Pharmacotherapy of the Upper Airway Flashcards Preview

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Flashcards in Pharmacotherapy of the Upper Airway Deck (17):

State whether activation of the following receptors leads to vasodilation or constriction:

  1. Muscarinic
  2. Histamine
  3. Bradykinin
  4. Alpha 1 Adrenergic

  1. Muscarinic: dilation
  2. Histamine: dilation
  3. Bradykinin: dilation
  4. Alpha 1 Adrenergic: constriction

**Dilations lead to congestion and rhinorrhea 

**Activation of the A1 adrenergic will override any negative dilations from other pathways


Which pathway is targeted by allergies?

H1 Histaminic


Which pathway is targeted by a cold?



The blocking of voltage sensitive sodium channels by 1st generation antihistamines has what effect?

Local anesthetic


T/F: 2nd generation antihistamines have a greater antagonistic effect on histamine receptors


About the same (or worse), they just avoid the sedative effect on the CNS


Which forms of rhinitis are best targeted by antihistamines? By decongestants?

Antihistamines: Allergic rhinitis

Decongestants: Viral rhinitis (also some allergic)


The primary use of antihistamines is to block receptor mediated effects of endogenous histamines.  These effects of histamine include all of the following EXCEPT:




D.Stimulation of afferent pain neurons

E.Increased capillary permeability (edema)

F.Contraction of GI tract smooth muscle (cramping)

B, C


Which of the following drugs is the most effective physiologic antagonist of histamine in smooth muscle?







B, D


**If someone is going into shock from histamine reaction- you give them epi

**Antihistamines, while effects are additive with epinephrine, are not sufficient alone for treatment


What's the difference between 1st generation/ 2nd generation antihistamines?

1st generation

  • CNS action: prevents nausea, vomiting, insomnia (sleep aid)
  • drying effect (mouth)
  • Cough suppression- Na channel block

2nd generation

  • Longer duration of action, 
  • very specific, only block H1
  • don't act on CNS (no sedation)
  • no antiemetic effects
  • no anticholinergic 


3.  Which of the following statements concerning clinical use of antihistamines is FALSE?

A.Can be used to produce a local anesthetic-type effect

B.Drugs of choice for treatment of allergic rhinitis

C.Overuse associated with rebound congestion

D.Commonly used in treating motion sickness

E.Antimuscarinic sedative effects of diphenhydramine are utilized in OTC sleep aid products

F.More effective than pseudoephedrine for viral cold symptoms

C, F


A 20-year-old woman is taking diphenhydramine for severe hay fever symptoms. Which of the following adverse effects is she most likely to report?

A.Increase in bladder tone

B.Dry mouth

C.Nervousness, anxiety


E.Uterine cramps



B, F


Select the TRUE statement comparing 1st generation antihistamines (diphenhydramine / Benadryl) to 2nd generation antihistamines (loratadine / Claritin):

A. 2nd generation agents are less expensive

B. 2nd generation agents are more effective at blocking histamine receptors

C. 2nd generation agents are not effective in the OTC treatment of insomnia

D. 1st generation agents are less likely to cause sedation

E. 1st generation agents produce less antimuscarinic side effects

F. 1st generation agents are effective in the OTC treatment of insomnia

C, F


What's the difference in action between the decongestants Pseudoephedrine (Sudafed) and Phenylephrine (Sudafed PE)?

Psuedoephedrine: indirectly stimulates alpha1 receptor by increasing NE

Phenylephrine: direct stimulation to alpha1 receptor


TRUE statements regarding pseudoephedrine include:

A.Effective against rhinorrhea and congestion due to allergies

B.Overuse associated with rebound congestion

C.Postural hypotension can be seen with higher doses

D.Greater decongestant efficacy than topical phenylephrine

E.More reliable oral bioavailability than phenylephrine

F.Agonist at alpha-1 adrenergic receptors

G.More effective antitussive agent than dextromethorphan

H.Increases neuronal release of NE

A. True

B. False (topical agents)

C. False- A1 receptor blocker (promethazine)

D. False

E. True

F. False (indirect agonist)

G. False

H. True


What medication is used as an antitussive?

Dextromethorphan (in Robitussin)

  • Antitussive dose:  15-30 mg via block of μ-opioid
  • Drug abuse dose:  > 500-1500 mg – via block of NMDA glutamate receptors 


TRUE statements regarding management of cough symptoms include:

A.Upper airway cough syndrome can be managed with loratadine and pseudoephedrine

B.Cough suppressants should always be used in conjunction with expectorants

C.An NSAID like naproxen may be of benefit in coughs due to common cold viruses

D.Codeine has greater antitussive efficacy and less dependence liability than dextromethorphan

E.Antihistamines are generally more effective as antitussives than opioid receptor agonists



What are the guidelines for treatment of cough in adults?

Acute cough due to common cold

  • 1st generation antihistamine/decongestant (e.g., brompheniramine / pseudoephedrine)
  • Naproxen (tid x 5 days): blocks inflammation that stimulates cough afferents
  • Other
    • Antitussives show mixed results
    • Zinc not recommended
    • 2nd generation antihistamines ineffective

Acute cough due to upper airway cough syndrome (postnasal drip)

  • 1st generation antihistamine/decongestant (e.g., brompheniramine / pseudoephedrine)