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
#1 drugs to treat asthma?
B2 agonists! Think of B2Rs are the asthma receptor, and think of the asthma receptor as a HELPFUL receptor...
26
List two Muscarinic Antagonists. Describe the dosing regimen for each. What respiratory disease are these drugs primarily used to treat?
1. Ipratropium (4x daily) 2. Tiotropium (1x daily) #1 Drugs to treat COPD; Also used to treat asthma * Think of muscarinic receptors as the COPD receptor (BAD receptor) * Commonly administered in combo inhalers with albuterol and such*
27
In addition to treating COPD, what is another use for ipratropium?
Decrease nasal discharge IPra helps a drIPPy nose!!
28
List some of the ADRs associated with muscarinic antagonists--why are they usually mild?
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
Which drug is a Methylxanthane? What is its MOA? (4) What is it used to treat? (2)
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
Describe the theraputic index for theophylline (low/ high?). | Describe the effects of theophylline toxicity.
Low therapeutic index Dose dependent toxicity Low dose: N/V/ HA. etc High dose: arrhythmia + seizure
31
How is Theophylline metabolized?
CYP1A2 in the liver--watch for inducers and inhibitors
32
List 4 corticosteroids used to treat obstructive lung disease. What is their MOA?
1. Beclomethasone 2. Triamcinolone acetate 3. Budesonide 4. Fluticasone Propionate MOA: Agonize glucocorticoid receptor--> ^ # B2Rs--> ^ responseiveness to LABA/ SABAs
33
Therapeutic applications (respiratory) for corticosteroids (inhaled/ PO/ IV):
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
3ADRs assocateed with inhaled corticosteroid use?
#1. Dysphonia (atrophy of vocal cords) 2. Oropharyngeal candidiasis (use spacer) 3. Cough
35
Name two Leukotriene inhibitors (LTis) and describe their dosing regimen. MOA? Therapeutic use? (2)
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
Zileuton: Drug Class and MOA Therapeutic Use + Dosing Regimen Meatabolism?
MOA: Inhib 5-Lipoxygenase (RLS)--> Inhib LT synthesis Tx: Same as Zafirlukast, Montelukast; admin 4x daily Hepatic metabolism (CYPs)
37
What are two common ADRs amongst all anti-leukotriene/LT-inhibitors?
- All have some degree of hepatotoxicity | - All can inhibit CYPs and compromise metabolism of other CYP metabolized drugs
38
Cromolyn, Nedocromil MOA Which one is still used and what is it used for?
Inhibit mast cell degranulation and histamine release Cromolyn still used Treats asthma and allergic rhinitis
39
``` Omalizumab MOA Therapeutic use Dosing regimen ADR ```
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
Alpha-1 Proteinase Inhibitor MOA Therapeutic use
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
Which opioids are used to treat cough? What is their MOA? What are their ADRs? (4) Important CI?
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
Dextromethorphan: MOA Therapeutic use ADRs
CENTRAL NMDA-R Antagonist Tx: cough ADRs: Can cause CNS depression in high doses (less toxic than codeine)
43
Benzonatate: MOA Therapeutic use
PERIPHERAL antagonism of vagal receptors in RT Tx: cough ADRs: Dizziness
44
Guaifenesin: MOA Therapeutic use ADR
MOA: Irritation of gastric mucosa; stimulation of respiratory tract secretions Tx: Used to clear mucus (Expectorant) ADR: Emetic
45
N-Acetylcysteine: MOA Therapeutic Use (6)
MOA: Cleaves disulfide bonds within mucus--> thins mucus--> facilitates clearance Tx: Adjunct treatment in CF, Acetaminophen OD, Chronic Bronchitis, Asthma/ COPD
46
Dornase Alpha: MOA Therapeutic Use (3)
MOA: DNAse--> cleaves extracellular DNA in mucus--> facilitates clearance Tx: Adjunct treatment in CF, asthma, COPD
47
Antihistamines Mentioned in This lecture (4) Which H receptor do they antagonize? Therapeutic uses?
1. Diphenhydramine 2. Bromopheniramine 3. Chlorpheniramine 4. Loratadine --H1-- Tx: allergic rhinitis (NOT common cold); Di also good for sleep
48
ADRs associated with antihistamines: (2) | CIs(2)
Associated with FIRST generation drugs: 1. Antimuscarinic activity (glaucoma, prostate hypertrophy are CIs) 2. Sedation
49
Drugs to treat Rhinits + their MOA (4): List some ADRs associated with these drugs (3) CIs (2)
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
Agonizing which alpha receptor in the nose helps patients breathe better?
A1 !
51
Oxymetazoline MOA and Use
A1/2 agonist= nasal decongestant