Short-term analgesic and anti-inflammatory activity
Disadv: Increased risk of gastric irritation and increased ulceration. To be avoided for pregnant women in their thrid trimester.

26
Q

State the function of paracetamol and its disadv

A

Paracetamol: Analgesic and anti-pyretic activity.
Disadv: No anti-inflammatory activity. Liver damage on overdose

27
Q

State the function of celecoxib and its disadv

A

Celecoxib: Specific COX-2 inhibitor, Fewer side effects
Disadv: Increased risk of stroke and heart attack, to be avoided for pregnant women in their third trimester.

28
Q

What are the adverse effects of increased COX-1 selectivity and increased COX-2 selectivity respectively?

A

COX-1: Increased risk of GI disturbances

COX-2: Increased risk of cardiac problems

29
Q

What is the half life of celecoxib?

A

11 hours.

30
Q

What are the drug interactions of aspirin?

A

Aspirin interacts with Warfarin and potentiate its anti-coagulative activity. Thus, there is increased risk of bleeding.

31
Q

Which 4 drugs are used as prophylaxis against headache and migraine?

A

Anti-histamines, Beta-antagonists, Tricyclic antidepressants, Serotonin 5HT2 antagonists

32
Q

Which 4 drugs are used to relieve headaches and migraines?

A

NSAIDs, Paracetamol, Anti-emetics, Serotonin 5HT1 agonists

33
Q

What is the mechanism of action of Triptan drugs?

A

Serotonin 5HT1 agonist. Constricts large blood vessels, Inhibit trigeminal nerve and desensitize sensory nerves.

34
Q

What is the mechanism of action of Pizotifen?

A

Serotonin 5HT2 antagonist. Also a histamine antagonist. May inhibit initial pro-inflammatory and vascular changes

35
Q

Which drugs inhibits COX1?

A

NSAIDs, such as Aspirin, Ibuprofen and Naproxen.

Anti-inflammatory drugs (2 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions