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Pulmonology > Pharm - Cough Suppressants Decongestants, Mucolytics > Flashcards

Pharm - Cough Suppressants Decongestants, Mucolytics Flashcards

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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
What are the contraindications for diphenhydramine? again, these are in categories based on MOA
prostate hypertrophy, urinary obstruction, peptic ulcer - b/c of antimuscarinic effects Asthma, COPD - b/c of depression of respiration MAOIs - again, serotonin syndrome / toxicity
26
what is codeine - what does it do and what is it related to?
an opiod analgesic and antitussive related to morphine
27
what receptors does codeine act on
acts on mu receptors
28
compare the affinity of codeine and morphine for the mu receptor
codeine has a lower affinity than morphine for the mu receptor
29
what is the MOA of Codeine
it depresses the cough reflex by a direct action on the cough center in the CNS
30
what happens to Codeine in metabolism
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
31
what are the side effects of Codeine (think about MOA - it has side effects in common w/ other 2 antitussives)
constipation, sedation, respiratory depression (all the opiods do this) - result of action in CNS histamine release, vasodilatoin, orthostatic hypotension, and dizziness
32
what are the contraindications for Codeine?
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
What is the MOA of the topical agent Camphor?
it activates the TRPV1 and TRPA1 channels on the cough receptor afferent nerves, intially activates them and then desensitizes them
34
what is the MOA of the topical agent menthol?
it acts on TRPM8 channels, initially activating then desnsitizing them
35
is Guaifenesin used for chronic cough?
no
36
what is Guaifenesin used for?
symptomatic relief of ineffective productive coughs - chest congestion
37
what is the MOA of Guaifenesin?
loosens and thins lower respiratory trat secretions by increasing the volume and reducing the viscosity of secretions
38
What is Guaifenesin used for in veterinary medicine, and why?
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
what are the side effects of Guaifenesin
dizziness, dry mouth, rash, diarrhea, drowsiness, nausea, vomiting, stomach pain, diarrhea, uric acid nephrolithiasis (in large doses)*
40
what is contraindication for Guaifenesin
hypersensitivity
41
what are the nasal decongestants? how do they affect histamine? what are they commonly formulated with?
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
what is the MOA of nasal decongestants
alpha-adrenergic agonist (sympathomimetic) - constricts blood vessels throughout the body
43
what is the effect of nasal decongestants
reduces supply of blood to the nose decreases the amount of blood in the sinusoid vessels decreases mucosal edema
44
what is a direct acting alpha antagonist used as a nasal decongestant?
Phenylephrine
45
what is the MOA of pseudoephedrine?
indirectly acting sympathomimetic - it binds presynaptic terminal, causes NE to be released into the synaptic cleft (same moa as ampehtamine)
46
How is PE metabolized?
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
How is Pseudoephedrine metabolized?
only to a minor extent, by N-demethylation to norpseudoephedrine
48
between Pseudoephedrine and Phenylephrine, which one gets into the brain better?
pseudoephedrine - it has longer duration of action, and it is not metabolized by MAO
49
which between pseudoephedrine and phenylephrine has a better bioavailability?
pseudoephedrine | but both have a short half life
50
what are the side effects of phenylephrine?
can increase BP at high doses, will see reflex bradycardia b/c phenylephrine has no effects on B receptors in heart
51
what are the side effects of Pseudoephedrine
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
which pt populations are most likely to experience the side effects of systemic decongestants?
children and elderly
53
what are two effects that can result from overuse of the systemic decongestants?
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
what are two notable precautions or contraindications for phenylephrine use and why
1) bradycardia - due to the reflex increase in vagal tone because of PE 2) heart block - again, due to the increase vagal tone
55
what is one major contraindication for pseudoephedrine and why
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
what are two other precautions and contraindications for the use of systemic decongestants
uncontrolled HTN | ventricular tachycardia
57
what is an alpha agonists that is used as a topical spray nasal decongestant? available OTC
oxymetazoline
58
what is the MOA of oxymetazoline?
direct alpha 1 adrenergic agonist
59
what are two other drugs that have similar MOAs as amphetamine (increase release of NE) and thus have the potential for abuse?
Levamfetamine | Benzedrex
60
what effect does amphetamine have at high doses?
hallucinogenic
61
Mucolytics are used in diseases where there is increased mucus production - some examples are
cystic fibrosis COPD Bronchiectasis Respiratory infections - TB
62
what are 4 non-pharmacologic ways to facilitate mucus clearance
provide adequate hydration remove causative factors optimize tracheobronchial clearance reduce inflammation
63
what are 4 examples of expectorants?
Iodinated glycerol Guiafenesin Bromohexine N-acetyl cysteine
64
what is the MOA of iodinated glycerol
promote the production of serosal fluid that is more watery
65
what is the MOA of bromohexine?
secretolytic, increases the production of serous mucous in the respiratory tract and decreases the viscosity of phlegm
66
what is the MOA of N-acetyl cysteine
breaks the disulfide bonds by substituting a sulfhydryl radical
67
what is a side effect of N-acetyl cysteine
bronchospasm
68
what are the 5 mucolytics we talked about?
1) N-acetyl cysteine 2) Sodium Bicarbonate 3) Dornase alfa (pulmozyme) 4) amiloride 5) Denufosol Tetrasodium
69
what do we need to know about sodium bicarbonate (MOA)?
it is a 2% sodium bicarb solution - used to increase the pH of mucus by weakening carbohydrate side chains
70
what is the MOA of Dornase Alfa?
it is a DNAse enzyme that digest extracellular DNA - it reduces viscosity of secretion during an infection this way
71
what are the indications for Dornase Alfa (pulmozyme)?
used in cystic fibrosis, chronic bronchitis, or bronchietasis
72
what is an important point about dornase alfa, i.e. when won't it work?
has no effect on non-infected sputum
73
what are the side effects of pulmozyme (dornase alfa)?
voice alteration, pharyngitis/laryngitis, rash, chest pain, conjunctivitis
74
what is the contraindication of Pulmozyme (dornase alfa)?
pts hypersensitive to Chinese Hamster Ovary cell products (Abteen)
75
what is the MOA and indication for amiloride
diuretic that can be given by aerosol for pts w/ cystic fibrosis
76
when is amiloride not very effective
bronchial asthma
77
what is the MOA of Denufosol Tetrasodium? make note of which receptors it activates
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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