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Pulmonology > Pharm - Cough Suppressants Decongestants, Mucolytics > Flashcards

Pharm - Cough Suppressants Decongestants, Mucolytics Flashcards

1
Q

what is the physiological definition of a cough? and definitions of phases

A

3 phase expulsive motor act
1 - inspiratory phase
2 - compressive phase - forced expiratory effort against a closed glottis
3 - expulsive phase - opening of glottis and rapid expiratory outflow

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2
Q

what is the clinical definition of a cough

A

forced expulsive maneuver, usually against a closed glottis, which is associated with a characteristic sound

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3
Q

define acute cough

A

one lasting less than 3 weeks

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4
Q

define subacute cough

A

one lasting 3 to 8 weeks

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5
Q

chronic cough

A

one lasting greater than 8 weeks

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6
Q

what are the nonpharmacologic treatment modalities for cough?

A
  • eliminating irritants
  • hard candies such as Jolly Ranchers (stay so hard, you can suck me for a long time, oh muh gah)
  • Lozenges
  • Humidifiers, or vaporizers
  • Hydration
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7
Q

what are the 2 broad categories of pharmacological treatment options for cough

A

1 - antitussives

2 - expectorants

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8
Q

when are antitussives the drug of choice? (what type of cough)

A

nonproductive cough

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9
Q

when are expectorants the drug of choice?

A

productive cough w/ thick secretions

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10
Q

what are the 3 systemic antitussive agents

A

Dextromethorphan
Diphenhydramine
Codeine

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11
Q

what are the 2 topical antitussive agents

A

Camphor

Menthol

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12
Q

what is the only FDA approved expectorant

A

Guaifenesin

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13
Q

what is the MOA of dextromethorphan?

A

suppresses the cough reflex by a direct action on the cough center in the medulla of the brain

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14
Q

what is dextromethorphan metabolized into and by what enzyme? what is the activity of this new product?

A

it is metabolized into dextrorphan by CYP2D6

dextrorphan is as active as the parent drug

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15
Q

what is dextromethorphan’s potency and relation to opiods

A

it is a non opiod, but has equal potency to codeine

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16
Q

what are the other actions of dextromethorphan and dextrorphan? why is this important?

A

they increase levels of serotonin
this increase in serotonin levels contributes to the ability to abuse this drug - it causes dissociative hallucinogenic effect at 12 to 75 times the TD

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17
Q

How is dextromethorphan protected in a pharmacy? wht age restrictions?

A

it must be kept behind the counter, must show ID to purchase it
18 in most states
21 in Mississippi (for obvious reasons)

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18
Q

what are the side effets of dextromethorphan?

A

dizziness, drowsiness, nauseau, upset stomach, vomiting, diarrhea, irritability, excitability, light headedness, and trouble sleeping

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19
Q

what is the major contraindication for dextromethorphan?

A

Monoamine oxidase inhibitor antidepressants - cause really high levels of serotonin - can cause convulsions and cardiac arrest

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20
Q

what are some other contraindications for dextromethorphan?

A

advanced respiratory insufficiency or hepatic disease

and if the pt is allergic to any ingredients of the product

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21
Q

how can you remember that dextromethorphan is contraindicated w/ MAOIs?

A

the Libby Zion story - she was on antidepressants, became sick, checked into hospital, residents prescribed her some codeine like drug, and she died b/c of cardiac arrest
Dad sued, now we have restrictions on number of hours residents can work each week

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22
Q

Diphenhydramine has 3 MOAs, what are they?

A

1) antihistamine-H1 receptor antagonist
2) suppresses the cough reflex by a direct effect on the cough center
3) antitussive effects due to its anticholinergic / antimuscarinic effects

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23
Q

what line therapy is Diphenhydramine for nonproductive cough caused by irritation? what are some of its other common uses?

A

2nd line

common cold, allergic rhinitis, chronic urticaria, motion sickness, parkinsonism, insomnia

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24
Q

what are the side effects of diphenhydramine? they are sort of in 2 categories based on the diff MOA

A

drowsiness and respiratory depression - due to direct effect in the brain
blurred vision, dry mouth, urinary retention, constipation - due to anticholinergic, antimuscarininc effects

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25
Q

What are the contraindications for diphenhydramine? again, these are in categories based on MOA

A

prostate hypertrophy, urinary obstruction, peptic ulcer - b/c of antimuscarinic effects
Asthma, COPD - b/c of depression of respiration
MAOIs - again, serotonin syndrome / toxicity

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26
Q

what is codeine - what does it do and what is it related to?

