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SFM4 > Respiratory Pharmacology > Flashcards

Respiratory Pharmacology Flashcards

1
Q

albuterol

A

class: inhaled SABA

clinical: bronchodilation
- prn quick relief of asthma sx
- exacerbations or pre-exercise
- prn only, lowest dose possible
- must be combined w/ ICS as SABA-only tx does not prevent exacerbations, and regular/frequent use may increase risk of exacerbations

route of administration: aerosol inhaler ± spacer ± nebulizer

metabolism: phase II liver (sulfotransferase)

adverse events:

  • tachycardia
  • tremor
  • tolerance
  • excess use w/o ICS -> increased risk of exacerbations
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2
Q

salmeterol

A

class: inhaled LABA

clinical: bronchodilation
- asthma
- COPD

metabolism: CYP3A4

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3
Q

formoterol

A

class: inhaled LABA w/ rapid onset

clinical: bronchodilation
- asthma
- COPD
- reliever and maintenance d/t rapid onset and long duration of action

metabolism: primarily glucuronidation
note: typically combined with ICS in ICS-formotorol dual formulation (Symbicort), which is preferred tx through most stages of asthma

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4
Q

vilanterol

A

class: inhaled LABA

clinical: bronchodilation
* COPD
- asthma
- once daily
- found in several combo products for COPD (both emphysema and chronic bronchitis)

metabolism: CYP3A4

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5
Q

ipratropium

A

class: inhaled SAMA
mechanism: pan-muscarinic ANTagonist

clinical:

  • COPD maintenance
  • acute asthma exacerbation in adults and peds (off-label)

route of administration:

  • inhaler ± spacer ± nebulizer
  • nasal spray

metabolism: CYP450

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6
Q

tiotropium

A

class: inhaled LAMA
mechanism: preferential M1 and M3 ANTagonist

clinical:
- maintenance COPD, asthma

metabolism: unmetabolized urinary

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7
Q

glycopyrrolate (glycopyrronium)

A

class: inhaled LAMA w/ fast onset
mechanism: preferential M3 ANTagonist

clinical:

  • maintenance COPD
  • fast-acting option for moderate to severe COPD

metabolism: unmetabolized urinary

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8
Q

umeclindinium

A

class: inhaled LAMA
mechanism: pan-muscarinic, preferential M3 ANTagonist

clinical:
- used in combo with vilanterol (LABA) for moderate to very severe COPD

route: once daily inhaled
metabolism: CYP450, but without changes in renal or hepatic impairment

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9
Q

beclomethasone

A

class: ICS

clinical:
- maintenance asthma

metabolism: prodrug; mostly fecal excretion

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10
Q

budesonide

A

class: ICS

clinical:

  • budenoside-formoterol (Symbicort) is most common/preferred tx for asthma maintenance and relief
  • decreased severity and duration of asthma attack
  • maintenance COPD (off-label)

metabolism: CYP3A4

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11
Q

fluticasone

A

class: ICS; of ICS, highest binding affinity and selectivity for glucocorticoid receptors, longest tissue retention

clinical:
- asthma
- allergic rhinitis
- emphysema

route: nasal spray
metabolism: CYP3A4

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12
Q

mometasone

A

class: ICS

clinical:

  • maintenance asthma
  • seasonal and perennial allergic rhinitis

route: intranasal
metabolism: CYP3A4

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13
Q

omalizumab

A

class: humanized IgG1 mAb, anti-IgE

mechanism: anti-IgE
- binds free IgE (only), reducing its availability for binding
- no basophil degranulation or cross linking

clinical:
- moderate to severe allergic asthma
- refractory idiopathic urticaria (hives)
- severe food allergy (off-label)

route: sc, iv

AEs:
- anaphylaxis after 1st dose or ongoing tx; receive all doses in monitored clinical setting

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14
Q

mepolizumab

reslizumab

A

class: humanized mAb vs IL-5
- eosinophils and basophils

clinical:
- severe allergic asthma

route:

  • mepolizumab: sc
  • reslizumab: iv
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15
Q

benralizumab

A

class: humanized mAb vs IL-5R
- eosinophils and basophils

mechanism:

  • IL-5R blocking, AND
  • IL-5R neutralization (prevents hetero-oligimerization to blockade downstream signalling)

clinical:

  • all asthma
  • seasonal and perennial allergic rhinitis

route: intranasal
metabolism: CYP3A4

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16
Q

dupilumab

A

class: human mAb vs IL4 and IL13

mechanism: targets Th2 pathway (extrinsic)
- both IL4 and IL13 are involved in eosinophil recruitment, especially together
- IL13 also involved in smooth muscle contraction and proliferation involved in bronchospasm and fibrosis

clinical:
- add-on maintenance moderate-to-severe allergic asthma

limitation:
- NOT for acute bronchospasm

route: sc

17
Q

tezepelumab

A

class: human mAb vs TSLP

clinical:
- add-on maintenance maintenance severe asthma

route: sc

18
Q

montelukast

zafirlukast

A

class: cysteine leukotriene receptor ANTagonists

clinical:

  • chronic asthma
  • prevention of exercise-induced bronchospasm
  • – esp in SABA-tolerant (i.e., SABA not effective)
  • allergic rhinitis
  • add-on medications only
  • – montelukast + intranasal glucocorticoid for initial treatment of moderate to severe allergic rhinitis

limitations: NOT rescue medications

19
Q

perfenidone

A

class: antifibrotic agent, anti-inflammatory
mechanism: TGF-beta ANTgonist
- inhibits collagen/ECM production, fibroblast proliferation

clinical:

