Drugs: Respiratory OTC (3)- Melissa*** Flashcards

1
Q

Short acting selective B2 agonists (4) –when do we take them?

A

Take Asthma Meds Periodically.

  • Terbutaline
  • Albuterol
  • Metaproterenol
  • Pirbuterol

THIS IS GENIUS

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2
Q

Long acting B2 agonists (3)–When do we take them?

A

Indicated For Steady use.

  • Indacaterol
  • Formoterol
  • Salmoterol
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3
Q

Two muscarinic antagonists for COPD

A

Poor old UNCLE IPRA suffers from really bad COPD.
(Tiotropium/ Ipratropium)
*Tio = uncle in Spanish

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4
Q

Which muscarinic antagonist is used for COPD + runny nose?

A

IPratropium helps a drIPPY nose. (Administered as nasal spray)

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5
Q

Most common ADR of inhaled corticosteroids?

A

Corticosteroids Cut my vocal Cords!!!!
(Vocal cord atrophy –> dysphonia)
*prevented with use of “spacer”

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6
Q

Describe the two predominant changes that occur with in the airways of Asthmatic patients:

What drug do we use to diagnose asthma?

A
  1. ^ inflammatory cells (mast, EOS, TH2) in airway
  2. ^ bronchospastic mediators (Hist, LTD4, PGD2)

Methacholine (Musc-R antagonist) challenge is done to dx asthma

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7
Q

How do patients with asthma react to methacholine challenge?

A

asthmatic patients will have STRONGER response to methacholine challenge than healthy patients

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8
Q

Describe three airway changes associated with COPD.

A
  1. ^ neutros, MQs, CTLs –> release factors–> destroy lung & ^^ secretions
  2. fibrosis/ scarring–> narrow airways
  3. emphysema and possible a1-proteinase inhibitor deficiency (order test in early onset patients)
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9
Q

How is allergic rhinitis mediated?

A

inflammation of nasal epithelium mediated by IgE–hypersensitivity response TYPE ONE.

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10
Q

What is the best way to administer drugs to diseased airways? What are three different mechanisms by which we deliver medication this way?

A

Inhalation!

  • metered dose inhaler (propels drug into airway)
  • spacer (reduced velocity of propelled drug and catches residue to avoid thrush, etc)
  • nebulizer (delivers drug as mist)
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11
Q

By what way is it possible for inhaled drugs to cause systemic side effects?

A

Majority of the drug will be depositied on the tongue and swallowed–> first pass metabolism–> systemic effects ensue

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12
Q

What are three drugs that are given orally to treat respiratory disease?

What is one caveat to oral administration of respiratory drugs?

A
  • corticosteroids
  • adrenergic agonists
  • Theophylline (ALWAYS oral)

*Dose is necessarily higher to get therapeutic effect ! 20:1!!

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13
Q

Describe the MOA of Adrenergic agonists used to treat respiratory obstructive disease:

A

Stimulate B2-Rs–> ^cAMP–> ^ PKA–> Relax bronchial sm. muscle

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14
Q

Short Acting B2-R Agonists: (SABA)

Therapeutic use?

A
  • quick relief during asthma attack

- NOT for daily use: overuse indicates more anti-inflammatory therapy is needed (corticosteroids/ LTis)

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15
Q

Long Acting B2-R Agonists: (LABA)

Therapeutic use? Duration of action?

A
  • Taken daily for control of asthma and COPD sx

- Duration of action is 12+ hrs

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16
Q

What is the most pervasive concern associated with chronic SABA use?
List some adverse effects (4)–what makes these worse?

A

Very concerned about B2-R DOWNREGULATION

ADRs (WORSE with ORAL dose):

  1. tremor
  2. restlessness
  3. hypokalemia (stimulates sm cells to take up K+)
  4. tachycardia
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17
Q

List 4 SELECTIVE SABAs

A
  1. Albuterol
  2. Terbutaline
  3. Pirbuterol
  4. Metaproterenol

Take Asthma Meds Periodically

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18
Q

List two NONSELECTIVE SABAs:

List some important ADRs

A

Isoproterenol, Epinepherine

ADRs: tachy, arrythmia, angina (due to B1 activity)

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19
Q

Isoproterenol:
Drug class
Therapeutic use
ROA

A

NONSELECTIVE SABA

  • rarely used; treats acute asthma attack; know its a bronchodilator
  • Inhalation or sublingual tablet

no longer on the market in US

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20
Q

Epinepherine:
Drug class
Therapeutic use
ROA

A

NONSELECTIVE SABA

  • acute asthma attack, anaphylaxis
  • Inhaled or SQ/IM (anaphylaxis)
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21
Q

List the three important LABAs
What is their primary theraputic use?
What is one caveat assocated with their use?

