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RRPA Pharmacology II > antihistamine-OTC meds > Flashcards

antihistamine-OTC meds Flashcards

1
Q

Where are histamines Stored?

A

They are stored in the forms of granules in the mast cells (tissues) or basophils (blood)

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2
Q

How are these histamines released?

A
  1. Immunologic release- IgE mediated, causes degranulate on exposure to antigen (Type I response)
  2. Amine Drugs- can displace histamine from storage (morphine, codeine, vancomycin)
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3
Q

What receptors do histamines act on?

A

H1, H2, and H3

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4
Q

What is histamines effect on cardiovascular H1 receptors? how bout H2 receptors?

A
  1. Vasodilation of arterioles-hypotension, nasal congestion
  2. Increased capillary permeability (hypovolemic shock, edema, urticaria/ hives)

Effect on H2 is direct cardiac stimulation and vasodilation

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5
Q

What will be the effect of histamines on the GI-tract?

A
  1. Contraction of smooth muscle (H1)

2. increased gastric acid secretion (H2)

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6
Q

When someone is having a bad allergic reaction there throat closes up. What effect do you think histamines have on bronchiolar smooth muscle?

A

Opens them SIKE…. its bronchoconstriction

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7
Q

What are the 4 major classes of antihistamines? (H1 receptor antagonists)

A
  1. H1 receptor blockade
  2. Muscarinic receptor blockade
  3. sodium channel blockade
  4. adrenergic receptor blockade
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8
Q

true or fals 1st gen antihistamines have additional blocking actions at non-H1 receptors?

A

true

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9
Q

What is one benefit of 2nd gen antihistamines compared to 1st gen when talking about H1 receptor blockade

A

2nd gen are highly specific for H1 receptors

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10
Q

Do both 1st gen and 2nd gen histamines have equal efficacy in blocking H1 receptors?

A

yes

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11
Q

Antihistamines have also work by a muscarinic receptor block. Out of the two 1st gen and 2nd gen which ones cause less sedation

A

2nd gen- they also have less complete CNS penetration

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12
Q

Anithistamines can act as an alpha 1 receptor block. What can this result in and what antihistamine causes this?

A

Can results in orthostatic hypotension

Promethazine

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13
Q

What generation of antihistamine is best for allergic rhinitis?

A

2nd-gen: not really sure why- maybe because its selectivity for H1 receptor is more specific

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14
Q

What can 1st gen antihistamines treat that 2nd gen can not.

A

1st gen antihistamines can be used for

  1. cough supression- Na channel block
  2. Motion sickness- H1 and M receptor block
  3. Nausea and vomiting- H1 and M receptor block
  4. Sleep aid for insomnia- H1 and M receptor block
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15
Q

Antihistamines are great for treating allergic rhinitis. But what it the best?

A

intranasal corticosteroids

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16
Q

Which gen of antihistamines has CNS penetration?

A

1st gen- resulting in more theraputic actions

helps with insomnia, motion sickness

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17
Q

How are antihistamines metabolized?

A

hepatic metabolism by CYP3A4

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18
Q

What are some the of the time frames for 1st gens to be metabolized

A

6-8-12 hours

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19
Q

What are some the of the time frames for 2nd gen antihistamines to be metabolized

A

12-24

12hrs for fexofenadine
24 hrs for loratadine

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20
Q

which gen has a greater chance of causing a sedation side effect

A

1st gen (benadryl)

21
Q

Which generation antihistamine 1st or 2nd produces an antimuscarininc action causing dry mouth?

A

1st generation

22
Q

Which generation antihistamine 1st or 2nd produces a paradoxical excitation

A

1st gen

23
Q

Which generation antihistamine 1st or 2nd produces a postural hypotensive effect?

A

1 st gen has an alpha 1 blocker effect (promethazine)

24
Q

What are the first gen antihistamines

A

Dimenhydrinate
diphenhydramine
Meclizine

25
Q

Which 1st gen has the lowest sedative effect?

A. Dimenhydrinate
B. diphenhydramine
C. Meclizine

A

C. Meclizine

26
Q

Which 1st gen has the highest antiemetic effect?

A. Dimenhydrinate
B. diphenhydramine
C. Meclizine

A

C. meclizine

27
Q

which 1st gen antihistamine has a medium anticholinergic effect?

A. Dimenhydrinate
B. diphenhydramine
C. Meclizine

A

yep C meclizine again

Both A and B have the exact same effects on sedation, antiemetic, and anticholinergic

28
Q

Can second gen antihistamine cross BBB and do they have any anticholinergic effects?

A

no they can not cross the BBB and they do not have any anticholinergic effects

29
Q

what are the 2nd gen antihistamine meds?

A

Cetirizine
Fexofenadine
loratadine

30
Q

Which of the following has the shortest duration?

A. Cetirizine
B. Fexofenadine
C. loratadine

A

B. lasts 12 hours, the others last 24

31
Q

what drug is treat nasal decongestion and only nasal decongestion?

A

sympathomimetics

32
Q

Mechanism of action for topical decongestants?

A

they stimulate alpha 1 receptors of nasal blood vessels which have been dilated due to histamines or bradykinin

so they vasoconstrict theses bad boys (blood vessels that is)

33
Q

Side effect of topical decongestants?

A

rebound congestion due to local ischemia-irritation (restrict use for 3-5 days)

34
Q

What are two kinds of topical nasal decongestants?

A

Phenylephrine

oxymetazoline

35
Q

from the following topical decongestants. Which is the most effective and which is the longer lasting?

A. Phenylephrine
B. oxymetazoline

A

A. is the most effective

B. is the longer lasting- reduces the chance of rebound congestion

36
Q

Which drug is a direct receptor agonist and which is an indirect receptor agonist?

A. Phenylephrine
B. Pseudoephedrine

A

A. is a direct

B. is an indirect

37
Q

How is oral phenylephrine and pseudoephedrine delivered

A

via systemic circulation to nasal vascular bed and they act on alpha 1 receptors

38
Q

which last longer oral decongestants or topical?

A

orals do. However they are less intense

39
Q

Side effects of oral decongestants?

A

they are systemic so headache, nausea, dizziness, increased BP-palpitations

40
Q

Which of the following is the safest and most effective oral decongestant?

Phenylephrine
or pseudoephedrine

A

pseudoephedrine

i think he said Phenylephrine doesn’t even really work?

41
Q

which drug directly suppresses the cough center?

A

codeine (the good stuff)

42
Q

Uses for anittussive agents?

A

reduce frequency of cough, especially dry non-productive cough

43
Q

MOA of antitussive agents?

A

Both central and peripheral

44
Q

Most effective MOA for cough suppression?

A

drugs that are agonists at endogenous u-opioid receptors

45
Q

Which drugs are act as agonists on endogenous u-opioid receptors

A
  1. Codeine
  2. Hydrocodone
  3. Hydromorphone
  4. Dextramorphone
46
Q

Most common adverse effects of Codeine, Hydrocodone, Hydromorphone

A

Nausea, drowsiness, constipation allergic reactions

47
Q

What is the most commonly used OTC cough med?

A

dextromorphan aka robitussin

48
Q

What drugs are the first line tx for both 1. acute cough due to common cold and 2. acute cough due to upper airway cough syndrome

A

brompheniramine/pseudophedrine

RRPA Pharmacology II (23 decks)

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