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Salmeterol (Serevent Diskus)
Prototype LABA
MOA: long acting bronchodilator agents: B1 activity is less than B2 activity.
-greatest B2 potency available (2x that of isoproterenol)
- -Black Box Warning: life threatening asthma related death is possible with all long acting agonists when used alone.
- -Must also use a corticosteroid with it
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Fromoterol fumarate (Foradil and Aerolizer)
Also have a nebulizer for this (Perforomist)
MOA:long acting bronchodilator
Caution: life threatening asthma related death is possible with all long acting agonists when used alone
200 times higher affinity for B2 receptors over B1, (S,S) is 1000 times less potent as a B2 agonist than the (RR) cpd
inhibitor of mast cell mediators such as histamine and leukotrienes
Two choral centers: racemic (S,S) and (R,R) diastereomers out of 4 possible--local delivery so dosage very low-side effects for a mix of compounds?
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Budesonide and Formoterol (Symbicort)
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Formoterol and Mometasone (Dulera)
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Arformoterol tartrate (Brovana Inhalation Solution)
Or called (R,R)-formoterol L-tartrate
Pure (R,R)-diastereomer (Foradil)
Long acting agents-usual warning associated with these drugs
Indication: ONLY for long term treatment of COPD, chronic bronchitis, emphysema--delivered via a nebulizer every 12 hours--NOT for acute rescue
MOA:inhibitor of mast cell mediators such as histamine and leukotrienes
No CYP inhibition
2 times as potent than the racemic drug Formeoterol
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Indacaterol maleate (Arcapta and Neohaler)
Indications: chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema
NOT INDICATED FOR ASTHMA
MOA: long acting beta2-adrenergic agonist.
- Must be used with the neohaler only
- when used alone it'll increase asthma related death
Only inhaled once a day so should increase compliance relative to twice-daily inhalers
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Fluticasone furoate and Vilanterol inhalation powder (Breo Ellipta)
Anti-inflammatory/LABA combo product
Indications: long-term, once daily, maintenance treatment of COPD. NOT INDICATED for relief of acute bronchospasm or for treatment of asthma.
DI's: cytochrome P450 3A4 inhibitors, MAOI, TCAs, Beta-blockers, diuretics
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Olodaterol (Striverdi and Respimat)
New Combo: Tiotropium bromide and olodaterol (Stiolto and Respimat)
Indications: long-term, once-daily, maintenance treatment of COPD including bronchitits and/or emphysema.
NOT indicated for relief of acute deterioration of COPD or for treatment of asthma
MOA: selective long acting B2 agonist
CYP 2C8 and 2C9 o-demethylation followed by glucuronidation
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