A
  1. Salmeterol
  2. Formoterol
  3. Indacaterol (indicated for once daily use in COPD)
  • Px therapy in persistent asthma or COPD (NOT for acute asthma attack)
  • MUST be co administered with corticosteroid or LTis (will otherwise ^ mortality)
22
Q

Which LABA is indicated for once daily use in COPD?

A

INDAcaterol is INDAcated

:)

23
Q

What is the most important ADR associated with LABA use? Why are corticosteroids helpful in preventing this from happening?

A

Airway tolerance –> Down-regulation of B2Rs

Corticosteroids will ^ # of B2Rs in the airway and prevent this from happening; thus we always coadminister!

24
Q

What is the structural difference between SABAs and LABAs:

A

LABAs have extended lipophilic chain that allows them to latch on to B2R.

25
Q

1 drugs to treat asthma?

A

B2 agonists! Think of B2Rs are the asthma receptor, and think of the asthma receptor as a HELPFUL receptor…

26
Q

List two Muscarinic Antagonists.
Describe the dosing regimen for each.
What respiratory disease are these drugs primarily used to treat?

A

1 Drugs to treat COPD; Also used to treat asthma

  1. Ipratropium (4x daily)
  2. Tiotropium (1x daily)
  • Think of muscarinic receptors as the COPD receptor (BAD receptor)
  • Commonly administered in combo inhalers with albuterol and such*
27
Q

In addition to treating COPD, what is another use for ipratropium?

A

Decrease nasal discharge

IPra helps a drIPPy nose!!

28
Q

List some of the ADRs associated with muscarinic antagonists–why are they usually mild?

A

Drugs are quaternary ammonium salts–> can NOT be absorbed into blood stream–> MILD systemic ADRs:

  1. bitter taste
  2. dry mouth
  3. glaucoma (don’t spray the shit in your eye! LOL.)
29
Q

Which drug is a Methylxanthane?
What is its MOA? (4)
What is it used to treat? (2)

A

Theophylline
MOA:
1. PDEi–> ^cAMP–> relaxation of sm muscle**
2. Adenosine R ANTAGONIST–> STOP bronchocnstrxn
3. Inhibits lung inflammation
4. Promotes diaphragm contraction–> ^ Respiration

Tx:

  • Adjunct px for chronic Asthma, COPD (+ first line tx when patients are refractory)
  • Adjunct to caffeine for apnea in pre-term infants (for when you’re in NICU with Miller next week :) YAY )
30
Q

Describe the theraputic index for theophylline (low/ high?).

Describe the effects of theophylline toxicity.

A

Low therapeutic index

Dose dependent toxicity
Low dose: N/V/ HA. etc
High dose: arrhythmia + seizure

31
Q

How is Theophylline metabolized?

A

CYP1A2 in the liver–watch for inducers and inhibitors

32
Q

List 4 corticosteroids used to treat obstructive lung disease.
What is their MOA?

A
  1. Beclomethasone
  2. Triamcinolone acetate
  3. Budesonide
  4. Fluticasone Propionate

MOA: Agonize glucocorticoid receptor–> ^ # B2Rs–> ^ responseiveness to LABA/ SABAs

33
Q

Therapeutic applications (respiratory) for corticosteroids (inhaled/ PO/ IV):

A

Inhaled:

  • DOC front line therapy for persistent asthma (may take several days to work; commonly administered in combo)
  • Not as effective for COPD

PO:
- Acute asthma exacerbation

IV:
- SEVERE acute asthma exacerbation

34
Q

3ADRs assocateed with inhaled corticosteroid use?

A

1. Dysphonia (atrophy of vocal cords)

  1. Oropharyngeal candidiasis (use spacer)
  2. Cough
35
Q

Name two Leukotriene inhibitors (LTis) and describe their dosing regimen.
MOA?
Therapeutic use? (2)

A
  1. Zafirlukast (2x daily)
  2. Montelukast (1x daily)

MOA: LT1R Antagonist–> INHIB cysteLTs (C4,D4,E4)–> INHIB bronchocnstrxn + airway inflammation

Tx: Coadmin with LABA/SABA for asthma and COPD in corticosteroid intolerant patients; allergic rhinitis (montelukast)

36
Q

Zileuton:
Drug Class and MOA
Therapeutic Use + Dosing Regimen
Meatabolism?

