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Spring Pharm > pulmonary > Flashcards

pulmonary Flashcards

1
Q

NANC

A

Non adrenergic non-cholinergic receptors. Present in bronchial smooth muscle. Release NO and VIP (nitric oxide) (vasoactive intestinal peptide) will relax smooth muscle

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2
Q

Activation of M3 receptors in bronchial smooth muscle

A

By PSNS (acetylcholine) leads to bronchoconstriction via activation -> increase IP3, increase Ca, BRONCHOCONSTRICTION + mucous secretion

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3
Q

growth factors r/t bronchial smooth muscle hypertrophy

A

Growth factors are released from inflammatory cells on smooth muscle cells and the smooth muscle itself can release pro inflammatory mediators and growth factors

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4
Q

epithelial loss in bronchioles means that

A

irritant receptors and C fibers are more accessible to irritant stimuli

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5
Q

gold standard of asthma is to

A

get inflammation under control, usually done via inhaled glucocorticoid

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6
Q

even with great technique, MDIs deliver

A

10% of the dose to the lungs

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7
Q

DPIs deliver

A

20% of dose to lungs, don’t require spacers

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8
Q

MOA of inhaled glucocorticoids

A

suppress inflammation by altering genetic transcription

target: glucocorticoid receptor alpha in cytoplasm of airway epithelial cells

  • increase transcription of B2 receptors and receptor responsiveness
  • increase transcription of genes for ANTI-inflammatory proteins
  • DECREASE transcription of genes for PRO-inflammatory proteins
    • decrease airway mucous production
    • decrease vascular pemeablity
  • induce APOPTOSIS in inflammatory cells
    • eoisinophils, TH2 lymphocytes
  • indirect inhibtion of mast cells over time
  • REVERSES many features of asthma, especially bronchial hyperreactivity
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9
Q

Most effective/important preventative treatment for asthma

A

Glucocorticoids

used as suppressive therapy, not curative

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10
Q

Inhaled Corticosteriods (4)

A

Budesonide

Beclomethasone

Triamcinolone

Fluticasone

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11
Q

IV corticosterids (2)

A

hydrocrotisone

methylprednisone

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12
Q

PO corticosteroids

A

Prednisone

Prednisolone

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13
Q

Adrenal Suppression r/t taking steroids

A

when discontinuing, must taper dose!

because adrenal suppresion happens

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14
Q

systemic (IV/PO) adverse effects of

CORTICOSTEROIDS

A

minor when taken <10 days

can be severe when used long term

  • myopathy/weakness
  • adrenal suppresion (must taper dose)
  • may require extra dose during times of physiological stress, may even need months after tapering off
  • infection risk is higher
  • suppression of growth and development (avoid in young kids)
  • Peptic Ulcer Disease (NSAIDs incresae the risk)
  • Weight gain, edema,
  • hypokalemia (some diuretics increase risk)
  • hyperglycemia - cortisol
  • mobilizing FFA - cortisol, advances atherosclerosis
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15
Q

Cromolyn

MOA:

Uses:
Dosing:
SE:

A

Cromolyn

MOA:

  • Stabilizes pulmonary mast cells
  • prevents antigen binding that would lead to antigen induced release of histmaine and inflammatory mediators

Uses:

  • prophylatic therapy of bronchial asthma
  • atopic individuals, i.e. exercise induced asthma
  • SUPPRESSES inflammation, not a rescue inhaler

Dosing:

  • must be taken 4 times per day
  • administed via inhalation - 8-10% enters systemic circulation
  • route: neb or MDI

SE:

  • safest of all, rare but serious SE
  • cough and/or bronchospasm
  • laryngeal edema
  • angioedema
  • urticaria
  • anaphylaxis
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16
Q

Leukotriene Modifiers (3)

A

Zileuton (Zyflo)

Zafirlukast (Accolate)

Montelukast (Singulair)

17
Q

leukotrienes C4, D4, and E4

A
  • Promote bronchoconstriction
  • Promote eosinophil infiltration
  • Promote mucus production and
  • Promote airway edema
18
Q

Leukotriene modifers compared to gluccocorticoids

A

LESS effective than inhaled gluccocorticoids

Also not effective in tx of acute asthma

19
Q

Zileuton (Zyflo)

class:

MOA:

Uses:

Dosing:

SE:

A

Zileuton (Zyflo)

Class:

  • leukotriene inhibitor/modifer?

