Brainscape's Knowledge GenomeTM

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


See full index

Pharm 6 > Antihistamines > Flashcards

Antihistamines Flashcards

0
Q

Histamine H1 receptor agonists, 1st generation

A
  • Chlorpheniramine
  • Diphenhydramine
  • Meclizine
  • Promethazine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
1
Q

Functional Histamine Antagonists

A
  • Cromolyn (Intal)

- Epinephrine

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

Histamine H1 receptor agonists, 2nd generation

A
  • Cetrizine

- Fexofenadine

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

Synthesis of Histamine: Formed from Amino acid _________ in a decarboxylation reaction with the enzyme ________ _____________.

  • Occurs primarily in ____ cells and __________.
  • Acts on specific histamine receptor
A

Histadine, Histadine decarcoxylase

-Mast cells and basophils

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

What cell releases histamine and is for pathogen defense. It is in most tissue, near blood vessels, enriched at body/environment interfaces?

A

Mast cells

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

Cell that releases histamine in blood

A

Basophils

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

What histamine receptor is widespread and most therapeutically relevant?

A

H1

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

What histamine receptor is widespread, gastric, cardiac

A

H2

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

What histamine receptor is presynaptic receptors in CNS

A

H3

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

What histamine receptor is in hematopoietic cells?

A

H4

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

Histamine receptors in allergic response cause:

A

1) Vascular smooth muscle dilation:
- H1 rec on endothelium (NO)
- H2 rec on smooth muscles cells (cAMP)- Flushing, fall in sytemic BP
2) Increased vascular permeability
3) Peripheral sensory nerve excitation

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

1) A _____ is rapid reddening due to dilation of small vessels
2) A ______ is due to increased vascular permeability
3) A ______ is due to neural activated vasodilation

A

1) Spot
2) Wheal
3) Flare

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

The ___ receptor is involved in bronchial contraction and GI contraction.

A

H1

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

The ___ receptor is involved in gastric acid secretion

A

H2

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

Histamine Pharmacology: A Physiological antagonist

A

Epinephrine- used in severe responses, anaphylactic shock

  • Vasoconstriction a1
  • Bronchodilation-B2
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Histamine release inhibitor and MOA

A

Cromolyn Sodium- Alters Cl- channel function; inhibits lung mast cell histamine release
-Aerosol, prophylactic use in asthma, hay fever

16
Q

1st generation antihistamines are metabolized by ______. 2nd generation by______.

A

1st- CYP450

2nd- CYP 3A4

17
Q

1st generation drugs used to treat Motion sickness and vertigo.

A

Diphenhydramine, promethazine, meclizine

18
Q

1st gen drugs for insomnia/sedative

A

Diphenhydramine, promethazine

19
Q

1st gen drugs as antiemetic

A

Promethazine, doxylamine

20
Q

Diphenhydramine (Benadryl) preparations and uses

A

Topical and oral.

  • Allergic rhinitis; pain and itching
  • Dermatologic pain and itching
  • Sleep aid (anti-musc.)
  • Motion sickness (anti-musc.)
21
Q

Diphenhydramine Adverse effects and cautions

A

a) Prominent sedation
b) Topical: allergic dermatitis
c) May reduce lactation and enters breast milk
d) Avoid in narrow angle glaucoma

22
Q

What drug is this? Used oral or topical. Used for allergic rhinitis, dermatologic pain and itch, and OTC cold remedies. Adverse effects include sedation (less than diphenhydramine) and less effect at muscarinic receptors.

A

Chlorpheniramine (Chlor- Trimeton)

23
Q

What drug is this: Oral use. Used as antiemetic, sedative. Adverse effects are similar to others, photosensitivity and additional side effect.

A

Promethazine (Phenergan)

24
Q

What drug is this: Oral for vertigo, prevent motion sickness. Less sedating than other 1st gen antihistamines.

A

Meclizine (Antivert)

25
Q

What drug is approved by FDA for morning sickness

A

Doxylamine (+pyridoxine=diclegis)

26
Q

2nd gen drug in oral prep for allergies. Used for allergic rhinitis and dermatologic pain and itch. Adverse effects include drowsiness and weak anti-muscarinic effects (dry mouth). Metabolized by CYP 3A4

A

Cetrizine (Zyrtec)

27
Q

T/F: Fexofenadine has no cardiotoxicity, and is not metabolized by the liver, and excreted unchanged in either urine or feces. It is a metabolite of Terfenadine.

A

True

29
Q

An oral drug for allergic symptoms that should not be taken with fruit juice. An OATP inhibitor. Used for allergic rhinitis and dermatologic pain and itching. Not sedating. Can cause nausea,vomiting, dysmenorrhea, drowsiness, and enters breast milk.

A

Fexofenadine (Allegra)

30
Q

T/F: 1st gen antihistamines enter CNS readily and 2nd are kept out

A

True- 2nd kept out by p-glycoprotein pumping=low sedating

31
Q

T/F: Better to take H1 antihistamines n a regular basis rather than as needed. Tolerance does not develop.

A

True

  • Symptom relief may be incomplete
  • Less effective with chronic/high antigen exposure
32
Q

Adverse effects of 1st gen antihistamines

A
  • Sedation
  • GI disorders- due to muscarinic, adrenergic and serotonin receptor block: constipation, diarrhea, loss of appetite, N/V, epigastric distress.
  • Anti-muscarinic: dry mouth, sinuses, urinary retention
  • Allergic rxns
  • Overdose looks like atropine overdose
  • Generally Avoid in children and elderly

Pharm 6 (9 decks)

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