A

MOA: Inhib 5-Lipoxygenase (RLS)–> Inhib LT synthesis
Tx: Same as Zafirlukast, Montelukast; admin 4x daily
Hepatic metabolism (CYPs)

37
Q

What are two common ADRs amongst all anti-leukotriene/LT-inhibitors?

A
  • All have some degree of hepatotoxicity

- All can inhibit CYPs and compromise metabolism of other CYP metabolized drugs

38
Q

Cromolyn, Nedocromil
MOA
Which one is still used and what is it used for?

A

Inhibit mast cell degranulation and histamine release
Cromolyn still used
Treats asthma and allergic rhinitis

39
Q
Omalizumab
MOA 
Therapeutic use
Dosing regimen
ADR
A

MOA:
Monoclonal Ab against IgE–> Inhibits IgE activation of Mast cells

Tx: Severe asthma refractory to treatment with steroids
Dosing: 2-4 weeks
ADR: Anaphylaxis

40
Q

Alpha-1 Proteinase Inhibitor
MOA
Therapeutic use

A

MOA:
Inhibits activity of elastase–> STOPS destruction of lung parenchyma

Tx: COPD patients with alpha-1-antitrypsin deficiency
A note about this deficiency: It causes PAS+ lesions in the liver. I had an Rx question on this, and because we get NO PATHOLOGY on obstructive disease, I had no idea.

41
Q

Which opioids are used to treat cough?
What is their MOA?
What are their ADRs? (4)
Important CI?

A

Hydrocodone, Codeine
MOA: LOW doses –> Suppress central medullary cough center

ADRs: Constipation, dysphoria, fatigue, addiction
CI: NOT GOOD FOR ASTHMATICS (can cause resp. depression)

42
Q

Dextromethorphan:
MOA
Therapeutic use
ADRs

A

CENTRAL NMDA-R Antagonist
Tx: cough
ADRs: Can cause CNS depression in high doses (less toxic than codeine)

43
Q

Benzonatate:
MOA
Therapeutic use

A

PERIPHERAL antagonism of vagal receptors in RT
Tx: cough
ADRs: Dizziness

44
Q

Guaifenesin:
MOA
Therapeutic use
ADR

A

MOA: Irritation of gastric mucosa; stimulation of respiratory tract secretions
Tx: Used to clear mucus (Expectorant)
ADR: Emetic

45
Q

N-Acetylcysteine:
MOA
Therapeutic Use (6)

A

MOA:
Cleaves disulfide bonds within mucus–> thins mucus–> facilitates clearance
Tx: Adjunct treatment in CF, Acetaminophen OD, Chronic Bronchitis, Asthma/ COPD

46
Q

Dornase Alpha:
MOA
Therapeutic Use (3)

A

MOA:
DNAse–> cleaves extracellular DNA in mucus–> facilitates clearance
Tx: Adjunct treatment in CF, asthma, COPD

47
Q

Antihistamines Mentioned in This lecture (4)
Which H receptor do they antagonize?
Therapeutic uses?

A
  1. Diphenhydramine
  2. Bromopheniramine
  3. Chlorpheniramine
  4. Loratadine
    –H1–
    Tx: allergic rhinitis (NOT common cold); Di also good for sleep
48
Q

ADRs associated with antihistamines: (2)

CIs(2)

A

Associated with FIRST generation drugs:

  1. Antimuscarinic activity (glaucoma, prostate hypertrophy are CIs)
  2. Sedation
49
Q

Drugs to treat Rhinits + their MOA (4):
List some ADRs associated with these drugs (3)
CIs (2)

A
  1. Ipratropium (antimuscarinic)
  2. Oxymetazoline (A1, A2 agonist)
  3. Pseudoephedrine (A1 agonist)
  4. Phenylephrine (A, B Agonist)

ADRs:

  1. nervousness, tremor, insomnia, dissiness
  2. tacky, HTN
  3. rebound congestion

CI: Uncontrolled HTN, Ischemic heart disease

50
Q

Agonizing which alpha receptor in the nose helps patients breathe better?

A

A1 !

51
Q

Oxymetazoline MOA and Use

A

A1/2 agonist= nasal decongestant