MOA:

  • Lipoxygenase inhibtor which blocks the biosynthesis of luekotriens from arachidonic acid, produces bronchodilation, ​

Uses:

  • improves asthma symptoms, has shown long term improvements in PFTs

Dosing:

  • low bioavailabiliity, low potency

SE:

  • Hepatotoxic 2-4%
  • monitor LFTs regualrly, early in tx
  • once a month for 3 months
  • Neuropyschiatric
    • depression, anxiety, suicidal ideation, hallucinations,
  • Cytochrome 450 interactions!
    • warfarin, propanolol, theophylline

NOT WIDELY USED

20
Q

Montelukast (Singulair)

Class:

MOA:

Uses:

Dosing:

SE:

A

Montelukast (Singulair)

Class:

  • leuktriene inhibitor

MOA:

  • blocks the ability of leukotrienes to bind ot leukotriene-1 receptor (blocks CystLT1)
  • improves bronchial tone, pulmonary function, asthma sypmtoms
  • MAX EFFECT 24 HRS AFTER 1ST DOSE

Uses:

  • used to tx patients <1 year old
  • exercise induced asthma >15 y/o
  • treat allergic rhinitis

Pk:

  • 99% PB
  • undergoes extensive cYP450

SE:

  • Rare psyschatric effects
    *
21
Q

Omalizumab

Class

MOA:

Uses:

Pk:

Dosing:

SE:

A

Omalizumab

Class:

  • Anti-IgE antibodies

MOA:

  • binds to IgE in blood, inactivating it, decrease IgE levels for up to a year
  • in response to lower IgE levels, decrease receptors on mast cells, basophils, and dendritic cells. This reduces the stimulation of T2 lymphocytes and decreases the late phase asthmatic reponse than would be expected with IgE alone

Uses:

  • decreases quantity of circulating IgE
  • only used in allergy induced asthma when inhaled glucocorticoids have failed

Pk:

  • given SQ for 2-4 weeks or IV
  • very expensive
  • 1/2L = 26 days

SE:

  • Injection site reactions
  • viral infection
  • URI and sinusitis
  • HA
  • pharyngitis
  • increase CV complications, increased MI, stroke, HF, dysrhytmias, thromboembolism,
  • possible increased risk of Ca

Rare adverse effect: triggering of an immune rsponse, anaphylaxis. Monitor 2 hours after 1st 3 doses, monitor 30 minutes after all subsequent doses

22
Q

drug binding to B2 receptor leads to

A

binding to GPCR -s

increase in cAMP

decrease in calicum

increase in conductance of potassium

bronchodilatin

inhibits mast cells

increase clearance of mucous

23
Q

most effective drugs for relief of acute bronchospasm and prevention of exercise induced bronchospasm

A

beta 2 adrengeric agonists

24
Q

short acting beta 2 agonists

A

albuterol, levalbuterol

25
Q

long acting beta 2 agonists

A

salmetrol ,terbutaline (PO/IV)

26
Q

Albuterol

dosing

DOA

isomers

A

Albuterol

dosing

100 mcg/puff

2 puffs q 4-6 hours

nebulizer: 2.5 to 5 mg in 5mL salie

DOA: 4 hours with some relief at 8 hours

2 isomers

R = albuterol /levabuterol more affinity for beta 2

S albuertol more affinity for beta 1

27
Q

metaproterenol (alupent)

A

beta 2 agonist for tx of asthma

admistered via MDI

not to exceed 16 puffs /day

  • rescue inhaler
28
Q

bitolerol

A

SELECTIVE beta 2 agonist that resembles albuterol

longer lasting

CV side affects are RARE

daily metered dose is 16-20 puffs/day

each dose is 270 mcgs

29
Q

Terbutaline

dosing

A

admistered oral, SC, inhaled

treats asthma

SC administration resembles EPI response

  • SC dose for child = 0.1 mg/kg
  • SC dose for adult = 0.25 mg q 15 minut

metered dose inhaler, 16-20 puffs/day

each dose is 200 mcg

30
Q

Salmetrol + Fluticasone/Formaterol

“ADVAIR”

A

Salmetrol + Fluticasone/Formaterol

“ADVAIR”

good for PREVENTION

not good for acute flare - up

long acting beta agonists, binds B2 receptor and prolongs activation

black box warning - may increase the risk of fatal or near fatal asthma attack.

Now these are always used in combination with inhaled steroid, not clear why giving with steroid has benefit

(B2 RECEPTORS MAY DOWNREGULATE OVER TIME)

31
Q

ipatropium

A

quartenary ammonia salt of atropine

antagonizes the effect of endogenous acetylcholine at M3

admistered via MDI

40-80 mcg in 2-4 puffs of nebulizer

SLOW onset: 30-90 minutes

DOA: 4-6 hours

not significantly absorbed compared to atropine

inadverant oral absorption: dry mouth and GI upset

32
Q

tiotropium

A

quarternary ammonium salt

long acting anti-cholinergic

NOT significantly absorbed across respiratory epithelium which results in few side effects

used for COPD

used in COPD as maintenance and resuce therapy but only used in acute exacerbation in asthma. Ipratropium has been shown to increase excerse tolerance, decrease dyspnea, and imporve gas exchange.

TIO reduces exacerbations, respiratory failure, and all causes of mortality

Spring Pharm (11 decks)

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