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Flashcards in HENT Deck (124):
1

What are decongestants?

alpha agonists that produce vasoconstriction

2

What does the vasoconstriction of decongestants result in?

-shrinkage of swollen nasal mucous membranes
-reduces nasal congestion and increases drainage of sinus secretions
-makes it easier to breathe
-help nasal stuffiness

3

How can decongestants be applied?

-topical OTC
-systemic (oral) OTC & Rx

4

What do decongestants stimulate (MOA)?

-stimulate alpha 1 adrenergic receptors in the nasal mucosa, constricting BVs

5

How does the vasoconstriction of decongestants decrease congestion?

-decrease blood flow to nasal mucosa
-less blood flow means less edema of mucosal passages
-less edema means less congestions
=more air passage through airways

6

Rate of absorption/onset of topical nasal decongestants

-absorbed quickly
-rapid onset of action

7

topical vs. oral decongestants:
-which one is more effective?

topical application of decongestants tend to be more effective compared to PO

8

topical vs. oral decongestants:
-which one has a longer effect?

-topical effect generally lasts longer than oral

9

topical vs. oral decongestants:
-which one is more effective and
-what are the benefits

-the topical route allows more of the drug to get where you want it
-with less systemic absorption
-and fewer side effects

10

How are topical nasal decongestants used? (dose and where)

1 to 2 sprays in each nostril every 12 hours

11

patient education about topical nasal decongestants

-keep applicator CLEAN
-spray & breath in
-don't let it drip down back of throat

12

Why don't you want nasal decongestants to drip down the back of the throat?

-can get systemic absorption and ADRs

13

It's difficult to prevent topical nasal decongestants from dripping down the back of the throat.
-What do you have to do because of this?

-If there is a contraindication to using PO decongestants, then nasal decongestants are contraindicated as well

14

Local ADRs of topical decongestants

-stinging, burning, dryness of mucous membranes in the nose
-rhinitis medicamentosa

15

What is rhinitis medicamentosa

-special ADR for topical decongestants
-happens >3-5 days use then you try to stop
-when you stop you get rebound congestion, often worse

16

tx of rhinitis medicamentosa

oral decongestans & nasal corticosteroids

17

Systemic ADRs of topical decongestants

-increased BP
-increased blood sugar
-increased intraocular pressure
-chest pain
-difficulty urinating

18

What causes the systemic ADRs of topical decongestants

-activation of adrenergic alpha receptors

19

Contraindications for topical decongestants

-CAD
-htn
-hyperthyroid
-DM
-narrow angle glaucoma
-BPH

20

Why is CAD (coronary artery disease) a contraindication for topical decongestants?

can increase rate & work of heart, increasing anemia

21

Why is HTN a contraindication for topical decongestants?

can increase BP

22

Why is Hyperthyroid a contraindication for topical decongestants?

can increase sx of hyperthyroidism

23

Why is DM (diabetes) a contraindication for topical decongestants?

metabolic effects can increase blood sugar

24

Why is narrow angle glaucoma a contraindication for topical decongestants?

can acutely close the angle in the eye causing acute angle closure glaucoma

25

Why is BPH (benign prostatic hypertrophy) a contraindication for topical decongestants?

cause urinary retention

26

Oral decongestants are less effective than topical, but what is their benefit?
their downside?

benefit: can use for longer period of time because don't get rebound effect
downside: more side effects

27

What receptor effects do oral decongestants have?

alpha (and maybe some beta)
-going for alpha 1 receptor effect

28

Which oral decongestant has more beta effects?

Pseudoephedrine (PSE)

29

What side effects do you see with PSE because of its beta receptor effect

-tachycardia
-increase BP
-insomnia due to CNS stimulation

30

examples of decongestants

-PSE
-phenylephrine

31

Why is PSE sold behind the counter?

Jonas making meth

32

ADRs of oral decongestants

CNS stim keeps you awake so don't take within 4-6h before bed
HTN-risk of stroke, (hx of stroke then don't give)
Palpitations - symp stim increases HR

33

_______ of nasal passages occurs frequently with many ENT diseases (what type of drug does this relate to?)

inflammation of nasal passages (where steroids come into play)

34

MOA of nasal corticosteroids

-nasal steroids suppress inflammation in the nasal passages
-decreases intracellular edema & nasal discharge produced by irritation
-making it easier to breath
-and reducing a runny nose

35

How long do you need to use nasal corticosteroids to see peak effect?
why?