A

an opiod analgesic and antitussive related to morphine

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27
Q

what receptors does codeine act on

A

acts on mu receptors

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28
Q

compare the affinity of codeine and morphine for the mu receptor

A

codeine has a lower affinity than morphine for the mu receptor

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29
Q

what is the MOA of Codeine

A

it depresses the cough reflex by a direct action on the cough center in the CNS

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30
Q

what happens to Codeine in metabolism

A

about 10% of codeine is metabolized (by CYP2D6) to morphine and other products - individuals w/ high level of this enzyme will build up more morphine

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31
Q

what are the side effects of Codeine (think about MOA - it has side effects in common w/ other 2 antitussives)

A

constipation, sedation, respiratory depression (all the opiods do this) - result of action in CNS
histamine release, vasodilatoin, orthostatic hypotension, and dizziness

32
Q

what are the contraindications for Codeine?

A

hypersensitivity, labor of premature birth, pregnancy category C, prostatic hypertrophy, individuals on sedatives, in patients with acute respiratory depression, asthma or COPD, following tonsillectomy and or adenoid surgery

33
Q

What is the MOA of the topical agent Camphor?

A

it activates the TRPV1 and TRPA1 channels on the cough receptor afferent nerves, intially activates them and then desensitizes them

34
Q

what is the MOA of the topical agent menthol?

A

it acts on TRPM8 channels, initially activating then desnsitizing them

35
Q

is Guaifenesin used for chronic cough?

A

no

36
Q

what is Guaifenesin used for?

A

symptomatic relief of ineffective productive coughs - chest congestion

37
Q

what is the MOA of Guaifenesin?

A

loosens and thins lower respiratory trat secretions by increasing the volume and reducing the viscosity of secretions

38
Q

What is Guaifenesin used for in veterinary medicine, and why?

A

it is used to induce and maintain anesthesia in horses in llama
it does not have any analgesic effect, it simply causes muscle relaxation
because the horses and llamas have a violent reaction to the analgesics like propofol and others

39
Q

what are the side effects of Guaifenesin

A

dizziness, dry mouth, rash, diarrhea, drowsiness, nausea, vomiting, stomach pain, diarrhea, uric acid nephrolithiasis (in large doses)*

40
Q

what is contraindication for Guaifenesin

A

hypersensitivity

41
Q

what are the nasal decongestants? how do they affect histamine? what are they commonly formulated with?

A

vasoconstrictive drugs that reduce nasal decongestion
they do not affect release of histamine or any other mediators involved in the allergic reaction
commonly formulated with antihistamines

42
Q

what is the MOA of nasal decongestants

A

alpha-adrenergic agonist (sympathomimetic) - constricts blood vessels throughout the body

43
Q

what is the effect of nasal decongestants

A

reduces supply of blood to the nose
decreases the amount of blood in the sinusoid vessels
decreases mucosal edema

44
Q

what is a direct acting alpha antagonist used as a nasal decongestant?

A

Phenylephrine

45
Q

what is the MOA of pseudoephedrine?

A

indirectly acting sympathomimetic - it binds presynaptic terminal, causes NE to be released into the synaptic cleft
(same moa as ampehtamine)

46
Q

How is PE metabolized?

A

rapidly by MAO (Monoamine oxidase) and COMT (catechol-O-methyl transferase) in the GI mucosa, liver, and other tissues - does not have long duration of aciton

47
Q

How is Pseudoephedrine metabolized?

A

only to a minor extent, by N-demethylation to norpseudoephedrine

48
Q

between Pseudoephedrine and Phenylephrine, which one gets into the brain better?

A

pseudoephedrine - it has longer duration of action, and it is not metabolized by MAO

49
Q

which between pseudoephedrine and phenylephrine has a better bioavailability?

A

pseudoephedrine

but both have a short half life

50
Q

what are the side effects of phenylephrine?

