Brainscape's Knowledge GenomeTM

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


See full index

medicinal chem > Antihistamines and Related Antiallergic Agents > Flashcards

Antihistamines and Related Antiallergic Agents Flashcards

You may prefer our related Brainscape-certified flashcards:
Periodic Table flashcards Chemistry 101 flashcards AP® Chemistry flashcards Organic Chemistry 101 flashcards
1
Q

Where does histamine synthesis occur?

A

in many tissues, including mast cells, parietal cells of the gastric mucosa, and neurons of the central nervous system (CNS) and in the periphery

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

Histamine gives a ___________ effect

A

local

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

What is used in the treatment of allergic inflammatory disorders?

A

H1 antihistamines

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

What is used in the treatment of gastric hypersecretory disorders?

A

H2 antihistamines

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

Histamine plays a physiologic role at several regions of the CNS via which receptors?

A

H3 and H4

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

The stimuli for release of histamine from tissues may include?

A
  • destruction of cells as a result of cold
  • allergies and anaphylaxis
  • toxins from organisms
  • venoms from insects and spiders
  • trauma
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Why are histamines released by injured tissues?

A

to recruit white blood cells at the site of injury by inducing vasodilation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the effect of H1 receptors on smooth muscle?

A

relaxation

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

What is the effect of H1 receptors on capillary permeability?

A

increases capillary permeability

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

How does histamine promote vasodilation of small blood vessels?

A

by causing the vascular endothelium to release nitric oxide

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

Effect of H1 receptors on bronchioles?

A

constriction

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

Which histamine receptors mediate many pathological processes, including allergic rhinitis, atopic dermatitis, conjunctivitis, urticarial, bronchoconstriction, asthma, and anaphylaxis?

A

H1

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

What is the main difference between first and second generation H1 antihistamines?

A

selectivity and side effects

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

________________ are useful in the treatment of allergy and inflammatory disorders

A

H1 antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

First-generation H1 antihistamines are effective in the treatment of?

A

allergic responses (e.g., hay fever, rhinitis, urticaria, and food allergy)

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

Adverse central effects of first-generation antihistamines include?

A

sedation, drowsiness, decreased cognitive ability,

and somnolence

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Peripheral side effects associated with cholinergic blockade include?

A

blurred vision, dry mouth, urinary retention, and constipation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Second-generation H1 antihistamines give what effects?

A

separation of CNS depressant and anticholinergic effects from peripheral antihistaminic effects

19
Q

Are first-generation H1 antihistamines selective?

A

no

20
Q

Are second-generation H1 antihistamines selective?

A

yes

21
Q

Advantages of second-generation H1 antihistamines?

A
  • more selective for H1 receptor

- less CNS effects

22
Q

Disadvantages of first-generation H1 antihistamines?

A
  • nonselective which leads to many side effects

- can reach CNS and cause sedation

23
Q

What happens when H1 antihistamines inhibit cholinergic receptors?

A
  • dry mouth
  • urinary retention
  • sinus tachycardia
24
Q

What happens when H1 antihistamines inhibit a-Adrenergic receptors?

A
  • hypotension
  • dizziness
  • reflex tachycardia
25
Q

What happens when H1 antihistamines inhibit serotonin receptors?

A

increased appetite

26
Q

What happens when H1 antihistamines inhibit histamine H1 receptors?

A
  • lowered allergic inflammation, itching, sneezing, and rhinorrhea
  • lowered neurotransmission in the CNS
  • sedation
  • lowered cognitive and psychomotor performance
  • increased appetite
27
Q

Most H1 antihistamines are?

A

inverse agonists

28
Q

What does the structural scaffold of H1 antagonists (first generation antihistamines) include?

A
  • tertiary amine
  • spacer
  • 2 aromatic or heteroaromatic rings
29
Q

What is the difference between H1 and H2?

A

H2 usually has an imidazole but H1 antagonist has only aromatic or heteroaromatic rings

30
Q

What are the oldest first-generation antihistamine that are not widely used anymore?

A

ethylenediamines

31
Q

Do ethylenediamines cause CNS effects mainly sedation?

A

yes

32
Q

The prototype of the aminoalkyl ethers is?

A

diphenhydramine

33
Q

Do ethanolamine ethers cause significant anticholinergic side effects and sedation?

A

yes

34
Q

What type of antihistamines is used as OTC sleep aids?

A

ethanolamine ethers

35
Q

Compounds with central anticholinergic and antihistaminic effects have been used as one approach to the treatment of?

A

Parkinson disease

36
Q

__________ are widely used OTC antihistamines for mild seasonal allergies.

A

alkyl amines

37
Q

Compared to the ethylenediamines and ethanolamine ether series, alkyl amines are characterized by a _________ duration for antihistaminic action and a ________ incidence of central sedative side effects

A

long; decreased

38
Q

Do piperazines give anticholinergic side effects and drowsiness?

A

yes

39
Q

What is the primary use of piperazines?

A

treatment of motion sickness and vertigo and for suppression of nausea and vomiting

40
Q

What is the effect of most tricyclic H1 antihistamines?

A

sedative effects and long durations of action

41
Q

Do second-generation H1 antihistamines penetrate the blood-brain barrier?

A

no because of their amphoteric nature or they are substrates for transporter proteins

42
Q

Name the second-generation H1 antihistamines with weak potential for producing sedation

A
  1. acrivastine
  2. cetririzine
  3. levocetirizine
43
Q

Name the second-generation H1 antihistamines that are nonsedating

A
  • desloratadine
  • fexofenadine
  • loratadine

medicinal chem (3 decks)

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