-hormones take longer to work
-use 2-3 weeks for peak effect
-don't work fast but work VERY well/ very effective

36

OTC topical decongestant nasal sprays (list)

-oxymetazoline (Afrin)
-Xylometazoline (Otrivin)
-Phenylephrine (Neo-Synephrine)
-Naphazoline (Privine)

37

Rx only topical decongestant nasal spray (list)

Tetrahydrozoline (Tyzine)

38

List common topical nasal steroids

-Fluticasone (Flonase & Veramyst)
-Beclomethasone (Vancenase, Beconase)
-Triamcinolone (Nasacort, Nasacort AQ)
-Budesonide (Rhinocort)
-Mometasone (Nasonex)
-Ciclesonide (Omnaris)
-Flunisolide (Nasalide)

39

Dose of topical nasal steroids

-1 to 2 sprays in each nostril twice per day

40

Make sure the patient can ______ before giving nasal steroids.
Why?

-Make sure patient can inhale before giving nasal steroids
-if no air going through nose, meds can't get far either

41

If pt. has poor nasal patency, what do you give them and why?

-give normal saline
-will quickly & temporarily decrease edema to allow increased air flow so medication can get in

42

No ________ or _________ for 10 mins after inhalation of nasal steroids
why?

no sneezing or blowing
-may blow med out

43

Local ADRs of topical nasal steroids

-stinging, HA, nose bleeds

44

Why do nose bleeds sometimes occur in topical nasal steroids

dry membranes

45

systemic ADRs of topical nasal steroids

-not many systemic effects because giving topically
-concern is mild growth suppression in children

46

Contraindications for topical nasal steroids

-ulceration of nasal septum
-recent nose surgery
-trauma
All because steroids cause poor wound healing

47

Functions of histamine

1. immediate allergic & inflammatory rxns
2. Gastric acid secretion
3. CNS - stim nerve endings that case pain & itch
-make sleepy and stimulate some cholinergic receptors

48

Which receptors in skin and mucous membranes are involved with histamine?

H1
-cause vasodilation leading to heat, redness, inflammation

49

_____ receptors are in gastric mucosa
And what do the blockers do

H2
H2-blockers reduce gastric acid secretion

50

Where are H1 receptors located?

smooth muscle, endothelium & brain

51

H1 blockers are used in...

allergic conditions to decrease itch & inflammatory response to allergic conditions

52

Effects of 1st generation H1 receptor antagonists

-strong sedative effect & more anticholinergic effects
-because they get into the CNS (where there are H1 receptors)

53

2nd generation H1 antagonists don't get into the _____ as well
-so how are effects different from 1st gen

don't get into CNS as well
-less sedating
-less anticholinergic
than 1st generation

54

1st Generation Anti Histamines are also called

non-selective antihistamines
or
sedating antihistamines

55

List of 1st Gen AntiHistamines

-Diphenhydramine (Benadryl)
-Chlorpheneramine (Chlortrimeton)
-Brompheneramine (Borvex)
-Clemastine (Tavist)
-Azaelastine (Astelin Nasal Spray)
-Meclizine (Antivert)
-Dimenhydrinate (Dramamine)
-Doxepin (Silenor)
-Hydroxyzine (Atarax/Vistaril)
-Promethazine (Phenergan)

56

2nd Generation AntiHistamines are also called

peripherally selective (periphery, not CNS)
or
non sedating antihistamines

57

List 2nd Gen AntiHistamines

-Cetirizine (Zyrtec)
-Levalcetirizine (Xyzal)
-Fexofenadine (Allegra)
-Loratidine (Claritin)
-Desloratidine (Clarinex)

58

Pharmacokinetics
What speed/absorption are antihistamines

-both 1st and 2nd gen rapidly and well absorbed orally

59

Pharmacokinetics
How are antihistamines distributed throughout body?

-widely distributed throughout body
-except 2nd gen b/c don't get into CNS & don't cause sleepiness

60

How long do antihistamines work?

1st gen- 4-6h
2nd gen- 12-24h

61

Pharmacodynamics (MOA)
antihistamines

-H1 antagonists
-bind receptor & block effect of native histamine

62

What receptors do histamine have primary effect on?
Why do they have effects on other receptors?

