Pharmacy Exam Review

Ashma & COPD

Last updated on: April 7th, 2020

Asthma

Background

  • Asthma is a predisposition of chronic inflammation of lungs, airways are narrowed and the effect is reversible.
  • Airway remodeling consists of fibrosis and increased goblet cells
  • Asthma pathology
  • Triggering drugs: beta blocker (think about the undesired effect of beta receptors), ASA, NSAIDs (BAN), sulfites. 
  • Mild persistent asthma: start low-dose ICS (e.g: Flovent HFA 88mcg BID, QVAR, Pulmicort), ICS - inhaled corticosteroids reduce inflammation and swelling.
  • Next for moderate persistent asthma: suggest a low-dose ICS + LABA (prevent more asthma attacks than increasing dose to medium-dose steroid)
·         Peak expiratory flow
  • Stand up straight, hold meter horizontally, blow into the meter. Repeat 2x and record the highest of 3 readings
  • Yellow zone: take 2-4 puffs of beta2-agonist every 20-min x 3 doses. After 1-hr, if at green: beta agonist & inhaled steroid for 7-10 days, if at yellow: beta agonist & oral steroid
  • Red zone (<50%): take up to 3 treatments of 4-6 puffs of beta2-agonist every 20-min. take oral steroid (40-60mg, 3-10 days). Call 911 or go to ER.
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  • Enhance coordination to administer inhaled med, prevent thrush and reduce cough

 

SABA (short-acting beta2 agonist)

  • Drugs: Epinephrine (Primatene), Albuterol (Proair, Proventil, Ventolin, AccuNeb), Levalbuterol (Xopenex), Maxair (pirbuterol, discontinued), Tornalate (bitolterol)
  • Binds to b-2 receptor causing relaxation of bronchial smooth muscle, can be taken right before exercise to prevent EIB (exercise induced bronchospasm)
  • SE: tremor/shakiness/tachycardia (epinephrine helps you to think about the stimulating effect of SABA), hypo-K & hyperglycemia (K & glucose goes opposite)
  • If SABA is used more than 2 day/wk, need to increase maintenance dose.
  • HFA produce softer and less forceful spray, patient may experience a different taste and warmer spray than CFC (D/C due to environmental concern)
  • Epinephrine (Primatene): should not be used due to non-beta2 selective.

 

LABA (long-acting beta2 agonist)

  • Drugs: Sameterol (Serevent), +fluticasone (Advair Diskus/HFA), formoterol (Foradil Aerolizer, Perforomist- nebulizer soln. fridge), + budesonide (Symbicort), + mometasone (Dulera), arformoterol (Brovana, a nebulizer solution), indacaterol (Arcapta Neohaler)
  • SE: tremor, shakiness, palpitation, hypo-K & hyperglycemia (K & glucose goes opposite)
  • BBW: increase asthma-related death, do not use LABA as monotherapy (now the BBW is gone from LABA/ICS combos, but is still in place for LABA alone without ICS)
  • LABA MUST be used with an inhaled steroid, since LABA alone doesn’t reduce inflammation.
  • Most are indicated for 12 years and above, except for a few: Serevent, Advair, Dulera, Foradil.
  • Mostly dosed at BID. Foil wrapped inhalers: good for 30 - 90 days after opening.

 

Mast cell stabilizer

  • Drug: Cromolyn sodium (Intal, OTC-NasalCrom)
  • MOA: Prevent mast cell release of histamine and leukotrienes by inhibiting degranulation after contact with allergens.
  • Prophylactic agent for bronchial asthma.
  • 2 puffs QID for >2 y/o

 

Corticosteroid

  • 1st line for long term therapy with persistent asthma
  • Beclomethasone HFA (Qvar HFA): do not shake
  • Budesonide (Pulmicort): ok for 1-8 years old
    • + formoterol (Symbicort)
  • Ciclesonide (Alevesco): prodrug, do not shake
  • Flunisolide (AeroBid, Aerospan)
  • Fluticasone (Flovent, Veramyst/Flonase nasal) + vilanterol (Breo)
  • Mometasone (Asmanex, Nasonex nasal) + formoterol (Dulera)
  • Triamcinolone (Azmacort, Nasacort nasal)

 

Leukotriene modifying agents

  • MOA: Leukotriene-receptor antagonists and modifier.
  • Drugs: Montelukast (Singulair); Zafirlukast (Accolate)
  • SE: upper respiratory tract infection, increase LFT, neuropsychiatric events
  • Singulair to prevent EIB: take 2-hrs before exercise, Singulair chewable tab contains phenylalanine (Avoid in patients with PKU).
  • Montelukast: QHS, substrate of 2C9; Zafirlukast: BID.
  • Zileuton (Zyflo)’s mechanism is slightly different as a leukotriene modifier, it is an inhibitor of 5-lipoxygenase (as verse to an antagonist at the receptor).
  • Zileuton CI in active liver disease, can increase concentrations of theophylline and warfarin. BID.

