Pharmacology

Pulmonary Drugs

Bronchodilators (SABA/LABA/LAMA), inhaled corticosteroids, biologics, antibiotics & pulmonary vasodilators

Bronchodilators

ClassDrugsMechanismOnset/DurationUseKey Points
SABA (Short-acting beta-2 agonist)Albuterol (Ventolin, ProAir), levalbuterol (Xopenex)β2 agonist → smooth muscle relaxation → bronchodilation; also stimulates mucociliary clearanceOnset: 5–15 min; Duration: 4–6 hrAsthma rescue, COPD exacerbation, bronchospasm, hyperkalemia (albuterol drives K+ into cells)Side effects: tachycardia, tremor, hypokalemia (high doses). Levalbuterol = R-isomer of albuterol; fewer cardiovascular side effects but more expensive
LABA (Long-acting beta-2 agonist)Salmeterol (Serevent), formoterol (Foradil), indacaterol (Arcapta), olodaterolβ2 agonist; prolonged binding to β2 receptorDuration 12–24 hrCOPD maintenance (monotherapy or with LAMA); asthma maintenance (ALWAYS with ICS — never monotherapy)LABA MONOTHERAPY in asthma is CONTRAINDICATED (Black box warning — increased asthma deaths); always combine with ICS. Formoterol: fast-onset LABA (can use as rescue in SMART regimen)
SAMA (Short-acting muscarinic antagonist)Ipratropium (Atrovent)M1/M3 muscarinic antagonist → reduces bronchoconstriction, reduces secretionsDuration 4–6 hrCOPD (add-on to SABA for exacerbations); asthma exacerbations (add to albuterol in ED)Side effects: dry mouth, urinary retention, constipation, tachycardia; avoid in narrow-angle glaucoma (may worsen); NOT absorbed systemically — minimal side effects inhaled
LAMA (Long-acting muscarinic antagonist)Tiotropium (Spiriva), umeclidinium (Incruse), aclidinium (Tudorza), glycopyrrolateM1/M3 muscarinic antagonist; prolonged duration (once daily)Duration 24 hr (tiotropium)COPD (1st-line maintenance); asthma (add-on for uncontrolled asthma on ICS+LABA)Tiotropium: most evidence in COPD; reduces exacerbations (UPLIFT trial). Same anticholinergic side effects as SAMA. Use with caution in BPH, narrow-angle glaucoma
MethylxanthinesTheophylline, aminophylline (IV)Phosphodiesterase inhibitor → ↑cAMP → bronchodilation; also stimulates respiratory drive; anti-inflammatoryOral; IV availableSevere COPD (3rd-line add-on); historically used for asthma; IV aminophylline for severe asthma/COPD exacerbationNARROW THERAPEUTIC INDEX (10–20 mcg/mL); toxicity: seizures, arrhythmias, N/V. Many drug interactions (CYP1A2 — cigarette smoking, ciprofloxacin, macrolides change levels)

Inhaled Corticosteroids (ICS)

DrugLow DoseMedium DoseHigh Dose
Fluticasone propionate (Flovent)88–264 mcg/day264–440 mcg/day>440 mcg/day
Budesonide (Pulmicort)180–540 mcg/day540–1080 mcg/day>1080 mcg/day
Beclomethasone (Qvar)80–240 mcg/day240–480 mcg/day>480 mcg/day
🏥 ICS Prescribing PearlsMechanism: reduce airway inflammation (IL-4, IL-5, IL-13 signaling), reduce eosinophils, reduce mucus hypersecretion. Side effects: oral candidiasis (instruct patient to rinse mouth with water after each use), dysphonia (hoarseness), potential HPA axis suppression with high doses. Systemic absorption minimal at low-medium doses. ICS are cornerstone of asthma control (Step 2 and above). In COPD: ICS-containing regimens for patients with high eosinophils (>300 cells/mcL) or frequent exacerbations.

Combination Inhaler Regimens

CombinationExamplesUse
ICS + LABAFluticasone/salmeterol (Advair), budesonide/formoterol (Symbicort), fluticasone/vilanterol (Breo Ellipta), mometasone/formoterol (Dulera)Asthma Step 3–4 (preferred controller); COPD with high eosinophils/exacerbations
LAMA + LABAUmeclidinium/vilanterol (Anoro Ellipta), tiotropium/olodaterol (Stiolto), glycopyrrolate/formoterol (Bevespi)COPD maintenance (preferred dual bronchodilator therapy for moderate-severe COPD)
ICS + LABA + LAMA (Triple therapy)Fluticasone/vilanterol/umeclidinium (Trelegy Ellipta), budesonide/formoterol/glycopyrrolate (Breztri)COPD with high exacerbation risk, or uncontrolled on dual therapy
🎯 Boards Pearl — SMART RegimenSMART (Single Maintenance And Reliever Therapy): budesonide/formoterol (Symbicort) used as BOTH daily controller AND rescue inhaler (replacing SABA). Formoterol has fast enough onset for rescue use. GINA guidelines support SMART for mild-moderate asthma — reduces severe exacerbations. Reduces overuse of SABA (high SABA use = marker of poor control).