-primary effect on H1 receptors
-structurally similar to drugs that block other receptors so have effects on other receptors (muscarinic, alpha, serotonin)

63

Effects common to anti-histamines (three effects that may be desired or side effects)


-sedation
-anti nausea and anti emetic
-anticholinergic

64

Sedative Effect of Anti Histamine
-mostly which generation?

-1st gen because penetrate CNS
-sometimes with 2nd gen, but less since less gets into CNS

65

Sedative effect of anti histamine can be ____ or not _____
-example/explain

desired or not desired
-OTC sleep aids are non addicting antihistamines

66

Example of not getting desired effect of sedative anti histamine

-sometimes children get excited with 1st gen antihistamines instead of getting sedated

67

Which generation of antihistamines can decrease nausea, vomitting, & dizziness

-1st gen better than 2nd gen
-work well for nausea/vom from vestibular dysfxn (motion sickness)

68

What drug is especially good for dizziness/disequilibrium

Meclizine (Antivert)

69

What drug is good for nausea

Promethazine (Phenergan)

70

ADRs of Antihistamines related to muscarinic effects

-can block muscarinic receptor so cause:

-urinary retention
-blurry vision
-dryng effect (decrease nasal, salivary & lacrimal secretions)

71

Clinical uses of H1 Antagonists

-Allergic rhinitis
-Pruritis
-Vertigo/motion sickness

72

Why are antihistamines good drugs for allergic rhinitis?

-Allergic rhinitis is hypersensitivity rxn (histamine released locally in nasal passages)
-histamine is primary mediator of many allergic rhinitis sx
-so antihistamines are drug of choice

73

Why are antihistamines given in pruritic conditions

-decrease itch (histamine is major cause of pruritis)
-may decrease awareness of itch by causing sedation

74

-Why are h1 antagonists good for vertigo/motion sickness

-histamine has blocking effect in inner ear or CNS

75

Toxicity Anti-Histamines

-sedation, hallucinatins, ataxia (occur more with better penetration into CNS, more in elderly; avoid taking antihistamines when driving/operating heavy machinery or with other sedating drugs)
-anticholinergic (dry mouth, constipation, difficulty voiding)- use carefully/not at all if already glaucoma, hyperthyroid, BPH
-excitation in children

76

Special Anti-Histamine: topical nasal antihistamine

-azelastine (astelin)
-first generation antihistamine given as topical in nasal passages
-2 sprays in each nostril BID, gives rapid improvement of sx
-less effective over time

77

side effects of azelastine

-(topical nasal antihistamine)
-side effects:
-HA
-dryness
-bitter taste
-drowsiness

78

Topical Ophthalmic Antihistamines

Ketotifen (zatidor, Claritin)
-1 gtt OU BID

79

Anti tussives are used to...

decrease cough, generally do this by suppressing cough reflext

80

When would you not want to suppress a cough?
and when WOULD you consider using?

-if cough is productive, don't suppress it--get the phlegm out

-if cough is dry and nonproductive, then suppress it OR if productive cough is keeping up at night, etc

81

List Anti tussives

Oral/systemic: dextromethorphan, narcotics (codeine)

topical

82

OTC oral cough suppressant

-dextromethorphan (DM)
-chemical isomer of the narcotic methorphan
-suppresses cough without pain relief or addiction
-no drowsiness

83

What are the primary group used when giving prescription antitussives?

Narcotics

84

Why/how narcotics as cough suppressants

-have effect on cough reflex in throat & brain (work centrally & peripherally)
-often available in liquid (cough syrup)

85

Common narcotic as cough suppressant

Codeine usually 10mg at a time
Ex: phenergan with codeine, robitussin AC, Tussionex

86

Topical Antitussives

-OTC
-Camphor & menthol
-rubbed on throat/chest & inhaled (vicks)
-also available as lozenge & throat sprays

87

MOA of topical antitussives

-stimulate cold sensory receptors and give sensation of cooling and local anesthetic effect that decreases cough

88

Mucolytic aka

Expectorant

89

What do expectorants do?

help bring up secretions

90

List mucolytics

**guaifenesin is only one
-Mucinex, Mucinex DM, Mucinex D

91

Uses & side effects of Guaifenesin

-used for productive cough to bring up phlegm more easily
-OTC, drink 8 oz water with it
-well tolerated w/few & mild side effects

92

Mast Cell Stabilizers

Cromolyn sodium (Nasalcrom)

93

Indications for mast cell stabilizers

-allergic rhinitis

94

When do mast cell stabilizers work best?

