Colds/allergies Flashcards

1
Q

What are the three main approaches a drug can take to treat a congested nose?

A
  • Sympathomimetic drugs
    • Increase or mimic (nor)adrenergic transmission
  • Antihistamine
    • H1 (not H2) receptor antagonists
  • Other
    • Not recommended
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What causes rhinitis?

A

Vasodilation and edema

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

What causes rhinorrhea?

A

Mucus secretion

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

Why does vasodilation cause a blocked nose?

A

Nasal cavity made up of erectile tissue, but can only expand inwards due to bone structure

Tissue expands inwards, circumference closes, increased airway resistance

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

How do sympathomimetic nasal decongestants work?

A

Act on sympathetic alpha1 or alpha2 receptors (either will cause vasoconstriction and alleviate rhinitis)

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

True/False? Sympathomimetic drugs work on all three problems associated with rhinitis (vasodilation, edema, mucus secretion)

A

False, only vasodilation

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

What is the difference between a direct and an indirect sympathomimetic? Name an example drug for each

A

Direct (Phenylephrine): acts directly on alpha1/2 receptor to cause vasoconstriction

Indirect ([pseudo]ephedrine/PPA): acts on NA terminal to release NA, which then acts on alpha receptors

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

What do alpha1 receptors do when stimulated?

A

G-Protein coupled cascade involving Protein Kinase C, IP3, Activated Ca-dependent kinase

End result is vasoconstriction

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

What do alpha2 receptors do when stimulated?

A

G-Protein coupled receptor cascade involving decreased cAMP, decreased PKA, adenylate cyclase

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

True/False? There is no cure for the common cold

A

True/False? There is no cure for the common cold

Zinc kind of helps but there are too many side effects

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

Why do some places ban the sale of pseudoephedrine?

A

Because you can make meth out of it

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

Name the two direct and indirect (4 total) decongestants and how they’re applied

A

Direct:

  • NA, adrenaline (n/a)
  • Phenylephrine (oral + topical)

Indirect:

  • Pseudoephedrine (oral)
  • PPA (oral topical)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is rebound withdrawal?

A

Nasal resistance shoots up during chronic decongestant use (use decongestants acutely only)

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

What are the different routes of decongestant administration, and which is most effective?

A

Inhaler

Syrup

Nasal Spray

Nasal spray is best, Syrup is less effective but lasts longer, inhaler is just bad

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

Why would someone administer decongestants orally instead of nasally?

A

To unblock the Eustachian tubes (local administration does not pass systemically)

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

Which anticongestant does not work when adminstered orally?

A

Phenylephrine (doesn’t work reliably)

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

How does PPA increase Blood Pressure?

A

It is an indirect agonist

Stimulates Beta1 receptors on the heart

Stimulates Alpha1 receptors in vessels*

*might have affinity for alpha 1 (increases bp but doesn’t effect heart

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

Phenylephrine was ineffective - why?

A

Acts on alpha1 receptors, however… reflex bradycardia? Something else?

19
Q

Why was PPA banned?

A

Stroke (hemorrhagic)

Heart attack

(young women would take megadoses to lose weight)

20
Q

What can direct alpha1 receptor stimulation cause (4)

A
  • hypertension
  • Stroke
  • insomnia/nervousness
  • Loss of appetite
21
Q

In what context would a2 agonists be better than a1 agonists? What happens if this is not the case?

A

Better safety profile, as effective - Apply topically to nose

But also used in autoreceptors in important places - if leaked into periphery, dangerous inhibition

22
Q

What is hay fever?

A

Seasonal allergic rhinitis

23
Q

How do allergies work?

A

eg pollen enters system, specific antibodies are produced, antibodies attach to mast cells, pollen attaches to mast cells on subsequent exposure, mast cells release inflammatory mediators, allergic reaction is triggered

24
Q

How do mast cells illicit an allergic response? (2 ways)

A
  • Releasing histamine which acts on H1 receptors
  • Releasing inflammatory mediators which act on (among other things) leukotriene receptors
25
Q

True/False? Leukotriene receptor antagonists are as effective as H1-blockers for allergic rhinitis

A

True/False? Leukotriene receptor antagonists are as effective as H1-blockers for allergic rhinitis

26
Q

Which histamine receptor is associated with allergenic symptoms? (H1/H2)

A

Which histamine receptor is associated with allergenic symptoms? (H1/H2)

H2 is associated with ulcers (found in gut)

27
Q

What is the difference between the two generations of H1 receptor blockers? Name two examples of each

A

1st Generation: sedating

  • Diphenhydramine (benadryl)
  • Chlorpheniramine

2nd Generation: non-sedating

  • Terfenadine
  • Hismanal
28
Q

Should you take an antihistamine if you have a cold? Why/why not?

A

No, different system affected, no clear effect

During a cold, kinin levels increase but not histamine levels

29
Q

Why is terfenadine non-sedating?

A

Drug doesn’t reach brain in concs sufficient enough to cause sedation (but saturates periphery)

Drug still gets into brain, just not enough to make you sleepy

30
Q

How do we know it wasn’t a matter of getting the dose right for terfenadine not causing sedation?

A

Complete saturation was observed in periphery

31
Q

Why doesn’t terfenadine cause sedation when it reaches the brain?

A

Acts competitively on the brain (if it reaches the brain)

designed NOT to reach brain

32
Q

What is the differnce in response cuve for chlorpheniramine and terfenadine?

A

Chlorpheniramine: Rapid onset, reversible

Terfenadine: slow onset, irreversible(?)

33
Q

What are spare receptors?

A

Receptors that are not bound to drug when cell is exhibiting maximum response

34
Q

Why does terfenadine not have a standard dose/response curve?

A

It occupies spare receptors

35
Q

Is terfenadine sedating?

A

No

36
Q

What are terfenadine’s heart interactions?

A

Certain drugs/grapefruit can pause terfenadine metabolism, and too much terfenadine can act on the heart and cause ventricular arrhytmia

37
Q

What are possible side effects of H1 antagonists? (6)

A
  • Muscarinic block (dry mouth, alleviates motion sickness)
  • Na Channel block (local anesthetic)
  • Alpha1 block (postural hypotension)
  • Competition for hepatic microsomes (drug interactions)
  • Allergies (some people are allergic to the drug)
  • CNS H1 block (sedation)
38
Q

What are possible side effects of second generation H1 antagonists?

A
  • Competition for hepatic microsomes (drug interaction)
39
Q

What is a new type of drug that’s more effective than antihistamines?

A

Glucocorticosteroid inhalers (not immediate, slow onset)

40
Q
A
41
Q

Are antihistamine drugs 100% effective? Why/Why not?

A

No, because mast cells release lots of other “inflammatory mediators”

42
Q

What is a scatchard plot?

A

Plot of bound/unbound ratio over drug conc

43
Q
A