 

Theophylline (Elixophyllin, Theo-24, Uniphyl, Theochron)

  • MOA: a methylxanthine derived from tea used for respiratory diseases (such as COPD, bronchospasm or asthma); Blocks phosphodiesterase resulting in increased cAMP, promotes release of epinephrine from adrenal cell, which causes bronchodilation, diuresis, CNS and cardiac stimulation.
  • SE: tachycardia, tremor, insomnia, avoid excessive caffeine, protein/carbohydrates (can alter theophylline level)
  • Signs of toxicity: >15mcg/mL: vomiting, >30: ventricular tachycardia, > 50: seizure.
  • Therapeutic range: 5 -15 mcg/mL, since it follows saturable kinetics (zero-order elimination), small dose results large increase in concentration. Max dose: 900mg/day
  • Substrates of 1A2, 3A4
    • Increased level due to 1A2 inhibition: oral contraceptives, zafirlukast/zileuton, acyclovir, cimetidine, ciprofloxacin, isoniazid
    • Decreased level by: CBZ/phenobarbital/phenytoin/primidone, rifampin, ritonavir, smoking, SJW, tipranavir/ritonavir, high protein diet, low carb diet, thyroid hormone
    • Theo decreases Li level due to increase renal excretion of Li.
    • IV aminophylline to PO theophylline: multiple IV dose by 0.8

 

Omalizumab (Xolair)

  • IgG monoclonal antibody inhibits IgE binding on mast cell and basophil.
  • SC at Dr office, >12 yo, 150-375mg SC q2-4 weeks
  • BBW: anaphylaxis reaction(applies to all monoclonal antibodies).

 

Tilade (nedocromil sodium)

  • Inhaled anti-inflammatory for the prevention of asthma. 
  • 2 puffs QID for >6 y/o

Chronic Obstructive Lung Disease (COPD)

Background

  • Chronic bronchitis and emphysema (destruction of the tissue of the lung), disease is not reversible.
  • Risk factors: smoking, alpha-1 antitrypsin deficiency (use alpha-1 proteinase inhibitor - Prolastin), occupational dust, air pollution
  • GOLD (Global Initiative for COPD) Stages or grades: a system used to classify different levels of COPD. 
    • GOLD 1: mild; GOLD 2: moderate; GOLD 3: severe; GOLD 4: very severe.
  • Spirometry results are based on two measurements:
    • Forced vital capacity (FVC): largest amount of air you can breathe out after breathing in as deeply as you can.
    • Forced expiratory volume (FEV-1): air you can exhale from your lungs in one second.

Anticholinergics

  • MOA: Block acetylcholine (decrease cGMP) at parasympathetic site, causing bronchodilation.
  • Caution in: myasthenia gravis, narrow angle glaucoma, BPH, bladder obstruction
  • SE: dry mouth, upper resp. tract infection
  • Only for COPD, do not use for rescue, QD dosing.
  • SAMA - short acting muscarinic antagonist
    • Ipratropium (Atrovent HFA): QID dosing
      • Spiriva: QD advantage in dosing
    • + albuterol (Combivent - peanut allergy, DuoNeb nebulizer)
  • LAMA - long acting muscarinic antagonist
    • Tiotropium (Spiriva): handihaler, Respimat; + oladaterol = Stiolto
    • Incruse Ellipta (umeclidinium) + vilanterol = Anoro Ellipta
    • Tudorza (aclidinium)
  • Trelegy Ellipta - (LAMA) umeclidinium + (LABA) vilanterol + inhaled corticosteroid (ICS) fluticasone
    • first “three-in-one” inhaler for COPD.
    • dry-powder inhaler, single puff once daily. Reserved for patients with exacerbations on a LAMA/LABA or who also have asthma.

 

Controller meds for COPD

 

Daliresp (roflumilast)

  • A phosphodiesterase 4 inhibitor used for COPD. A CYP3A4 substrate.
  • 500mcg po
  • SE: weight loss, liver impairment

 

Combivent Respimat instruction

  • Turn the clear base in the direction of the arrow until it clicks (half a turn)
  • Breath out slowly and fully, seal your lips around the mouthpiece without covering the air vent. Point the inhaler to the back of your throat
  • Press the dose release button and inhale the mist

 

Spiriva Handihaler

  • Breath out and away completely. With the handihaler in your mouth, breathe in deeply until your lung is full
  • You should hear or feel the capsule vibrate (rattle)
  • To take your full daily dose, you must inhale twice from the same capsule
  • Watch a short clip on how to use:

 

Pulmicort flexhaler

  • Hold the inhaler upright, twist the brown grip as far as it goes in one direction, then twist it all the way back in the other direction
  • Turn away from inhaler then breathe out.
  • Inhale the dose deeply

 

Foradil aerolizer

  • Breathe in as steadily and deeply as you can
  • Remove the inhaler while holding your breath for 5-10 seconds
  • Breathe away from inhaler.

 

Dry powder inhalers:

  • Spiriva Handihaler
  • Foradil Aerolizer
  • Diskus: Advair, Flovent, Asmanex, Serevent
  • Ellipt:Incruse, Anora, Trelegy
  • Pulmicort Flexhaler (budesonide) 

 

Brethine (terbutaline)

  • It works by relaxing muscles in the airways to improve breathing.
  • Terbutaline is used to treat or prevent bronchospasm (wheezing, chest tightness, trouble breathing) in people with lung conditions such as asthma, bronchitis, or emphysema.

 

 




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