BEFORE symptoms, work best at preventing allergic rhinitis symptoms
-(once the mast cell degranulates & histamine is released, the drug really has no effect)

95

MOA of mast cell stabilizers

-stabilizes mast cells so there is no degranulation & release of histamine

96

how are mast cell stabilizers given? and how long until they start to work

topically (spray up nose)
-takes 1-2 weeks to start to work and have to take 3-4 times per day
-not very convenient or poplular

97

ADRs of mast cell stabilizers

-few, some nasal stinging & sneezing

98

What is the drug of choice for sneezing and rhinorrhea from pregnancy?

mast cell stabilizers because not absorbed so there's no risk to fetus

99

Cholinergic Blockers

Ipratropium nasal spray (atrovent)

100

MOA of cholinergic blockers
and mode of delivery

antagonize cholinergic receptors in nasal passages
(anticholinergic)
-inhibits secretions from serous and seromucous glands lining the nasal mucosa
-topical

101

indications for cholinergic blockers

dries up rhinorrhea

102

ADRs of cholinergic blockers

HA, dry nose, nose bleeds

103

Leukotriene inhibitors

-montelukast (singulair)
-zarfirlukast (accolate)

104

MOA & delivery of leukotriene inhibitors

-MOA: leukotrienes released in response to allergic rxns
-these drugs inhibit leukotrienes and decrease response in allergic/hypersensitivity rxns
-oral

105

indications for leukotriene inhibitors

-in ear, nose, & throat disease only use for allergic or seasonal rhinitis
-more of role in asthma

106

What class would you use for vertigo/motion sickness?

H1

107

What do H1 drugs suppress to treat vertigo/motion sickness?
And which drug is best?

-vestibular suppressant
-dizziness/vertigo are sx seen with vestibular dysfxn
-1st gen H1 blockers work best, Meclizine

108

Which drug effective for motion sickness?

-also a vestibular problem
-dimenhydrinate (dramamine) a sedating H1 blocker

109

What is Allergic Rhinitis

a hypersensitivity reaction up the nose and in the throat to an antigen in the air

110

Primary drugs used for allergic rhinitis

-Antihistamines (help sx of sneezing, rhinorrhea, itching, & conjuncivitis
-Decongestants for nasal congestion
-Nasal corticosteroids (treat all, but take time)

111

Second line drugs for allergic rhinitis

-Ipratropium (rhinorrhea)
-Anti tussive if dry cough
-expectorant if productive

112

How to pick H1 blocker for allergic rhinitis

-1st & 2nd gen work equally well
-1st gen cause drowsiness (good @ bedtime if trouble sleeping)
-2nd gen cause less sedation
-try one, if doesn't work, try the other

113

If using one H1 blocker for allergic rhinitis but effect wears off, what do you do?

Works but effects wear off then try a new h1 blocker
-switching groups often helps restore effectiveness

114

What do you combine for allergic rhinitis
-pros & cons of combining drugs?

-decongestant, antihistamine, antitussive together
-pros: convenient
-cons: may get exposure to drugs you don't need

115

May combine drugs for allergic rhinitis but what is better?

to just use what controls the symptoms. Look at effect of one drug and add another group if necessary

116

Cold aka

URI or viral rhinitis

117

Note about allergic rhinitis vs viral rhinitis (sx? drugs?)

-similar sx to allergic rhinitis but different pathology so
-meds work differently

118

What meds proven beneficial in colds?

decongestants and antipyretics

119

what medications might help a little for viral rhinitis/cold

antitussives, nasal steroids, ipratropium

120

Which medications don't help colds at all and may slow down improvement

antihistamines

121

Meds in sinusitis are similar to

allergic rhinitis

122

When should antihistamines be used for sinusitis?

ONLY if patient has allergic rhinitis TOO.
-if you think there is bacterial involvement, antihistamines may slow down improvement

123

Medications and sinusitis

-antihistamines only if allergic TOO
-nasal steroids help only a little
-abx only if bacterial
-don't know effect of decongestants

124

A 42 year old male presents for a “sinus infection” that just won’t go away. He has been taking a generic over the counter cough and cold preparation. On his last visit his BP was 128/78. Currently his BP is 148/96. Which of the following drug groups do you suspect is in his OTC medication?

-decongestants (he has probably been taking pseudo ephedrine)