Biologics for Severe Asthma

Drug (Brand)TargetIndicationNotes
Omalizumab (Xolair)Anti-IgEModerate-severe allergic asthma; elevated IgE; sensitized to year-round allergenSQ q2–4 weeks; reduces exacerbations 25–50%; monitor for anaphylaxis post-injection (30 min); also approved for CIU (chronic idiopathic urticaria)
Mepolizumab (Nucala)Anti-IL-5Severe eosinophilic asthma (eosinophils ≥150 cells/mcL)SQ monthly; reduces exacerbations ~53%; also approved for EGPA, COPD with eosinophilia
Benralizumab (Fasenra)Anti-IL-5RαSevere eosinophilic asthmaSQ q4 weeks × 3 doses then q8 weeks; directly depletes eosinophils; rapid eosinophil reduction
Dupilumab (Dupixent)Anti-IL-4Rα (blocks IL-4 + IL-13)Moderate-severe asthma with eosinophilic phenotype OR oral corticosteroid-dependent; also atopic dermatitis, CRSwNP, EoE, COPDSQ q2 weeks; improves lung function, reduces exacerbations; injection site reactions; conjunctivitis; no anaphylaxis risk like omalizumab
Tezepelumab (Tezspire)Anti-TSLP (thymic stromal lymphopoietin)Severe uncontrolled asthma regardless of eosinophil count — broadest indicationSQ monthly; reduces exacerbations across all asthma phenotypes (eosinophilic AND non-eosinophilic)

Systemic Corticosteroids

IndicationDrug / DoseNotes
Asthma exacerbationPrednisone 40–60mg PO × 5–7 days (no taper for short courses); methylprednisolone IV for severeReduces need for hospitalization, speeds recovery; no added benefit of longer courses in most cases
COPD exacerbationPrednisone 40mg PO × 5 days (REDUCE trial: equivalent to 14 days)Reduces treatment failure and hospital LOS; no survival benefit; 5-day course standard of care
Croup (laryngotracheobronchitis)Dexamethasone 0.15–0.6mg/kg PO/IM × 1 dose; nebulized epinephrine for severeSingle dose dexamethasone = standard of care; reduces return visits and hospitalization

Pulmonary Antibiotics

IndicationFirst-Line TreatmentAlternativeDuration
CAP (outpatient, no comorbidities)Amoxicillin 1g TID or doxycycline 100mg BIDAzithromycin (avoid in high macrolide resistance areas)5 days
CAP (outpatient, with comorbidities or recent antibiotic use)Amoxicillin-clavulanate + macrolide OR respiratory fluoroquinolone (levofloxacin 750mg daily or moxifloxacin 400mg daily)Respiratory FQ monotherapy5–7 days
CAP (inpatient, non-ICU)Beta-lactam (ceftriaxone, ampicillin-sulbactam) + macrolide (azithromycin)Respiratory fluoroquinolone monotherapy5–7 days
CAP (ICU)Beta-lactam + azithromycin OR beta-lactam + respiratory FQ; add MRSA coverage (vancomycin/linezolid) if risk factorsPenicillin allergy: aztreonam + respiratory FQ7–14 days (based on clinical response)
COPD exacerbation with purulent sputumAzithromycin, doxycycline, or amoxicillin-clavulanate (based on local resistance patterns and prior exacerbation history)Respiratory FQ if gram-negative risk (frequent exacerbations, prior FQ use)5–7 days
PCP pneumonia (HIV/immunocompromised)TMP-SMX (Bactrim) DS BID × 21 days; add prednisone if PaO2 <70 or A-a gradient >35Atovaquone, clindamycin + primaquine, or pentamidine21 days
🎯 Boards PearlRespiratory fluoroquinolones (levofloxacin, moxifloxacin): excellent S. pneumoniae + atypical organism coverage. AVOID as first-line to preserve for resistant cases. Azithromycin: prolongs QT — check for drug interactions (other QT-prolonging drugs). Atypical pneumonia ("walking pneumonia"): Mycoplasma, Chlamydophila → treat with macrolide or doxycycline (NOT beta-lactams — no cell wall). Legionella: respiratory FQ or macrolide; NOT beta-lactams.

VTE / PE Pharmacotherapy

ScenarioDrug of ChoiceNotes
Acute PE, hemodynamically stableRivaroxaban (15mg BID × 21d → 20mg daily) or apixaban (10mg BID × 7d → 5mg BID) — DOACs preferredDOACs non-inferior to warfarin with less bleeding; no bridging needed; faster onset
Acute PE, massive (hemodynamically unstable)Systemic thrombolytics: tPA (alteplase 100mg IV over 2 hrs); followed by anticoagulationAbsolute contraindications: active intracranial process, recent stroke within 3 months, major surgery within 10 days, recent serious bleed
PE in pregnancyLMWH (enoxaparin) throughout pregnancy and 6 weeks postpartum (DOACs and warfarin contraindicated in pregnancy)No anti-Xa monitoring needed unless extremes of weight or renal impairment
VTE secondary prophylaxis (provoked)3 months of anticoagulation; then stop and reassessProvoked (surgery, immobility, hospitalization): 3 months then discontinue. Unprovoked: extended therapy indefinitely if low bleed risk