A

can increase BP at high doses, will see reflex bradycardia b/c phenylephrine has no effects on B receptors in heart

51
Q

what are the side effects of Pseudoephedrine

A

Pseudoephedrine induces the release of NE so it activates everything
CV stimulation: increase BP, tachycardia, palpitation, arrhythmias
CNS stimulation: restlessness, insomnia, anxiety, tremors, fear, or hallucinations

52
Q

which pt populations are most likely to experience the side effects of systemic decongestants?

A

children and elderly

53
Q

what are two effects that can result from overuse of the systemic decongestants?

A

1) can cause infection due to vasoconstriction and inability to clear bacteria
2) rebound congestion - ischemia as a result of local vasoconstriction or local irritation by the drug

54
Q

what are two notable precautions or contraindications for phenylephrine use and why

A

1) bradycardia - due to the reflex increase in vagal tone because of PE
2) heart block - again, due to the increase vagal tone

55
Q

what is one major contraindication for pseudoephedrine and why

A

hyperthyroidism - hyperthyroidism causes increase in expression of beta adrenergic receptors - never give medication to a pt w/ hyperthyroidism that will increase NE - this will lead to heart problems

56
Q

what are two other precautions and contraindications for the use of systemic decongestants

A

uncontrolled HTN

ventricular tachycardia

57
Q

what is an alpha agonists that is used as a topical spray nasal decongestant? available OTC

A

oxymetazoline

58
Q

what is the MOA of oxymetazoline?

A

direct alpha 1 adrenergic agonist

59
Q

what are two other drugs that have similar MOAs as amphetamine (increase release of NE) and thus have the potential for abuse?

A

Levamfetamine

Benzedrex

60
Q

what effect does amphetamine have at high doses?

A

hallucinogenic

61
Q

Mucolytics are used in diseases where there is increased mucus production - some examples are

A

cystic fibrosis
COPD
Bronchiectasis
Respiratory infections - TB

62
Q

what are 4 non-pharmacologic ways to facilitate mucus clearance

A

provide adequate hydration
remove causative factors
optimize tracheobronchial clearance
reduce inflammation

63
Q

what are 4 examples of expectorants?

A

Iodinated glycerol
Guiafenesin
Bromohexine
N-acetyl cysteine

64
Q

what is the MOA of iodinated glycerol

A

promote the production of serosal fluid that is more watery

65
Q

what is the MOA of bromohexine?

A

secretolytic, increases the production of serous mucous in the respiratory tract and decreases the viscosity of phlegm

66
Q

what is the MOA of N-acetyl cysteine

A

breaks the disulfide bonds by substituting a sulfhydryl radical

67
Q

what is a side effect of N-acetyl cysteine

A

bronchospasm

68
Q

what are the 5 mucolytics we talked about?

A

1) N-acetyl cysteine
2) Sodium Bicarbonate
3) Dornase alfa (pulmozyme)
4) amiloride
5) Denufosol Tetrasodium

69
Q

what do we need to know about sodium bicarbonate (MOA)?

A

it is a 2% sodium bicarb solution - used to increase the pH of mucus by weakening carbohydrate side chains

70
Q

what is the MOA of Dornase Alfa?

A

it is a DNAse enzyme that digest extracellular DNA - it reduces viscosity of secretion during an infection this way

71
Q

what are the indications for Dornase Alfa (pulmozyme)?

A

used in cystic fibrosis, chronic bronchitis, or bronchietasis

72
Q

what is an important point about dornase alfa, i.e. when won’t it work?

A

has no effect on non-infected sputum

73
Q

what are the side effects of pulmozyme (dornase alfa)?

A

voice alteration, pharyngitis/laryngitis, rash, chest pain, conjunctivitis

74
Q

what is the contraindication of Pulmozyme (dornase alfa)?

A

pts hypersensitive to Chinese Hamster Ovary cell products (Abteen)

75
Q

what is the MOA and indication for amiloride

A

diuretic that can be given by aerosol for pts w/ cystic fibrosis

76
Q

when is amiloride not very effective

A

bronchial asthma

77
Q

what is the MOA of Denufosol Tetrasodium? make note of which receptors it activates

A

enhances mucosal hydration and mucus clearance by activating Cl- secretion and inhibiting epithelial Na+ transport via activation of P2Y2 receptors (the same receptors as for ATP)

Pulmonology (31 decks)

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