  • idiopathic pulmonary fibrosis (IPF)
  • slows progression but does not halt or reverse disease

route: po

metabolism: primarily CYP1A2
- caution in liver pts
- d/c other CYP1A2-metabolizd drugs

20
Q

nintedanib

A

class: antifibrotic agent
mechanism: TYRK inhibitor, multiple pathways:
- VEGFR
- FGFR (fibroblast growth factor)
- PDGF (platelet-derived growth factor)

clinical

  • IPF
  • systemic scleroderma (SSc) interstitial lung disease (ILD)
  • other fibrotic ILDs
  • slows progression but does not halt or reverse disease

route: po
metabolism: hydrolic ester cleavage + glucouronidation

AEs:

  • GI
  • c/i in pregnancy, childbearing potential; do not b/c pregnant for at least 3 mo after d/c
21
Q

prednisone

A

class: systemic corticosteroid
mechanism: generalized immunosuppression
- inhibits migration of polymorphonuclear lymphocytes (PMNs)
- reverses capillary permeability p/w
- reduced immune cell count and activity

clinical: generalized immunosuppression ± targeted immunosuppressants; some specific indications in pulm:
- IPF
- cryptogenic organizing pneumonia (COP)

use:
- initial tx 4-8 wk
- when stable, taper as tolerated over 6-12 mo

route: po, iv, im

metabolism:

  • prodrug –> prednisolone
  • 4x potency of hydrocortisone

AEs: so many, dose and duration dependent

  • hypothalamic-pituitary-adrenal (HPA) axis suppression
  • infection
  • hyperglycemia/metabolic syndrome
  • osteoporosis
  • cataracts
  • myopathy
  • adrenal suppression
  • cushingoid
22
Q

azathioprine

A 
class: immunosuppressive antimetabolite
mechanism:
- inhibits purine and protein synthesis
- reduced lymphocyte count
- reduced Ig synthesis

clinical:

  • connective tissue disease (CTD)/autoimmune-associated interstitial lung disease (ILD)
  • transplant rejection prophylaxis

metabolism:
- prodrug –> 6-mercaptopuring (6-MP) –> 6-thioguanine (6-TGN) and others (active)

AEs:

  • black box: malignancy
  • infection
  • GI
  • BM suppression
    • leukocytopenia (common)
    • thrombocytopenia (less common)
    • anemia (uncommon)
23
Q

mycophenolate mofetil (MMF)

A

class: immunosuppressive antimetabolite
mechanism:
- inhibits purine synthesis via ANTagonism of inosine monophosphate dehydrogenase
- depletes guanosine preferentially in lymphocytes
- reduced lymphocyte count and activity
- reduced Ig synthesis

clinical:
- first-line in systemic sclerosis (SSc)

route: po, iv

metabolism:

  • prodrug –> mycophenolic acid (MPA) (active)
  • glucouronidation and excretion

AEs:

  • black box:
    • c/i in pregnancy
    • malignancy
    • serious infection
  • hematologic leukopenia
  • GI
24
Q

abx for hospital-acquired pneumonia (HAP)

A

**antipseudomonals:

one of:

  • piperacillin/tazobactam (most common iv, more severe cases)
  • cefepime
  • ceftazidime
  • imipenem
  • meropenem

if severe, +
- cipro
or
- aminoglycoside: amikacin, gentamicin, tobramycin

empirically, to cover MRSA b/f cultures are back:
- vancomycin
or
- linezolid

when cultures return:

  • d/c vancomycin/linezolid if cultures confirm pseudomonas
  • de-escalate to most narrow-spectrum antibiotic
  • adjust per results of antibiotic sensitivity testing
25
Q

outpatient abx for community-acquired pneumonia (CAP)

A

amoxicillin ± clavulanate
- no comorbidities
and
- low suspicion for mycoplasma, clamydophila, legionella

if comorbidities (diabetes, cancer, others):
- amoxicillin/clavulanate + azithromycin (preferred)
or
- cefpodoxime + azithromycin, levofloxacin, or moxyfloxacin

26
Q

inpatient abx for community-acquired pneumonia (CAP)

A

third-get cephalosporins + macrolide, e.g.
- ceftriaxone + azithromycin (most common)

  • cef covers “typicals” e.g. strep pneumoniae, H. influenza, M. catarrhalis
  • macrolide covers “atypicals” e.g. chlamydophilia, mycoplasma, legionella

OR

respiratory fluoroquinolone

  • levofloxacin
  • moxifloxacin

(cover both typical and atypical)

27
Q

abx for latent TB

A 
- rifampin x4 mo
or
- isoniazid x9 mo
or
- isoniazid + rifampin or rifapentine x3 mo
28
Q

abx for active TB

A
  • rifampin + isoniazid + pyrazinamide + ethambutol
  • consider transitioning to more narrow regimen after initial tx
  • minimum total treatment >6 mo
29
Q

tx for coccidioidomycosis

A

very long course of fluconazole (anti-fungal)

30
Q

tx for histoplasmosis

A

mild: may clear spontaneously

mild-to-moderate: itraconazole

severe: amphoterrible

31
Q

tx for blastomycosis

A

mild: may clear spontaneously

mild-to-moderate: itraconazole

severe: amphoterrible

SFM4 (10 decks)

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