RESPIRATORY DRUGS

RAPID-ACTING RESCUE DRUGS

MOA Uses Side Effects Other
“SABA s
Asthma & COPD Rescue:
SHORT-ACTING 2-AGONISTS 2 → Gs → ↑cAMP→ Less 1 cardiac side effects
Onset: 5-10 min
Albuterol Smooth muscle: Tremor with levalbuterol
Peak: 30 min
Levalbuterol PKA → MLCK-P → bronchodilation Tachycardia, arrhythmia ( 1)
Duration: 3-6 hrs
Pirbuterol Inflammatory cells: Hypokalemia (rare) Desensitization/tolerance with
Bitolterol Sustained ↑cAMP → ↓release of long-term use → ↓side effects
Inhaled > oral or
Terbutaline histamine, 5HT, PGs, LTs & ↓efficacy
SubQ (terbutaline)
Metaproterenol
Limited use – patients Metabolized by P450
PDE inhibitors → ↑cAMP (see SABAs)
METHYLXANTHINES who can t use 2 agonists ↑Clearance = P450 inducers
Adenosine antagonists → A2
Theophylline Nausea, vomiting, headache, GI (Drugs & smoking), high-
receptor →↓bronchoconstriction, Asthma & COPD Rescue
Aminophylline discomfort (PDE4) protein diet, barbecued meat,
↓inflammatory mediator release Peak: 1-2 hours
Dyphilline Arrhythmias (PDE3, A1) children
↑IL-10 release → ↓Inflammation & Duration: varies
Oxtriphylline Diuresis, Epileptic seizures (A1) ↓Clearance = P450 inhibitors
↑apoptosis of eosinophils & neut s (Sustained-release forms
Caffeine Behavioral disturbances (Drugs - LT inhibitors), CHF,
↓NFkB to nucleus→↓Pro-infl. genes can be controllers)
Theobromine Liver Dx, pneumonia, viruses,
↑HDAC → ↑Anti-inflammatory genes
Inhaled or oral high-carb diet
If cannot use 2 agonists
ANTI-MUSCARINICS Asthma & COPD Bitter taste (ipratropium)
Ipratropium Onset: 5-15 min Headaches
Tiotropium M3 competitive antagonists Peak: 1-2 hrs ↓Secretions (dry mouth/eyes) Spiriva = Tiotropium
Atropine Duration: I - 6-8 hrs ↓Urination
Stramonium T - 24 hrs Tachycardia (rare)
Inhaled or oral

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 RESPIRATORY DRUGS
LONG-TERM CONTROLLERS
MOA Uses Side Effects Other
2 → Gs → ↑cAMP→ Lipophilic moiety prevents rapid
Asthma & COPD Control
“LABA s Smooth muscle: Tremors metabolism
Onset: 15-30 min
LONG-ACTING 2-AGONISTS PKA → MLCK-P → Arrhythmia LABA’s should only be used as
Peak: 22 hours (overnight)
bronchodilation Hypo/hypertension sole Rx in exercise-induced
Formoterol Inflammatory cells:
Duration: 24 hours
Vascular headaches asthma & COPD & never alone in
Salmeterol Sustained ↑cAMP → ↓release of Tolerance kids ↑risk of serious fatal asthma
Inhaled
histamine, 5HT, PGs, LTs attack b/c does not ↓inflammation
CORTICOSTEROIDS
Inhaled: Beclomethasone* IV forms may be used in inpatient
Fluticasone Inhaled: setting to prevent the late phase
Lipophilic → binds nuclear R →
Mometasone Oropharyngeal candidiasis of an acute asthma episode
gene regulation: Asthma & COPD Control
Triamcinolone Dysphonia
↑Anti-inflammatory genes Onset: 5-8 hrs
Often combined in step-up
Flunisolide ↓Pro-inflammatory genes Duration: 6-24 hrs
Oral: dosages with LABA in control
Budesonide Immunosuppression
Mood, ↑appetite inhalers to treat moderate-severe
Ciclesonide* Do not prevent/Rx acute attacks
Hyperglycemia (diabetics) uncontrolled asthma & COPD
Oral: Prednisone *=prodrugs converted to active (no bronchodilation effects)
Candidiasis
Prednisolone form by lung esterases
Osteoporosis **Single most effective class of
IV: Hydrocortisone anti-asthma Rx (monotherapy)
Methylprednisolone
Prophylaxis of mild-moderate allergic
↓Late-phase Cl- channel asthma in children
CROMOLYNS SAFEST drugs (esp. cromolyn)
→ mast cell stabilization → Allergic rhinitis (cromolyn)
Cromolyn (< 12 yrs.) initial degranulation in acute ↑Coughing, wheezing
“C s = cromolyn, controller,
Nedocromil (>12 yrs) phase & ↓late response (also Asthma Control
children, Cl- channels
stabilized eos and neuts) Duration: weeks
Inhaled
“Responder mild chronic asthma
LEUKOTRIENE MODIFIERS Allergic rhinitis
Good for Aspirin-induced asthma
5α lipoxygenase inhibitor: Churg-Strauss Syndrome –
Zileuton ↓LT synthesis/receptor binding → irreversible vascular Many Drug Interactions:
Asthma & COPD Control
↓bronchial smooth muscle necrosis in lungs esp. Metabolized by
LT receptor antagonists: contraction → bronchodilation
Onset: 3-6 hours
w/ lukasts CYP2C9 & CYP3A4
Montelukast Peak: 4 hours
Hepatic dysfunction (rare) Inhibitor of
Zafirlukast Duration: 24 hours
CYP2C8 & CYP2C9
Inhaled or oral (-lukasts)
Only useful in allergic asthma
Moderate-severe persistent cases in
IgE ANTAGONISM which environmental allergens are Injection site reactions
Last-resort drug
inescapable Anaphylaxis
Omalizumab Anti-IgE antibody → blocks IgE
(to mouse part of Ab)
(bronchothermoplasty needed in
from binding allergens Allergic Asthma Control non-allergic asthma as it does not
Infections
Peak: 7-8 days respond to anti-IgE Rx)
Cancer
Duration: 26 days
Monthly SubQ injection
Drug Interactions:
COPD Control Only GI - nausea, vomiting, ↑ by Cimetidine, Conivaptan
PDE4 INHIBITION Onset: 1 hr diarrhea by Ciprofloxacin, Rifampin
PDE inhibition → ↑cAMP
Romflumilast Duration: 17hr (30 for metabolite) Contraindications: hepatic Causes ↑immunosuppressants
Oral impairment, depression not beclomethasone, budesonide,
fluticasone (LABAs)

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